Optical active 1,4-dihydropyridine compounds as bradykinin...

Details Optical active 1,4-dihydropyridine compounds as bradykinin... Optical active 1,4-dihydropyridine compounds as bradykinin...

C - Chemistry, Metallurgy

07

D

C07D 211/90 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 451/04 (2006.01) C07D 451/14 (2006.01) C07D 453/02 (2006.01) C07D 453/06 (2006.01)

Patent

CA 2245041

This invention provides a compound of the forrnula ( I): <see fig. 1> and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; R1 and R2 are independently C1-4 alkyl; R3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group selected from C5-10 azacycloalkyl, C6-l0 diazacycloalkyl, C7-10 azabicycloalkyl and the like; and R4 is selected from (a) substituted or unsubstituted C1-8 alkyl; (b) substituted or unsubstituted amino; (c) substituted or unsubstituted C2-6 alkanoyl; (d) substituted or unsubstituted C3-8 cycloalkyl or C7-14 bicycloalkyl; (e) substituted or unsubstituted C5-10 azacycloalkyl or C6-10 diazacycloalkyl, and (f) substituted or unsubstituted C7-14 mono- or di-azabicycloalkyl. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound, and intermediates of the above compounds.

L'invention fournit un composé de la formule (I) : <voir fig. I> et ses sels utilisables en pharmacie. Dans la formule, A1 et A2 sont chacun un atome d'halogène; R1 et R2 sont indépendamment l'un de l'autre un alkyle en C1-4; R3 est un groupement phényle ou naphthyle substitué ou non substitué; Y est un groupement hétérocyclique choisi entre un azacycloalkyle en C5-10, un diazacycloalkyle en C6-10, un azabicycloalkyle en C7-10 et autres groupements du genre; et R4 est choisi entre (a) un alkyle en C1-8 substitué ou non substitué; (b) une amine substituée ou non substituée; (c) un alcanoyle en C2-6 substitué ou non substitué; (d) un cycloalkyle en C3-8 ou un bicycloalkyle en C7-14 substitué ou non substitué; (e) un azacycloalkyle en C5-10 ou un diazacycloalkyle en C6-10 substitué ou non substitué et (f) un mono-azabicycloalkyle ou un di-azabicycloalkyle en C7-14 substitué ou non substitué. Ces composés sont utiles pour le traitement de conditions médicales causées par la bradykinine comme l'inflammation, la maladie cardio-vasculaire, la douleur, etc. Cette invention fournit aussi une composition pharmaceutique comprenant le composé susmentionné, ainsi que des intermédiaires des composés susmentionnés.

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