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1.发明公开
公开(公告)号：EP1230219A1
公开(公告)日：2002-08-14
申请号：EP00913317.4
申请日：2000-02-22
申请人： G.D. Searle & Co.
发明人： Barta, Thomas E. , Becker, Daniel P. , Bedell, Louis J. , Boehm, Terri L. , Carroll, Jeffery N. , De Crescenzo, Gary A. , Fobian, Yvette M. , Freskos, John N. , Getman, Daniel P. , McDonald, Joseph J. , Hanson, Gunnar J. , Hockerman, Susan L. , Howard, Susan C. , Kolodziej, Steve A. , Li, Hui , Mischke, Deborah A. , Rico, Joseph G. , Stehle, Nathan W. , Tollerson, Michael B. , Vernier, William F. , Villamil, Clara I. , Rao, Shashidahar N.
IPC分类号： C07D211/66
CPC分类号： C07D451/02 , A61K31/445 , C07D207/16 , C07D211/66 , C07D211/78 , C07D221/22 , C07D221/24 , C07D225/02 , C07D239/04 , C07D239/10 , C07D239/14 , C07D239/22 , C07D263/06 , C07D265/30 , C07D277/06 , C07D279/06 , C07D281/06 , C07D285/16 , C07D307/24 , C07D309/08 , C07D319/06 , C07D327/02 , C07D333/38 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , Y02A50/411
摘要： A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
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2.发明公开Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors 失效磺酰基烷酰基氨基 - 羟乙基氨基 - 磺酰胺als Inhibitoren der retroviralen Protease
公开(公告)号：EP1052250A1
公开(公告)日：2000-11-15
申请号：EP00114155.5
申请日：1996-03-07
申请人： G.D. SEARLE & CO.
发明人： Getman, Daniel P. , Decrescenzo, Gary A. , Freskos, John N. , Vazquez, Michael L. , Sikorski, James A. , Devadas, Balkudru , Nagarajan, Srinivasan , McDonald, Joseph J.
IPC分类号： C07C311/00 , C07D317/62 , C07D319/18 , C07D277/64 , C07D307/82 , C07D235/32 , C07D277/82 , A61K31/34 , A61K31/36 , A61K31/415 , A61K31/425
CPC分类号： C07D235/06 , C07C311/29 , C07C311/41 , C07C317/44 , C07D215/36 , C07D217/04 , C07D235/30 , C07D235/32 , C07D249/18 , C07D249/20 , C07D263/56 , C07D277/62 , C07D277/82 , C07D303/36 , C07D307/79 , C07D317/62 , C07D319/18
摘要： Selected sulfonylalkanoylamino hydroxyethylamine 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： 选择的磺酰基烷酰基氨基羟基胺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（例如人免疫缺陷病毒（HIV）蛋白酶），预防性地预防逆转录病毒感染或逆转录病毒扩散的组合物和方法，以及 治疗逆转录病毒感染。
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3.发明公开Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors 失效Verbindungen der Struktur bis-Aminosäure-Hydroxyethylamino-Sulfonamid als Inhibitoren der retroviralen Protease
公开(公告)号：EP1188766A1
公开(公告)日：2002-03-20
申请号：EP01129219.0
申请日：1996-03-07
申请人： G.D. Searle & Co.
发明人： Getman, Daniel P. , Decrescenzo, Gary A. , Freskos, John N. , Vasquez, Michael L. , Sikorski, James A. , Devadas, Balekudru , Nagarajan, Srinivasan , Brown, David L. , McDonald, Joseph J.
CPC分类号： C07K5/06026 , A61K38/00 , A61K39/00 , C07K14/20 , C07K16/1207
摘要： Selected bis-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： 选择的双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（例如人免疫缺陷病毒（HIV）蛋白酶），预防性地预防逆转录病毒感染或逆转录病毒扩散的组合物和方法，以及 治疗逆转录病毒感染。
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4.发明授权Method for making intermediates useful in synthesis of retroviral protease inhibitors 失效一种中间体的制备过程中，逆转录病毒蛋白酶化合物的制备的抑制是有用的
公开(公告)号：EP0855388B1
公开(公告)日：2002-03-06
申请号：EP98103779.9
申请日：1994-10-31
申请人： G.D. SEARLE & CO.
发明人： Ng, John S. , Przybyla, Claire A. , Mueller, Richard A. , Vazquez, Michael L. , Getman, Daniel P. , Freskos, John J. , Decrescenzo, Gary A. , Bertenshaw, Deborah E. , Heintz, Robert M. , Zhang, Suhong , Liu, Chin , Laneman, Scott A.
IPC分类号： C07C275/24 , C07C273/18 , C07C213/02 , C07C261/04 , C07C269/04
CPC分类号： C07C273/1854 , C07B2200/07 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C221/00 , C07C223/02 , C07C253/30 , C07C255/26 , C07C269/04 , C07C271/16 , C07C271/18 , C07C271/20 , C07C273/1827 , C07C275/24 , C07C309/73 , C07D303/36 , C07F7/1852 , C07C215/08
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5.发明公开Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors 失效用作逆转录病毒蛋白酶抑制剂的磺酰基烷酰基氨基羟乙基氨基磺酸
公开(公告)号：EP0885880A3
公开(公告)日：1999-10-06
申请号：EP98114523.8
申请日：1993-10-29
发明人： Vazquez, Michael L. , Mueller, Richard A. , Talley, John J. , Getman, Daniel P. , Decrescenzo, Gary A. , Sun, Eric T.
IPC分类号： C07C311/44 , A61K31/16
CPC分类号： C07C317/46 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/42 , C07D213/76 , C07D295/13 , C07D295/26 , C07D307/66 , C07D333/36
摘要： Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： 磺酰基烷酰基氨基羟乙基氨基磺酸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.发明公开Sulfonylalkanoylamino hydroxyethylamino sulfamic acids useful as retroviral protease inhibitors 失效Sulfonylalkanoylaminohydroxyethylaminosulfamidsäuren如逆转录病毒蛋白酶抑制剂的
公开(公告)号：EP0885880A2
公开(公告)日：1998-12-23
申请号：EP98114523.8
申请日：1993-10-29
发明人： Vazquez, Michael L. , Mueller, Richard A. , Talley, John J. , Getman, Daniel P. , Decrescenzo, Gary A. , Sun, Eric T.
IPC分类号： C07C311/44 , A61K31/16
CPC分类号： C07C317/46 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/42 , C07D213/76 , C07D295/13 , C07D295/26 , C07D307/66 , C07D333/36
摘要： Sulfonylalkanoylamino hydroxyethylamino sulfamic acid compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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7.发明授权N-substituted Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors 失效N-取代物羟乙基氨基磺酰胺衍生物verwendbar als抑制剂逆转录病毒蛋白酶
公开(公告)号：EP0810208B1
公开(公告)日：2002-01-02
申请号：EP97113206.3
申请日：1993-10-29
发明人： Vasquez, Michael L. , Mueller, Richard A. , Talley, John J. , Getman, Daniel P. , De Crescenzo, Gary A. , Sun, Eric T.
IPC分类号： C07C307/06 , C07C307/08 , C07C307/10 , C07D295/22 , A61K31/18 , A61K31/325 , A61K31/45
CPC分类号： C07D295/26 , A61K38/00 , C07C307/06 , C07C2601/14 , C07D215/48 , C07D303/36 , C07D401/12 , C07K5/06026 , C07K5/06139
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8.发明公开
公开(公告)号：EP1076062A1
公开(公告)日：2001-02-14
申请号：EP00114911.1
申请日：1996-03-07
申请人： G.D. SEARLE & CO.
发明人： Getman, Daniel P. , Descrescenzo, Gary A. , Freskos, John N. , Vasquez, Michael L. , Sikorski, James A. , Devadas, Balekudru , Nagarajan, Srinivasan , Brown, David L. , McDonald, Joseph J.
CPC分类号： C07K5/06026 , A61K38/00
摘要： Selected bis-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： 选择的双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（例如人免疫缺陷病毒（HIV）蛋白酶），预防性地预防逆转录病毒感染或逆转录病毒扩散的组合物和方法，以及 治疗逆转录病毒感染。
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9.发明公开Method for making intermediates useful in synthesis of retroviral protease inhibitors 失效一种中间体的制备过程中，抑制用于逆转录病毒蛋白酶的化合物可用SINT的制备
公开(公告)号：EP0855388A3
公开(公告)日：1999-07-14
申请号：EP98103779.9
申请日：1994-10-31
申请人： G.D. SEARLE & CO.
发明人： Ng, John S. , Przybyla, Claire A. , Mueller, Richard A. , Vazquez, Michael L. , Getman, Daniel P. , Freskos, John J. , Decrescenzo, Gary A. , Bertenshaw, Deborah E. , Heintz, Robert M. , Zhang, Suhong , Liu, Chin , Laneman, Scott A.
IPC分类号： C07C275/24 , C07C273/18 , C07C213/02 , C07C261/04 , C07C269/04
CPC分类号： C07C273/1854 , C07B2200/07 , C07C213/00 , C07C213/02 , C07C213/08 , C07C215/28 , C07C221/00 , C07C223/02 , C07C253/30 , C07C255/26 , C07C269/04 , C07C271/16 , C07C271/18 , C07C271/20 , C07C273/1827 , C07C275/24 , C07C309/73 , C07D303/36 , C07F7/1852 , C07C215/08
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 cyanohydrin from a chiral alpha amino aldehyde.
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10.发明公开N-substituted Hydroxyethylamino sulfamic acid derivatives useful as retroviral protease inhibitors 失效Hydroxyethylaminosulfamidsäure衍生物可用作逆转录病毒蛋白酶的抑制剂
公开(公告)号：EP0810208A2
公开(公告)日：1997-12-03
申请号：EP97113206.3
申请日：1993-10-29
发明人： Vazquez, Michael L. , Mueller, Richard A. , Talley, John J. , Getman, Daniel P. , De Crescenzo, Gary A. , Sun, Eric T.
IPC分类号： C07C307/06 , C07C307/08 , C07C307/10 , C07D295/22 , A61K31/185
CPC分类号： C07D295/26 , A61K38/00 , C07C307/06 , C07C2601/14 , C07D215/48 , C07D303/36 , C07D401/12 , C07K5/06026 , C07K5/06139
摘要： The present invention (divisional of PCT/US93/10552 = EP 94 900 506.0) is related to N-substituted hydroxyethylamino sulfamic acid derivatives of the formula
which are useful as retorviral protease inhibitors and in the preparation of compounds of the above parent application.
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