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1. 发明专利

CA3005874A1 STABLE ANALOGS OF CYP450 LIPID METABOLITES AND INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE 未知
公开(公告)号：CA3005874A1
公开(公告)日：2017-05-26
申请号：CA3005874
申请日：2016-11-17
申请人： MASSACHUSETTS EYE & EAR INFIRMARY , UNIV CALIFORNIA , CONNOR KIP M , HASEGAWA EIICHI , HAMMOCK BRUCE D , LEE KIN SING STEPHEN
发明人： CONNOR KIP M , HASEGAWA EIICHI , HAMMOCK BRUCE D , LEE KIN SING STEPHEN
IPC分类号： A61K31/202 , A61P27/02
摘要： This disclosure relates to methods of reducing inflammation, angiogenesis, vascular leakage and neovascularization by administering to a subject in need thereof one or more stable analogs of CYP450 lipid metabolites (e.g., eicosanoids) and one or more inhibitors of a soluble epoxide hydrolase (sEH). This disclosure also relates to methods of treating disorders associated with inflammation, angiogenesis, vascular leakage and neovascularization by administering to a subject in need thereof one or more stable analogs of CYP450 lipid metabolites (e.g., eicosanoids) and one or more inhibitors of a soluble epoxide hydrolase (sEH). This disclosure further relates to pharmaceutical compositions and kits comprising at least one stable analog of CYP450 lipid metabolites (e.g., eicosanoids) and at least one inhibitor of a soluble epoxide hydrolase (sEH).

2. 发明专利

AU2016356767A1 Stable analogs of CYP450 lipid metabolites and inhibitors of soluble epoxide hydrolase 未知
公开(公告)号：AU2016356767A1
公开(公告)日：2018-06-07
申请号：AU2016356767
申请日：2016-11-17
申请人： MASSACHUSETTS EYE & EAR INFIRMARY , UNIV CALIFORNIA
发明人： CONNOR KIP M , HASEGAWA EIICHI , HAMMOCK BRUCE D , LEE KIN SING STEPHEN
IPC分类号： A61K31/202 , A61P27/02
摘要： This disclosure relates to methods of reducing inflammation, angiogenesis, vascular leakage and neovascularization by administering to a subject in need thereof one or more stable analogs of CYP450 lipid metabolites (e.g., eicosanoids) and one or more inhibitors of a soluble epoxide hydrolase (sEH). This disclosure also relates to methods of treating disorders associated with inflammation, angiogenesis, vascular leakage and neovascularization by administering to a subject in need thereof one or more stable analogs of CYP450 lipid metabolites (e.g., eicosanoids) and one or more inhibitors of a soluble epoxide hydrolase (sEH). This disclosure further relates to pharmaceutical compositions and kits comprising at least one stable analog of CYP450 lipid metabolites (e.g., eicosanoids) and at least one inhibitor of a soluble epoxide hydrolase (sEH).

3. 发明申请

WO2006045119A3 IMPROVED INHIBITORS FOR THE SOLUBLE EPOXIDE HYDROLASE 审中-公开
标题翻译：改进的可溶性环氧化物水解抑制剂
公开(公告)号：WO2006045119A3
公开(公告)日：2007-02-08
申请号：PCT/US2005038282
申请日：2005-10-20
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , KIM IN-HAE , MORISSEAU CHRISTOPHE , WATANABE TAKAHO , NEWMAN JOHN W
发明人： HAMMOCK BRUCE D , KIM IN-HAE , MORISSEAU CHRISTOPHE , WATANABE TAKAHO , NEWMAN JOHN W
IPC分类号： C07D405/12 , A61K31/40 , A61K31/425 , C07D207/50
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。

4. 发明申请

WO2006133257A9 USE OF CIS-EPOXYEICOSATRIENOIC ACIDS AND INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE TO REDUCE CARDIOMYOPATHY 审中-公开
标题翻译：独联体环氧乙烷酸和可溶性环氧化物水解酶抑制剂减少心脏病的用途
公开(公告)号：WO2006133257A9
公开(公告)日：2007-05-10
申请号：PCT/US2006022054
申请日：2006-06-06
申请人： UNIV CALIFORNIA , CHIAMVIMONVAT NIPAVAN , HAMMOCK BRUCE D
发明人： CHIAMVIMONVAT NIPAVAN , HAMMOCK BRUCE D
IPC分类号： A61K31/336 , C12N15/113
CPC分类号： C12N15/1137 , A61K31/185 , A61K31/336 , A61K45/06 , C12N2310/11 , C12N2310/14 , C12Y303/02009 , A61K2300/00
摘要： The invention provides methods for inhibiting cardiomyopathy and for inhibiting cardiac arrhythmia, by administering to an individual in need thereof a cis-epoxyeicosantrienoic acid, an inhibitor of soluble epoxide hydrolase (sEH), or both. In some embodiments, the method comprises administering to the individual a nucleic acid encoding an inhibitor of sEH. Cardiomyopathies treatable by the methods of the invention include cardiac hypertrophy and dilated cardiomyopathy.
摘要翻译：本发明提供抑制心肌病和抑制心律失常的方法，通过向有需要的个体施用顺式 - 环氧二十碳三烯酸，可溶性环氧化物水解酶（sEH）抑制剂或两者。在一些实施方案中，该方法包括向个体施用编码sEH抑制剂的核酸。可通过本发明的方法治疗的心肌病包括心脏肥大和扩张型心肌病。

5. 发明申请

WO2006086108A3 USE OF INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE TO SYNERGIZE ACTIVITY OF COX AND 5-LOX INHIBITORS 审中-公开
标题翻译：使用可溶性环氧化物水解酶抑制剂来协调COX和5-LOX抑制剂的活性
公开(公告)号：WO2006086108A3
公开(公告)日：2007-01-11
申请号：PCT/US2006000914
申请日：2006-01-10
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , SCHMELZER KARA , INCEOGLU AHMET BORA
发明人： HAMMOCK BRUCE D , SCHMELZER KARA , INCEOGLU AHMET BORA
IPC分类号： A61K31/42 , A61K31/415
CPC分类号： A61K31/17 , A61K31/12 , A61K31/132 , A61K31/167 , A61K31/192 , A61K31/196 , A61K31/20 , A61K31/201 , A61K31/202 , A61K31/22 , A61K31/336 , A61K31/341 , A61K31/365 , A61K31/40 , A61K31/403 , A61K31/405 , A61K31/407 , A61K31/415 , A61K31/42 , A61K31/444 , A61K31/5415 , A61K31/557 , A61K31/60 , A61K31/603 , A61K31/606 , A61K31/612 , A61K31/616 , A61K31/635 , A61K45/06 , A61K2300/00
摘要： The invention relates to methods, compositions , and uses of those compositions for making medicaments, for potentiating the beneficial effects of inhibitors of COX-1, COX-2, and 5-LOX, and reducing adverse effects, by also administering inhibitors of soluble epoxide hydrolase ("sEH"), with or without also administering one or more cis-epoxyeicosantrienoic acids. The invention further relates to the use of inhibitors of sEH as analgesics and to methods and compositions of epoxides of eicosapentaenoic acid and docosahexaenoic acid to reduce pain or inflammation or both.
摘要翻译：本发明涉及这些用于制备药物的组合物的方法，组合物和用途，用于增强COX-1，COX-2和5-LOX抑制剂的有益效果，以及通过还施用可溶性环氧化物的抑制剂来减少不良反应水解酶（“sEH”），有或没有也施用一种或多种顺式 - 环氧二十碳三烯酸。本发明还涉及sEH抑制剂作为止痛剂的用途以及二十碳五烯酸和二十二碳六烯酸的环氧化物的方法和组合物，以减少疼痛或炎症或两者。

6. 发明申请

WO2008008732A3 SUBSTITUTED AMINOPYRIDINES AS FLUORESCENT REPORTERS FOR AMIDE HYDROLASES 审中-公开
标题翻译：作为酰胺水溶液的荧光报告物的替代氨基亚胺
公开(公告)号：WO2008008732A3
公开(公告)日：2008-12-18
申请号：PCT/US2007073076
申请日：2007-07-09
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , HUANG HUAZHANG , NISHI KOSUKE
发明人： HAMMOCK BRUCE D , HUANG HUAZHANG , NISHI KOSUKE
IPC分类号： C12Q1/34 , C07D213/75 , C07K2/00 , C12Q1/37
CPC分类号： C07D213/75
摘要： The present invention provides conjugates comprising a substituted aminopyridine covalently attached to an organic molecule via an amide bond. Such conjugates find utility as substrates for amide hydrolases, where the substituted aminopyridine acts as a fluorescent reporter of amide hydrolase activity. As a result, the conjugates described herein can advantageously be used in assays to detect amide hydrolase activity based upon measuring the fluorescence of a substituted aminopyridine that is released after amide hydrolysis. The conjugates of the present invention are also particularly useful in screening assays, which enable the identification of inhibitory molecules for amide hydrolases and other enzymes. The identified amide hydrolase inhibitors can be used in the treatment of a variety of diseases and disorders associated with aberrant amide hydrolase activity.
摘要翻译：本发明提供包含通过酰胺键共价连接到有机分子上的取代的氨基吡啶的缀合物。这种缀合物可用作酰胺水解酶的底物，其中取代的氨基吡啶用作酰胺水解酶活性的荧光报告物。结果，本文所述的缀合物可有利地用于测定酰胺水解酶活性的测定中，其基于测量酰胺水解后释放的取代的氨基吡啶的荧光。本发明的缀合物在筛选测定中也是特别有用的，其能够鉴定酰胺水解酶和其它酶的抑制分子。鉴定的酰胺水解酶抑制剂可用于治疗与异常酰胺水解酶活性相关的各种疾病和病症。

7. 发明申请

WO2006045119A9 IMPROVED INHIBITORS FOR THE SOLUBLE EPOXIDE HYDROLASE 审中-公开
标题翻译：改进的可溶性环氧化物水解酶抑制剂
公开(公告)号：WO2006045119A9
公开(公告)日：2006-05-26
申请号：PCT/US2005038282
申请日：2005-10-20
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , KIM IN-HAE , MORISSEAU CHRISTOPHE , WATANABE TAKAHO , NEWMAN JOHN W
发明人： HAMMOCK BRUCE D , KIM IN-HAE , MORISSEAU CHRISTOPHE , WATANABE TAKAHO , NEWMAN JOHN W
IPC分类号： A61K31/336
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：提供可溶性环氧化物水解酶（sEH）的抑制剂，其包含多个药效团并可用于治疗疾病。

8. 发明申请

WO2004089296A3 IMPROVED INHIBITORS FOR THE SOLUBLE EPOXIDE HYDROLASE 审中-公开
标题翻译：改进的可溶性环氧化物水解抑制剂
公开(公告)号：WO2004089296A3
公开(公告)日：2006-03-09
申请号：PCT/US2004010298
申请日：2004-04-02
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , KIM IN-HAE , MORISSEAU CHRISTOPHE , WATANABE TAKAHO , NEWMAN JOHN W
发明人： HAMMOCK BRUCE D , KIM IN-HAE , MORISSEAU CHRISTOPHE , WATANABE TAKAHO , NEWMAN JOHN W
IPC分类号： A61K20060101 , A61K6/00 , A61K31/365 , A61K31/381 , A61K31/4015 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/513 , A61K38/04 , A61K38/05 , A61K38/06 , A61K38/08 , C07C275/26 , C07C275/30 , C07C275/42 , C07C311/05 , C07C311/51 , C07C275/00
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。

9. 发明申请

WO2005089380A3 REDUCING NEPHROPATHY WITH INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE AND EPOXYEICOSANOIDS 审中-公开
标题翻译：减少可溶性环氧化物水解酶和环氧乙烷的抑制剂
公开(公告)号：WO2005089380A3
公开(公告)日：2007-09-27
申请号：PCT/US2005008765
申请日：2005-03-16
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , WATANABE TAKAHO , MA SEUNG JIN , BENNETT SUSAN E , STERN JUDITH S , MORISSEAU CHRISTOPHE , KIM IN-HAE
发明人： HAMMOCK BRUCE D , WATANABE TAKAHO , MA SEUNG JIN , BENNETT SUSAN E , STERN JUDITH S , MORISSEAU CHRISTOPHE , KIM IN-HAE
IPC分类号： A61K31/70 , A61K31/17 , A61K31/355
CPC分类号： A61K31/70 , A61K31/17 , A61K31/355
摘要： The invention provides uses and methods for reducing nephropathy in persons with diabetes mellitus (particularly Type 2 diabetes), in persons with metabolic syndrome, in persons with triglyceride levels over 215 mg/dL, and in persons with a cholesterol level over 200 mg/dL, by administering an inhibitor of soluble epoxide hydrolase ("sEH"). Optionally, a cis-epoxyeicosantrienoic acid ("EET") can be administered with the sEH inhibitor. The invention further provides for using EETs in conjunction with one or more sEH inhibitors to reduce hypertension, and for compositions of EETs coated with a material insoluble in an acid of pH 3 but soluble in a solution with a pH of 7.4 or higher.
摘要翻译：本发明提供了在甘油三酯水平超过215mg / dL的人中以及胆固醇水平超过200mg / dL的人中减少糖尿病（特别是2型糖尿病）患有代谢综合征患者的肾病的用途和方法，通过施用可溶性环氧化物水解酶（“sEH”）的抑制剂。任选地，顺式 - 环氧二十碳三烯酸（“EET”）可与sEH抑制剂一起施用。本发明进一步提供使用EET与一种或多种sEH抑制剂联合以降低高血压，以及用不溶于pH 3但可溶于pH 7.4或更高的溶液的材料涂覆的EET组合物。

10. 发明申请

WO2005094373A2 USE OF CIS-EPOXYEICOSANTRIENOIC ACIDS AND INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE TO REDUCE PULMONARY INFILTRATION BY NEUTROPHILS 审中-公开
标题翻译：使用可溶性环氧化物水解酶的CIS-环氧亚氨基三乙酸和抑制剂减少中性粒细胞的浸润
公开(公告)号：WO2005094373A2
公开(公告)日：2005-10-13
申请号：PCT/US2005010781
申请日：2005-03-31
申请人： UNIV CALIFORNIA , HAMMOCK BRUCE D , PINKERTON KENT E , SMITH KEVIN R , WATANABE TAKAHO , MA SEUNG JIN
发明人： HAMMOCK BRUCE D , PINKERTON KENT E , SMITH KEVIN R , WATANABE TAKAHO , MA SEUNG JIN
IPC分类号： A61K31/335
CPC分类号： A61K31/558 , A61K9/146 , A61K31/17 , A61K31/20 , A61K45/06
摘要： It has now been discovered that inhibitors of soluble epoxide hydrolase ("sEH") are useful in reducing the severity of or inhibiting the progression of obstructive pulmonary diseases, restrictive airway diseases, and asthma. Administering a cis-epoxyeicosantrienoic acid ("EET") in addition to the inhibitor is at least additive, and may be synergistic, in reducing or inhibiting these conditions and diseases, as measured by reduced numbers of neutrophils present in the lung. The inhibitor of sEH may be a nucleic acid, such as a small interfering RNA.
摘要翻译：现在已经发现，可溶性环氧化物水解酶（“sEH”）的抑制剂可用于降低阻塞性肺疾病，限制性气道疾病和哮喘的严重性或抑制其进展。除了抑制剂之外，还施用顺式 - 环氧二十碳三烯酸（“EET”）至少是添加剂，并且可以协同作用，以减少或抑制这些病症和疾病，如通过减少存在于肺中的嗜中性粒细胞数量所测量的。 sEH的抑制剂可以是核酸，例如小的干扰RNA。

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