专利检索 ap:"Deborah Mischke" 第 1 页

1.

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。

2.

发明申请
(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效
标题翻译：（R） - 用于抑制胆固醇酯转移蛋白活性的卤代取代稠合杂环氨基化合物

公开(公告)号：US20050043294A1

公开(公告)日：2005-02-24

申请号：US10929013

申请日：2004-08-27

申请人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel

发明人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel

IPC分类号： C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07D213/65 , C07D251/42 , C07D307/42 , C07D333/20 , A61K31/55 , A61K31/137 , A61K31/47

CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20

摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.

摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代的芳基和杂芳基（R） - 手性卤代1-取代氨基 - （n + 1） - 阿尔卡醇化合物，化合物，组合物和方法用于治疗动脉粥样硬化和其他冠状动脉疾病。描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。

3.

发明申请
(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效

公开(公告)号：US20060229304A1

公开(公告)日：2006-10-12

申请号：US11373770

申请日：2006-03-09

申请人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel

发明人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel

IPC分类号： A61K31/538 , C07D265/36 , A61K31/138

CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20

摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.

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.

发明授权
Esters of N,N'-methylene-bis-[N-[(diaryloxyphosphinyl)methyl]glycine] as herbicides 失效
标题翻译： N，N'-亚甲基 - 双 - [N - [（二芳氧基氧膦基）甲基]甘氨酸]酯作为除草剂

公开(公告)号：US4601744A

公开(公告)日：1986-07-22

申请号：US698484

申请日：1985-02-05

申请人： James A. Sikorski , Deborah Mischke , Gerard A. Dutra

发明人： James A. Sikorski , Deborah Mischke , Gerard A. Dutra

IPC分类号： A01N57/22 , C07F9/40 , A01N57/06

CPC分类号： A01N57/22 , C07F9/4006

摘要： This invention relates to novel esters of N,N'-methylene-bis-[N-[(diaryloxyphosphinyl)methyl]glycine] which are useful as herbicides. The invention also relates to herbicidal methods and compositions employing the novel esters.

摘要翻译： 本发明涉及可用作除草剂的N，N'-亚甲基 - 双 - [N - [（二芳氧基氧膦基）甲基]甘氨酸]的新酯。本发明还涉及使用新型酯的除草方法和组合物。

6.

发明申请
(R)-Chiral Halogenated Substituted Fused Heterocyclic Amino Compounds Useful for Inhibiting Cholesterol Ester Transfer Protein Activity 审中-公开
标题翻译：（R） - 用于抑制胆固醇酯转移蛋白活性的手性卤代取代的稠合杂环氨基化合物

公开(公告)号：US20070219274A1

公开(公告)日：2007-09-20

申请号：US11693161

申请日：2007-03-29

申请人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michelle Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel

发明人： James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michelle Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel

IPC分类号： A61K31/135 , C07C211/43

CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20

摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.

摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代的芳基和杂芳基（R） - 手性卤代1-取代氨基 - （n + 1） - 阿尔卡醇化合物，化合物，组合物和方法用于治疗动脉粥样硬化和其他冠状动脉疾病。描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。

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。

8.

发明申请
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。