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AMINOPIPERIDINE DERIVATIVES AS INTEGRIN alpha v beta 3 ANTAGONISTS
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Title:
AMINOPIPERIDINE DERIVATIVES AS INTEGRIN alpha v beta 3 ANTAGONISTS
Author:
YAMAMOTO, MIKIO
;
MURAKAMI, SHOICHI
;
KUBOTA, DAI
;
AJITO, KEIICHI
;
ISHIKAWA, MINORU
;
KATANO, KIYOAKI
;
HACHISU, MITSUGU
Subjects:
CHEMISTRY
;
HETEROCYCLIC COMPOUNDS
;
METALLURGY
;
ORGANIC CHEMISTRY
Description:
Compounds having integrin alpha v beta 3 antagonism, cell adhesion inhibitory effect, GP IIb/IIIa antagonism and/or human platelet agglutination inhibitory effect; and remedies for cardiovascular diseases, diseases in association with neovascularization, cerebrovascular diseases, etc. and platelet agglutination inhibitors. The above compounds involve derivatives represented by general formula (I), pharmaceutically acceptable salts thereof and solvates of the same, wherein A represents a 5- to 7-membered heterocycle containing two nitrogen atoms; D represents >NH2, >CH2, etc.; X and Z represent each CH or N; R and R represent each alkyl, halogeno, etc.; Q represents >C=O, >CH2, etc.; R represents H, alkyl, aralkyl, etc.; R represents H, alkynyl, etc.; R represents H, substituted amino, etc.; R represents H or alkyl; m is from 0 to 5; n is from 0 to 4; p and q are each from 1 to 3; and r is 0 or 1. L'invention concerne des composés présentant un antagonisme à l'intégrine alpha v beta 3, un effet d'inhibition d'adhésion cellulaire, un antagonisme à GP IIb/IIIa et/ou un effet d'inhibition d'agglutination de plaquettes humaines ; l'invention concerne également des médicaments destinés au traitement d'affections cardiovasculaires, d'affections associées à une néovascularisation, d'affections cérébrales, etc. Les composés selon l'invention comprennent des dérivés représentés par la formule (I), leurs sels acceptables du point de vue pharmaceutique et leurs solvates. Dans la formule (I) de l'invention, A représente un hétérocycle de 5 à 7 éléments contenant deux atomes d'azote ; D représente >NH2, >CH2, etc. ; X et Z représentent chacun CH ou N ; R et R représentent chacun un alkyle, un halogéno etc. ; Q représente >C = 0, >CH2, etc. ; R représente H, un alkyle, un aralkyle, etc. ; R représente H, Un alcynyle, etc. ; R représente H, un amino substitué, etc. ; R représente H ou un alkyle ; m désigne un nombre de 0 à 5 ; n désigne un nombre de 0 à 4 ; p et q désignent chacun un nombre de 1 à 3 ; et r désigne 0 ou 1.
Creation Date:
1999
Language:
English;French;Japanese
Source:
esp@cenet
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