Patent classifications
C07D239/72
SOX11 INHIBITORS FOR TREATING MANTLE CELL LYMPHOMA
Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.
SOX11 INHIBITORS FOR TREATING MANTLE CELL LYMPHOMA
Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS FOR THERAPEUTIC USES
Heterocyclic compounds of formula I shown below and pharmaceutical compositions containing one of such compounds: Also disclosed is a method of treating a condition modulated by the colony-stimulating factor-1 receptor with one of the heterocyclic compounds.
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ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
The present disclosure relates to an organic electroluminescent compound represented by formula 1, and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, it is possible to provide an organic electroluminescent device having improved driving voltage, luminous efficiency, lifetime properties, and/or power efficiency.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
4,6-DI- AND 2,4,6-TRISUBSTITUTED QUINAZOLINE DERIVATIVES USEFUL FOR TREATING VIRAL INFECTIONS
This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NR′R″, C.sub.1-7alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.
4,6-DI- AND 2,4,6-TRISUBSTITUTED QUINAZOLINE DERIVATIVES USEFUL FOR TREATING VIRAL INFECTIONS
This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NR′R″, C.sub.1-7alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R′ and R″ are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.