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1. 发明申请

WO2011051490A2 HETEROCYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO2011051490A2
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066584
申请日：2010-11-02
申请人： N.V. ORGANON , ADAM, Julia , GILLESPIE, Jonathan , LAATS, Steven , MACLEAN, John Kinnaird Ferguson , McARTHUR, Duncan Robert
发明人： ADAM, Julia , GILLESPIE, Jonathan , LAATS, Steven , MACLEAN, John Kinnaird Ferguson , McARTHUR, Duncan Robert
IPC分类号： C07D401/10
CPC分类号： C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D413/10
摘要： The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
摘要翻译：本发明涉及式（I）的杂环衍生物或其药学上可接受的盐或溶剂化物，其中变量如说明书中所定义。本发明进一步涉及包含所述杂环衍生物的药物组合物，并涉及它们在治疗中的应用，例如治疗或预防由谷氨酸功能障碍如精神分裂症和广泛性焦虑症所介导的障碍。

2. 发明申请

WO2008101995A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO2008101995A1
公开(公告)日：2008-08-28
申请号：PCT/EP2008/052141
申请日：2008-02-21
申请人： N.V. ORGANON , ADAM, Julia
发明人： ADAM, Julia
IPC分类号： C07D413/04 , C07D417/04 , A61K31/425 , A61K31/433 , A61K31/4245 , A61P29/00
CPC分类号： C07D417/04 , C07D413/04
摘要： The invention relates to indole derivative having the general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein X 1 , X 2 and X 3 are independently selected from N, O, S and CH;Y represents CH 2 , O, S or SO 2 ;R 1 is H, (C 1-4 )-alkyl, (C 1-4 )alkyloxy, CN orhalogen;R 2 , R 2 ', R 3 , R 3 ', R 4 ,R 4 ', R 5 and R 5 ' are independently hydrogen, (C 1-4 )alkyl (optionally substituted with OH) or CO-OR 8 ; orone pair of geminal substituents R 3 and R 3 ' or R 5 and R 5 ' together represent a keto group, and the others are all hydrogen or (C 1-4 )alkyl; or R 2 and R 5 together represent a methylene or an ethylene bridge, and R 2 '2, R 3 , R 3 ', R 4 , R 4 ' and R 5 ' are hydrogen; n is 1 or 2; R 6 is H, (C 1-4 )alkyl (optionally substituted with OH, (C 1-4 )alkyloxy, CO-NR 9 R 10 , CO-OR 11 or 1,2,4-oxadiazol-3-yl), SO 2 NR 12 R 13 or COOR 14 ; R 7 is H or halogen; R 8 is (C 1-4 )alkyl; R 9 and R 10 are independently hydrogen, (C 1-4 )alkyl or (C 3-7 )cycloalkyl, the alkyl groups being optionally substituted with OH or (C 1-4 )alkyloxy; R 11 is H or (C 1-4 )alkyl; R 12 and R 13 are independently H or (C 1-4 )alkyl; R 14 is (C 1-6 )alkyl; or a pharmaceutically acceptable salt thereof,as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式（I）的吲哚衍生物，其中A表示5元芳族杂环，其中X 1，X 2和X 3 独立地选自N，O，S和CH; Y表示CH 2，O，S或SO 2; R 1 8 ; 一对偕取代基R 3和R 3或R 5和R 5一起代表酮基基团，其余全部是氢或（C 1-4烷基）烷基; 或R 2和R 5一起表示亚甲基或乙烯桥，R 2'2，R 3

3. 发明申请

WO2008100977A2 THERAPEUTIC RELEASE AGENTS 审中-公开
标题翻译：治疗药物
公开(公告)号：WO2008100977A2
公开(公告)日：2008-08-21
申请号：PCT/US2008/053785
申请日：2008-02-13
申请人： N.V. ORGANON , DASSE, Olivier , PARROTT, Jeff, A. , PUTMAN, David , ADAM, Julia
发明人： DASSE, Olivier , PARROTT, Jeff, A. , PUTMAN, David , ADAM, Julia
IPC分类号： A61K31/27 , C07C271/56
CPC分类号： C07C271/56
摘要： Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. Esters of alkylcarbamic acids are disclosed that are inhibitors of FAAH activity. Compounds disclosed herein inhibit FAAH activity. Described herein are processes for the preparation of esters of alkylcarbamic acid compounds, compositions that include them, and methods of use thereof.
摘要翻译：脂肪酸酰胺水解酶（FAAH）活性的药理学抑制导致脂肪酸酰胺水平升高。公开了烷基氨基甲酸酯作为FAAH活性的抑制剂。本文公开的化合物抑制FAAH活性。本文描述的是制备烷基氨基甲酸化合物的酯的方法，包括它们的组合物及其使用方法。

4. 发明公开

EP2125795A1 INDOLE DERIVATIVES 有权
标题翻译：吲哚衍生物
公开(公告)号：EP2125795A1
公开(公告)日：2009-12-02
申请号：EP08709170.8
申请日：2008-02-21
申请人： N.V. Organon
发明人： ADAM, Julia
IPC分类号： C07D413/04 , C07D417/04 , A61K31/425 , A61K31/433 , A61K31/4245 , A61P29/00
CPC分类号： C07D417/04 , C07D413/04
摘要： The invention relates to indole derivative having the general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH;Y represents CH2, O, S or SO2;R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN orhalogen;R2, R2 ', R3, R3 ', R4,R4 ', R5 and R5 ' are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO-OR8; orone pair of geminal substituents R3 and R3 ' or R5 and R5 ' together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2and R5 together represent a methylene or an ethylene bridge, and R2 '2, R3, R3 ', R4, R4 ' and R5 ' are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO-NR9R10, CO-OR11or 1,2,4-oxadiazol-3-yl), SO2NR12R13or COOR14; R7 is H or halogen; R 8 is (C1-4)alkyl; R9and R10are independently hydrogen, (C1-4)alkyl or (C 3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof,as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

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