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1. 发明授权

US08501783B2 Conformationally restricted urea inhibitors of soluble epoxide hydrolase 有权
标题翻译：构象限制的可溶性环氧化物水解酶的脲抑制剂
公开(公告)号：US08501783B2
公开(公告)日：2013-08-06
申请号：US13455861
申请日：2012-04-25
申请人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless, Jr.
发明人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless, Jr.
IPC分类号： A61K31/445
CPC分类号： C07D211/58 , C07D209/08 , C07D211/26 , C07D211/96 , C07D213/40 , C07D235/30 , C07D295/20 , C07D295/205 , C07D401/06 , C07D401/12 , C07D487/18 , C12Q1/34
摘要： Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要翻译：提供了可溶性环氧化物水解酶（sEH）的抑制剂，其包含多个药效团并且可用于治疗疾病。

2. 发明申请

US20130137726A1 CONFORMATIONALLY RESTRICTED UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE 有权
标题翻译：可溶性环氧化物水解物的一致的限制性尿素抑制剂
公开(公告)号：US20130137726A1
公开(公告)日：2013-05-30
申请号：US13455861
申请日：2012-04-25
申请人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless, JR.
发明人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless, JR.
IPC分类号： C07D211/58 , C07D211/96 , C07D401/06
CPC分类号： C07D211/58 , C07D209/08 , C07D211/26 , C07D211/96 , C07D213/40 , C07D235/30 , C07D295/20 , C07D295/205 , C07D401/06 , C07D401/12 , C07D487/18 , C12Q1/34
摘要： Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要翻译：提供了可溶性环氧化物水解酶（sEH）的抑制剂，其包含多个药效团并且可用于治疗疾病。

3. 发明授权

US08188289B2 Conformationally restricted urea inhibitors of soluble epoxide hydrolase 有权
标题翻译：构象限制的可溶性环氧化物水解酶的脲抑制剂
公开(公告)号：US08188289B2
公开(公告)日：2012-05-29
申请号：US11685674
申请日：2007-03-13
申请人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless
发明人： Bruce D. Hammock , Paul D. Jones , Christophe Morisseau , Huazhang Huang , Hsing-Ju Tsai , Richard Gless
IPC分类号： C07D211/60 , C07D211/30
CPC分类号： C07D211/58 , C07D209/08 , C07D211/26 , C07D211/96 , C07D213/40 , C07D235/30 , C07D295/20 , C07D295/205 , C07D401/06 , C07D401/12 , C07D487/18 , C12Q1/34
摘要： Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要翻译：提供了可溶性环氧化物水解酶（sEH）的抑制剂，其包含多个药效团并且可用于治疗疾病。

4. 发明申请

US20110098322A1 PREPARATION OF NOVEL 1,3-SUBSTITUTED UREAS AS INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE 审中-公开
标题翻译：作为可溶性环氧化物水解酶抑制剂的新型1,3-取代的尿素的制备
公开(公告)号：US20110098322A1
公开(公告)日：2011-04-28
申请号：US12672405
申请日：2008-08-05
申请人： James R. Sanborn , Bruce D. Hammock , Sung Hee Hwang , Paul D. Jones , Christophe Morisseau
发明人： James R. Sanborn , Bruce D. Hammock , Sung Hee Hwang , Paul D. Jones , Christophe Morisseau
IPC分类号： A61K31/4468 , C07C275/26 , C07C255/60 , C07C275/24 , C07C229/66 , C07D211/32 , C07D211/58 , C07D211/96 , C12N9/99 , A61K31/17 , A61K31/277 , A61K31/196 , A61K31/24 , A61K31/445
CPC分类号： C07D211/96 , C07C275/24 , C07C275/26 , C07C2601/14 , C07D211/58
摘要： The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.
摘要翻译：本发明提供可以抑制可溶性环氧化物水解酶活性的化合物。特别地，本发明提供式Ⅰ化合物。

5. 发明授权

US09096532B2 Pyrazole inhibitors of COX-2 and sEH 有权
标题翻译：吡唑类抑制剂COX-2和sEH
公开(公告)号：US09096532B2
公开(公告)日：2015-08-04
申请号：US13993317
申请日：2011-12-12
申请人： Bruce D. Hammock , Sung Hee Hwang , Karen Wagner , Christophe Morisseau , Aaron Wecksler , Guodong Zhang
发明人： Bruce D. Hammock , Sung Hee Hwang , Karen Wagner , Christophe Morisseau , Aaron Wecksler , Guodong Zhang
IPC分类号： A61K31/635 , C07D231/10 , C07D231/12 , C07D231/40 , C07D231/14
CPC分类号： C07D231/12 , C07D231/14 , C07D231/40
摘要： The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo.
摘要翻译：本发明提供化合物和组合物，例如一系列化合物，其中1,5-双芳基吡唑基团可通过不可裂解的共价链与脲基团缀合，其可用作双重COX-2 / sEH抑制剂。本文公开的化合物具有与花生四烯酸级联相关的活性。使用脂多糖（LPS）诱导的大鼠疼痛模型证明了这些化合物的活性。与相同剂量的塞来昔布（即，COX-2抑制剂）相比，本发明的化合物与同样剂量的t-AUCB（即sEH抑制剂）相比，表现出优异的抗异常性疼痛活性，并且还作为与联合给药相同剂量的塞来昔布和t-AUCB相比。本发明的双重抑制剂在伤害性行为测定中表现出增强的体内抗异常性疼痛活性。此外，本发明的化合物还证明对体内，体内和体内对内皮细胞（HUVEC）具有有效的抗血管生成作用并抑制血管生成。本发明的双重抑制剂还表现出对血管内肿瘤生长缓慢的抗血管生成作用。

6. 发明授权

US08476043B2 Inhibitors for the soluble epoxide hydrolase 有权
标题翻译：可溶性环氧化物水解酶的抑制剂
公开(公告)号：US08476043B2
公开(公告)日：2013-07-02
申请号：US12631577
申请日：2009-12-04
申请人： Bruce D. Hammock , In-Hae Kim , Christophe Morisseau , Takaho Watanabe , John W. Newman
发明人： Bruce D. Hammock , In-Hae Kim , Christophe Morisseau , Takaho Watanabe , John W. Newman
IPC分类号： C12P19/48 , C07C211/16 , C12Q1/34
CPC分类号： C07D295/088 , C07C233/06 , C07C233/08 , C07C235/14 , C07C275/26 , C07C311/04 , C07C311/05 , C07C311/18 , C07C311/41 , C07C311/51 , C07C323/44 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2603/18 , C07C2603/74 , C07D209/18 , C07D213/04 , C07D233/61 , C07D233/64 , C07D279/12 , C07D295/13 , C07D295/32 , C07D403/06 , C07K5/0205
摘要： Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要翻译：提供了可溶性环氧化物水解酶（sEH）的抑制剂，其包含多个药效团并且可用于治疗疾病。

7. 发明申请

US20140038923A1 PYRAZOLE INHIBITORS OF COX-2 AND SEH 有权
标题翻译： COX-2和SEH的吡唑抑制剂
公开(公告)号：US20140038923A1
公开(公告)日：2014-02-06
申请号：US13993317
申请日：2011-12-12
申请人： Bruce D. Hammock , Sung Hee Hwang , Karen Wagner , Christophe Morisseau , Aaron Wecksler , Guodong Zhang
发明人： Bruce D. Hammock , Sung Hee Hwang , Karen Wagner , Christophe Morisseau , Aaron Wecksler , Guodong Zhang
IPC分类号： C07D231/12 , C07D231/14
CPC分类号： C07D231/12 , C07D231/14 , C07D231/40
摘要： The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo.
摘要翻译：本发明提供化合物和组合物，例如一系列化合物，其中1,5-双芳基吡唑基团可通过不可裂解的共价链与脲基团缀合，其可用作双重COX-2 / sEH抑制剂。本文公开的化合物具有与花生四烯酸级联相关的活性。使用脂多糖（LPS）诱导的大鼠疼痛模型证明了这些化合物的活性。与相同剂量的塞来昔布（即，COX-2抑制剂）相比，本发明的化合物与同样剂量的t-AUCB（即sEH抑制剂）相比，表现出优异的抗异常性疼痛活性，并且还作为与联合给药相同剂量的塞来昔布和t-AUCB相比。本发明的双重抑制剂在伤害性行为测定中表现出增强的体内抗异常性疼痛活性。此外，本发明的化合物还证明对体内，体内和体内对内皮细胞（HUVEC）具有有效的抗血管生成作用并抑制血管生成。本发明的双重抑制剂还表现出对血管内肿瘤生长缓慢的抗血管生成作用。

8. 发明申请

US20110245331A1 INHIBITORS OF EPOXIDE HYDROLASES FOR THE TREATMENT OF HYPERTENSION 审中-公开
标题翻译：用于治疗高血压的环氧化物水解物的抑制剂
公开(公告)号：US20110245331A1
公开(公告)日：2011-10-06
申请号：US13113028
申请日：2011-05-20
申请人： Deanna L. Kroetz , Darryl C. Zeldin , Bruce D. Hammock , Christophe Morisseau
发明人： Deanna L. Kroetz , Darryl C. Zeldin , Bruce D. Hammock , Christophe Morisseau
IPC分类号： A61K31/7088 , A61P9/12 , C12N9/96 , C12Q1/34
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 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。

9. 发明申请

US20090326039A1 INHIBITORS FOR THE SOLUBLE EPOXIDE HYDROLASE 有权
标题翻译：可溶性环氧化物水解物的抑制剂
公开(公告)号：US20090326039A1
公开(公告)日：2009-12-31
申请号：US12396391
申请日：2009-03-02
申请人： Bruce D. Hammock , In-Hae Kim , Christophe Morisseau , Takaho Watanabe , John W. Newman
发明人： Bruce D. Hammock , In-Hae Kim , Christophe Morisseau , Takaho Watanabe , John W. Newman
IPC分类号： C12N9/99 , A61K31/17 , A61K31/215 , A61K31/195 , A61K31/401 , C12Q1/34
CPC分类号： C07C275/26 , C07C275/30 , C07C275/42 , C07C311/04 , C07C311/05 , C07C311/51 , C07C323/59 , C07C2601/02 , C07C2601/14 , C07C2603/74 , C07D207/16 , C07D233/24 , C07D233/64
摘要： Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
摘要翻译：提供了可溶性环氧化物水解酶（sEH）的抑制剂，其包含多个药效团并且可用于治疗疾病。

10. 发明申请

US20090215894A1 INHIBITION OF PHOSPHATASE ACTIVITY OF SOLUBLE EPOXIDE HYDROLASE AMINO TERMINUS AND USES THEREOF 审中-公开
标题翻译：可溶性环氧化物水解酶氨基末端磷酸酶活性的抑制及其用途
公开(公告)号：US20090215894A1
公开(公告)日：2009-08-27
申请号：US12063573
申请日：2006-08-14
申请人： Bruce D. Hammock , Christophe Morisseau , John W. Newman
发明人： Bruce D. Hammock , Christophe Morisseau , John W. Newman
IPC分类号： A61K31/20 , C12N9/99 , A61K31/10 , C07C309/00
CPC分类号： A61K31/285 , C07C305/06 , C07C305/10
摘要： Inhibitors of the phosphatase activity of soluble epoxide hydrolase (sEH) are provided and are useful for in the treatment of diseases. These Inhibitors are based on derivatives of various epoxide hydrolase substrates that mimic the enzyme substrate so that there Is stable Interaction with the enzyme catalytic site. These inhibitors are potentially useful for the treatment of hypertension, vascular inflammation, renal inflammation, and lung disease.
摘要翻译：提供可溶性环氧化物水解酶（sEH）的磷酸酶活性的抑制剂，可用于治疗疾病。这些抑制剂基于模拟酶底物的各种环氧化物水解酶底物的衍生物，使得与酶催化位点具有稳定的相互作用。这些抑制剂可用于治疗高血压，血管炎症，肾脏炎症和肺部疾病。

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