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2. 发明公开

EP0780386A1 Matrix metalloprotease inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：EP0780386A1
公开(公告)日：1997-06-25
申请号：EP96119780.3
申请日：1996-12-10
申请人： F. HOFFMANN-LA ROCHE AG , AGOURON PHARMACEUTICALS, INC.
发明人： Bender, Steven Lee , Broka, Chris Allen , Campbell, Jeffrey Allen , Castelhano, Arlindo Lucas , Fisher, Lawrence Emerson , Hendricks, Robert Than , Sarma, Keshab
IPC分类号： C07D309/08 , C07D211/54 , C07D213/64 , C07D401/06 , C07D407/12 , C07D413/12 , C07D405/12 , A61K31/35 , A61K31/445
CPC分类号： C07D213/643 , C07D211/54 , C07D309/08 , C07D401/06 , C07D407/12 , C07D409/12 , C07D413/12 , Y10S514/825 , Y10S514/885 , Y10S514/90 , Y10S514/903
摘要： 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 , -SO 2 NR 8 R 9 , -SO 2 R 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.
摘要翻译：下式的化合物：其中：n为0,1或2; Y是羟基或XONH-，其中X是氢或低级烷基; R 1是氢或低级烷基; R 2是氢，低级烷基，杂烷基，芳基，芳烷基，芳基杂环烷基，环烷基，环烷基烷基，杂芳基，杂芳烷基，杂芳基杂烷基，杂环，杂环 - 低级烷基，杂环低级杂烷基或-NR 6 R 7，其中：R 6是氢，低级烷基，环烷基或环烷基烷基，芳基，杂芳基和杂芳烷基; R 7是氢，低级烷基，环烷基或环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基，-C（O）R 8，-C（O）NR 8 R 9，-SO 2 NR 8 R 9，-SO 2 R 10，芳氧基羰基或烷氧基羰基; 或R 6和R 7与它们所连接的氮原子一起代表杂环基; 其中R 8和R 9独立地是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基或杂烷基。 R 10为低级烷基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基，杂烷基或杂环; 或R 1和R 2与它们所连接的碳原子一起代表环烷基或杂环基; R 3是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基，杂芳烷基，杂烷基或低级烷氧基; R 4是氢，低级烷基，环烷基或环烷基烷基; 或R 2和R 3与它们所连接的碳一起代表环烷基或杂环基; 或R 3和R 4与它们所连接的碳一起代表环烷基或杂环基; R 5是低级烷基，环烷基，环烷基烷基，芳基，芳烷基，杂芳基或杂芳烷基; 或其药学上可接受的盐或酯表现出有用的药理学性质，特别是用作基质金属蛋白酶抑制剂，特别是用于间质胶原酶。

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