Azetidines

Details Azetidines Azetidines

C - Chemistry, Metallurgy

07

D

C07D 401/06 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 211/88 (2006.01) C07D 401/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 451/06 (2006.01)

Patent

CA 2195923

The present invention provides compounds of the formula (?):- (see fig. I) (I) and the pharmaceutically acceptable salts thereof, wherein R is C3-C7 cycloalkyl, aryl or C1-C6 alkyl, said C1-C6 alkyl being optionally substituted by fluoro, -COOH, -COO(C1-C4) alkyl, C3-C7 cycloalkyl, adamantyl, aryl or het1, and said C3-C7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C1- C4 alkyl, C3-C7 cycloalkyl, C1-C4 alkoxy, hydroxy, fluoro, fluoro(C1-C4) alkyl and fluoro(C1-C4)alkoxy; R' is phenyl, benzyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo and trifluoromethyl; R represents various groups; X is C1-C4 alkylene; and X1 is a direct link or C1-C6 alkylene. Such compounds and salts are useful as tachykinin antagonists.

a présente invention se rapporte à des composés de formule (?): - (voir fig. I) (I) et à leurs sels pharmaceutiquement acceptables, où R est un cycloalkyle en C3-C7, un aryle ou un alkyle en C1-C6, ledit alkyle en C1-C6 pouvant, facultativement, être substitué par un groupe fluoro, -COOH, un -COO-alkyle en C1-C4, un cycloalkyle en C3-C7, un adamantyle, un aryle ou un het1 et ledit cycloalkyle en C3-C7 pouvant, facultativement, être substitué par un ou deux substituants choisis chacun indépendamment parmi des groupements alkyle en C1-C4, cycloalkyle en C3-C7, alkoxy en C1-C4, hydroxy, fluoro, alkyle en C1-C4 portant un fluoro ou alkoxy en C1-C4 portant un fluoro; R' est un phényle, un benzyle, un naphtyle, un thiényle, un benzothiényle ou un indolyle, chacun pouvant, facultativement, être substitué par un ou deux substituants choisis indépendamment parmi les alkyles en C1-C4, les alkoxy en C1-C4, les halogènes et le trifluorométhyle; R

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