公开(公告)号：US20030207344A1

公开(公告)日：2003-11-06

申请号：US10338486

申请日：2003-01-07

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

发明人： Bruce D. Hammock ,  Guomin Shan ,  Rong Zhang

IPC分类号： C12Q001/34 ,  C07D219/08 ,  C07D215/12 ,  C07D311/78 ,  C07D311/02 ,  C07D209/14 ,  C07C255/36

CPC分类号： C07D295/155 ,  C07C255/37 ,  C07C255/38 ,  C07C255/39 ,  C07C271/24 ,  C07C2601/14 ,  C07D303/40 ,  C07K5/0812

摘要： Ethers and esters of cyanohydrins that contain optically detectable moieties are highly effective for detecting, monitoring, and measuring the activity of enzymes that cause the cleavage of certain types of substrates. The cyanohydrins function as proaldehydes and proketones, spontaneously converting to aldehydes and ketones, respectively, which provide a large increase in optical detectability relative to both the starting esters and ethers and the cyanohydrins.

摘要翻译： 含有光学可检测部分的氰醇的醚和酯对于检测，监测和测量导致某些类型底物裂解的酶的活性是非常有效的。 氰醇作为醛和原酮，分别自发转化成醛和酮，这相对于起始酯和醚和氰醇都提供了大的光学可检测性的增加。

公开(公告)号：US20030119900A1

公开(公告)日：2003-06-26

申请号：US10328495

申请日：2002-12-23

申请人： The Regents of the University of California

发明人： Deanna L. Kroetz ,  Darryl C. Zeldin ,  Bruce D. Hammock ,  Christophe Morisseau

IPC分类号： A61K031/335 ,  A61K031/17 ,  A61K031/66

CPC分类号： A61K31/325 ,  A61K31/00 ,  A61K31/336

摘要： The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 1 wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.

摘要翻译： 本发明提供在治疗高血压的治疗应用中抑制环氧化物水解酶的化合物。 用于实施本发明的一类优选的化合物具有式1所示的结构，其中Z是氧或硫，W是碳磷或硫，X和Y各自独立地是氮，氧或硫，并且X还可以是碳， 当X为氮时，R 1为R 4为氢，R 2为氢时，当X为硫或氧时不存在，当Y为氮时为R4，当Y为硫或氧时不存在，R 1和R 3为 各自独立地为C1-C20取代或未取代的烷基，环烷基，芳基，酰基或杂环。

公开(公告)号：US20040092487A1

公开(公告)日：2004-05-13

申请号：US10694641

申请日：2003-10-27

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  THE GOVERNMENT OF THE U.S., as represented by the Sec. of the Dept. of Health and Human Services

发明人： Deanna L. Kroetz ,  Darryl C. Zeldin ,  Bruce D. Hammock ,  Christophe Morisseau

IPC分类号： A61K048/00 ,  A61K031/66 ,  A61K031/335 ,  A61K031/325 ,  A61K031/17

CPC分类号： A61K31/325 ,  A61K31/00 ,  A61K31/336

摘要： The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 1 wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.

摘要翻译： 本发明提供在治疗高血压的治疗应用中抑制环氧化物水解酶的化合物。 用于实施本发明的一类优选的化合物具有式1所示的结构，其中Z是氧或硫，W是碳磷或硫，X和Y各自独立地是氮，氧或硫，并且X还可以是碳， 当X为氮时，R 1为R 4为氢，R 2为氢时，当X为硫或氧时不存在，当Y为氮时为R4，当Y为硫或氧时不存在，R 1和R 3为 各自独立地为C1-C20取代或未取代的烷基，环烷基，芳基，酰基或杂环。

公开(公告)号：US20030139469A1

公开(公告)日：2003-07-24

申请号：US10056284

申请日：2002-01-23

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

发明人： Robert H. Weiss ,  Bruce D. Hammock

IPC分类号： A61K031/335 ,  A61K031/17 ,  A61K031/13 ,  A61K031/045

CPC分类号： A61K31/335 ,  A61K31/00 ,  A61K31/045 ,  A61K31/13 ,  A61K31/17

摘要： The present invention provides methods of slowing or inhibiting vascular smooth muscle (VSM) cell proliferation to slow the development or recurrence of atherosclerosis by contacting VSM cells with soluble epoxide hydrolase (sEH) inhibitors. Further, the methods of the invention can be used to slow or to inhibit vascular restenosis after angioplasty and the stenosis of vascular stents. Further, the methods of the invention can be used to slow or to inhibit the stenosis of hemodialysis grafts and other natural and synthetic vascular grafts.

摘要翻译： 本发明提供了通过使VSM细胞与可溶性环氧化物水解酶（sEH）抑制剂接触来减缓或抑制血管平滑肌（VSM）细胞增殖以减缓动脉粥样硬化的发展或复发的方法。 此外，本发明的方法可用于减缓或抑制血管成形术和血管支架狭窄后的血管再狭窄。 此外，本发明的方法可用于减缓或抑制血液透析移植物和其它天然和合成血管移植物的狭窄。