专利检索 ap:"Louis Bedell" 第 1 页

1.

发明申请
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。

2.

发明授权
Biaryl substituted heterocycle inhibitors of LTA4H for treating inflammation 失效
标题翻译：用于治疗炎症的LTA4H的二芳基取代的杂环抑制剂

公开(公告)号：US08598359B2

公开(公告)日：2013-12-03

申请号：US12136874

申请日：2008-06-11

申请人： Vincent Sandanayaka , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao , Rama K. Mishra

发明人： Vincent Sandanayaka , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao , Rama K. Mishra

IPC分类号： C07D211/20 , A61K31/445

CPC分类号： C07D403/12 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D207/263 , C07D207/46 , C07D211/22 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12

摘要： The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is

摘要翻译： 本发明涉及可用于治疗和预防和预防炎性疾病和病症的LTA4H（白三烯A4水解酶）的联芳基取代的杂环抑制剂的化学属。化合物具有通式Psi：一个例子

3.

发明申请
Sulfonyl aryl or heteroaryl hydroxamic acid compounds 审中-公开
标题翻译：磺酰基芳基或杂芳基异羟肟酸化合物

公开(公告)号：US20050075374A1

公开(公告)日：2005-04-07

申请号：US10867391

申请日：2004-06-14

申请人： Louis Bedell , Joseph McDonald , Thomas Barta , Daniel Becker , Shashidhar Rao , John Freskos , Brent Mischke , Daniel Getman , Gary DeCrescenzo , Clara Villamil

发明人： Louis Bedell , Joseph McDonald , Thomas Barta , Daniel Becker , Shashidhar Rao , John Freskos , Brent Mischke , Daniel Getman , Gary DeCrescenzo , Clara Villamil

IPC分类号： C07C311/16 , C07C311/21 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/14 , C07D207/16 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/54 , C07D211/62 , C07D213/30 , C07D213/82 , C07D295/15 , C07D295/26 , C07D309/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D211/84 , A61K31/4015 , A61K31/44

CPC分类号： C07D295/26 , C07C311/16 , C07C311/21 , C07C317/22 , C07C317/44 , C07C323/65 , C07D207/14 , C07D207/16 , C07D211/16 , C07D211/18 , C07D211/46 , C07D211/54 , C07D211/62 , C07D213/30 , C07D213/82 , C07D295/15 , C07D309/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12

摘要： A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring 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： 公开了包括抑制基质金属蛋白酶活性的磺酰芳族或杂芳族环异羟肟酸化合物，其处理方法包括将具有MMP酶抑制有效量的考虑的磺酰芳族或杂芳族环异羟肟酸化合物施用于具有条件与病理基质金属蛋白酶活性相关。

4.

发明申请
BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION 失效
标题翻译： LTA4H用于治疗炎症的BIARYL取代的杂合物抑制剂

公开(公告)号：US20090163462A1

公开(公告)日：2009-06-25

申请号：US12136874

申请日：2008-06-11

申请人： Vincent SANDANAYAKA , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao , Rama K. Mishra

发明人： Vincent SANDANAYAKA , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao , Rama K. Mishra

IPC分类号： A61K31/40 , C07D207/04 , C07D207/16 , C07D401/06 , A61K31/44 , A61K31/454 , A61K31/5377 , A61P29/00 , A61K31/397 , A61K31/495 , A61K31/445 , C07D211/06 , C07D241/04 , C07D413/12

CPC分类号： C07D403/12 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D207/263 , C07D207/46 , C07D211/22 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12

摘要： The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is

摘要翻译： 本发明涉及可用于治疗和预防和预防炎性疾病和病症的LTA4H（白三烯A4水解酶）的联芳基取代的杂环抑制剂的化学属。化合物具有通式Psi：一个例子

5.

发明授权
Biaryl substituted heterocycle inhibitors of LTA4H for treating inflammation 失效
标题翻译：用于治疗炎症的LTA4H的二芳基取代的杂环抑制剂

公开(公告)号：US07402684B2

公开(公告)日：2008-07-22

申请号：US11426287

申请日：2006-06-23

申请人： Vincent Sandanayaka , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao , Rama K. Mishra

发明人： Vincent Sandanayaka , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao , Rama K. Mishra

IPC分类号： C07D207/08 , A61K31/40

CPC分类号： C07D403/12 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D207/263 , C07D207/46 , C07D211/22 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12

摘要： The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is

摘要翻译： 本发明涉及可用于治疗和预防和预防炎性疾病和病症的LTA4H（白三烯A4水解酶）的联芳基取代的杂环抑制剂的化学属。化合物具有通式Psi：一个例子

6.

发明申请
BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION 审中-公开

公开(公告)号：US20070078263A1

公开(公告)日：2007-04-05

申请号：US11426284

申请日：2006-06-23

申请人： Vincent Sandanayaka , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao

发明人： Vincent Sandanayaka , Jasbir Singh , Mark Gurney , Bjorn Mamat , Peng Yu , Louis Bedell , Lei Zhao

IPC分类号： C07D417/02 , C07D413/02 , C07D403/02

CPC分类号： C07D403/12 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D207/263 , C07D207/46 , C07D211/22 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12

摘要： The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: An example is

7.

发明申请
Aromatic sulfone hydroxamic acid metalloprotease inhibitor 审中-公开
标题翻译：芳香砜异羟肟酸金属蛋白酶抑制剂

公开(公告)号：US20060084688A1

公开(公告)日：2006-04-20

申请号：US11046645

申请日：2005-01-28

申请人： Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Theresa Fletcher , John Freskos , Daniel Getman , Gunnar Hanson , Susan Hockerman , Carol Howard , Stephen Kolodziej , Madeleine Li , Joseph McDonald , Deborah Mischke , Patrick Mullins , Joseph Rico , Nathan Stehle , Clara Villamil

发明人： Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Theresa Fletcher , John Freskos , Daniel Getman , Gunnar Hanson , Susan Hockerman , Carol Howard , Stephen Kolodziej , Madeleine Li , Joseph McDonald , Deborah Mischke , Patrick Mullins , Joseph Rico , Nathan Stehle , Clara Villamil

IPC分类号： A61K31/426 , A61K31/421 , A61K31/4166 , A61K31/19

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。