SUBSTITUTED ARYL ETHER COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Abstract

The present invention relates to a compound having the following formula, or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, preparation method thereof, pharmaceutical composition comprising the same and use of the compound in the manufacture of a medicament for preventing or treating tumor, wherein the substituents are as defined in the specification.

##STR00001##

Claims

1. A substituted aryl ether compound having the following formula, or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof: ##STR00491## wherein: R.sup.1 is selected from: 1) hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, hydroxy, halogen, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from: halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; 2) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl; or 2-N,N-dimethylaminoethylamino, 2-hydroxyethylamino, 2-morpholinoethylamino, 2-thiomorpholinylethylamino, 2-(4-N-methylpiperazinyl)ethylamino, 3-N,N-dimethylaminopropylamino, 3-N,N-diethylaminopropylamino, 3-N,N-diisopropylaminopropylamino, 3-hydroxypropylamino, 3-morpholinopropylamino, 3-thiomorpholinylpropylamino, 3-(4-N-methylpiperazinyl)propylamino, N-methylpiperidyl-4-amino, N-ethylpiperidyl-4-amino, N-isopropylpiperidyl-4-amino, N-acetylpiperidyl-4-amino; 3) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C3 fluorine-containing alkyl, C3-C6 cycloalkyl, halogen, nitro, cyano, hydroxy, optionally substituted heterocyclyl, C1-C6 alkoxycarbonyl, C1-C6 acyl; 4) a five- or six-membered heterocyclic ring comprising one or more heteroatoms selected from N, O and S, said five- or six-membered heterocyclic ring being optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, hydroxy, amino, C1-C6 alkoxycarbonyl, C1-C6 acyl, cyano, optionally substituted heterocyclyl, including but not limited to: morpholino, 3,5-dimethylmorpholino, thiomorpholinyl, tetrahydropyrrolyl, 3-N,N-dimethyltetrahydropyrrolyl, 3-N,N-diethyltetrahydropyrrolyl; piperidinyl, 4-N,N-dimethylaminopiperidinyl, 4-N,N-diethylaminopiperidinyl, 4-N,N-diisopropylaminopiperidinyl, 4-hydroxypiperidinyl, 4-(N-methylpiperazinyl)piperidinyl, 4-(N-ethylpiperazinyl)piperidinyl, 4-(N-isopropylpiperazinyl)piperidinyl, 4-(N-acetylpiperazinyl)piperidinyl, 4-(N-t-butoxyformylpiperazinyl)piperidinyl, 4-(N-methanesulfonylpiperazinyl)piperidinyl, 4-(N-(2-hydroxyethyl)piperazinyl)piperidinyl, 4-(N-(2-cyanoethyl)piperazinyl)piperidinyl, 4-(N-(3-hydroxypropyl)piperazinyl)piperidinyl, 4-(N-(2-N,N-dimethylethyl)piperazinyl)piperidinyl, 4-(N-(2-N,N-diethylethyl)piperazinyl)piperidinyl, 4-(N-(3-N,N-dimethylpropyl)piperazinyl)piperidinyl, 4-(N-(3-N,N-diethylpropyl)piperazinyl)piperidinyl, 4-(tetrahydropyrrolyl)piperidinyl, 4-(3-N,N-dimethyltetrahydropyrrolyl)piperidinyl; N-methylpiperazinyl, N-ethylpiperazinyl, N-isopropylpiperazinyl, N-acetylpiperazinyl, N-t-butoxyformylpiperazinyl, N-methanesulfonylpiperazinyl, N-(2-hydroxyethyl)piperazinyl, N-(2-cyanoethyl)piperazinyl, N-(3-hydroxypropyl)piperazinyl, N-(2-N,N-dimethylethyl)piperazinyl, N-(2-N,N-diethylethyl)piperazinyl, N-(3-N,N-dimethylpropyl)piperazinyl, N-(3-N,N-diethylpropyl)piperazinyl, 2-oxo-piperazin-4-yl, N(N-methyl-4-piperidinyl)piperazinyl, N(N-ethyl-4-piperidinyl)piperazinyl, N(N-acetyl-4-piperidinyl)piperazinyl; preferably, R.sup.1 is selected from: 1) hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy, halogen, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from: halogen atom, amino, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; 2) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, C3-C7 cycloalkyl; 3) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C1-C3 fluorine-containing alkyl, C3-C6 cycloalkyl, halogen, amino, hydroxy, optionally substituted heterocyclyl; R.sup.2 is selected from: hydrogen, halogen atom, C1-C6 alkylamino, di(C1-C6 alkyl) amino, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, amino, hydroxy, optionally substituted C6-C10 aryl or optionally substituted heteroaryl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; preferably, R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, C1-C6 fluorine-containing alkyl, optionally substituted C6-C10 aryl or optionally substituted heteroaryl; R.sup.3 is selected from optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from optionally substituted C6-C10 aryl or optionally substituted heteroaryl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, optionally substituted heterocyclyl, the substituent thereof being selected from: optionally substituted heterocyclyl, hydroxy, C1-C6 fluorine-containing alkyl, optionally substituted C6-C10 aryl, optionally substituted heteroaryl; A is selected from NR.sub.4CHN, NR.sub.5NCH, CHCHNR.sub.6, NNR.sub.7CH, NR.sub.8CHCH, CHCHS, SCHCH, the dotted line denotes that when A is: NR.sub.4CHN, NR.sub.5NCH, CHCHNR.sub.6, NR.sub.8CHCH, CHCHS, SCHCH, there is a double bond at this site; X is N or CH; preferably N; L is selected from: NHCO, CONH, CO, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; preferably NHCO, CONH, CO; the pharmaceutically acceptable salt is an inorganic acid salt or an organic acid salt, wherein the inorganic acid salt is selected from hydrochloride, hydrobromide, nitrate, sulfate or phosphate; the organic acid salt is selected from formate, acetate, propionate, benzoate, maleate, fumarate, succinate, tartrate, citrate, alkyl sulfonate or aryl sulfonate; preferably, said alkyl sulfonate is methyl sulfonate or ethyl sulfonate; said aryl sulfonate is benzenesulfonate or p-toluenesulfonate.

2. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00492## wherein, R.sup.1 is selected from: hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from: halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; preferably, R.sup.1 is selected from: hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from: halogen atom, amino, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; more preferably, R.sup.1 is selected from: hydrogen, C1-C6 alkoxy, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from: fluoro, chloro, bromo, amino, hydroxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl; most preferably, R.sup.1 is selected from: ##STR00493## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom; preferably, R.sup.2 is selected from: hydrogen, halogen atom, C1-C6 alkyl, C1-C6 fluorine-containing alkyl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl; most preferably, R.sup.2 is selected from: H, 4-Cl, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from: halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from: mono- or di-substituted or unsubstituted C6-C10 aryl or heteroaryl, the substituent thereof being: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocyclyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl, heterocyclyl substituted by C1-C6 alkyl; more preferably, R.sup.3 is ##STR00494## wherein one of Z.sub.1-Z.sub.5 is CF.sub.3, the rest being H; or any two of Z.sub.2, Z.sub.3, Z.sub.4 each are independently selected from CF.sub.3, ##STR00495## the rest one and Z.sub.1, Z.sub.5 being H; most preferably, R.sup.3 is ##STR00496## wherein Z.sub.4 is CF.sub.3, the rest being H; or Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is ##STR00497## the rest one and Z.sub.1, Z.sub.5 being H; R.sub.4 is selected from: hydrogen, C1-C6 alkyl, C1-C6 fluorine-containing alkyl, tri(C1-C6 alkyl) silyl C1-C6 alkoxy C1-C6 alkyl; preferably, R.sub.4 is selected from: hydrogen, methyl, ethyl, propyl, isopropyl, trifluoromethyl, tri(C1-C6 alkyl) silyl C1-C6 alkoxy C1-C6 alkyl; R.sub.4, most preferably, is selected from hydrogen, methyl, isopropyl, trimethylsilylethoxymethyl (-SEM); L is selected from: NHCO, CONH, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH.

3. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00498## wherein, R.sup.1 is selected from: 1) hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, hydroxy; 2) optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; 3) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl; 4) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C3 fluorine-containing alkyl, C3-C6 cycloalkyl, halogen, nitro, cyano, hydroxy, optionally substituted heterocyclyl, C1-C6 alkoxycarbonyl, C1-C6 acyl; preferably, R.sup.1 is selected from: 1) hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy; 2) optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, amino, hydroxy; 3) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, C3-C7 cycloalkyl; 4) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C1-C3 fluorine-containing alkyl, C3-C6 cycloalkyl, halogen, amino, hydroxy, optionally substituted heterocyclyl; more preferably, R.sup.1 is selected from: 1) hydrogen, hydroxy; 2) optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl, amino, hydroxy; 3) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl; 4) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethylcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, fluoro, chloro, bromo, hydroxy, optionally substituted heterocyclyl; most preferably, R.sup.1 is selected from: ##STR00499## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom; preferably, R.sup.2 is selected from: hydrogen, halogen atom, C1-6 alkyl, C1-C6 fluorine-containing alkyl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl; most preferably, R.sup.2 is selected from: H, 4-Cl, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from optionally substituted C6-C10 aryl or optionally substituted heteroaryl, optionally substituted C1-C6 alkyl, the substituent thereof being selected from: optionally substituted C1-C6 alkyl, optionally substituted heterocyclyl, hydroxy, C1-C6 fluorine-containing alkyl, optionally substituted C6-C10 aryl, optionally substituted heteroaryl; more preferably, R.sup.3 is selected from: optionally substituted or unsubstituted C1-C6 alkyl, the substituent thereof being selected from: optionally substituted heterocyclyl, hydroxy; mono- or di-substituted or unsubstituted C6-C10 aryl, the substituent thereof being selected from: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocyclyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl, heterocyclyl substituted by one of C1-C6 amido, C1-C6 amido C1-C6 alkyl or C1-C6 alkyl, heteroaryl substituted by C1-C6 alkyl; most preferably, R.sup.3 is selected from: 1) ##STR00500## 2) ##STR00501## wherein Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, Z.sub.5 are all H; or Z.sub.4 is CF.sub.3, the rest being H; or Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is selected from CF.sub.3, ##STR00502## the rest one and Z.sub.1, Z.sub.5 being H; or, when L is CO, R.sup.3 is ##STR00503## R.sub.5 is selected from: hydrogen, C1-C6 alkyl, C1-C6 fluorine-containing alkyl; preferably, R.sub.5 is selected from: hydrogen, methyl, ethyl, propyl, isopropyl, trifluoromethyl; most preferably, R.sub.5 is hydrogen, methyl, ethyl, or isopropyl; L is selected from: NHCO, CONH, CO, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH, CO.

4. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00504## wherein, R.sup.1 is selected from: 1) hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, hydroxy; 2) optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; 3) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl; 4) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C3 fluorine-containing alkyl, C3-C6 cycloalkyl, halogen, nitro, cyano, hydroxy, optionally substituted heterocyclyl, C1-C6 alkoxycarbonyl, C1-C6 acyl; preferably, R.sup.1 is selected from: 1) hydrogen, hydroxy, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl; 2) optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, amino, hydroxy; 3) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, C3-C7 cycloalkyl; 4) arylamino or heteroarylamino, wherein the aryl or heteroaryl is optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, C1-C3 fluorine-containing alkyl, C3-C6 cycloalkyl, halogen, hydroxy, optionally substituted heterocyclyl; more preferably, R.sup.1 is selected from: 1) hydrogen, hydroxy; 2) optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl, amino, hydroxy; 3) amino or amino bearing one or two substituent(s) on the nitrogen, the substituent thereof being selected from methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl; most preferably, R.sup.1 is selected from: H, OH, ##STR00505## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, optionally substituted C6-C10 aryl or optionally substituted heteroaryl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; preferably, R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, C1-C6 fluorine-containing alkyl, optionally substituted C6-C10 aryl or optionally substituted heteroaryl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl, pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, imidazolyl, thiazolyl, isothiazolyl, thioxazolyl, pyrrolyl, furyl, oxazolyl, isoxazolyl, pyrazolyl, thienyl, indazolyl, quinolyl, isoquinolyl; most preferably, R.sup.2 is selected from: H, ##STR00506## at 4-position, 4-Cl, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from mono- or di-substituted or unsubstituted C6-C10 aryl or heteroaryl, the substituent thereof being: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocyclyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl, heterocyclyl substituted by one of C1-C6 amido, C1-C6 amido C1-C6 alkyl or C1-C6 alkyl, heteroaryl substituted by C1-C6 alkyl; more preferably, R.sup.3 is ##STR00507## wherein one of Z.sub.1-Z.sub.5 is CF.sub.3, the rest being H; or any two of Z.sub.2, Z.sub.3, Z.sub.4 each are independently selected from CF.sub.3, ##STR00508## the rest one and Z.sub.1, Z.sub.5 being H; most preferably, R.sup.3 is ##STR00509## wherein Z.sub.4 is CF.sub.3, the rest being H; or Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is ##STR00510## the rest one and Z.sub.1, Z.sub.5 being H; R.sub.6 is selected from: hydrogen, C.sub.1-6 alkyl, C1-C6 fluorine-containing alkyl; preferably, R.sub.6 is selected from: hydrogen, methyl, ethyl, propyl, isopropyl, trifluoromethyl; R.sub.6, most preferably, is hydrogen, methyl; L is selected from: NHCO, CONH, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH.

5. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00511## wherein, R.sup.1 is selected from: hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; preferably, R.sup.1 is selected from: hydrogen, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, amino, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; more preferably, R.sup.1 is selected from: hydrogen, C1-C6 alkoxy, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, amino, hydroxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl; most preferably, R.sup.1 is selected from: H, ##STR00512## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom; preferably, R.sup.2 is selected from: hydrogen, halogen atom, C.sub.1-6 alkyl, C1-C6 fluorine-containing alkyl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl; R.sup.2, most preferably, is selected from: H, 4-Cl, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from: optionally substituted C1-C6 alkyl, the substituent thereof being halogen atom, optionally substituted heterocyclyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from mono- or di-substituted or unsubstituted C6-C10 aryl or heteroaryl, the substituent thereof being: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocyclyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, heterocyclyl substituted by C1-C6 alkyl, heteroaryl substituted by C1-C6 alkyl; more preferably, R.sup.3 is ##STR00513## wherein one of Z.sub.1-Z.sub.5 is CF.sub.3 or CF.sub.3O, the rest being H: or any two of Z.sub.2, Z.sub.3, Z.sub.4 each are independently selected from CF.sub.3, ##STR00514## the rest one and Z.sub.1, Z.sub.5 being H; R.sup.3, most preferably, is ##STR00515## wherein Z.sub.4 is CF.sub.3 or CF.sub.3O, the rest being H; or Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is ##STR00516## the rest one and Z.sub.1, Z.sub.5 being H; R.sub.7 is selected from: C.sub.1-6 alkyl, C1-C6 fluorine-containing alkyl; preferably, R.sub.7 is selected from: methyl, ethyl, propyl, isopropyl, trifluoromethyl; most preferably, R.sub.7 is selected from methyl; L is selected from: NHCO, CONH, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH.

6. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00517## wherein, R.sup.1 is selected from: hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; preferably, R.sup.1 is selected from: hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, amino, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; more preferably, R.sup.1 is selected from: hydrogen, C1-C6 amido, C1-C6 alkoxy, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, amino, hydroxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl; most preferably, R.sup.1 is selected from: ##STR00518## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom; preferably, R.sup.2 is selected from: hydrogen, halogen atom, C.sub.1-6 alkyl, C1-C6 fluorine-containing alkyl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl; R.sup.2, most preferably, is selected from: H, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from: optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from: halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from: mono- or di-substituted or unsubstituted C6-C10 aryl or heteroaryl, the substituent thereof being: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocycyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl, heterocyclyl substituted by C1-C6 alkyl; more preferably, R.sup.3 is ##STR00519## wherein one of Z.sub.1-Z.sub.5 is CF.sub.3, the rest being H; or any two of Z.sub.2, Z.sub.3, Z.sub.4 each are independently selected from CF.sub.3, ##STR00520## the rest one and Z.sub.1, Z.sub.5 being H; R.sup.3, most preferably, is ##STR00521## wherein Z.sub.4 is CF.sub.3, the rest being H; or Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is ##STR00522## the rest one and Z.sub.1, Z.sub.5 being H; R.sub.8 is selected from: hydrogen, C1-C6 alkyl, C1-C6 fluorine-containing alkyl; preferably, R.sub.8 is selected from: hydrogen, methyl, ethyl, propyl, isopropyl, trifluoromethyl; most preferably, R.sub.8 is selected from hydrogen, methyl; L is selected from: NHCO, CONH, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH.

7. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00523## wherein, R.sup.1 is selected from: hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; preferably, R.sup.1 is selected from: hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, amino, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; more preferably, R.sup.1 is selected from: hydrogen, C1-C6 alkoxy, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, amino, hydroxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl; most preferably, R.sup.1 is selected from: ##STR00524## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom; preferably, R.sup.2 is selected from: hydrogen, halogen atom, C.sub.1-6 alkyl, C1-C6 fluorine-containing alkyl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl; R.sup.2, most preferably, is selected from: H, 4-Cl, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from: optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from: mono- or di-substituted or unsubstituted C6-C10 aryl or heteroaryl, the substituent thereof being: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocycyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl, heterocyclyl substituted by C1-C6 alkyl; more preferably, R.sup.3 is ##STR00525## wherein any two of Z.sub.2, Z.sub.3, Z.sub.4 each are independently selected from CF.sub.3, ##STR00526## the rest one and Z.sub.1, Z.sub.5 being H; R.sup.3, most preferably, is ##STR00527## wherein Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is ##STR00528## the rest one and Z.sub.1, Z.sub.5 being H; L is selected from: NHCO, CONH, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH.

8. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound has the following structure: ##STR00529## wherein, R.sup.1 is selected from: hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, optionally substituted C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from halogen atom, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, nitro, cyano, amino, hydroxy; preferably, R.sup.1 is selected from: hydrogen, C1-C6 amido, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, amino, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 fluorine-containing alkyl; more preferably, R.sup.1 is selected from: hydrogen, C1-C6 alkoxy, optionally substituted C3-C7 cycloalkyl, hydroxy, amino, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, the substituent thereof being selected from fluoro, chloro, bromo, amino, hydroxy, methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, fluoromethyl, difluoromethyl, trifluoromethyl, trifluoroethyl; most preferably, R.sup.1 is selected from: ##STR00530## R.sup.2 is selected from: hydrogen, halogen atom, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom; preferably, R.sup.2 is selected from: hydrogen, halogen atom, C.sub.1-6 alkyl, C1-C6 fluorine-containing alkyl; more preferably, R.sup.2 is selected from: hydrogen, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, trifluoromethyl; most preferably, R.sup.2 is selected from: H, 4-Cl, 4-CH.sub.3, 6-CH.sub.3; R.sup.3 is selected from: optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, optionally substituted C3-C7 cycloalkyl, the substituent thereof being selected from halogen atom, optionally substituted C6-C10 aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 oxygen-containing alkyl, C1-C6 fluorine-containing alkyl, C1-C6 fluorine-containing alkoxy, nitro, cyano, amino, hydroxy; preferably, R.sup.3 is selected from: mono- or di-substituted or unsubstituted C6-C10 aryl or heteroaryl, the substituent thereof being: optionally substituted C1-C6 alkyl, the substituent on the C1-C6 alkyl being heterocyclyl substituted by C1-C6 alkyl; C1-C6 fluorine-containing alkyl; heterocycyl substituted by C1-C6 alkyl; heteroaryl substituted by C1-C6 alkyl; more preferably, R.sup.3 is ##STR00531## wherein any two of Z.sub.2, Z.sub.3, Z.sub.4 each are independently selected from CF.sub.3, ##STR00532## the rest one and Z.sub.1, Z.sub.5 being H; R.sup.3, most preferably, is ##STR00533## wherein Z.sub.4 is CF.sub.3, one of Z.sub.2, Z.sub.3 is ##STR00534## the rest one and Z.sub.1, Z.sub.5 being H; L is selected from: NHCO, CONH, NHSO.sub.2, SO.sub.2NH, NHCONH, NHCSNH, COO, OCO; L, preferably, is selected from: NHCO, CONH.

9. A compound according to claim 1 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, characterized in that the compound is selected from: ##STR00535## ##STR00536## ##STR00537## ##STR00538## ##STR00539## ##STR00540## ##STR00541## ##STR00542## ##STR00543## ##STR00544## ##STR00545## ##STR00546## ##STR00547## ##STR00548## ##STR00549## ##STR00550## ##STR00551## ##STR00552## ##STR00553## ##STR00554## ##STR00555## ##STR00556## ##STR00557## ##STR00558## ##STR00559## ##STR00560## ##STR00561## ##STR00562## ##STR00563## ##STR00564## ##STR00565## ##STR00566## ##STR00567## ##STR00568## ##STR00569## ##STR00570## ##STR00571## ##STR00572## ##STR00573## ##STR00574## ##STR00575## ##STR00576## ##STR00577## ##STR00578## ##STR00579## ##STR00580## ##STR00581## ##STR00582## ##STR00583## ##STR00584## ##STR00585## ##STR00586## ##STR00587## ##STR00588## ##STR00589## ##STR00590## ##STR00591## ##STR00592## ##STR00593## ##STR00594## ##STR00595## ##STR00596## ##STR00597## ##STR00598## ##STR00599## ##STR00600## ##STR00601## ##STR00602## ##STR00603## ##STR00604## ##STR00605## ##STR00606## ##STR00607## ##STR00608## ##STR00609## ##STR00610## ##STR00611## ##STR00612## ##STR00613## ##STR00614## ##STR00615## ##STR00616## ##STR00617## ##STR00618## ##STR00619## ##STR00620## ##STR00621## ##STR00622## ##STR00623## ##STR00624## ##STR00625## ##STR00626## ##STR00627## ##STR00628##

10. A pharmaceutical composition, comprising a compound and a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof according to any one of claims 1-9 and a pharmaceutically acceptable carrier, diluent or excipient.

11. A preparation method of a compound according to any one of claims 1-9, comprising the following steps: a) reacting a compound of formula 1 with a compound of formula 2 under alkaline conditions to obtain a compound of formula 3 ##STR00629## b) reacting the compound of formula 3 under Suzuki coupling reaction or Buchwald coupling reaction or basic conditions to obtain a compound of formulas I-VII ##STR00630## wherein R.sub.1, R.sub.2, R.sub.3, A, X, L are as defined above; R refers to a reactive group, selected from hydrogen, boric acid group or borate ester group and the like.

12. A preparation method according to claim 11, characterized in that: a) in the step of preparing the compound of formula 3, the base used is selected from an organic base (such as n-butyl lithium, sodium methoxide, sodium ethoxide, potassium t-butoxide and the like) or an inorganic base (such as sodium carbonate, potassium carbonate, cesium carbonate and the like), preferably sodium carbonate or potassium carbonate; b) in the step of preparing the compounds of formulas I-VII, when the reaction is Suzuki coupling reaction, the metal catalyst used is a transition metal catalyst (such as Pd(dppf)Cl.sub.2.CH.sub.2Cl.sub.2, Pd(OAc).sub.2, Pd(PPh.sub.3).sub.4, Ni(cod.sub.2), Ni(dppf)Cl.sub.2 and the like), preferably Pd(dppf)Cl.sub.2.CH.sub.2Cl.sub.2; the solvent used is, but not limited to, toluene, tetrahydrofuran, N,N-dimethylformamide, water or a mixed solvent, preferably tetrahydrofuran/water mixed solvent; the base used is, but not limited to, sodium carbonate, potassium carbonate, cesium carbonate, potassium carbonate, sodium hydroxide, barium hydroxide, potassium fluoride, cesium fluoride, sodium tert-butoxide, preferably sodium carbonate or potassium carbonate; c) in the step of preparing the compounds of formulas I-VII, when the reaction is Buchwald coupling reaction, the metal catalyst used is a transition metal catalyst (such as Pd.sub.2(dba).sub.3, Pd(OAc).sub.2, Pd(dppf)Cl.sub.2.CH.sub.2CH.sub.2 and the like), preferably Pd.sub.2(dba).sub.3; the solvent used is, but not limited to, toluene, tetrahydrofuran, N,N-dimethylformamide, tert-butanol, preferably tert-butanol; the base used is, but not limited to, potassium carbonate, cesium carbonate, sodium tert-butoxide, lithium hexamethyldisilazide (LHMDS), preferably potassium carbonate or cesium carbonate; d) in the step of preparing the compounds of formulas I-VII, when the reaction is under alkaline conditions, the base used is selected from an organic base (such as triethylamine, pyridine, 4-dimethylaminopyridine, diisopropylethylamine and the like) or an inorganic base (such as sodium carbonate, potassium carbonate, cesium carbonate and the like), preferably triethylamine or diisopropylethylamine; the solvent used is, but not limited to, toluene, tetrahydrofuran, N,N-dimethylformamide, tert-butanol, preferably tetrahydrofuran.

13. Use of a compound according to any one of claims 1-9 or a stereoisomer thereof, a prodrug thereof, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof or a pharmaceutical composition according to claim 10 in the manufacture of a medicament for preventing or treating a disease associated with RET kinase accompanied by abnormal cell proliferation, morphological changes, hyperkinesia and the like in vivo, and in the manufacture of a medicament for preventing or treating a disease associated with angiogenesis or cancer metastasis, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

14. Use according to claim 13, wherein the tumor is any one selected from lung adenocarcinoma, colon cancer, multiple endocrinoma type 2, medullary thyroid cancer, papillary thyroid carcinoma, bladder pheochromocytoma, paraganglioma, preferably lung adenocarcinoma.

Description

MODE OF CARRYING OUT THE INVENTION

[0227] The embodiments of the present invention are described in detail below by way of specific examples, but in any case they cannot be construed as limiting the present invention.

##STR00052##

[0228] The above compound of formula was divided into several types for preparation.

##STR00053## ##STR00054##

[0229] The compounds of formula I:

##STR00055## ##STR00056## ##STR00057##

wherein,
Synthetic scheme of compound I-a:

##STR00058##

Preparation of Compound 3a

[0230] Compound 2 (281.2 mg, 1 mmol) was dissolved in dimethyl sulfoxide, to which was added K.sub.2CO.sub.3 at room temperature, followed by stirring for half an hour. Then, compound Ia (223.3 mg, 1.1 mmol) was added, and reaction was carried out at room temperature overnight. The reaction system was extracted with water/ethyl acetate (315 mL), then the organic phase was washed with saturated sodium chloride solution, dried with anhydrous sodium sulfate, concentrated, and separated by silica gel column chromatography (dichloromethane/methanol) to obtain compound 3a (white solid, 441.5 mg, 93.3%). MS (ESI) m/z 448 [M+H].sup.+.

Preparation of compound I-a

Method A:

[0231] Compound 3 (0.1 mmol), aryl boric acid (0.15 mmol), PdCl.sub.2(dppf)-CH.sub.2Cl.sub.2 (20% m %), Na.sub.2CO.sub.3 (0.4 mmol) were added to 1 mL of 1,4-dioxane and 0.33 mL of H.sub.2O, the system was purged with nitrogen, and placed in an oil bath preheated to 100 C. and stirred with heating overnight. The reaction system was filtered to remove solids and concentrated, followed by separation with silica gel column chromatography to obtain compound I-a.

Method B:

[0232] Compound 3 (0.1 mmol), aryl boric acid (0.15 mmol), PdCl.sub.2(dppf)-CH.sub.2Cl.sub.2 (20% m %), Na.sub.2CO.sub.3 (0.4 mmol) were added to 1 mL of 1,4-dioxane and 0.33 mL of H.sub.2O, the system was purged with nitrogen, and placed in an oil bath preheated to 100 C. and stirred with heating overnight. The reaction system was filtered and concentrated, followed by separation with preparative thin layer chromatography to obtain compound I-a.

Method C:

[0233] Compound 3 (0.1 mmol), aryl boric acid (0.15 mmol), PdCl.sub.2(dppf)-CH.sub.2Cl.sub.2 (20% m %), Na.sub.2CO.sub.3 (0.4 mmol) were added to 1 mL of 1,4-dioxane and 0.33 mL of H.sub.2O, the system was purged with nitrogen, and placed in an oil bath preheated to 100 C. and stirred with heating overnight. The reaction system was filtered and concentrated, followed by purification with reverse phase preparative HPLC (using 0.35% trifluoroacetic acid-containing aqueous solution and methanol as mobile phase), and vacuum concentration to obtain compound I-a.

Method D:

[0234] Compound 3 (0.1 mmol) was dissolved in 1 mL of t-BuOH, to which was added compounds 5a-5c (0.2 mmol). The reaction was carried out at room temperature, until complete reaction of compound 3 (TLC tracking). The reaction system was concentrated, followed by separation with silica gel column chromatography (dichloromethane/ammonia in methanol) to obtain compound I-a.

Method E:

[0235] Compound 3 (0.1 mmol), aryl boric acid (0.15 mmol), PdCl.sub.2(dppf).CH.sub.2Cl.sub.2 (20% m %), Na.sub.2CO.sub.3 (0.4 mmol) were added to 1 mL of 1,4-dioxane and 0.33 mL of H.sub.2O, the system was purged with nitrogen, and placed in an oil bath preheated to 100 C. and stirred with heating overnight. The reaction system was filtered to remove solids and concentrated, followed by separation with silica gel column chromatography to obtain a compound. The obtained compound was dissolved in 1 mL of dichloromethane, to which was added trifluoroacetic acid (10 eq). The reaction was carried out at room temperature overnight. The reaction system was concentrated and dried, to which was then added 1 mL of methanol, 0.5 mL of 7.0 N NH.sub.3 solution in methanol, followed by reacting overnight. The resulting product was concentrated, and separated with silica gel column chromatography (dichloromethane/ammonia in methanol to obtain compound I-a.

[0236] Compounds II, III, IV, V, VI, VII all could be synthesized by a similar method.

[0237] Some raw materials and intermediates involved in the specific synthetic processes are given as follows:

1.

##STR00059##

CAS:5451-40-1, Bide, Shanghai;

[0238] 2.

##STR00060##

obtained from the reaction of 1 and methyl iodide (CAS:74-88-4, Xiya Reagent, Shandong);
3.

##STR00061##

obtained from the reaction of 2,4,6-trichloro-5-pyrimidine formaldehyde (CAS: 50270-27-4, Bide, Shanghai) and hydrazine hydrate (CAS: 7803-57-8, Energy, Shanghai);
4.

##STR00062##

obtained from the reaction of 2,4,6-trichloro-5-pyrimidine formaldehyde and methyl hydrazine (CAS:60-34-4, Xiya Reagent, Shandong);
5.

##STR00063##

CAS: 63200-54-4, PharmaBlock, Nanjing, Jiangsu;

[0239] 6.

##STR00064##

obtained from the reaction of 5 and dimethyl sulfate (CAS: 77-78-1 Xiya Reagent, Shandong);
7.

##STR00065##

CAS: 959432-77-0, Sundia, Shanghai;

[0240] 8.

##STR00066##

CAS: 5912-18-5, Efe, Shanghai;

[0241] 9.

##STR00067##

obtained from the reaction of 8 and methyl iodide (CAS: 74-88-4, Xiya Reagent, Shandong);
10.

##STR00068##

CAS: 16234-14-3, PharmaBlock, Nanjing, Jiangsu;

[0242] 11.

##STR00069##

CAS: 18740-39-1, Chemlin, Jiangsu;

[0243] 12.

##STR00070##

obtained from the condensation of 3-trifluoromethylbenzoic acid (CAS: 454-92-2, Energy, Shanghai) and 3-aminophenol (CAS: 591-27-5, Energy, Shanghai);
13

##STR00071##

obtained by the reaction including the following steps: protecting phenolic hydroxy of m-hydroxybenzoic acid (CAS: 99-06-9, Efe, Shanghai) with acetyl, then reacting the above product with thionyl chloride (CAS: 7719-09-7, Aladdin, Shanghai) to obtain

##STR00072##

and further reacting the product in the previous step with m-aminotrifluorotoluene (CAS: 98-16-8, Energy, Shanghai) while removing the acetyl;
14.

##STR00073##

obtained by the reaction including the following steps: condensing

##STR00074##

(CAS: 859213-39-1, J&K, Beijing) and

[0244] ##STR00075##

(CAS: 2835-95-2, Bide, Shanghai) to obtain

##STR00076##

and then reacting the above product with N-methylpiperazine (CAS: 109-01-3, Energy, Shanghai);
15.

##STR00077##

obtained by the reaction including the following steps: protecting phenolic hydroxy of 3-hydroxy-4-methylbenzoic acid (CAS: 586-30-1, Accela ChemBio, Shanghai) with acetyl, then reacting the above product with thionyl chloride to obtain

##STR00078##

and further reacting the product in the previous step with

##STR00079##

(CAS: 694499-26-8, Shuya, Shanghai) while removing the acetyl;
16.

##STR00080##

obtained using 2-chloro-5-hydroxybenzoic acid (CAS: 56961-30-9, Shuya, Shanghai) as starting raw material, by a method similar to that for the synthesis of 15;
17.

##STR00081##

CAS: 1692-25-7, Energy, Shanghai;

[0245] 18.

##STR00082##

CAS: 1692-15-5, Energy, Shanghai;

[0246] 19.

##STR00083##

CAS: 98-80-6, Adamas, Switzerland;

[0247] 20.

##STR00084##

CAS: 87199-18-6, Energy, Shanghai;

[0248] 21.

##STR00085##

CAS: 71597-85-8, Bide, Shanghai;

[0249] 22.

##STR00086##

CAS: 1679-18-1, Energy, Shanghai;

[0250] 23.

##STR00087##

CAS: 63503-60-6, Energy, Shanghai;

[0251] 24.

##STR00088##

CAS: 5720-05-8, Energy, Shanghai;

[0252] 25.

##STR00089##

CAS: 55552-70-0, Energy, Shanghai;

[0253] 26.

##STR00090##

CAS: 6165-69-1, Energy, Shanghai;

[0254] 27.

##STR00091##

CAS: 62-53-3, Adamas, Switzerland;

[0255] 28.

##STR00092##

CAS: 106-49-0, Adamas, Switzerland;

[0256] 29.

##STR00093##

CAS: 462-08-8, Energy, Shanghai;

[0257] 30

##STR00094##

CAS: 765-30-0, Energy, Shanghai;

[0258] 31.

##STR00095##

CAS: 141-91-3, Energy, Shanghai;

[0259] 32.

##STR00096##

CAS: 110-91-8, Aladdin, Shanghai;

[0260] 33.

##STR00097##

CAS: 124-40-3, Meryer, Shanghai.

[0261] The table below lists the specific compounds and structure identification data.

TABLE-US-00001 TABLE 1 Structure and characterization of compounds I No. Structure .sup.1H NMR and/or MS data I-a-1 [00098] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.63 (s, 1H), 9.28 (s, 1H), 8.59 (d, J = 3.8 Hz, 1H), 8.49 (s, 1H), 8.46 (d, J = 7.9 Hz, 1H), 8.27 (s, 1H), 8.24 (d, J = 7.8 Hz, 1H), 7.94 (d, J = 7.7 Hz, 1H), 7.90 (s, 1H), 7.76 (t, J = 7.8 Hz, 1H), 7.72 (d, J = 8.2 Hz, 1H), 7.51 (t, J = 8.1 Hz, 1H), 7.45 (dd, J = 7.8, 4.8 Hz, 1H), 7.17 (d, J = 7.9 Hz, 1H), 3.91 (s, 1H). MS (ESI) m/z 491 [M + H].sup.+. I-a-2 [00099] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 8.29 (s, 1H), 8.26 (d, J = 7.9 Hz, 1H), 8.05 (s, 1H), 7.98 (d, J = 7.8 Hz, 1H), 7.82 (t, J = 2.1 Hz, 1H), 7.80 (t, J = 7.8 Hz, 1H), 7.64 (ddd, J = 8.2, 1.9, 0.8 Hz, 1H), 7.45 (t, J = 8.2 Hz, 1H), 7.06 (ddd, J = 8.2, 2.3, 0.9 Hz, 1H), 3.68 (s, 3H), 3.60-3.58 (m, 4H), 3.55 (d, J = 4.9 Hz, 4H). MS (ESI) m/z 499 [M + H].sup.+. I-a-3 [00100] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.60 (s, 1H), 8.29 (s, 1H), 8.26 (d, J = 7.9 Hz, 1H), 8.04 (s, 1H), 7.98 (d, J = 7.8 Hz, 1H), 7.91 (t, J = 2.1 Hz, 1H), 7.80 (dd, J = 9.9, 5.7 Hz, 1H), 7.62 (dd, J = 8.1, 1.1 Hz, 1H), 7.45 (t, J = 8.1 Hz, 1H), 7.06 (dd, J = 8.1, 1.7 Hz, 1H), 3.68 (s, 3H), 3.53-3.46 (m, 2H), 2.44 (dd, J = 12.7, 10.9 Hz, 2H), 1.24 (d, J = 22.2 Hz, 2H), 1.05 (d, J = 5.8 Hz, 6H). MS (ESI) m/z 527 [M + H].sup.+. I-b-1 [00101] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 9.25 (dd, J = 2.2, 0.8 Hz, 1H), 8.62 (dd, J = 4.7, 1.7 Hz, 1H), 8.53 (s, 1H), 8.46-8.44 (m, 1H), 8.28 (s, 1H), 8.25 (d, J = 7.9 Hz, 1H), 7.96 (d, J = 7.8 Hz, 1H), 7.81 (d, J = 2.1 Hz, 1H), 7.78 (t, J = 7.8 Hz, 1H), 7.68 (dd, J = 8.3, 2.1 Hz, 1H), 7.49 (ddd, J = 8.0, 4.8, 0.8 Hz, 1H), 7.43 (d, J = 8.4 Hz, 1H), 5.76 (s, 1H), 3.94 (s, 3H), 2.14 (s, 3H). MS (ESI) m/z 505 [M + H].sup.+. I-b-2 [00102] MS (ESI) m/z 541 [M + H].sup.+. I-b-3 [00103] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 8.28 (s, 1H), 8.25 (d, J = 7.9 Hz, 1H), 8.03 (s, 1H), 7.96 (d, J = 7.8 Hz, 1H), 7.78 (q, J = 7.0 Hz, 2H), 7.56 (dd, J = 8.2, 2.1 Hz, 1H), 7.33 (d, J = 8.7 Hz, 1H), 3.68 (s, 3H), 3.50-3.43 (m, 2H), 2.41 (dd, J = 12.6, 11.0 Hz, 2H), 2.12 (s, 3H), 1.22 (d, J = 4.7 Hz, 2H), 1.02 (dd, J = 10.1, 5.2 Hz, 6H). MS (ESI) m/z 541 [M + H].sup.+. I-d-1 [00104] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.63 (s, 1H), 9.26 (s, 1H), 8.62 (d, J = 3.4 Hz, 1H), 8.54 (s, 1H), 8.45 (d, J = 7.7 Hz, 1H), 8.25 (s, 1H), 8.07 (d, J = 8.1 Hz, 1H), 8.03 (s, 1H), 8.00 (d, J = 7.0 Hz, 1H), 7.76-7.69 (m, 2H), 7.60 (t, J = 7.8 Hz, 1H), 7.46 (d, J = 7.2 Hz, 2H), 3.94 (s, 3H). MS (ESI) m/z 491 [M + H].sup.+. 1-d-2 [00105] .sup.1H NMR (600 MHz, DMSO-d.sub.6)) 10.63 (s, 1H), 8.66 (d, J = 5.9 Hz, 2H), 8.58 (s, 1H), 8.25 (s, 1H), 8.06 (d, J = 8.4 Hz, 1H), 8.04-7.98 (m, 4H), 7.72 (ddd, J = 11.3, 8.2, 5.1 Hz, 2H), 7.60 (t, J = 8.0 Hz, 1H), 7.46 (d, J = 7.8 Hz, 1H), 3.95 (s, 3H). MS (ESI) m/z 491 [M + H].sup.+. I-d-3 [00106] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 8.25 (s, 1H), 8.06 (d, J = 9.5 Hz, 2H), 7.93 (d, J = 1.7 Hz, 1H), 7.91 (d, J = 7.7 Hz, 1H), 7.64 (t, J = 7.9 Hz, 1H), 7.61 (t, J = 8.0 Hz, 1H), 7.57 (dd, J = 8.1, 1.3 Hz, 1H), 7.47 (d, J = 7.7 Hz, 1H), 3.69 (s, 3H), 3.59-3.56 (m, 4H), 3.52 (d, J = 3.9 Hz, 4H). MS (ESI) m/z 499 [M + H].sup.+. I-d-4 [00107] MS (ESI) m/z 527 [M + H].sup.+. I-e-1 [00108] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.51 (s, 1H), 9.18 (s, 1H), 8.59 (d, J = 3.4 Hz, 1H), 8.52 (s, 1H), 8.38 (d, J = 8.1 Hz, 1H), 8.20 (s, 1H), 8.03 (d, J = 8.5 Hz, 1H), 7.94 (m, J = 10.1 Hz, 2H), 7.61 (d, J = 7.8 Hz, 1H), 7.56 (t, J = 7.9 Hz, 1H), 7.45 (dd, J = 7.9, 4.9 Hz, 1H), 7.42 (d, J = 7.8 Hz, 1H), 3.92 (s, 3H), 2.22 (s, 3H). MS (ESI) m/z 505 [M + H].sup.+. I-e-2 [00109] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 8.65 (dd, J = 4.5, 1.6 Hz, 2H), 8.58 (s, 1H), 8.22 (s, 1H), 8.05 (d, J = 8.3 Hz, 1H), 7.99-7.95 (m, 4H), 7.63 (d, J = 7.8 Hz, 1H), 7.58 (t, J = 8.0 Hz, 1H), 7.44 (d, J = 7.7 Hz, 1H), 3.95 (s, 3H), 2.24 (s, 3H). MS (ESI) m/z 505 [M + H].sup.+. I-e-3 [00110] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.49 (s, 1H), 8.23 (s, 1H), 8.06 (s, 2H), 7.89-7.86 (m, 2H), 7.59 (t, J = 8.0 Hz, 1H), 7.53 (d, J = 7.7 Hz, 1H), 7.45 (d, J = 7.7 Hz, 1H), 3.69 (s, 3H), 3.56-3.53 (m, 4H), 3.46 (s, 4H), 2.21 (s, 3H). MS (ESI) m/z: 513 [M + H].sup.+. I-e-4 [00111] .sup.1H NMR (600 MHz, DMSO-d.sub.6)) 10.48 (s, 1H), 8.24 (s, 1H), 8.05 (d, J = 7.4 Hz, 2H), 7.97 (d, J = 1.7 Hz, 1H), 7.88 (dd, J = 7.9, 1.7 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.54 (d, J = 8.1 Hz, 1H), 7.45 (d, J = 7.8 Hz, 1H), 3.69 (s, 3H), 3.48-3.41 (m, 2H), 3.18 (d, J = 5.2 Hz, 2H), 2.44-2.37 (m, 2H), 2.24 (s, 3H), 1.04-0.99 (m, 6H), MS (ESI) m/z 541 [M + H].sup.+. I-f-1 [00112] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.73 (s, 1H), 9.31 (d, J = 2.3 Hz, 1H), 8.67-8.62 (m, 1H), 8.52 (s, 1H), 8.49 (dt, J = 8.0, 2.0 Hz, 1H), 8.24 (d, J = 2.0 Hz, 1H), 8.00-7.91 (m, 1H), 7.61-7.54 (m, 2H), 7.55-7.46 (m, 3H), 7.46-7.40 (m, 1H), 3.92 (s, 3H), 2.48 (s, 3H). MS (ESI) m/z 505 [M + H].sup.+. I-f-2 [00113] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.74 (s, 1H), 8.68 (s, 2H), 8.55 (s, 1H), 8.25 (s, 1H), 8.06 (s, 2H), 7.96 (d, J = 8.3 Hz, 1H), 7.61-7.55 (m, 2H), 7.53-7.46 (m, 2H), 7.44 (d, J = 7.7 Hz, 1H), 3.92 (s, 3H), 2.48 (s, 3H). MS (ESI) m/z 505 [M + H].sup.+. I-f-3 [00114] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.68 (s, 1H), 8.23 (s, 1H), 8.06 (s, 1H), 7.95 (d, J = 8.1 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.48 (d, J = 2.3 Hz, 1H), 7.46 (d, J = 8.0 Hz, 1H), 7.40-7.37 (m, 1H), 3.68 (s, 3H), 3.59 (s, 4H), 3.55 (s, 4H), 2.42 (s, 3H). MS (ESI) m/z 513 [M + H].sup.+. I-h-1 [00115] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.62 (s, 1H), 8.72 (s, 1H), 8.71-8.63 (m, 2H), 8.24 (s, 1H), 8.22 (dd, J = 8.2, 1.9 Hz, 1H), 8.10-8.05 (m, 2H), 7.92 (d, J = 8.0 Hz, 1H), 7.90 (t, J = 2.2 Hz, 1H), 7.72 (dd, J = 8.2, 2.0 Hz, 1H), 7.53 (t, J = 8.1 Hz, 1H), 7.18 (dd, J = 8.1, 2.5 Hz, 1H), 5.48-4.64 (m, 1H), 3.67 (s, 2H), 2.41 (s, 8H), 2.45-2.32 (m, 8H), 1.65 (d, J = 6.8 Hz, 6H). MS (ESI) m/z 631 [M + H].sup.+. I-j-1 [00116] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.49-8.44 (m, 2H), 8.31 (s, 1H), 8.25 (d, J = 1.8 Hz, 1H), 8.15 (dd, J = 8.1, 1.8 Hz, 1H), 8.13-8.09 (m, 2H), 7.92 (d, J = 8.2 Hz, 1H), 7.47 (d, J = 2.5 Hz, 1H), 7.38 (d, J = 8.3 Hz, 1H), 7.18 (dd, J = 8.3, 2.5 Hz, 1H), 3.90 (s, 3H), 3.69 (s, 2H), 2.34 (s, 3H), 2.26 (s, 3H). MS (ESI) m/z 617 [M + H].sup.+. I-j-2 [00117] TFA Salt MS (ESI) m/z 615 [M + H].sup.+. I-j-3 [00118] TFA Salt MS (ESI) m/z 650 [M + H].sup.+. I-j-4 [00119] TFA Salt MS (ESI) m/z 631 [M + H].sup.+. I-j-5 [00120] TFA salt MS (ESI) m/z 630 [M + H].sup.+. I-j-6 [00121] TFA salt MS (ESI) m/z 605 [M + H].sup.+. I-j-7 [00122] TFA Salt MS (ESI) m/z 621 [M + H].sup.+. I-l-1 [00123] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.64 (s, 1H), 8.78 (s, 2H), 8.69 (s, 1H), 8.22 (d, J = 2.1 Hz, 1H), 8.18 (d, J = 5.2 Hz, 2H), 8.12-8.08 (m, 1H), 8.04 (s, 1H), 8.02-8.00 (m, 1H), 7.75-7.73 (m, 2H), 7.71 (d, J = 8.6 Hz, 1H), 7.24-7.03 (m, 1H), 3.41 (d, J = 10.5 Hz, 2H), 3.04 (s, 2H), 2.91 (s, 2H), 2.81 (s, 3H), 2.39 (s, 2H). MS (ESI) m/z 589 [M + H].sup.+. I-l-2 [00124] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 9.27 (d, J = 1.5 Hz, 1H), 8.62 (dd, J = 4.7, 1.7 Hz, 1H), 8.54 (s, 1H), 8.47-8.44 (m, 1H), 8.20 (d, J = 2.1 Hz, 1H), 8.04 (dd, J = 8.5, 1.9 Hz, 1H), 8.02 (t, J = 1.8 Hz, 1H), 7.99 (dt, J = 7.5, 1.4 Hz, 1H), 7.73 (t, J = 7.8 Hz, 1H), 7.71-7.68 (m, 2H), 7.48 (ddd, J = 8.0, 4.8, 0.7 Hz, 1H), 3.94 (s, 3H), 3.56 (s, 2H), 2.16 (s, 3H). MS (ESI) m/z 603 [M + H].sup.+. I-l-3 [00125] TFA Salt MS (ESI) m/z 603 [M + H].sup.+. I-l-4 [00126] MS (ESI) m/z 719 [M + H].sup.+. I-m-1 [00127] .sup.1H NMR (600 MHz, DMSO) 10.49 (s, 1H), 8.64 (d, J = 5.7 Hz, 3H), 8.18 (d, J = 1.9 Hz, 1H), 8.05 (d, J = 8.6 Hz, 1H), 7.99 (s, 1H), 7.98-7.96 (m, 1H), 7.93 (dd, J = 4.6, 1.4 Hz, 2H), 7.68 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 3.56 (s, 2H), 2.46-2.35 (m, 8H), 2.26 (s, 3H), 2.23 (s, 3H). MS (ESI) m/z 603 [M + H].sup.+. I-m-2 [00128] TFA Salt .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 9.21 (s, 1H), 8.67 (s, 1H), 8.56 (s, 1H), 8.51 (d, J = 7.9 Hz, 1H), 8.19 (d, J = 2.0 Hz, 1H), 8.10-8.07 (m, 1H), 7.98-7.95 (m, 2H), 7.69 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 7.9 Hz, 1H), 7.58 (s, 1H), 3.95 (s, 3H), 3.39 (s, 2H), 2.98 (d, J = 73.2 Hz, 4H), 2.80 (s, 3H), 2.39 (s, 2H), 2.25 (s, 3H). MS (ESI) m/z: 617 [M + H].sup.+. I-m-3 [00129] TFA Salt .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.49 (s, 1H), 8.65 (dd, J = 4.5, 1.6 Hz, 2H), 8.58 (s, 1H), 8.18 (d, J = 2.2 Hz, 1H), 8.04 (dd, J = 8.5, 2.0 Hz, 1H), 7.99-7.94 (m, 4H), 7.68 (d, J = 8.6 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 3.95 (s, 3H), 3.55 (s, 2H), 2.24 (s, 3H), 2.17 (s, 3H). MS (ESI) m/z 617 [M + H].sup.+. I-m-4 [00130] MS (ESI) m/z 733 [M + H].sup.+. I-n-1 [00131] .sup.1H NMR (600 MHz, DMSO) 10.69 (s, 1H), 8.68 (d, J = 5.8 Hz, 2H), 8.62 (s, 1H), 8.19 (s, 1H), 8.04 (d, J = 5.9 Hz, 2H), 7.99 (d, J = 8.1 Hz, 1H), 7.69 (d, J = 8.4 Hz, 1H), 7.59 (d, J = 2.1 Hz, 1H), 7.53 (dd, J = 8.3, 2.3 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 3.60 (s, 2H), 3.53-3.14 (m, 8H), 2.48 (s, 3H), 1.22 (s, 3H). MS (ESI) m/z 603 [M + H].sup.+. I-n-2 [00132] TFA Salt .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.70 (s, 1H), 9.32 (s, 1H), 8.68 (d, J = 3.6 Hz, 1H), 8.56 (dt, J = 8.0, 1.8 Hz, 1H), 8.54 (s, 1H), 8.20 (d, J = 1.6 Hz, 1H), 8.01 (d, J = 8.3 Hz, 1H), 7.70 (d, J = 8.5 Hz, 1H), 7.59-7.55 (m, 2H), 7.52 (dd, J = 8.3, 2.4 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 3.94 (s, 4H), 3.42- 3.37 (m, 2H), 3.06-2.88 (m, 4H), 2.80 (s, 3H), 2.48 (s, 3H), 2.38 (s, 2H). MS (ESI) m/z 617 [M + H].sup.+. I-n-3 [00133] TFA Salt .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.83 (d, J = 5.9 Hz, 2H), 8.68 (d, J = 5.9 Hz, 2H), 8.51 (d, J = 2.9 Hz, 1H), 8.11 (d, J = 2.4 Hz, 1H), 7.90-7.82 (m, 1H), 7.71 (d, J = 8.2 Hz, 1H), 7.51 (d, J = 3.0 Hz, 1H), 7.44 (d, J = 8.2 Hz, 1H), 7.41-7.37 (m, 1H), 4.01 (d, J = 3.2 Hz, 3H), 3.74 (s, 2H), 2.86 (d, J = 2.8 Hz, 3H), 2.90-2.55 (m, 8H), 2.50 (d, J = 2.9 Hz, 3H). MS (ESI) m/z 617 [M + H].sup.+. I-n-4 [00134] TFA Salt MS (ESI) m/z 615 [M + H].sup.+. I-n-5 [00135] TFA Salt MS (ESI) m/z: 650 [M + H].sup.+. I-n-6 [00136] TFA Salt MS (ESI) m/z 650 [M + H].sup.+. I-n-7 [00137] TFA Salt MS (ESI) m/z 631.25 [M + H].sup.+. I-n-8 [00138] TFA Salt MS (ESI) m/z 631 [M + H].sup.+. I-n-9 [00139] MS (ESI) m/z 630 [M + H].sup.+. I-n-10 [00140] MS (ESI) m/z 630 [M + H].sup.+. I-n-11 [00141] TFA Salt MS (ESI) m/z 605 [M + H].sup.+. I-n-12 [00142] TFA Salt MS (ESI) m/z 621 [M + H].sup.+. I-n-13 [00143] TFA Salt MS (ESI) m/z 539 [M + H].sup.+. I-n-14 [00144] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.62-8.58 (m, 2H), 8.58 (s, 1H), 8.26-8.18 (m, 2H), 8.11 (d, J = 2.2 Hz, 1H), 7.92-7.84 (m, 1H), 7.76 (d, J = 8.6 Hz, 1H), 7.56 (d, J = 2.5 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 7.45 (dd, J = 8.3, 2.5 Hz, 1H), 5.09 (p, J = 6.7 Hz, 1H), 3.65 (s, 2H), 2.67-2.45 (m, 11H), 2.31 (s, 3H), 1.75 (d, J = 6.8 Hz, 6H). MS (ESI) m/z 645 [M + H].sup.+. I-n-15 [00145] MS (ESI) m/z 733 [M + H].sup.+. I-o-1 [00146] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 9.21 (d, J = 2.0 Hz, 1H), 8.51 (dd, J = 4.9, 1.7 Hz, 1H), 8.47 (dt, J = 8.1, 2.0 Hz, 1H), 8.33 (s, 1H), 8.09 (d, J = 2.2 Hz, 1H), 7.88 (dd, J = 8.7, 2.3 Hz, 1H), 7.73 (d, J = 8.5 Hz, 1H), 7.66-7.63 (m, 1H), 7.62 (s, 1H), 7.50 (dd, J = 8.7, 2.8 Hz, 1H), 7.41 (dd, J = 8.0, 4.8 Hz, 1H), 3.91 (s, 3H), 3.62 (s, 2H), 2.65- 2.40 m, 8H), 2.30 (s, 3H). MS (ESI) m/z 638 [M + H].sup.+. I-o-2 [00147] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.62-8.58 (m, 2H), 8.44 (s, 1H), 8.24-8.16 (m, 2H), 8.09 (d, J = 2.2 Hz, 1H), 7.88 (dd, J = 8.6, 2.2 Hz, 1H), 7.77 (d, J = 8.5 Hz, 1H), 7.70-7.69 (m, 2H), 7.55 (dd, J = 8.7, 2.8 Hz, 1H), 4.01 (s, 3H), 3.65 (s, 2H), 2.67-2.42 (m, 8H), 2.31 (s, 3H). MS (ESI) m/z: 638 [M + H].sup.+. I-o-3 [00148] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.91 (s, 1H), 8.49 (s, 1H), 8.28-8.23 (m, 2H), 8.16 (d, J = 2.2 Hz, 1H), 7.92 (dd, J = 8.5, 2.1 Hz, 1H), 7.77-7.68 (m, 3H), 7.62 (dd, J = 8.8, 2.8 Hz, 1H), 7.49-7.41 (m, 3H), 3.92 (s, 3H), 3.55 (s, 2H), 2.15 (s, 3H). MS (ESI) m/z 637 [M + H].sup.+. I-o-4 [00149] MS (ESI) m/z 670 [M + H].sup.+. I-o-5 [00150] MS (ESI) m/z 670 [M + H].sup.+. I-o-6 [00151] MS (ESI) m/z 652 [M + H].sup.+. I-o-7 [00152] MS (ESI) m/z 652 [M + H].sup.+. I-o-8 [00153] MS (ESI) m/z 651 [M + H].sup.+. I-o-9 [00154] MS (ESI) m/z 651 [M + H].sup.+. I-o-10 [00155] TFA Salt MS (ESI) m/z 626 [M + H].sup.+. I-o-11 [00156] TFA Salt MS (ESI) m/z 642 [M + H]+ I-o-12 [00157] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.52 (t, J = 3.1 Hz, 3H), 8.14-8.09 (m, 2H), 8.03 (d, J = 2.2 Hz, 1H), 7.81 (dd, J = 8.5, 2.2 Hz, 1H), 7.68 (d, J = 8.5 Hz, 1H), 7.65-7.58 (m, 2H), 7.47 (dd, J = 8.8, 2.8 Hz, 1H), 5.02-4.93 (m, 1H), 3.56 (s, 2H), 2.52-2.29 (m, 8H), 2.21 (s, 3H), 1.66 (d, J = 6.8 Hz, 6H). MS (ESI) m/z: 666 [M + H].sup.+. I-r-1 [00158] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.62-8.49 (m, 2H), 8.42 (s, 1H), 8.23-8.14 (m, 2H), 8.07 (s, 1H), 7.88 (s, 1H), 7.58 (d, J = 2.5 Hz, 1H), 7.48 (d, J = 8.4 Hz, 1H), 7.43 (dd, J = 8.4, 2.4 Hz, 2H), 4.00 (s, 3H), 3.60 (s, 2H), 2.65-2.40 (m, 8H), 2.56 (s, 3H), 2.29 (s, 3H). MS (ESI) m/z 617 [M + H].sup.+. I-r-2 [00159] MS (ESI) m/z 645 [M + H].sup.+. I-r-3 [00160] TFA salt .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.74 (s, 1H), 9.48 (s, 1H), 9.27 (s, 1H), 8.66 (s, 1H), 8.59 (s, 1H), 8.48 (d, J = 7.9 Hz, 1H), 8.06 (s, 1H), 8.03 (s, 1H), 7.58 (s, 1H), 7.56-7.49 (m, 3H), 7.42 (s, 1H), 3.68 (s, 2H), 3.03 (s, 2H), 2.96 (d, J = 10.5 Hz, 2H), 2.78 (s, 3H), 2.49 (s, 3H). MS (ESI) m/z: 603 [M + H].sup.+. I-s-1 [00161] MS (ESI) m/z 666 [M + H].sup.+.

TABLE-US-00002 TABLE 2 Structure and characterization of compounds II No. Structure 1H NMR and/or MS data II-b-1 [00162] .sup.1H NMR (600 MHz, Chloroform-d) 9.61 (s, 1H), 8.94-8.43 (m, 2H), 8.15 (s, 1H), 8.08 (s, 1H), 7.84-7.70 (m, 3H), 7.63-7.36 (m, 4H), 7.29 (d, J = 7.6 Hz, 1H), 4.15 (d, J = 2.8 Hz, 3H), 2.17 (d, J = 2.8 Hz, 3H). MS(ESI) m/z 505[M + H].sup.+. II-b-2 [00163] .sup.1H NMR (600 MHz, Chloroform-d) 8.15-8.10 (m, 2H), 8.07-8.04 (m, 1H), 7.83-7.79 (m, 1H), 7.64 (d, J = 2.2 Hz, 1H), 7.62 (t, J = 7.8 Hz, 1H), 7.46 (dd, J = 8.2, 2.3 Hz, 1H), 7.35 (s, 1H), 7.28 (d, J = 2.8 Hz, 1H), 3.89 (s, 3H), 3.77-3.70 (m, 8H), 2.18 (s, 3H). MS(ESI) m/z 513[M + H].sup.+. II-b-3 [00164] MS(ESI) m/z 541[M + H].sup.+. II-e-1 [00165] .sup.1H NMR (600 MHz, Chloroform-d) 9.42 (s, 1H), 8.80-8.46 (m, 3H), 7.99 (s, 1H), 7.96 (s, 1H), 7.93 (s, 1H), 7.83 (d, J = 9.3 Hz, 2H), 7.46 (s, 2H), 7.39 (d, J = 7.2 Hz, 1H), 4.17 (s, 3H), 2.25 (s, 3H). MS(ESI) m/z 505[M + H].sup.+. II-e-2 [00166] H NMR (600 MHz, Chloroform-d) 8.74 (s, 1H), 8.65 (s, 2H), 8.09 (d, J = 4.9 Hz, 2H), 7.97 (s, 1H), 7.96 (d, J = 1.8 Hz, 1H), 7.89 (ddd, J = 13.8, 8.4, 1.9 Hz, 2H), 7.84 (d, J = 1.7 Hz, 1H), 7.49 (d, J = 7.9 Hz, 2H), 7.45 (t, J = 8.0 Hz, 1H), 7.38 (dd, J = 7.8, 1.7 Hz, 1H), 4.20 (s, 3H), 2.26 (s, 3H). MS(ESI) m/z 505[M + H].sup.+. II-e-3 [00167] .sup.1H NMR (600 MHz, Chloroform-d) 8.17 (s, 1H), 7.95 (d, J = 1.9 Hz, 1H), 7.92-7.87 (m, 1H), 7.78 (dd, J = 7.9, 1.9 Hz, 1H), 7.74 (d, J = 1.9 Hz, 1H), 7.57 (s, 1H), 7.50 (t, J = 8.0 Hz, 1H), 7.43 (dd, J = 12.1, 7.8 Hz, 2H), 3.90 (s, 3H), 3.69 (s, 8H), 2.27 (s, 3H). MSI(ESI) m/z 513[M + H].sup.+. II-e-4 [00168] MS(ESI) m/z 541[M + H].sup.+. II-h-1 [00169] .sup.1H NMR (600 MHz, Chloroform-d) 9.49 (d, J = 2.3 Hz, 1H), 8.77 (s, 1H), 8.63-8.56 (m, 2H), 8.14 (d, J = 1.8 Hz, 1H), 8.03 (dd, J = 8.2, 1.8 Hz, 1H), 7.91 (d, J = 8.2 Hz, 1H), 7.89 (t, J = 2.2 Hz, 1H), 7.87 (s, 1H), 7.55 (dd, J = 7.6, 1.9 Hz, 1H), 7.46 (t, J = 8.1 Hz, 1H), 7.36-7.30 (m, 1H), 7.18- 7.09 (m, 1H), 4.15 (s, 3H), 3.68 (s, 2H), 2.50 (s, 8H), 2.30 (s, 3H). MS(ESI) m/z 603[M + H].sup.+. II-h-2 [00170] .sup.1H NMR (600 MHz, Chloroform-d) 8.80 (s, 1H), 8.68-8.62 (m, 2H), 8.22-8.17 (m, 2H), 8.14 (d, J = 1.8 Hz, 1H), 8.04 (dd, J = 8.2, 1.8 Hz, 1H), 7.92 (d, J = 8.2 Hz, 1H), 7.90 (t, J = 2.2 Hz, 1H), 7.88 (s, 1H), 7.61-7.55 (m, 1H), 7.49 (t, J = 8.1 Hz, 1H), 7.13 (dd, J = 7.9, 2.3 Hz, 1H), 4.19 (s, 3H), 3.69 (s, 2H), 2.31 (s, 3H). MS(ESI) m/z 603[M + H].sup.+. II-h-3 [00171] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.72 (s, 1H), 9.81 (s, 1H), 9.37-9.28 (m, 1H), 8.73-8.63 (m, 1H), 8.53 (dt, J = 8.0, 1.9 Hz, 1H), 8.30 (d, J = 1.7 Hz, 1H), 8.26 (dd, J = 8.2, 1.8 Hz, 1H), 8.12 (s, 1H), 7.96 (t, J = 2.2 Hz, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.77 (dd, J = 8.1, 1.9 Hz, 1H), 7.58 (t, J = 8.2 Hz, 1H), 7.54 (dd, J = 8.0, 4.7 Hz, 1H), 7.25 (dd, J = 8.0, 2.3 Hz, 1H), 3.79 (s, 2H), 3.41 (d, J = 12.2 Hz, 2H), 3.07 (s, 2H), 2.92 (d, J = 12.6 Hz, 2H), 2.81 (s, 3H), 2.42 (t, J = 12.2 Hz, 2H). MS(ESI) m/z: 589[M + H].sup.+. II-h-4 [00172] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.73 (s, 1H), 9.79 (s, 1H), 8.75 (d, J = 5.2 Hz, 2H), 8.30 (d, J = 1.8 Hz, 1H), 8.27 (dd, J = 8.1, 1.8 Hz, 1H), 8.17- 8.09 (m, 2H), 7.96 (t, J = 2.2 Hz, 1H), 7.93 (d, J = 8.1 Hz, 1H), 7.77 (dd, J = 8.4, 1.9 Hz, 1H), 7.58 (t, J = 8.2 Hz, 1H), 7.25 (dd, J = 7.8, 2.2 Hz, 1H), 3.79 (s, 2H), 3.44-3.38 (m, 2H), 3.07 (s, 2H), 2.92 (d, J = 12.7 Hz, 2H), 2.81 (s, 3H), 2.42 (t, J = 12.2 Hz, 2H). MS(ESI) m/z: 589[M + H].sup.+. II-i-1 [00173] .sup.1H NMR (600 MHz, Chloroform-d) 9.42 (d, J = 2.1 Hz, 1H), 9.28 (s, 1H), 8.53 (ddd, J = 7.9, 4.4, 1.8 Hz, 2H), 8.13 (d, J = 1.8 Hz, 1H), 8.01 (dd, J = 8.2, 1.8 Hz, 1H), 7.83 (d, J = 8.2 Hz, 1H), 7.75 (d, J = 2.2 Hz, 1H), 7.69 (s, 1H), 7.47 (dd, J = 8.3, 2.2 Hz, 1H), 7.27 (dt, J = 8.0, 3.5 Hz, 1H), 7.23 (d, J = 8.3 Hz, 1H), 4.10 (s, 3H), 3.62 (s, 2H), 2.45 (s, 8H), 2.25 (s, 3H), 2.12 (s, 3H). MS(ESI) m/z 617[M + H].sup.+. II-i-2 [00174] .sup.1H NMR (600 MHz, Chloroform-d) 9.01 (s, 1H), 8.64-8.59 (m, 2H), 8.19-8.14 (m, 2H), 8.11 (d, J = 1.9 Hz, 1H), 8.01 (dd, J = 8.1, 1.9 Hz, 1H), 7.88 (d, J = 8.2 Hz, 1H), 7.78 (d, J = 2.2 Hz, 1H), 7.74 (s, 1H), 7.51 (dd, J = 8.4, 2.2 Hz, 1H), 7.30 (d, J = 8.3 Hz, 1H), 4.17 (s, 3H), 3.65 (s, 2H), 2.48 (s, 8H), 2.27 (s, 3H), 2.16 (s, 3H). MS(ESI) m/z 617[M + H].sup.+. II-i-3 [00175] .sup.1H NMR (600 MHz, Chloroform-d.sub.6) 10.54 (s, 1H), 8.56 (s, 1H), 8.23 (d, J = 1.8 Hz, 1H), 8.21 (d, J = 8.1 Hz, 1H), 8.13 (s, 1H), 7.92 (d, J = 8.2 Hz, 1H), 7.74 (d, J = 2.1 Hz, 1H), 7.63 (dd, J = 8.3, 2.2 Hz, 1H), 7.38 (d, J = 8.4 Hz, 1H), 4.06 (s, 3H), 3.67 (s, 2H), 2.42 (s, 8H), 2.17 (s, 3H), 2.07 (s, 3H). MS(ESI) m/z 540[M + H].sup.+ II-j-1 [00176] .sup.1H NMR (600 MHz, Chloroform-d) 9.45 (d, J = 2.2 Hz, 1H), 8.60 (dd, J = 13.0, 6.4 Hz, 2H), 8.33 (s, 1H), 8.19 (s, 1H), 8.05 (d, J = 8.1 Hz, 1H), 7.97 (dd, J = 11.0, 5.3 Hz, 2H), 7.85 (s, 1H), 7.35-7.27 (m, 2H), 7.07 (dd, J = 8.2, 2.5 Hz, 1H), 4.14 (s, 3H), 3.71 (s, 2H), 2.41 (s, 3H), 2.30 (s, 3H). MS(ESI) m/z [M + H].sup.+. II-j-2 [00177] .sup.1H NMR (600 MHz, Chloroform-d) 8.64 (d, J = 5.0 Hz, 2H), 8.37 (s, 1H), 8.20 (d, J = 5.0 Hz, 2H), 8.16 (s, 1H), 8.04 (d, J = 8.2 Hz, 1H), 8.00 (s, 1H), 7.96 (d, J = 8.2 Hz, 1H), 7.84 (s, 1H), 7.34 (d, J = 8.2 Hz, 1H), 7.11 (dd, J = 8.3, 2.3 Hz, 1H), 4.15 (s, 3H), 3.70 (s, 2H), 2.57-2.47 (m, 8H), 2.42 (s, 3H), 2.29 (s, 3H). MS(ESI) m/z 617[M + H].sup.+. II-j-3 [00178] MS(ESI) m/z 606[M + H].sup.+. II-j-4 [00179] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.25 (s, 1H), 8.35-8.28 (m, 2H), 8.27-8.21 (m, 1H), 7.93 (d, J = 8.1 Hz, 1H), 7.89 (s, 1H), 7.75 (d, J = 5.1 Hz, 1H), 7.63 (dd, J = 5.1, 3.0 Hz, 1H), 7.49 (d, J = 2.5 Hz, 1H), 7.45 (d, J = 8.4 Hz, 1H), 7.27 (dd, J = 8.3, 2.5 Hz, 1H), 4.07 (s, 3H), 3.69 (s, 2H), 2.46 (s, 8H), 2.33 (s, 3H). MS(ESI) m/z 622[M + H].sup.+. II-j-5 [00180] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.31 (s, 1H), 9.88 (s, 1H), 9.41 (d, J = 2.2 Hz, 1H), 8.78 (dd, J = 5.1, 1.6 Hz, 1H), 8.74 (dt, J = 8.2, 1.9 Hz, 1H), 8.34 (d, J = 1.8 Hz, 1H), 8.29 (dd, J = 8.1, 1.8 Hz, 1H), 8.06 (s, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.70 (dd, J = 8.1, 5.0 Hz, 1H), 7.51 (d, J = 2.5 Hz, 1H), 7.48 (d, J = 8.4 Hz, 1H), 7.31 (dd, J = 8.3, 2.5 Hz, 1H), 3.80 (s, 2H), 3.43 (dd, J = 11.9, 9.0 Hz, 2H), 3.11-3.02 (m, 2H), 2.94 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.44 (t, J = 12.2 Hz, 2H), 2.35 (s, 3H). MS(ESI) m/z: 603[M + H].sup.+. II-j-6 [00181] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.31 (s, 1H), 9.68 (s, 1H), 8.84-8.75 (m, 2H), 8.34 (d, J = 1.8 Hz, 1H), 8.29 (dd, J = 8.1, 1.8 Hz, 1H), 8.26-8.19 (m, 2H), 8.08 (s, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.52 (d, J = 2.5 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 7.32 (dd, J = 8.3, 2.6 Hz, 1H), 3.79 (s, 2H), 3.45-3.38 (m, 2H), 3.07 (s, 2H), 2.93 (d, J = 12.2 Hz, 2H), 2.82 (s, 3H), 2.45-2.37 (m, 2H), 2.35 (s, 3H). MS(ESI) m/z: 603[M + H].sup.+. II-k-1 [00182] .sup.1H NMR (600 MHz, Chloroform-d) 9.51 (d, J = 2.1 Hz, 1H), 8.70-8.61 (m, 3H), 8.57 (s, 1H), 8.20 (d, J = 1.7 Hz, 1H), 8.08-8.00 (m, 3H), 7.56 (d, J = 8.6 Hz, 1H), 7.36 (ddd, J = 7.2, 4.3, 0.9 Hz, 1H), 7.14 (dd, J = 8.7, 2.8 Hz, 1H), 4.20 (s, 3H), 3.75 (s, 2H), 2.57 (s, 8H), 2.34 (s, 3H). MS(ESI) m/z: 638[M + H].sup.+. II-k-2 [00183] .sup.1H NMR (600 MHz, Chloroform-d) 8.77-8.67 (m, 3H), 8.57 (s, 1H), 8.24-8.21 (m, 2H), 8.20 (d, J = 1.7 Hz, 1H), 8.08-8.01 (m, 3H), 7.59 (d, J = 8.7 Hz, 1H), 7.16 (dd, J = 8.7, 2.8 Hz, 1H), 4.23 (s, 3H), 3.76 (s, 2H), 2.59 (s, 8H), 2.35 (s, 3H). MS(ESI) m/z: 638[M + H].sup.+. II-k-3 [00184] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 9.77 (s, 1H), 9.39 (d, J = 2.3 Hz, 1H), 8.78 (dd, J = 5.0, 1.7 Hz, 1H), 8.71 (dt, J = 8.1, 1.9 Hz, 1H), 8.35 (d, J = 1.9 Hz, 1H), 8.30 (d, J = 9.3 Hz, 2H), 7.95 (d, J = 8.2 Hz, 1H), 7.78 (d, J = 5.9 Hz, 1H), 7.77 (s, 1H), 7.70 (dd, J = 8.1, 5.0 Hz, 1H), 7.48 (dd, J = 8.8, 2.8 Hz, 1H), 3.80 (s, 2H), 3.45-3.38 (m, 2H), 3.07 (t, J = 11.9 Hz, 2H), 2.94 (d, J = 12.6 Hz, 2H), 2.82 (s, 3H), 2.43 (t, J = 12.3 Hz, 2H). MS(ESI) m/z: 624[M + H].sup.+. II-k-4 [00185] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 9.84 (s, 1H), 8.91-8.83 (m, 2H), 8.36 (dd, J = 6.5, 1.8 Hz, 3H), 8.34 (s, 1H), 8.31 (dd, J = 8.1, 1.8 Hz, 1H), 7.95 (d, J = 8.3 Hz, 1H), 7.80-7.76 (m, 2H), 7.49 (dd, J = 8.8, 2.8 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.13-3.03 (m, 2H), 2.94 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.44 (t, J = 12.3 Hz, 2H). MS(ESI) m/z: 624[M + H].sup.+. II-l-1 [00186] MS(ESI) m/z 603[M + H].sup.+. II-l-2 [00187] MS(ESI) m/z 603[M + H].sup.+. II-m-1 [00188] .sup.1H NMR (600 MHz, Chloroform-d) 9.37 (d, J = 2.1 Hz, 1H), 8.95 (s, 1H), 8.56 (dd, J = 4.8, 1.7 Hz, 1H), 8.43 (dt, J = 8.0, 2.0 Hz, 1H), 7.91 (dd, J = 8.6, 2.2 Hz, 1H), 7.88 (s, 2H), 7.84 (d, J = 8.5 Hz, 2H), 7.71 (d, J = 8.5 Hz, 1H), 7.42 (d, J = 7.8 Hz, 1H), 7.25 (dd, J = 8.0, 4.8 Hz, 1H), 4.12 (s, 3H), 3.61 (s, 2H), 2.51 (s, 8H), 2.31 (s, 3H), 2.23 (s, 3H). MS(ESI) m/z 617[M + H].sup.+. II-m-2 [00189] .sup.1H NMR (600 MHz, Chloroform-d) 8.67 (d, J = 6.8 Hz, 1H), 8.64-8.60 (m, 2H), 8.07-8.02 (m, 2H), 7.95 (s, 1H), 7.91 (dd, J = 8.5, 2.3 Hz, 1H), 7.87 (dt, J = 4.4, 2.2 Hz, 2H), 7.83 (d, J = 1.7 Hz, 1H), 7.71 (d, J = 8.5 Hz, 1H), 7.49 (d, J = 8.0 Hz, 1H), 4.20 (s, 3H), 3.63 (s, 2H), 2.57 (s, 8H), 2.37 (s, 3H), 2.26 (s, 3H). MS(ESI) m/z 617[M + H].sup.+. II-m-3 [00190] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 8.22-8.19 (m, 3H), 8.13 (s, 1H), 8.10 (dd, J = 8.6, 2.1 Hz, 1H), 8.01 (d, J = 1.6 Hz, 1H), 8.01-7.97 (m, 1H), 7.70 (d, J = 8.6 Hz, 1H), 7.65 (d, J = 7.9 Hz, 1H), 7.48 (d, J = 7.0 Hz, 1H), 7.45 (t, J = 7.4 Hz, 2H), 4.13 (s, 3H), 3.71 (s, 2H), 2.81 (s, 3H), 2.24 (s, 3H). MS(ESI) m/z 616[M + H].sup.+. II-m-4 [00191] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 8.21 (d, J = 2.1 Hz, 1H), 8.13-8.08 (m, 4H), 8.01 (d, J = 1.7 Hz, 1H), 7.99 (dd, J = 7.9, 1.8 Hz, 1H), 7.71 (d, J = 8.6 Hz, 1H), 7.64 (d, J = 7.9 Hz, 1H), 7.25 (d, J = 8.0 Hz, 1H), 4.11 (s, 3H), 3.71 (s, 2H), 3.41 (s, 2H), 3.06 (s, 2H), 2.95 (s, 2H), 2.81 (s, 3H), 2.44 (s, 2H), 2.33 (s, 3H), 2.24 (s, 3H). MS(ESI) m/z 630[M + H].sup.+. II-m-5 [00192] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 8.20 (d, J = 2.2 Hz, 1H), 8.19 (t, J = 1.9 Hz, 1H), 8.15-8.12 (m, 2H), 8.09 (dd, J = 8.6, 2.2 Hz, 1H), 8.04 (d, J = 1.7 Hz, 1H), 8.00 (dd, J = 7.9, 1.8 Hz, 1H), 7.70 (d, J = 8.6 Hz, 1H), 7.65 (d, J = 8.0 Hz, 1H), 7.56 (ddd, J = 8.0, 2.3, 1.1 Hz, 1H), 7.49 (t, J = 7.9 Hz, 1H), 4.13 (s, 3H), 3.69 (s, 2H), 3.40 (s, 2H), 3.04 (s, 2H), 2.92 (s, 2H), 2.81 (s, 3H), 2.41 (s, 2H), 2.25 (s, 3H). MS(ESI) m/z 650[M + H].sup.+. II-m-6 [00193] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 8.19 (d, J = 8.0 Hz, 3H), 8.11 (s, 1H), 8.10-8.07 (m, 1H), 8.02-7.97 (m, 2H), 7.70 (d, J = 8.6 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.52 (d, J = 8.3 Hz, 2H), 4.12 (s, 3H), 3.70 (s, 2H), 3.40 (s, 2H), 3.05 (s, 2H), 2.93 (s, 2H), 2.81 (s, 3H), 2.42 (s, 2H), 2.24 (s, 3H). MS(ESI) m/z 650[M + H].sup.+. II-m-7 [00194] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 8.20 (d, J = 2.1 Hz, 1H), 8.09 (d, J = 7.3 Hz, 2H), 8.04-7.97 (m, 2H), 7.70 (d, J = 8.6 Hz, 1H), 7.68- 7.61 (m, 3H), 7.22 (t, J = 7.9 Hz, 1H), 6.88 (dd, J = 8.0, 2.4 Hz, 1H), 4.11 (s, 3H), 3.70 (s, 2H), 3.04 (s, 2H), 3.05 (s, 2H), 2.93 (s, 2H), 2.80 (s, 3H), 2.40 (d, J = 13.5 Hz, 2H), 2.24 (s, 3H). MS(ESI) m/z 632 [M + H].sup.+. II-m-8 [00195] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 8.21 (d, J = 2.2 Hz, 1H), 8.10 (dd, J = 8.6, 2.2 Hz, 1H), 8.06 (d, J = 1.9 Hz, 1H), 8.05 (d, J = 2.8 Hz, 2H), 7.98 (d, J = 8.0 Hz, 2H), 7.71 (d, J = 8.6 Hz, 1H), 7.64 (d, J = 7.8 Hz, 1H), 6.94-6.71 (m, 2H), 4.08 (s, 3H), 3.70 (s, 2H), 3.41 (s, 2H), 3.05 (s, 2H), 2.93 (s, 2H), 2.81 (s, 3H), 2.42 (s, 2H), 2.23 (s, 3H). MS(ESI) m/z 632 [M + H].sup.+. II-m-9 [00196] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 8.21 (d, J = 2.1 Hz, 1H), 8.15 (d, J = 1.4 Hz, 1H), 8.10 (dd, J = 8.6, 2.1 Hz, 1H), 8.00 (d, J = 1.7 Hz, 1H), 7.99-7.95 (m, 1H), 7.91 (s, 1H), 7.76 (t, J = 1.7 Hz, 1H), 7.71 (d, J = 8.5 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 6.88 (d, J = 1.6 Hz, 1H), 4.06 (s, 3H), 3.73 (s, 2H), 3.42 (s, 2H), 3.12-3.01 (m, 2H), 2.96 (s, 2H), 2.81 (s, 3H), 2.46 (s, 2H), 2.23 (s, 3H). MS(ESI) m/z 606 [M + H].sup.+. II-m-10 [00197] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 8.20 (d, J = 2.1 Hz, 1H), 8.13 (d, J = 2.9 Hz, 1H) 8.10 (dd, J = 8.6 2.1 Hz, 1H), 8.04 (s, 1H), 8.00 (d, J = 1.7 Hz, 1H), 7.99-7.96 (m, 1H), 7.71 (d, J = 8.6 Hz, 1H), 7.65-7.59 (m, 3H), 4.09 (s, 3H), 3.71 (s, 2H), 3.41 (s, 2H), 3.04 (d, J = 14.1 Hz, 2H), 2.94 (s, 2H), 2.81 (s, 3H), 2.42 (s, 2H), 2.24 (s, 3H). MS(ESI) m/z 622[M + H].sup.+. II-m-11 [00198] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.47 (s, 1H), 9.87 (s, 1H), 8.75 (s, 1H), 8.18 (d, J = 2.2 Hz, 1H), 8.09 (d, J = 4.6 Hz, 1H), 8.04 (dd, J = 8.5, 2.2 Hz, 1H), 7.96 (dd, J = 6.1, 2.0 Hz, 3H), 7.69 (d, J = 8.6 Hz, 1H), 7.60 (d, J = 8.5 Hz, 1H), 7.12 (d, J = 9.0 Hz, 1H), 3.93 (s, 3H), 3.55 (s, 2H), 2.37 (s, 8H), 2.22 (s, 3H), 2.16 (s, 3H). MS(ESI) m/z 632[M + H].sup.+. II-m-12 [00199] MS(ESI) m/z 631[M + H].sup.+. II-m-13 [00200] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.46 (s, 1H), 9.57 (s, 1H), 8.18 (d, J = 2.2 Hz, 1H), 8.04 (dd, J = 8.6, 2.2 Hz, 1H), 8.00-7.89 (m, 3H), 7.69 (d, J = 8.6 Hz, 1H), 7.59 (d, J = 7.9 Hz, 1H), 7.44 (s, 2H), 6.91 (s, 2H), 3.90 (s, 3H), 3.55 (s, 2H), 2.45- 2.31 (m, 8H), 2.23 (s, 3H), 2.16 (s, 6H). MS(ESI) m/z 645[M + H].sup.+. II-m-14 [00201] MS(ESI) m/z 595[M + H].sup.+. II-m-15 [00202] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.45 (s, 1H), 8.18 (d, J = 2.1 Hz, 1H), 8.04 (dd, J = 8.6, 2.1 Hz, 1H), 7.93-7.86 (m, 2H), 7.73-7.65 (m, 2H), 7.56 (d, J = 8.4 Hz, 1H), 3.84 (s, 3H), 3.57 (d, J = 5.9 Hz, 8H), 2.44-2.35 (m, 8H), 2.21 (s, 3H), 2.17 (s, 3H). MS(ESI) m/z 625[M + H].sup.+. II-m-16 [00203] MS(ESI) m/z 653[M + H].sup.+. II-m-17 [00204] MS(ESI) m/z 638[M + H].sup.+. II-m-18 [00205] MS(ESI) m/z 583[M + H].sup.+. II-m-19 [00206] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.53 (s, 1H), 8.56 (s, 1H), 8.27 (s, 1H), 8.19 (d, J = 2.2 Hz, 1H), 8.09 (dd, J = 8.5, 2.3 Hz, 1H), 7.93 (dd, J = 7.9, 1.8 Hz, 1H), 7.90 (d, J = 1.8 Hz, 1H), 7.70 (d, J = 8.5 Hz, 1H), 7.59 (d, J = 8.1 Hz, 1H), 4.08 (s, 3H), 3.41 (d, J = 12.1 Hz, 2H), 3.10-2.99 (m, 2H), 2.93 (d, J = 12.3 Hz, 2H), 2.80 (s, 3H), 2.45-2.34 (m, 2H), 2.18 (s, 3H). MS(ESI) m/z 540[M + H].sup.+. II-m-20 [00207] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 9.74 (s, 1H), 9.25 (s, 1H), 8.78-8.66 (m, 1H), 8.56 (dt, J = 8.1, 2.0 Hz, 1H), 8.29-8.18 (m, 2H), 8.10 (dd, J = 8.6, 2.1 Hz, 1H), 8.02 (d, J = 1.7 Hz, 1H), 8.00 (dd, J = 7.9, 1.8 Hz, 1H), 7.71 (d, J = 8.6 Hz, 1H), 7.68-7.61 (m, 2H), 3.71 (s, 2H), 3.45-3.37 (m, 2H), 3.05 (s, 2H), 2.94 (s, 2H), 2.81 (s, 3H), 2.41 (d, J = 15.1 Hz, 2H), 2.26 (s, 3H). MS(ESI) m/z: 603[M + H].sup.+. II-m-21 [00208] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 9.62 (s, 1H), 8.78 (d, J = 5.3 Hz, 2H), 8.22 (s, 1H), 8.20 (d, J = 2.1 Hz, 1H), 8.13 (d, J = 5.4 Hz, 2H), 8.09 (dd, J = 8.6, 2.1 Hz, 1H), 8.02 (d, J = 1.7 Hz, 1H), 8.00 (dd, J = 7.9, 1.8 Hz, 1H), 3.68 (s, 2H), 3.40 (d, J = 12.1 Hz, 2H), 3.05 (d, J = 12.3 Hz, 2H), 2.92 (d, J = 12.4 Hz, 2H), 2.80 (s, 3H), 2.43- 2.33 (m, 2H), 2.26 (s, 3H), MS(ESI) m/z: 603[M + H].sup.+. II-m-22 [00209] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 8.89-8.73 (m, 2H), 8.28-8.22 (m, 2H), 8.20 (d, J = 2.3 Hz, 2H), 8.09 (dd, J = 8.6, 2.2 Hz, 1H), 8.05- 7.98 (m, 2H), 7.71 (d, J = 8.6 Hz), 1H), 7.66 (d, J = 7.9 Hz, 1H), 4.60 (q, J = 7.3 Hz, 2H), 3.70 (s 2H), 3.42 (d, J = 15.7 Hz, 2H), 3.05 (s, 2H), 2.93 (s, 2H), 2.81 (s, 3H), 2.43 (s, 2H), 2.26 (s, 3H), 1.52 (t, J = 7.2 Hz, 3H). MS(ESI) m/z: 632 [M + H].sup.+. II-m-23 [00210] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 8.82 (d, J = 5.4 Hz, 2H), 8.25 (d, J = 5.4 Hz, 2H), 8.20 (d, J = 2.6 Hz, 2H), 8.09 (dd, J = 8.6, 2.1 Hz, 1H), 8.01 (d, J = 7.0 Hz, 2H), 7.70 (d, J = 8.6 Hz, 1H), 7.66 (d, J = 8.1 Hz, 1H), 5.32 (p, J = 6.7 Hz, 1H), 3.70 (s, 2H), 3.41 (s, 2H), 3.05 (s, 2H), 2.93 (s, 2H), 2.81 (s, 3H), 2.41 (d, J = 17.3 Hz, 2H), 2.27 (s, 3H), 1.59 (d, J = 6.7 Hz, 6H). ME (ESI) m/z: 631 [M + H].sup.+. II-n-1 [00211] MS(ESI) m/z 617[M + H].sup.+. II-n-2 [00212] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.67 (s, 1H), 8.78-8.71 (m, 2H), 8.19-8.13 (m, 4H), 7.96 (dd, J = 8.5, 2.1 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.61 (d, J = 2.4 Hz, 1H), 7.55 (dd, J = 8.3, 2.5 Hz, 1H), 7.51 (d, J = 8.4 Hz, 1H), 4.15 (s, 3H), 3.56 (s, 2H), 2.49 (s, 3H), 2.42-2.36 (m, 8H), 2.19 (s, 3H). MS(ESI) m/z 617[M + H].sup.+. II-o-1 [00213] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.98 (s, 1H), 9.40 (s, 1H), 8.76 (d, J = 4.8 Hz, 1H), 8.66 (dt, J = 8.0, 2.0 Hz, 1H), 8.31 (s, 1H), 8.17 (d, J = 2.1 Hz, 1H), 7.97 (dd, J = 8.5, 2.1 Hz, 1H), 7.83-7.76 (m, 2H), 7.73 (d, J = 8.6 Hz, 1H), 7.69 (dd, J = 8.8, 2.9 Hz, 1H), 7.64 (dd, J = 8.1, 4.8 Hz, 1H), 4.15 (s, 3H), 3.69 (s, 2H), 3.41 (d, J = 12.1 Hz, 2H), 3.04 (s, 2H), 2.93 (d, J = 13.1 Hz, 2H), 2.81 (s, 3H), 2.40 (s, 2H). MS(ESI) m/z 638[M + H].sup.+. II-o-2 [00214] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.94 (s, 1H), 8.77-8.70 (m, 2H), 8.32 (s, 1H), 8.17-8.13 (m, 3H), 7.93 (dd, J = 8.5, 2.2 Hz, 1H), 7.80 (d J = 2.8 Hz, 1H), 7.78 (d, J = 8.7 Hz, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.68 (dd, J = 8.7, 2.9 Hz, 1H), 4.15 (s, 3H), 3.56 (s, 2H), 2.38 (s, 8H), 2.18 (s, 3H). MS(ESI) m/z 638[M + H].sup.+. II-p-1 [00215] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 7.75 (d, J = 6.6 Hz, 2H), 7.37 (d, J = 5.2 Hz, 2H). 7.79 (d, J = 3.9 Hz, 2H), 7.20 (t, J = 5.9 Hz, 2H), 7.13 (s, 2H), 6.93-6.85 (m, 1H), 6.84-679 (m, 1H), 6.62 (s, 1H), 3.35 (d, J = 4.7 Hz, 3H), 2.79 (d, J = 4.9 Hz, 3H), 1.73 (s, 8H). MS (ESI m/z 603[M + H].sup.+. II-p-2 [00216] MS(ESI) m/z 603[M + H].sup.+. II-s-1 [00217] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 9.27 (d, J = 2.2 Hz, 1H), 8.66 (dd, J = 4.7, 1.8 Hz, 1H), 8.49 (dt, J = 8.0, 2.0 Hz, 1H), 8.19 (s, 1H), 8.16 (s, 1H), 8.05-7.97 (m, 3H), 7.65 (d, J = 8.0 Hz, 1H), 7.51 (dd, J = 8.0, 4.7 Hz, 1H), 7.34 (s, 1H), 4.14 (s, 3H), 3.52 (s, 2H), 2.36 (s, 9H), 2.24 (s, 3H), 2.16 (s, 3H), MS(ESI) m/z 617[M + H].sup.+. II-s-2 [00218] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 8.73-8.67 (m, 2H), 8.19 (s, 1H), 8.16 (d, J = 1.9 Hz, 1H), 8.06-8.04 (m, 2H), 8.03 (d, J = 1.8 Hz, 1H), 8.02-7.99 (m, 2H), 7.66 (d, J = 8.0 Hz, 1H), 7.35 (s, 1H), 4.16 (s, 3H), 3.53 (s, 2H), 2.45-2.33 (m, 8H), 2.24 (s, 3H), 2.19 (s, 3H). MS(ESI) m/z: 617[M + H].sup.+ II-t-1 [00219] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.86 (s, 1H), 9.38 (s, 1H), 8.69 (d, J = 4.8 Hz, 1H), 8.57 (dt, J = 8.0, 2.0 Hz, 1H), 8.21-8.16 (m, 3H), 8.10 (s, 1H), 7.72 (d, J = 1.8 Hz, 1H), 7.66 (d, J = 2.5 Hz, 1H), 7.57 (dd, J = 8.4, 2.5 Hz, 1H), 7.55-7.51 (m, 2H), 7.47 (s, 1H), 4.13 (s, 3H), 2.52 (s, 3H), 2.17 (s, 3H). MS(ESI) m/z 585[M + H].sup.+. II-t-2 [00220] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.87 (s, 1H), 8.75-8.70 (m, 2H), 8.18 (d, J = 1.6 Hz, 2H), 8.15 (s, 1H), 8.14-8.11 (m, 2H), 8.10 (s, 1H), 7.72 (t, J = 1.7 Hz, 1H), 7.66 (d, J = 2.5 Hz, 1H), 7.57 (dd, J = 8.3, 2.5 Hz, 1H), 7.53 (d, J = 8.4 Hz, 1H), 7.45 (t, J = 1.3 Hz, 1H), 4.13 (s, 3H), 2.55 (s, 2H), 2.52 (s, 3H), 2.17 (d, J = 1.0 Hz, 3H). MS(ESI) m/z 585[M + H].sup.+. II-v-1 [00221] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.84 (s, 1H), 9.27 (d, J = 2.1 Hz, 1H), 8.68 (dd, J = 4.8, 1.7 Hz, 1H), 8.53-8.47 (m, 3H), 8.23 (s, 1H), 8.04 (d, J = 1.8 Hz, 1H), 8.02 (dd, J = 7.9, 1.8 Hz, 1H), 7.82 (s, 1H), 7.69 (d, J = 7.9 Hz, 1H), 7.53 (dd, J = 8.0, 4.8 Hz, 1H), 4.15 (s, 3H), 2.26 (s, 3H), ES(ESI) m/z 573[M + H].sup.+. II-v-2 [00222] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.28 (s, 1H), 9.29 (s, 1H), 8.71 (s, 1H), 8.56 (d, J = 8.0 Hz, 1H), 8.19 (s, 1H), 7.98 (d, J = 9.0 Hz, 2H), 7.76 (d, J = 8.1 Hz, 2H), 7.64 (d, J = 7.8 Hz, 1H), 7.59 (d, J = 7.0 Hz, 1H), 7.34 (t, J = 7.8 Hz, 2H), 7.10 (t, J = 7.4 Hz, 1H), 4.15 (s, 3H), 2.24 (d, s 3H). MS(ESI) m/z 437 [M + H].sup.+. II-v-3 [00223] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 9.27 (d, J = 2.0 Hz, 1H), 8.92-8.84 (m, 1H), 8.73 (dd, J = 5.0, 1.6 Hz, 1H), 8.58 (dt, J = 8.1, 2.0 Hz, 1H), 7.63 (dd, J = 8.0, 4.9 Hz, 1H), 7.53 (d, J = 7.8 Hz, 1H), 7.44 (d, J = 1.5 Hz, 1H), 7.38 (dd, J = 7.8, 1.6 Hz, 1H), 4.12 (s, 3H), 3.60 (s, 8H), 2.20 (s, 3H). MS (ESI) m/z 431[M + H].sup.+. II-v-4 [00224] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 9.27 (dd, J = 2.2 0.8 Hz, 1H), 8.68 (dd, J = 4.8, 1.7 Hz, 1H), 8.50-- 8.47 (m, 1H), 8.46 (t, J = 5.7 Hz, 1H), 8.15 (s, 1H), 7.85-7.80 (m, 2H), 7.56 (dd, J = 8.4, 0.8 Hz, 1H), 7.52 (ddd, J = 8.0, 4.8, 0.9 Hz, 1H), 4.14 (s, 3H), 3.54 (t, J = 4.6 Hz, 4H), 3.37 (q, J = 6.8 Hz, 2H), 2.45 (t, J = 7.0 Hz, 2H), 2.39 (s, 4H), 2.21 (s, 3H). MS(ESI) m/z 474[M + H].sup.+. II-v-5 [00225] MS(ESI) m/z 444 [M + H].sup.+. II-v-6 [00226] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 9.29 (d, J = 2 Hz, 1H), 8.75 (dd, J = 5.1, 1.7 Hz, 1H), 8.62 (dt, J = 8.0, 1.9 Hz, 1H), 8.49 (t, J = 5.7 Hz, 1H), 8.11 (s, 1H), 7.86 (dq, J = 2.9, 1.8 Hz, 2H), 7.66 (dd, J = 8.1, 4.9 Hz, 1H), 7.58-7.53 (m, 1H), 4.14 (s, 3H), 3.51 (t, J = 6.2 Hz, 2H), 3.32 (q, J = 6.0 Hz, 2H), 2.21 (s, 3H), MS(ESI) m/z 405[M + H].sup.+. II-v-7 [00227] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.43 (s, 1H), 9.28 (s, 1H), 8.67 (s, 1H), 8.48 (dd, J = 7.9, 2.0 Hz, 1H), 8.18 (s, 1H), 8.11 (d, J = 2.4 Hz, 1H), 8.05-7.94 (m, 3H), 7.78 (t, J = 5.9 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.51 (d, J = 8.8 Hz, 2H), 4.13 (s, 3H), 2.99 (t, J = 6.4 Hz, 2H), 2.90 (dt, J = 11.8, 3.5 Hz, 2H), 2.67 (td, J = 11.5, 2.4 Hz, 2H), 2.24 (s, 3H), 2.09 (q, J = 7.6 Hz, 2H), 1.74-1.63 (m, 2H), 1.51 (ddq, J = 11.0, 7.4, 3.7 Hz, 1H), 1.22 (td, J = 12.1, 3.9 Hz, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS(ESI) m/z: 673 [M + H].sup.+. II-v-8 [00228] .sup.1H NMR (600 MHz, Chloroform-d) 9.38 (s, 1H), 8.64-8.54 (m, 2H), 8.05 (d, J = 5.2 Hz, 2H), 7.95- 7.81 (m, 5H), 7.43 (d, J = 7.9 Hz, 1H), 7.22 (d, J = 8.5 Hz, 1H), 4.16 (s, 3H), 3.83 (dtd, J = 11.5, 7.6, 4.4 Hz, 1H), 2.91 (d, J = 10.5 Hz, 2H), 2.68 (t, J = 11.2 Hz, 2H), 2.33 (s, 3H), 2.18 (q, J = 7.6 Hz, 2H), 1.88 (dd, J = 12.8, 4.1 Hz, 2H), 1.55 (tt, J = 11.6, 6.0 Hz, 2H), 1.12 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 659 [M + H].sup.+. II-v-9 [00229] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.58 (d, J = 5.2 Hz, 2H), 8.21-8.16 (m, 2H), 8.10 (s, 1H), 8.02 (d, J = 2.5 Hz, 1H), 7.96-7.91 (m, 2H), 7.89 (dd, J = 8.7, 2.6 Hz, 1H), 7.57 (d, J = 7.9 Hz, 1H), 7.44 (d, J = 8.8 Hz, 1H), 4.19 (s, 3H), 3.13 (t, J = 6.3 Hz, 2H), 3.04-2.96 (m, 2H), 2.73 (td, J = 11.5, 2.3 Hz, 2H), 2.28 (s, 3H), 2.23 (q, J = 7.6 Hz, 2H), 1.80-1.73 (m, 2H), 1.63 (td, J = 7.3, 3.7 Hz, 1H), 1.28 (s, 2H), 1.17-1.14 (m, 3H). MS (ESI) m/z: 673 [M + H]+. II-v-10 [00230] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.43 (s, 1H), 9.29 (s, 1H), 8.76-8.69 (m, 1H), 8.59 (dt, J = 8.1, 1.9 Hz, 1H), 8.18 (s, 1H), 8.11 (d, J = 2.4 Hz, 1H), 8.04-7.95 (m, 3H), 7.88 (t, J = 5.9 Hz, 1H), 7.63 (dd, J = 16.7, 7.8 Hz, 2H), 7.52 (d, J = 8.8 Hz, 1H), 4.15 (s, 3H), 2.98 (t, J = 6.3 Hz, 2H), 2.93-2.87 (m, 2H), 2.67 (td, J = 11.4, 2.3 Hz, 2H), 2.24 (s, 3H), 1.82 (s, 3H), 1.70 (dd, J = 13.4, 3.5 Hz, 2H), 1.50 (ddq, J = 11.3, 7.8, 3.9 Hz, 1H), 1.23 (qd, J = 11.7, 3.8 Hz, 2H). MS (ESI) m/z: 659 [M + H].sup.+. II-v-11 [00231] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.44 (s, 1H), 8.81 (s, 2H), 8.22 (s, 2H), 8.20 (s, 1H), 8.11 (d, J = 2.5 Hz, 1H), 8.05-7.96 (m, 3H), 7.88 (t, J = 5.9 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.51 (d, J = 8.8 Hz, 1H), 4.17 (s, 3H), 2.98 (t, J = 6.4 Hz, 2H), 2.93-2.84 (m, 2H), 2.67 (td, J = 11.5, 2.3 Hz, 2H), 2.24 (s, 3H), 1.82 (s, 3H), 1.73-1.63 (m, 2H), 11.50 (ddd, J = 11.2, 7.4, 3.9 Hz, 1H), 1.28-1.13 (m, 2H). MS (ESI) m/z: 659 [M + H].sup.+. II-v-12 [00232] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.45 (s, 1H), 9.35 (d, J = 2.0 Hz, 1H), 8.91-8.83 (m, 2H), 8.18 (s, 1H), 8.12 (d, J = 2.5 Hz, 1H), 8.01 (td, J = 10.7, 2.2 Hz, 3H), 7.90 (dd, J = 8.1, 5.3 Hz, 1H), 7.76 (d, J = 7.8 Hz, 1H), 7.65 (d, J = 7.9 Hz, 1H), 7.56 (d, J = 8.9 Hz, 1H), 4.17 (s, 3H), 3.69 (dtd, J = 11.2, 7.1, 3.8 Hz, 1H), 2.95-2.84 (m, 2H), 2.78 (td, J = 11.6, 2.5 Hz, 2H), 2.25 (s, 3H), 2.07 (q, J = 7.6 Hz, 2H), 1.84-1.74 (m, 2H), 1.52 (qd, J = 11.4, 3.9 Hz, 2H), 0.99 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 659 [M + H].sup.+. II-v-13 [00233] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.44 (s, 1H), 8.79 (d, J = 5.4 Hz, 2H), 8.21 (s, 1H), 8.19-8.17 (m, 2H), 8.13 (d, J = 2.5 Hz, 1H), 8.01 (td, J = 10.9, 5.3 Hz, 3H), 7.85 (d, J = 7.8 Hz, 1H), 7.65 (d, J = 8.0 Hz, 1H), 7.56 (d, J = 9.0 Hz, 1H), 4.17 (s, 3H), 3.69 (dt, J = 7.7, 5.4 Hz, 1H), 2.95-2.86 (m, 2H), 2.78 (td, J = 11.5, 2.5 Hz, 2H), 2.25 (s, 3H), 1.81 (s, 5H), 1.51 (qd, J = 11.4, 3.9 Hz, 2H). MS (ESI) m/z: 645 [M + H].sup.+ II-v-14 [00234] .sup.1H NMR (600 MHz, Chloroform-d) 9.40 (s, 1H), 9.04 (s, 1H), 8.61 (s, 1H), 8.50 (d, J = 7.9 Hz, 1H), 7.88 (s, 2H), 7.87-7.80 (m, 3H), 7.40 (d, J = 7.8 Hz, 1H), 7.31 (d, J = 11.6 Hz, 1H), 7.25 (d, J = 8.6 Hz, 1H), 4.78 (d, J = 7.9 Hz, 1H), 4.13 (s, 3H), 3.40 (dt, J = 8.5, 4.2 Hz, 1H), 3.06 (q, J = 7.4 Hz, 2H), 2.97 (dt, J = 12.5, 3.9 Hz, 2H), 2.77-2.67 (m, 2H), 2.22 (s, 3H), 2.01 (dd, J = 13.0, 3.8 Hz, 2H), 1.77-1.62 (m, 2H), 1.38 (t, J = 7.3 Hz, 3H). MS (ESI) m/z: 695 [M + H].sup.+ II-v-15 [00235] .sup.1H NMR (600 MHz, Chloroform-d) 9.04 (s, 1H), 8.60 (s, 2H), 8.06 (s, 2H), 7.91 (s, 1H), 7.90-7.86 (m, 2H), 7.84 (d, J = 1.7 Hz, 1H), 7.81 (d, J = 2.5 Hz, 1H), 7.44 (d, J = 8.0 Hz, 1H), 7.24 (d, J = 8.8 Hz, 1H), 4.92 (d, J = 7.9 Hz, 1H), 4.16 (s, 3H), 3.39 (ddt, J = 14.7, 10.6, 5.4 Hz, 1H), 3.05 (q, J = 7.4 Hz, 2H), 2.96 (dd, J = 11.0, 5.4 Hz, 2H), 2.77- 2.67 (m, 2H), 2.23 (s, 3H), 2.04-1.93 (m, 2H), 1.75-1.64 (m, 2H), 1.36 (t, J = 7.4 Hz, 3H). MS (ESI) m/z: 695 [M + H].sup.+ II-v-16 [00236] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.44 (s, 1H), 9.25 (d, J = 2.1 Hz, 1H), 8.74 (dd, J = 5.0, 1.6 Hz, 1H), 8.58 (dt, J = 8.1, 1.8 Hz, 1H), 8.19 (s, 1H), 8.11 (d, J = 2.6 Hz, 1H), 8.02 (dd, J = 8.5, 2.2 Hz, 2H), 7.99 (dd, J = 7.9, 1.8 Hz, 1H), 7.80 (t, J = 5.9 Hz, 1H), 7.69-7.65 (m, 1H), 7.64 (d, J = 8.2 Hz, 1H), 7.51 (d, J = 8.8 Hz, 1H), 2.98 (t, J = 6.3 Hz, 2H), 2.94-2.87 (m, 2H), 2.67 (td, J = 11.6, 2.3 Hz, 2H), 2.25 (s, 3H), 2.09 (q, J = 7.6 Hz, 2H), 1.72-1.64 (m, 2H), 1.55-1.45 (m, 1H), 1.23 (qd, J = 12.1, 3.8 Hz, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 659 [M + H].sup.+ II-v-17 [00237] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.43 (s, 1H), 8.87-8.75 (m, 2H), 8.23 (s, 1H), 8.20-8.15 (m, 2H), 8.11 (d, J = 2.5 Hz, 1H), 8.02 (dd, J = 8.0, 2.1 Hz, 2H), 8.00 (dd, J = 7.9, 1.8 Hz, 1H), 7.79 (t, J = 5.9 Hz, 1H), 7.65 (d, J = 8.0 Hz, 1H), 7.52 (d, J = 8.8 Hz, 1H), 2.99 (t, J = 6.4 Hz, 2H), 2.94- 2.86 (m, 2H), 2.67 (td, J = 11.6, 2.4 Hz, 2H), 2.25 (s, 3H), 2.09 (q, J = 7.6 Hz, 2H), 1.69 (dd, J = 13.4, 3.6 Hz, 2H), 1.51 (ddd, J = 11.2, 7.3, 3.9 Hz, 1H). 1.24 (qd, J = 11.9, 3.9 Hz, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 659 [M + H].sup.+

TABLE-US-00003 TABLE 3 Structure and characterization of compounds III No. Structure .sup.1H NMR and/or MS data III-b-1 [00238] .sup.1H NMR (600 MHz, Chloroform-d) 9.29 (d, J = 2.0 Hz, 1H), 8.97 (s, 1H), 8.51-8.42 (m, 2H), 8.16 (s, 1H), 8.07 (d, J = 7.9 Hz, 1H), 7.82 (d, J = 2.1 Hz, 1H), 7.72 (d, J = 7.8 Hz, 1H), 7.52 (t, J = 7.8 Hz, 1H), 7.37 (dd, J = 8.3, 2.1 Hz, 1H), 7.33 (d, J = 3.1 Hz, 1H), 7.27-7.20 (m, 2H), 6.68 (d, J = 3.1 Hz, 1H), 4.17 (s, 3H), 2.19 (s, 3H). MS(ESI) m/z 504[M + H].sup.+. III-b-2 [00239] .sup.1H NMR (600 MHz, Chloroform-d) 8.34 (s, 1H), 8.15 (s, 1H), 8.10 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 7.8 Hz, 1H), 7.71 (d, J = 2.2 Hz, 1H), 7.62 (t, J = 7.8 Hz, 1H), 7.44 (dd, J = 8.3, 2.2 Hz, 1H), 7.28 (d, J = 8.5 Hz, 1H), 7.15 (d, J = 3.0 Hz, 1H), 6.40 (d, J = 3.1 Hz, 1H), 4.05 (s, 3H), 2.21 (s, 3H). MS(ESI) m/z 512[M + H].sup.+. III-b-3 [00240] .sup.1H NMR (600 MHz, Chloroform-d) 8.22 (s, 1H), 8.14 (s, 1H), 8.08 (d, J = 7.9 Hz, 1H), 7.81 (d, J = 7.8 Hz, 1H), 7.76 (d, J = 2.2 Hz, 1H), 7.62 (t, J = 7.8 Hz, 1H), 7.40 (dd, J = 8.2, 2.2 Hz, 1H), 7.29 (d, J = 1.8 Hz, 1H), 7.13 (d, J = 3.1 Hz, 1H), 6.37 (d, J = 3.0 Hz, 1H), 4.24 (d, J = 13.0 Hz, 2H), 4.05 (s, 3H), 3.56 (dtt, J = 12.6, 6.1, 3.0 Hz, 2H), 2.44 (dd, J = 13.0, 10.6 Hz, 2H), 2.22 (s, 3H), 1.13 (d, J = 6.2 Hz, 6H). MS(ESI) m/z 540[M + H].sup.+. III-e-1 [00241] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.54 (t, J = 2.4 Hz, 1H), 10.54 (s, 1H), 9.17 (s, 1H), 8.61- 8.45 (m, 1H), 8.38 (dt, J = 8.1, 2.0 Hz, 1H), 8.22 (d, J = 1.9 Hz, 1H), 8.08-8.04 (m, 1H), 8.03 (d, J = 1.8 Hz, 1H), 7.97 (dd, J = 7.9, 1.8 Hz, 1H), 7.91 (t, J = 3.0 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.48-7.43 (m, 1H), 7.41 (dd, J = 8.0, 4.7 Hz, 1H), 6.77 (dd, J = 3.0, 1.8 Hz, 1H), 2.28 (s, 3H). MS(ESI) m/z 490[M + H].sup.+. III-e-2 [00242] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.61 (t, J = 2.3 Hz, 1H), 10.54 (s, 1H), 8.60 (s, 2H), 8.22 (d, J = 1.9 Hz, 1H), 8.10-8.05 (m, 1H), 8.04 (d, J = 1.8 Hz, 1H), 7.98 (dd, J = 8.0, 1.9 Hz, 1H), 7.95 (q, J = 3.3 Hz, 3H), 7.64 (d, J = 8.0 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.48-7.42 (m, 1H), 6.81 (dd, J = 3.0, 1.8 Hz, 1H), 2.28 (s, 3H). MS(ESI) m/z 490[M + H].sup.+. III-e-3 [00243] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 9.15 (dd, J = 2.2, 0.8 Hz, 1H), 8.56 (dd, J = 4.8, 1.7 Hz, 1H), 8.38 (dt, J = 8.0, 1.9 Hz, 1H), 8.23 (d, J = 1.9 Hz, 1H), 8.12-8.03 (m, 2H), 7.97 (dd, J = 7.9, 1.8 Hz, 1H), 7.89 (d, J = 3.0 Hz, 1H), 7.63 (dd, J = 7.9, 0.8 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.47-7.41 (m, 2H), 6.73 (d, J = 3.2 Hz, 1H), 4.21 (s, 3H), 2.31 (s, 3H). MS(ESI) m/z 504[M + H].sup.+. III-e-4 [00244] .sup.1H NMR (600 MHz, Chloroform-d) 8.67 (s, 1H), 8.54 (d, J = 5.2 Hz, 2H), 8.01 (s, 1H), 7.98 (d, J = 5.0 Hz, 2H), 7.90-7.84 (m, 3H), 7.50 (d, J = 7.9 Hz, 1H), 7.47 (t, J = 8.0 Hz, 1H), 7.42 (d, J = 3.1 Hz, 1H), 7.40 (dd, J = 8.0, 1.4 Hz, 1H), 6.76 (d, J = 3.1 Hz, 1H), 4.19 (s, 3H), 2.31 (s, 3H). MS(ESI) m/z 504[M + H].sup.+. III-e-5 [00245] .sup.1H NMR (600 MHz, Chloroform-d) 8.34-8.28 (m, 1H), 7.97 (d, J = 2.0 Hz, 1H), 7.90 (dd, J = 8.3, 2.0 Hz, 1H), 7.78 (d, J = 1.8 Hz, 1H), 7.75 (dd, J = 7.9, 1.9 Hz, 1H), 7.48 (t, J = 8.0 Hz, 1H), 7.42 (dd, J = 12.7, 7.8 Hz, 2H), 7.16 (d, J = 3.0 Hz, 1H), 6.36 (d, J = 3.0 Hz, 1H), 4.05 (s, 3H), 3.65 (t, J = 4.8 Hz, 4H), 3.48 (t, J = 4.8 Hz, 4H), 2.30 (s, 3H). MS(ESI) m/z 512[M + H].sup.+. III-e-6 [00246] .sup.1H NMR (600 MHz, Chloroform-d) 8.34 (s, 1H), 8.15 (s, 1H), 8.10 (d, J = 7.9 Hz, 1H), 7.80 (d, J = 7.8 Hz, 1H), 7.71 (d, J = 2.2 Hz, 1H), 7.62 (t, J = 7.8 Hz, 1H), 7.44 (dd, J = 8.3, 2.2 Hz, 1H), 7.28 (d, J = 8.5 Hz, 1H), 7.15 (d, J = 3.0 Hz, 1H), 6.40 (d, J = 3.1 Hz, 1H), 4.05 (s, 3H), 2.21 (s, 3H). MS(ESI) m/z 512[M + H].sup.+. III-h-1 [00247] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.62 (s, 1H), 10.70 (s, 1H), 9.35 (d, J = 2.0 Hz, 1H), 8.84-8.81 (m, 1H), 8.77 (dd, J = 5.2, 1.5 Hz, 1H), 8.30 (d, J = 1.8 Hz, 1H), 8.27 (dd, J = 8.2, 1.8 Hz, 1H), 7.97 (t, J = 2.2 Hz, 1H), 7.95-7.92 (m, 2H), 7.80 (dd, J = 8.1, 5.2 Hz, 1H), 7.72 (dd, J = 8.3, 1.9 Hz, 1H), 7.55 (t, J = 8.2 Hz, 1H), 7.25-7.23 (m, 1H), 6.80 (dd, J = 3.0, 1.8 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.07 (t, J = 12.1 Hz, 2H), 2.93 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.44 (t, J = 12.5 Hz, 2H). MS (ESI) m/z 588 [M + H].sup.+. III-h-2 [00248] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.79 (s, 1H), 10.74 (s, 1H), 8.86 (d, J = 5.9 Hz, 2H), 8.43 (d, J = 5.9 Hz, 2H), 8.30 (d, J = 1.7 Hz, 1H), 8.27 (dd, J = 8.1, 1.8 Hz, 1H), 8.01 (t, J = 2.9 Hz, 1H), 7.97 (t, J = 2.2 Hz, 1H), 7.93 (d, J = 8.1 Hz, 1H), 7.74 (dd, J = 8.2, 1.8 Hz, 1H), 7.56 (t, J = 8.2 Hz, 1H), 7.28-7.23 (m, 1H), 6.87 (q, J = 3.1, 1.8 Hz, 1H), 3.79 (s, 3H), 3.42 (d, J = 11.7 Hz, 2H), 3.07 (t, J = 12.1 Hz, 2H), 2.92 (d, J = 12.7 Hz, 2H), 2.81 (s, 3H), 2.43 (t, J = 12.3 Hz, 2H). MS (ESI) m/z 588 [M + H].sup.+. III-h-3 [00249] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.70 (s, 1H), 9.33 (s, 1H), 8.79 (d, J = 8.3 Hz, 1H), 8.76 (d, J = 5.1 Hz, 1H), 8.31 (s, 1H), 8.27 (d, J = 8.6 Hz, 1H), 8.00 (t, J = 2.2 Hz, 1H), 7.94-7.91 (m, 2H), 7.78 (dd, J = 8.1, 5.2 Hz, 1H), 7.71 (dd, J = 8.5, 1.9 Hz, 1H), 7.55 (t, J = 8.1 Hz, 1H), 7.27-7.24 (m, 1H), 6.76 (d, J = 3.1 Hz, 1H), 4.17 (s, 3H), 3.80 (s, 2H), 3.42 (d, J = 12.1 Hz, 2H), 3.07 (t, J = 11.9 Hz, 2H), 2.93 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.43 (t, J = 12.2 Hz, 2H). MS (ESI) m/z 602 [M + H].sup.+. III-h-4 [00250] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.72 (s, 1H), 8.85-8.82 (m, 2H), 8.41-8.39 (m, 2H), 8.31 (d, J = 1.8 Hz, 1H), 8.27 (dd, J = 8.1, 1.8 Hz, 1H), 8.00 (t, J = 2.2 Hz, 1H), 7.97 (d, J = 3.1 Hz, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.73 (dd, J = 7.8, 1.9 Hz, 1H), 7.55 (t, J = 8.1 Hz, 1H), 7.27-7.24 (m, 1H), 6.83 (d, J = 3.1 Hz, 1H), 4.19 (s, 3H), 3.79 (s, 2H), 3.42 (d, J = 12.1 Hz, 2H), 3.07 (t, J = 12.0 Hz, 2H), 2.92 (d, J = 12.6 Hz, 2H), 2.82 (s, 3H), 2.44 (t, J = 12.3 Hz, 2H). MS (ESI) m/z 602 [M + H].sup.+. III-i-1 [00251] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.68 (s, 1H), 10.64 (s, 1H), 9.30 (d, J = 2.0 Hz, 1H), 8.77 (t, 2H), 8.29 (s, 1H), 8.25 (d, J = 8.7 Hz, 1H), 7.96 (t, J = 3.0 Hz, 1H), 7.92 (d, J = 8.2 Hz, 1H), 7.89 (d, J = 2.1 Hz, 1H), 7.81 (dd, J = 8.1, 5.2 Hz, 1H), 7.66 (dd, J = 8.4, 2.2 Hz, 1H), 7.44 (d, J = 8.4 Hz, 1H), 6.81 (dd, J = 3.0, 1.9 Hz, 1H), 3.79 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.06 (t, J = 11.9 Hz, 2H), 2.92 (d, J = 12.3 Hz, 2H), 2.81 (s, 3H), 2.43 (t, J = 12.4 Hz, 2H), 2.18 (s, 3H). MS (ESI) m/z 602 [M + H].sup.+. III-i-2 [00252] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.83 (s, 1H), 10.65 (s, 1H), 8.86 (d, J = 6.7 Hz, 2H), 8.40 (d, J = 6.8 Hz, 2H), 8.29 (s, 1H), 8.25 (dd, J = 8.1, 1.8 Hz, 1H), 8.02 (t, J = 3.0 Hz, 1H), 7.92 (d, J = 8.2 Hz, 1H), 7.88 (d, J = 2.0 Hz, 1H), 7.68 (dd, J = 8.3, 2.1 Hz, 1H), 7.44 (d, J = 8.4 Hz, 1H), 6.88-6.87 (m, 1H), 3.78 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.06 (t, J = 12.1 Hz, 2H), 2.92 (d, J = 12.8 Hz, 2H), 2.81 (s, 3H), 2.42 (t, J = 12.2 Hz, 2H), 2.17 (s, 3H). MS (ESI) m/z 602 [M + H].sup.+. III-i-3 [00253] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.62 (s, 1H), 9.26 (d, J = 1.9 Hz, 1H), 8.75-8.68 (m, 2H), 8.29 (d, J = 1.8 Hz, 1H), 8.25 (dd, J = 8.1, 1.8 Hz, 1H), 7.94-7.90 (m, 3H), 7.73 (dd, J = 8.1, 5.1 Hz, 1H), 7.64 (dd, J = 8.3, 2.2 Hz, 1H), 7.43 (d, J = 8.5 Hz, 1H), 6.76 (d, J = 3.1 Hz, 1H), 4.20 (s, 3H), 3.79 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.07 (t, J = 11.9 Hz, 2H), 2.92 (d, J = 12.6 Hz, 2H), 2.81 (s, 3H), 2.43 (t, J = 12.5 Hz, 2H), 2.20 (s, 3H). MS (ESI) m/z 616 [M + H].sup.+. III-i-4 [00254] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.64 (s, 1H), 8.80 (d, J = 6.6 Hz, 2H), 8.30 (d, J = 6.6 Hz, 3H), 8.25 (dd, J = 8.0, 1.9 Hz, 1H), 7.97 (d, J = 3.0 Hz, 1H), 7.93-7.91 (m, 2H), 7.66 (dd, J = 8.3, 2.1 Hz, 1H), 7.43 (d, J = 8.4 Hz, 1H), 6.82 (d, J = 3.0 Hz, 1H), 4.21 (s, 3H), 3.78 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.06 (t, J = 11.9 Hz, 2H), 2.92 (d, J = 12.8 Hz, 2H), 2.81 (s, 3H), 2.43 (t, J = 12.2 Hz, 2H), 2.20 (s, 3H). MS (ESI) m/z 616 [M + H].sup.+. III-j-1 [00255] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.63 (s, 1H), 10.30 (s, 1H), 9.40 (s, 1H), 8.89 (d, J = 8.1 Hz, 1H), 8.79 (d, J = 5.2 Hz, 1H), 8.34 (s, 1H), 8.30 (d, J = 8.7 Hz, 1H), 7.94-7.92 (m, 2H), 7.83 (t, 1H), 7.51 (d, J = 2.5 Hz, 1H), 7.45 (d, J = 8.4 Hz, 1H), 7.31 (q, J = 8.3, 2.5 Hz, 1H), 6.79 (dd, J = 3.0 1.8 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 12.1 Hz, 2H), 3.07 (s, 2H), 2.93 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.46-2.41 (m, 2H), 2.34 (s, 3H). MS (ESI) m/z 602 [M + H].sup.+. III-j-2 [00256] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.80 (s, 1H), 10.32 (s, 1H), 8.90 (d, J = 5.9 Hz, 2H), 8.55 (d, J = 6.4 Hz, 2H), 8.33 (s, 1H), 8.30 (d, J = 8.6 Hz, 1H), 8.00 (t, J = 2.9 Hz, 1H), 7.94 (d, J = 8.2 Hz, 1H), 7.51 (d, J = 2.4 Hz, 1H), 7.46 (d, J = 8.4 Hz, 1H), 7.32 (dd, J = 8.3, 2.5 Hz, 1H), 6.86 (dd, J = 3.0, 1.8 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 12.0 Hz, 2H), 3.08 (t, 2H), 2.93 (d, J = 12.5 Hz, 2H), 2.81 (s, 3H), 2.44 (t, J = 12.2 Hz, 2H), 2.34 (s, 3H). MS (ESI) m/z 602 [M + H].sup.+. III-j-3 [00257] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.35 (s, 1H), 10.28 (s, 1H), 8.32 (s, 1H), 8.30 (d, J = 8.2 Hz, 1H), 8.22-8.20 (m, 2H), 7.93 (d, J = 8.3 Hz, 1H), 7.83 (t, J = 2.8 Hz, 1H), 7.45 (dd, J = 8.4, 5.6 Hz, 2H), 7.39 (dd, J = 5.3, 3.4 Hz, 3H), 7.29 (d, J = 2.5 Hz, 1H), 6.70 (dd, J = 3.0, 1.5 Hz, 1H), 3.77 (s, 2H), 2.65 (s, 3H), 2.33 (s, 3H). MS (ESI) m/z 601[M + H].sup.+. III-j-4 [00258] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.30 (s, 1H), 10.21 (s, 1H), 8.29 (s, 1H), 8.26 (d, J = 8.2 Hz, 1H), 8.01 (dd, J = 3.1, 1.2 Hz, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.80 (t, J = 2.9 Hz, 1H), 7.64 (dd, J = 5.0, 1.2 Hz, 1H), 7.53 (dd, J = 5.0, 3.1 Hz, 1H), 7.46 (d, J = 2.5 Hz, 1H), 7.42 (d, J = 8.7 Hz, 1H), 7.25 (dd, J = 8.3, 2.5 Hz, 1H), 6.66 (dd, J = 3.0, 1.8 Hz, 1H), 3.68 (s, 2H), 2.32 (s, 3H), 2.19 (s, 3H). MS (ESI) m/z 607[M + H].sup.+. III-j-5 [00259] MS (ESI) m/z 616 [M + H].sup.+. III-j-6 [00260] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.33 (s, 1H), 8.89 (d, J = 6.8 Hz, 2H), 8.51 (d, J = 6.7 Hz, 2H), 8.34 (s, 1H), 8.31 (dd, J = 8.2, 1.8 Hz, 1H), 7.97- 7.92 (m, 2H), 7.54 (d, J = 2.6 Hz, 1H), 7.46 (d, J = 8.4 Hz, 1H), 7.34 (dd, J = 8.3, 2.5 Hz, 1H), 6.82 (d, J = 3.1 Hz, 1H), 4.18 (s, 3H), 3.80 (s, 2H), 3.43 (d, J = 11.9 Hz, 2H), 3.07 (s, 2H), 2.93 (d, J = 12.2 Hz, 2H), 2.82 (s, 3H), 2.45 (s, 2H), 2.34 (s, 3H). MS (ESI) m/z 616 [M + H].sup.+. III-j-7 [00261] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.24 (s, 1H), 8.30 (s, 1H), 8.27 (d, J = 7.8 Hz, 1H), 8.20 (d, J = 5.0 Hz, 2H), 7.93 (d, J = 7.8 Hz, 1H), 7.79 (s, 1H), 7.50 (s, 1H), 7.44 (d, J = 7.9 Hz, 1H), 7.39 (s, 3H), 7.30 (d, J = 7.0 Hz, 1H), 6.66 (s, 1H), 4.13 (s, 3H), 3.68 (s, 2H), 2.33 (s, 3H), 2.18 (s, 3H). MS (ESI) m/z 615[M + H].sup.+. III-j-8 [00262] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.23 (s, 1H), 8.29 (s, 1H), 8.26 (d, J = 8.1 Hz, 1H), 8.01 (dd, J = 3.1, 1.1 Hz, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.77 (d, J = 3.0 Hz, 1H), 7.63 (dd, J = 5.0, 1.1 Hz, 1H), 7.53 (dd, J = 5.0, 3.1 Hz, 1H), 7.49 (d, J = 2.4 Hz, 1H), 7.42 (d, J = 8.4 Hz, 1H), 7.28 (dd, J = 8.3, 2.5 Hz, 1H), 6.62 (d, J = 3.0 Hz, 1H), 4.12 (s, 3H), 3.68 (s, 2H), 2.32 (s, 3H), 2.17 (s, 3H). MS (ESI) m/z 621[M + H].sup.+. III-j-9 [00263] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.28 (s, 1H), 10.20 (s, 1H), 8.28 (s, 1H), 8.26 (d, J = 8.2 Hz, 1H), 8.09-8.07 (m, 1H), 7.93 (d, J = 8.1 Hz, 1H), 7.78 (t, J = 2.9 Hz, 1H), 7.68 (t, J = 1.7 Hz, 1H), 7.46 (d, J = 2.4 Hz, 1H), 7.41 (d, J = 8.4 Hz, 1H), 7.23 (dd, J = 8.3, 2.5 Hz, 1H), 6.89=6.87 (m, 1H), 6.63 (dd, J = 2.9, 1.8 Hz, 1H), 3.68 (s, 2H), 2.31 (s, 3H), 2.18 (s, 3H). MS (ESI) m/z: 589[M + H].sup.+ III-j-10 [00264] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.22 (s, 1H), 8.29 (s, 1H), 8.26 (d, J = 8.1 Hz, 1H), 8.08 (d, J = 0.7 Hz, 1H), 7.93 (d, J = 8.1 Hz, 1H), 7.76 (d, J = 3.0 Hz, 1H), 7.68 (d, J = 1.6 Hz, 1H), 7.49 (d, J = 2.4 Hz, 1H), 7.41 (d, J = 8.4 Hz, 1H), 7.26 (dd, J = 8.3, 2.4 Hz, 1H), 6.87 (d, J = 1.0 Hz, 1H), 6.58 (d, J = 3.0 Hz, 1H), 4.11 (s, 3H), 3.68 (s, 2H), 2.31 (s, 3H). 2.18 (s, 3H). MS (ESI) m/z: 605[M + H].sup.+ III-j-11 [00265] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.39 (s, 1H), 10.20 (s, 1H), 8.29 (s, 1H), 8.26 (d, J = 8.1 Hz, 1H), 8.21 (d, J = 8.5 Hz, 2H), 7.93 (d, J = 8.2 Hz, 1H), 7.84 (s, 1H), 7.48 (d, J = 2.3 Hz, 1H), 7.46 (d, J = 8.5 Hz, 2H), 7.43 (d, J = 8.4 Hz, 1H), 7.27 (dd, J = 8.3, 2.4 Hz, 1H), 6.71 (d, J = 2.7 Hz, 1H), 3.68 (s, 2H), 2.33 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 636[M + H].sup.+ III-j-12 [00266] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.23 (s, 1H), 8.30 (s, 1H), 8.27 (d, J = 8.6 Hz, 1H), 8.21-8.18 (m, 2H), 7.93 (d, J = 8.1 Hz, 1H), 7.81 (d, J = 3.0 Hz, 1H), 7.49 (d, J = 2.4 Hz, 1H), 7.46-7.44 (m, 2H), 7.43 (d, J = 8.5 Hz, 1H), 7.29 (dd, J = 8.3, 2.5 Hz, 1H), 2.32 (s, 3H), 2.19 (s, 3H). MS (ESI) m/z: 650[M + H].sup.+ III-j-13 [00267] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.75 (d, J = 14.7 Hz, 1H), 10.27 (d, J = 9.5 Hz, 1H), 8.30 (d, J = 6.4 Hz, 1H), 8.26 (d, 1H), 8.02-7.98 (m, 2H), 7.93 (dd, J = 7.3, 4.4 Hz, 2H), 7.48-7.44 (m, 2H), 7.28 (dd, J = 8.3, 2.5 Hz, 1H), 6.85-6.81 (m, 2H), 6.70 (dt, J = 7.8, 3.9 Hz, 1H), 3.79 (s, 2H), 3.40 (s, 2H), 3.04 (d, J = 27.6 Hz, 2H), 2.89 (m, 2H), 2.80 (s, 3H), 2.39 (t, 2H), 2.32 (s, 3H). MS (ESI) m/z: 617[M + H].sup.+ III-j-14 [00268] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.23 (s, 1H), 9.70 (s, 1H), 8.30 (s, 1H), 8.26 (d, J = 8.1 Hz, 1H), 8.02 (t, J = 5.7 Hz, 2H), 7.93 (d, J = 8.2 Hz, 1H), 7.73 (d, J = 3.0 Hz, 1H), 7.46 (d, J = 2.4 Hz, 1H), 7.42 (d, J = 8.4 Hz, 1H), 7.28 (dd, J = 8.3, 2.5 Hz, 1H), 6.76 (d, J = 8.7 Hz, 2H), 6.58 (d, J = 3.0 Hz, 1H), 4.10 (s, 3H), 3.68 (s, 2H), 2.32 (s, 3H), 2.19 (s, 3H). MS (ESI) m/z: 631[M + H].sup.+ III-j-15 [00269] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.07 (d, J = 25.0 Hz, 1H), 10.22 (s, 1H), 8.27 (s, 1H), 8.24 (d, J = 8.0 Hz, 1H), 7.91 (d, J = 8.1 Hz, 1H), 7.88 (d, J = 8.7 Hz, 2H), 7.70 (t, J = 2.8 Hz, 1H), 7.43-7.40 (m, 2H), 7.23 (dd, J = 8.3, 2.5 Hz, 1H), 6.57 (dd, J = 2.9, 1.6 Hz, 1H), 6.53 (d, J = 8.7 Hz, 2H), 3.80-3.75 (m, 2H), 3.67 (s, 2H), 2.31 (s, 3H), 2.18 (s, 3H). MS (ESI) m/z: 616[M + H].sup.+ III-j-16 [00270] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.31 (s, 1H), 8.31 (s, 1H), 8.27 (d, J = 8.0 Hz, 1H), 7.93 (t, J = 6.3 Hz, 1H), 7.91 (d, J = 8.8 Hz, 2H), 7.88 (d, J = 3.0 Hz, 1H), 7.48 (d, J = 2.5 Hz, 1H), 7.46 (d, J = 8.6 Hz, 1H), 7.31 (dd, J = 8.3, 2.5 Hz, 1H), 6.74 (d, J = 8.8 Hz, 2H), 6.63 (d, J = 3.0 Hz, 1H), 4.13 (s, 3H), 3.79 (s, 2H), 3.40 (s, 2H), 3.06 (s, 2H), 2.92 (s, 2H), 2.80 (s, 3H), 2.43 (s, 2H), 2.32 (s, 3H). MS (ESI) m/z: 631[M + H].sup.+ III-j-17 [00271] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.28 (s, 1H), 8.31 (s, 1H), 8.27 (d, J = 8.1 Hz, 1H), 8.25 (d, J = 2.9 Hz, 1H), 7.94 (d, J = 8.2 Hz, 1H), 7.49 (d, J = 2.2 Hz, 1H), 7.47 (d, J = 8.6 Hz, 1H), 7.26 (dd, J = 8.3, 2.3 Hz, 1H), 7.00 (d, J = 2.9 Hz, 1H), 6.52 (s, 1H), 4.23 (s, 3H), 3.79 (s, 2H), 3.17 (s, 1H), 3.07 (s, 2H), 2.93 (d, J = 12.3 Hz, 2H), 2.82 (s, 3H), 2.46-2.38 (m, 4H), 2.31 (s, 3H). MS (ESI) m/z: 594 [M + H].sup.+ III-j-18 [00272] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.22 (d, J = 6.8 Hz, 1H), 8.27 (s, 1H), 8.25 (d, J = 6.7 Hz, 1H), 8.22 (t, J = 7.2 Hz, 1H), 7.91 (t, J = 7.4 Hz, 1H), 7.75 (t, J = 5.4 Hz, 1H), 7.38 (d, J = 8.4 Hz, 1H), 7.32 (d, J = 2.4 Hz, 1H), 7.15 (dd, 1H), 6.59 (d, J = 3.1 Hz, 1H), 4.10 (s, 3H), 3.67 (s, 2H), 2.26 (s, 3H), 2.18 (s, 3H). MS (ESI) m/z: 539 [M + H].sup.+ III-k-1 [00273] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.50 (s, 1H), 10.47 (s, 1H), 9.30 (d, J = 1.5 Hz, 1H), 8.59 (dd, J = 4.7, 1.7 Hz, 1H), 8.50 (dt, J = 8.0, 1.9 Hz, 1H), 8.32 (s, 1H), 8.27 (d, J = 8.1 Hz, 1H), 7.94 (d, J = 8.2 Hz, 1H), 7.90 (t, J = 2.9 Hz, 1H), 7.74 (t, J = 5.3 Hz, 2H), 7.48-7.44 (m, 2H), 6.76 (dd, J = 2.9, 1.8 Hz, 1H), 3.71 (s, 2H), 2.36 (s, 3H). MS (ESI) m/z: 623[M + H].sup.+ III-k-2 [00274] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.72 (s, 1H), 10.52 (s, 1H), 8.80 (d, J = 4.8 Hz, 2H), 8.37 (d, J = 6.0 Hz, 2H), 8.35 (d, J = 1.5 Hz, 1H), 8.32- 8.29 (m, 1H), 7.99 (t, J = 2.9 Hz, 1H), 7.95 (d, J = 8.2 Hz, 1H), 7.76 (dd, J = 7.5, 5.8 Hz, 2H), 7.48 (dd, J = 8.8, 2.8 Hz, 1H), 6.85 (dd, J = 3.0, 1.8 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 11.6 Hz, 2H), 3.07 (t, J = 11.2 Hz, 2H), 2.93 (d, J = 12.4 Hz, 2H), 2.82 (s, 3H), 2.47-2.38 (m, 2H). MS (ESI) m/z: 623[M + H].sup.+ III-k-3 [00275] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 9.33 (s, 1H), 8.70-8.65 (m, 2H), 8.36 (d, J = 1.5 Hz, 1H), 8.30 (dd, J = 8.1, 1.5 Hz, 1H), 7.95 (d, J = 8.2 Hz, 1H), 7.89 (d, J = 3.1 Hz, 1H), 7.78- 7.74 (m, 2H), 7.63 (dd, J = 7.6, 5.2 Hz, 1H), 7.49 (dd, J = 8.8, 2.8 Hz, 1H), 6.74 (d, J = 3.1 Hz, 1H), 4.16 (s, 3H), 3.42 (d, J = 12.2 Hz, 2H), 3.07 (t, J = 11.2 Hz, 2H), 2.93 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.42 (t, J = 22.0, 10.4 Hz, 2H). MS (ESI) m/z: 637[M + H].sup.+ III-k-4 [00276] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 8.82 (d, J = 5.0 Hz, 2H), 8.39 (d, J = 5.9 Hz, 2H), 8.36 (d, J = 1.5 Hz, 1H), 8.31 (dd, J = 8.1, 1.5 Hz, 1H), 7.97-7.94 (m, 2H), 7.80 (d, J = 2.8 Hz, 1H), 7.76 (d, J = 8.8 Hz, 1H), 7.50 (dd, J = 8.8, 2.8 Hz, 1H), 6.81 (d, J = 3.1 Hz, 1H), 4.18 (s, 3H), 3.42 (d, J = 11.2 Hz, 2H), 3.07 (t, J = 11.1 Hz, 2H), 2.93 (d, J = 11.8 Hz, 2), 2.82 (s, 3H), 2.44 (t, J = 11.5 Hz, 2H). MS (ESI) m/z: 637[M + H].sup.+ III-k-5 [00277] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.38 (s, 1H), 10.49 (s, 1H), 8.34 (d, J = 1.3 Hz, 1H), 8.31-8.27 (m, 1H), 8.12 (dd, J = 1.5, 0.6 Hz, 1H), 7.95 (d, J = 8.2 Hz, 1H), 7.83 (t, J = 2.9 Hz, 1H), 7.72- 7.69 (m, 3H), 7.40 (dd, 1H), 6.90 (dd, J = 1.8, 0.6 Hz, 1H), 6.65 (dd, J = 3.0, 1.9 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 11.9 Hz, 2H), 3.07 (t, J = 11.1 Hz, 2H), 2.93 (d, J = 12.5 Hz, 2H), 2.82 (s, 3H), 2.43 (t, J = 11.8 Hz, 2H), MS (ESI) m/z: 612[M + H].sup.+ III-k-6 [00278] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.46 (s, 1H), 8.31 (d, J = 1.2 Hz, 1H), 8.26 (d, J = 8.1 Hz, 1H), 8.11-8.09 (m, 1H), 7.95 (d, J = 8.2 Hz, 1H), 7.78 (d, J = 3.0 Hz, 1H), 7.74 (d, J = 2.8 Hz, 1H), 7.72-7.69 (m, 2H), 7.43 (dd, 1H), 6.88-6.87 (m, 1H), 6.60 (d, J = 3.0 Hz, 1H), 4.11 (s, 3H), 3.69 (s, 2H), 2.17 (s, 3H). MS (ESI) m/z: 626[M + H].sup.+ III-k-7 [00279] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.34 (s, 1H), 10.45 (s, 1H), 8.30 (d, J = 1.3 Hz, 1H), 8.28-8.25 (m, 1H), 8.03 (dd, J = 3.1, 1.2 Hz, 1H), 7.95 (d, J = 8.2 Hz, 1H), 7.82 (t, J = 2.9 Hz, 1H), 7.74- 7.70 (m, 2H), 7.66 (dd, J = 5.0, 1.1 Hz, 1H), 7.54 (dd, J = 5.0, 3.1 Hz, 1H), 7.42 (dd, J = 8.8, 2.8 Hz, 1H), 6.68 (dd, J = 3.0, 1.7 Hz, 1H), 3.69 (s, 2H), 2.18 (s, 3H). MS (ESI) m/z: 628 [M + H].sup.+ III-k-8 [00280] .sup.1H NMR (600 MHz, MeOH) 8.35 (s, 2H), 8.26 (d, J = 8.2 Hz, 1H), 8.05-8.01 (m, 2H), 7.91 (d, J = 3.0 Hz, 1H), 7.76-7.72 (m, 2H), 7.58 (dt, J = 8.0, 4.0 Hz, 1H), 7.41 (dd, J = 8.8, 2.7 Hz, 1H), 6.75 (d, J = 3.0 Hz, 1H), 4.27 (s, 3H), 3.90 (s, 2H), 3.51 (s, 2H), 3.21 (s, 2H), 3.06 (d, J = 7.9 Hz, 2H), 2.93 (s, 3H), 2.56 (s, 2H). MS (ESI) m/z: 642[M + H].sup.+ III-k-9 [00281] .sup.1H NMR (600 MHz, MeOH) 8.35 (d, J = 1.4 Hz, 1H), 8.26 (dd, J = 8.1, 1.5 Hz, 1H), 8.05-8.01 (m, 5H), 7.74 (d, 1H), 7.41 (dd, J = 8.8, 2.8 Hz, 1H), 6.94-6.90 (m, 2H), 6.83 (d, J = 3.0 Hz, 1H), 3.89 (s, 2H), 3.51 (s, 2H), 3.21 (d J = 5.7 Hz, 2H), 3.05 (s, 2H), 2.93 (s, 3H), 2.57 (s, 2H). MS (ESI) m/z: 638[M + H].sup.+ III-k-10 [00282] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.47 (s, 1H), 9.73 (s, 1H), 8.31 (d, J = 1.2 Hz, 1H), 8.27 (d, J = 8.1 Hz, 1H), 8.05-8.00 (m, 2H), 7.95 (d, J = 8.2 Hz, 1H), 7.76 (d, J = 3.0 Hz, 1H), 7.72 (dd, J = 5.8, 2.9 Hz, 2H), 7.44 (dd, J = 8.8, 2.8 Hz, 1H), 6.79-6.75 (m, 2H), 6.60 (d, J = 3.0 Hz, 1H), 4.11 (s, 3H), 3.70 (s, 2H), 2.23 (s, 3H). MS (ESI) m/z: 662[M + H].sup.+ III-k-11 [00283] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.15 (s, 1H), 10.44 (s, 1H), 8.30 (s, 1H), 8.26 (d, J = 8.1 Hz, 1H), 7.94 (d, J = 8.2 Hz, 1H), 7.89 (d, J = 8.6 Hz, 2H), 7.74 (t, J = 2.9 Hz, 1H), 7.71 (d, J = 8.8 Hz, 1H), 7.68 (d, J = 2.8 Hz, 1H), 7.40 (dd, J = 8.8, 2.8 Hz, 1H), 6.59 (dd, J = 2.8, 1.8 Hz, 1H), 6.54 (d, J = 8.6 Hz, 2H), 5.38 (s, 2H), 3.68 (s, 2H), 2.17 (s, 3H). MS (ESI) m/z: 637[M + H].sup.+ III-k-12 [00284] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.44 (s, 1H), 8.26 (d, J = 28.6 Hz, 2H), 7.96-7.83 (m, 3H), 7.73-7.65 (m, 3H), 7.52 (d, J = 33.2 Hz, 1H), 7.41 (s, 1H), 4.07 (s, 2H), 2.51 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 651[M + H].sup.+ III-k-13 [00285] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.45 (s, 1H), 10.50 (s, 1H), 8.35 (s, 1H), 8.29 (d, J = 8.1 Hz, 1H), 8.22 (d, J = 8.6 Hz, 2H), 7.95 (d, J = 8.2 Hz, 1H), 7.87 (t, J = 2.9 Hz, 1H), 7.74-7.71 (m, 2H), 7.47 (d, J = 8.6 Hz, 2H), 7.44 (dd, J = 8.8, 2.8 Hz, 1H), 6.72 (dd, J = 2.9, 1.9 Hz, 1H), 3.80 (s, 2H), 3.42 (d, J = 11.6 Hz, 2H), 3.07 (t, J = 11.0 Hz, 2H), 2.93 (d, J = 12.3 Hz, 2H), 2.81 (s, 3H), 2.43 (t, J = 11.8 Hz, 2H). MS (ESI) m/z: 656[M + H].sup.+ III-k-14 [00286] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.47 (s, 1H), 8.32 (s, 1H), 8.27 (d, J = 8.1 Hz, 1H), 8.22-8.18 (m, 2H), 7.95 (d, J = 8.2 Hz, 1H), 7.83 (d, J = 3.0 Hz, 1H), 7.76 (d, J = 2.7 Hz, 1H), 7.73 (d, J = 8.8 Hz, 1H), 7.48-7.44 (m, 3H), 6.68 (d, J = 3.0 Hz, 1H), 4.13 (s, 3H), 3.70 (s, 2H), 2.26 (s, 3H). MS (ESI) m/z: 670[M + H].sup.+ III-k-15 [00287] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.45 (s, 1H), 10.51 (s, 1H), 8.32 (s, 1H), 8.27 (d, J = 8.1 Hz, 1H), 8.07 (d, J = 8.1 Hz, 2H), 7.94 (d, J = 8.2 Hz, 1H), 7.85 (t, J = 2.8 Hz, 1H), 7.72 (t, J = 5.9 Hz, 2H), 7.42 (dd, J = 8.7, 2.8 Hz, 1H), 7.22 (d, J = 8.1 Hz, 2H), 6.70 (t, 1H), 3.79 (s, 2H), 3.39 (s, 2H), 3.06 (s, 2H), 2.91 (s, 2H), 2.80 (s, 3H), 2.43 (s, 2H), 2.32 (s, 3H). MS (ESI) m/z: 636[M + H].sup.+ III-k-16 [00288] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.51 (s, 1H), 8.36 (d, J = 1.3 Hz, 1H), 8.31-8.28 (m, 1H), 8.08 (d, J = 8.2 Hz, 2H), 7.95 (d, J = 8.2 Hz, 1H), 7.82 (d, J = 3.0 Hz, 1H), 7.75-7.72 (m, 2H), 7.46 (dd, J = 8.8, 2.8 Hz, 1H), 7.22 (d, J = 8.0 Hz, 2H), 6.65 (d, J = 3.0 Hz, 1H), 4.13 (s, 3H), 3.80 (s, 2H), 3.42 (d, J = 11.9 Hz, 2H), 3.07 (t, J = 11.2 Hz, 2H), 2.94 (d, J = 12.4 Hz, 2H), 2.82 (s, 3H), 2.43 (t, J = 11.8 Hz, 2H), 2.32 (s, 3H). MS (ESI) m/z: 650[M + H].sup.+ III-k-17 [00289] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.40 (s, 1H), 10.50 (s, 1H), 8.32 (s, 1H), 8.27 (d, J = 8.1 Hz, 1H), 8.21-8.18 (m, 2H), 7.94 (d, J = 8.2 Hz, 1H), 7.84 (t, J = 2.9 Hz, 1H), 7.73 (d, J = 8.8 Hz, 1H), 7.70 (d, J = 2.8 Hz, 1H), 7.44-7.39 (m, 4H), 6.72 (dd, J = 2.9, 1.9 Hz, 1H), 3.78 (s, 2H), 3.39 (d, J = 11.4 Hz, 2H), 3.05 (d, J = 10.5 Hz, 2H), 2.92 (d, J = 10.9 Hz, 2H), 2.80 (s, 3H), 2.42 (t, J = 11.8 Hz, 2H). MS (ESI) m/z: 622[M + H].sup.+ III-k-18 [00290] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.40 (s, 1H), 8.29 (s, 1H), 8.24 (d, J = 8.1 Hz, 1H), 8.18 (dd, J = 7.6, 1.9 Hz, 2H), 7.92 (d, J = 8.1 Hz, 1H), 7.77 (d, J = 3.0 Hz, 1H), 7.74 (d, J = 2.7 Hz, 1H), 7.71 (d, J = 8.8 Hz, 1H), 7.44 (dd, J = 8.8, 2.8 Hz, 1H), 7.41-7.37 (m, 3H), 6.66 (d, J = 3.0 Hz, 1H), 4.11 (s, 3H), 3.66 (s, 2H), 2.15 (d, J = 7.1 Hz, 3H). MS (ESI) m/z: 636[M + H].sup.+ III-l-1 [00291] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.51 (s, 1H), 10.60 (s, 1H), 9.23 (d, J = 2.0 Hz, 1H), 8.55 (dd, J = 4.7, 1.7 Hz, 1H), 8.42 (dt, J = 7.9, 1.9 Hz, 1H), 8.20 (d, J = 2.2 Hz, 1H), 8.04 (dq, J = 4.5, 2.2 Hz, 2H), 8.02-7.96 (m, 1H), 7.90 (d, J = 3.1 Hz, 1H), 7.75-7.71 (m, 2H), 7.69 (d, J = 8.6 Hz, 1H), 7.42 (dd, J = 7.9, 4.7 Hz, 1H), 6.77 (d, J = 3.0 Hz, 1H), 3.55 (s, 2H), 2.38 (s, 8H), 2.17 (s, 3H). MS(ESI) m/z: 588[M + H].sup.+. III-l-2 [00292] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.59 (s, 1H), 10.60 (s, 1H), 8.60 (d, J = 5.4 Hz, 2H), 8.21 (d, J = 2.1 Hz, 1H), 8.08-8.04 (m, 2H), 8.03-7.99 (m, 3H), 7.94 (d, J = 3.0 Hz, 1H), 7.73 (d, J = 7.2 Hz, 2H), 7.70 (d, J = 8.6 Hz, 1H), 6.80 (d, J = 3.0 Hz, 1H), 3.56 (s, 2H), 2.44-2.35 (m, 8H), 2.19 (s, 3H). MS(ESI) m/z: 588[M + H].sup.+. III-l-3 [00293] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.67 (s, 1H), 9.24 (s, 1H), 8.69 (d, J = 4.2 Hz, 1H), 8.64-8.60 (m, 1H), 8.23 (d, J = 2.1 Hz, 1H), 8.11 (dd, J = 8.6, 1.9 Hz, 1H), 8.07 (d, J = 2.0 Hz, 1H), 8.01 (dt, J = 6.5, 1.8 Hz, 1H), 7.92 (d, J = 3.1 Hz, 1H), 7.75 (dd, J = 5.5, 3.5 Hz, 2H), 7.72 (d, J = 8.6 Hz, 1H), 6.76 (d, J = 3.1 Hz, 1H), 4.19 (s, 3H), 3.70 (s, 2H), 3.05 (s, 2H), 2.93 (s, 2H), 2.81 (s, 3H), 2.40 (s, 2H). MS (ESI) m/z: 602[M + H].sup.+. III-l-4 [00294] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.71 (s, 1H), 8.84 (s, 2H), 8.35 (s, 2H), 8.24 (d, J = 1.6 Hz, 1H), 8.12 (d, J = 8.4 Hz, 1H), 8.09 (s, 1H), 8.03 (d, J = 6.8 Hz, 1H), 7.99 (d, J = 3.0 Hz, 1H), 4.21 (s, 3H), 3.71 (s, 2H), 3.06 (s, 2H), 2.93 (s, 2H), 2.81 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-m-1 [00295] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.54 (d, J = 2.9 Hz, 1H), 10.50 (s, 1H), 9.16 (d, J = 2.1 Hz, 1H), 8.54 (dd, J = 4.8, 1.7 Hz, 1H), 8.37 (dt, J = 8.0, 2.0 Hz, 1H), 8.18 (d, J = 2.2 Hz, 1H), 8.04 (dd, J = 8.6, 2.2 Hz, 1H), 8.02 (d, J = 1.8 Hz, 1H), 7.97 (dd, J = 7.9, 1.8 Hz, 1H), 7.91 (t, J = 2.8 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 7.41 (dd, J = 8.0, 4.7 Hz, 1H), 6.77 (d, J = 2.8 Hz, 1H), 3.56 (s, 2H), 2.39 (s, 8H), 2.28 (s, 3H), 2.18 (s, 3H). MS(ESI) m/z: 602[M + H].sup.+. III-m-2 [00296] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.62 (s, 1H), 10.51 (s, 1H), 8.59 (d, J = 5.4 Hz, 2H), 8.19 (d, J = 2.1 Hz, 1H), 8.13-8.01 (m, 2H), 7.98 (dd, J = 7.9, 1.8 Hz, 1H), 7.95 (q, J = 2.8, 2.3 Hz, 3H), 7.69 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 6.81 (d, J = 3.0 Hz, 1H), 3.57 (s, 2H), 2.43 (s, 8H), 2.27 (s, 3H), 2.25 (s, 3H). MS(ESI) m/z: 602[M + H].sup.+. III-m-3 [00297] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.11 (s, 1H), 8.09-8.06 (m, 2H), 7.94 (s, 1H), 7.90 (d, J = 8.0 Hz, 2H), 7.72 (t, J = 6.8 Hz, 2H), 7.55 (d, J = 8.0 Hz, 1H), 7.32 (d, J = 6.4 Hz, 3H), 6.73 (d, J = 3.0 Hz, 1H), 3.63 (s, 2H), 2.31 (s, 3H), 2.29 (s, 3H). MS (ESI) m/z: 601[M + H].sup.+. III-m-4 [00298] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.56 (s, 1H), 10.57 (s, 1H), 8.21 (d, J = 1.9 Hz, 1H), 8.11 (d, J = 8.5 Hz, 1H), 8.03 (d, J = 1.4 Hz, 1H), 7.96 (d, J = 8.2 Hz, 3H), 7.91 (t, J = 2.9 Hz, 1H), 7.71 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 7.18 (d, J = 8.1 Hz, 2H), 6.73 (dd, J = 2.8, 1.9 Hz, 1H), 3.72 (s, 2H), 3.05 (s, 2H), 2.95 (s, 2H), 2.81 (s, 3H), 2.29 (d, J = 6.7 Hz, 6H). MS (ESI) m/z: 615[M + H].sup.+. III-m-5 [00299] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.57 (s, 1H), 10.56 (s, 1H), 8.21 (s, 1H), 8.10 (d, J = 8.2 Hz, 1H), 8.06 (d, J = 6.6 Hz, 2H), 8.02 (d, J = 6.8 Hz, 1H), 7.97 (d, J = 7.9 Hz, 1H), 7.92 (s, 1H), 7.70 (d, J = 8.4 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.41 (d, J = 7.7 Hz, 2H), 6.77 (s, 1H), 3.69 (s, 2H), 3.04 (s, 2H), 2.92 (s, 2H), 2.81 (s, 3H), 2.40 (s, 2H), 2.29 (s, 3H). MS (ESI) m/z: 635[M + H].sup.+. III-m-6 [00300] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.50 (s, 1H), 10.49 (s, 1H), 8.18 (s, 1H), 8.10-8.01 (m, 4H), 7.96 (d, J = 8.2 Hz, 1H), 7.90 (s, 1H), 7.71-7.66 (m, 2H), 7.62 (d, J = 8.2 Hz, 1H), 7.43 (d, J = 8.5 Hz, 2H), 6.74 (s, 1H), 3.55 (s, 2H), 2.27 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 635[M + H].sup.+. III-m-7 [00301] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.46 (s, 1H), 10.54 (s, 1H), 8.20 (d, J = 2.1 Hz, 1H), 8.10 (dd, J = 8.6, 1.9 Hz, 1H), 7.99 (d, J = 1.6 Hz, 1H), 7.97 (dd, J = 7.9, 1.7 Hz, 1H), 7.88 (t, J = 2.9 Hz, 1H), 7.70 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 7.56-7.54 (m, 1H), 7.49 (d, J = 7.8 Hz, 1H), 7.13 (t, J = 7.9 Hz, 1H), 6.78-6.74 (m, 1H), 6.72 (dd, J = 3.0, 1.9 Hz, 1H), 3.68 (s, 2H), 3.40 (d, J = 9.5 Hz, 2H), 3.04 (s, 2H), 2.92 (d, J = 10.5 Hz, 2H), 2.80 (s, 3H), 2.39 (s, 2H), 2.27 (s, 3H). MS (ESI) m/z: 617[M + H].sup.+. III-m-8 [00302] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.38 (s, 1H), 10.49 (s, 1H), 8.19 (s, 1H), 8.05 (d, J = 8.2 Hz, 1H), 8.01 (s, 1H), 7.93 (d, J = 13.7 Hz, 2H), 7.83 (s, 1H), 7.69 (d, J = 8.0 Hz, 1H), 7.65 (s, 1H), 7.59 (d, J = 7.6 Hz, 1H), 6.75 (s, 1H), 6.66 (s, 1H), 3.55 (s, 2H), 2.26 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 591 [M + H].sup.+. III-m-9 [00303] .sup.1H NMR (600 MHz, Chloroform-d) 9.44 (s, 1H), 9.12 (d, J = 2.0 Hz, 1H), 8.42 (dd, J = 4.8, 1.6 Hz, 1H), 8.22 (dt, J = 8.1, 1.9 Hz, 1H), 7.93 (d, J = 2.1 Hz, 1H), 7.88-7.85 (m, 2H), 7.82 (dd, J = 7.9, 1.7 Hz, 1H), 7.65 (d, J = 8.5 Hz, 1H), 7.35 (d, J = 7.9 Hz, 1H), 7.31-7.28 (m, 1H), 7.09 (dd, J = 8.0, 4.8 Hz, 1H), 6.63 (d, J = 3.0 Hz, 1H), 4.09 (s, 3H), 3.58 (s, 2H), 2.31 (s, 3H), 2.21 (s, 3H). MS(ESI) m/z: 616[M + H].sup.+. III-m-10 [00304] .sup.1H NMR (600 MHz, Chloroform-d) 9.21 (s, 1H), 8.52-8.46 (m, 2H), 7.95 (d, J = 2.2 Hz, 1H), 7.87 (td, J = 4.7, 3.9, 1.8 Hz, 3H), 7.85-7.82 (m, 2H), 7.70 (d, J = 8.5 Hz, 1H), 7.45 (d, J = 7.8 Hz, 1H), 7.36 (d, J = 3.1 Hz, 1H), 6.70 (d, J = 3.1 Hz, 1H), 4.11 (s, 3H), 3.61 (s, 2H), 2.51 (s, 8H), 2.30 (s, 3H), 2.26 (s, 3H). MS (ESI) m/z: 616[M + H].sup.+. III-m-11 [00305] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 8.19 (s, 1H), 8.07 (dd, J = 13.2, 7.9 Hz, 4H), 7.95 (d, J = 8.0 Hz, 1H), 7.84 (d, J = 2.9 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.37-7.33 (m, 3H), 6.69 (d, J = 3.0 Hz, 1H), 4.19 (s, 3H), 3.55 (s, 2H), 2.30 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 615[M + H].sup.+. III-m-12 [00306] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 8.18 (d, J = 2.1 Hz, 1H), 8.05 (dd, J = 10.5, 1.6 Hz, 2H), 7.94 (dd, J = 11.2, 4.9 Hz, 3H), 7.82 (d, J = 3.1 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.61 (d, J = 8.1 Hz, 1H), 7.14 (d, J = 8.0 Hz, 2H), 6.66 (d, J = 3.1 Hz, 1H), 4.17 (s, 3H), 3.55 (s, 2H), 2.29 (s, 3H), 2.27 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 629[M + H].sup.+. III-m-13 [00307] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 8.19 (s, 1H), 8.08 (s, 1H), 8.05 (d, J = 7.8 Hz, 2H), 8.00 (d, J = 7.3 Hz, 1H), 7.96 (d, J = 7.9 Hz, 1H), 7.88 (d, J = 2.8 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.43-7.37 (m, 2H), 6.72 (d, J = 2.7 Hz, 1H), 4.20 (s, 3H), 3.55 (s, 2H), 2.51 (s, 2H), 2.31 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 650[M + H].sup.+. III-m-14 [00308] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.52 (s, 1H), 8.18 (s, 1H), 8.05 (d, J = 8.5 Hz, 4H), 7.95 (d, J = 8.0 Hz, 1H), 7.86 (d, J = 2.7 Hz, 1H), 7.69 (d, J = 8.4 Hz, 1H), 7.61 (d, J = 8.0 Hz, 2H), 7.42 (d, J = 8.5 Hz, 1H), 6.70 (d, J = 2.9 Hz, 3H), 4.19 (d, J = 7.0 Hz, 2H), 2.29 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 650[M + H].sup.+. III-m-15 [00309] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.59 (s, 1H), 8.22 (s, 1H), 8.11 (d, J = 8.6 Hz, 1H), 8.01 (s, 1H), 7.96 (d, J = 7.8 Hz, 1H), 7.85 (d, J = 2.7 Hz, 1H), 7.71 (d, J = 8.5 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.53 (s, 1H), 7.47 (d, J = 7.8 Hz, 1H), 7.13 (t, J = 7.9 Hz, 1H), 6.77 (d, J = 8.0 Hz, 1H), 6.68 (d, J = 2.8 Hz, 1H), 4.19 (s, 3H), 3.73 (s, 2H), 3.42 (s, 2H), 3.01 (d, J = 62.2 Hz, 4H), 2.81 (s, 3H), 2.45 (s, 2H), 2.30 (s, 3H). MS (ESI) m/z: 631[M + H].sup.+. III-m-16 [00310] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.60 (s, 1H), 8.22 (s, 1H), 8.11 (d, J = 8.2 Hz, 1H), 8.02 (s, 1H), 7.95 (d, J = 8.0 Hz, 1H), 7.89 (d, J = 8.3 Hz, 2H), 7.84 (s, 1H), 7.71 (d, J = 8.5 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 6.74 (d, J = 8.4 Hz, 2H), 6.64 (d, J = 2.1 Hz, 1H), 4.18 (s, 3H), 3.70 (s, 2H), 2.99 (d, J = 69.4 Hz, 4H), 2.81 (s, 3H), 2.42 (s, 2H), 2.30 (s, 3H). MS (ESI) m/z: 631[M + H].sup.+. III-m-17 [00311] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.51 (s, 1H), 8.19 (s, 1H), 8.06 (d, J = 8.4 Hz, 1H), 8.03 (s, 1H), 7.94-7.90 (m, 2H), 7.80 (d, J = 2.0 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.66 (s, 1H), 7.58 (d, J = 7.9 Hz, 1H), 6.74 (s, 1H), 6.62 (d, J = 2.0 Hz, 1H), 4.17 (s, 3H), 3.55 (s, 2H), 2.29 (s, 3H), 2.17 (s, 3H). MS (ESI) m/z: 605[M + H].sup.+. III-m-18 [00312] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.51 (s, 1H), 8.19 (s, 1H), 8.06 (d, J = 8.3 Hz, 1H), 8.03 (s, 1H), 7.94 (d, J = 7.9 Hz, 1H), 7.84 (s, 1H), 7.82 (s, 1H), 7.69 (d, J = 8.4 Hz, 1H), 7.60 (d, J = 7.8 Hz, 1H), 7.50 (s, 2H), 6.65 (d, J = 2.9 Hz, 1H), 4.17 (s, 3H), 3.55 (s, 2H), 2.29 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 621[M + H].sup.+. III-m-19 [00313] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.47 (s, 1H), 8.19 (d, J = 2.2 Hz, 1H), 8.07-8.04 (m, 1H), 7.89 (d, J = 1.7 Hz, 1H), 7.86 (dd, J = 7.9, 1.8 Hz, 1H), 7.70 (d, J = 8.5 Hz, 1H), 7.52 (d, J = 8.0 Hz, 1H), 7.46 (d, J = 3.0 Hz, 1H), 6.18 (d, J = 3.0 Hz, 2H), 3.99 (s, 3H), 3.56 (s, 2H), 2.64 (d, J = 4.8 Hz, 3H), 2.25 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 568[M + H].sup.+. III-m-20 [00314] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.64 (s, 1H), 8.22 (s, 1H), 8.11 (d, J = 8.6 Hz, 1H), 8.00 (s, 1H), 7.93 (d, J = 7.9 Hz, 1H), 7.79 (s, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.58 (d, J = 8.0 Hz, 1H), 6.40 (s, 1H), 4.10 (s, 3H), 3.72 (s, 2H), 3.59 (s, 4H), 3.46 (s, 4H), 3.06 (s, 2H), 2.95 (s, 2H), 2.81 (s, 3H), 2.45 (s, 2H), 2.29 (s, 3H). MS (ESI) m/z: 624[M + H].sup.+. III-m-21 [00315] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.62 (s, 1H), 8.23 (s, 1H), 8.08 (d, J = 11.1 Hz, 2H), 7.93 (d, J = 7.8 Hz, 1H), 7.77 (d, J = 2.6 Hz, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.58 (d, J = 7.9 Hz, 1H), 6.39 (d, J = 2.6 Hz, 1H), 4.10 (s, 3H), 3.70 (s, 2H), 3.47 (d, J = 63.3 Hz, 4H), 2.99 (d, J = 74.8 Hz, 4H), 2.81 (s, 3H), 2.32 (s, 2H), 1.00 (d, J = 5.6 Hz, 6H). MS (ESI) m/z: 652[M + H].sup.+. III-m-22 [00316] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 8.41 (s, 1H), 8.21 (s, 1H), 8.11 (d, J = 7.8 Hz, 1H), 7.92 (s, 3H), 7.71 (d, J = 8.1 Hz, 1H), 7.57 (d, J = 8.2 Hz, 1H), 6.69 (s, 1H), 4.19 (s, 3H), 3.71 (s, 2H), 3.05 (s, 2H), 2.95 (s, 2H), 2.81 (s, 3H), 2.41 (d, J = 19.7 Hz, 2H), 2.24 (s, 3H). MS (ESI) m/z: 539[M + H].sup.+. III-m-23 [00317] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.49 (s, 1H), 8.19 (d, J = 1.8 Hz, 1H), 8.07 (d, J = 8.5 Hz, 1H), 7.97 (d, J = 1.3 Hz, 1H), 7.89-7.84 (m, 1H), 7.70 (d, J = 8.6 Hz, 1H), 7.55 (d, J = 2.9 Hz, 1H), 7.53 (d, J = 8.0 Hz, 1H), 6.23 (d, J = 2.9 Hz, 1H), 4.03 (s, 3H), 3.57 (s, 2H), 3.42 (s, 3H), 2.24 (s, 3H), 2.13 (s, 3H). MS (ESI) m/z: 637[M + H].sup.+. III-m-24 [00318] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.19 (d, J = 2.2 Hz, 1H), 7.99 (dd, J = 8.5, 2.0 Hz, 1H), 7.94- 7.92 (m, 2H), 7.78 (d, J = 8.5 Hz, 1H), 7.66 (d, J = 2.9 Hz, 1H), 7.57 (d, J = 8.5 Hz, 1H), 6.45 (d, J = 2.9 Hz, 1H), 4.19 (s, 3H), 3.79 (s, 2H), 3.08 (s, 6H), 2.92 (s, 3H), 2.37 (s, 3H). MS (ESI) m/z: 582[M + H].sup.+. III-m-25 [00319] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.31 (s, 1H), 10.50 (s, 1H), 8.19 (d, J = 2.1 Hz, 1H), 8.08-8.05 (m, 1H), 7.89 (dd, J = 7.9, 1.7 Hz, 1H), 7.84 (d, J = 1.7 Hz, 1H), 7.70 (d, J = 8.6 Hz, 1H), 7.53 (d, J = 8.1 Hz, 1H), 5.95 (d, J = 2.8 Hz, 1H), 3.98 (s, 3H), 3.57 (s, 2H), 2.23 (d, J = 12.8 Hz, 6H). MS (ESI) m/z: 555[M + H].sup.+. III-m-26 [00320] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.30 (s, 1H), 10.49 (s, 1H), 9.70 (s, 1H), 8.19 (d, J = 1.7 Hz, 1H), 8.05 (d, J = 8.3 Hz, 1H), 8.00 (s, 1H), 7.95 (d, J = 7.9 Hz, 1H), 7.91 (d, J = 8.7 Hz, 2H), 7.81 (t, J = 2.8 Hz, 1H), 7.69 (d, J = 8.6 Hz, 1H), 7.62 (d, J = 8.1 Hz, 1H), 6.72 (d, J = 8.7 Hz, 2H), 6.66 (d, J = 1.7 Hz, 1H), 3.55 (s, 2H), 2.26 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 617[M + H].sup.+ III-m-27 [00321] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.50 (s, 1H), 10.54 (s, 1H), 8.21 (d, J = 2.0 Hz, 1H), 8.12-8.09 (m, 1H), 8.01 (d, J = 1.6 Hz, 1H), 7.95 (dd, J = 7.9, 1.7 Hz, 1H), 7.88 (t, J = 2.2 Hz, 2H), 7.70 (d, J = 8.6 Hz, 1H), 7.62 (d, J = 8.2 Hz, 1H), 7.54-7.50 (m, 2H), 6.71 (dd, J = 3.0, 1.9 Hz, 1H), 3.69 (s, 2H), 3.04 (s, 2H), 2.93 (d, J = 13.8 Hz, 2H), 2.81 (s, 3H), 2.39 (s, 2H), 2.28 (s, 3H). MS (ESI) m/z: 607[M + H].sup.+ III-n-1 [00322] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.45 (s, 1H), 10.67 (s, 1H), 9.28 (d, J = 2.1 Hz, 1H), 8.58 (dd, J = 4.8, 1.7 Hz, 1H), 8.47 (dt, J = 8.0, 2.0 Hz, 1H), 8.19 (d, J = 2.1 Hz, 1H), 7.96 (dd, J = 8.5, 2.1 Hz, 1H), 7.88 (t, J = 2.7 Hz, 1H), 7.69 (d, J = 8.5 Hz, 1H), 7.57 (d, J = 2.5 Hz, 1H), 7.54 (dd, J = 8.3, 2.6 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 7.45 (dd, J = 7.9, 4.7 Hz, 1H), 6.75 (d, J = 2.9 Hz, 1H), 3.56 (s, 2H), 2.48 (s, 3H), 2.20 (s, 3H). MS(ESI) m/z: 602[M + H].sup.+. III-n-2 [00323] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.69 (s, 1H), 8.68-8.57 (m, 2H), 8.19 (d, J = 2.2 Hz, 1H), 8.11-8.03 (m, 2H), 8.02-7.94 (m, 1H), 7.91 (d, J = 3.1 Hz, 1H), 7.69 (d, J = 8.5 Hz, 1H), 7.59 (d, J = 2.5 Hz, 1H), 7.54 (dd, J = 8.3, 2.5 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 6.78 (d, J = 3.1 Hz, 1H), 5.75 (s, 1H), 3.56 (s, 2H), 2.48 (s, 3H), 2.23 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-n-3 [00324] .sup.1H NMR (600 MHz, Chloroform-d) 9.30 (t, J = 2.7 Hz, 1H), 8.96 (d, J = 36.4 Hz, 1H), 8.50 (dt, J = 4.8, 2.3 Hz, 1H), 8.36-8.25 (m, 1H), 7.90 (d, J = 11.8 Hz, 2H), 7.71 (d, J = 8.4 Hz, 1H), 7.51 (d, J = 2.4 Hz, 1H), 7.32 (dtd, J = 17.9, 7.9, 7.4, 2.7 Hz, 3H), 7.21 (dd, J = 8.0, 4.4 Hz, 1H), 6.64- 6.62 (m, 1H), 4.13 (d, J = 2.3 Hz, 3H), 3.64 (s, 2H), 2.59 (s, 3H), 2.37 (d, J = 2.2 Hz, 3H). MS(ESI) m/z: 616[M + H].sup.+. III-n-4 [00325] .sup.1H NMR (600 MHz, Chloroform-d) 9.00 (s, 1H), 8.53-8.45 (m, 2H), 7.99-7.92 (m, 2H), 7.92- 7.83 (m, 2H), 7.72 (d, J = 8.4 Hz, 1H), 7.50 (d, J = 1.7 Hz, 1H), 7.40-7.34 (m, 3H), 6.71 (d, J = 3.0 Hz, 1H), 4.13 (s, 3H), 3.63 (s, 2H), 2.59 (s, 3H), 2.33 (s, 3H). MS(ESI) m/z: 616[M + H].sup.+. III-o-1 [00326] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.49 (s, 1H), 10.93 (s, 1H), 9.31 (s, 1H), 8.60 (d, J = 3.7 Hz, 1H), 8.48 (dt, J = 8.0, 1.9 Hz, 1H), 8.17 (d, J = 2.1 Hz, 1H), 7.93 (dd, J = 8.5, 1.8 Hz, 1H), 7.90 (d, J = 3.0 Hz, 1H), 7.75 (dd, J = 5.8, 2.9 Hz, 2H), 7.71 (d, J = 8.6 Hz, 1H), 7.67 (dd, J = 8.8, 2.8 Hz, 1H), 7.46 (dd, J = 7.9, 4.8 Hz, 1H), 6.76 (t, J = 3.8 Hz, 1H), 3.55 (s, 2H), 2.15 (s, 3H). MS (ESI) m/z: 623[M + H].sup.+. III-o-2 [00327] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.78 (s, 1H), 10.99 (s, 1H), 8.87 (s, 2H), 8.45 (s, 2H), 8.18 (d, J = 2.0 Hz, 1H), 8.01 (t, J = 2.9 Hz, 1H), 7.98- 7.95 (m, 1H), 7.78-7.75 (m, 2H), 7.73 (d, J = 8.6 Hz, 1H), 7.70 (dd, J = 8.8, 2.8 Hz, 1H), 6.87 (dd, J = 2.9, 1.8 Hz, 1H), 3.69 (s, 2H), 3.04 (s, 2H), 2.92 (s, 2H), 2.81 (s, 3H), 2.39 (s, 2H). MS (ESI) m/z: 623[M + H].sup.+ III-o-3 [00328] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.93 (s, 1H), 9.28 (d, J = 1.8 Hz, 1H), 8.59 (dd, J = 4.7, 1.6 Hz, 1H), 8.46 (dt, J = 8.0, 1.9 Hz, 1H), 8.16 (d, J = 2.1 Hz, 1H), 7.93 (dd, J = 8.5, 1.9 Hz, 1H), 7.86 (d, J = 3.0 Hz, 1H), 7.79 (d, J = 2.8 Hz, 1H), 7.76 (d, J = 8.7 Hz, 1H), 7.73-7.70 (m, 2H), 7.46 (dd, J = 7.9, 4.7 Hz, 1H), 6.72 (d, J = 3.0 Hz, 1H), 4.14 (s, 3H), 3.56 (s, 2H), 2.17 (s, 3H). MS (ESI) m/z: 637[M + H].sup.+. III-o-4 [00329] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.94 (s, 1H), 8.63 (dd, J = 4.5, 1.5 Hz, 2H), 8.17 (d, J = 2.1 Hz, 1H), 8.05 (dd, J = 4.5, 1.5 Hz, 2H), 7.94 (dd, J = 8.5, 1.9 Hz, 1H), 7.89 (d, J = 3.1 Hz, 1H), 7.81 (d, J = 2.8 Hz, 1H), 7.76 (d, J = 8.7 Hz, 1H), 7.73-7.69 (m, 2H), 6.75 (d, J = 3.0 Hz, 1H), 4.14 (s, 3H), 3,56 (s, 2H), 2.15 (s, 3H). MS (ESI) m/z: 637[M + H].sup.+. III-p-1 [00330] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.51 (s, 1H), 10.61 (s, 1H), 9.23 (d, J = 2.0 Hz, 1H), 8.56 (dd, J = 4.7, 1.6 Hz, 1H), 8.42 (dt, J = 8.0, 1.9 Hz, 1h), 8.19 (s, 1H), 8.07 (s, 1H), 8.03-8.00 (m, 2H), 7.91 (d, J = 3.0 Hz, 1H), 7.77-7.70 (m, 2H), 7.43 (dd, J = 8.0, 4.7 Hz, 1H), 7.36 (s, 1H), 6.77 (d, J = 3.0 Hz, 1H), 3.54 (s, 2H), 3.18 (s, 4H), 2.16 (s, 3H). MS (ESI) m/z: 588[M + H].sup.+. III-p-2 [00331] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.59 (s, 1H), 10.61 (s, 1H), 8.61 (dd, J = 4.5, 1.6 Hz, 2H), 8.19 (s, 1H), 8.08 (d, J = 2.1 Hz, 1H), 8.04-8.00 (m, 4H), 7.95 (d, J = 2.9 Hz, 1H), 7.77-7.70 (m, 2H), 7.36 (s, 1H), 6.81 (d, J = 3.0 Hz, 1H), 3.53 (s, 2H), 2.15 (s, 3H). MS (ESI) m/z: 588[M + H].sup.+. III-p-3 [00332] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.63 (s, 1H), 9.21 (d, J = 2.1 Hz, 1H), 8.56 (dd, J = 4.7, 1.6 Hz, 1H), 8.40 (dt, J = 8.0, 1.9 Hz, 1H), 8.19 (s, 1H), 8.08 (s, 1H), 8.04-7.99 (m, 2H), 7.88 (d, J = 3.1 Hz, 1H), 7.76-7.72 (m, 2H), 7.42 (dd, J = 8.0, 4.7 Hz, 1H), 7.36 (s, 1H), 6.73 (d, J = 3.1 Hz, 1H), 4.18 (s, 3H), 3.53 (s, 2H), 2.15 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-p-4 [00333] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.63 (s, 1H), 8.61 (dd, J = 4.5, 1.6 Hz, 2H), 8.19 (s, 1H), 8.08 (s, 1H), 8.03-8.00 (m, 2H), 7.98 (dd, J = 4.5, 1.6 Hz, 2H), 7.92 (d, J = 3.1 Hz, 1H),7.74 (dd, J = 3.4, 1.8 Hz, 2H), 7.36 (s, 1H), 6.77 (d, J = 3.1 Hz, 1H), 4.19 (s, 3H), 3.54 (s, 2H), 2.16 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-q-1 [00334] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.54 (s, 1H), 10.51 (s, 1H), 9.17 (d, J = 1.9 Hz, 1H), 8.55 (dd, J = 4.7, 1.6 Hz, 1H), 8.38 (dt, J = 8.0, 1.9 Hz, 1H), 8.17 (s, 1H), 8.05 (d, J = 1.6 Hz, 1H), 8.01- 7.97 (m, 2H), 7.92 (d, J = 2.9 Hz, 1H), 7.64 (d, J = 8.1 Hz, 1H), 7.41 (dd, J = 8.0, 4.7 Hz, 1H), 7.34 (s, 1H), 6.78 (d, J = 3.0 Hz, 1H), 3.52 (s, 2H), 2.28 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-q-2 [00335] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.62 (s, 1H), 10.52 (s, 1H), 8.59 (dd, J = 4.6, 1.4 Hz, 2H), 8.18 (s, 1H), 8.18 (s, 1H), 8.06 (d, J = 1.5 Hz, 1H), 8.02-7.97 (m, 2H), 7.97-7.93 (m, 3H), 7.64 (d, J = 8.1 Hz, 1H), 7.34 (s, 1H), 6.81 (d, J = 3.0 Hz, 1H), 3.52 (s, 2H), 2.28 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-q-3 [00336] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.53 (s, 1H), 9.14 (d, J = 1.5 Hz, 1H), 8.54 (dd, J = 4.7, 1.6 Hz, 1H), 8.38-8.34 (m, 1H), 8.17 (s, 1H), 8.06 (d, J = 1.5 Hz, 1H), 8.00 (s, 1H), 7.97 (dd, J = 7.9, 1.6 Hz, 1H), 7.89 (d, J = 3.0 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 7.41 (d, J = 7.9, 4.8 Hz, 1H), 7.34 (s, 1H), 6.73 (d, J = 3.1 Hz, 1H), 4.21 (s, 3H), 3.52 (s, 2H), 2.31 (s, 3H), 2.15 (s, 3H). MS (ESI) m/z: 616[M + H].sup.+. III-q-4 [00337] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.53 (s, 1H), 8.58 (dd, J = 4.6, 1.5 Hz, 2H), 8.17 (s, 1H), 8.07 (d, J = 1.7 Hz, 1H), 8.01 (s, 1H), 7.98 (dd, J = 7.9, 1.7 Hz, 1H), 7.94-7.90 (m, 3H), 7.63 (d, J = 8.1 Hz, 1H), 7.34 (s, 1H), 6.77 (d, J = 3.1 Hz, 1H), 4.21 (s, 3H), 3.52 (s, 2H), 3.18 (s, 4H), 2.30 (s, 3H), 2.14 (s, 3H). MS (ESI) m/z: 616[M + H].sup.+. III-r-1 [00338] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.58 (s, 1H), 10.77 (s, 1H), 9.33 (s, 1H), 8.73 (s, 2H), 8.10 (s, 1H), 8.06 (s, 1H), 7.93 (s, 1H), 7.73 (s, 1H), 7.57 (d, J = 15.2 Hz, 2H), 7.53-7.44 (m, 2H), 6.79 (s, 1H), 3.86 (s, 2H), 2.80 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-r-2 [00339] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.53 (s, 1H), 10.72 (s, 1H), 8.63 (dd, J = 4.5, 1.6 Hz, 2H), 8.16 (s, 1H), 8.07 (dd, J = 4.5, 1.6 Hz, 2H), 7.94 (s, 1H), 7.91 (d, J = 3.0 Hz, 1H), 7.62 (d, J = 2.5 Hz, 1H), 7.54 (dd, J = 8.3, 2.5 Hz, 1H), 7.49 (d, J = 8.5 Hz, 1H), 7.35 (s, 1H), 6.79 (d, J = 3.0 Hz, 1H), 3.53 (s, 2H), 2.49 (s, 3H), 2.18 (s, 3H). MS (ESI) m/z: 602[M + H].sup.+. III-r-3 [00340] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.72 (s, 1H), 9.26 (dd, J = 2.2, 0.7 Hz, 1H), 8.58 (dd, J = 4.7, 1.7 Hz, 1H), 8.46-8.43 (m, 1H), 8.14 (s, 1H), 7.92 (s, 1H), 7.85 (d, J = 3.1 Hz, 1H), 7.63 (d, J = 2.5 Hz, 1H), 7.63 (d, J = 2.5 Hz, 1H), 7.57 (dd, J = 8.3, 2.5 Hz, 1H), 7.49 (d, J = 8.5 Hz, 1H), 7.44 (ddd, J = 8.0, 4.8, 0.8 Hz, 1H), 7.35 (s, 1H), 6.71 (d, J = 3.0 Hz, 1H), 4.15 (s, 3H), 3.52 (s, 2H), 2.48 (s, 3H), 2.14 (s, 3H). MS (ESI) m/z: 616[M + H].sup.+. III-r-4 [00341] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.84 (s, 1H), 8.90 (s, 2H), 8.45 (s, 2H), 8.10 (d, J = 21.8 Hz, 2H), 7.98 (s, 1H), 7.66-7.59 (m, 2H), 7.52 (d, J = 8.3 Hz, 2H), 6.83 (s, 1H), 4.19 (s, 3H), 3.96 (s, 2H), 2.82 (s, 3H). MS (ESI) m/z: 616[M + H].sup.+. III-u-1 [00342] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.69 (s, 1H), 10.89 (s, 1H), 9.63 (d, J = 1.7 Hz, 1H), 9.22 (d, J = 2.1 Hz, 1H), 8.72 (dd, J = 5.2, 1.6 Hz, 1H), 8.67-8.64 (m, 1H), 8.58 (s, 1H), 8.24 (s, 1H), 8.07 (d, J = 1.8 Hz, 1H), 8.04-8.01 (m, 2H), 7.98 (t, J = 3.0 Hz, 1H), 7.94 (s, 1H), 7.73 (q, J = 8.1, 5.1 Hz, 1H), 7.68 (d, J = 8.0 Hz, 1H), 6.82 (q, J = 3.1, 1.8 Hz, 1H), 2.36 (d, J = 1.2 Hz, 3H), 2.30 (s, 3H). MS (ESI) m/z: 570 [M + H].sup.+. III-u-2 [00343] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.81 (s, 1H), 10.91 (s, 1H), 9.55 (s, 1H), 8.77 (d, J = 5.7 Hz, 2H), 8.56 (s, 1H), 8.23 (t, 3H), 8.08 (d, J = 1.8 Hz, 1H), 8.05-7.99 (m, 3H), 7.93 (s, 1H), 7.68 (d, J = 8.01 Hz, 1H), 6.87 (s, 3H), 2.35 (s, 5H), 2.30 (s, 3H). MS (ESI) m/z: 570 [M + H].sup.+. III-u-3 [00344] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.93 (s, 1H), 9.61 (d, J = 1.7 Hz, 1H), 9.17 (d, J = 2.1 Hz, 1H), 8.66 (d, J = 4.9 Hz, 1H), 8.58-8.54 (m, 2H), 8.25 (s, 1H), 8.09 (d, J = 1.8 Hz, 1H), 8.03-8.00 (m, 2H), 7.94-7.91 (m, 2H), 7.67 (d, J = 8.1 Hz, 1H), 7.67-7.61 (m, 1H), 6.76 (d, J = 3.1 Hz, 1H), 4.22 (s, 3H), 2.36 (d, J = 1.1 Hz, 3H), 2.33 (s, 3H). MS (ESI) m/z: 584 [M + H].sup.+. III-u-4 [00345] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.95 (s, 1H), 9.58 (d, J = 1.7 Hz, 1H), 8.78 (d, J = 6.6 Hz, 2H), 8.57 (s, 1H), 8.26 (s, 1H), 8.23-8.21 (m, 2H), 8.10 (d, J = 1.8 Hz, 1H), 8.04-8.01 (m, 2H), 7.99 (d, J = 3.1 Hz, 1H), 7.93 (s, 1H), 7.67 (d, J = 8.5 Hz, 1H), 6.84 (d, J = 3.1 Hz, 1H), 4.24 (s, 3H), 2.36 (d, J = 1.2 Hz, 3H), 2.32 (s, 3H). MS (ESI) m/z: 584 [M + H].sup.+. III-v-1 [00346] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.04 (s, 1H), 8.86 (s, 4H), 8.43 (d, J = 5.2 Hz, 2H), 8.02 (d, J = 1.8 Hz, 1H), 8.01 (d, J = 3.1 Hz, 1H), 7.97 (d, J = 2.4 Hz, 1H), 7.93 (dd, J = 8.5, 2.3 Hz, 2H), 7.85 (t, J = 10.2 Hz, 2H), 7.68 (d, J = 8.6 Hz, 1H), 6.86 (d, J = 3.1 Hz, 1H), 4.21 (s, 3H), 3.67 (s, 2H), 3.03 (s, 2H), 2.89 (s, 2H), 2.81 (s, 3H), 2.41 (s, 2H). MS (ESI) m/z: 679[M + H].sup.+. II-v-2 [00347] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.46 (s, 1H), 9.14 (d, J = 2.0 Hz, 1H), 8.57 (dd, J = 4.8, 1.7 Hz, 1H), 8.40 (dt, J = 8.0, 2.0 Hz, 1H), 8.13 (d, J = 2.5 Hz, 1H), 8.06-8.01 (m, 2H), 7.95 (dd, J = 7.9, 1.8 Hz, 1H), 7.89 (d, J = 3.1 Hz, 1H), 7.85 (d, J = 7.8 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.55 (d, J = 7.8 Hz, 1H), 7.62 (d J = 8.0 Hz, 1H), 7.55 (d, J = 8.8 Hz, 1H), 7.45 (dd, J = 8.0, 4.8 Hz, 1H), 6.73 (d, J = 3.0 Hz, 1H), 4.20 (s, 3H), 3.69 (dtd, J = 11.0, 6.9, 3.8 Hz, 1H), 2.90 (dd, J = 11.8, 3.9 Hz, 2H), 2.78 (td, J = 11.6, 2.5 Hz, 2H), 2.30 (s, 3H), 1.81 (s, 5H), 1.58-1.45 (m, 2H). MS (ESI) m/z: 644 [M + H].sup.+. III-v-3 [00348] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.45 (s, 1H), 8.82-8.75 (m, 2H), 8.29-8.20 (m, 2H), 8.12 (d, J = 2.5 Hz, 1H), 8.06-8.20 (m, 2H), 8.12 (d, J = 2.5 Hz, 1H), 8.06-8.00 (m, 2H), 8.01-7.95 (m, 2H), 7.88 (t, J = 5.9 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 7.52 (d, J = 8.8 Hz, 1H), 6.83 (d, J = 3.1 Hz, 1H), 4.23 (s, 3H), 2.98 (t, J = 6.4 Hz, 2H), 2.94-2.88 (m, 2H), 2.68 (td, J = 11.5, 2.3 Hz, 2H), 2.31 (s, 3H), 1.82 (s, 3H), 1.73-1.66 (m, 2H), 1.50 (ddt, J = 11.2, 7.7, 3.9 Hz, 1H), 1.24 (qd, J = 11.9, 3.9 Hz, 2H). MS (ESI) m/z: 658 [M + H].sup.+. III-v-4 [00349] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.45 (d, J = 1.9 Hz, 1H), 9.20 (s, 1H), 8.73 (s, 1H), 8.66 (d, J = 8.0 Hz, 1H), 8.11 (d, J = 2.2 Hz, 1H), 8.05 (s, 1H), 8.03 (d, J = 9.2 Hz, 1H), 7.96 (d, J = 7.9 Hz, 1H), 7.92 (d, J = 2.5 Hz, 1H), 7.82-7.78 (m, 1H), 7.76-7.73 (m, 1H), 7.61 (d, J = 7.9 Hz, 1H), 7.51 (d, J = 8.9 Hz, 1H), 6.76 (t, J = 2.4 Hz, 1H), 4.21 (d, J = 1.9 Hz, 3H), 2.99 (t, J = 6.4 Hz, 2H), 2.90 (d, J = 10.8 Hz, 2H), 2.67 (t, J = 11.3 Hz, 2H), 2.30 (d, J = 1.8 Hz, 3H), 2.09 (qd, J = 7.6, 1.9 Hz, 2H), 1.69 (d, J = 12.4 Hz, 2H), 1.50 (d, J = 9.4 Hz, 1H), 1.24 (q, J = 11.6 Hz, 2H), 1.00 (td, J = 7.6, 1.9 Hz, 3H). MS (ESI) m/z: 672 [M + H].sup.+ III-v-5 [00350] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.46 (s, 1H), 8.80 (d, J = 5.7 Hz, 2H), 8.29-8.21 (m, 2H), 8.12 (d, J = 2.5 Hz, 1H), 8.05 (d, J = 1.7 Hz, 1H), 8.03 (dd, J = 8.8, 2.5 Hz, 1H), 7.99 (d, J = 3.2 Hz, 1H), 7.97 (dd, J = 7.9, 1.8 Hz, 1H), 7.81 (t, J = 5.9 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 7.52 (d, J = 8.8 Hz, 1H), 6.84 (d, J = 3.0 Hz, 1H), 4.23 (s, 3H), 2.99 (t, J = 6.4 Hz, 2H), 2.93-2.86 (m, 2H), 2.67 (td, J = 11.6, 2.4 Hz, 2H), 2.30 (s, 3H), 2.09 (q, J = 7.6 Hz, 2H), 1.69 (dd, J = 13.3, 3.6 Hz, 2H), 1.51 (ddd, J = 11.2, 7.4, 4.0 Hz, 1H), 1.29-1.18 (m, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 672 [M + H].sup.+ III-v-6 [00351] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.44 (s, 1H), 9.13 (d, J = 2.1 Hz, 1H), 8.54 (dd, J = 4.7, 1.7 Hz, 1H), 8.35 (dt, J = 8.1, 2.0 Hz, 1H), 8.10 (d, J = 2.5 Hz, 1H), 8.02 (dd, J = 7.0, 2.1 Hz, 2H), 7.94 (dd, J = 7.9, 1.8 Hz, 1H), 7.89 (t, J = 6.1 Hz, 1H), 7.87 (d, J = 3.1 Hz, 1H), 7.61 (d, J = 8.0 Hz, 1H), 7.51 (d, J = 8.8 Hz, 1H), 7.40 (dd, J = 8.0, 4.7 Hz, 1H), 6.72 (d, J = 3.1 Hz, 1H), 4.20 (s, 3H), 2.98 (t, J = 6.4 Hz, 2H), 2.94- 2.87 (m, 2H), 2.67 (td, J = 11.6, 2.3 Hz, 2H), 2.29 (s, 3H), 1.82 (s, 3H), 1.75-1.65 (m, 2H), 1.50 (qd, J = 7.5, 3.9 Hz, 1H), 1.23 (qd, J = 12.1, 3.9 Hz, 2H). MS (ESI) m/z: 658 [M + H].sup.+ III-v-7 [00352] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.44 (s, 1H), 9.15 (s, 1H), 8.54 (s, 1H), 8.35 (dt, J = 8.1, 1.9 Hz, 1H), 8.13 (d, J = 2.5 Hz, 1H), 8.03 (q, J = 4.2, 3.3 Hz, 2H), 7.95 (d, J = 7.8 Hz, 1H), 7.88 (t, J = 2.2 Hz, 1H), 7.74 (d, J = 7.8 Hz, 1H), 7.62 (d, J = 8.0 Hz, 1H), 7.55 (t, J = 8.8 Hz, 1H), 7.41 (dd, J = 7.9, 4.8 Hz, 1H), 6.73 (t, J = 2.3 Hz, 1H), 4.35 (t, J = 5.1 Hz, 2H), 4.20 (d, J = 1.7 Hz, 3H), 3.69 (d, J = 10.5 Hz, 1H), 2.90 (d, J = 11.2 Hz, 2H), 2.78 (t, J = 11.2 Hz, 2H), 2.30 (s, 3H), 1.80 (d, J = 12.1 Hz, 2H), 1.60- 1.47 (m, 2H), 1.00 (td, J = 7.6, 1.7 Hz, 3H). MS (ESI) m/z: 658 [M + H].sup.+ III-v-8 [00353] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.46 (s, 1H), 8.79 (d, J = 5.6 Hz, 2H), 8.29-8.20 (m, 2H), 8.13 (d, J = 2.5 Hz, 1H), 8.05 (d, J = 1.7 Hz, 1H), 8.03 (dd, J = 8.8, 2.6 Hz, 1H), 7.99 (d, J = 3.2 Hz, 1H), 7.97 (dd, J = 8.0, 1.9 Hz, 1H), 7.76 (d, J = 3.2 Hz, 1H), 7.97 (dd, J = 8.0, 1.9 Hz, 1H), 7.76 (d, J = 7.8 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 7.56 (d, J = 8.8 Hz, 1H), 6.84 (d, J = 3.1 Hz, 1H), 4.23 (s, 3H), 3.69 (ddd, J = 11.0, 7.6, 4.1 Hz, 1H), 2.94-2.85 (m, 2H), 2.78 (td, J = 11.5, 2.4 Hz, 2H), 2.31 (s, 3H), 2.07 (q, J = 7.6 Hz, 2H), 1.80 (dd, J = 12.9, 4.3 Hz, 2H), 1.59-1.43 (m, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 658 [M + H].sup.+ III-v-9 [00354] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.47 (s, 1H), 8.92-8.78 (m, 2H), 8.38-8.28 (m, 2H), 8.13 (d, J = 2.5 Hz, 1H), 8.06 (d, J = 1.7 Hz, 1H), 8.04 (dd, J = 8.8, 2.5 Hz, 1H), 8.00 (d, J = 3.1 Hz, 1H), 7.98 (dd, J = 7.9, 1.8 Hz, 1H), 7.86 (d, J = 7.8 Hz, 1H), 7.63 (d, J = 8.0 Hz, 1H), 7.55 (d, J = 8.8 Hz, 1H), 6.85 (d, J = 3.1 Hz, 1H), 4.24 (s, 3H), 3.69 (ddt, J = 14.7, 11.1, 6.2 Hz, 1H), 2.90 (dt, J = 11.7, 4.0 Hz, 2H), 2.78 (td, J = 11.4, 2.4 Hz, 2H), 2.31 (s, 3H), 1.81 (s, 5H), 1.56- 1.45 (m, 2H). MS (ESI) m/z: 644 [M + H].sup.+ III-v-10 [00355] .sup.1H NMR (600 MHz, Chloroform-d) 9.70 (s, 1H), 9.23 (d, J = 7.9 Hz, 1H), 9.10 (d, J = 1.8 Hz, 1H), 8.61 (d, J = 5.3 Hz, 1H), 7.96 (t, J = 2.6 Hz, 1H), 7.89 (dd, J = 8.7, 2.6 Hz, 1H), 7.86-7.78 (m, 1H), 7.72 (d, J = 8.0 Hz, 1H), 7.70 (s, 1H), 7.47 (d, J = 3.1 Hz, 1H), 7.43 (d, J = 7.8 Hz, 1H), 7.26 (d, J = 8.6 Hz, 1H), 6.75 (d, J = 3.0 Hz, 1H), 4.66 (s, 1H), 4.25 (s, 3H), 3.40 (s, 1H), 3.07 (q, J = 7.4 Hz, 2H), 2.97 (dd, J = 11.7, 4.1 Hz, 2H), 2.81-2.65 (m, 2H), 2.25 (s, 3H), 2.00 (dd, J = 12.7, 3.9 Hz, 2H), 1.70 (qd, J = 11.0, 3.8 Hz, 2H), 1.38 (t, J = 7.2 Hz, 3H). MS (ESI) m/z: 694 [M + H].sup.+ III-v-11 [00356] .sup.1H NMR (600 MHz, Chloroform-d) 9.38 (s, 1H), 8.47 (d, J = 5.4 Hz, 2H), 7.94-7.83 (m, 6H), 7.42 (d, J = 7.9 Hz, 1H), 7.36 (d, J = 3.1 Hz, 1H), 7.22 (d, J = 8.7 Hz, 1H), 6.69 (d, J = 3.1 Hz, 1H), 4.85 (d, J = 7.9 Hz, 1H), 4.11 (s, 3H), 3.38 (dtd, J = 11.0, 6.9, 4.1 Hz, 1H), 3.03 (q, J = 7.3 Hz, 2H), 2.98-2.91 (m, 2H), 2.77- 2.67 (m, 2H), 2.25 (s, 3H), 1.99 (dd, J = 12.6, 4.1 Hz, 2H), 1.76-1.63 (m, 2H), 1.36 (t, J = 7.4 Hz, 3H). MS (ESI) m/z: 694 [M + H].sup.+ III-v-12 [00357] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.70 (t, J = 2.3 Hz, 1H), 10.44 (s, 1H), 9.23 (s, 1H), 8.74 (d, J = 5.1 Hz, 1H), 8.70 (dt, J = 8.1, 1.8 Hz, 1H), 8.12 (d, J = 2.5 Hz, 1H), 8.07-8.00 (m, 2H), 8.01-7.91 (m, 2H), 7.81 (t, J = 5.9 Hz, 1H), 7.77 (dd, J = 8.2, 5.2 Hz, 1H), 7.62 (d, J = 8.1 Hz, 1H), 7.51 (d, J = 8.8 Hz, 1H), 6.81 (dd, J = 3.0, 1.8 Hz, 1H), 2.99 (t, J = 6.4 Hz, 2H), 2.94- 2.86 (m, 2H), 2.73-2.63 (m, 2H), 2.28 (s, 3H), 2.09 (q, J = 7.6 Hz, 2H), 1.72-1.63 (m, 2H), 1.51 (ddd, J = 11.2, 7.3, 3.9 Hz, 1H), 1.24 (qd, J = 12.2, 4.0 Hz, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 658 [M + H].sup.+ III-v-13 [00358] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.83 (t, J = 2.4 Hz, 1H), 10.42 (s, 1H), 8.82 (d, J = 5.8 Hz, 2H), 8.34-8.29 (m, 2H), 8.11 (d, J = 2.5 Hz, 1H), 8.06-8.01 (m, 3H), 7.98 (dd, J = 7.9, 1.8 Hz, 1H), 7.80 (t, J = 5.9 Hz, 1H), 7.64 (d, J = 8.1 Hz, 1H), 7.52 (d, J = 8.9 Hz, 1H), 6.88 (dd, J = 3.1, 1.8 Hz, 1H), 2.99 (t, J = 6.4 Hz, 2H), 2.90 (dt, J = 11.7, 3.6 Hz, 2H), 2.67 (td, J = 11.6, 2.4 Hz, 2H), 2.28 (s, 3H), 2.09 (q, J = 7.6 Hz, 2H), 1.74- 1.63 (m, 2H), 1.51 (ddq, J = 11.0, 7.6, 3.8 Hz, 1H), 1.29-1.18 (m, 2H), 1.00 (t, J = 7.6 Hz, 3H). MS (ESI) m/z: 658 [M + H].sup.+

TABLE-US-00004 TABLE 4 Structure and characterization of compounds IV No. Structure .sup.1H NMR and/or MS data IV-a-1 [00359] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.63 (s, 1H), 9.25 (d, J = 1.5 Hz, 1H), 8.67 (d, J = 0.5 Hz, 1H), 8.62-8.57 (m, 1H), 8.48 (dt, J = 8.0, 1.9 Hz, 1H), 8.25 (s, 1H), 8.22 (d, J = 7.9 Hz, 1H), 7.92 (d, J = 7.8 Hz, 1H), 7.90 (t, J = 2.1 Hz, 1H), 7.74 (t, J = 7.8 Hz, 1H), 7.71 (dd, J = 8.2, 1.1 Hz, 1H), 7.51 (t, J = 8.2 Hz, 1H), 7.47 (dd, J = 7.9, 4.8 Hz, 1H), 7.18 (ddd, J = 8.1, 2.3, 0.8 Hz, 1H), 4.18 (s, 3H). MS (ESI) m/z 491 [M + H].sup.+. IV-a-2 [00360] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.69 (s, 1H), 8.75 (d, J = 0.8 Hz, 1H), 8.68 (d, J = 5.1 Hz, 2H), 8.30 (s, 1H), 8.27 (d, J = 8.2 Hz, 1H), 8.10-8.04 (m, 2H), 8.00-7.97 (m, 1H), 7.94 (t, J = 2.2 Hz, 1H), 7.80 (t, J = 7.8 Hz, 1H), 7.76 (ddd, J = 8.2, 2.0, 0.9 Hz, 1H), 7.56 (t, J = 8.2 Hz, 1H), 7.23 (ddd, J = 8.1, 2.3, 0.9 Hz, 1H), 4.24 (s, 3H). MS (ESI) m/z: 4.91 [M + H].sup.+. IV-a-3 [00361] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.65 (s, 1H), 8.29 (s, 1H), 8.29 (d, J = 0.4 Hz, 1H), 8.27 (d, J = 7.8 Hz, 1H), 7.99 (d, J = 7.8 Hz, 1H), 7.94 (t, J = 2.1 Hz, 1H), 7.81 (t, J = 7.7 Hz, 1H), 7.67-7.64 (m, 1H), 7.48 (t, J = 8.2 Hz, 1H), 7.09 (ddd, J = 8.1, 2.3, 0.9 Hz, 1H), 4.00 (s, 3H), 1.24 (s, 4H), 1.05 (s, 6H). MS (ESI) m/z: 527[M + H].sup.+. IV-b-1 [00362] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.60 (s, 1H), 9.25 (d, J = 1.6 Hz, 1H), 8.73 (s, 1H), 8.63 (dd, J = 4.7, 1.7 Hz, 1H), 8.47 (dt, J = 8.0, 1.9 Hz, 1H), 8.29 (s, 1H), 8.26 (d, J = 7.9 Hz, 1H), 7.95 (d, J = 7.8 Hz, 1H), 7.87 (d, J = 2.0 Hz, 1H), 7.78 (t, J = 7.8 Hz, 1H), 7.70 (dd, J = 8.3, 2.1 Hz, 1H), 7.48 (ddd, J = 8.0, 4.8, 0.6 Hz, 1H), 7.44 (d, J = 8.5 Hz, 1H), 5.75 (s, 1H), 4.24 (s, 3H), 2.14 (s, 3H). MS (ESI) m/z: 505 [M + H].sup.+. IV-b-2 [00363] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.59 (s, 1H), 8.73 (s, 1H), 8.67 (s, 2H), 8.28 (s, 1H), 8.25 (d, J = 7.9 Hz, 1H), 8.03 (d, J = 5.0 Hz, 2H), 7.96 (d, J = 7.8 Hz, 1H), 7.85 (d, J = 2.1 Hz, 1H), 7.78 (t, J = 7.8 Hz, 1H), 7.69 (dd, J = 8.3, 2.2 Hz, 1H), 7.44 (d, J = 8.4 Hz, 1H), 4.24 (s, 3H), 2.12 (s, 3H). MS (ESI) m/z: 505 [M + H].sup.+. IV-b-3 [00364] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 8.28 (s, 1H), 8.27-8.24 (m, 2H), 7.97 (d, J = 7.8 Hz, 1H), 7.83 (d, J = 2.1 Hz, 1H), 7.79 (t, J = 7.8 Hz, 1H), 7.59 (dd, J = 8.3, 2.1 Hz, 1H), 7.36 (d, J = 8.6 Hz, 1H), 4.00 (s, 3H), 3.50-3.41 (m, 3H), 2.45-2.38 (m, 2H), 2.12 (s, 4H), 1.03 (d, J = 3.9 Hz, 6H). MS (ESI) m/z: 541[M + H].sup.+. IV-c-1 [00365] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 9.27 (s, 1H), 8.81 (s, 1H), 8.58 (s, 1H), 8.50 (s, 1H), 8.36-8.15 (m, 3H), 7.85 (s, 1H), 7.68 (s, 1H), 7.53 (s, 1H), 7.41 (s, 2H), 7.20 (s, 1H), 4.17 (s, 3H), 2.35 (s, 3H). MS (ESI) m/z: 505 [M + H].sup.+. IV-c-2 [00366] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.29 (s, 1H), 8.72 (d, J = 0.7 Hz, 1H), 8.69-8.67 (m, 2H), 8.32 (d, J = 1.7 Hz, 1H), 8.29 (d, J = 7.9 Hz, 1H), 8.12- 8.07 (m, 2H), 7.99-7.96 (m, 1H), 7.82-7.76 (m, 1H), 7.51 (d, J = 2.5 Hz, 1H), 7.46 (dd, J = 8.3, 0.9 Hz, 1H), 7.29 (dd, J = 8.3, 2.6 Hz, 1H), 4.23 (d, J = 0.7 Hz, 3H), 2.34 (s, 3H). MS (ESI) m/z: 505 [M + H].sup.+. IV-d-1 [00367] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.64 (s, 1H), 9.24 (dd, J = 2.3, 0.9 Hz, 1H), 8.77 (d, J = 0.8 Hz, 1H), 8.63 (dd, J = 4.8, 1.8 Hz, 1H), 8.46 (dt, J = 8.0, 2.0 Hz, 1H), 8.25 (d, J = 2.0 Hz, 1H), 8.09- 8.01 (m, 3H), 7.79-7.72 (m, 2H), 7.60 (t, J = 8.0 Hz, 1H), 7.55-7.40 (m, 2H), 4.24 (s, 3H). MS (ESI) m/z: 491 [M + H].sup.+. IV-d-2 [00368] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.67 (s, 1H), 8.80 (s, 1H), 8.71 (s, 1H), 8.26 (s, 1H), 8.06 (td, J = 11.2, 10.0, 6.4 Hz, 5H), 7.76 (d, J = 6.1 Hz, 2H), 7.61 (t, J = 8.0 Hz, 1H), 7.47 (d, J = 7.7 Hz, 1H), 4.26 (s, 3H). MS (ESI) m/z: 491[M + H].sup.+. IV-e-1 [00369] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 9.19 (s, 1H), 8.79 (s, 1H), 8.63 (s, 1H), 8.42 (dt, J = 8.0, 2.0 Hz, 1H), 8.23 (d, J = 2.0 Hz, 1H), 8.06 (dd, J = 8.1, 2.0 Hz, 1H), 8.02 (d, J = 1.8 Hz, 1H), 7.99 (dd, J = 7.9, 1.9 Hz, 1H), 7.67-7.62 (m, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.52-7.39 (m, 2H), 4.25 (s, 3H), 2.25 (s, 3H). MS (ESI) m/z: 505 [M + H].sup.+. IV-e-2 [00370] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 8.79 (s, 1H), 8.71-8.60 (m, 2H), 8.23 (d, J = 1.9 Hz, 1H), 8.07 (dt, J = 8.3, 1.3 Hz, 1H), 8.03 (d, J = 1.8 Hz, 1H), 8.00 (dd, J = 8.0, 1.8 Hz, 1H), 7.99- 7.97 (m, 2H), 7.66-7.63 (m, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.49-7.35 (m, 1H), 4.27 (s, 3H), 2.25 (s, 3H). MS (ESI) m/z: 505 [M + H].sup.+. IV-e-3 [00371] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.50 (s, 0H), 8.36 (d, J = 0.7 Hz, 1H), 8.26-8.19 (m, 1H), 8.10- 8.00 (m, 1H), 7.95-7.84 (m, 1H), 7.60 (t, J = 8.0 Hz, 1H), 7.55 (dd, J = 7.9, 1.0 Hz, 1H), 7.46 (ddd, J = 7.8, 1.8, 0.9 Hz, 1H), 4.03 (d, J = 0.6 Hz, 3H), 3.54 (t, J = 4.7 Hz, 4H), 3.47 (s, 4H), 2.21 (s, 3H). MS (ESI) m/z: 513 [M + H].sup.+. IV-e-4 [00372] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.49 (s, 1H), 8.35 (s, 1H), 8.24 (d, J = 2.0 Hz, 1H), 8.08-8.03 (m, 1H), 8.01 (d, J = 1.9 Hz, 1H), 7.92 (dd, J = 7.9, 1.9 Hz, 1H), 7.60 (t, J = 8.0 Hz, 1H), 7.56 (d, J = 8.0 Hz, 1H), 7.46 (d, J = 7.8 Hz, 1H), 4.21 (s, 0H), 4.02 (s, 3H), 3.44 (s, 2H), 3.34 (s, 2H), 2.41 (t, J = 11.8 Hz, 2H), 2.23 (s, 3H), 1.01 (s, 6H). MS (ESI) m/z: 541 [M + H].sup.+. IV-f-1 [00373] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.70 (s, 1H), 9.29 (dd, J = 2.3, 0.8 Hz, 1H), 8.74 (d, J = 0.7 Hz, 1H), 8.65 (dd, J = 4.8, 1.7 Hz, 1H), 8.50 (dt, J = 8.0, 1.9 Hz, 1H), 8.22 (s, 1H), 7.95 (d, J = 8.4 Hz, 1H), 7.61-7.52 (m, 3H), 7.53-7.47 (m, 2H), 4.23 (d, J = 0.6 Hz, 3H), 2.48 (s, 3H). MS (ESI) m/z: 505[M + H].sup.+. IV-f-2 [00374] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.71 (s, 1H), 8.75 (s, 1H), 8.71-8.64 (m, 2H), 8.22 (s, 1H), 8.10- 8.04 (m, 2H), 7.95 (d, J = 8.4 Hz, 1H), 7.64- 7.41 (m, 5H), 4.24 (s, 3), 2.48 (s, 3H). MS (ESI) m/z: 505[M + H].sup.+. IV-g-1 [00375] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 5 10.67 (s, 1H), 9.30 (d, J = 2.2 Hz, 1H), 8.75 (s, 1H), 8.66 (d, J = 4.8 Hz, 1H), 8.50 (d, J = 8.0 Hz, 1H), 7.91 (s, 1H), 7.70 (d, J = 8.3 Hz, 1H), 7.59 (d, J = 2.5 Hz, 1H), 7.56 (dd, J = 8.3, 2.5 Hz, 1H), 7.50 (t, 2H), 7.47 (d, J = 8.2 Hz, 1H), 7.09 (d, J = 8.5 Hz, 1H), 4.24 (s, 3H), 2.49 (s, 3H). MS (ESI) m/z: 521 [M + H].sup.+. IV-g-2 [00376] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.68 (s, 1H), 8.77 (s, 1H), 8.69 (d, J = 6.1 Hz, 2H), 8.08 (d, J = 6.1 Hz, 2H), 7.91 (s, 1H), 7.71-7.68 (m, 1H), 7.61 (d, J = 2.5 Hz, 1H), 7.56 (dd, J = 8.3, 2.6 Hz, 1H), 7.52 (s, 1H), 7.50 (d, J = 4.2 Hz, 1H), 7.47 (d, J = 8.2 Hz, 1H), 4.25 (s, 3H), 2.49 (s, 3H). MS (ESI) m/z: 521 [M + H].sup.+. IV-h-1 [00377] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.67 (s, 1H), 9.29 (d, J = 1.7 Hz, 1H), 8.73 (s, 1H), 8.64 (dd, J = 4.7, 1.7 Hz, 1H), 8.50 (s, 1H), 8.26 (s, 1H), 8.24 (d, J = 8.2 Hz, 1H), 7.95 (t, J = 2.1 Hz, 1H), 7.92 (d, J = 8.1 Hz, 1H), 7.81-772 (m, 1H), 7.56 (s, 1H), 7.49 (dd, J = 8.0, 4.8 Hz, 1H), 7.22 (dd, J = 8.1, 1.7 Hz, 1H), 4.23 (s, 3H), 3.69 (s, 2H), 2.49- 2.41 (m, 8H), 2.25 (s, 3H). MS (ESI) m/z: 603[M + H].sup.+. IV-h-2 [00378] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.66 (s, 1H), 8.73 (s, 1H), 8.68 (dd, J = 4.5, 1.5 Hz, 2H), 8.25 (s, 1H), 8.24 (d, J = 8.2 Hz, 1H), 8.08 (dd, J = 4.5, 1.6 Hz, 2H), 7.95 (t, J = 2.1 Hz, 1H), 7.92 (d, J = 8.1 Hz, 1H), 7.79-7.73 (m, 1H), 7.56 (t, J = 8.2 Hz, 1H), 7.22 (dd, J = 8.1, 1.6 Hz, 1H), 4.24 (s, 3H), 3.67 (s, 2H), 2.47-2.34 (m, 8 H), 2.19 (s, 3H). MS (ESI) m/z: 603[M + H].sup.+. IV-i-1 [00379] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 9.24 (d, J = 1.5 Hz, 1H), 8.73 (s, 1H), 8.63 (dd, J = 4.7, 1.6 Hz, 1H), 8.47 (dt, J = 8.0, 1.9 Hz, 1H), 8.24 (s, 1H), 8.21 (d, J = 8.1 Hz, 1H), 7.91 (d, J = 8.2 Hz, 1H), 7.85 (d, J = 1.9 Hz, 1H), 7.68 (dd, J = 8.3, 2.0 Hz, 1H), 7.52-7.46 (m, 1H), 7.43 (d, J = 8.6 Hz, 1H), 4.23 (s, 3H), 3.66 (s, 2H), 2.45-2.28 (m, 8H), 2.16 (s, 3H), 2.13 (s, 3H). MS (ESI) m/z: 617 [M + H].sup.+. IV-i-2 [00380] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 8.72 (s, 1H), 8.69-8.63 (m, 2H), 8.24 (d, J = 1.8 Hz, 1H), 8.21 (dd, J = 8.2, 1.8 Hz, 1H), 8.06-7.99 (m, 2H), 7.90 (d, J = 8.1 Hz, 1H), 7.86 (d, J = 2.1 Hz, 1H), 7.68 (dd, J = 8.3, 2.2 Hz, 1H), 7.43 (d, J = 8.4 Hz, 1H), 4.24 (s, 3H), 3.65 (s, 2H), 2.43-2.22 (m, 8H), 2.14 (s, 3H), 2.13 (s, 3H). MS (ESI) m/z: 617 [M + H].sup.+. IV-l-1 [00381] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 9.23 (d, J = 2.1 Hz, 1H), 8.77 (s, 1H), 8.62 (dd, J = 4.8, 1.7 Hz, 1H), 8.51-8.44 (m, 1H), 8.19 (d, J = 2.2 Hz, 1H), 8.06-7.99 (m, 3H), 7.77-7.67 (m, 3H), 7.47 (dd, J = 7.9, 4.6 Hz, 1H), 4.24 (s, 3H), 3.55 (s, 2H), 2.42-2.31(m, 8H), 2.15 (s, 3H) MS (ESI) m/z: 603 [M + H].sup.+. IV-l-2 [00382] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.60 (s, 1H), 8.78 (s, 1H), 8.69-8.64 (m, 2H), 8.21 (d, J = 2.2 Hz, 1H), 8.07-8.00 (m, 5H), 7.79-7.72 (m, 2H), 7.70 (d, J = 8.6 Hz, 1H), 4.26 (s, 3H), 3.56 (s, 2H), 2.45-2.34 (m, 8H), (s, 8H), 2.18 (s, 3H). MS (ESI) m/z: 603 [M + H].sup.+. IV-m-1 [00383] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.50 (s, 1H), 9.19 (d, J = 2.1 Hz, 1H), 8.79 (s, 1H), 8.62 (dd, J = 4.8, 1.7 Hz, 1H), 8.42 (dt, J = 8.0, 2.0 Hz, 1H), 8.18 (d, J = 2.2 Hz, 1H), 8.06-7.96 (m, 3H), 7.69 (d, J = 8.6 Hz, 1H), 7.64 (d, J = 8.0 Hz, 1H), 7.47 (dd, J = 8.0, 4.7 Hz, 1H), 4.25 (s, 3H), 3.56 (s, 2H), 2.44-2.29 (s, 8H), 2.25 (s, 3H), 2.17 (s, 3H). MS (ESI) m/z: 617 [M + H].sup.+. IV-m-2 [00384] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.51 (s, 1H), 8.79 (s, 1H), 8.67-8.63 (m, 2H), 8.18 (d, J = 2.2 Hz, 1H), 8.05 (dd, J = 8.6, 2.2 Hz, 1H), 8.02 (d, J = 1.8 Hz, 1H), 7.99 (dd, J = 7.9, 1.8 Hz, 1H), 7.98- 7.96 (m, 2H), 7.68 (d, J = 8.6 Hz, 1H), 7.63 (d, J = 8.1 Hz, 1H), 4.26 (s, 3H), 3.55 (s, 2H), 2.42-2.33 (m, 8H), , 2.24 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 617 [M + H].sup.+. IV-n-1 [00385] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.69 (s, 1H), 9.30 (s, 1H), 8.75 (s, 1H), 8.66 (s, 1H), 8.50 (d, J = 7.0 Hz, 1H), 8.19 (s, 1H), 7.97 (d, J = 8.0 Hz, 1H), 7.69 (d, J = 8.1 Hz, 1H), 7.58 (s, 1H), 7.55 (d, J = 8.1 Hz, 1H), 7.51 (s, 1H), 7.50 (s, 1H), 4.24 (s, 3H), 3.56 (s, 2H), 3.35 (s, 2H), 2.49 (s, 3H), 2.44- 2.37 (m, 6H), 2.22 (s, 3H). MS (ESI) m/z: 617[M + H].sup.+. IV-n-2 [00386] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.71 (s, 1H), 8.75 (s, 1H), 8.68 (d, J = 5.5 Hz, 2H), 8.19 (s, 1H), 8.07 (d, J = 5.8 Hz, 2H), 7.97 (d, J = 8.4 Hz, 1H), 7.68 (d, J = 8.5 Hz, 1H), 7.59 (d, J = 2.3 Hz, 1H), 7.54 (dd, J = 8.3, 2.3 Hz, 1H), 7.49 (d, J = 8.4 Hz, 1H), 4.24 (s, 3H), 3.55 (s, 2H), 3.36 (s, 2H), 2.48 (s, 3H), 2.43-2.29 (m, 6H), 2.19 (s, 3H). MS (ESI) m/z: 617[M + H].sup.+. IV-n-3 [00387] MS (ESI) m/z: 615[M + H].sup.+. IV-n-4 [00388] MS (ESI) m/z: 651 [M + H].sup.+. IV-n-5 [00389] MS (ESI) m/z: 651 [M + H].sup.+. IV-n-6 [00390] MS (ESI) m/z: 631[M + H].sup.+. IV-n-7 [00391] MS (ESI) m/z: 631[M + H].sup.+. IV-n-8 [00392] MS (ESI) m/z: 630 [M + H].sup.+. IV-n-9 [00393] MS (ESI) m/z: 630 [M + H].sup.+. IV-n-10 [00394] MS (ESI) m/z: 605[M + H].sup.+. IV-n-11 [00395] MS (ESI) m/z: 621[M + H].sup.+. IV-o-1 [00396] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 9.29 (d, J = 2.1 Hz, 1H), 8.61-8.55 (m, 2H), 8.51 (s, 1H), 8.10 (d, J = 2.2 Hz, 1H), 7.88 (dd, J = 8.5, 2.2 Hz, 1H), 7.76 (d, J = 8.5 Hz, 1H), 7.71-7.66 (m, 2H), 7.57 (dd, J = 8.7, 2.8 Hz, 1H), 7.48 (dd, J = 8.0, 4.9 Hz, 1H), 4.26 (s, 3H), 3.65 (s, 2H), 2.59-2.49(m, 8H), 2.34 (s, 3H). MS (ESI) m/z: 638 [M + H].sup.+. IV-o-2 [00397] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.92 (s, 1H), 8.82 (s, 1H), 8.76-8.64 (m, 2H), 8.16 (d, J = 2.2 Hz, 1H), 8.12-8.03 (m, 2H), 7.99-7.83 (m, 1H), 7.78 (d, J = 2.9 Hz, 1H), 7.77 (d, J = 8.7 Hz, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.68 (dd, J = 8.8, 2.8 Hz, 1H), 4.25 (s, 3H), 3.56 (s, 2H), 2.43-2.35 (m, 8H), 2.19 (s, 3H). MS (ESI) m/z: 638[M + H].sup.+. IV-o-3 [00398] MS (ESI) m/z: 635 [M + H].sup.+. IV-o-4 [00399] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.95 (s, 1H), 9.53 (s, 1H), 8.79 (s, 1H), 8.19 (t, J = 1.9 Hz, 1H), 8.18-8.13 (m, 2H), 7.97 (dd, J = 8.5, 2.2 Hz, 1H), 7.79 (d, J = 2.8 Hz, 1H), 7.77 (d, J = 8.7 Hz, 1H), 7.71 (d, J = 8.7 Hz, 1H), 7.68 (dd, J = 8.8, 2.8 Hz, 1H), 7.55 (ddd, J = 7.9, 2.3, 1.1 Hz, 1H), 7.50 (t, J = 7.8 Hz, 1H), 4.24 (s, 3H), 3.67 (s, 2H), 3.43- 3.36 (m, 2H), 3.07-2.98 (m, 2H), 2.94-2.87 (m, 2H), 2.80 (s, 3H), 2.45-2.23 (m, 2H). MS (ESI) m/z: 670 [M + H].sup.+. IV-o-5 [00400] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.94 (s, 1H), 9.55 (s, 1H), 8.77 (s, 1H), 8.22 (d, J = 8.6 Hz, 2H), 8.14 (d, J = 2.2 Hz, 1H), 7.99 (dd, J = 8.5, 2.2 Hz, 1H), 7.78 (d, J = 2.8 Hz, 1H), 7.76 (d, J = 8.8 Hz, 1H), 7.72 (d, J = 8.6 Hz, 1H), 7.66 (dd, J = 8.8, 2.8 Hz, 1H), 4.23 (s, 3H), 3.67 (s, 2H), 3.44-3.32 (m, 2H), 3.06-2.97 (m, 2H), 2.94-2.85 (m, 2H), 2.80 (s, 3H), 2.41-2.30 (m, 2H). MS (ESI) m/z: 671 [M + H].sup.+. IV-o-6 [00401] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.90 (s, 1H), 9.59 (s, 1H), 8.73 (s, 1H), 8.15 (d, J = 2.2 Hz, 1H), 7.92 (dd, J = 8.6 2.2 Hz, 1H), 7.79-7.61 (m, 6H), 7.23 (t, J = 7.9 Hz, 1H), 6.86 (dd, J = 7.9, 2.5 Hz, 1H), 4.21 (s, 3H), 3.55 (s, 2H), 3.17 (s, 3H), 2.45- 2.24(m, 8H) MS (ESI) m/z: 652 [M + H].sup.+. IV-o-7 [00402] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.90 (s, 1H), 9.92 (s, 1H), 8.68 (s, 1H), 8.16 (d, J = 2.3 Hz, 1H), 8.08-8.04 (m, 2H), 7.92 (dd, J = 8.5, 2.2 Hz, 1H), 7.75 (d, J = 1.7 Hz, 1H) 7.74 (d, J = 4.2 Hz, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.64 (dd, J = 8.8, 2.8 Hz, 1H), 6.92-6.63 (m, 2H), 4.19 (s, 3H), 3.56 (d, J = 2.8 Hz, 2H), 2.44-2.30(m, 8H), 2.17 (s, 3H). MS (ESI) m/z: 652 [M + H].sup.+. IV-o-8 [00403] MS (ESI) m/z: 650 [M + H].sup.+. IV-o-9 [00404] MS (ESI) m/z: 650[M + H].sup.+. IV-o-10 [00405] MS (ESI) m/z: 626[M + H].sup.+. IV-o-11 [00406] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.91 (s, 1H), 8.72 (s, 1H), 8.15 (d, J = 2.2 Hz, 1H), 8.12 (dd, J = 3.1, 1.2 Hz, 1H), 7.94 (dd, J = 8.5, 2.2 Hz, 1H), 7.76 (d, J = 2.8 Hz, 1H), 7.74 (d, J = 8.8 Hz, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.68 (dd, J = 5.0, 1.2 Hz, 1H), 7.64 (dd, J = 8.7, 2.8 Hz, 1H), 7.60 (dd, J = 5.0, 3.1 Hz, 1H), 4.21 (s, 3H), 3.58 (s, 2H), 2.48- 2.36(m, 8H), 2.28 (s, 3H). MS (ESI) m/z: 643 [M + H].sup.+. IV-o-12 [00407] MS (ESI) m/z: 539 [M + H]+. IV-r-1 [00408] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.70 (s, 1H), 8.76 (s, 1H), 8.70-8.65 (m, 2H), 8.14 (s, 1H), 8.10- 8.03 (m, 2H), 7.92 (s, 1H), 7.62 (d, J = 2.5 Hz, 1H), 7.54 (dd, J = 8.3, 2.5 Hz, 1H), 7.50 (d, J = 8.4 Hz, 1H), 7.35 (s, 1H), 4.24 (s, 3H), 3.53 (s, 2H), 2.49 (s, 3H), 2.45-2.29 (m, 8H), 2.19 (s, 3H). MS (ESI) m/z: 617[M + H].sup.+. IV-t-1 [00409] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.87 (s, 1H), 9.38 (s, 1H), 8.77 (s, 2H), 8.52 (d, J = 8.0 Hz, 1H), 8.22 (s, 1H), 8.19 (s, 1H), 8.11 (s, 1H), 7.73 (s, 1H), 7.64 (d, J = 2.5 Hz, 1H), 7.58 (dd, J = 8.3, 2.5 Hz, 1H), 7.54 (s, 1H), 7.52 (s, 1H), 7.49 (s, 1H), 4.24 (s, 3H), 2.17 (s, 3H), 1.34 (s, 3H). MS (ESI) m/z: 585[M + H].sup.+.

TABLE-US-00005 TABLE 5 Structure and characterization of compounds V No. Structure .sup.1H NMR and/or MS data V-a-1 [00410] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.98 (s, 1H), 10.57 (s, 1H), 9.22 (s, 1H), 8.59 (d, J = 4.3 Hz, 1H), 8.36 (d, J = 7.6 Hz, 1H), 8.30-8.21 (m, 2H), 7.97 (d, J = 7.8 Hz, 1H), 7.78 (t, J = 7.9 Hz, 1H), 7.74-7.69 (m, 2H), 7.52-7.43 (m, 3H), 7.30 (s, 1H), 7.04 (d, J = 7.9 Hz, 1H), 6.12 (s, 1H), MS (ESI) m/z: 475 [M + H].sup.+. V-a-2 [00411] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.04 (s, 1H), 10.58 (s, 1H), 8.66 (d, J = 6.0 Hz, 2H), 8.27 (s, 1H), 8.24 (d, J = 7.9 Hz, 1H), 8.00 (d, J = 6.1 Hz, 2H), 7.97 (d, J = 7.8 Hz, 1H), 7.78 (t, J = 7.8 Hz, 1H), 7.75-7.69 (m, 2H), 7.52-7.46 (m, 2H), 7.37 (s, 1H), 7.04 (dd, J = 8.1, 2.3 Hz, 1H), 6.15 (dd, J = 3.3, 1.9 Hz, 1H). MS (ESI) m/z: 475 [M + H].sup.+. V-a-3 [00412] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 9.29 (d, J = 1.7 Hz, 1H), 8.60 (dd, J = 4.7, 1.6 Hz, 1H), 8.44 (ddd, J = 8.0, 2.2, 1.7 Hz, 1H), 8.27 (s, 1H), 8.24 (d, J = 7.8 Hz, 1H), 7.97 (d, J = 7.8 Hz, 1H), 7.78 (t, J = 7.8 Hz, 1H), 7.75-7.67 (m, 2H), 7.55-7.44 (m, 3H), 7.34 (s, 1H), 7.03 (ddd, J = 8.1, 2.4, 0.8 Hz, 1H), 6.11 (d, J = 3.5 Hz, 1H), 3.91 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-a-4 [00413] .sup.1H NMR (600 MHz, Chloroform-d) 9.02 (s, 1H), 8.55 (dd, J = 4.6, 1.6 Hz, 2H), 8.14 (s, 1H), 8.06 (d, J = 7.8 Hz, 1H), 7.90 (dd, J = 4.6, 1.6 Hz, 2H), 7.74 (d, J = 7.8 Hz, 1H), 7.68-7.57 (m, 2H), 7.54 (t, J = 7.8 Hz, 1H), 7.39 (t, J = 8.1 Hz, 1H), 7.14 (d, J = 3.5 Hz, 1H), 7.10 (s, 1H), 6.98 (ddd, J = 8.1, 2.3, 0.7 Hz, 1H), 6.30 (d, J = 3.4 Hz, 1H), 3.94 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-b-1 [00414] .sup.1H NMR (600 MHz, Chloroform-d) 9.18 (d, J = 1.6 Hz, 1H), 8.57 (d, J = 4.6 Hz, 1H), 8.29 (d, J = 8.0 Hz, 1H), 8.18 (s, 1H), 8.12 (s, 1H), 8.05 (d, J = 7.8 Hz, 1H), 7.79 (d, J = 7.8 Hz, 1H), 7.60 (t, J = 7.8 Hz, 1H), 7.56 (d, J = 1.6 Hz, 1H), 7.50 (dd, J = 8.3, 1.8 Hz, 1H), 7.37-7.32 (m, 2H), 7.27 (d, J = 3.6 Hz, 1H), 6.93 (s, 1H), 6.41 (d, J = 3.6 Hz, 1H), 2.27 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-b-2 [00415] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.01 (s, 1H), 10.50 (s, 1H), 8.65 (dd, J = 4.6, 1.5 Hz, 2H), 8.25 (s, 1H), 8.22 (d, J = 8.0 Hz, 1H), 7.98-7.93 (m, 3H), 7.76 (t, J = 7.8 Hz, 1H), 7.69 (dd, J = 8.3, 2.0 Hz, 1H), 7.62 (d, J = 2.0 Hz, 1H), 7.48-7.46 (m, 1H), 7.42 (d, J = 8.4 Hz, 1H), 7.22 (s, 1H), 6.08 (dd, J = 3.4, 1.9 Hz, 1H), 2.22 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-b-3 [00416] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.50 (s, 1H), 9.26 (d, J = 2.0 Hz, 1H), 8.60 (dd, J = 4.7, 1.3 Hz, 1H), 8.41 (d, J = 8.0 Hz, 1H), 8.25 (s, 1H), 8.22 (d, J = 7.9 Hz, 1H), 7.95 (d, J = 7.8 Hz, 1H), 7.76 (t, J = 7.8 Hz, 1H), 7.72-7.67 (m, 1H), 7.63 (d, J = 2.1 Hz, 1H), 7.50 (dd, J = 7.9, 4.8 Hz, 1H), 7.47 (d, J = 3.5 Hz, 1H), 7.41 (d, J = 8.4 Hz, 1H), 7.19 (s, 1H), 6.04 (d, J = 3.5 Hz, 1H), 3.90 (s, 3H), 2.21 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-b-4 [00417] .sup.1H NMR (600 MHz, Chloroform-d) 8.88 (s, 1H), 8.52 (d, J = 3.7 Hz, 2H), 8.10 (s, 1H), 8.02 (d, J = 7.8 Hz, 1H), 7.82 (d, J = 5.6 Hz, 2H), 7.71 (d, J = 7.8 Hz, 1H), 7.55 (dd, J = 8.2, 1.7 Hz, 1H), 7.50 (t, J = 7.8 Hz, 1H), 7.45 (d, J = 1.6 Hz, 1H), 7.28 (d, J = 8.3 Hz, 1H), 7.11 (d, J = 3.5 Hz, 1H), 6.92 (s, 1H), 6.26 (d, J = 3.4 Hz, 1H), 3.92 (s, 3H), 2.22 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-c-1 [00418] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.95 (s, 1H), 10.21 (s, 1H), 9.19 (s, 1H), 8.59 (d, J = 4.5 Hz, 1H), 8.37-8.33 (m, 1H), 8.30 (s. 1H), 8.27 (d, J = 7.9 Hz, 1H), 7.97 (d, J = 7.7 Hz, 1H), 7.78 (t, J = 7.8 Hz, 1H), 7.49 (dd, J = 7.9, 4.7 Hz, 1H), 7.45- 7.42 (m, 1H), 7.40 (d, J = 8.4 Hz, 1H), 7.33 (d, J = 2.4 Hz, 1H), 7.21 (s, 1H), 7.11 (dd, J = 8.3, 2.6 Hz, 1H), 6.16 (dd, J = 3.4, 2.0 Hz, 1H), 2.30 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-c-2 [00419] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 8.59 (d, J = 5.7 Hz, 2H), 8.31 (s, 1H), 8.25 (d, J = 7.9 Hz, 1H), 8.04 (d, J = 6.2 Hz, 2H), 7.92 (d, J = 7.7 Hz, 1H), 7.75 (t, J = 7.9 Hz, 1H), 7.43 (d, J = 8.4 Hz, 1H), 7.38 (d, J = 3.5 Hz, 1H), 7.35 (d, J = 2.3 Hz, 1H), 7.22 (s, 1H), 7.11 (dd, J = 8.3, 2.5 Hz, 1H), 6.38 (d, J = 3.5 Hz, 1H), 2.39 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-c-3 [00420] .sup.1H NMR (600 MHz, Chloroform-d) 9.47 (s, 1H), 9.08 (d, J = 7.0 Hz, 1H), 8.76 (s, 1H), 8.40 (s, 1H), 8.20 (s, 1H), 8.15 (d, J = 7.4 Hz, 1H), 7.89 (s, 1H), 7.85-7.77 (m, 2H), 7.65 (t, J = 7.8 Hz, 1H), 7.35 (d, J = 8.2 Hz, 1H), 7.22 (d, J = 3.4 Hz, 1H), 7.09 (s, 1H), 7.04 (dd, J = 8.2, 2.3 Hz, 1H), 6.53 (d, J = 3.4 Hz, 1H), 3.96 (s, 3H), 2.42 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-c-4 [00421] .sup.1H NMR (600 MHz, Chloroform-d) 8.78 (s, 2H), 8.54 (s, 2H), 8.16 (s, 1H), 8.12-8.07 (m, 2H), 7.92 (d, J = 1.7 Hz, 1H), 7.84 (d, J = 7.7 Hz, 1H), 7.67 (t, J = 7.8 Hz, 1H), 7.35 (d, J = 8.3 Hz, 1H), 7.29 (d, J = 4.8 Hz, 2H), 7.02 (dd, J = 8.2, 2.3 Hz, 1H), 6.48 (d, J = 3.3 Hz, 1H), 3.99 (s, 3H), 2.44 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-d-1 [00422] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 9.11 (d, J = 1.7 Hz, 1H), 8.49 (dd, J = 4.8, 1.4 Hz, 1H), 8.33-8.28 (m, 1H), 8.13 (s, 1H), 7.91 (d, J = 8.1 Hz, 1H), 7.86 (d, J = 8.2 Hz, 1H), 7.83-7.81 (m, 1H), 7.58 (t, J = 7.9 Hz, 1H), 7.50 (t, J = 8.0 Hz, 1H), 7.45 (dd, J = 8.0, 4.9 Hz, 1H), 7.42-7.39 (m, 2H), 7.31 (d, J = 3.5 Hz, 1H), 7.31 (d, J = 3.5 Hz, 1H), 7.08 (s, 1H), 7.08 (s, 1H), 6.20 (d, J = 3.5 Hz, 1H). MS (ESI) m/z: 475 [M + H].sup.+. V-d-2 [00423] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.08 (s, 1H), 10.60 (s, 1H), 8.65 (dd, J = 4.6, 1.6 Hz, 2H), 8.24 (s, 1H), 8.05 (d, J = 8.5 Hz, 1H), 7.99 (dd, J = 4.6, 1.6 Hz, 2H), 7.93 (d, J = 7.8 Hz, 1H), 7.87 (s, 1H), 7.67 (t, J = 7.9 Hz, 1H), 7.60 (t, J = 8.0 Hz, 1H), 7.52-7.48 (m, 2H), 7.46 (d, J = 7.8 Hz, 1H), 7.35 (s, 1H), 6.12 (dd, J = 3.1, 1.4 Hz, 1H). MS (ESI) m/z: 475 [M + H].sup.+. V-d-3 [00424] .sup.1H NMR (600 MHz, Chloroform-d) 9.16 (d, J = 2.0 Hz, 1H), 8.96 (s, 1H), 8.50 (dd, J = 4.8, 1.4 Hz, 1H), 8.23 (dt, J = 8.0, 1.9 Hz, 1H), 7.96 (s, 1H), 7.86 (d, J = 8.2 Hz, 1H), 7.79-7.77 (m, 1H), 7.76- 7.74 (m, 1H), 7.50 (t, J = 7.9 Hz, 1H), 7.43 (t, J = 8.0 Hz, 1H), 7.37 (d, J = 7.8 Hz, 1H), 7.36-7.33 (m, 1H), 7.31-7.29 (m, 1H), 7.08 (d, J = 3.5 Hz, 1H), 6.96 (s, 1H), 6.17 (d, J = 3.5 Hz, 1H), 3.91 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-d-4 [00425] .sup.1H NMR (600 MHz, Chloroform-d) 8.81 (s, 1H), 8.57 (dd, J = 4.7, 1.4 Hz, 2H), 7.96 (s, 1H), 7.88- 7.85 (m, 3H), 1.6 Hz, 3H), 7.80 (ddd, J = 7.7, 1.5, 0.9 Hz, 1H), 7.75-7.73 (m, 1H), 7.55 (t, J = 7.9 Hz, 1H), 7.46 (t, J = 8.0 Hz, 1H), 7.38 (ddd, J = 7.0, 5.0, 3.2 Hz, 2H), 7.16 (d, J = 3.5 Hz, 1H), 7.06 (s, 1H), 6.20 (d, J = 3.5 Hz, 1H), 3.97 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-e-1 [00426] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.98 (s, 1H), 10.49 (s, 1H), 9.17 (d, J = 2.2 Hz, 1H), 8.58 (dd, J = 4.7, 1.6 Hz, 1H), 8.33-8.29 (m, 1H), 8.20 (s, 1H), 8.03 (d, J = 8.1 Hz, 1H), 7.93 (dd, J = 7.9, 1.7 Hz, 1H), 7.82 (d, J = 1.6 Hz, 1H), 7.64-7.55 (m, 2H), 7.48 (dd, J = 8.0, 4.7 Hz, 1H), 7.45-7.41 (m, 2H), 7.08 (s, 1H), 6.03 (dd, J = 3.4, 2.0 Hz, 1H), 2.31 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-e-2 [00427] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.05 (s, 1H), 10.49 (s, 1H), 8.64 (dd, J = 4.5, 1.6 Hz, 2H), 8.20 (s, 1H), 8.03 (d, J = 8.9 Hz, 1H), 7.97-7.90 (m, 3H), 7.82 (d, J = 1.7 Hz, 1H), 7.62 (d, J = 8.3 Hz, 1H), 7.58 (t, J = 8.0 Hz, 1H), 7.48 (dd, J = 3.4, 2.6 Hz, 1H), 7.44 (d, J = 7.9 Hz, 1H), 7.16 (s, 1H), 6.05 (dd, J = 3.4, 1.9 Hz, 1H), 2.31 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-e-3 [00428] .sup.1H NMR (600 MHz, Chloroform-d) 9.18 (s, 1H), 9.13 (dd, J = 2.3, 0.7 Hz, 1H), 8.45 (dd, J = 4.8, 1.6 Hz, 1H), 8.17-8.13 (m, 1H), 7.95 (s, 1H), 7.82 (d, J = 8.2 Hz, 1H), 7.78 (dd, J = 7.9, 1.8 Hz, 1H), 7.72 (d, J = 1.8 Hz, 1H), 7.41-7.35 (m, 2H), 7.33 (d, J = 7.8 Hz, 1H), 7.22 (ddd, J = 8.0, 4.8, 0.7 Hz, 1H), 7.05 (d, J = 3.5 Hz, 1H), 6.78 (s, 1H), 6.11 (d, J = 3.5 Hz, 1H), 3.89 (s, 3H), 2.31 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-e-4 [00429] .sup.1H NMR (600 MHz, Chloroform-d) 9.41 (s, 1H), 8.46 (dd, J = 4.6, 1.5 Hz, 2H), 7.95 (s, 1H), 7.84- 7.79 (m, 2H), 7.77 (dd, J = 4.6, 1.6 Hz, 2H), 7.73 (d, J = 1.6 Hz, 1H), 7.41-7.35 (m, 2H), 7.32 (d, J = 7.8 Hz, 1H), 7.11 (d, J = 3.5 Hz, 1H), 6.85 (s, 1H), 6.12 (d, J = 3.5 Hz, 1H), 3.93 (s, 3H), 2.32 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-f-1 [00430] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.98 (s, 1H), 10.66 (s, 1H), 9.19 (d, J = 1.9 Hz, 1H), 8.59 (dd, J = 4.7, 1.5 Hz, 1H), 8.36-8.31 (m, 1H), 8.23 (s, 1H), 7.94 (d, J = 8.3 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.49 (dd, J = 7.7, 5.0 Hz, 1H), 7.47-7.40 (m, 4H), 7.29 (dd, J = 8.3, 2.6 Hz, 1H), 7.21 (s, 1H), 6.16 (dd, J = 3.3, 1.9 Hz, 1H), 2.44 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-f-2 [00431] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.04 (s, 1H), 10.66 (s, 1H), 8.66 (d, J = 6.0 Hz, 2H), 8.23 (s, 1H), 7.97 (d, J = 6.1 Hz, 2H), 7.94 (d, J = 8.2 Hz, 1H), 7.59 (t, J = 8.0 Hz, 1H), 7.52-7.48 (m, 1H), 7.47-7.40 (m, 3H), 7.33-7.27 (m, 2H), 6.18 (dd, J = 3.1, 1.8 Hz, 1H), 2.45 (s, 3H). MS (ESI) m/z: 489 [M + H].sup.+. V-f-3 [00432] .sup.1H NMR (600 MHz, Chloroform-d) 9.17 (d, J = 2.0 Hz, 1H), 8.74 (s, 1H), 8.56 (dd, J = 4.7, 1.2 Hz, 1H), 8.27 (d, J = 8.0 Hz, 1H), 7.97 (s, 1H), 7.90 (d, J = 7.9 Hz, 1H), 7.46 (t, J = 8.0 Hz, 1H), 7.40- 7.36 (m, 2H), 7.36-7.34 (m, 1H), 7.33-7.30 (m, 1H), 7.18 (dd, J = 8.3, 2.5 Hz, 1H), 7.10 (d, J = 3.5 Hz, 1H), 6.95 (s, 1H), 6.24 (d, J = 3.4 Hz, 1H), 3.93 (s, 3H), 2.56 (d, J = 8.9 Hz, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-f-4 [00433] .sup.1H NMR (600 MHz, Chloroform-d) 8.73 (s, 1H), 8.53 (d, J = 6.0 Hz, 2H), 7.94 (s, 1H), 7.88-7.82 (m, 3H), 7.46 (t, J = 8.0 Hz, 1H), 7.40 (d, J = 7.8 Hz, 1H), 7.34 (dd, J = 6.7, 5.8 Hz, 2H), 7.20 (dd, J = 8.3, 2.6 Hz, 1H), 7.16 (d, J = 3.5 Hz, 1H), 7.01 (s, 1H), 6.27 (d, J = 3.5 Hz, 1H), 3.95 (s, 3H), 2.57 (s, 3H). MS (ESI) m/z: 503 [M + H].sup.+. V-h-1 [00434] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.04 (s, 1H), 10.55 (s, 1H), 8.65 (dd, J = 4.6, 1.5 Hz, 2H), 8.21 (s, 1H), 8.21-8.18 (m, 1H), 7.99 (dd, J = 4.6, 1.6 Hz, 2H), 7.90 (d, J = 8.1 Hz, 1H), 7.73-7.69 (m, 2H), 7.48 (dt, J = 14.3, 5.3 Hz, 2H), 7.36 (s, 1H), 7.09-6.95 (m, 1H), 6.15 (dd, J = 3.4, 1.9 Hz, 1H), 3.66 (s, 2H), 2.41 (s, 8H), 2.18 (s, 3H). MS (ESI) m/z: 587 [M + H].sup.+. V-l-1 [00435] .sup.1H NMR (600 MHz, Chloroform-d) 11.51 (s. 1H), 9.19 (d, J = 1.9 Hz, 1H), 8.78 (s, 1H), 8.58 (dd, J = 4.8, 1.5 Hz, 1H), 8.14-8.08 (m, 1H),, 7.90- 7.84 (m, 2H), 7.81-7.76 (m, 2H), 7.72 (d, J = 8.2 Hz, 1H), 7.52 (t, J = 7.9 Hz, 1H), 7.39-7.30 (m, 2H), 7.09 (dd, J = 3.3, 2.4 Hz, 1H), 6.93 (s, 1H), 6.18 (dd, J = 3.4, 1.9 Hz, 1H), 3.61 (s, 2H), 2.51 (s, 8H), 2.31 (s, 3H). MS (ESI) m/z: 588 [M + H].sup.+. V-l-2 [00436] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.08 (s, 1H), 10.55 (s, 1H), 8.65 (d, J = 6.0 Hz, 2H), 8.19 (d, J = 2.1 Hz, 1H), 8.03 (d, J = 8.7 Hz, 1H), 7.99 (d, J = 6.1 Hz, 2H), 7.92 (d, J = 7.5 Hz, 1H), 7.86 (s, 1H), 7.70 (d, J = 8.4 Hz, 1H), 7.66 (t, J = 8.0 Hz, 1H), 7.52-7.47 (m, 2H), 7.35 (s, 1H), 6.11 (dd, J = 3.3, 1.9 Hz, 1H), 3.57 (s, 2H), 2.40 (m, 8H), 2.19 (s, 3H). MS (ESI) m/z: 588 [M + H].sup.+. V-l-3 [00437] .sup.1H NMR (600 MHz, Chloroform-d) 9.19 (d, J = 1.7 Hz, 1H), 8.56 (d, J = 4.7 Hz, 1H), 8.44 (s, 1H), 8.29 (d, J = 8.0 Hz, 1H), 7.90-7.84 (m, 2H), 7.79- 7.74 (m, 2H), 7.73 (s, 1H), 7.54 (t, J = 7.9 Hz, 1H), 7.40-7.32 (m, 2H), 7.12 (d, J = 3.4 Hz, 1H), 7.01 (s, 1H), 6.21 (d, J = 3.4 Hz, 1H), 3.95 (s, 3H), 3.63 (s, 2H), 2.51 (s, 8H), 2.30 (s, 3H). MS (ESI) m/z: 601 [M + H].sup.+. V-l-4 [00438] .sup.1H NMR (600 MHz, Chloroform-d) 8.87 (s, 1H), 8.55 (dd, J = 4.6, 1.5 Hz, 2H), 7.89-7.83 (m, 4H), 7.82-7.78 (m, 1H), 7.74 (dd, J = 4.7, 2.6 Hz, 2H), 7.54 (t, J = 7.9 Hz, 1H), 7.37 (ddd, J = 8.1, 2.3, 0.8 Hz, 1H), 7.15 (d, J = 3.5 Hz, 1H), 7.04 (s, 1H), 6.19 (d, J = 3.5 Hz, 1H), 3.96 (s, 3H), 3.62 (s, 2H), 2.45 (m, J = 58.3 Hz, 8H), 2.30 (s, 3H). MS (ESI) m/z: 601 [M + H].sup.+. V-m-1 [00439] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.98 (s, 1H), 10.44 (s, 1H), 9.19-9.15 (m, 1H), 8.58 (dd, J = 4.7, 1.6 Hz, 1H), 8.33-8.28 (m, 1H), 8.16 (d, J = 2.1 Hz, 1H), 8.01 (dd, J = 8.6, 2.0 Hz, 1H), 7.92 (dd, J = 7.9, 1.7 Hz, 1H), 7.81 (d, J = 1.7 Hz, 1H), 7.68 (d, J = 8.7 Hz, 1H), 7.61 (d, J = 8.1 Hz, 1H), 7.48 (ddd, J = 8.0, 4.8, 0.8 Hz, 1H), 7.43 (dd, J = 3.4, 2.5 Hz, 1H), 7.08 (s, 1H), 6.03 (dd, J = 3.4, 2.0 Hz, 1H), 3.55 (s, 2H), 2.47-2.27 (m, 11H), 2.18 (s, 3H). MS (ESI) m/z: 602 [M + H].sup.+. V-m-2 [00440] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.05 (s, 1H), 10.45 (s, 1H), 8.64 (dd, J = 4.5, 1.6 Hz, 2H), 8.16 (d, J = 2.1 Hz, 1H), 8.01 (dd, J = 8.5, 2.0 Hz, 1H), 7.97-7.91 (m, 3H), 7.82 (d, J = 1.5 Hz, 1H), 7.68 (d, J = 8.6 Hz, 1H), 7.61 (d, J = 8.1 Hz, 1H), 7.49- 7.46 (m, 1H), 7.16 (s, 1H), 6.05 (dd, J = 3.4, 1.8 Hz, 1H), 3.54 (s, 2H), 2.30 (m, 11H), 2.16 (s, 3H). MS (ESI) m/z: 602 [M + H].sup.+. V-m-3 [00441] .sup.1H NMR (600 MHz, Chloroform-d) 9.15 (s, 1H), 8.57-8.50 (m, 2H), 8.23 (d, J = 7.9 Hz, 1H), 7.87- 7.82 (m, 2H), 7.76 (dd, J = 7.9, 1.3 Hz, 1H), 7.72 (d, J = 8.2 Hz, 1H), 7.68 (s, 1H), 7.44 (d, J = 7.9 Hz, 1H), 7.31 (d, J = 5.0 Hz, 1H), 7.09 (d, J = 3.4 Hz, 1H), 6.83 (s, 1H), 6.17 (d, J = 3.2 Hz, 1H), 3.93 (s, 3H), 3.61 (s, 2H), 2.50 (m, 8H), 2.34 (s, 3H), 2.30 (s, 3H). MS (ESI) m/z: 615 [M + H].sup.+. V-m-4 [00442] .sup.1H NMR (600 MHz, Chloroform-d) 8.60 (d, J = 5.6 Hz, 2H), 8.41 (s, 1H), 7.89-7.82 (m, 4H), 7.78 (d, J = 8.0 Hz, 1H), 7.72 (d, J = 8.5 Hz, 1H), 7.67 (s, 1H), 7.48 (d, J = 7.9 Hz, 1H), 7.16 (d, J = 3.4 Hz, 1H), 6.93 (s, 1H), 6.19 (d, J = 3.4 Hz, 1H), 3.98 (s, 3H), 3.63 (s, 2H), 2.54 (m, 8H), 2.36 (s, 3H), 2.35 (s, 3H). MS (ESI) m/z: 615 [M + H].sup.+. V-n-1 [00443] .sup.1H NMR (600 MHz, Chloroform-d) 11.42 (s, 1H), 9.15 (d, J = 1.9 Hz, 1H), 8.59 (dd, J = 4.7, 1.4 Hz, 1H), 8.54 (s, 1H), 8.10 (d, J = 8.0 Hz, 1H), 7.89- 7.81 (m, 2H), 7.75 (d, J = 8.5 Hz, 1H), 7.39-7.33 (m, 2H), 7.31 (d, J = 8.4 Hz, 1H), 7.18 (dd, J = 8.3, 2.5 Hz, 1H), 7.08-7.05 (m, 1H), 6.90 (s, 1H), 6.19 (d, J = 2.2 Hz, 1H), 3.62 (s, 2H), 2.59-2.36 (m, 11H), 2.31 (s, 3H). MS (ESI) m/z: 602 [M + H].sup.+. V-n-2 [00444] .sup.1H NMR (600 MHz, Chloroform-d) 11.27 (s, 1H), 8.96 (s, 1H), 8.56 (d, J = 5.9 Hz, 2H), 7.91 (d, J = 8.2 Hz, 1H), 7.86 (s, 1H), 7.76 (d, J = 8.5 Hz, 1H), 7.67 (d, J = 5.8 Hz, 2H), 7.40 (d, J = 2.2 Hz, 1H), 7.34 (d, J = 8.4 Hz, 1H), 7.20 (dd, J = 8.3, 2.5 Hz, 1H), 7.09-7.05 (m, 1H), 6.88 (s, 1H), 6.32 (dd, J = 3.2, 2.0 Hz, 1H), 3.62 (s, 2H), 2.65-2.40 (m, 11H), 2.30 (s, 3H). MS (ESI) m/z: 602 [M + H].sup.+. V-n-3 [00445] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.89 (s, 1H), 10.66 (s, 1H), 8.18 (d, J = 1.8 Hz, 1H), 7.98 (dt, J = 10.0, 2.6 Hz, 2H), 7.68 (d, J = 8.5 Hz, 1H), 7.48- 7.44 (m, 2H), 7.43-7.39 (m, 3H), 7.38 (t, J = 4.6 Hz, 1H), 7.29 (dd, J = 8.3, 2.6 Hz, 1H), 7.10 (s, 1H), 6.17 (dd, J = 3.4, 2.0 Hz, 1H), 3.63 (s, 2H), 3.36 (s, 6H), 3.18 (s, 2H), 2.71 (s, 3H), 2.43 (s, 3H). MS (ESI) m/z: 600 [M + H].sup.+. V-n-4 [00446] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.92 (d, J = 33.9 Hz, 1H), 10.67 (s, 1H), 8.18 (d, J = 1.7 Hz, 1H), 8.08 (t, J = 1.8 Hz, 1H), 7.96 (d, J = 7.1 Hz, 1H), 7.94-7.90 (m, 1H), 7.68 (d, J = 8.6 Hz, 1H), 7.48 (t, J = 7.8 Hz, 1H), 7.44 (ddd, J = 5.9, 2.7, 1.8 Hz, 2H), 7.40 (dd, J = 9.3, 5.5 Hz, 2H), 7.28 (dd, J = 8.3, 2.6 Hz, 1H), 7.19 (s, 1H), 6.14 (dt, J = 27.9, 13.9 Hz, 1H), 3.64 (s, 2H), 3.40 (s, 6H), 3.17 (s, 2H), 2.75 (s, 3H), 2.41 (d, J = 11.0 Hz, 3H). MS (ESI) m/z: 635 [M + H].sup.+. V-n-5 [00447] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.92 (s, 1H), 10.66 (s, 1H), 8.18 (s, 1H), 8.02 (d, J = 8.5 Hz, 2H), 7.98 (d, J = 8.2 Hz, 1H), 7.69 (d, J = 8.5 Hz, 1H), 7.51 (d, J = 8.5 Hz, 2H), 7.45-7.39 (m, 3H), 7.29 (dd, J = 8.3, 2.3 Hz, 1H), 7.13 (s, 1H), 6.17 (s, 1H), 3.65 (s, 2H), 3.02 (s, 2H), 2.89 (d, J = 10.5 Hz, 2H), 2.79 (s, 3H), 2.51 (s, 2H), 2.43 (s, 3H), 2.39 (d, J = 14.6 Hz, 2H). MS (ESI) m/z: 635 [M + H].sup.+. V-n-6 [00448] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.87 (s, 1H), 10.69 (s, 1H), 8.19 (d, J = 1.7 Hz, 1H), 7.96 (d, J = 8.4 Hz, 1H), 7.68 (d, J = 8.6 Hz, 1H), 7.40 (dd, J = 4.7, 2.6 Hz, 2H), 7.38 (d, J = 2.6 Hz, 2H), 7.36- 7.35 (m, 1H), 7.35-7.33 (m, 1H), 7.28 (d, J = 2.6 Hz, 1H), 7.26 (d, J = 2.6 Hz, 1H), 6.98 (s, 1H), 6.78 (ddd, J = 8.0, 2.5, 0.9 Hz, 1H), 6.19 (dd, J = 3.4, 2.0 Hz, 1H), 3.64 (s, 2H), 3.43-3.33 (m, 2H), 3.03 (d, J = 21.5 Hz, 2H), 2.87 (d, J = 10.6 Hz, 2H), 2.78 (s, 3H), 2.42 (s, 3H), 2.40-2.36 (m, 2H). MS (ESI) m/z: 616 [M + H].sup.+. V-n-7 [00449] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.78 (s, 1H), 10.66 (s, 1H), 9.85 (s, 1H), 8.18 (d, J = 1.6 Hz, 1H), 7.98 (d, J = 8.5 Hz, 1H), 7.86-7.77 (m, 2H), 7.69 (d, J = 8.6 Hz, 1H), 7.41 (d, J = 8.5 Hz, 1H), 7.38 (d, J = 2.6 Hz, 1H), 7.34 (dd, J = 3.3, 2.6 Hz, 1H), 7.27 (s, 2H), 6.84 (m, 2H), 6.13 (dd, J = 3.4, 2.0 Hz, 1H), 3.66 (s, 2H), 3.40 (d, J = 10.8 Hz, 2H), 3.01 (d, J = 15.4 Hz, 2H), 2.90 (d, J = 11.1 Hz, 2H), 2.80 (s, 3H), 2.43 (s, 3H), 2.40-2.33 (m, 2H). MS (ESI) m/z: 616 [M + H].sup.+. V-n-8 [00450] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.81 (s, 1H), 10.64 (s, 1H), 8.18 (d, J = 1.6 Hz, 1H), 7.95 (d, J = 8.3 Hz, 1H), 7.68 (d, J = 8.6 Hz, 1H), 7.44-7.36 (m, 1H), 7.27 (dd, J = 8.3, 2.6 Hz, 1H), 7.22 (d, J = 1.7 Hz, 1H), 7.11-7.03 (m, 1H), 6.95 (s, 1H), 6.65-6.52 (m, 1H), 6.28-6.10 (m, 1H), 5.15 (s, 2H), 3.58 (s, 2H), 3.43 (d, J = 5.2 Hz, 4H), 2.63 (s, 2H), 2.47 (s, 2H), 2.43 (s, 3H), 2.38 (s, 3H). MS (ESI) m/z: 615 [M + H].sup.+. V-n-9 [00451] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.97 (s, 1H), 10.68 (s, 1H), 8.19 (d, J = 1.6 Hz, 1H), 7.98 (d, J = 8.7 Hz, 1H), 7.90 (d, J = 8.6 Hz, 2H), 7.70 (d, J = 8.6 Hz, 1H), 7.45-7.39 (m, 3H), 7.30 (dd, J = 8.3, 2.6 Hz, 1H), 7.09 (d, J = 8.5 Hz, 2H), 7.06 (s, 1H), 6.17 (d, J = 2.1 Hz, 1H), 3.70 (s, 2H), 3.41 (s, 2H), 3.06 (s, 2H), 2.92 (s, 2H), 2.81 (s, 3H), 2.43 (s, 3H), 2.41-2.38 (m, 2H). MS (ESI) m/z: 615 [M + H].sup.+. V-n-10 [00452] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.81 (t, J = 2.3 Hz, 1H), 10.64 (s, 1H), 8.24 (dd, J = 1.6, 0.8 Hz, 1H), 8.18 (d, J = 2.2 Hz, 1H), 7.97 (dd, J = 8.3, 2.1 Hz, 1H), 7.74 (t, J = 1.7 Hz, 1H), 7.68 (d, J = 8.5 Hz, 1H), 7.41-7.36 (m, 1H), 7.35 (d, J = 2.7 Hz, 1H), 7.33 (dd, J = 3.5, 2.5 Hz, 1H), 7.23 (dd, J = 8.4, 2.7 Hz, 1H), 7.06-6.81 (m, 2H), 6.04 (dd, J = 3.5, 2.0 Hz, 1H), 3.66 (s, 2H), 3.39 (d, J = 12.1 Hz, 2H), 3.02 (t, J = 11.9 Hz, 2H), 2.90 (d, J = 12.7 Hz, 2H), 2.80 (s, 3H), 2.41 (s, 3H), 2.40-2.38 (m, 2H). MS (ESI) m/z: 590 [M + H].sup.+. V-n-11 [00453] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.85 (s, 1H), 10.66 (s, 1H), 8.19 (d, J = 1.8 Hz, 1H), 8.03 (dd, J = 3.0, 1.3 Hz, 1H), 7.98 (d, J = 8.4 Hz, 1H), 7.72- 7.67 (m, 2H), 7.61 (dd, J = 5.0, 3.0 Hz, 1H), 7.40 (d, J = 8.5 Hz, 1H), 7.39-7.35 (m, 2H), 7.25 (dd, J = 8.3, 2.6 Hz, 1H), 7.12 (s, 1H), 6.09 (dd, J = 3.4, 2.0 Hz, 1H), 3.67 (s, 2H), 3.41 (dd, J = 16.1, 3.8 Hz, 2H), 3.05 (d, J = 15.8 Hz, 2H), 2.91 (d, J = 10.2 Hz, 2H), 2.80 (s, 3H), 2.42 (s, 3H), 2.40-2.36 ( m, 2H). MS (ESI) m/z: 606 [M + H].sup.+. V-n-12 [00454] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.71 (s, 1H), 10.62 (s, 1H), 8.18 (d, J = 1.6 Hz, 1H), 7.95 (d, J = 8.4 Hz, 1H), 7.68 (d, J = 8.6 Hz, 1H), 7.38 (d, J = 8.5 Hz, 1H), 7.34 (d, J = 2.6 Hz, 1H), 7.28 (dd, J = 3.4, 2.5 Hz, 1H), 7.21 (dd, J = 8.3, 2.6 Hz, 1H), 6.98 (s, 1H), 6.02 (dd, J = 3.4, 2.0 Hz, 1H), 3.59 (s, 2H), 3.49-3.40 (s, 41H), 3.18 (s, 2H), 2.71 (s, 2H), 2.43 (s, 3H), 2.41 (s, 3H). MS (ESI) m/z: 590 [M + H].sup.+. V-n-13 [00455] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.61 (s, 1H), 10.67 (s, 1H), 10.33 (s, 1H), 8.18 (d, J = 1.6 Hz, 1H), 7.95 (d, J = 8.2 Hz, 1H), 7.67 (d, J = 8.6 Hz, 1H), 7.36 (d, J = 8.5 Hz, 1H), 7.32 (d, J = 2.6 Hz, 1H), 7.22-7.18 (m, 2H), 6.15 (dd, J = 3.4, 2.0 Hz, 1H), 3.62 (s, 2H), 3.59 (s, 2H), 3.36 (s, 2H), 3.02 (s, 2H), 2.87 (d, J = 19.8 Hz, 2H), 2.77 (s, 3H), 2.40 (s, 3H), 2.02 (s, 3H). MS (ESI) m/z: 581 [M + H].sup.+. V-n-14 [00456] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 11.25 (s, 1H), 10.63 (s, 1H), 9.88 (s, 1H), 8.18 (s, 1H), 7.97 (d, J = 8.5 Hz, 1H), 7.68 (t, J = 6.6 Hz, 1H), 7.37 (t, J = 8.3 Hz, 1H), 7.11 (s, 1H), 6.99 (dd, J = 3.4, 2.4 Hz, 1H), 6.14 (s, 1H), 5.89 (dd, J = 3.4, 2.0 Hz, 1H), 3.65 (s, 2H), 3.39 (s, 8H), 3.36-3.33 (m, 2H), 3.02 (s, 2H), 2.89 (d, J = 11.4 Hz, 2H), 2.80 (s, 3H), 2.40 (s, 3H), 2.38-2.33 (m, 2H). MS (ESI) m/z: 609 [M + H].sup.+. V-n-15 [00457] .sup.1H NMR (600 MHz, Methanol-d.sub.4) 9.54 (s, 1H), 9.18 (d, J = 8.2 Hz, 1H), 8.81 (d, J = 5.6 Hz, 1H), 8.16 (s, 1H), 8.12 (dd, J = 8.0, 5.9 Hz, 1H), 7.92 (d, J = 8.4 Hz, 1H), 7.77 (d, J = 8.5 Hz, 1H), 7.42 (d, J = 8.4 Hz, 1H), 7.39 (d, J = 3.4 Hz, 1H), 7.36 (d, J = 2.0 Hz, 1H), 7.29 (s, 1H), 7.24 (dd, J = 8.4, 2.3 Hz, 1H), 6.28 (d, J = 3.4 Hz, 1H), 3.96 (s, 3H), 3.85 (s, 2H), 3.35 (d, J = 11.7 Hz, 3H), 2.93 (s, 8H), 2.51 (s, 3H). MS (ESI) m/z: 615 [M + H].sup.+. V-n-16 [00458] .sup.1H NMR (600 MHz, Chloroform-d) 8.59 (d, J = 6.0 Hz, 2H), 8.25 (s, 1H), 7.89-7.80 (m, 4H), 7.76 (d, J = 8.5 Hz, 1H), 7.37-7.31 (m, 2H), 7.21 (dd, J = 8.3, 2.5 Hz, 1H), 7.17 (d, J = 3.5 Hz, 1H), 7.05 (s, 1H), 6.28 (d, J = 3.4 Hz, 1H), 3.97 (s, 3H), 3.63 (s, 2H), 2.56 (s, 3H), 2.54-2.47 (m, 8H), 2.32 (s, 3H). MS (ESI) m/z: 615 [M + H].sup.+. V-r-1 [00459] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 12.04 (s, 1H), 10.65 (s, 1H), 8.65 (dd, J = 4.5, 1.6 Hz, 2H), 8.14 (s, 1H), 7.97 (dd, J = 4.5, 1.6 Hz, 2H), 7.90 (s, 1H), 7.50 (dd, J = 3.4, 2.6 Hz, 1H), 7.44 (d, J = 2.6 Hz, 1H), 7.41 (d, J = 8.5 Hz, 1H), 7.34 (s, 1H), 7.30- 7.27 (m, 2H), 6.18 (dd, J = 3.4, 1.9 Hz, 1H), 3.52 (s, 2H), 2.44 (s, 3H), 2.39 (s, 8H), 2.18 (s, 3H). MS (ESI) m/z: 601 [M + H].sup.+.

TABLE-US-00006 TABLE 6 Structure and characterization of compounds VI No. Structure .sup.1H NMR and/or MS data VI-h-1 [00460] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.68 (s, 1H), 9.35 (s, 1H), 8.70 (d, J = 4.2 Hz, 1H), 8.63-8.58 (m, 1H), 8.56 (d, J = 5.3 Hz, 1H), 8.30 (d, J = 1.8 Hz, 1H), 8.26 (dd, J = 8.2, 1.7 Hz, 1H), 7.97 (t, J = 2.2 Hz, 1H), 7.93 (d, J = 8.1 Hz, 1H), 7.79 (d, J = 5.3 Hz, 1H), 7.75 (dd, J = 8.1, 1.9 Hz, 1H), 7.66- 7.54 (m, 4H), 7.27 (dd, J = 8.0, 2.6 Hz, 1H), 3.79 (s, 2H), 3.42 (d, J = 18.8 Hz, 3H), 3.07 (s, 2H), 2.92 (d, J = 12.2 Hz, 2H), 2.82 (s, 3H), 2.45-2.37 (m, 2H). MS (ESI) m/z: 605 [M + H].sup.+. VI-h-2 [00461] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.68 (s, 1H), 8.83-8.76 (m, 2H), 8.60 (d, J = 5.4 Hz, 1H), 8.32- 8.30 (m, 1H), 8.26 (dd, J = 8.2, 1.8 Hz, 1H), 8.24- 8.19 (m, 2H), 7.98 (s, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.83 (d, J = 5.4 Hz, 1H), 7.76 (dd, J = 8.1, 1.9 Hz, 1H), 7.58 (t, J = 8.2 Hz, 1H), 7.28 (dd, 8.1, 2.3 Hz, 1H), 3.80 (s, 2H), 3.15 (s, 2H), 3.07 (s, 2H), 2.93 (d, J = 12.7 Hz, 2H), 2.82 (s, 3H), 2.46- 2.37 (m, 2H). MS (ESI) m/z: 605 [M + H].sup.+. VI-i-1 [00462] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.60 (s, 1H), 9.29 (d, J = 2.2 Hz, 1H), 8.68 (dd, J = 4.9, 1.7 Hz, 1H), 8.56 (d, J = 5.4 Hz, 1H), 8.56-8.53 (m, 1H), 8.29 (d, J = 1.8 Hz, 1H), 8.25 (dd, J = 8.1, 1.8 Hz, 1H), 7.92 (d, J = 8.2 Hz, 1H), 7.89 (d, J = 2.1 Hz, 1H), 7.79 (d, J = 5.3 Hz, 1H), 7.69 (dd, J = 8.4, 2.2 Hz, 1H), 7.56 (dd, J = 8.0, 4.9 Hz, 1H), 7.45 (d, J = 8.4 Hz, 1H), 3.78 (s, 2H), 3.41 (d, J = 12.1 Hz, 2H), 3.06 (s, 2H), 2.92 (d, J = 12.7 Hz, 2H), 2.81 (s, 3H), 2.45-2.37 (m, 2H), 2.16 (s, 3H). MS (ESI) m/z: 619 [M + H].sup.+. VI-i-2 [00463] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.66 (s, 1H), 8.81-8.75 (m, 2H), 8.62 (d, J = 5.3 Hz, 1H), 8.20- 8.15 (m, 2H), 8.14-8.11 (m, 2H), 8.09 (t, J = 2.0 Hz, 1H), 8.04 (dt, J = 7.3, 1.5 Hz, 1H), 7.85 (d, J = 5.4 Hz, 1H), 7.82-7.75 (m, 2H), 7.45 (s, 1H), 3.74 (s, 2H), 3.42 (s, 1H), 3.13 (s, 1H), 3.02 (d, J = 27.2 Hz, 4H), 2.80 (s, 3H), 2.39 (d, J = 1.9 Hz, 1H). MS (ESI) m/z: 619 [M + H].sup.+. VI-j-1 [00464] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.27 (s, 1H), 9.37 (d, J = 2.1 Hz, 1H), 8.72 (dd, J = 4.8, 1.6 Hz, 1H), 8.65 (dt, J = 8.1, 2.0 Hz, 1H), 8.55 (d, J = 5.4 Hz, 1H), 8.33 (d, J = 1.8 Hz, 1H), 8.29 (d, J = 8.2 Hz, 1H), 7.93 (d, J = 8.2 Hz, 1H), 7.78 (d, J = 5.4 Hz, 1H), 7.61 (dd, J = 8.0, 4.9 Hz, 1H), 7.52 (d, J = 2.5 Hz, 1H), 7.48 (d, J = 8.4 Hz, 1H), 7.34 (dd, J = 8.3, 2.6 Hz, 1H), 3.41 (d, J = 12.2 Hz, 2H), 3.07 (s, 2H), 2.93 (d, J = 12.6 Hz, 2H), 2.82 (s, 3H), 2.46-2.38 (m, 2H), 2.34 (s, 3H). MS (ESI) m/z: 619 [M + H].sup.+. VI-j-2 [00465] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.28 (s, 1H), 8.87-8.77 (m, 2H), 8.59 (d, J = 5.3 Hz, 1H), 8.35- 8.31 (m, 3H), 8.29 (dd, J = 8.1, 1.8 Hz, 1H), 7.94 (d, J = 8.1 Hz, 1H), 7.82 (d, J = 5.4 Hz, 1H), 7.54 (d, J = 2.5 Hz, 1H), 7.48 (d, J = 8.4 Hz, 1H), 7.35 (dd, J = 8.3, 2.6 Hz, 1H), 3.42 (d, J = 12.1 Hz, 2H), 3.07 (t, J = 12.3 Hz, 2H), 2.93 (d, J = 12.6 Hz, 2H), 2.82 (s, 3H), 2.42 (t, J = 12.1 Hz, 2H), 2.35 (s, 3H). MS (ESI) m/z: 619 [M + H].sup.+. VI-l-1 [00466] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.63 (s, 1H), 9.29 (d, J = 2.2 Hz, 1H), 8.68 (d, J = 4.8 Hz, 1H), 8.58 (d, J = 5.4 Hz, 1H), 8.53 (dt, J = 8.0, 2.0 Hz, 1H), 8.21 (d, J = 2.2 Hz, 1H), 8.11 (dd, J = 8.6, 2.2 Hz, 1H), 8.08 (t, J = 1.9 Hz, 1H), 8.03 (d, J = 7.4 Hz, 1H), 7.83-7.75 (m, 3H), 7.71 (d, J = 8.6 Hz, 1H), 7.55 (dd, J = 8.0, 4.8 Hz, 1H), 3.68 (s, 2H), 3.40 (d, J = 12.2 Hz, 2H), 3.04 (s, 2H), 2.92 (d, J = 12.6 Hz, 2H), 2.81 (s, 3H), 2.37 (t, J = 12.0 Hz, 2H). MS (ESI) m/z: 605 [M + H].sup.+. VI-m-1 [00467] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.54 (s, 1H), 9.23 (d, J = 2.1 Hz, 1H), 8.67 (dd, J = 4.8, 1.7 Hz, 1H), 8.58 (d, J = 5.4 Hz, 1H), 8.48 (dt, 8.0, 2.0 Hz, 1H), 8.19 (d, J = 2.2 Hz, 1H), 8.10 (dd, 8.6, 2.2 Hz, 1H), 8.05 (d, J = 1.7 Hz, 1H), 7.99 (dd, J = 7.9, 1.8 Hz, 1H), 7.81 (d, J = 5.3 Hz, 1H), 7.70 (d, J = 8.6 Hz, 1H), 7.66 (d, J = 8.1 Hz, 1H), 7.54 (dd, 8.0, 4.8 Hz, 1H), 3.67 (s, 2H), 3.40 (d, J = 12.1 Hz, 2H), 3.03 (s, 2H), 2.91 (d, J = 12.6 Hz, 2H), 2.80 (s, 3H), 2.42-2.33 (m, 2H), 2.27 (s, 3H). MS (ESI) m/z: 619 [M + H].sup.+. VI-n-1 [00468] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.70 (s, 1H), 9.34 (d, J = 2.1 Hz, 1H), 8.76-8.71 (m, 1H), 8.61 (dt, J = 8.0, 2.0 Hz, 1H), 8.56 (d, J = 5.3 Hz, 1H), 8.19 (d, J = 2.2 Hz, 1H), 8.04-7.97 (m, 1H), 7.79 (d, J = 5.4 Hz, 1H), 7.70 (d, J = 8.5 Hz, 1H), 7.65- 7.58 (m, 3H), 7.52 (d, J = 8.5 Hz, 1H), 3.68 (s, 2H), 3.40 (d, J = 12.4 Hz, 2H), 3.03 (s, 2H), 2.92 (d, J = 12.4 Hz, 2H), 2.81 (s, 3H), 2.49 (s, 3H), 2.39 (d, J = 11.7 Hz, 2H). MS (ESI) m/z: 619 [M + H].sup.+. VI-o-1 [00469] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.96 (s, 1H), 9.35 (d, J = 2.2 Hz, 1H), 8.71 (dd, J = 4.8, 1.7 Hz, 1H), 8.61-8.54 (m, 2H), 8.16 (d, J = 2.2 Hz, 1H), 7.98 (dd, J = 8.5, 2.2 Hz, 1H), 7.82 (d, J = 2.8 Hz, 1H), 7.81-7.77 (m, 2H), 7.75-7.70 (m, 2H), 7.58 (dd, J = 8.0, 4.8 Hz, 1H), 3.68 (s, 2H), 3.40 (d, J = 12.1 Hz, 2H), 3.03 (s, 2H), 2.91 (d, J = 12.7 Hz, 2H), 2.81 (s, 3H), 2.42-2.31 (m, 2H). MS (ESI) m/z: 640 [M + H].sup.+. VI-o-2 [00470] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.65 (s, 1H), 9.29 (d, J = 2.1 Hz, 1H), 8.69 (dd, J = 4.8, 1.7 Hz, 1H), 8.59 (d, J = 5.4 Hz, 1H), 8.53 (dd, J = 8.0, 2.0 Hz, 1H), 8.13 (s, 1H), 8.12-8.07 (m, 2H), 8.03 (dt, J = 7.4, 1.6 Hz, 1H), 7.84-7.75 (m, 3H), 7.56 (dd, J= 8.0, 4.8 Hz, 1H), 7.44 (s, 1H), 3.41 (s, 3H), 3.02 (d, J = 33.1 Hz, 4H), 2.79 (s, 3H), 2.45-2.35 (m, 3H). MS (ESI) m/z: 605 [M + H].sup.+. VI-p-1 [00471] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.65 (s, 1H), 9.29 (d, J = 2.1 Hz, 1H), 8.69 (dd, J = 4.8, 1.7 Hz, 1H), 8.59 (d, J = 5.4 Hz, 1H), 8.53 (dd, J = 8.0, 2.0 Hz, 1H), 8.13 (s, 1H), 8.12-8.07 (m, 2H), 8.03 (dt, J = 7.4, 1.6 Hz, 1H), 7.84-7.75 (m, 3H), 7.56 (dd, J = 8.0, 4.8 Hz, 1H), 7.44 (s, 1H), 3.41 (s, 3H), 3.02 (d, J = 33.1 Hz, 4H), 2.79 (s, 3H), 2.45-2.35 (m, 3H). MS (ESI) m/z: 605 [M + H].sup.+. VI-p-2 [00472] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.66 (s, 1H), 6.81-8.73 (m, 2H), 8.62 (d, J = 5.4 Hz, 1H), 8.16- 8.14 (m, 2H), 8.12 (d, J = 2.2 Hz, 2H), 8.09 (d, J = 2.0 Hz, 1H), 8.06-8.03 (m, 1H), 7.85 (d, J = 5.4 Hz, 1H), 7.82-7.75 (m, 2H), 7.45 (s, 1H), 3.73 (s, 2H), 3.43 (d, J = 10.3 Hz, 2H), 3.02 (d, J = 35.2 Hz, 4H), 2.79 (s, 3H), 2.47-2.35 (m, 2H). MS (ESI) m/z: 605 [M + H].sup.+. VI-q-1 [00473] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 9.24 (d, J = 2.2 Hz, 1H), 8.69 (dd, J = 4.9, 1.7 Hz, 1H), 8.59 (d, J = 5.4 Hz, 1H), 8.52 (dt, J = 8.0, 1.9 Hz, 1H), 8.13 (s, 1H), 8.10 (s, 1H), 8.06 (d, J = 1.8 Hz, 1H), 8.00 (dd, J = 8.0, 1.8 Hz, 1H), 7.81 (d, J = 5.4 Hz, 1H), 7.66 (d, J = 8.1 Hz, 1H), 7.57 (dd, J = 8.1, 4.9 Hz, 1H), 7.44 (s, 1H), 3.78 (s, 2H), 3.42 (s, 2H), 3.04 (s, 4H), 2.79 (s, 3H), 2.28 (s, 3H). MS (ESI) m/z: 619 [M + H].sup.+. VI-q-2 [00474] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.57 (s, 1H), 8.76 (d, J = 5.4 Hz, 2H), 8.63 (d, J = 5.3 Hz, 1H), 8.15-8.09 (m, 4H), 8.07 (d, J = 1.8 Hz, 1H), 8.01 (dd, J = 7.9, 1.8 Hz, 1H), 7.86 (d, J = 5.4 Hz, 1H), 7.67 (d, J = 8.1 Hz, 1H), 7.43 (s, 1H), 3.74 (s, 2H), 3.42 (d, J = 5.9 Hz, 1H), 3.07 (d, J = 61.2 Hz, 3H), 2.79 (s, 3H), 2.47-2.36 (m, 2H), 2.28 (s, 3H). MS (ESI) m/z: 619 [M + H].sup.+.

TABLE-US-00007 TABLE 7 Structure and characterization of compounds VII No. Structure .sup.1H NMR and/or MS data VII-h-1 [00475] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10,64 (s, 1H), 9.36 (d, J = 2.3 Hz, 1H), 8.90-8.65 (m, 2H), 8.26 (d, J = 1.8 Hz, 1H), 8.23 (dd, J = 8.3, 1.7 Hz, 1H), 7.96 (d, J = 6.0 Hz, 1H), 7.91 (d, J = 8.2 Hz, 1H), 7.81 (dd, J = 8.1, 5.1 Hz, 1H), 7.77 (t, J = 2.2 Hz, 1H), 7.72 (dd, J = 8.3, 1.9 Hz, 1H), 7.58 (s, 1H), 7.52 (t, J = 8.2 Hz, 1H), 7.45 (d, J = 6.0 Hz, 1H), 7.09 (dd, J = 8.0, 2.4 Hz, 1H), 3.79 (s, 2H), 3.41 (d, J = 12.1 Hz, 2H), 3.06 (s, 2H), 2.91 (d, J = 12.7 Hz, 2H), 2.81 (s, 3H), 2.45-2.39 (m, 2H). MS (ESI) m/z: 604 [M + H].sup.+. VII-h-2 [00476] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 8.73-8.60 (m, 2H), 8.21 (s, 1H), 8.19 (d, J = 8.1 Hz, 1H), 8.01-7.98 (m, 2H), 7.96 (d, J = 6.0 Hz, 1H), 7.91 (d, J = 8.2 Hz, 1H), 7.75-7.71 (m, 2H), 7.54-7.48 (m, 2H), 7.45 (d, J = 6.0 Hz, 1H), 7.08 (dd, J = 8.3, 2.4 Hz, 1H), 3.66 (s, 2H), 2.47-2.18 (m, 8H), 2.16 (s, 3H). MS (ESI) m/z: 604 [M + H].sup.+. VII-i-1 [00477] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.55 (s, 1H), 9.28 (d, J = 2.2 Hz, 1H), 8.74 (dd, J = 5.1, 1.4 Hz, 1H), 8.82 (dt, J = 8.1, 1.9 Hz, 1H), 8.24 (d, J = 1.8 Hz, 1H), 8.21 (dd, J = 8.1, 1.8 Hz, 1H), 7.95 (d, J = 6.0 Hz, 1H), 7.89 (d, J = 8.2 Hz, 1H), 7.72 (dd, J = 8.1, 5.0 Hz, 1H), 7.69-7.65 (m, 2H), 7.49 (d, J = 6.0 Hz, 1H), 7.44 (d, J = 8.7 Hz, 1H), 7.31 (s, 1H), 3.77 (s, 2H), 3.40 (d, J = 12.1 Hz, 2H), 3.05 (t, J = 12.2 Hz, 2H), 2.90 (d, J = 12.7 Hz, 2H), 2.80 (s, 3H), 2.42 (t, J = 11.9 Hz, 2H), 2.22 (s, 3H). MS (ESI) m/z: 618 [M + H].sup.+. VII-i-2 [00478] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.49 (s, 1H), 8.72-8.57 (m, 2H), 8.19 (s, 1H), 8.17 (d, J = 8.1 Hz, 1H), 7.96 (dd, J = 6.1, 1.3 Hz, 1H), 7.96-7.92 (m, 2H), 7.89 (d, J = 8.1 Hz, 1H), 7.68 (dd, J = 8.3, 2.0 Hz, 1H), 7.65 (d, J = 2.1 Hz, 1H), 7.50 (d, J = 6.1 Hz, 1H), 7.44 (d, J = 8.4 Hz, 1H), 7.28 (d, J = 1.2 Hz, 1H), 3.65 (s, 2H), 2.47-2.24 (m, 8H), 2.21 (s, 3H), 2.15 (d, J = 1.5 Hz, 3H). MS (ESI) m/z: 618 [M + H].sup.+. VII-j-1 [00479] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.19 (s, 1H), 9.17 (d, J = 2.3 Hz, 1H), 8.63 (dd, J = 4.7, 1.6 Hz, 1H), 8.37 (dt, J = 8.1, 2.0 Hz, 1H), 8.25 (s, 1H), 8.22 (d, J = 8.1 Hz, 1H), 7.92-7.86 (m, 2H), 7.51 (dd, J = 8.0, 4.7 Hz, 1H), 7.46 (d, J = 6.1 Hz, 1H), 7.43 (d, J = 8.4 Hz, 1H), 7.39 (d, J = 2.6 Hz, 1H), 7.36 (s, 1H), 7.17 (dd, J = 8.3, 2.7 Hz, 1H), 3.66 (s, 2H), 2.47-2.28 (m, 8H), 2.30 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 618 [M + H].sup.+. VII-j-2 [00480] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.19 (s, 1H), 8.77-8.55 (m, 2H), 8.26 (s, 1H), 8.23 (d, J = 7.4 Hz, 1H), 7.99-7.96 (m, 2H), 7.95 (d, J = 6.0 Hz, 1H), 7.91 (d, J = 8.1 Hz, 1H), 7.48 (d, J = 5.9 Hz, 1H), 7.44-7.40 (m, 2H), 7.39 (d, J = 2.6 Hz, 1H), 7.17 (dd, J = 8.3, 2.7 Hz, 1H), 3.66 (s, 2H), 2.47- 2.27 (m, 8H), 2.31 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 618 [M + H].sup.+. VII-l-1 [00481] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 9.18 (dd, J = 2.4, 0.8 Hz, 1H), 8.63 (dd, J = 4.8, 1.6 Hz, 1H), 8.37 (dt, J = 8.0, 2.0 Hz, 1H), 8.18 (d, J = 2.2 Hz, 1H), 8.04-8.00 (m, 1H), 7.95 (dd, J = 7.9, 1.3 Hz, 1H), 7.94-7.89 (m, 2H), 7.73-7.65 (m, 2H), 7.56 (ddd, J = 8.2, 2.5, 1.0 Hz, 1H), 7.50 (ddd, J = 8.0, 4.7, 0.8 Hz, 1H), 7.45 (d, J = 6.0 Hz, 1H), 7,40 (s, 1H), 3.55 (s, 2H), 2.47-2.17 (m, 8H), 2.15 (s, 3H). MS (ESI) m/z: 604 [M + H].sup.+. VII-l-2 [00482] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.56 (s, 1H), 8.73-8.54 (m, 2H), 8.19 (d, J = 2.2 Hz, 1H), 8.03 (dd, J = 8.5, 2.2 Hz, 1H), 8.01-7.95 (m, 4H), 7.94 (t, J = 2.1 Hz, 1H), 7.73-7.68 (m, 2H), 7.57 (ddd, J = 8.1, 2.5, 0.9 Hz, 1H), 7.49 (d, J = 6.0 Hz, 1H), 7.45 (s, 1H), 3.56 (s, 2H), 2.48-2.17 (m, 8H), 2.15 (s, 3H). MS (ESI) m/z: 604 [M + H].sup.+. VII-n-1 [00483] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.64 (s, 1H), 9.16 (d, J = 2.3 Hz, 1H), 8.63 (dd, J = 4.8, 1.6 Hz, 1H), 8.35 (dt, J = 8.0, 2.0 Hz, 1H), 8.16 (d, J = 2.2 Hz, 1H), 7.91 (t, J = 7.5 Hz, 2H), 7.67 (d, J = 8.5 Hz, 1H), 7.52-7.49 (m, 2H), 7.46 (s, 1H), 7.44 (d, J = 3.0 Hz, 1H), 7.36 (dd, J = 8.4, 2.6 Hz, 1H), 7.34 (s, 1H), 3.54 (s, 2H), 2.43 (s, 3H), 2.45-2.17 (m, 8H), 2.14 (s, 3H). MS (ESI) m/z: 618 [M + H].sup.+. VII-n-2 [00484] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.66 (s, 1H), 8.76 (d, J = 5.4 Hz, 2H), 8.17 (d, J = 2.2 Hz, 1H), 8.15-8.12 (m, 2H), 8.00 (d, J = 6.0 Hz, 1H), 7.97 (dd, J = 8.4, 2.1 Hz, 1H), 7.68 (d, J = 8.5 Hz, 1H), 7.50 (d, J = 2.6 Hz, 1H), 7.49-7.44 (m, 3H), 7.39 (dd, J = 8.3, 2.7 Hz, 1H), 3.65 (s, 2H), 3.39 (d, J = 12.2 Hz, 2H), 3.02 (s, 2H), 2.89 (d, J = 12.6 Hz, 2H), 2.80 (s, 3H), 2.44 (s, 3H), 2.36 (t, J = 12.7 Hz, 2H). MS (ESI) m/z: 618 [M + H].sup.+. VII-o-1 [00485] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.85 (s, 1H), 9.22 (d, J = 2.4 Hz, 1H), 8.64 (dd, J = 4.7, 1.7 Hz, 1H), 8.42 (dt, J = 8.0, 2.1 Hz, 1H), 8.14 (d, J = 2.2 Hz, 1H), 7.93 (d, J = 6.0 Hz, 1H), 7.88 (dd, J = 8.5, 2.2 Hz, 1H), 7.69 (t, J = 8.9 Hz, 2H), 7.65 (d, J = 3.0 Hz, 1H), 7.52 (dd, J = 8.0, 4.8 Hz, 1H), 7.49 (s, 1H), 7.47 (dd, J = 8.8, 2.9 Hz, 1H), 7.44 (d, J = 6.0 Hz, 1H), 3.55 (s, 2H), 2.47-2.20 (m, 8H), 2.14 (s, 3H). MS (ESI) m/z: 638 [M + H].sup.+. VII-o-2 [00486] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.83 (s, 1H), 8.74-8.54 (m, 2H), 8.14 (d, J = 2.3 Hz, 1H), 8.06- 8.02 (m, 2H), 7.99 (d, J = 6.0 Hz, 1H), 7.89 (dd, J = 8.6, 2.2 Hz, 1H), 7.74-7.68 (m, 2H), 7.67 (d, J = 2.9 Hz, 1H), 7.55 (s, 1H), 7.49 (dd, J = 8.8, 3.0 Hz, 1H), 7.47 (d, J = 6.0 Hz, 1H), 3.56 (s, 2H), 2.48-2.20 (m, 8H), 2.16 (s, 3H). MS (ESI) m/z: 638 [M + H].sup.+. VII-p-1 [00487] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.65 (s, 1H), 9.29 (s, 1H), 8.73 (d, J = 5.0 Hz, 1H), 8.61 (dd, J = 8.3, 2.2 Hz, 1H), 8.12 (d, J = 2.1 Hz, 2H), 8.00- 7.94 (m, 2H), 7.94-7.91 (m, 1H), 7.75-7.65 (m, 2H), 7.58 (ddd, J = 8.1, 2.5, 1.0 Hz, 1H), 7.51- 7.42 (m, 3H), 3.83 (s, 2H), 3.65-2.83 (m, 8H), 2.80 (s, 3H). MS (ESI) m/z: 604 [M + H].sup.+. VII-p-2 [00488] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.58 (s, 1H), 8.81-8.61 (m, 2H), 8.16 (d, J = 1.9 Hz, 1H), 8.00- 7.96 (m, 5H), 7.94 (t, J = 2.0 Hz, 1H), 7.70 (t, J = 7.9 Hz, 1H), 7.56 (dd, J = 8.1, 2.5 Hz, 1H), 7.48 (d, J = 6.0 Hz, 1H), 7.43 (s, 1H), 7.35 (s, 1H), 3.52 (s, 2H), 2.45-2.20 (m, 8H), 2.13 (s, 3H). MS (ESI) m/z: 604 [M + H].sup.+. VII-u-1 [00489] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.83 (s, 1H), 9.62 (d, J = 1.7 Hz, 1H), 9.29 (s, 1H), 8.76 (d, J = 5.0 Hz, 1H), 8.68 (dt, J = 7.6, 1.7 Hz, 1H), 8.53 (t, J = 2.0 Hz, 1H), 8.20 (d, J = 1.8 Hz, 1H), 8.02 (t, J = 1.5 Hz, 1H), 8.00-7.96 (m, 2H), 7.92 (t, J = 1.7 Hz, 1H), 7.88 (d, J = 1.8 Hz, 1H), 7.77 (dd, J = 8.1, 5.1 Hz, 1H), 7.68 (d, J = 8.0 Hz, 1H), 7.55 (d, J = 6.1 Hz, 1H), 7.27 (s, 1H), 2.35 (d, J = 1.1 Hz, 3H), 2.33 (s, 3H). MS (ESI) m/z: 586 [M + H].sup.+. VII-u-2 [00490] .sup.1H NMR (600 MHz, DMSO-d.sub.6) 10.62 (s, 1H), 6.82-8.44 (m, 2H), 8.24 (d, J = 2.0 Hz, 1H), 8.18 (d, J = 1.4 Hz, 1H), 8.10 (d, J = 1.9 Hz, 1H), 7.99 (d, J = 6.0 Hz, 1H), 7.97 (dd, J = 8.0, 1.8 Hz, 1H), 7.94-7.91 (m, 2H), 7.88 (d, J = 1.7 Hz, 1H), 7.71 (s, 1H), 7.67 (d, J = 8.1 Hz, 1H), 7.55 (d, J = 6.0 Hz, 1H), 7.45 (s, 1H), 7.18 (s, 1H), 2.31 (s, 3H), 2.16 (s, 3H). MS (ESI) m/z: 586 [M + H].sup.+.

Test Example

[0262] Biological Activity Assay:

[0263] Growth inhibitory activity of compounds on cell lines stably transfected with kinase

[0264] The activity of compounds against kinase RET is evaluated by their effect of inhibiting growth of cell lines stably transfected with kinase CCDC6-RET-BaF3, KIF5B-RET-BaF3, and wild-type BaF3 (Proc. Natl. Acad. Sci. USA., 2006, 103, 3153-8.). The growth of the cell lines stably transfected with kinase CCDC6-RET-BaF3, KIF5B-RET-BaF3 depends on their kinase activity. If a compound can inhibit the activity of the kinase RET per se or the activity of the RET signaling pathway, the compound can inhibit the growth of BaF3 cells stably transfected with kinase. While the growth of wild-type BaF3 cells does not depend on the activity of RET or RET signaling pathway, the effect of a compound on the growth of wild-type BaF3 cells can be used to evaluate its broad-spectrum toxicity. Therefore, a larger ratio between IC.sub.50 of a compound to wild-type BaF3 and IC.sub.50 of the compound to the cell lines stably transfected with kinase CCDC6-RET-BaF3, KIF5B-RET-BaF3 indicates better targeting.

[0265] The specific test method is given as follows:

[0266] 1) Medium: DMEM (Dulbecco's modified eagle medium) or RPMI 1640 (containing 10% fetal bovine serum, 100 g/mL ampicillin, 100 g/mL streptomycin).

[0267] 2) Reagents: MTS reaction solution (containing 2 mg/mL of MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner Salt]; 100 g/mL PES (phenazine methosulfate)).

[0268] 3) Compound test: cells stably transfected with kinase (CCDC6-RET-BaF3, KIF5B-RET-BaF3) or wild-type BaF3 cells (210.sup.4 cells/well) were incubated into a 96-well culture plate, the volume of cell culture fluid was 90 L, and then 10 L of the compound at each gradient concentration was added (the highest concentration was 10 M, which was diluted stepwise by , and 8 concentration points were set in total; the system contained 0.1% DMSO (dimethyl sulfoxide)). The cell plate with uniformly mixed compound was cultured in a cell culture incubator (37 C.; 5% CO.sub.2) for 48 h, then 20 L of MTS reaction solution was added, uniformly mixed and incubated in the cell culture incubator (37 C.; 5% CO.sub.2) for 1-4 hr, OD values at 490 nm were measured by a microplate reader (VARIOSKAN FLASH, Thermo). Three parallels were set in each group of experiments, with 0.1% (a final concentration) DMSO as a negative control, and a medium without cells or compounds as a blank control. The cell growth inhibition rate was calculated by the following formula:

Cell growth inhibition rate %=1(OD.sub.experimental groupOD.sub.blank group)/(OD.sub.negative groupOD.sub.blank group)100%

[0269] 4) IC.sub.50 calculation: The semi-inhibitory concentration of the compound acting on cell growth was calculated using GradPad Prism 5 software according to the measured cell growth inhibition rate.

TABLE-US-00008 TABLE 8 Growth inhibitory activity of compounds on cell lines stably transfected with kinase and wild-type Ba/F3 cells* CCDC6-RET KIF5B-RET WT Ba/F3 Cmpd ID (IC.sub.50/nM) (IC.sub.50/nM) (IC.sub.50/nM) I-d-2 1541 5714 >10000 I-f-2 4845 8120 n.d. I-h-1 4934 2290 n.d. II-e-1 1974 2241 n.d. II-e-2 1428 1767 >10000 II-h-1 1112 952.7 n.d. II-h-2 140.2 106.2 n.d. II-h-3 342.8 820.3 4089 II-h-4 78.58 299.6 3927 II-i-1 476.6 411 n.d. II-i-2 616.6 469.2 n.d. II-i-3 880.8 1036 n.d. I-j-1 0.7407 2.739 n.d. I-j-2 2128 1578 2107 I-j-3 1416 1431 1768 I-j-4 1011 1611 1793 I-j-5 1876 2369 4205 I-j-6 221 1178 4220 I-j-7 1027 1437 2412 I-l-1 476.3 1947 >10000 I-l-2 3614 17751 1356 I-l-3 25.22 5.882 >10000 I-m-1 504.4 810.4 >10000 I-m-2 710.2 1300 n.d. I-m-3 447.4 1046 n.d. I-n-1 297.5 899.9 >10000 I-n-2 3212 3636 1612 I-n-3 8.378 40.5 n.d. I-n-4 2700 2373 n.d. I-n-5 1539 1505 n.d. I-n-6 1785 1380 n.d. I-n-7 1557 1454 n.d. I-n-8 1206 1328 n.d. I-n-9 1549 1476 n.d. I-n-10 1402 1403 n.d. I-n-11 1205 1962 n.d. I-n-12 2032 1864 n.d. I-n-13 3005 4845 n.d. I-n-14 163.2 46.98 n.d. I-o-1 1465 1392 n.d. I-o-2 20.6 3.146 n.d. I-o-3 1383 1383 n.d. I-o-4 1404 1407 n.d. I-o-5 1317 1387 n.d. I-o-6 1290 1358 n.d. I-o-7 903.3 1207 n.d. I-o-8 1586 1490 n.d. I-o-9 1392 1497 n.d. I-o-10 1367 1907 n.d. I-o-11 1676 1565 n.d. I-o-12 55.22 153.8 n.d. II-j-1 4166 4418 n.d. II-j-2 13.09 5,797 n.d. II-j-3 1417 3206 n.d. II-j-4 2070 2357 n.d. II-j-5 2371 3888 7402 II-j-6 7.958 44.21 4230 II-k-1 2068 1394 n.d. II-k-2 15.8 114 n.d. II-k-3 567 1347 1344 II-k-4 37.68 103.8 >10000 II-m-1 35.21 8.282 n.d. II-m-2 30.23 17.82 n.d. II-m-3 348 97.74 n.d. II-m-4 847,6 152.3 n.d. II-m-5 807.3 319.6 n.d. II-m-6 696 114 n.d. II-m-7 178.1 28.31 n.d. II-m-8 165.7 56.89 n.d. II-m-9 75.14 14.61 n.d. II-m-10 449.3 36.38 n.d. II-m-11 31.78 14.94 n.d. II-m-12 123.2 69.66 n.d. II-m-13 253.4 172.2 n.d. II-m-14 9.31 21.64 n.d. II-m-15 110.6 18.03 n.d. II-m-16 383.5 84.55 n.d. II-m-17 1100 159.9 n.d. II-m-18 256.7 34.28 n.d. II-m-19 54.93 123.6 n.d. II-m-20 10.57 74.34 >10000 II-m-21 73.39 240.4 4779 II-m-22 >10000 442061 n.d. II-m-23 1104 915.8 n.d. II-n-2 1518 440.4 n.d. II-o-1 4167 4019 n.d. II-o-2 108 130.4 n.d. II-p-1 267.9 250.5 n.d. II-p-2 458.4 521.3 n.d. II-s-1 264.2 482.4 n.d. II-s-2 187.9 355.2 n.d. II-t-2 1569 2616 n.d. II-v-1 7228 7945 n.d. II-v-7 1201 1203 n.d. II-v-8 346 407.4 n.d. II-v-9 961.5 934.4 n.d. II-v-10 491.9 462.6 n.d. II-v-11 546.1 646.5 n.d. II-v-12 364.3 118.3 n.d. II-v-13 533.3 587.4 n.d. II-v-14 73.89 69.27 n.d. II-v-15 114.4 135 n.d. II-v-16 2487 3067 n.d. II-v-17 899.8 1044 n.d. III-h-1 2814 1539 n.d. III-h-2 16.78 16.4 n.d. III-h-3 4098 2139 n.d. III-h-4 194.8 179.9 n.d. III-i-1 4108 2846 n.d. III-i-2 1396 773.9 n.d. III-i-3 4343 3627 n.d. III-i-4 2020 1327 n.d. III-j-1 5943 3253 n.d. III-j-2 6.06 2.323 n.d. III-j-3 2482 2349 3776 III-j-4 1363 1717 3409 III-j-5 4264 3102 n.d. III-j-6 27.99 13.21 n.d. III-j-7 1268 1367 2564 III-j-8 1135 1315 1881 III-j-9 97.6 463.9 4258 III-j-10 233.6 427.8 1456 III-j-11 1529 1568 1365 III-j-12 2662 2973 2151 III-j-13 1715 2402 4153 III-j-14 876.3 1379 1344 III-j-15 744.6 619.9 1205 III-j-16 2039 1468 2277 III-j-18 477.1 1353 >10000 III-k-1 1862 1320 4155 III-k-2 0.79 17.2 1342 III-k-3 1248 1188 1167 III-k-4 11.2 70.7 1622 III-k-5 1488 1915 4365 III-k-6 989.7 1012 2474 III-k-7 2961 1900 3715 III-k-8 3458 3576 3990 III-k-9 1188 1489 1650 III-k-10 2297 2438 1439 III-k-11 451.1 495.9 1289 III-k-12 1813 2662 n.d. III-k-13 1447 1547 1603 III-k-15 2201 2380 n.d. III-k-16 2087 3194 3631 III-k-17 1411 2615 2633 III-k-18 4125 3994 3887 III-l-2 22.68 5.705 n.d. III-l-3 1403 1544 n.d. III-l-4 18.67 11.31 n.d. III-m-1 4503 2102 n.d. III-m-2 3626 1306 n.d. III-m-3 2706 2406 3100 III-m-4 2723 3863 3459 III-m-5 3758 4041 3919 III-m-6 3772 3948 2786 III-m-7 1412 2346 4328 III-m-8 1238 1712 4097 III-m-9 1254 3049 1444 III-m-10 543.9 1049 622.9 III-m-12 4021 4277 3576 III-m-13 3510 2995 3394 III-m-14 2919 2720 3192 III-m-15 2958 3931 7206 III-m-16 3672 4422 4362 III-m-17 3153 2761 n.d. III-m-18 2965 2678 3511 III-m-19 2512 3273 4023 III-m-20 2961 2500 3554 III-m-21 3491 3747 2921 III-m-22 597.1 854.1 >10000 III-m-23 514.7 476.6 463.5 III-m-24 3122 3232 3080 III-m-26 1318 2898 4096 III-m-27 1401 1501 34462 III-n-2 53.72 21 n.d. III-n-4 43.12 17.18 n.d. III-o-1 2154 1547 1626 III-o-2 17.4 13.43 1290 III-o-3 1278 1334 1299 III-o-4 6.046 13.31 1154 III-p-1 4404 2917 3550 III-p-2 449.3 672.5 >10000 III-p-3 4530 3379 n.d. III-p-4 3234 3652 >10000 III-q-1 1330 1537 1432 III-q-2 351.2 593.7 843.2 III-q-3 1403 1396 1380 III-q-4 901.1 1268 1334 III-r-1 4454 4770 n.d. III-r-2 385.6 535.3 4134 III-r-3 3773 2721 3651 III-r-4 186.8 324.9 1378 III-v-1 431.3 834.5 >10000 III-v-2 <4 35927 n.d. III-v-3 23766 21289 n.d. III-v-4 <4 76095 n.d. III-v-5 <4 304425 n.d. III-v-6 <4 48058 n.d. III-v-7 147612 14159 n.d. III-v-8 10940 4339 n.d. III-v-9 4210 1750 n.d. III-v-10 <4 34976 n.d. III-v-11 3334 1457 n.d. III-v-12 149.3 191 n.d. III-v-13 18303 13834 n.d. IV-b-2 5870 4166 n.d. IV-c-2 1683 2838 n.d. IV-e-2 2907 8445 2225 IV-n-2 171.7 172.9 n.d. IV-n-3 4148 3543 n.d. IV-n-4 3904 1711 n.d. IV-n-5 2959 2317 n.d. IV-n-6 4307 4228 n.d. IV-n-7 2811 3938 n.d. IV-n-8 2087 1623 n.d. IV-n-9 1826 1569 n.d. IV-n-10 2163 1842 n.d. IV-n-11 5221 4212 n.d. IV-o-1 1981 1722 n.d. IV-o-2 88.63 12.13 n.d. IV-o-3 4313 4183 n.d. IV-o-4 4279 3106 n.d. IV-o-5 4090 3390 n.d. IV-o-6 4016 3403 n.d. IV-o-7 1505 1610 n.d. IV-o-8 172.1 151.7 n.d. IV-o-9 4815 4362 n.d. IV-o-10 4290 3760 n.d. IV-o-11 3030 1620 n.d. IV-o-12 990.2 2514 n.d. V-I-1 1462 1462 2073 V-I-2 168.6 168.6 3395 V-I-3 587.1 595.2 1245 V-I-4 337.1 142.8 1416 V-m-1 1023 473.3 1375 V-m-2 1350 978.4 904.8 V-m-3 1174 613.2 3366 V-m-4 1240 811.2 1417 V-n-1 2902 2117 2309 V-n-2 579.7 616.1 2071 V-n-12 565.7 672.8 n.d. V-n-16 471.8 388.4 n.d. V-r-1 2960 2806 n.d. VI-h-2 561.1 493.1 3904 VI-i-1 1954 1472 1533 VI-i-2 5702 7418 n.d. VI-j-1 2695 3957 3383 VI-j-2 3.076 16.96 3942 VI-l-1 2643 3218 4621 VI-m-1 1236 1252 1583 VI-n-1 3244 2836 4191 VI-o-1 2171 2871 3990 VI-o-2 39.84 99.42 1961 VI-q-1 3568 3427 4357 VI-q-2 1517 1470 1516 VII-h-2 636.9 1078 n.d. VII-i-2 1357 1332 n.d. VII-j-1 810.5 1282 n.d. VII-j-2 95.61 189.4 n.d. VII-l-1 1017 1351 n.d. VII-l-2 215 314.6 n.d. VII-n-1 1688 1777 n.d. VII-n-2 221.4 404.9 n.d. VII-o-1 1568 1626 n.d. VII-o-2 326.2 498.8 n.d. Cabozantinib 226.5 301.8 n.d. *n.d. means not determined, Cabozantinib acts as a positive control.

[0270] Growth inhibitory activity of compounds on kinase RET-positive non-small cell lung cancer cells LC-2/AD

[0271] The specific test method is given as follows:

[0272] 1) Medium: DMEM (Dulbecco's modified eagle medium) or RPMI 1640 (containing 10% fetal bovine serum, 100 g/mL ampicillin, 100 g/mL streptomycin).

[0273] 2) Reagents: MTS reaction solution (containing 2 mg/mL of MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner Salt]; 100 g/mL PES (phenazine methosulfate)).

[0274] 3) Compound test: LC-2/AD cells (210.sup.4 cells/well) were incubated into a 96-well culture plate, the volume of cell culture fluid was 90 L, and then 10 L of the compound at each gradient concentration was added (the highest concentration was 10 M, which was diluted stepwise by , and 8 concentration points were set in total; the system contained 0.1% DMSO (dimethyl sulfoxide)). The cell plate with uniformly mixed compound was cultured in a cell culture incubator (37 C.; 5% CO.sub.2) for 48 h, then 20 L of MTS reaction solution was added, uniformly mixed and incubated in the cell culture incubator (37 C.; 5% CO.sub.2) for 1-4 hr; OD values at 490 nm were measured by a microplate reader (VARIOSKAN FLASH, Thermo). Three parallels were set in each group of experiments, with 0.1% (a final concentration) DMSO as a negative control, and a medium without cells or compounds as a blank control. The cell growth inhibition rate was calculated by the following formula:

Cell growth inhibition rate %=1(OD.sub.experimental groupOD.sub.blank group)/(OD.sub.negative groupOD.sub.blank group)100%

[0275] 4) IC.sub.50 calculation: The semi-inhibitory concentration of the compound acting on cell growth was calculated using GradPad Prism 5 software according to the measured cell growth inhibition rate.

TABLE-US-00009 TABLE 9 Growth inhibitory activity of some compounds on non-small cell lung cancer cells LC-2/AD* LC-2/AD Cmpd ID (IC.sub.50/nM) I-n-3 818.4 II-m-1 300.7 IV-n-2 1401 Cabozantinib 4148 *Cabozantinib acts as a positive control

[0276] What has been described above are only some embodiments of the invention. It will be apparent to those skilled in the art that various modifications and improvements can be made without departing from the spirit of the invention, all of which fall into the protection scope of the invention.