Abstract: The present invention relates to the compound of formula (I) and salts, stereoisomers, tautomers, isotopologues, or N-oxides thereof. The present invention is further concerned with the use of such a compound or salt, stereoisomer, tautomer, isotopologues, or N-oxide thereof as medicament and a pharmaceutical composition comprising said compound.

Abstract: The present invention relates to pyrazolidine derivatives and related compounds, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of such compounds and pharmaceutical compositions for the prophylaxis and treatment of medical conditions that can be affected by inhibiting lactate dehydrogenase (LDH), in particular LDHA and/or LDHB.

Abstract: Disclosed are substituted tricyclic benzimidazoles compounds as defined herein in formula (I) or pharmaceutically acceptable salts thereof. The compounds of the invention selectively inhibit CDK8 and are therefore useful for treating diseases related to this kinase, especially colorectal and melanoma cancers and other solid and hemathological malignancies, autoimmune diseases and inflammatory diseases. Also disclosed are processes for preparing these compounds.

Abstract: A process for the preparation of a compound of formula (I) and of a acid salt (T) wherein R1 is selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R2 and R3, are, independently of each other, selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R4, R5, R6 and R7, are independently of each other, selected from the group consisting of H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, and wherein the acid salt is a 2,3-Ditoluoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid salt, 2,3-Dianisoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid mono(dimethylamide) salt or a mixture of two or more thereof, wherein the tartaric acid salt (T) of the compound of formula (I) contains at least 90% by weight of the tartaric salt of the compound of formula (Ia) based on the total weight of the acid salt of the compound of formula (I).

Abstract: Disclosed are substituted tricyclic benzimidazoles compounds as defined herein in formula (I) or pharmaceutically acceptable salts thereof. The compounds of the invention selectively inhibit CDK8 and are therefore useful for treating diseases related to this kinase, especially colorectal and melanoma cancers and other solid and hemathological malignancies, autoimmune diseases and inflammatory diseases. Also disclosed are processes for preparing these compounds.