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公开(公告)号:US6013649A
公开(公告)日:2000-01-11
申请号:US900028
申请日:1997-07-22
申请人: John N. Freskos , S. Zaheer Abbas , Gary A. DeCrescenzo , Daniel P. Getman , Robert M. Heintz , Brent V. Mischke , Joseph J. McDonald
发明人: John N. Freskos , S. Zaheer Abbas , Gary A. DeCrescenzo , Daniel P. Getman , Robert M. Heintz , Brent V. Mischke , Joseph J. McDonald
IPC分类号: C07D295/08 , A61K31/10 , A61K31/165 , A61K31/17 , A61K31/192 , A61K31/216 , A61K31/22 , A61K31/27 , A61K31/4164 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/5375 , A61K31/5377 , A61P43/00 , C07C317/22 , C07C317/32 , C07C323/65 , C07C327/22 , C07C327/24 , C07C327/26 , C07C327/28 , C07C327/32 , C07D213/34 , C07D213/70 , C07D233/84 , C07D277/20 , C07D277/36 , C07D295/12 , A61K31/535 , A01N37/02 , A01N37/10 , A01N37/18 , A01N41/12 , A01N43/40 , A01N43/50 , A01N43/78
CPC分类号: A61K31/10 , A61K31/17 , A61K31/4164 , A61K31/426 , A61K31/4402 , A61K31/4406 , A61K31/5377 , C07C317/22 , C07C323/65 , C07C327/24 , C07C327/26 , C07C2101/08 , C07C2101/14
摘要: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfone inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.
摘要翻译: 本发明涉及蛋白酶(蛋白酶)抑制剂,更具体地涉及用于基质金属蛋白酶13(MMP-13)的硫醇砜抑制剂,蛋白酶抑制剂的组合物,用于合成蛋白酶抑制剂的中间体,用于制备蛋白酶抑制剂的方法和方法 用于治疗与MMP-13相关的病理基质金属蛋白酶活性相关的病理状况。
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公开(公告)号:US06476027B1
公开(公告)日:2002-11-05
申请号:US09254531
申请日:1999-12-06
申请人: Clara I. Villamil , John N. Freskos , Brent V. Mischke , Patrick B. Mullins , Robert M. Heintz , Daniel P. Getman , Joseph J. McDonald , Gary A. DeCrescenzo , Thomas E. Barta , Daniel P. Becker
发明人: Clara I. Villamil , John N. Freskos , Brent V. Mischke , Patrick B. Mullins , Robert M. Heintz , Daniel P. Getman , Joseph J. McDonald , Gary A. DeCrescenzo , Thomas E. Barta , Daniel P. Becker
IPC分类号: A61K3116
CPC分类号: C07D213/30 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/16 , C07D211/62 , C07D213/82 , C07D295/15
摘要: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译: 公开了包括抑制基质金属蛋白酶活性的N-羟基磺酰基丁酰胺化合物,其处理方法包括将具有MMP酶抑制有效量的预期N-羟基磺酰基丁酰胺化合物施用于具有与病理基质相关的病症的宿主 金属蛋白酶活性。
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公开(公告)号:US06451791B1
公开(公告)日:2002-09-17
申请号:US09230205
申请日:1999-06-04
申请人: Robert M. Heintz , Daniel P. Getman , Joseph J. McDonald , Gary A. DeCrescenzo , Susan C. Howard , S. Zaheer Abbas
发明人: Robert M. Heintz , Daniel P. Getman , Joseph J. McDonald , Gary A. DeCrescenzo , Susan C. Howard , S. Zaheer Abbas
IPC分类号: A61K3118
CPC分类号: C07C311/46 , C07D213/42 , C07D213/82 , C07D295/13 , C07D309/12 , C07D417/12
摘要: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译: 公开了一种特别抑制基质金属蛋白酶活性的酰氨基芳香环磺酰胺异羟肟酸化合物,其中包括将预期的氨基芳香环磺酰胺异羟肟酸化合物以有效的MMP抑制作用给具有与病理学相关的病症的宿主 基质金属蛋白酶活性。
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公开(公告)号:US06716844B2
公开(公告)日:2004-04-06
申请号:US10005437
申请日:2001-12-03
申请人: John N. Freskos , Terri L. Boehm , Brent V. Mischke , Robert M. Heintz , Joseph J. McDonald , Gary A. DeCrescenzo , Susan C. Howard
发明人: John N. Freskos , Terri L. Boehm , Brent V. Mischke , Robert M. Heintz , Joseph J. McDonald , Gary A. DeCrescenzo , Susan C. Howard
IPC分类号: C07D40302
CPC分类号: C07D213/30 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/16 , C07D211/62 , C07D213/82 , C07D295/15
摘要: An aromatic sulfonyl aipha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译: 公开了特别抑制基质金属蛋白酶活性的芳香族磺酰基亚氨基 - 羟基异羟肟酸化合物,其中包括将预期的具有MMP酶抑制有效量的芳族磺酰基α-羟基异羟肟酸化合物施用于具有 与病理基质金属蛋白酶活性相关的病症。
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公开(公告)号:US06362183B1
公开(公告)日:2002-03-26
申请号:US09254535
申请日:1999-06-04
申请人: John N. Freskos , Terri L. Boehm , Brent V. Mischke , Robert M. Heintz , Joseph J. McDonald , Gary A. DeCrescenzo , Susan C. Howard
发明人: John N. Freskos , Terri L. Boehm , Brent V. Mischke , Robert M. Heintz , Joseph J. McDonald , Gary A. DeCrescenzo , Susan C. Howard
IPC分类号: C07D40302
CPC分类号: C07D213/30 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/16 , C07D211/62 , C07D213/82 , C07D295/15
摘要: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译: 公开了一种特别抑制基质金属蛋白酶活性的芳族磺酰基α-羟基异羟肟酸化合物,其包括将预期的具有MMP酶抑制有效量的芳族磺酰基α-羟基异羟肟酸化合物施用于宿主 具有与病理基质金属蛋白酶活性相关的病症。
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公开(公告)号:US06747027B1
公开(公告)日:2004-06-08
申请号:US08898175
申请日:1997-07-22
申请人: Gary DeCrescenzo , Zaheer S. Abbas , John N. Freskos , Daniel P. Getman , Robert M. Heintz , Brent V. Mischke , Joseph J. McDonald
发明人: Gary DeCrescenzo , Zaheer S. Abbas , John N. Freskos , Daniel P. Getman , Robert M. Heintz , Brent V. Mischke , Joseph J. McDonald
IPC分类号: A61K314965
CPC分类号: C07D295/13 , C07C311/17 , C07C311/29 , C07C323/49 , C07D207/48 , C07D211/96 , C07D213/42 , C07D317/62 , C07D409/04
摘要: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.
摘要翻译: 本发明涉及蛋白酶(蛋白酶)抑制剂,更具体地涉及用于基质金属蛋白酶13(MMP-13)的硫醇磺酰胺抑制剂,蛋白酶抑制剂的组合物,用于合成蛋白酶抑制剂的中间体,用于制备蛋白酶抑制剂的方法和方法 用于治疗与MMP-13相关的病理基质金属蛋白酶活性相关的病理状况。
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公开(公告)号:US6087359A
公开(公告)日:2000-07-11
申请号:US254534
申请日:1999-09-10
申请人: Daniel P. Getman , Daniel P. Becker , Thomas E. Barta , Clara I. Villamil , Susan L. Hockerman , Louis J. Bedell , Hui Li , John N. Freskos , Robert M. Heintz , Joseph J. McDonald , Gary A. DeCrescenzo
发明人: Daniel P. Getman , Daniel P. Becker , Thomas E. Barta , Clara I. Villamil , Susan L. Hockerman , Louis J. Bedell , Hui Li , John N. Freskos , Robert M. Heintz , Joseph J. McDonald , Gary A. DeCrescenzo
IPC分类号: C07D295/13 , C07D309/12 , A61K31/5375 , A61K31/5377 , C07D295/15 , C07D413/12
CPC分类号: C07D295/13 , C07D309/12
摘要: A thioaryl sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated thioaryl sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
摘要翻译: PCT No.PCT / US98 / 04298 Sec。 371 1999年9月10日第 102(e)1999年9月10日PCT PCT 1998年3月4日PCT公布。 第WO98 / 39313号公报 日本9月11日,日本公开了一种特别是抑制基质金属蛋白酶活性的硫代芳基磺酰胺异羟肟酸化合物,其处理方法包括将具有MMP酶抑制有效量的预期硫代芳基磺酰胺异羟肟酸化合物施用于具有相关病症的宿主 具有病理基质金属蛋白酶活性。
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公开(公告)号:US06846954B2
公开(公告)日:2005-01-25
申请号:US10199481
申请日:2002-07-22
申请人: Michael L Vazquez , Richard A. Mueller , John J. Talley , Daniel P Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
发明人: Michael L Vazquez , Richard A. Mueller , John J. Talley , Daniel P Getman , Gary A. DeCrescenzo , John N. Freskos , Robert M. Heintz , Deborah E. Bertenshaw
IPC分类号: C07D295/12 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4433 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K38/00 , A61P31/12 , C07C311/05 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C313/06 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/57 , C07C323/67 , C07C327/38 , C07D209/08 , C07D211/78 , C07D213/30 , C07D213/53 , C07D213/56 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/54 , C07D239/02 , C07D239/26 , C07D277/24 , C07D277/30 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/06 , C07K5/078 , C07C311/19
CPC分类号: C07C311/05 , A61K38/00 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要: α- and β-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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公开(公告)号:US5968942A
公开(公告)日:1999-10-19
申请号:US294468
申请日:1994-08-23
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Deborah E. Bertenshaw , Robert M. Heintz
IPC分类号: A61K31/18 , A61K31/34 , A61K31/38 , A61K31/44 , A61K31/495 , A61K31/535 , A61K38/00 , C07C303/00 , C07C311/05 , C07C311/18 , C07C311/29 , C07C311/41 , C07C311/47 , C07C317/10 , C07C317/14 , C07C317/44 , C07C323/67 , C07D207/46 , C07D209/08 , C07D211/70 , C07D211/72 , C07D213/24 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/54 , C07D239/26 , C07D265/30 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D307/93 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/36 , C07D405/12 , C07D417/12 , C07K5/06 , C07K5/078 , A61K31/36 , C07D317/50
CPC分类号: C07C311/05 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07D209/08 , C07D213/30 , C07D213/42 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/64 , C07D239/26 , C07D241/18 , C07D241/44 , C07D263/34 , C07D277/24 , C07D277/62 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D307/85 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/48 , C07D405/12 , C07D417/12 , C07D493/04 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/18 , C07C2102/10
摘要: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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公开(公告)号:US5482947A
公开(公告)日:1996-01-09
申请号:US152934
申请日:1993-11-15
申请人: John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Ko-Chung Lin , Michael L. Vazquez , Richard A. Mueller , Kathryn L. Reed , Robert M. Heintz , Michael Clare , John N. Freskos , Eric T. Sun
发明人: John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Ko-Chung Lin , Michael L. Vazquez , Richard A. Mueller , Kathryn L. Reed , Robert M. Heintz , Michael Clare , John N. Freskos , Eric T. Sun
IPC分类号: A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C269/06 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/02 , C07K5/06 , C07K5/078
CPC分类号: C07K5/06191 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C04B35/632 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/06 , C07C271/20 , C07C271/22 , C07C275/14 , C07C275/18 , C07C275/22 , C07C275/24 , C07C275/28 , C07C311/47 , C07C317/44 , C07C317/50 , C07C323/60 , C07C329/06 , C07C335/08 , C07C335/12 , C07D213/81 , C07D215/48 , C07D215/50 , C07D215/54 , C07D217/26 , C07D235/06 , C07D235/24 , C07D239/38 , C07D241/44 , C07D295/13 , C07D295/15 , C07D303/36 , C07D307/85 , C07D401/12 , C07K5/0207 , C07K5/021 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07B2200/07 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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