Title:
【発明の名称】マトリックスメタロプロテアーゼ阻害因子
Document Type and Number:
Japanese Patent JPH09501430
Kind Code:
A
Abstract:
Compounds of formula (I), wherein the dashed lines denote optional double bonds; and when n is 1, 2 or 3; m is 3 or 4; A is -CH2-; R<1> is a) -CH2-R<4> where R<4> is mercapto, acetylthio, carboxy, hydroxyaminocarbonyl, N-hydroxyformamidomethyl, alkoxycarbonyl, aryloxycarbonyl, aralcoxycarbonyl, benzyloxyaminocarbonyl, or (i), where R<6> is optionally substituted aryl, wherein the aryl group is quinol-2-yl, naphth-1-yl, naphth-2-yl, pyridyl or phenyl; b) -CH(R<7>)-R<8> where R<7> is alkyl, hydroxy, amino, aminomethyl, alkylsulphonylamidomethyl, aralkylsulphonylamidomethyl, alkoxycarbonyl, alkoxycarbonylaminomethyl, alkylaminocarbonylamidomethyl, benzoxazoleaminomethyl, aminocarbonyl, or carboxy; and R<8> is carboxy, hydroxyaminocarbonyl, alkoxycarbonyl or aralkoxycarbonyl; c) -NH-CH(R<9>) -R<10> where R<9> is hydrogen, alkyl or aralkyl, and R<10> is carboxy, alkoxycarbonyl, aralkoxycarbonyl, phosphonyl or dialkylphosphonyl; R<2> is alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; and R<3> is hydrogen, halo, alkyl or alkoxy; or when n is 2 or 3; m is 3 or 4; A is -N(R<11>)-, where R<11> is hydrogen or alkyl; and R<1>, R<2> and R<3> are as defined above; or when n is 0; m is 4, 5 or 6; A is -CH(R<12>)-, where R<12> is carboxy, alkoxycarbonyl or optionally substituted carbamoyl; and R<1>, R<2> and R<3> are as defined above; as single stereoisomers or mixtures thereof; or pharmaceutically acceptable salts thereof; are useful in inhibiting matrix metalloprotease activity in mammals.
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Inventors:
Castellano, Arlind El
Liac, Ten Jay
Horn, steven
Yuan, Zenkyo
Kranz, Alexander
Liac, Ten Jay
Horn, steven
Yuan, Zenkyo
Kranz, Alexander
Application Number:
JP50644995A
Publication Date:
February 10, 1997
Filing Date:
July 27, 1994
Export Citation:
Assignee:
Syntex (USA), Inc.
International Classes:
A61K31/40; A61K31/437; A61P1/02; A61P29/00; A61P35/00; A61P43/00; C07D487/04; C07D487/08; C07D498/08; C07F9/30; C07F9/645; C07F9/6561; (IPC1-7): C07D487/04; A61K31/40; C07F9/645
Attorney, Agent or Firm:
Aoyama Ryo (2 outside people)