Patent classifications
C07D219/08
TRIARYLAMINE DERIVATIVE AND ORGANIC ELECTROLUMINESCENT DEVICE THEREOF
Provided are a triarylamine derivative and an organic electroluminescent device thereof, which relate to the technical field of organic electroluminescence. The triarylamine derivative has a relatively high triplet energy level, high hole mobility, a high refractive index and good film formability and thermal stability and can effectively reduce the driving voltage of the organic electroluminescent device, improve the luminescence efficiency, and extend the service life of the device when applied to the organic electroluminescent device. The triarylamine derivative has a good application effect and a good industrialization prospect in the organic electroluminescent device.
TRIARYLAMINE DERIVATIVE AND ORGANIC ELECTROLUMINESCENT DEVICE THEREOF
Provided are a triarylamine derivative and an organic electroluminescent device thereof, which relate to the technical field of organic electroluminescence. The triarylamine derivative has a relatively high triplet energy level, high hole mobility, a high refractive index and good film formability and thermal stability and can effectively reduce the driving voltage of the organic electroluminescent device, improve the luminescence efficiency, and extend the service life of the device when applied to the organic electroluminescent device. The triarylamine derivative has a good application effect and a good industrialization prospect in the organic electroluminescent device.
OXOACRIDINYL ACETIC ACID DERIVATIVES AND METHODS OF USE
Compounds of Formula I or pharmaceutically acceptable salts or esters thereof capable of binding to and modulating the activity of a stimulator of interferon genes (STING) protein are provided. Methods involving compounds of Formula I as effective modulators of STING are also provided.
OXOACRIDINYL ACETIC ACID DERIVATIVES AND METHODS OF USE
Compounds of Formula I or pharmaceutically acceptable salts or esters thereof capable of binding to and modulating the activity of a stimulator of interferon genes (STING) protein are provided. Methods involving compounds of Formula I as effective modulators of STING are also provided.
hTERT MODULATORS AND METHODS OF USE
The present invention provides hTERT modulators and methods for producing and using the same. In particular, the present invention provide a compound of the formula:
##STR00001##
whereas, n, R.sup.1, R.sup.2, R.sup.3, R.sup.H and R.sup.12 are as defined herein.
hTERT MODULATORS AND METHODS OF USE
The present invention provides hTERT modulators and methods for producing and using the same. In particular, the present invention provide a compound of the formula:
##STR00001##
whereas, n, R.sup.1, R.sup.2, R.sup.3, R.sup.H and R.sup.12 are as defined herein.
RADIOLABELLED COMPOUND OF A QUATERNARY AMMONIUM SALT OF A POLYCYCLIC AROMATIC AMINE AND METHODS OF MANUFACTURING AND DIAGNOSTIC USE THEREOF
The disclosure relates to a radioisotope-labelled compound having a structure according to formula I, wherein a wavy line indicates a single bond between a non-nodal carbon atom of a polycyclic aromatic system and an R.sup.1 substituent selected from a hydrogen; a halogen; a hydroxy; a protected hydroxy; a C.sub.1-4 alkoxy; a nitro group; an amino group; an amino group having 1 hydrogen replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogens replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogen atoms replaced with C.sub.2-5 alkylene to form a heterocyclic ring; a chain C.sub.1-6 carbon group; a chain C.sub.1-6 carbon group having a substituent selected from a halogen, carboxyl, a formyl, and a C.sub.1-4 alkanesulfonic; a phenyl group; a phenyl group having 1-5 substituents independently selected from halogens, a chain C.sub.1-6 carbon, a halogenated chain C.sub.1-6 carbon substituent, a hydroxy, a protected hydroxy, a C.sub.1-4 alkoxy, and an amino group having 1-2 atoms of hydrogen replaced with C.sub.1-6 alkyl; wherein R.sup.2 is a chain aliphatic substituent having: a total of 1-16 carbon atoms, an atom of .sup.18F fluorine radioisotope replacing a hydrogen atom at one of the carbon atoms, and a —CH.sub.2 fragment as a terminal member of a chain, wherein the chain connects to one of a hydrogen, a phenyl group, and a phenyl group having 1-3 substituents selected from halogens and C.sub.1-6 alkyl, and wherein if the chain contains at least 2 carbon atoms and there is a bivalent link between the chain carbon atoms, then the bivalent link is selected from the group consisting of an oxygen atom —O—, a sulfur atom —S—, and a C.sub.3-6 cycloalkylene; wherein R.sup.3 and R.sup.4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to adjacent non-nodal carbon atoms of a B ring to form an aromatic C ring fused with an A and B ring system, having R.sup.1 substituents at non-nodal carbon atoms; wherein n is an integer of 9; wherein X.sup.− is a pharmaceutically acceptable counter ion selected from: an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkane carboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid, a hydrate thereof, and a solvate thereof.
##STR00001##
RADIOLABELLED COMPOUND OF A QUATERNARY AMMONIUM SALT OF A POLYCYCLIC AROMATIC AMINE AND METHODS OF MANUFACTURING AND DIAGNOSTIC USE THEREOF
The disclosure relates to a radioisotope-labelled compound having a structure according to formula I, wherein a wavy line indicates a single bond between a non-nodal carbon atom of a polycyclic aromatic system and an R.sup.1 substituent selected from a hydrogen; a halogen; a hydroxy; a protected hydroxy; a C.sub.1-4 alkoxy; a nitro group; an amino group; an amino group having 1 hydrogen replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogens replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogen atoms replaced with C.sub.2-5 alkylene to form a heterocyclic ring; a chain C.sub.1-6 carbon group; a chain C.sub.1-6 carbon group having a substituent selected from a halogen, carboxyl, a formyl, and a C.sub.1-4 alkanesulfonic; a phenyl group; a phenyl group having 1-5 substituents independently selected from halogens, a chain C.sub.1-6 carbon, a halogenated chain C.sub.1-6 carbon substituent, a hydroxy, a protected hydroxy, a C.sub.1-4 alkoxy, and an amino group having 1-2 atoms of hydrogen replaced with C.sub.1-6 alkyl; wherein R.sup.2 is a chain aliphatic substituent having: a total of 1-16 carbon atoms, an atom of .sup.18F fluorine radioisotope replacing a hydrogen atom at one of the carbon atoms, and a —CH.sub.2 fragment as a terminal member of a chain, wherein the chain connects to one of a hydrogen, a phenyl group, and a phenyl group having 1-3 substituents selected from halogens and C.sub.1-6 alkyl, and wherein if the chain contains at least 2 carbon atoms and there is a bivalent link between the chain carbon atoms, then the bivalent link is selected from the group consisting of an oxygen atom —O—, a sulfur atom —S—, and a C.sub.3-6 cycloalkylene; wherein R.sup.3 and R.sup.4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to adjacent non-nodal carbon atoms of a B ring to form an aromatic C ring fused with an A and B ring system, having R.sup.1 substituents at non-nodal carbon atoms; wherein n is an integer of 9; wherein X.sup.− is a pharmaceutically acceptable counter ion selected from: an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkane carboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid, a hydrate thereof, and a solvate thereof.
##STR00001##
NOVEL ACRIDINIUM SALT AND METHOD FOR PRODUCING SAME
The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt.
##STR00001##
wherein R.sup.1 is C1-C6 alkyl or C1-C6 alkyloxy; R.sup.2 is hydrogen or C1-C6 alkyloxy; R.sup.3 is hydrogen, halogen, C1-C6 alkyl or C1-C6 alkyloxy; R.sup.4 is hydrogen, C1-C6 alkyloxy, halo C1-C6 alkyloxy or C1-C6 alkylamino; R.sup.5 is C1-C3 alkyl; and X.sup.− is an anion.
Oxoacridinyl acetic acid derivatives and methods of use
Compounds of Formula I or pharmaceutically acceptable salts or esters thereof capable of binding to and modulating the activity of a stimulator of interferon genes (STING) protein are provided. Methods involving compounds of Formula I as effective modulators of STING are also provided.