C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/14 (2006.01) A61K 31/401 (2006.01) A61P 9/10 (2006.01) C07D 403/12 (2006.01) C07D 407/12 (2006.01) C07D 409/14 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07D 498/04 (2006.01) C07K 5/06 (2006.01) C07K 5/08 (2006.01) C07K 5/10 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2418041
Novel pyrrolidine derivatives, being useful as chymase inhibitor or intermediate for synthesis of the active compounds, which has the formula (I): wherein R1 is cycloalkyl, substituted or unsubstituted phenyl or naphthyl, indanyl, thienyl, furyl, substituted or unsubstituted indolyl, benzofuryl, substituted or unsubstituted benzothienyl, etc.; R2 is H, alkyl, phenyl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl; R3 is (i) substituted or unsubstituted monocyclic heterocyclic group, (ii) substituted or unsubstituted, benzene- or pyridine-fused heterocyclic group, or (iii) a group (a): R4 and R5 are independently H or OH, but R4 and R5 are not simultaneously H, or both form oxo; n is 0, 1, 2 or 3; or a salt thereof.
L'invention concerne des dérivés de la pyrrolidine, utiles en tant qu'inhibiteurs de la chymase ou en tant qu'intermédiaire pour la synthèse de ses composés actifs, de formule (I): dans laquelle R?1¿ est cycloalkyle, phényle substitué ou non substitué ou naphthyle substitué ou non substitué, indanyle, thiényle, furyle, indolyle substitué ou non substitué, benzofuryle, benzothiényle substitué ou non substitué, etc.; R?2¿ représente H, alkyle, phényl-alkyle inférieur, cycloalkyle ou cycloalkyl-alkyle inférieur; R?3¿ signifie (i) un groupe monocyclique hétérocyclique substitué ou non substitué, (ii) un groupe hétérocyclique fondu par benzène ou par pyridine, substitué ou non substitué, ou (iii) un groupe (a): ; R?4¿ et R?5¿ sont indépendamment H ou OH, mais pas simultanément H, ou tous deux forment oxo; n est 0, 1, 2 ou 3; ou un sel de ceux-ci.
Boyle Robert George
Deguchi Takashi
Fujitani Buichi
Honda Yayoi
Kiyoshi Akihiko
Dainippon Pharmaceutical Co. Ltd.
Kirby Eades Gale Baker
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