M-substituted benzoic acid derivatives having integrin...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/42 (2006.01) A61K 31/606 (2006.01) A61P 7/02 (2006.01) A61P 9/00 (2006.01) A61P 19/00 (2006.01) A61P 35/00 (2006.01) C07C 229/54 (2006.01) C07C 229/60 (2006.01) C07D 211/52 (2006.01) C07D 239/14 (2006.01) C07D 401/04 (2006.01) C07D 401/12 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2392209

m-Substituted benzoic acid derivatives represented by general formula (I) and exhibiting integrin .alpha.v.beta.3 antagonism; and intermediates for preparing the same [wherein A is an optionally substituted mono- or bi-cyclic heterocycle group containing two nitrogen atoms, or the like; D is a bond, >NR4, >CR5R6, -NR4-CR5R6-, or the like; X is CH or N; R7 to R9 are each hydroxyl, alkyl, or the like; Q is >C=O or the like; J is a bond or alkylene; and R10 is optionally substituted hydroxyl, amino, or the like]. These derivatives are useful in the treatment or prevention of cardiovascular diseases, vascularization-related diseases, cerebrovascular diseases, cancers and metastases thereof, immunologic diseases, bone diseases, and so on.

Dérivés d'acide benzoïque à substitution m de formule générale (I), qui présentent un antagonisme contre l'intégrine .alpha.¿v?.beta.¿3?, et intermédiaires permettant de préparer lesdits dérivés. Dans la formule, A est un groupe hétérocycle monocyclique ou bicyclique éventuellement substitué contenant deux atomes d'azote, ou analogue, D est une liaison, >NR?4¿, >CR?5¿R?6¿, -NR?4¿-CR?5¿R?6¿-, ou analogue, X représente CH ou N, R?7¿ à R?9¿ représentent chacun hydroxyle, alkyle, ou analogue, Q représente >C=O, ou analogue, J représente une liaison ou alkylène, et R?10¿ est hydroxyle, amino éventuellement substitué, ou analogue. Lesdits dérivés sont utiles pour traiter ou prévenir les maladies cardiovasculaires, les maladies associées à la vascularisation, les maladies cérébrovasculaires, les cancers et leurs métastases, les maladies immunologiques, les maladies osseuses etc.

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