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公开(公告)号:US20050101641A1
公开(公告)日:2005-05-12
申请号:US10992483
申请日:2004-11-17
申请人: John Freskos , Yvette Fobian , Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Susan Hockerman , Darren Kassab , Steve Kolodziej , Joseph McDonald , Deborah Mischke , Monica Norton , Joseph Rico , John Talley , Clara Villamil , Lijuan Wang
发明人: John Freskos , Yvette Fobian , Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Susan Hockerman , Darren Kassab , Steve Kolodziej , Joseph McDonald , Deborah Mischke , Monica Norton , Joseph Rico , John Talley , Clara Villamil , Lijuan Wang
IPC分类号: C07D491/048 , A61K31/35 , A61K31/351 , A61K31/357 , A61K31/381 , A61K31/397 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/4178 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/4355 , A61K31/4433 , A61K31/445 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/455 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/53 , A61K31/5377 , A61P1/02 , A61P1/04 , A61P1/16 , A61P7/00 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/18 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P39/00 , A61P43/00 , C07D211/66 , C07D309/08 , C07D309/12 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , A61K31/401
CPC分类号: C07D401/12 , A61K31/351 , A61K31/41 , A61K31/453 , A61K31/454 , C04B35/632 , C07D211/66 , C07D309/08 , C07D309/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , Y02A50/411
摘要: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
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2.Piperidinyl-and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors 失效
标题翻译: 哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸及其作为蛋白酶抑制剂的用途公开(公告)号:US20050009838A1
公开(公告)日:2005-01-13
申请号:US10618288
申请日:2003-04-25
申请人: Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , David Brown , Jeffery Carroll , Yiyuan Chen , Yvette Fobian , John Freskos , Alan Gasiecki , Margaret Grapperhaus , Robert Heintz , Susan Hockerman , Darren Kassab , Ish Khanna , Stephen Kolodziej , Mark Massa , Joseph McDonald , Brent Mischke , Deborah Mischke , Patrick Mullins , Mark Nagy , Monica Norton , Joseph Rico , Michelle Schmidt , Nathan Stehle , John Talley , William Vernier , Clara Villamil , Lijuan Wang , Thomas Wynn
发明人: Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , David Brown , Jeffery Carroll , Yiyuan Chen , Yvette Fobian , John Freskos , Alan Gasiecki , Margaret Grapperhaus , Robert Heintz , Susan Hockerman , Darren Kassab , Ish Khanna , Stephen Kolodziej , Mark Massa , Joseph McDonald , Brent Mischke , Deborah Mischke , Patrick Mullins , Mark Nagy , Monica Norton , Joseph Rico , Michelle Schmidt , Nathan Stehle , John Talley , William Vernier , Clara Villamil , Lijuan Wang , Thomas Wynn
IPC分类号: C07D295/22 , A61K31/451 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P1/02 , A61P1/04 , A61P1/14 , A61P1/16 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/08 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P31/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P37/02 , A61P39/00 , A61P41/00 , A61P43/00 , C07D211/66 , C07D211/96 , C07D213/74 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/445 , C07D211/26
CPC分类号: C07D213/74 , C07D211/66 , C07D211/96 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
摘要翻译: 本发明一般涉及蛋白酶(也称为“蛋白酶”)抑制剂,尤其涉及哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸,其特别是抑制基质金属蛋白酶(也称为“基质金属蛋白酶”或“MMP “)活性和/或蛋白聚糖蛋白聚糖酶活性。 这种异羟肟酸通常在结构上对应于下式:(其中A 1,A 2,Y,E 1,E 2,E 3和R x如 本说明书),并且还包括这些化合物的盐。 本发明还涉及这种异羟肟酸的组合物,用于合成这种异羟肟酸的中间体,制备这种异羟肟酸的方法,以及用于治疗与MMP活性和/或蛋白聚糖蛋白聚糖酶活性相关的病症(特别是病理状态)的方法。
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3.Hydroxamic acid and amide compounds and their use as protease inhibitors 审中-公开
标题翻译: 羟肟酸和酰胺化合物及其作为蛋白酶抑制剂的用途公开(公告)号:US20060074243A1
公开(公告)日:2006-04-06
申请号:US11270391
申请日:2005-11-10
申请人: Daniel Becker , Yiyuan Chen , John Freskos , Alan Gasiecki , Margaret Grapperhaus , Donald Hansen , Robert Heintz , Darren Kassab , Ish Khanna , Stephen Kolodziej , Sergio Mantegani , Mark Massa , Joseph McDonald , Deborah Mischke , Mark Nagy , Ettore Perrone , Joseph Rico , Michelle Schmidt , Dale Spangler , John Talley , Mahima Trivedi , Thomas Wynn
发明人: Daniel Becker , Yiyuan Chen , John Freskos , Alan Gasiecki , Margaret Grapperhaus , Donald Hansen , Robert Heintz , Darren Kassab , Ish Khanna , Stephen Kolodziej , Sergio Mantegani , Mark Massa , Joseph McDonald , Deborah Mischke , Mark Nagy , Ettore Perrone , Joseph Rico , Michelle Schmidt , Dale Spangler , John Talley , Mahima Trivedi , Thomas Wynn
IPC分类号: C07D211/68
CPC分类号: C07D241/12 , C07C317/46 , C07D211/66 , C07D213/34 , C07D309/08 , C07D335/02 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. These compounds generally correspond in structure to Formula I: wherein A1, A2, A3, E1, E2, E3, and E4 are as defined in this patent. This invention also is directed to compositions of such compounds, intermediates for the syntheses of such compounds, methods for making such compounds, and methods for treating conditions associated with MMP activity and/or aggrecanase activity, particularly pathological conditions.
摘要翻译: 本发明一般涉及异羟肟酸和酰胺化合物(包括这些化合物的盐),更具体地说,涉及芳基 - 和杂芳基 - 芳基磺酰基甲基异羟肟酸和酰胺,其特别是抑制蛋白酶活性,特别是基质金属蛋白酶(也称为 作为“基质金属蛋白酶”或“MMP”)活性和/或蛋白聚糖蛋白聚糖酶活性。 这些化合物通常在结构上对应于式I:其中A 1,A 2,A 3,E 1, E 2,E 3和E 4如本专利中所定义。 本发明还涉及这些化合物的组合物,用于合成这些化合物的中间体,制备这些化合物的方法,以及用于治疗与MMP活性和/或蛋白聚糖蛋白聚糖酶活性特别是病理状况相关的病症的方法。
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公开(公告)号:US20050004230A1
公开(公告)日:2005-01-06
申请号:US10793672
申请日:2004-03-05
申请人: John Talley , Daniel Getman , Gary DeCrescenzo , Kathryn Reed , Ko-Chung Lin , John Freskos , Michael Clare , Donald Rogier , Robert Heintz , Michael Vazquez , Richard Mueller
发明人: John Talley , Daniel Getman , Gary DeCrescenzo , Kathryn Reed , Ko-Chung Lin , John Freskos , Michael Clare , Donald Rogier , Robert Heintz , Michael Vazquez , Richard Mueller
IPC分类号: A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/472 , A61K38/55 , A61P31/12 , C07D207/16 , C07D211/60 , C07D217/26 , C07D241/04 , C07D401/12 , C07K5/06 , C07K14/81 , A61K31/165 , A61K31/16 , C07C233/02
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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5.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-氨基酸和β-氨基酸羟乙基氨基磺酰胺公开(公告)号:US20070078173A1
公开(公告)日:2007-04-05
申请号:US11526101
申请日:2006-09-25
申请人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos , Robert Heintz , Deborah Bertenshaw
发明人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos , Robert Heintz , Deborah Bertenshaw
IPC分类号: A61K31/44 , A61K31/18 , C07D213/24 , C07C311/45
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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公开(公告)号:US20060166895A1
公开(公告)日:2006-07-27
申请号:US11331344
申请日:2006-01-13
申请人: John Talley , Daniel Getman , Gary DeCrescenzo , Kathryn Reed , Ko-Chung Lin , John Freskos , Michael Clare , Donald Rogier , Robert Heintz , Michael Vazquez , Richard Mueller
发明人: John Talley , Daniel Getman , Gary DeCrescenzo , Kathryn Reed , Ko-Chung Lin , John Freskos , Michael Clare , Donald Rogier , Robert Heintz , Michael Vazquez , Richard Mueller
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.
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7.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:US20060276493A1
公开(公告)日:2006-12-07
申请号:US11433797
申请日:2006-05-15
申请人: Michael Vasquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos , Deborah Bertenshaw , Robert Heintz
发明人: Michael Vasquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos , Deborah Bertenshaw , Robert Heintz
IPC分类号: A61K31/513 , A61K31/4412 , A61K31/4706 , A61K31/426 , A61K31/421 , A61K31/381 , A61K31/34 , A61K31/18
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,特别是HIV蛋白酶的抑制剂是有效的。
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8.Succinoylamino 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琥珀酰氨基羟乙基氨基磺酰胺公开(公告)号:US20050004043A1
公开(公告)日:2005-01-06
申请号:US10784916
申请日:2004-02-24
申请人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos
发明人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John 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.
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蛋白酶的抑制剂。
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9.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-氨基酸和β-氨基酸羟乙基氨基磺酰胺公开(公告)号:US20050267171A1
公开(公告)日:2005-12-01
申请号:US11110943
申请日:2005-04-21
申请人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos , Deborah Bertenshaw , Robert Heintz
发明人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , John Freskos , Deborah Bertenshaw , Robert Heintz
IPC分类号: A61K31/16 , A61K31/18 , A61K31/44 , A61K38/00 , C07C311/05 , C07C311/18 , C07C311/20 , C07C311/29 , C07C311/41 , C07C311/46 , C07C317/10 , C07C317/14 , C07C317/44 , C07C323/67 , C07C327/42 , C07D209/08 , C07D213/24 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/54 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06 , C07K5/078
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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10.Alpha- and beta-amino acid hydroxyethylamino sulfonyl urea derivatives 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脲衍生物公开(公告)号:US20060094789A1
公开(公告)日:2006-05-04
申请号:US11235524
申请日:2005-09-27
申请人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , Eric Sun
发明人: Michael Vazquez , Richard Mueller , John Talley , Daniel Getman , Gary DeCrescenzo , Eric Sun
IPC分类号: A61K31/4172 , A61K31/405 , A61K31/401 , A61K31/18
CPC分类号: C07D213/42 , C07C307/06 , C07D215/48 , C07D215/50 , C07D215/54 , C07D235/06 , C07D239/38 , C07D307/85 , C07K5/06026 , C07K5/06139 , C07K5/06191
摘要: α- and β-amino acid hydroxyethylamino sulfonyl urea derivative 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。
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