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1. 发明申请

WO2004034968A3 COMBINATION THERAPY FOR CONTROLLING APPETITES 审中-公开
标题翻译：用于控制提示的组合治疗
公开(公告)号：WO2004034968A3
公开(公告)日：2005-03-10
申请号：PCT/US0325760
申请日：2003-08-15
申请人： UNIV CALIFORNIA , PIOMELLI DANIELE , DE FONSECA FERNANDO RODRIGUEZ , FU JIN , GAETANI SILVANA
发明人： PIOMELLI DANIELE , DE FONSECA FERNANDO RODRIGUEZ , FU JIN , GAETANI SILVANA
IPC分类号： A61K31/415 , A61K31/70 , A61K45/06 , A61K31/445 , A61K31/535
CPC分类号： A61K31/415 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： The invention provides methods and pharmaceutical compositions for administering a PPARalpha agonist (e.g., OEA-like agonist, OEA-like compound), an OEA-like appetite reducing compound, or a FAAH inhibitor and a CB1 cannabinoid receptor antagonist to a subject in order to reduce the consumption or ingestion of food, ethanol or other appetizing substances as well as in treating appetency disorders related to the excess consumption of food, ethanol, and other appetizing substances. The combination therapy can also be useful for reducing body fat or body weight and modulating lipid metabolism.
摘要翻译：本发明提供了用于向受试者施用PPARα激动剂（例如，OEA样激动剂，OEA样化合物），类似OEA的食欲降低化合物或FAAH抑制剂和CB1大麻素受体拮抗剂的方法和药物组合物，以便减少食物，乙醇或其他开胃物质的消耗或摄入，以及治疗与食物，乙醇和其他开胃物质过量消费有关的食欲障碍。联合治疗也可用于减少体脂肪或体重并调节脂质代谢。

2. 发明申请

WO2005002524A2 COMPOUNDS, COMPOSITIONS AND THERAPEUTIC USES OF OLEOYLETHANOLAMIDE-LIKE COMPOUNDS AND MODULATORS OF PPARα 审中-公开
标题翻译：化合物，组合物和治疗用途的乙酰氨基酚类化合物和PPARα的调节剂
公开(公告)号：WO2005002524A2
公开(公告)日：2005-01-13
申请号：PCT/US2004/021394
申请日：2004-07-01
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , FU, Jin , GAETANI, Silvana , PIOMELLI, Daniele
发明人： FU, Jin , GAETANI, Silvana , PIOMELLI, Daniele
IPC分类号： A61K
CPC分类号： A61K31/20
摘要： The present invention provides compounds, compositions, and methods for the treatment of disorders and conditions mediated by PPARa. The invention relates to the surprising discovery that oleoylethanolamide (OEA) is an endogenous high affinity and selective ligand of PPARa. The compounds of the invention include, but are not limited to, specific PPARa agonists sharing the receptor binding properties of OEA and fatty acid alkanolamides and their homologs which also are PPARa agonists. Such OEA-like compounds include, but are not limited to, compounds of the following formula: in which n is from 0 to 5, the sum of a and b can be from 0 to 4; Z is a member selected from the group consisting of -C(O)N(Ro) ; (Ro)NC(O) ; OC(O) ; (O)CO ; O; NRo; and S; and wherein Ro and R2 are members independently selected from the group consisting of unsubstituted or unsubstituted alkyl, hydrogen, C1 -C6 alkyl, and lower (C1-C6) acyl, and wherein up to eight hydrogen atoms are optionally substituted by methyl or a double bond, and the bond between carbons c and d may be unsaturated or saturated, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了用于治疗由PPARα介导的病症和病症的化合物，组合物和方法。本发明涉及令人惊奇的发现，即油基乙醇酰胺（OEA）是PPARα的内源性高亲和力和选择性配体。本发明的化合物包括但不限于分享了OEA和脂肪酸链烷醇酰胺及其同系物的受体结合性质的特异性PPARα激动剂，它们也是PPARα激动剂。这种OEA类化合物包括但不限于下式的化合物：其中n为0至5，a和b的和可以为0至4; Z是选自-C（O）N（Ro）; （Ro）NC（O）; OC（O）; （O）CO; O; NRO; 和S; 并且其中R a和R 2是独立地选自未取代或未取代的烷基，氢，C 1 -C 6烷基和低级（C 1 -C 6）酰基的成员，并且其中多达8个氢原子任选地被甲基或双碳和c之间的键可以是不饱和的或饱和的，或其药学上可接受的盐。

3. 发明申请

WO2005002524A3 COMPOUNDS, COMPOSITIONS AND THERAPEUTIC USES OF OLEOYLETHANOLAMIDE-LIKE COMPOUNDS AND MODULATORS OF PPARalpha 审中-公开
标题翻译：类脂酰胺酰胺化合物和PPARα调节剂的化合物，组合物和治疗用途
公开(公告)号：WO2005002524A3
公开(公告)日：2005-04-28
申请号：PCT/US2004021394
申请日：2004-07-01
申请人： UNIV CALIFORNIA , FU JIN , GAETANI SILVANA , PIOMELLI DANIELE
发明人： FU JIN , GAETANI SILVANA , PIOMELLI DANIELE
IPC分类号： A61K20060101 , A61K31/195 , A61K31/20
CPC分类号： A61K31/20
摘要： The present invention provides compounds, compositions, and methods for the treatment of disorders and conditions mediated by PPARa. The invention relates to the surprising discovery that oleoylethanolamide (OEA) is an endogenous high affinity and selective ligand of PPARa. The compounds of the invention include, but are not limited to, specific PPARa agonists sharing the receptor binding properties of OEA and fatty acid alkanolamides and their homologs which also are PPARa agonists. Such OEA-like compounds include, but are not limited to, compounds of the following formula: in which n is from 0 to 5, the sum of a and b can be from 0 to 4; Z is a member selected from the group consisting of -C(O)N(Ro) ; (Ro)NC(O) ; OC(O) ; (O)CO ; O; NRo; and S; and wherein Ro and R2 are members independently selected from the group consisting of unsubstituted or unsubstituted alkyl, hydrogen, C1 -C6 alkyl, and lower (C1-C6) acyl, and wherein up to eight hydrogen atoms are optionally substituted by methyl or a double bond, and the bond between carbons c and d may be unsaturated or saturated, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了用于治疗由PPARα介导的病症和病症的化合物，组合物和方法。本发明涉及令人惊讶的发现，即油酰乙醇酰胺（OEA）是PPARα的内源性高亲和力和选择性配体。本发明的化合物包括但不限于共享OEA和脂肪酸链烷醇酰胺及其同系物（其也是PPARα激动剂）的受体结合特性的特异性PPARα激动剂。这样的OEA样化合物包括但不限于下式的化合物：其中n为0-5，a和b之和可以为0-4; Z是选自-C（O）N（Ro）; （Ro）NC（O）; OC（O）; （O）CO; O; NRO; 和S; 并且其中R 0和R 2独立地选自未取代或未取代的烷基，氢，C 1 -C 6烷基和低级（C 1 -C 6）酰基，并且其中至多8个氢原子任选被甲基或双键，并且碳c和d之间的键可以是不饱和的或饱和的，或其药学上可接受的盐。

4. 发明申请

WO2004034968A2 COMBINATION THERAPY FOR CONTROLLING APPETITES 审中-公开
标题翻译：用于控制提示的组合治疗
公开(公告)号：WO2004034968A2
公开(公告)日：2004-04-29
申请号：PCT/US2003/025760
申请日：2003-08-15
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez , FU, Jin , GAETANI, Silvana
发明人： PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez , FU, Jin , GAETANI, Silvana
IPC分类号： A61K
CPC分类号： A61K31/415 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： The invention provides methods and pharmaceutical compositions for administering a PPARα agonist (e.g., OEA-like agonist, OEA-like compound), an OEA-like appetite reducing compound, or a FAAH inhibitor and a CB1 cannabinoid receptor antagonist to a subject in order to reduce the consumption or ingestion of food, ethanol or other appetizing substances as well as in treating appetency disorders related to the excess consumption of food, ethanol, and other appetizing substances. The combination therapy can also be useful for reducing body fat or body weight and modulating lipid metabolism.
摘要翻译：本发明提供了用于向受试者施用PPARα激动剂（例如，OEA样激动剂，OEA样化合物），类似OEA的食欲降低化合物或FAAH抑制剂和CB1大麻素受体拮抗剂的方法和药物组合物，以便减少食物，乙醇或其他开胃物质的消耗或摄入，以及治疗与食物，乙醇和其他开胃物质过量消费有关的食欲障碍。联合治疗也可用于减少体脂肪或体重并调节脂质代谢。

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