公开(公告)号：US6150415A

公开(公告)日：2000-11-21

申请号：US252148

申请日：1999-02-18

申请人： Bruce D. Hammock ,  Christophe H. Morisseau ,  Jiang Zheng ,  Marvin H. Goodrow ,  Tonya Severson ,  James Sanborn

发明人： Bruce D. Hammock ,  Christophe H. Morisseau ,  Jiang Zheng ,  Marvin H. Goodrow ,  Tonya Severson ,  James Sanborn

IPC分类号： C12N9/14 ,  A01N47/10 ,  A01N47/28 ,  A61K31/00 ,  A61K31/155 ,  A61K31/17 ,  A61K31/20 ,  A61K31/336 ,  A61K38/46 ,  A61P11/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C275/06 ,  C07C275/26 ,  C07C333/06 ,  C12N9/99

CPC分类号： A61K31/155 ,  A61K31/00 ,  A61K31/17 ,  A61K31/20 ,  A61K31/27 ,  A61K31/336 ,  A61K31/7088 ,  G01N2500/10

摘要： Biologically stable inhibitors of soluble epoxide hydrolases are provided. The inhibitors can be used, for example, to selectively inhibit epoxide hydrolase in therapeutic applications such as treating inflammation, for use in affinity separations of the epoxide hydrolases, and in agricultural applications. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 ##STR1## wherein X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R.sub.1 -R.sub.4 is hydrogen, R.sub.2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R.sub.4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R.sub.1 and R.sub.3 are each independently a substituted or unsubstituted alkyl, haloalkyl, cycloalkyl, aryl, acyl, or heterocyclic, or being a metabolite or degradation product thereof.

摘要翻译： 提供了生物稳定的可溶性环氧化物水解酶抑制剂。 抑制剂可用于例如在治疗应用中选择性抑制环氧化物水解酶，例如治疗炎症，用于环氧化物水解酶的亲和分离，以及在农业应用中。 用于实施本发明的优选类化合物具有式1所示的结构，其中X和Y各自独立地为氮，氧或硫，X可以进一步为碳，R 1 -R 4中的至少一个为氢，R 2为氢 当X是氮而X是硫或氧时不存在，当Y是氮时，R4是氢，当Y是硫或氧时不存在，R 1和R 3各自独立地是取代或未取代的烷基，卤代烷基，环烷基，芳基 ，酰基或杂环，或其代谢产物或降解产物。

公开(公告)号：US20060035869A1

公开(公告)日：2006-02-16

申请号：US11240444

申请日：2005-09-29

申请人： Bruce Hammock ,  Christophe Morisseau ,  Jiang Zheng ,  Marvin Goodrow ,  Tonya Severson ,  James Sanborn

发明人： Bruce Hammock ,  Christophe Morisseau ,  Jiang Zheng ,  Marvin Goodrow ,  Tonya Severson ,  James Sanborn

IPC分类号： A61K31/17 ,  A61K31/66

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

摘要： Biologically stable inhibitors of soluble epoxide hydrolases are provided. The inhibitors can be used, for example, to selectively inhibit epoxide hydrolase in therapeutic applications such as treating inflammation, for use in affinity separations of the epoxide hydrolases, and in agricultural applications. A preferred class of compounds for practicing the invention have the structure shown by Formula 1 wherein 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 are each independently a substituted or unsubstituted alkyl, haloalkyl, cycloalkyl, aryl, acyl, or heterocyclic, or being a metabolite or degradation product thereof.

摘要翻译： 提供了生物稳定的可溶性环氧化物水解酶抑制剂。 抑制剂可用于例如在治疗应用中选择性抑制环氧化物水解酶，例如治疗炎症，用于环氧化物水解酶的亲和分离，以及在农业应用中。 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X和Y各自独立地为氮，氧或硫，X可以进一步为碳，R 1， -R 4是氢，当X是氮时，R 2是氢，但当X是硫或氧时，R 2不是存在的，R 4是氢 当Y为氮时，当Y为硫或氧时不存在，R 1和R 3各自独立地为取代或未取代的烷基，卤代烷基，环烷基，芳基，酰基 ，或杂环，或其代谢产物或降解产物。