C07C257/12

HIV REPLICATION INHIBITING PYRIMIDINES

This invention concerns HIV replication inhibitors of formula

##STR00001##

the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(?O).sub.pR.sup.6, NHS(?O).sub.pR.sup.6, C(?O)R.sup.6, NHC(?O)H, C(?O)NHNH.sub.2, NHC(?O)R.sup.6, C(?NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, N?N, O, C(?O), C.sub.1-4alkanediyl, CHOH, S, S(?O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(?O)NHR.sup.13; C(?O)NR.sup.13R.sup.14; C(?O)R.sup.15; CH?NNHC(?O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(?NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV REPLICATION INHIBITING PYRIMIDINES

This invention concerns HIV replication inhibitors of formula

##STR00001##

the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(?O).sub.pR.sup.6, NHS(?O).sub.pR.sup.6, C(?O)R.sup.6, NHC(?O)H, C(?O)NHNH.sub.2, NHC(?O)R.sup.6, C(?NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, N?N, O, C(?O), C.sub.1-4alkanediyl, CHOH, S, S(?O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(?O)NHR.sup.13; C(?O)NR.sup.13R.sup.14; C(?O)R.sup.15; CH?NNHC(?O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(?NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

PHENOXYHALOGENPHENYLAMIDINES AND THE USE THEREOF AS FUNGICIDES

The present invention relates phenoxyhalogenphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the phenoxyhalogenphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Halogen-substituted phenoxyphenylamidines and the use thereof as fungicides

The present invention relates to halogen-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the halogen-substituted phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Halogen-substituted phenoxyphenylamidines and the use thereof as fungicides

The present invention relates to halogen-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the halogen-substituted phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

HALOGEN-SUBSTITUTED PHENOXYPHENYLAMIDINES AND THE USE THEREOF AS FUNGICIDES

The present invention relates to halogen-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the halogen-substituted phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

HALOGEN-SUBSTITUTED PHENOXYPHENYLAMIDINES AND THE USE THEREOF AS FUNGICIDES

The present invention relates to halogen-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to an agrochemical formulation for this purpose, comprising the halogen-substituted phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

HIV replication inhibiting pyrimidines

This invention concerns HIV replication inhibitors of formula ##STR00001##
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(?O).sub.pR.sup.6, NHS(?O).sub.pR.sup.6, C(?O)R.sup.6, NHC(?O)H, C(?O)NHNH.sub.2, NHC(?O)R.sup.6, C(?NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, N?N, O, C(?O), C.sub.1-4alkanediyl, CHOH, S, S(?O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(?O)NHR.sup.13; C(?O)NR.sup.13R.sup.14; C(?O)R.sup.15; CH?NNHC(?O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(?NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV replication inhibiting pyrimidines

This invention concerns HIV replication inhibitors of formula ##STR00001##
the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a.sup.1=a.sup.2-a.sup.3=a.sup.4- and -b.sup.1=b.sup.2-b.sup.3=b.sup.4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R.sup.1 is hydrogen; aryl; formyl; C.sub.1-6alkylcarbonyl; C.sub.1-6alkyl; C.sub.1-6alkyloxycarbonyl; substituted C.sub.1-6alkyl, C.sub.1-6alkylcarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyloxy; substituted C.sub.1-6alkyloxyC.sub.1-6alkylcarbonyl; R.sup.2 is hydroxy, halo, optionally substituted C.sub.1-6alkyl, C.sub.3-7cycloalkyl, optionally substituted C.sub.2-6alkenyl, optionally substituted C.sub.2-6alkynyl, C.sub.1-6alkyloxy, C.sub.1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C.sub.1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, S(?O).sub.pR.sup.6, NHS(?O).sub.pR.sup.6, C(?O)R.sup.6, NHC(?O)H, C(?O)NHNH.sub.2, NHC(?O)R.sup.6, C(?NH)R.sup.6 or a 5-membered heterocycle; X.sub.1 is NR.sup.5, NHNH, N?N, O, C(?O), C.sub.1-4alkanediyl, CHOH, S, S(?O).sub.p, X.sub.2C.sub.1-4alkanediyl- or C.sub.1-4alkanediyl-X.sub.2; R.sup.3 is NHR.sup.13; NR.sup.13R.sup.14; C(?O)NHR.sup.13; C(?O)NR.sup.13R.sup.14; C(?O)R.sup.15; CH?NNHC(?O)R.sup.16; substituted C.sub.1-6alkyl; optionally substituted C.sub.1-6alkyloxyC.sub.1-6alkyl; substituted C.sub.2-6alkenyl; substituted C.sub.2-6alkynyl; C.sub.1-6alkyl substituted with hydroxy and a second substituent; C(?NOR.sup.8)C.sub.1-4alkyl; R.sup.7; or X.sub.3R.sup.7; R.sup.4 is halo, hydroxy, C.sub.1-6alkyl, C.sub.3-7cycloalkyl, C.sub.1-6alkyloxy, cyano, nitro, polyhaloC.sub.1-6alkyl, polyhaloC.sub.1-6alkyloxy, aminocarbonyl, C.sub.1-6alkyloxycarbonyl, C.sub.1-6alkylcarbonyl, formyl, amino, mono- or di(C.sub.1-4alkyl)amino; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

AMINO ACID BASED AMPHOTERIC SURFACTANT
20180127360 · 2018-05-10 ·

Disclosed is a novel amino acid derived surfactant which is prepared by forming the salt of an alkylaminopropionic acid and a basic amino acid such as arginine which is useful in cosmetic and personal care compositions.