Inhibitors of dipeptidyl peptidase IV
AssigneeFerring B.V.
InventorsDavid Michael Evans, Gary Robert William Pitt
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Abstract
Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV. Pharmaceutical compositions of the compounds of the invention, or pharmaceutically acceptable salts thereof, are useful in the treatment of, inter alia, type 2 diabetes
Claims10
A compound selected from compounds of formula 1, tautomers and stereoisomers, diastereoisomers, enantiomers and epimers thereof, and pharmaceutically acceptable salts of said compounds, tautomers, stereoisomers, diastereoisomers, enantiomers and epimers,
- wherein:
- R1 is either a hydrogen atom or a nitrile group;
- X1 is selected from a sulphur atom, an oxygen atom, a sulphonyl group and a methylene group;
- X2 is a carbonyl group, a methylene group or a covalent bond;
- Het is an aromatic nitrogen-containing heterocycle selected from pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl and benz-fused analogues thereof, all of which may optionally be substituted on one or more carbon atoms, and where the substituents are selected from C1–C6 alkyl, hydroxy, C1–C6 alkyloxy, amino, C1–C6 alkylamino, di(C1–C6 alkyl)amino, fluoro, chloro, bromo, trifluoromethyl, nitro, cyano, carboxy and C1–C6 alkyloxycarbonyl groups;
- and
- n is 1–5.
A compound according to claim wherein the stereochemistry of the nitrile group is as shown in formula 2
Dependencies are inferred from the claim text.