Patent classifications
C07D233/68
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 heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating 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 heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating 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.
SMALL-MOLECULE REGULATOR OF TLR8
Provided in the present disclosure is a small-molecule regulator of TLR8; a compound of formula (I) or the pharmaceutically acceptable salt thereof provided in the present disclosure has good TLR8 regulatory activity and can be used to prevent or treat diseases mediated by TLR8.
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SMALL-MOLECULE REGULATOR OF TLR8
Provided in the present disclosure is a small-molecule regulator of TLR8; a compound of formula (I) or the pharmaceutically acceptable salt thereof provided in the present disclosure has good TLR8 regulatory activity and can be used to prevent or treat diseases mediated by TLR8.
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SUBSTITUTED 4-AMINO-1H-IMIDAZO[4,5-c]QUINOLINE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION
Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.
SUBSTITUTED 4-AMINO-1H-IMIDAZO[4,5-c]QUINOLINE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION
Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.
Photoreversible acylation reagents
Reagents and methods to cloak and uncloak RNA polymers and applications thereof are provided. Photocloaking molecules are used to label RNA polymers. Radiant energy is used to remove photoreleaseable protecting adducts and revert a RNA polymer to its native form.
Substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds and improved methods for their preparation
Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.
Substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds and improved methods for their preparation
Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators.
AROMATIC SULFONAMIDE DERIVATIVES
Substituted aromatic sulfonamides of formula (I)
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pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.