发明授权
- 专利标题: Aromatic sulfone hydroxamic acid metalloprotease inhibitor
- 专利标题(中): 芳香砜异羟肟酸金属蛋白酶抑制剂
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申请号: US10337942申请日: 2003-01-07
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公开(公告)号: US06890937B2公开(公告)日: 2005-05-10
- 发明人: Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , Jeffery N. Carroll , Gary A. DeCrezcenzo , Theresa R. Fletcher , John N. Freskos , Daniel P. Getman , Gunnar J. Hanson , Susan L. Hockerman , Carol P. Howard , Stephen A. Kolodziej , Madeleine H. Li , Joseph J. McDonald , Deborah A. Mischke , Patrick B. Mullins , Joseph G. Rico , Nathan W. Stehle , Clara I. Villamil
- 申请人: Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , Jeffery N. Carroll , Gary A. DeCrezcenzo , Theresa R. Fletcher , John N. Freskos , Daniel P. Getman , Gunnar J. Hanson , Susan L. Hockerman , Carol P. Howard , Stephen A. Kolodziej , Madeleine H. Li , Joseph J. McDonald , Deborah A. Mischke , Patrick B. Mullins , Joseph G. Rico , Nathan W. Stehle , Clara I. Villamil
- 申请人地址: US MO St. Louis
- 专利权人: Pharmacia Corporation
- 当前专利权人: Pharmacia Corporation
- 当前专利权人地址: US MO St. Louis
- 代理机构: Harness, Dickey & Pierce, P.L.C.
- 优先权: WO9925687 19971114
- 主分类号: A61K31/16
- IPC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 ; C07D211/06
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 R1 and R2 are both hydrido or R1 and R2 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. R3 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.
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