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1. 发明申请

US20130217764A1 PERIPHERALLY RESTRICTED FAAH INHIBITORS 有权
标题翻译：外用限制性FAAH抑制剂
公开(公告)号：US20130217764A1
公开(公告)日：2013-08-22
申请号：US13812777
申请日：2011-07-22
申请人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Todd A. Ostomel
发明人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Todd A. Ostomel
IPC分类号： C07C271/56
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，并且抑制了与伤害性处理相关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。本发明的化合物根据式（I）：其中R1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。

2. 发明授权

US09187413B2 Peripherally restricted FAAH inhibitors 有权
标题翻译：外周限制的FAAH抑制剂
公开(公告)号：US09187413B2
公开(公告)日：2015-11-17
申请号：US13812777
申请日：2011-07-22
申请人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Giovanna Guiducci , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Jason R. Clapper , Guillermo Moreno-Sanz , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： C07C233/00 , A61K31/265 , A61K31/16 , A61K31/165 , C07C271/56
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，并且抑制了与伤害性处理相关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。本发明的化合物根据式（I）：其中R1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

US20120010283A1 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：US20120010283A1
公开(公告)日：2012-01-12
申请号：US13211219
申请日：2011-08-16
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： A61K31/27 , C07C255/60 , A61P27/06 , A61P25/04 , A61P25/22 , A61P25/08 , A61P25/18 , C07C271/56 , A61P25/24
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: 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：提供了下式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之一，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-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。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。

4. 发明授权

US08003693B2 Modulation of anxiety through blockade of anandamide hydrolysis 有权
标题翻译：通过封闭anandamide水解调节焦虑
公开(公告)号：US08003693B2
公开(公告)日：2011-08-23
申请号：US11496051
申请日：2006-07-28
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： A61K31/27
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: 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：提供了下式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之一，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-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。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。

5. 发明申请

US20090082435A1 Methods, Compositions, And Compounds For Modulation Of Monoacylglycerol Lipase, Pain, And Stress-Related Disorders 审中-公开
标题翻译：用于调节单酰甘油脂肪酶，疼痛和应激相关疾病的方法，组合物和化合物
公开(公告)号：US20090082435A1
公开(公告)日：2009-03-26
申请号：US11912386
申请日：2006-04-26
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Andrea Hohmann
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia , Andrea Hohmann
IPC分类号： A61K31/27 , C12Q1/44 , C07C271/02 , C12N9/18 , A61P29/00
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，调节应激诱导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。

6. 发明授权

US07176201B2 Modulation of anxiety through blockade of anandamide hydrolysis 有权
标题翻译：通过封闭anandamide水解调节焦虑
公开(公告)号：US07176201B2
公开(公告)日：2007-02-13
申请号：US10681858
申请日：2003-10-07
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： A61K31/5355 , A61K31/445 , C07C271/56 , C07C255/59 , C07C271/44 , C07D265/30
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: 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：提供下式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; 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' 和R 2可以任选地一起形成取代或未取代的N-杂环或具有与它们各自连接的N原子的取代或未取代的杂芳基。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。

7. 发明申请

US20100311711A1 Inhibitors of NAAA and Methods Thereof 审中-公开
标题翻译： NAAA的抑制剂及其方法
公开(公告)号：US20100311711A1
公开(公告)日：2010-12-09
申请号：US12678060
申请日：2008-10-10
申请人： Daniele Piomelli , Giorgio Tarzia , Marco Mor , Andrea Duranti , Andrea Tontini
发明人： Daniele Piomelli , Giorgio Tarzia , Marco Mor , Andrea Duranti , Andrea Tontini
IPC分类号： A61K31/397 , C12N9/99 , A61K31/337 , A61K31/38 , A61K31/382 , A61K31/381 , A61K31/35 , A61K31/34 , A61K31/44 , A61K31/40 , A61P25/00
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。

8. 发明申请

US20090048337A1 Modulation of anxiety through blockade of anandamide hydrolysis 有权
标题翻译：通过封闭anandamide水解调节焦虑
公开(公告)号：US20090048337A1
公开(公告)日：2009-02-19
申请号：US11496051
申请日：2006-07-28
申请人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
发明人： Daniele Piomelli , Andrea Duranti , Andrea Tontini , Marco Mor , Giorgio Tarzia
IPC分类号： A61K31/27 , C07C271/56
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之一，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-杂环或具有取代或未取代的杂芳基，其中N 它们各自附着的原子。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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