专利检索 ap:("Mark E. Schnute" OR "Peter G. Ruminski" OR "Cathleen E. Hanau" OR "Joseph W. Stobach" OR "Jeffery Carroll" OR "Kirby Sample") AND inv:"Jeffery Carroll" 第 1 页

1.

发明申请
HETERO BICYCLIC CARBOXAMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS 审中-公开
标题翻译：异双环酰胺酰胺衍生物及其药物用途和组合物

公开(公告)号：US20110009435A1

公开(公告)日：2011-01-13

申请号：US12663157

申请日：2008-05-19

申请人： Mark E. Schnute , Peter G. Ruminski , Cathleen E. Hanau , Joseph W. Stobach , Jeffery Carroll , Kirby Sample

发明人： Mark E. Schnute , Peter G. Ruminski , Cathleen E. Hanau , Joseph W. Stobach , Jeffery Carroll , Kirby Sample

IPC分类号： A61K31/517 , C07D491/04 , C07D239/72 , A61K31/519 , A61P37/00 , A61P17/06 , A61P19/02 , A61P35/00 , A61P11/00 , A61P11/06 , A61P1/06

CPC分类号： C07D239/90 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D495/04

摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.

摘要翻译： 本发明涉及式I化合物及其药学上可接受的盐，其制备方法，用于制备的中间体和含有这些化合物的组合物以及这些化合物作为抗炎剂的用途。

2.

发明授权
MIF inhibitors and their uses 有权

公开(公告)号：US09050334B2

公开(公告)日：2015-06-09

申请号：US13184058

申请日：2011-07-15

申请人： Anderson Gaweco , John K. Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

发明人： Anderson Gaweco , John K. Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

IPC分类号： C07D215/38 , A61K31/47 , C07D215/54 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14

CPC分类号： A61K31/47 , C07D215/54 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14

摘要： The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.

3.

发明授权
MIF inhibitors and their uses 有权
标题翻译： MIF抑制剂及其用途

公开(公告)号：US09133164B2

公开(公告)日：2015-09-15

申请号：US14237136

申请日：2012-04-13

申请人： Anderson Gaweco , John Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

发明人： Anderson Gaweco , John Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

IPC分类号： C07D215/227 , C07D401/12 , C07D215/56 , C07D295/185 , C07D401/04 , C07D401/14 , C07D409/14 , C07D205/04

CPC分类号： C07D401/12 , C07D205/04 , C07D215/227 , C07D215/56 , C07D295/185 , C07D401/04 , C07D401/14 , C07D409/14

摘要： The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.

摘要翻译： 本发明涉及MIF抑制剂; 包含有效量的MIF抑制剂的组合物; 以及用于治疗或预防与MIF相关的疾病的方法。

4.

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。

5.

发明申请
MIF INHIBITORS AND THEIR USES 有权
标题翻译： MIF抑制剂及其用途

公开(公告)号：US20150065480A1

公开(公告)日：2015-03-05

申请号：US14237136

申请日：2012-04-13

申请人： Anderson Gaweco , John Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

发明人： Anderson Gaweco , John Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

IPC分类号： C07D401/12 , C07D401/14 , C07D401/04 , C07D409/14

CPC分类号： C07D401/12 , C07D205/04 , C07D215/227 , C07D215/56 , C07D295/185 , C07D401/04 , C07D401/14 , C07D409/14

摘要： The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.

摘要翻译： 本发明涉及MIF抑制剂; 包含有效量的MIF抑制剂的组合物; 以及用于治疗或预防与MIF相关的疾病的方法。

6.

发明申请
Sulfamato hydroxamic acid metalloprotease inhibitor 失效
标题翻译：磺酰胺异羟肟酸金属蛋白酶抑制剂

公开(公告)号：US20050049280A1

公开(公告)日：2005-03-03

申请号：US10887450

申请日：2004-07-08

申请人： Terri Boehm , Deborah Mischke , Gary DeCrescenzo , Joseph Rico , Shashidhar Rao , Darren Kassab , Jeffery Carroll

发明人： Terri Boehm , Deborah Mischke , Gary DeCrescenzo , Joseph Rico , Shashidhar Rao , Darren Kassab , Jeffery Carroll

IPC分类号： C07D211/46 , C07D211/66 , C07D309/08 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D491/10 , A61K31/445 , A61K31/18 , A61K31/4015

CPC分类号： C07D401/14 , C07D211/46 , C07D211/66 , C07D309/08 , C07D405/12 , C07D405/14 , C07D409/12 , C07D491/10

摘要： A sulfamato hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato 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： 公开了特别是抑制基质金属蛋白酶活性的氨基磺酸异羟肟酸化合物，其制备方法，可用于那些合成的中间体化合物，以及包括将预期的氨基磺酰氨基异羟肟酸化合物施用于MMP抑制有效的治疗方法相当于具有与病理基质金属蛋白酶活性相关的病症的宿主。

7.

发明申请
MIF INHIBITORS AND THEIR USES 有权
标题翻译： MIF抑制剂及其用途

公开(公告)号：US20120035150A1

公开(公告)日：2012-02-09

申请号：US13184058

申请日：2011-07-15

申请人： Anderson Gaweco , John K. Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

发明人： Anderson Gaweco , John K. Walker , Joseph B. Monahan , Jerry W. Cubbage , Jeffery Carroll

IPC分类号： A61K31/4709 , C07D401/14 , A61K31/506 , A61P9/00 , A61P25/00 , A61P9/10 , A61P37/00 , A61P29/00 , A61P11/06 , A61P11/00 , A61P17/06 , A61P19/02 , A61P1/00 , A61P1/04 , A61P25/28 , A61P27/02 , A61P21/04 , A61P31/14 , A61P37/08 , A61P37/06 , A61P19/04 , A61P3/10 , A61P17/00 , A61P3/00 , A61P3/04 , A61P3/08 , A61P35/00 , A61P35/02 , A61P35/04 , A61P27/16 , C07D409/14

CPC分类号： A61K31/47 , C07D215/54 , C07D401/12 , C07D401/14 , C07D409/14 , C07D417/14

摘要： The invention relates to MIF inhibitors; compositions comprising an effective amount of a MIF inhibitor; and methods for treating or preventing diseases associated with MIF.

摘要翻译： 本发明涉及MIF抑制剂; 包含有效量的MIF抑制剂的组合物; 以及用于治疗或预防与MIF相关的疾病的方法。

8.

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。