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

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...

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Hauptverfasser: VERNIERES JEAN-CLAUDE, JANIAK PHILIP, FOSSEY VALERIE, LASSALLE GILBERT, PETIT FREDERIC, ALTENBURGER JEAN-MICHEL
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creator VERNIERES JEAN-CLAUDE
JANIAK PHILIP
FOSSEY VALERIE
LASSALLE GILBERT
PETIT FREDERIC
ALTENBURGER JEAN-MICHEL
description 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.
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[Image] [Image] ACTIVITY : Cardiant; Vasotropic; Antiinflammatory; Antiarteriosclerotic; Respiratory-Gen.; Nephrotropic; Antidiabetic; Hypotensive. 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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.</abstract><oa>free_for_read</oa></addata></record>
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS
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