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71.
公开(公告)号:US6063795A
公开(公告)日:2000-05-16
申请号:US307711
申请日:1999-05-10
申请人: Daniel P Getman , Gary A DeCrescenzo , John N Freskos , Michael L Vazquez , James A Sikorski , Balekudru Devadas , Srinivasan Nagarajan , David L Brown , Joseph J McDonald
发明人: Daniel P Getman , Gary A DeCrescenzo , John N Freskos , Michael L Vazquez , James A Sikorski , Balekudru Devadas , Srinivasan Nagarajan , David L Brown , Joseph J McDonald
IPC分类号: A61K38/55 , A61K31/18 , A61K38/00 , A61P3/00 , A61P31/12 , A61P31/18 , C07D215/48 , C07K5/062 , C07K5/078 , A61K31/445 , C07D405/12
CPC分类号: C07K5/06165 , C07K5/06139 , A61K38/00
摘要: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
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72..alpha.- and .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
标题翻译: 可用作逆转录病毒蛋白酶抑制剂的α-和β-氨基酸羟乙基氨基磺酰胺公开(公告)号:US06060476A
公开(公告)日:2000-05-09
申请号:US204827
申请日:1994-03-02
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
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 , C07D213/64 , 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 , 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.
摘要翻译: α-和β-氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。
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公开(公告)号:US6022994A
公开(公告)日:2000-02-08
申请号:US41016
申请日:1998-03-12
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号: A61K31/145 , A61K38/04 , C07C307/02 , C07C311/06 , C07C311/19 , C07C327/02 , C07D233/54 , C07D233/64 , C07K5/04
CPC分类号: C07C311/05 , C07C311/18 , C07C311/29
摘要: Succinoylamino 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: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:US5872298A
公开(公告)日:1999-02-16
申请号:US833737
申请日:1997-04-09
申请人: John S Ng , Claire A Przybyla , Richard A Mueller , Michael L Vazquez , Daniel P Getman , John J Freskos , Gary A DeCrescenzo , Deborah E Bertenshaw , Robert M Heintz , Suhong Zhang , Chin Liu , Scott A Laneman
发明人: John S Ng , Claire A Przybyla , Richard A Mueller , Michael L Vazquez , Daniel P Getman , John J Freskos , Gary A DeCrescenzo , Deborah E Bertenshaw , Robert M Heintz , Suhong Zhang , Chin Liu , Scott A Laneman
IPC分类号: A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K38/00 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C269/04 , C07C269/06 , C07C271/16 , C07F7/18 , C07K5/078 , C07C311/27
CPC分类号: C07C269/06 , A61K31/17 , A61K31/195 , A61K31/197 , A61K31/27 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07C213/00 , C07C213/02 , C07C213/08 , C07C269/04 , C07F7/188 , C07K5/06139 , A61K38/00 , C07B2200/07
摘要: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.
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公开(公告)号:US5760076A
公开(公告)日:1998-06-02
申请号:US541747
申请日:1995-10-10
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号: A61K31/18 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/381 , A61K31/4406 , A61K31/4409 , A61K31/215 , A61K31/19
CPC分类号: A61K31/5375 , A61K31/18 , A61K31/195 , A61K31/197 , A61K31/216 , A61K31/381 , A61K31/4406 , A61K31/4409
摘要: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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77.Sulfonylalkanoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors 失效
标题翻译: 用作逆转录病毒蛋白酶抑制剂的磺酰基烷酰基氨基羟基乙基氨基磺酰脲衍生物公开(公告)号:US5756498A
公开(公告)日:1998-05-26
申请号:US589563
申请日:1996-01-11
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Eric T. Sun
IPC分类号: C07C311/44 , C07D213/40 , C07D213/75 , C07D233/64 , C07D307/66 , C07D333/36 , C07D521/00 , C07D211/28 , A61K31/38 , C07D265/30
CPC分类号: C07D213/40 , C07C311/44 , C07D213/75 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/66 , C07D333/36
摘要: Sulfonylalkanoylamino hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. In accordance with the present invention, compounds of Formula (I) are disclosed ##STR1## wherein the substituents are as defined in the specification.
摘要翻译: 磺酰基烷酰基氨基羟基乙基氨基磺酰脲衍生物化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。 根据本发明,公开了式(I)化合物,其中取代基如说明书中所定义。
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公开(公告)号:US5714605A
公开(公告)日:1998-02-03
申请号:US541350
申请日:1995-10-10
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号: A61K31/255 , A61K31/18 , A61K31/195 , A61K31/197 , A61K31/381 , A61K31/4406 , A61K31/4409 , A61P31/12 , A61P31/18 , C07C311/05 , C07C311/18 , C07C311/29 , C07C327/38 , C07D265/30 , C07D211/70 , C07D333/20 , C07D333/30
CPC分类号: A61K31/5375 , A61K31/18 , A61K31/195 , A61K31/197 , A61K31/381 , A61K31/4406 , A61K31/4409 , C07C311/05 , C07C311/18 , C07C311/29
摘要: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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79.Sulfonylalkanoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
标题翻译: 用作逆转录病毒蛋白酶抑制剂的磺酰基烷酰氨基羟乙基氨基磺酰胺公开(公告)号:US5639769A
公开(公告)日:1997-06-17
申请号:US587688
申请日:1996-01-17
申请人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人: Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号: A61K31/225 , A61K31/18 , A61K31/63 , A61P31/12 , C07C311/18 , C07C317/44 , C07C327/38 , C07D307/79 , C07D319/16 , A61K31/38 , A61K31/44
CPC分类号: A61K31/63 , A61K31/18 , C07C317/44
摘要: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译: 含磺酰胺的羟乙胺化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。
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公开(公告)号:US5610190A
公开(公告)日:1997-03-11
申请号:US476009
申请日:1995-06-07
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.
摘要翻译: 含尿素的羟胺化合物作为逆转录病毒蛋白酶抑制剂是有效的,特别是作为HIV蛋白酶的抑制剂。
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