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公开(公告)号：US08106197B2
公开(公告)日：2012-01-31
申请号：US11598765
申请日：2006-11-14
申请人： Jingrong Jean Cui , Dilip Bhumralkar , Iriny Botrous , Ji Yu Chu , Lee A. Funk , Cathleen Elizabeth Hanau , G. Davis Harris , Lei Jia , Joanne Johnson , Stephen A. Kolodziej , Pei-Pei Kung , Xiaoyuan (Sharon) Li , Jason (Qishen) Lin , Jerry Jialun Meng , Mitchell David Nambu , Christopher G. Nelson , Mason Alan Pairish , Hong Shen , Michelle Tran-Dube , Allison Walter , Fang-Jie Zhang , Jennifer Zhang
发明人： Jingrong Jean Cui , Dilip Bhumralkar , Iriny Botrous , Ji Yu Chu , Lee A. Funk , Cathleen Elizabeth Hanau , G. Davis Harris , Lei Jia , Joanne Johnson , Stephen A. Kolodziej , Pei-Pei Kung , Xiaoyuan (Sharon) Li , Jason (Qishen) Lin , Jerry Jialun Meng , Mitchell David Nambu , Christopher G. Nelson , Mason Alan Pairish , Hong Shen , Michelle Tran-Dube , Allison Walter , Fang-Jie Zhang , Jennifer Zhang
IPC分类号： C07D241/02
CPC分类号： C07D213/73 , A61K45/06 , C07D401/12 , C07D413/12
摘要： Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET.
摘要翻译： 提供式（1）的氨基吡啶和氨基吡嗪化合物，包括这些化合物的组合物及其使用方法。 优选的式1化合物具有作为蛋白激酶抑制剂的活性，包括作为c-MET的抑制剂。
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公开(公告)号：US07230098B2
公开(公告)日：2007-06-12
申请号：US10786610
申请日：2004-02-26
申请人： Jingrong Jean Cui , Dilip Bhumralkar , Iriny Botrous , Ji Yu Chu , Lee A. Funk , Cathleen Elizabeth Hanau , G. Davis Harris , Lei Jia , Joanne Johnson , Stephen A. Kolodziej , Pei-Pei Kung , Xiaoyuan (Sharon) Li , Jason (Qishen) Lin , Jerry Jialun Meng , Mitchell David Nambu , Christopher G. Nelson , Mason Alan Pairish , Hong Shen , Michelle Tran-Dube , Allison Walter , Fang-Jie Zhang , Jennifer Zhang
发明人： Jingrong Jean Cui , Dilip Bhumralkar , Iriny Botrous , Ji Yu Chu , Lee A. Funk , Cathleen Elizabeth Hanau , G. Davis Harris , Lei Jia , Joanne Johnson , Stephen A. Kolodziej , Pei-Pei Kung , Xiaoyuan (Sharon) Li , Jason (Qishen) Lin , Jerry Jialun Meng , Mitchell David Nambu , Christopher G. Nelson , Mason Alan Pairish , Hong Shen , Michelle Tran-Dube , Allison Walter , Fang-Jie Zhang , Jennifer Zhang
IPC分类号： C07D417/00 , C07D413/00 , C07D401/00 , C07D211/68 , C07D211/72
CPC分类号： C07D213/73 , A61K45/06 , C07D401/12 , C07D413/12
摘要： Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET
摘要翻译： 提供式（1）的氨基吡啶和氨基吡嗪化合物，包括这些化合物的组合物及其使用方法。 优选的式1化合物具有作为蛋白激酶抑制剂的活性，包括作为c-MET的抑制剂
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公开(公告)号：US06909001B2
公开(公告)日：2005-06-21
申请号：US10729794
申请日：2003-12-05
申请人： David R. Anderson , Shridhar G. Hegde , Stephen A. Kolodziej , William F. Vernier , Emily J. Reinhard
发明人： David R. Anderson , Shridhar G. Hegde , Stephen A. Kolodziej , William F. Vernier , Emily J. Reinhard
IPC分类号： C07D471/02 , C07D471/04 , C07D491/04 , C07D491/052 , C07D491/14 , C07D491/153 , C07D495/04 , C07D507/00
CPC分类号： C07D491/04 , C07D471/04 , C07D491/14 , C07D495/04
摘要： A method of making aminocyanopyridine compounds which are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2 is described.
摘要翻译： 描述了能够抑制丝裂原活化蛋白激酶活化蛋白激酶-2的氨基吡啶化合物的制备方法。
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4.发明授权Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors 失效哌啶基和哌嗪基 - 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：US07119203B2
公开(公告)日：2006-10-10
申请号：US10618288
申请日：2003-04-25
申请人： Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , David L. Brown , Jeffery N. Carroll , Yiyuan Chen , Yvette M. Fobian , John N. Freskos , Alan F. Gasiecki , Margaret L. Grapperhaus , Robert M. Heintz , Susan L. Hockerman , Darren J. Kassab , Ish K. Khanna , Stephen A. Kolodziej , Mark A. Massa , Joseph J. McDonald , Brent V. Mischke , Deborah A. Mischke , Patrick B. Mullins , Mark A. Nagy , Monica B. Norton , Joseph G. Rico , Michelle A. Schmidt , Nathan W. Stehle , John J. Talley , William F. Vernier , Clara I. Villamil , Lijuan J. Wang , Thomas A. Wynn
发明人： Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , David L. Brown , Jeffery N. Carroll , Yiyuan Chen , Yvette M. Fobian , John N. Freskos , Alan F. Gasiecki , Margaret L. Grapperhaus , Robert M. Heintz , Susan L. Hockerman , Darren J. Kassab , Ish K. Khanna , Stephen A. Kolodziej , Mark A. Massa , Joseph J. McDonald , Brent V. Mischke , Deborah A. Mischke , Patrick B. Mullins , Mark A. Nagy , Monica B. Norton , Joseph G. Rico , Michelle A. Schmidt , Nathan W. Stehle , John J. Talley , William F. Vernier , Clara I. Villamil , Lijuan J. Wang , Thomas A. Wynn
IPC分类号： C07D405/14 , C07D405/12 , A61K31/496
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。 这样的异羟肟酸通常在结构上对应于下式：（其中A 1，A 2，Y，E 1， 2，E 3和R x如本说明书中所定义），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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公开(公告)号：US5474782A
公开(公告)日：1995-12-12
申请号：US246631
申请日：1994-05-20
IPC分类号： A61K31/195 , A61K9/70
CPC分类号： A61K31/195
摘要： A wound-healing composition and method utilizing a compound of the Formula (I) ##STR1## or a pharmaceutically acceptable salt thereof.
摘要翻译： 一种伤口愈合组合物和利用式（I）化合物或其药学上可接受的盐的方法。
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公开(公告)号：US06890937B2
公开(公告)日：2005-05-10
申请号：US10337942
申请日：2003-01-07
申请人： Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , Jeffery N. Carroll , Gary A. DeCrezcenzo , Theresa R. Fletcher , John N. Freskos , Daniel P. Getman , Gunnar J. Hanson , Susan L. Hockerman , Carol P. Howard , Stephen A. Kolodziej , Madeleine H. Li , Joseph J. McDonald , Deborah A. Mischke , Patrick B. Mullins , Joseph G. Rico , Nathan W. Stehle , Clara I. Villamil
发明人： Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , Jeffery N. Carroll , Gary A. DeCrezcenzo , Theresa R. Fletcher , John N. Freskos , Daniel P. Getman , Gunnar J. Hanson , Susan L. Hockerman , Carol P. Howard , Stephen A. Kolodziej , Madeleine H. Li , Joseph J. McDonald , Deborah A. Mischke , Patrick B. Mullins , Joseph G. Rico , Nathan W. Stehle , Clara I. Villamil
IPC分类号： A61K31/16 , A61K31/167 , A61K31/27 , A61K31/35 , A61K31/351 , A61K31/357 , A61K31/366 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/39 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/444 , A61K31/445 , A61K31/4465 , A61K31/4525 , A61K31/454 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5375 , A61K31/54 , A61K31/541 , A61P1/02 , A61P1/04 , A61P9/10 , A61P13/00 , A61P19/00 , A61P19/02 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C317/44 , C07C319/06 , C07D211/66 , C07D211/94 , C07D211/96 , C07D239/04 , C07D279/06 , C07D309/08 , C07D309/12 , C07D319/06 , C07D327/02 , C07D333/38 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D521/00 , C07D211/06
CPC分类号： C07D231/12 , A61K31/19 , A61K31/4166 , A61K31/421 , A61K31/426 , C07C317/44 , C07D207/48 , C07D211/54 , C07D211/66 , C07D211/86 , C07D211/94 , C07D211/96 , C07D225/02 , C07D233/56 , C07D239/04 , C07D249/08 , C07D263/06 , C07D265/06 , C07D279/06 , C07D281/08 , C07D309/08 , C07D309/28 , C07D319/06 , C07D325/00 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
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. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
摘要翻译： 公开了一种处理方法，其包括施用有效量的显示出一种或多种基质金属蛋白酶（MMP）酶如MMP-2，MMP-9和MMP-13的优异抑制活性的芳香族砜异羟肟酸，同时显示 至少对具有与病理基质金属蛋白酶活性相关的病症的宿主的MMP-1的抑制显着降低。 施用的酶抑制剂在结构上对应于下式（I）或其药学上可接受的盐，其中R 1和R 2都是氢或R 2， 1和R 2与它们所键合的原子一起形成在环中含有一个，两个或三个杂原子的5-至8-元环，其为氧，硫， 或氮气。 式（I）中的R 3是任选取代的芳基或任选取代的杂芳基。 还公开了具有这些选择活性的金属蛋白酶抑制剂化合物，制备这种化合物的方法和使用抑制剂的药物组合物。
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