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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：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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13.发明授权
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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15.发明授权&agr;-and &bgr;-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效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：US06417387B1
公开(公告)日：2002-07-09
申请号：US09798255
申请日：2001-03-05
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： C07C30300
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.
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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16.再颁专利α- and β- amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 有权α-和β-二羧酸 - 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：USRE42889E1
公开(公告)日：2011-11-01
申请号：US11788947
申请日：2007-04-23
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 , C07D213/42 , 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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17.发明授权公开(公告)号：US07115618B2
公开(公告)日：2006-10-03
申请号：US10812343
申请日：2004-03-30
申请人： Michael J. 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 J. 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.
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18.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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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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20.再颁专利公开(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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