5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS

摘要

5,6-Bisaryl-2-pyridine-carboxamide compounds (I) and their salts, enantiomers, diastereoisomers or racemic mixture, are new. 5,6-Bisaryl-2-pyridine-carboxamide compounds of formula (I) and their salts, enantiomers, diastereoisomers or racemic mixture, are new. X, Y 1N or CR3; R3 : H, halo, alkyl or alkoxy; A : (hetero)aryl or heterocycloalkyl like phenyl, thienyl, thiazolyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, pyrazolyl or pyrrolidinone (all optionally substituted by 1-3 groups like halo, (fluoro)alkyl, OH, alkoxy, -NRR1a, -NR-CO-alkyl, -SO- or -SO 2-alkyl); W 1bond or (cyclo)alkylene (optionally substituted by 1 or 2 groups like halo, alkyl, OH or alkoxy); B 1-NR4R5 or heterocyclic ring of formula (a); either R4, R5 : (cyclo)alkyl or fluoroalkyl; or NR4R5 : 5 or 6 membered ring e.g. pyrrolidinyl or piperidinyl (optionally substituted by alkyl); m, n : 0-2; R1a, R6, R7 : H or alkyl; either R1, R2 : H, (cyclo)alkyl, phenyl, benzyl or -CH 2-indolyl (all optionally substituted by halo, (fluoro)alkyl, OH or -O-CO-alkyl); or CR1R2 : mono-/polycyclic ring like cycloalkyl, indanyl, tetrahydropyranyl, piperidine, tetrahydronaphtyl, bicyclo[2.2.1]heptyl, bicyclo[3.3.1]nonyl or adamantyl (all optionally substituted by halo, (fluoro)alkyl, OH, alkoxy, formyl or acetyl); and p : 0-1. [Image] [Image] ACTIVITY : Cardiant; Vasotropic; Antiinflammatory; Antiarteriosclerotic; Respiratory-Gen.; Nephrotropic; Antidiabetic; Hypotensive. MECHANISM OF ACTION : Urotensine II receptor antagonist.