发明名称 Aromatic sulfone hydroxamic acid metalloprotease inhibitor.
摘要 A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R<SUP>1 </SUP>and R<SUP>2 </SUP>are both hydrido or R<SUP>1 </SUP>and R<SUP>2 </SUP>together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R<SUP>3 </SUP>in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
申请公布号 ZA9810412(B) 申请公布日期 1999.12.09
申请号 ZA19980010412 申请日期 1998.11.13
申请人 G D SEARLE & CO. 发明人 THOMAS E. BARTA;DANIEL P. BECKER;TERRI L. BOEHM;GARY A. DE CRESCENZO;CLARA I. VILLAMIL;JOSEPH J. MCDONALD;JOHN N. FRESKOS;DANIEL P. GETMAN
分类号 A61K31/16;A61K31/167;A61K31/27;A61K31/35;A61K31/351;A61K31/357;A61K31/366;A61K31/38;A61K31/381;A61K31/382;A61K31/39;A61K31/4427;A61K31/443;A61K31/4433;A61K31/444;A61K31/445;A61K31/4465;A61K31/4525;A61K31/454;A61K31/496;A61K31/505;A61K31/506;A61K31/5375;A61K31/54;A61K31/541;A61P1/02;A61P1/04;A61P9/10;A61P13/00;A61P19/00;A61P19/02;A61P25/28;A61P27/02;A61P29/00;A61P35/00;A61P35/04;A61P43/00;C07C317/44;C07C319/06;C07D211/66;C07D211/94;C07D211/96;C07D239/04;C07D279/06;C07D309/08;C07D309/12;C07D319/06;C07D327/02;C07D333/38;C07D335/02;C07D337/04;C07D401/06;C07D401/12;C07D405/12;C07D405/14;C07D407/12;C07D409/12;C07D409/14;C07D413/06;C07D413/12;C07D413/14;C07D417/12;C07D521/00 主分类号 A61K31/16
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