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1. 发明申请

WO2017076932A1 INDOLIN-2-ONE DERIVATIVES USEFUL IN THE TREATMENT OF CNS DISEASES 审中-公开
标题翻译：吲哚啉-2-酮衍生物用于治疗中枢神经系统疾病
公开(公告)号：WO2017076932A1
公开(公告)日：2017-05-11
申请号：PCT/EP2016/076473
申请日：2016-11-03
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GAUFRETEAU, Delphine , HILPERT, Hans , HUMM, Roland , KOLCZEWSKI, Sabine , MUSER, Thorsten , PLANCHER, Jean-Marc , STOLL, Theodor
IPC分类号： C07D401/14 , A61K31/404 , A61K31/44 , A61K31/506 , C07D403/14 , C07D409/14 , A61P25/00 , A61P25/18
CPC分类号： C07D409/14 , A61K31/404 , A61K31/44 , A61K31/506 , C07D401/14 , C07D403/14
摘要： The present invention is concerned with indolin-2-one derivatives of general formula (I) wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from (II) R 1 is S(0)2lower alkyl, S(0)2NR 4 R 5 , S(0) 2 cycloalkyl, S-lower alkyl or S(0) 2 -azetidin-l-yl; R 4 and R 5 are independently from each other hydrogen, lower alkyl or (CH 2)2 OCH 3 ; or the group A-R 1 may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from (III) R 2 is hydrogen or cycloalkyl; R 3 is methyl or halogen; n is 1 or 2; X is N, N + 0" or CH; --- the dotted line may be nothing or -CH 2 -; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive- compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co- morbid epilepsy.
摘要翻译：本发明涉及通式（I）的吲哚啉-2-酮衍生物，其中A是苯基或含有一个或两个N原子的六元杂芳基，其选自（II）R 1是S（O）2低级烷基，S（O）2 NR 4 R 5，S（O）2 环烷基，S-低级烷基或S（O）2 - 杂环丁烷-1-基; R 4和R 5彼此独立地为氢，低级烷基或（CH 2）2 OCH 3， ; 或基团A-R 1可与来自基团A的两个相邻碳原子一起形成另外的选自（III）R 2的稠合环为氢或环烷基; R 3是甲基或卤素; n是1或2; X是N，N“+ 0” 或CH; ---虚线可能是空的或-CH 2 = - ; 以及其药学上可接受的盐与外消旋混合物或其相应的对映异构体和/或光学异构体和/或立体异构体。这些化合物可用于治疗与精神分裂症阳性（精神病）和阴性症状，药物滥用，酒精和药物成瘾，强迫症，认知障碍，双相性精神障碍，心境障碍，重性抑郁症，治疗耐药抑郁症，焦虑症，阿尔茨海默病，自闭症，帕金森病，慢性疼痛，边缘型人格障碍，神经退行性疾病，睡眠障碍，慢性疲劳综合征，僵硬，炎性疾病，哮喘，亨廷顿病，ADHD，肌萎缩性侧索硬化，自身免疫性疾病，病毒和真菌感染，心血管疾病，眼科和炎症性视网膜疾病和平衡问题，癫痫和神经发育障碍与合并症的癫痫。

2. 发明申请

WO2017076842A1 INDOLIN-2-ONE DERIVATIVES 审中-公开
标题翻译：吲哚啉-2-酮衍生物
公开(公告)号：WO2017076842A1
公开(公告)日：2017-05-11
申请号：PCT/EP2016/076315
申请日：2016-11-02
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GAUFRETEAU, Delphine , KOLCZEWSKI, Sabine , PLANCHER, Jean-Marc , STOLL, Theodor
IPC分类号： C07D403/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/08 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , A61K31/403 , A61P25/00 , A61P27/02 , A61P37/00 , A61P31/00 , A61P9/00
CPC分类号： C07D403/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/08
摘要： The present invention is concerned with indolin-2-one derivatives of general formula (I) wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.
摘要翻译：本发明涉及通式（I）的二氢吲哚-2-酮衍生物，其中取代基如权利要求1中所定义。所述化合物可用于治疗与正精神病）以及精神分裂症，物质滥用，酒精和药物成瘾，强迫症，认知障碍，双相性精神障碍，情绪障碍，重性抑郁症，治疗抵抗性抑郁症，焦虑症，阿尔茨海默病，孤独症，帕金森病，慢性疼痛，边缘型人格障碍，神经退行性疾病，睡眠障碍，慢性疲劳综合症，僵硬，炎性疾病，哮喘，亨廷顿病，ADHD，肌萎缩性侧索硬化，关节炎，自身免疫病，病毒和真菌感染，心血管疾病，眼科和炎性视网膜疾病和平衡问题，癫痫和伴发病癫痫的神经发育障碍。

3. 发明申请

WO2014202493A1 INDOLIN-2-ONE OR PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE DERIVATIVES 审中-公开
标题翻译：吲哚-2-酮或吡咯并吡啶/吡啶-2-酮衍生物
公开(公告)号：WO2014202493A1
公开(公告)日：2014-12-24
申请号：PCT/EP2014/062491
申请日：2014-06-16
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： BRUNNER, Daniela , HILPERT, Hans , KOLCZEWSKI, Sabine , LIMBERG, Anja , MALBERG, Jessica , PRINSSEN, Eric , RIEMER, Claus , SHANKAR, Bavani G. , STOLL, Theodor
IPC分类号： C07D405/14 , C07D413/14 , C07D401/04 , C07D403/04 , C07D413/04 , C07H19/044 , C07D417/04 , C07D471/04 , C07D487/04 , C07D498/04 , A61P25/00 , A61K31/44 , A61K31/4409 , A61K31/4406 , A61K31/4402
CPC分类号： A61K31/4439 , A61K31/19 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/437 , A61K31/438 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/5383 , A61K31/55 , A61K31/7064 , A61K45/06 , C07C53/06 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D498/04 , C07H19/044
摘要： The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R 1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF 3 , (CH 2 ) o -lower alkoxy, cycloalkyl optionally substituted by CF 3 , or heterocycloalkyl optionally substituted by lower alkyl; R 2 is hydrogen, lower alkyl, (CH 2 ) o -cycloalkyl, (CH 2 ) o -O-cycloalkyl, (CH 2 ) o -lower alkoxy, CH 2 ) o -lower alkoxy substituted by halogen, (CH 2 ) o -heterocycloalkyl optionally substituted by lower alkyl, (CH 2 ) o -S(O) 2 -cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH 2 ) o -S(O) 2 -lower alkyl, lower alkyl substituted by halogen or CH 2 CH(OH)CF 3 ; R 3 is halogen or lower alkyl; X is CH or N; X 1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.
摘要翻译：本发明涉及通式（I）的2-氧代-2,3-二氢 - 吲哚，其中Ar是含有一个，两个或三个选自N，S或O的杂原子的杂芳基; R 1是氢，低级烷基，卤素，氨基，二甲基氨基，氰基，被卤素取代的低级烷基，被羟基取代的低级烷基，CH（OH）CF 3，（CH 2）O-低级烷氧基，任选被CF 3取代的环烷基或任选地被低级烷基取代; R2是氢，低级烷基，（CH2）O-环烷基，（CH2）O-环烷基，（CH2）O-低级烷氧基，CH2）被卤素取代的-O-低级烷氧基，任选被低级烷基取代的（CH 2），（CH 2）oS（O）2-环烷基，被一个或两个羟基取代的低级烷基，被一个或两个低级烷氧基取代的低级烷基，（CH 2）o S（O）2-低级烷基，被卤素或CH 2 CH （OH）CF 3; R3是卤素或低级烷基; X是CH或N; X1是CH或N; n为1或2; o为0,1,2或3; m为0,1或2; 虚线是不是一个债券; 以及其药学上可接受的盐与外消旋混合物或其相应的对映异构体和/或光学异构体和/或立体异构体。该化合物可用于治疗某些中性神经系统疾病，其为阳性（精神病）精神分裂症，药物滥用，酒精和药物成瘾，强迫症，认知障碍，双相情感障碍，情绪障碍，重症抑郁症，耐药性抑郁症，焦虑症，阿尔茨海默病，孤独症，帕金森病，慢性疼痛，边界线人格障碍，睡眠障碍，慢性疲劳综合征，僵硬，关节炎中的抗炎作用和平衡问题。

4. 发明申请

WO2009109491A1 2-AMINOQUINOLINE DERIVATIVES 审中-公开
标题翻译： 2-氨基喹啉衍生物
公开(公告)号：WO2009109491A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052193
申请日：2009-02-25
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
发明人： KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
IPC分类号： C07D215/38 , C07D215/48 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , A61K31/47 , A61K31/4709 , A61P25/30 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/14
CPC分类号： C07D215/38 , C07D215/48 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12
摘要： The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT 5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned'with compounds of the general Formula (I), wherein R 1 and R 2 are as described herein.
摘要翻译：本发明涉及作为5-HT5A受体拮抗剂的2-氨基喹啉衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗抑郁症，焦虑症，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，病症饮食行为，性功能障碍，睡眠障碍，滥用药物，运动障碍如帕金森病，精神病或胃肠道疾病。特别地，本发明涉及通式（I）的化合物，其中R 1和R 2如本文所述。

5. 发明申请

WO2006117305A1 (3,4-DIHYDRO-QUINAZOLIN-2-YL)-(2-ARYLOXY-ETHYL)-AMINES HAVING AN ACTIVITY ON THE 5-HT RECEPTOR 审中-公开
标题翻译：（3,4-DIHYDRO-喹唑啉-2-基） - （2-氰基乙基） - 胺在5-HT受体上具有活性
公开(公告)号：WO2006117305A1
公开(公告)日：2006-11-09
申请号：PCT/EP2006/061779
申请日：2006-04-24
申请人： F. HOFFMANN-LA ROCHE AG , ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
发明人： ALANINE, Alexander , GOBBI, Luca Claudio , KOLCZEWSKI, Sabine , LUEBBERS, Thomas , PETERS, Jens-Uwe , STEWARD, Lucinda
IPC分类号： C07D239/84 , C07D409/04 , C07D413/04 , A61K31/517 , A61P25/24 , A61P25/18
CPC分类号： C07D239/84 , A61K31/517 , C07D409/04 , C07D413/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R is hydrogen or halogen; or R 1 and R are together with the carbon atom to which they are attached -CH=CH-CH=CH-; R 2 is hydrogen, lower alkyl, phenyl optionally substituted by halogen, or is hetaryl, optionally substituted by lower alkyl; R 3 is hydrogen, lower alkyl, phenyl, benzyl, lower alkenyl, lower alkoxy, phenyloxy, benzyloxy, S-lower alkyl, halogen, CN, lower alkyl substituted by halogen or O-lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl, aryl is phenyl or naphthyl; n is 1, 2 or 3; m is 1 or 2; and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. It has been found that the compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I or a pharmaceutically acceptable salt thereof for the manufacture of medicaments for the treatment of certain CNS disorders.
摘要翻译：本发明涉及其中R 1为氢，低级烷基，低级烷氧基，卤素或被卤素取代的低级烷基的式（I）化合物; R是氢或卤素; 或R 1和R 2与它们所连接的碳原子一起-CH = CH-CH = CH-; R 2是氢，低级烷基，任选被卤素取代的苯基，或者是杂芳基，任选被低级烷基取代; R 3是氢，低级烷基，苯基，苄基，低级烯基，低级烷氧基，苯氧基，苄氧基，S-低级烷基，卤素，CN，被卤素取代的低级烷基或被卤素; R 4是氢或低级烷基，芳基是苯基或萘基; n为1,2或3; m为1或2; 和其药学上可接受的酸加成盐和互变异构体。已经发现式I化合物对5-HT5A受体具有良好的活性。因此，本发明提供式I化合物或其药学上可接受的盐在制备用于治疗某些CNS疾病的药物中的用途。

6. 发明申请

WO2005003117A1 IMIDAZOLE DERIVATIVES III 审中-公开
标题翻译：咪唑衍生物III
公开(公告)号：WO2005003117A1
公开(公告)日：2005-01-13
申请号：PCT/EP2004/007177
申请日：2004-07-01
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , CECCARELLI, Simona, Maria , JAESCHKE, Georg , KOLCZEWSKI, Sabine , PORTER, Richard, Hugh, Philip , VIEIRA, Eric
发明人： BUETTELMANN, Bernd , CECCARELLI, Simona, Maria , JAESCHKE, Georg , KOLCZEWSKI, Sabine , PORTER, Richard, Hugh, Philip , VIEIRA, Eric
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , A61K31/4178 , A61K31/4439
摘要： The present invention relates to imidazole derivatives of the general formula (I), wherein R 1 , R 2 , R 3 and R 4 are as defined in the description as well as pharmaceutically acceptable salts and processes for the preparation thereof. The invention also relates to medicaments containing said imidazole derivatives and to their use for the manufacture of medicaments for the treatment and prevention of mGluR5 receptor mediated disorders such as acute and/or chronic neurological disorders, in particular anxiety, or for the treatment of chronic and acute pain.
摘要翻译：本发明涉及通式（I）的咪唑衍生物，其中R 1，R 2，R 3和R 4如说明书中所定义，以及其药学上可接受的盐和方法其制备。本发明还涉及含有所述咪唑衍生物的药物及其制备用于治疗和预防mGluR5受体介导的疾病如急性和/或慢性神经障碍，特别是焦虑或用于治疗慢性和/或慢性神经障碍急性疼痛。

7. 发明申请

WO2011161006A1 AMIDO-TROPANE DERIVATIVES 审中-公开
标题翻译： AMIDO-TROPANE衍生物
公开(公告)号：WO2011161006A1
公开(公告)日：2011-12-29
申请号：PCT/EP2011/060073
申请日：2011-06-17
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel
IPC分类号： C07D451/02 , A61K31/46 , A61P25/00
CPC分类号： C07D451/02 , A61K9/2018 , A61K9/2054 , A61K9/4858 , A61K9/4866
摘要： The present invention relates to a compound of general formula (I) wherein R 1 , R 2 and R 3 are independently from each other hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1), and that they have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2和R 3彼此独立地为氢，低级烷基，低级烷氧基，环烷基，被卤素或S-低级烷基取代的低级烷基; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。已经发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且它们对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性。该化合物可用于治疗神经和神经精神障碍。

8. 发明申请

WO2011023667A1 CARBOCYCLIC GLYT1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CARBOCYCLIC GLYT1受体拮抗剂
公开(公告)号：WO2011023667A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062281
申请日：2010-08-24
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , PINARD, Emmanuel
发明人： KOLCZEWSKI, Sabine , PINARD, Emmanuel
IPC分类号： C07C233/79 , C07C235/62 , C07C323/62 , C07D205/04 , C07D207/06 , C07D211/08 , C07D307/06 , C07D335/02 , C07D487/10 , C07D295/135 , A61K31/166 , A61K31/397 , A61K31/40 , A61K31/4453 , A61K31/495
CPC分类号： A61K31/166 , A61K31/397 , A61K31/40 , A61K31/4453 , A61K31/495 , A61K31/5375 , C07C233/79 , C07C235/62 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/06 , C07D207/10 , C07D207/12 , C07D211/38 , C07D211/46 , C07D295/12 , C07D295/20 , C07D309/14 , C07D335/02 , C07D487/10
摘要： The present invention relates to the use of a compound of general formula (I) wherein R 1 /R 2 are independently from each other hydrogen, lower alkyl, -CH 2 ) o -cycloalkyl for o being 0 or 1, or are benzyl or heterocycloalkyl; or R 1 and R 2 are together with the N-atom to which they are attached a ring containing -(CH 2 ) 3 -, -(CH 2 ) 4 -, -(CH 2 ) 5 -, -(CH 2 ) 2 -O-(CH 2 ) 2 -, -(CH 2 ) 2 -S-(CH 2 ) 2 -, -(CH 2 ) 2 -NR-(CH 2 ) 2 -, -(CH 2 ) 2 -C(O)-(CH 2 ) 2 -, -(CH 2 ) 2 -CF 2 -(CH 2 ) 2 -, -CH 2 -CHR-(CH 2 ) 2 , -CHR-(CH 2 ) 3 , CHR-(CH 2 ) 2 -CHR-, or is the ring 2,6-diaza-spiro[3.3]heptane-2-carboxylic acid tert-butyl ester and R is hydroxy, halogen, cycloalkyl, or C(O)O-lower alkyl; X is -(CH 2 ) 4 -, -(CH 2 ) 3 -, -(CH 2 ) 2 - or -CH 2 -; R 3 is S-lower alkyl, CF 3 , OCHF 2 , lower alkoxy, lower alkyl, phenyl, cycloalkyl or halogen; R 4 is CF 3 , lower alkoxy, lower alkyl, halogen and n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers thereof for the manufacture of a medicament for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1 / R 2彼此独立地是O，O或1的氢，低级烷基，-CH 2）o - 环烷基，或者是苄基或杂环烷基; （CH 2）3 - ， - （CH 2）4 - ， - （CH 2）5 - ， - （CH 2）2 -O-（CH 2）） - ， - （CH 2）2 -S-（CH 2）2 - ， - （CH 2）2 -NR-（CH 2）2 - ， - （CH 2）2 -C（O） - （CH 2）2 -CF 2 - （CH 2）2 - ， - CH 2 -CHR-（CH 2）2，-CHR-（CH 2）3，CHR-（CH 2）2 -CHR-，或环2,6-二氮杂 - 螺[3.3]庚烷-2-羧酸叔丁酯，R是羟基，卤素，环烷基或C（O）O-低级烷基; X是 - （CH 2）4 - ， - （CH 2）3 - ， - （CH 2）2 - 或-CH 2 - ; R3是S-低级烷基，CF3，OCHF2，低级烷氧基，低级烷基，苯基，环烷基或卤素; R4为CF3，低级烷氧基，低级烷基，卤素，n为1或2; 或其药学上可接受的酸加成盐，或其相应的对映体和/或光学异构体，用于制备用于治疗精神病，疼痛，记忆功能障碍和学习，注意力缺陷，精神分裂症，痴呆症或阿尔茨海默病。

9. 发明申请

WO2009112395A1 2-AMINOQUINOLINES AS 5-HT5A RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 2-AMINOQUINOLINES作为5-HT5A受体拮抗剂
公开(公告)号：WO2009112395A1
公开(公告)日：2009-09-17
申请号：PCT/EP2009/052484
申请日：2009-03-03
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
发明人： KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
IPC分类号： A61P3/06 , A61P25/00 , A61K31/4709 , C07D215/38 , C07D405/12
CPC分类号： C07D405/12 , C07D215/38 , C07D491/08
摘要： The present invention is concerned with 2-Aminoquinoline derivatives as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders. In particular, the present invention is concerned with compounds of the general formula (I) wherein R and R are as described herein.
摘要翻译：本发明涉及作为5-HT5A受体拮抗剂的2-氨基喹啉衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗抑郁症，焦虑症，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，病症饮食行为，性功能障碍，睡眠障碍，滥用药物，运动障碍如帕金森病，精神病或胃肠道疾病。特别地，本发明涉及通式（I）的化合物，其中R和R如本文所述。

10. 发明申请

WO2009109502A1 2-AMINOQUINOLINES 审中-公开
标题翻译： 2-氨基喹啉
公开(公告)号：WO2009109502A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052253
申请日：2009-02-26
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
发明人： KOLCZEWSKI, Sabine , RIEMER, Claus , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
IPC分类号： A61P25/00 , A61K31/47 , A61K31/4709 , C07D215/38 , C07D401/04 , C07D405/12 , C07D413/04 , C07D405/14
CPC分类号： C07D215/38 , C07D401/04 , C07D401/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds of the general formula (I) wherein A, R 1 , R 2 , R 3 , R 4 , and R 5 are as described herein and the use thereof as 5-HT 5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The compounds of the general formula (I) are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中A，R 1，R 2，R 3，R 4和R 5如本文所述，及其作为5-HT 5 A受体拮抗剂的用途，其制备方法，含有它们的药物组合物及其用途作为药物。通式（I）的化合物可用于预防和/或治疗抑郁症，焦虑症，精神分裂症，恐慌症，广场恐惧症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆症饮食行为障碍，性功能障碍，睡眠障碍，滥用药物，运动障碍如帕金森病，精神病或胃肠疾病。

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