C07C255/54

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR

The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

Phenoxyalkylamine compound

The invention provides a compound having a selective inhibitory activity against highly-expressed LAT-1 in tumor cell. The compound is represented by the formula (I): ##STR00001##
wherein each symbol is as defined in the specification, or a salt thereof, and a LAT-1 inhibitor comprising the same.

Phenoxyalkylamine compound

The invention provides a compound having a selective inhibitory activity against highly-expressed LAT-1 in tumor cell. The compound is represented by the formula (I): ##STR00001##
wherein each symbol is as defined in the specification, or a salt thereof, and a LAT-1 inhibitor comprising the same.

PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN THE PREPARATION OF HEPATITIS C VIRUS (HCV) INHIBITORS

The present invention generally relates to a process for preparation of 9-halo-3-(2-haloacetyl)-10,11-dihydro-5H-dibenzo[c,g]chromen-8(9H)-one of Formula I, which is an intermediate in the preparation of Hepatitis C Virus (HCV) inhibitors.

PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN THE PREPARATION OF HEPATITIS C VIRUS (HCV) INHIBITORS

The present invention generally relates to a process for preparation of 9-halo-3-(2-haloacetyl)-10,11-dihydro-5H-dibenzo[c,g]chromen-8(9H)-one of Formula I, which is an intermediate in the preparation of Hepatitis C Virus (HCV) inhibitors.

INDANE DERIVATIVES AS HYPOXIA INDUCIBLE FACTOR-2(ALPHA) INHIBITORS
20210380536 · 2021-12-09 ·

The present disclosure provides certain indane compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

INDANE DERIVATIVES AS HYPOXIA INDUCIBLE FACTOR-2(ALPHA) INHIBITORS
20210380536 · 2021-12-09 ·

The present disclosure provides certain indane compounds that are Hypoxia Inducible Factor 2α (HIF-2α) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2α. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

METHOD OF MAKING PERFLUOROCYCLOBUTANE-CONTAINING MONOMER

The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.

METHOD OF MAKING PERFLUOROCYCLOBUTANE-CONTAINING MONOMER

The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.