Title:
【発明の名称】マトリックスメタロプロテアーゼ阻害剤
Document Type and Number:
Japanese Patent JP2921673
Kind Code:
B2
Abstract:
Compounds of the formula: wherein: n is 0, 1 or 2; Y is hydroxy or XONH-, where X is hydrogen or lower alkyl; R<1> is hydrogen or lower alkyl; R<2> is hydrogen, lower alkyl, heteroalkyl, aryl, aralkyl, arylheteroalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heteroarylheteroalkyl, heterocyclo, heterocylo-lower alkyl, heterocyclo-lower heteroalkyl or -NR<6>R<7>, wherein: R<6> is hydrogen, lower alkyl, cycloalkyl or cycloalkylalkyl, aryl, heteroaryl and heteroaralkyl; R<7> is hydrogen, lower alkyl, cycloalkyl or cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, -C(O)R<8>, -C(O)NR<8>R<9>, -SO2NR<8>R<9>, -SO2R<10>, aryloxycarbonyl, or alkoxycarbonyl; or R<6> and R<7> together with the nitrogen atom to which they are attached represent a heterocyclo group; wherein R<8> and R<9> are independently hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl or heteroalkyl; and R<10> is lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heteroalkyl or heterocyclo; or R<1> and R<2> together with the carbon atom to which they are attached represent a cycloalkyl or heterocyclo group; R<3> is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heteroalkyl or lower alkoxy; R<4> is hydrogen, lower alkyl, cycloalkyl or cycloalkylalkyl; or R<2> and R<3> together with the carbons to which they are attached represent a cycloalkyl or heterocyclo group; or R<3> and R<4> together with the carbon to which they are attached represent a cycloalkyl or heterocyclo group; and R<5> is lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or pharmaceutically acceptable salts or esters thereof exhibit useful pharmacological properties, in particular for use as matrix metalloprotease inhibitors, particularly for interstitial collagenases.
Inventors:
SUTEIIBUN RII BENDAA
KURISU AREN BUROOKA
JEFURII AREN KYANBERU
AARINDO RUUKASU KASUTERUHANO
ROBAATO ZAN HENDORITSUKUSU
KEISHOOBU SAAMA
ROORENSU EMAASON FUITSUSHAA
KURISU AREN BUROOKA
JEFURII AREN KYANBERU
AARINDO RUUKASU KASUTERUHANO
ROBAATO ZAN HENDORITSUKUSU
KEISHOOBU SAAMA
ROORENSU EMAASON FUITSUSHAA
Application Number:
JP34075296A
Publication Date:
July 19, 1999
Filing Date:
December 20, 1996
Export Citation:
Assignee:
EFU HOFUMAN RA ROSHU UNTO CO AG
AGUURON PHARM INC
AGUURON PHARM INC
International Classes:
A61K31/00; A61K31/10; A61K31/165; A61K31/18; A61K31/185; A61K31/34; A61K31/341; A61K31/35; A61K31/351; A61K31/38; A61K31/381; A61K31/382; A61K31/44; A61K31/4402; A61K31/4427; A61K31/4433; A61K31/445; A61K31/4465; C07D333/34; A61P1/00; A61P1/02; A61P3/00; A61P5/00; A61P19/00; A61P19/10; A61P27/00; A61P27/02; A61P29/00; A61P35/00; A61P43/00; C07C259/06; C07C315/02; C07C317/44; C07C323/51; C07D211/54; C07D213/64; C07D213/643; C07D307/14; C07D309/08; C07D335/02; C07D401/04; C07D401/06; C07D405/12; C07D407/12; C07D409/12; C07D413/12; (IPC1-7): C07C317/44; A61K31/00; A61K31/165; A61K31/34; A61K31/35; A61K31/38; A61K31/44; A61K31/445; C07C323/51; C07D211/54; C07D213/64; C07D307/14; C07D309/08; C07D333/34; C07D335/02; C07D401/04; C07D409/12
Domestic Patent References:
| JP5527116A | ||||
| JP4502008A | ||||
| JP7505387A |
Attorney, Agent or Firm:
Hajime Tsukuni (1 person outside)