ALTENBURGER, JEAN-MICHEL,FOSSEY, VALERIE,LASSALLE, GILBERT,PETIT, FREDERIC,VERNIERES, JEAN-CLAUDE,JANIAK, PHILIP
申请号：
EP07823409.3
公开号：
EP2059508B1
申请日:
2007.08.09
申请国别(地区):
EP
年份:
2012
代理人:
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.L'invention concerne des composés répondant à la formule (I) : dans laquelle X, Y, U, A, B, W, Z, R1 et R2 sont tels que définis dans la description. Procédé de préparation et application en thérapeutique.
