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1. 发明申请

US20060074243A1 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。

2. 发明申请

US20050009838A1 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。

3. 发明申请

US20140292177A1 Lateral Traverse Discharge Spark Plug 审中-公开
标题翻译：横向排气火花塞
公开(公告)号：US20140292177A1
公开(公告)日：2014-10-02
申请号：US13855131
申请日：2013-04-02
申请人： Mark Nagy
发明人： Mark Nagy
IPC分类号： H01T13/20
CPC分类号： H01T13/20 , H01T21/06
摘要： A lateral transverse discharge spark plug (10) which consists of a cylindrical metallic shell (20) having a tubular ceramic insulator (22), including an insulator attachment end (28) enclosed therein. An offset center electrode (30) is surrounded by the ceramic insulator. The offset center electrode has a firing tip (36) extending from the insulator distal end. A ground electrode 38 is attached to a side of the metallic shell, and the ground electrode has a first gap (#1GAP) distanced from the offset center electrode. The offset center electrode and the ground electrode protrude from the cylindrical metallic shell attachment end and the end of said ceramic insulator in a terminally aligned orientation. A second embodiment utilizing a center electrode (31) is also disclosed.
摘要翻译：横向横向放电火花塞（10），其由具有管状陶瓷绝缘体（22）的圆柱形金属壳（20）组成，包括封闭在其中的绝缘体附接端（28）。偏移中心电极（30）被陶瓷绝缘体包围。偏移中心电极具有从绝缘体远端延伸的点火尖端（36）。接地电极38附接到金属壳的一侧，接地电极具有与偏移中心电极相距的第一间隙（＃1GAP）。偏移中心电极和接地电极以圆柱形的金属壳安装端和所述陶瓷绝缘体的端部以终端排列的方向突出。还公开了利用中心电极（31）的第二实施例。

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