C07D261/08

PHARMACEUTICAL COMPOUNDS

The invention provides a composition of matter which:

(i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or
(ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A);
wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by:

##STR00001##

or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R.sup.1 is trifluoromethyl; R.sup.2 is hydrogen; R.sup.3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar.sup.1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R.sup.5 as defined herein; and R.sup.4; R.sup.5 when present, R.sup.6 and R.sup.7 independently selected from various substituents as defined herein.

Also provided are individual atropisomers, pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers.

CANNABINOID DERIVATIVES

This disclosure relates to cannabinoid derivatives of Formula (I), wherein R4 or R7 is a carboxamide group, pharmaceutical compositions comprising these compounds and methods of using the cannabinoid derivatives. These compounds are potential cannabinoid receptor inhibitors, including CB1 and CB2 receptors.

CANNABINOID DERIVATIVES

This disclosure relates to cannabinoid derivatives of Formula (I), wherein R4 or R7 is a carboxamide group, pharmaceutical compositions comprising these compounds and methods of using the cannabinoid derivatives. These compounds are potential cannabinoid receptor inhibitors, including CB1 and CB2 receptors.

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR USE AS PROTEOLYSIS TARGETING CHIMERA LIGANDS
20230078913 · 2023-03-16 ·

The present invention relates to bifunctional Proteolysis Targeting Chimeric ligands (Protac compounds) comprising a ligase modulator/binder and a molecule that binds to a protein target of interest, and methods of treating various diseases and conditions with the Protac compounds, including diseases associated with androgen receptors.

[1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##

[1.1.1] bicyclo compounds as indoleamine 2,3-dioxygenase inhibitors

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##

MODULATORS OF INTEGRATED STRESS RESPONSE PATHWAY

The present disclosure relates generally to therapeutic agents that may be useful as modulators of Integrated Stress Response (ISR) pathway.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001##

or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

Anti-fibrotic compounds

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.