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1. 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.

2. 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.

3. 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。

4. 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。

5. 发明申请

WO2007079593A1 NOVEL ELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES 审中-公开
标题翻译：具有抗静电活性的新型ELATONIN配体，如睡眠诱导性质
公开(公告)号：WO2007079593A1
公开(公告)日：2007-07-19
申请号：PCT/CA2007/000055
申请日：2007-01-12
申请人： MCGILL UNIVERSITY , UNIVERSITA DEGLI STUDI DI PARMA , UNIVERSITA DEGLI STUDI DI MILANO , UNIVERSITA DEGLI STUDI DI URBINO , GOBBI, Gabriella , MOR, Marco , RIVARA, Silvia , FRASCHINI, Franco , TARZIA, Giorgio , BEDINI, Annalida , SPADONI, Gilberto , LUCINI, Valeria
发明人： GOBBI, Gabriella , MOR, Marco , RIVARA, Silvia , FRASCHINI, Franco , TARZIA, Giorgio , BEDINI, Annalida , SPADONI, Gilberto , LUCINI, Valeria
IPC分类号： C07C237/04 , A61P25/00 , A61P25/24
CPC分类号： C07C233/43 , C07C233/36
摘要： Novel melatonin ligands of Formula (I) or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1 , 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR 8 ;Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C r C 6 alkyl, C 3 -C 6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, -OCF 3 , CF 3 , C 1 -C 8 alkyl, C 1 C 8 alkyloxy, C 1 C 8 alkylthio, halogen and -Z-(CH 2 ) P -A; R 1 is selected from the group consisting of C 1 C 4 alkyl, C 3 -C 6 cycloalkyl, CF 3 , hydroxy-substituted C 1 C 4 alkyl, hydroxy-substituted C 3 -C 6 cycloalkyl, and NHR 5 , wherein R 5 is C 1 C 3 alkyl or C 3 -C 6 cycloalkyl; R 2 is selected from the group consisting of: hydrogen, C 1 C 4 alkyl, C 1 C 4 alkyloxy, OCF 3 , CF 3 , hydroxyl, and halogen; R 3 is selected from the group consisting of hydrogen, C 1 C 4 alkyl, C 1 C 4 alkyloxy, OCF 3 , CF 3 , hydroxyl, and halogen; R and R 3 may be connected together to form an -0-(CH 2 ) v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R 4 is selected from the group consisting of hydrogen, C 1 C 4 alkyl, C 1 C 4 alkyloxy, OCF 3 , CF 3 , hydroxyl, and halogen; R 6 is selected from the group consisting of hydrogen and C 1 C 6 alkyl; R 7 is selected from the group consisting of hydrogen, C 1 C 4 alkyl, C 1 C 4 alkyloxy, OCF 3 , CF 3 , hydroxyl, and halogen; and R 8 is selected from the group consisting of hydrogen and C 1 C 4 alkyl.
摘要翻译：式（I）的新型褪黑素配体或其药学上可接受的盐，其中：n为1或2; m为0,1或2; p为0,1,2,3,4,5,6,7或8; v为2或3; A是芳基或杂芳基; Z是O，S或NR 8; Y选自氢，芳基，杂芳基，C 1 -C 6烷基， C 3 -C 6环烷基，R选自氢，羟基，-OCF 3，CF 3 C 1 -C 8烷基，C 1 -C 8烷氧基，C 1 -C 6烷基，C 1 -C 8烷基，烷基硫基，卤素和-Z-（CH 2 CH 2） - ， - N - ， - R 1选自C 1 -C 4烷基，C 3 -C 3烷基，C 1 -C 4烷基，C 3 -C 4烷基， 6个环烷基，CF 3，羟基取代的C 1 -C 4烷基，羟基取代的C 3， C 1 -C 6环烷基和NHR 5，其中R 5是C 1 -C 3 C 1 -C 6烷基或C 3 -C 6环烷基; R 2选自：氢，C 1 -C 4烷基，C 1 -C 4烷基，烷基氧基，OCF 3，CF 3，羟基和卤素; R 3 3选自氢，C 1 -C 4烷基，C 1 -C 4亚烷基烷氧基，OCF 3，CF 3，羟基和卤素; R和R 3可以连接在一起以形成与它们所在的碳原子一起表示的-O-（CH 2 CH 2）连接5或6元杂环系统; R 4选自氢，C 1 -C 4烷基，C 1 -C 4亚烷基烷氧基，OCF 3，CF 3，羟基和卤素; R 6选自氢和C 1 -C 6烷基; R 6选自氢和C 1 -C 6烷基; R 7选自氢，C 1 -C 4烷基，C 1 -C 3亚烷基烷氧基，OCF 3，CF 3，羟基和卤素; 和R 8选自氢和C 1 -C 4烷基。

6. 发明申请

WO2014144547A3 AMIDE DERIVATIVES OF LACTAM BASED N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) INHIBITORS 审中-公开
公开(公告)号：WO2014144547A3
公开(公告)日：2014-09-18
申请号：PCT/US2014/029007
申请日：2014-03-14
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , UNIVERSITA DEGLI STUDI DI URBINO "CARLO BO" , FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , UNIVERSITA DEGLI STUDI DI PARMA
发明人： PIOMELLI, Daniele , MOR, Marco , TARZIA, Giorgio , BERTOZZI, Fabio , NUZZI, Andrea , FIASELLA, Annalisa , BANDIERA, Tiziano , REGGIANI, Angelo Mario
IPC分类号： A61K31/397
摘要： Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

7. 发明申请

WO2013078430A1 DISUBSTITUTED BETA-LACTONES AS INHIBITORS OF N-ACYLETHANOLAMINE ACID AMIDASE (NAAA) 审中-公开
标题翻译：作为N-乙酰氨基磺酸氨基酸酶（NAAA）的抑制剂的分离的试剂
公开(公告)号：WO2013078430A1
公开(公告)日：2013-05-30
申请号：PCT/US2012/066421
申请日：2012-11-21
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , IIT - ISTITUTO ITALIANO DI TECNOLOGIA , UNIVERSITY DEGLI STUDI DI URBINO , UNIVERSITA DEGLI STUDI DI PARMA
发明人： PIOMELLI, Daniele , BANDIERA, Tiziano , MOR, Marco , TARZIA, Giorgio , BERTOZZI, Fabio , PONZANO, Stefano
IPC分类号： A61K31/337 , A61K31/38 , A61P29/00 , A61P17/00
CPC分类号： A61K31/365 , A61K9/0014 , A61K31/38 , C07D305/12 , C07D405/12 , C07D407/12 , C07D409/12
摘要： The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.
摘要翻译：本发明提供用于抑制N-酰基乙醇胺酸酰胺酶（NAAA）的化合物和药物组合物。 NAAA的抑制被认为是在特征为浓度降低的PEA和OEA的条件下维持棕榈酰乙醇酰胺（PEA）和油基乙醇酰胺（OEA），NAAA的两种底物的水平的方法。本发明还提供了治疗炎症性疾病和疼痛的方法以及其中PEA和OEA水平降低与病症相关的其它病症。

8. 发明申请

WO2003011864A1 DERIVATIVES OF TRIAZOLYL-IMIDAZOPYRIDINE AND OF THE TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2a RECEPTOR AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：作为腺苷A2a受体的配体及其作为药物使用的三唑并咪唑并噻唑啉的衍生物有用
公开(公告)号：WO2003011864A1
公开(公告)日：2003-02-13
申请号：PCT/IT2002/000489
申请日：2002-07-25
申请人： SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A. , TARZIA, Giorgio , PIERSANTI, Giovanni , MINETTI, Patrizia , DI CESARE, Maria, Assunta , GALLO, Grazia , GIORGI, Fabrizio , GIORGI, Luca
发明人： TARZIA, Giorgio , PIERSANTI, Giovanni , MINETTI, Patrizia , DI CESARE, Maria, Assunta , GALLO, Grazia , GIORGI, Fabrizio , GIORGI, Luca
IPC分类号： C07D473/34
CPC分类号： C07D471/04 , A61K31/198 , A61K31/435 , A61K31/52 , C07D473/34 , A61K2300/00
摘要： Compounds of formula (I) wherein the groups are as defined in the description, said compounds being antagonists of the adenosine A 2a receptor and useful as medicaments, in particular for the treatment of Parkinson's disease are disclosed.
摘要翻译：公开了式（I）化合物，其中基团如说明书中所定义，所述化合物是腺苷A2a受体的拮抗剂，可用作药物，特别是用于治疗帕金森病。

9. 发明申请

WO2003000252A1 5-HALO-TRYPTAMINE DERIVATIVES USED AS LIGANDS OF THE 5-HT6 AND/OR 5-HT7 SEROTONIN RECEPTORS 审中-公开
标题翻译：用作5-HT6和/或5-HT7丝氨酸受体的配体的5-羟基喹啉衍生物
公开(公告)号：WO2003000252A1
公开(公告)日：2003-01-03
申请号：PCT/IT2002/000398
申请日：2002-06-17
申请人： SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A. , DI CESARE, Maria, Assunta , MINETTI, Patrizia , TARZIA, Giorgio , SPADONI, Gilberto
发明人： DI CESARE, Maria, Assunta , MINETTI, Patrizia , TARZIA, Giorgio , SPADONI, Gilberto
IPC分类号： A61K31/405
CPC分类号： C07D209/16 , A61K31/405
摘要： Compounds of Formula (I): (I); wherein: R 1 and R 2 either the same or different, are H or linear or branched C 1 -C 6 alkyl; R 3 = linear or branched C 1 -C 6 alkyl; R 4 = halogen, and pharmaceutically acceptable salts thereof are useful as active ingredients in the preparation of medicaments used as ligands of the 5-HT 6 and/or 5-HT 7 serotoninergic receptors.
摘要翻译：式（I）的化合物：（I）; 其中：R 1和R 2相同或不同，为H或直链或支链C 1 -C 6烷基; R3 =直链或支链C1-C6烷基; R4 =卤素及其药学上可接受的盐可用作制备用作5-HT6和/或5-HT7血清素能受体的配体的药物的活性成分。

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