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1. 发明申请

WO2009049238A1 COMPOSITIONS AND METHODS OF INHIBITING N-ACYLETHANOLAMINE-HYDROLYZING ACID AMIDASE 审中-公开
标题翻译：抑制N-乙酰氨基 - 羟基丙酸酰胺酶的组合物和方法
公开(公告)号：WO2009049238A1
公开(公告)日：2009-04-16
申请号：PCT/US2008/079621
申请日：2008-10-10
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , TARZIA, Giorgio , MOR, Marco , DURANTI, Andrea , TONTINI, Andrea
发明人： PIOMELLI, Daniele , TARZIA, Giorgio , MOR, Marco , DURANTI, Andrea , TONTINI, Andrea
IPC分类号： A61K8/00 , A61K8/18 , A61Q5/00
CPC分类号： A61K31/337 , A61K31/165 , A61K31/195 , A61K31/365 , C07D305/10
摘要： Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.
摘要翻译：预期化合物和药物组合物可抑制N-酰基 - 乙醇胺水解酸酰胺酶（NAAA），从而增加NAAA，棕榈酰乙醇酰胺（PEA）底物的浓度。 NAAA抑制被认为有效减轻与降低浓度的PEA有关的病症。除其他用途之外，各种NAAA抑制剂被特别考虑作为治疗炎性疾病的治疗剂。

2. 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。

3. 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。

4. 发明申请

WO2006116773A3 METHODS, COMPOSITIONS, AND COMPOUNDS FOR MODULATION OF MONOACYLGLYCEROL LIPASE, PAIN, AND STRESS-RELATED DISORDERS 审中-公开
公开(公告)号：WO2006116773A3
公开(公告)日：2006-11-02
申请号：PCT/US2006/016843
申请日：2006-04-26
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , THE UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. , UNIVERSITA DEGLI STUDI DI URBINO , UNIVERSITA DEGLI STUDI DI PARMA , PIOMELLI, Daniele , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Giorgio , HOHMANN, Andrea
发明人： PIOMELLI, Daniele , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Giorgio , HOHMANN, Andrea
IPC分类号： A01N47/10 , A01N47/06 , A61K31/27 , A61K31/265
摘要： Methods, compositions, and compounds for inhibiting monoacyglycerol lipase, and for treating pain, for modulating stress-induced analgesia or for treating stress-induced disorders in mammals are provided.

5. 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.

6. 发明申请

WO2006116773A2 METHODS, COMPOSITIONS, AND COMPOUNDS FOR MODULATION OF MONOACYLGLYCEROL LIPASE, PAIN, AND STRESS-RELATED DISORDERS 审中-公开
标题翻译：方法，组合物和化合物用于调节单糖胆碱脂质，疼痛和压力相关疾病
公开(公告)号：WO2006116773A2
公开(公告)日：2006-11-02
申请号：PCT/US2006016843
申请日：2006-04-26
申请人： UNIV CALIFORNIA , UNIV GEORGIA RES FOUND , UNIV DEGLI STUDI URBINO , UNIV PARMA , PIOMELLI DANIELE , DURANTI ANDREA , TONTINI ANDREA , MOR MARCO , TARZIA GIORGIO , HOHMANN ANDREA
发明人： PIOMELLI DANIELE , DURANTI ANDREA , TONTINI ANDREA , MOR MARCO , TARZIA GIORGIO , HOHMANN ANDREA
IPC分类号： A61K31/4025
CPC分类号： A61K31/17
摘要： Methods, compositions, and compounds for inhibiting monoacyglycerol lipase, and for treating pain, for modulating stress-induced analgesia or for treating stress-induced disorders in mammals are provided.
摘要翻译：提供了用于抑制单甘油脂肪酶和用于治疗疼痛，调节应激诱发的镇痛或用于治疗哺乳动物中的应激诱导的疾病的方法，组合物和化合物。

7. 发明申请

WO2004033422A3 MODULATION OF ANXIETY THROUGH BLOCKADE OF ANANDAMIDE HYDROLYSIS 审中-公开
标题翻译：通过水杨苷水解的片段调节
公开(公告)号：WO2004033422A3
公开(公告)日：2004-07-29
申请号：PCT/US0331844
申请日：2003-10-07
申请人： UNIV 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： C07C271/00 , C07C271/56 , C07C275/54 , C07C311/29 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , A61K31/21
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, CH2, 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 R1 and R2 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 R1 and R2 is absent, and that, if Z is N, optionally R1 and R2 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的芳族部分; 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; 并且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，则不存在R 1和R 2中的一个，并且如果Z是N，则任选地R 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杂芳基，其中它们各自连接的N原子。提供了包含式（I）化合物的药物组合物及其用于抑制FAAH和/或治疗食欲障碍，青光眼，疼痛，失眠以及包括焦虑障碍，癫痫和抑郁症在内的神经和心理障碍的方法。

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