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1.Method for making intermediates useful in the synthesis of retroviral protease inhibitors 失效
标题翻译: 制备可用于合成逆转录病毒蛋白酶抑制剂的中间体的方法公开(公告)号:US5648511A
公开(公告)日:1997-07-15
申请号:US452187
申请日:1995-05-25
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 , C07D253/00
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.
摘要翻译: 对于易于大规模制备基于羟基脲的手性HIV蛋白酶抑制剂的中间体描述了合成。 该方法包括由手性α氨基醛形成非对映选择性环氧化物或羟腈。
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2.
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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4.
公开(公告)号:USRE43802E1
公开(公告)日:2012-11-13
申请号:US13238923
申请日:2011-09-21
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: A61K31/36
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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5.α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
标题翻译: α-和α-氨基酸羟乙基氨基磺酰胺,可用作逆转录病毒蛋白酶抑制剂公开(公告)号:US07829564B2
公开(公告)日:2010-11-09
申请号:US11952520
申请日:2007-12-07
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: A61K31/44 , A61K31/46 , A61K31/535
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.
摘要翻译: α-和β-氨基酸羟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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6.α- and β-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-氨基酸和β-氨基酸羟乙基氨基磺酰胺公开(公告)号:US07531538B2
公开(公告)日:2009-05-12
申请号:US11433797
申请日:2006-05-15
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 , C07C311/00
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 , C07D213/42 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D217/26 , C07D233/64 , C07D239/26 , C07D241/18 , C07D241/44 , C07D261/08 , C07D263/34 , C07D263/56 , C07D277/24 , C07D277/62 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/45 , C07D307/79 , C07D307/85 , C07D317/62 , C07D333/32 , C07D333/34 , C07D333/48 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D493/04 , 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.
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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7.α- and β-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:US07320983B2
公开(公告)日:2008-01-22
申请号:US11526101
申请日:2006-09-25
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: A61K31/36 , C07D317/50
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.
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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8.α- and β-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:US06924286B1
公开(公告)日:2005-08-02
申请号:US10633376
申请日:2003-08-04
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 , C07C303/00 , C07C311/47 , C07D207/46 , C07D211/70 , C07D211/72 , C07D213/24 , C07D265/30 , C07D307/93 , C07D333/32 , C07D333/36
CPC分类号: C07D333/48 , C07D333/32 , C07D493/04
摘要: α- and β-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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9.&agr;- and &bgr;-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:US06500832B1
公开(公告)日:2002-12-31
申请号:US09525161
申请日:2000-03-14
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: A61K31505
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: &agr;- and &bgr;-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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10.
公开(公告)号:US06455581B1
公开(公告)日:2002-09-24
申请号:US08451090
申请日:1995-05-25
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: A61K3127
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: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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