C07D473/04

2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors

Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): ##STR00001##
that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.

2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors

Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): ##STR00001##
that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.

SMALL MOLECULES AGAINST CEREBLON TO ENHANCE EFFECTOR T CELL FUNCTION

Disclosed are small molecules against cereblon to enhance effector T cell function. Methods of making these molecules and methods of using them to treat various disease states are also disclosed.

Crystalline linagliptin intermediate and process for preparation of linagliptin

The present invention provides novel crystalline forms B1 & B2 of linagliptin intermediate of structural formula V and methods for production of novel crystalline form of linagliptin intermediate represented by the following structural formula V.

Crystalline linagliptin intermediate and process for preparation of linagliptin

The present invention provides novel crystalline forms B1 & B2 of linagliptin intermediate of structural formula V and methods for production of novel crystalline form of linagliptin intermediate represented by the following structural formula V.

2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors

Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): ##STR00001##
that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.

DUAL SELECTIVE PI3 DELTA AND GAMMA KINASE INHIBITORS

The present invention relates to dual delta () and gamma () PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

DUAL SELECTIVE PI3 DELTA AND GAMMA KINASE INHIBITORS

The present invention relates to dual delta () and gamma () PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

XANTHINE DERIVATIVES AND USES THEREOF AS INHIBITORS OF BROMODOMAINS OF BET PROTEINS

The present invention relates to a compound having the following formula (I): (I) wherein: R is a (C.sub.1-C.sub.6)alkyl group; R is preferably H; Ar is a (C.sub.5-C.sub.12)arylene radical; X.sub.1 is C(O) or SO.sub.2; and R is chosen from the group consisting of possibly substituted (C.sub.1-C.sub.6)alkyl, heteroaryl, (C.sub.5-C.sub.12)aryl, and (hetero)cycloalkyl groups, or a pharmaceutically acceptable salt and/or tautomeric form thereof, or its racemates, diastereomers or enantiomers

##STR00001##

XANTHINE DERIVATIVES AND USES THEREOF AS INHIBITORS OF BROMODOMAINS OF BET PROTEINS

The present invention relates to a compound having the following formula (I): (I) wherein: R is a (C.sub.1-C.sub.6)alkyl group; R is preferably H; Ar is a (C.sub.5-C.sub.12)arylene radical; X.sub.1 is C(O) or SO.sub.2; and R is chosen from the group consisting of possibly substituted (C.sub.1-C.sub.6)alkyl, heteroaryl, (C.sub.5-C.sub.12)aryl, and (hetero)cycloalkyl groups, or a pharmaceutically acceptable salt and/or tautomeric form thereof, or its racemates, diastereomers or enantiomers

##STR00001##