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公开(公告)号:US07115632B1
公开(公告)日:2006-10-03
申请号:US09569034
申请日:2000-05-11
申请人: Louis J Bedell , Joseph J McDonald , Thomas E Barta , Daniel P Becker , Rao N Shashidhar , John N Freskos , Brent V Mischke , Daniel P Getman , Gary A DeCrescenzo , Clara I Villamil
发明人: Louis J Bedell , Joseph J McDonald , Thomas E Barta , Daniel P Becker , Rao N Shashidhar , John N Freskos , Brent V Mischke , Daniel P Getman , Gary A DeCrescenzo , Clara I Villamil
IPC分类号: A61K31/445 , C07D401/12
CPC分类号: C07C311/16 , C07C311/21 , C07C317/44 , C07D207/48 , C07D211/96 , C07D295/26
摘要: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.
摘要翻译: 公开了包括抑制基质金属蛋白酶活性的磺酰芳族或杂芳族环异羟肟酸化合物,其处理方法包括将具有MMP酶抑制有效量的考虑的磺酰芳族或杂芳族环异羟肟酸化合物施用于具有条件 与病理基质金属蛋白酶活性相关。 考虑的化合物在结构上对应于下式,其中W和R基团在其他地方定义。
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公开(公告)号:US06583299B1
公开(公告)日:2003-06-24
申请号:US09572019
申请日:2000-05-16
申请人: Susan L Hockerman , Daniel P. Becker , Louis J Bedell , Gary A DeCrescenzo , John N Freskos , Daniel P Getman , Robert M Heintz , Madeleine H Li , Brent V Mischke , Clara I Villamil , Thomas E Barta
发明人: Susan L Hockerman , Daniel P. Becker , Louis J Bedell , Gary A DeCrescenzo , John N Freskos , Daniel P Getman , Robert M Heintz , Madeleine H Li , Brent V Mischke , Clara I Villamil , Thomas E Barta
IPC分类号: C07D31500
CPC分类号: C07K5/06026 , A61K38/00 , C07C317/48 , C07C317/50 , C07C323/65 , C07D307/58
摘要: A family of molecules is disclosed that inhibit matrix metalloprotease (MMP) activity, and particularly inhibit the activity of one or more of MMP-2, MMP-9, or MMP-13, while generally exhibiting little activity against MMP-1. A contemplated compound also exhibits little inhibition of the production of TNF. A contemplated compound is an &agr;-amino-&bgr;-sulfonyl carbocyclo, heterocyclo, aryl, or heteroaryl hydroxamic acid. Also disclosed are processes for preparing a contemplated compound and for treating a mammal having a condition associated with pathological matrix metalloprotease activity.
摘要翻译: 公开了分子家族抑制基质金属蛋白酶(MMP)活性,特别是抑制MMP-2,MMP-9或MMP-13中的一种或多种的活性,而通常对MMP-1几乎没有活性。 预期的化合物也对TNF的产生几乎没有抑制作用。 预期的化合物是α-氨基-β-磺酰基碳环,杂环基,芳基或杂芳基异羟肟酸。 还公开了制备预期化合物和用于治疗具有与病理基质金属蛋白酶活性相关的病症的哺乳动物的方法。
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公开(公告)号:US06750228B1
公开(公告)日:2004-06-15
申请号:US09570731
申请日:2000-05-12
申请人: Thomas E Barta , Daniel P Becker , Louis J Bedell , Terri L Boehm , Jeffrey N Carroll , Gary A DeCrescenzo , Yvette M Fobian , John N Freskos , Daniel P Getman , Joseph J McDonald , Madeleine H Li , Susan L Hockerman , Susan C Howard , Steve A Kolodziej , Deborah A Mischke , Joseph G Rico , Nathan W Stehle , Michael B Tollefson , William F Vernier , Clara I Villamil
发明人: Thomas E Barta , Daniel P Becker , Louis J Bedell , Terri L Boehm , Jeffrey N Carroll , Gary A DeCrescenzo , Yvette M Fobian , John N Freskos , Daniel P Getman , Joseph J McDonald , Madeleine H Li , Susan L Hockerman , Susan C Howard , Steve A Kolodziej , Deborah A Mischke , Joseph G Rico , Nathan W Stehle , Michael B Tollefson , William F Vernier , Clara I Villamil
IPC分类号: A61K31445
CPC分类号: C07D231/12 , C07D211/66 , C07D233/56 , C07D249/08 , C07D309/08 , C07D335/02 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12
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. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor. A contemplated compound corresponds in structure to formula B, below,
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公开(公告)号:US5985872A
公开(公告)日:1999-11-16
申请号:US448795
申请日:1995-05-24
申请人: Norman Anthony Abood , Daniel L. Flynn , Daniel P. Becker , Brian M. Bax , Hui Li , Roger A. Nosal , Lori A Schretzman , Clara I Villamil
发明人: Norman Anthony Abood , Daniel L. Flynn , Daniel P. Becker , Brian M. Bax , Hui Li , Roger A. Nosal , Lori A Schretzman , Clara I Villamil
IPC分类号: C07D265/22 , A61K31/535 , A61P31/12 , A61P43/00 , C07D265/12 , C07D265/24 , C07D413/04 , C07D413/12 , C07D417/12
CPC分类号: C07D265/24 , C07D413/04 , C07D413/12 , C07D417/12
摘要: A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.28 is selected from (a) amino substituted with one or two radicals selected from alkyl, aralkyl, heterocycoalkyl, heterocyclo, and aryl, and (b) amino acid residues and derivatives thereof; wherein R.sup.29 is selected from hydrido, alkyl, halo, ##STR2## wherein R.sup.30 is selected from alkyl, alkoxy, alkylamino, carboxyalkyl, alkoxyalkyl, alkylaminoalkyl, cycloalkyl, heterocyclo, heterocycloalkyl, heterocycloalkoxy, alkylaminoalkoxy, alkylaminoalkylamino, heterocycloalkylamino, and N-aralkylamino; wherein R.sup.31 is alkyl; wherein R.sup.32 is alkyl and aryl; or a pharmaceutically-acceptable salt thereof.
摘要翻译: 一类用于治疗病毒感染的化合物。 特别感兴趣的化合物由式II定义,其中R28选自(a)被一个或两个选自烷基,芳烷基,杂核烷基,杂环和芳基的基取代的氨基,和(b)氨基酸残基及其衍生物; 其中R 29选自氢,烷基,卤素,其中R 30选自烷基,烷氧基,烷基氨基,羧基烷基,烷氧基烷基,烷基氨基烷基,环烷基,杂环基,杂环烷基,杂环烷氧基,烷基氨基烷氧基,烷基氨基烷基氨基,杂环烷基氨基和N-芳烷基氨基。 其中R31是烷基; 其中R32是烷基和芳基; 或其药学上可接受的盐。
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