C07D473/04

Method for preparing a marked purine derivative, said derivative and uses thereof

The present invention relates to a method for preparing a 2-fluoropurine marked with the radioisotope .sup.18F comprising a fluorination step for a 2-nitropurine derivative. The present invention comprises a 2-fluoropurine derivative marked with the radioisotope .sup.18F which can be obtained by or during a method according to the invention and its various uses.

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.

POLYMORPHS

The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

POLYMORPHS

The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

SPECIFICALLY-SHAPED CRYSTAL OF COMPOUND AND METHOD FOR PRODUCING SAME

The present invention provides a method for obtaining a specifically-shaped crystal (specifically, spherocrystal) of a compound with good reproducibility. This method for producing a specifically-shaped crystal (specifically spherocrystal) of a compound comprises: (1) a step for preparing a supersaturated solution of a compound having a degree of supersaturation equal to or higher than a critical degree of supersaturation; and (2) a step for precipitating a specifically-shaped crystal (specifically spherocrystal) of a compound from the supersaturated solution.

Polymorphs

The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

Polymorphs

The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament.

INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF LINAGLIPTIN AND ITS SALTS

Disclosed are new intermediates for the synthesis of Linagliptin and of its salts and a process for its preparation involving said intermediates.

INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF LINAGLIPTIN AND ITS SALTS

Disclosed are new intermediates for the synthesis of Linagliptin and of its salts and a process for its preparation involving said intermediates.

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.