C07C317/46

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 propanamides, 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 propanamides, 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.

Cyclic compound

Provided is a compound, such as ethyl 6-((2-chloro-4-fluorobenzyl)sulfonyl) -3-hydroxycyclohex-1-ene-1-carboxylate or an optical isomer thereof, having a superior Toll-like receptor 4 (TLR4) signaling inhibitory action, which may be useful as a prophylactic or therapeutic drug for diseases such as autoimmune diseases and/or inflammatory diseases, or chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver failure, and ischemia reperfusion injury (IRI).

Cyclic compound

Provided is a compound, such as ethyl 6-((2-chloro-4-fluorobenzyl)sulfonyl) -3-hydroxycyclohex-1-ene-1-carboxylate or an optical isomer thereof, having a superior Toll-like receptor 4 (TLR4) signaling inhibitory action, which may be useful as a prophylactic or therapeutic drug for diseases such as autoimmune diseases and/or inflammatory diseases, or chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver failure, and ischemia reperfusion injury (IRI).

ROR GAMMA (RORy) MODULATORS

The present application relates to compounds according to (Formula IA) or (Formula IB):

##STR00001## or a pharmaceutically acceptable salt thereof.

The compounds can be used as inhibitors of ROR and are useful for the treatment of ROR mediated diseases.

ROR GAMMA (RORy) MODULATORS

The present application relates to compounds according to (Formula IA) or (Formula IB):

##STR00001## or a pharmaceutically acceptable salt thereof.

The compounds can be used as inhibitors of ROR and are useful for the treatment of ROR mediated diseases.

ARYL ETHERS AND USES THEREOF

The present disclosure relates to HIF-2 inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2 scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

ARYL ETHERS AND USES THEREOF

The present disclosure relates to HIF-2 inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2 scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

LXR agonists and uses thereof

This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.

LXR agonists and uses thereof

This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.