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公开(公告)号：US06762187B2
公开(公告)日：2004-07-13
申请号：US10245710
申请日：2002-09-18
申请人： John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
发明人： John J. Talley , Daniel P. Getman , Gary A. DeCrescenzo , Kathryn L. Reed , Ko-Chung Lin , John Nicholas Freskos , Michael Clare , Donald Joseph Rogier, Jr. , Robert M. Heintz , Michael L. Vazquez , Richard A. Mueller
IPC分类号： A61K314965
CPC分类号： C07D401/12 , C07D207/16 , C07D211/60 , C07D217/26
摘要： N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： 含有羟基胺化合物的N-杂环部分作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶抑制剂。
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62.发明授权Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效可用作逆转录病毒蛋白酶抑制剂的琥珀酰氨基羟乙基氨基磺酰胺公开(公告)号：US06727282B2
公开(公告)日：2004-04-27
申请号：US10237184
申请日：2002-09-09
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： C07C30702
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.
摘要翻译： 琥珀酰氨基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蛋白酶抑制剂。
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公开(公告)号：US06656954B2
公开(公告)日：2003-12-02
申请号：US09997552
申请日：2001-11-29
申请人： Louis J. Bedell , Joseph J. McDonald , Thomas E. Barta , Daniel P. Becker , Shashidhar N. Rao , John N. Freskos , Brent V. Mischke , Daniel P. Getman , Gary A. DeCrescenzo
发明人： Louis J. Bedell , Joseph J. McDonald , Thomas E. Barta , Daniel P. Becker , Shashidhar N. Rao , John N. Freskos , Brent V. Mischke , Daniel P. Getman , Gary A. DeCrescenzo
IPC分类号： A61K31445
CPC分类号： C07D213/30 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/16 , C07D211/62 , C07D213/82 , C07D295/15
摘要： A sulfonyl divalent 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 divalent 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.
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公开(公告)号：US06638952B1
公开(公告)日：2003-10-28
申请号：US09254530
申请日：1999-12-23
申请人： Hui Li , Daniel P. Becker , Clara I. Villamil , Terri L. Boehm , Daniel P. Getman , Joseph J. McDonald , Gary A. DeCrescenzo
发明人： Hui Li , Daniel P. Becker , Clara I. Villamil , Terri L. Boehm , Daniel P. Getman , Joseph J. McDonald , Gary A. DeCrescenzo
IPC分类号： A61K31445
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-cycloamino hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-cycloamino 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： 公开了芳族磺酰基α-环氨基异羟肟酸化合物，其特别是抑制基质金属蛋白酶活性，其处理方法包括将预期的具有MMP酶抑制有效量的芳族磺酰基α-环氨基异羟肟酸化合物给予具有条件 与病理基质金属蛋白酶活性相关。
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公开(公告)号：US06492367B1
公开(公告)日：2002-12-10
申请号：US10084713
申请日：2002-02-26
申请人： Gary A DeCrescenzo , Joseph G Rico , Terri Boehm , Jeffery N Carroll , Darren J Kassab , Deborah A Mischke , Shashidhar Rao
发明人： Gary A DeCrescenzo , Joseph G Rico , Terri Boehm , Jeffery N Carroll , Darren J Kassab , Deborah A Mischke , Shashidhar Rao
IPC分类号： A61K31496
CPC分类号： C07D211/46 , C07D211/66 , C07D211/96 , C07D295/26 , C07D309/08 , C07D309/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D491/10 , Y02P20/582
摘要： A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato 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： 公开了特别是抑制基质金属蛋白酶活性的氨基磺酸异羟肟酸化合物，其制备方法，可用于那些合成的中间体化合物，以及包括将预期的氨基磺酰氨基异羟肟酸化合物施用于MMP抑制有效的治疗方法 相当于具有与病理基质金属蛋白酶活性相关的病症的宿主。
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66.发明授权Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors 失效杂环羰基氨基酸羟乙基氨基磺酰胺逆转录病毒蛋白酶抑制剂公开(公告)号：US06407134B1
公开(公告)日：2002-06-18
申请号：US09775682
申请日：2001-02-05
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： A61K314025
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06139 , C07K5/06165
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.
摘要翻译： 选择的杂环羰基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。 本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人类免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及 治疗逆转录病毒感染。
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公开(公告)号：US06380258B2
公开(公告)日：2002-04-30
申请号：US09230209
申请日：1999-06-24
申请人： Louis J. Bedell , Joseph J. McDonald , Thomas E. Barta , Daniel P. Becker , Shashidhar N. Rao , John N. Freskos , Brent V. Mischke , Daniel P. Getman , Gary A. DeCrescenzo
发明人： Louis J. Bedell , Joseph J. McDonald , Thomas E. Barta , Daniel P. Becker , Shashidhar N. Rao , John N. Freskos , Brent V. Mischke , Daniel P. Getman , Gary A. DeCrescenzo
IPC分类号： A61K31165
CPC分类号： C07D213/30 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/16 , C07D211/62 , C07D213/82 , C07D295/15
摘要： A sulfonyl divalent 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 divalent 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.
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68.发明授权Succinoylamino hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效可用作逆转录病毒蛋白酶抑制剂的琥珀酰氨基羟乙基氨基磺酰胺公开(公告)号：US06313345B1
公开(公告)日：2001-11-06
申请号：US09419816
申请日：1999-10-18
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： C07C30702
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.
摘要翻译： 琥珀酰氨基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蛋白酶抑制剂。
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69.发明授权公开(公告)号：US06248775B1
公开(公告)日：2001-06-19
申请号：US09288080
申请日：1999-04-08
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： A61K3138
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 , C07D213/81 , 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
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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70.发明授权Alpha- and beta-amino acid hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors 失效可用作逆转录病毒蛋白酶抑制剂的α-氨基酸和β-氨基酸羟基氨基氨基磺酸衍生物
公开(公告)号：US06156768A
公开(公告)日：2000-12-05
申请号：US379545
申请日：1995-02-02
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： A61K31/16 , A61K31/195 , A61K31/40 , A61K38/00 , C07C307/06 , C07D215/48 , C07D295/26 , C07K5/06 , C07K5/078 , C07D401/12 , A61K31/4709
CPC分类号： C07D295/26 , C07C307/06 , C07D215/48 , C07D303/36 , C07D401/12 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07C2101/14
摘要： Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors: ##STR1##
摘要翻译： PCT No.PCT / US93 / 10552 Sec。 371日期：1995年2月2日 102（e）1995年2月2日PCT PCT 1993年10月29日PCT公布。 公开号WO94 / 10134 日期1994年5月11日由下式表示的α-和β-氨基酸羟乙氨基氨基磺酸衍生物可用作逆转录病毒蛋白酶抑制剂：
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