C07D237/28

Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase

Compounds of formula (VII), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pertaining to said compounds.

Imino sulfanone inhibitors of ENPP1

The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.

Imino sulfanone inhibitors of ENPP1

The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.

MEMBRANE-ACTIVE ANTI-BACTERIAL COMPOUNDS AND USES THEREOF

In an embodiment, the present disclosure pertains to methods of inhibiting bacterial growth. Generally, the methods include exposing bacteria to an anti-bacterial compound as disclosed herein. In some embodiments, the exposing occurs in vivo in a subject in order to treat or prevent a bacterial infection. In additional embodiments, the present disclosure pertains to anti-bacterial compounds that are suitable for inhibiting bacterial growth.

MEMBRANE-ACTIVE ANTI-BACTERIAL COMPOUNDS AND USES THEREOF

In an embodiment, the present disclosure pertains to methods of inhibiting bacterial growth. Generally, the methods include exposing bacteria to an anti-bacterial compound as disclosed herein. In some embodiments, the exposing occurs in vivo in a subject in order to treat or prevent a bacterial infection. In additional embodiments, the present disclosure pertains to anti-bacterial compounds that are suitable for inhibiting bacterial growth.

Fused bicyclic benzoheteroaromatic compounds and methods of use thereof

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, isotopic form, stereoisomer or prodrug thereof, wherein A, B, X, R1, R2a, R2b, R2c, L, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. ##STR00001##

NOVEL CDK 8/19 INHIBITORS

The present invention relates to novel compounds of formula (1), which have the properties of a CDK8/19 inhibitor, and to a pharmaceutical composition containing said compounds, and to the use of said compounds and composition as pharmaceutical preparations for treating diseases or disorders.

NOVEL CDK 8/19 INHIBITORS

The present invention relates to novel compounds of formula (1), which have the properties of a CDK8/19 inhibitor, and to a pharmaceutical composition containing said compounds, and to the use of said compounds and composition as pharmaceutical preparations for treating diseases or disorders.

CINNOLINE COMPOUNDS AND USES THEREOF

Cinnoline compounds of formula (I):

##STR00001##

variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the cinnoline compounds.

CINNOLINE COMPOUNDS AND USES THEREOF

Cinnoline compounds of formula (I):

##STR00001##

variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the cinnoline compounds.