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11. 发明申请

WO2002080860A2 METHODS, COMPOUNDS, AND COMPOSITIONS FOR REDUCING BODY FAT AND MODULATING FATTY ACID METABOLISM 审中-公开
标题翻译：用于减少身体脂肪和调节脂肪酸代谢的方法，化合物和组合物
公开(公告)号：WO2002080860A2
公开(公告)日：2002-10-17
申请号：PCT/US2002/009773
申请日：2002-03-27
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez
发明人： PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez
IPC分类号： A61K
CPC分类号： A61K31/16 , A61K31/164
摘要： Methods, pharmaceutical compositions, and compounds for reducing body weight, modulating body lipid metabolism, and reducing food intake in mammals are provided. The compounds of the invention include fatty acid ethanolamide compounds, homologues and analogs of which the prototype is the endogenous fatty acid ethanolamide, oleoylethanolamide.
摘要翻译：提供了用于减少体重，调节体脂代谢和减少哺乳动物食物摄入的方法，药物组合物和化合物。本发明的化合物包括脂肪酸乙醇酰胺化合物，其原型是内源性脂肪酸乙醇酰胺的同系物和类似物，油基乙醇酰胺。

12. 发明申请

WO2013028570A3 META-SUBSTITUTED BIPHENYL PERIPHERALLY RESTRICTED FAAH INHIBITORS 审中-公开
标题翻译：金属取代的联苯二烯外围限制性FAAH抑制剂
公开(公告)号：WO2013028570A3
公开(公告)日：2013-04-18
申请号：PCT/US2012051478
申请日：2012-08-17
申请人： UNIV CALIFORNIA , FOND ISTITUTO ITALIANO DI TECNOLOGIA , UNI DEGLI STUDI DI URBINO CARLO BO , UNIV PARMA , PIOMELLI DANIELE , MORENO-SANZ GUILLERMO , BANDIERA TIZIANO , MOR MARCO , TARZIA GIORGIO
发明人： PIOMELLI DANIELE , MORENO-SANZ GUILLERMO , BANDIERA TIZIANO , MOR MARCO , TARZIA GIORGIO
IPC分类号： C07C233/06 , A61K31/165 , A61P29/00 , C07C233/23 , C07D309/14
CPC分类号： C07C271/56 , C07C269/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D309/14
摘要： The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.
摘要翻译：本发明提供制备和使用脂肪酸酰胺水解酶（FAAH）的外周限制性抑制剂的方法。本发明提供抑制FAAH活性并增加中枢神经系统（CNS）外的氨基酰胺水平的化合物和组合物。本发明还提出了抑制FAAH的方法以及治疗诸如但不限于疼痛，炎症，免疫病症，皮炎，粘膜炎，周围感觉神经元，神经性皮炎和膀胱过度活动症的过度反应的病症的方法。因此，本发明还提供了用于治疗其中选择性抑制外周FAAH（与CNS FAAH相反））有益的化合物，方法和药物组合物。

13. 发明申请

WO2013028570A2 META-SUBSTITUTED BIPHENYL PERIPHERALLY RESTRICTED FAAH INHIBITORS 审中-公开
标题翻译： META取代的联苯外周限制性FAAH抑制剂
公开(公告)号：WO2013028570A2
公开(公告)日：2013-02-28
申请号：PCT/US2012/051478
申请日：2012-08-17
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , UNIVERSITA DEGLI STUDI DI URBINO "Carlo Bo" , UNIVERSITA DEGLI STUDI DI PARMA , PIOMELLI, Daniele , MORENO-SANZ, Guillermo , BANDIERA, Tiziano , MOR, Marco , TARZIA, Giorgio
发明人： PIOMELLI, Daniele , MORENO-SANZ, Guillermo , BANDIERA, Tiziano , MOR, Marco , TARZIA, Giorgio
IPC分类号： C07C233/06 , C07C233/23 , C07D309/14 , A61K31/165 , A61P29/00
CPC分类号： C07C271/56 , C07C269/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D309/14
摘要： The present invention provides methods of making and using peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH). The present invention provides compounds and compositions that suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). The present invention also sets forth methods for inhibiting FAAH as well as methods for treating conditions such as, but not limited to, pain, inflammation, immune disorders, dermatitis, mucositis, the over reactivity of peripheral sensory neurons, neurodermatitis, and an overactive bladder. Accordingly, the invention also provides compounds, methods, and pharmaceutical compositions for treating conditions in which the selective inhibition of peripheral FAAH (as opposed to CNS FAAH) would be of benefit.
摘要翻译：本发明提供制备和使用脂肪酸酰胺水解酶（FAAH）的外周限制性抑制剂的方法。本发明提供抑制FAAH活性并增加中枢神经系统（CNS）外的anandamide水平的化合物和组合物。本发明还提出了抑制FAAH的方法以及用于治疗诸如但不限于疼痛，炎症，免疫病症，皮炎，粘膜炎，外周感觉神经元的过度反应性，神经性皮炎和膀胱过动症的病症的方法。因此，本发明还提供了用于治疗其中外周FAAH的选择性抑制（与CNS FAAH相反）会有益的病症的化合物，方法和药物组合物。

14. 发明申请

WO2012015704A2 PERIPHERALLY RESTRICTED FAAH INHIBITORS 审中-公开
标题翻译：外用限制性FAAH抑制剂
公开(公告)号：WO2012015704A2
公开(公告)日：2012-02-02
申请号：PCT/US2011045114
申请日：2011-07-22
申请人： UNIV CALIFORNIA , UNI DEGLI STUDI DI URBINO CARLO BO , UNIV PARMA , PIOMELLI DANIELE , CLAPPER JASON R , MORENO-SANZ GUILLERMO , DURANTI ANDREA , TONTINI ANDREA , MOR MARCO , TARZIA GIORGIO
发明人： PIOMELLI DANIELE , CLAPPER JASON R , MORENO-SANZ GUILLERMO , DURANTI ANDREA , TONTINI ANDREA , MOR MARCO , TARZIA GIORGIO
IPC分类号： C07C271/56 , A61K31/27 , A61P29/00 , A61P37/00
CPC分类号： C07C271/56 , C07C2601/14
摘要： Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.
摘要翻译：提供脂肪酸酰胺水解酶（FAAH）的外周限制性抑制剂。该化合物可以抑制FAAH活性，并增加中枢神经系统（CNS）外的氨基酰胺水平。尽管它们相对不能进入脑和脊髓，但化合物减弱了指示炎症和周围神经损伤的啮齿动物模型中的持续疼痛的行为反应，并且抑制了牵连伤害性处理的脊髓区域中的有害刺激诱发的神经元激活。 CBi受体阻断防止这些影响。因此，本发明还提供了用于治疗其中外周FAAH的抑制将是有益的病症的方法和药物组合物。本发明的化合物是根据式（I）：其中R 1是极性基团。在一些实施方案中，R 1选自羟基及其生理上可水解的酯。 R2和R3独立地选自氢和取代或未取代的烃基; 每个R 4独立地选自卤素和取代或未取代的烃基，n是0至4的整数; 每个R 5独立地选自卤素和取代或未取代的烃基，m是0-3的整数; 并且R 6是取代或未取代的环己基; 及其药学上可接受的盐。

15. 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。

16. 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。

17. 发明申请

WO2004033422A2 MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS 审中-公开
标题翻译：丙二酰胺水解后阻塞的焦虑调节
公开(公告)号：WO2004033422A2
公开(公告)日：2004-04-22
申请号：PCT/US2003/031844
申请日：2003-10-07
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Georgio
发明人： PIOMELLI, Daniele , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Georgio
IPC分类号： C07D
CPC分类号： C07C311/29 , C07C271/56 , C07C275/54 , C07C2601/14 , C07D209/08 , C07D211/06 , C07D215/06 , C07D307/79 , C07D487/04
摘要： Fatty acid amide hydrolase inhibitors of the Formula (I) are provided, wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that, if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N -heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula (I) and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.
摘要翻译：提供了式（I）的脂肪酸酰胺水解酶抑制剂，其中X是NH，CH 2，O或S; Q是O或S; Z是O或N; R是选自取代或未取代的芳基; 取代或未取代的联苯基，取代或未取代的萘基和取代或未取代的苯基; 取代或未取代的三联苯基; 取代或未取代的环烷基，杂芳基或烷基; 且R 1和R 2独立地选自H，取代或未取代的烷基，取代或未取代的杂烷基和取代或未取代的苯基，取代或未取代的联苯基，取代或未取代的芳基和取代或未取代的杂芳基; 条件是如果Z是O，则R 1和R 2中的一个不存在，并且如果Z是N，则任选地R 1 1 和R 2'可以任选地一起形成取代或未取代的N - 杂环或取代或未取代的与它们各自连接的N原子相连的杂芳基。提供了包含式（I）化合物的药物组合物和使用它们抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及神经和心理障碍，包括焦虑症，癫痫和抑郁症的方法。

18. 发明申请

WO2012167133A3 INHIBITORS OF ANANDAMIDE TRANSPORT AND THEIR THERAPEUTIC USES 审中-公开
标题翻译： ANANDAMIDE运输的抑制剂及其治疗用途
公开(公告)号：WO2012167133A3
公开(公告)日：2013-05-10
申请号：PCT/US2012040531
申请日：2012-06-01
申请人： UNIV CALIFORNIA , IIT ISTITUTO ITALIANO DI TECNOLOGIA , PIOMELLI DANIELE , FU JIN , BOTTEGONI GIOVANNI , CAVALLI ANDREA , BANDIERA TIZIANO
发明人： PIOMELLI DANIELE , FU JIN , BOTTEGONI GIOVANNI , CAVALLI ANDREA , BANDIERA TIZIANO
IPC分类号： A61K31/502 , A61K31/495 , A61P25/00 , A61P29/00
CPC分类号： C07D237/34 , A61K31/495 , A61K31/502 , C07K14/435 , C12N15/11 , G01N33/5008
摘要： Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.
摘要翻译：提供了对应于FLAT，细胞内anandamide降解酶的部分胞质变体，脂肪酸酰胺水解酶-1（FAAH-1）的核酸和多肽序列。 FLAT没有酰胺酶活性，但是结合内源性抗生素Aandamide并促进其转运到细胞中。鉴定了用于抑制anandamide转运的化学支架。本发明的组合物在体外阻止氨酰胺内化，在体内中断anandamide失活，并在炎性疼痛的小鼠模型中引起严重的CB1大麻素受体介导的镇痛。因此，本发明还提供了用于治疗其中调节anandamide转运有益的病症的方法和药物组合物。

19. 发明申请

WO2012167133A2 INHIBITORS OF ANANDAMIDE TRANSPORT AND THEIR THERAPEUTIC USES 审中-公开
标题翻译： ANANDAMIDE运输的抑制剂及其治疗用途
公开(公告)号：WO2012167133A2
公开(公告)日：2012-12-06
申请号：PCT/US2012/040531
申请日：2012-06-01
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , IIT - ISTITUTO ITALIANO DI TECNOLOGIA , PIOMELLI, Daniele , FU, Jin , BOTTEGONI, Giovanni , CAVALLI, Andrea , BANDIERA, Tiziano
发明人： PIOMELLI, Daniele , FU, Jin , BOTTEGONI, Giovanni , CAVALLI, Andrea , BANDIERA, Tiziano
IPC分类号： A61K31/502 , A61K31/495 , A61P29/00 , A61P25/00
CPC分类号： C07D237/34 , A61K31/495 , A61K31/502 , C07K14/435 , C12N15/11 , G01N33/5008
摘要： Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.
摘要翻译：提供了对应于FLAT，细胞内anandamide降解酶的部分胞质变体，脂肪酸酰胺水解酶-1（FAAH-1）的核酸和多肽序列。 FLAT没有酰胺酶活性，但是结合内源性抗生素Aandamide并促进其转运到细胞中。鉴定了用于抑制anandamide转运的化学支架。本发明的组合物在体外阻止氨酰胺内化，在体内中断anandamide失活，并在炎症性疼痛的小鼠模型中引起严重的CB1大麻素受体介导的镇痛。因此，本发明还提供了用于治疗其中调节anandamide转运有益的病症的方法和药物组合物。

20. 发明申请

WO2012015704A3 PERIPHERALLY RESTRICTED FAAH INHIBITORS 审中-公开
公开(公告)号：WO2012015704A3
公开(公告)日：2012-02-02
申请号：PCT/US2011/045114
申请日：2011-07-22
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , UNIVERSITA DEGLI STUDI DI URBINO "CARLO BO" , UNIVERSITA DEGLI STUDI DI PARMA , PIOMELLI, Daniele , CLAPPER, Jason, R. , MORENO-SANZ, Guillermo , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Giorgio
发明人： PIOMELLI, Daniele , CLAPPER, Jason, R. , MORENO-SANZ, Guillermo , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Giorgio
IPC分类号： C07C271/56 , A61K31/27 , A61P29/00 , A61P37/00
摘要： Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R 1 is a polar group. In some embodiments, R 1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R 2 and R 3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R 4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R 5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R 6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.

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