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1. 发明申请

WO2010086259A1 PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK3受体拮抗剂的哌啶衍生物
公开(公告)号：WO2010086259A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050591
申请日：2010-01-19
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/454 , A61K31/4545 , A61P25/24 , A61P25/04 , A61P25/18 , A61P25/16 , A61P25/22
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compounds of formula (I) wherein Ar 1 is aryl or a six membered heteroaryl; Ar 2 is aryl or a six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, lower alkyl, phenyl, optionally substituted by halogen, or is a five membered heteroaryl, optionally substituted by lower alkyl, or is aryl optionally substituted by halogen; is a six membered heterocyclic group, wherein X is -N(SO 2 CH 3 ); R 6 is hydrogen; Y is -N(R 7' )- R 7' is a 6-membered heteroaryl group, optionally substituted by cyano or C(O)-cycloalkyl, wherein the cycloalkyl group is optionally substituted by lower alkyl, n is 1; m is 1; o is1; p is 1; s is 0; t is 1; u is 1; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonist for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）的化合物，其中Ar 1是芳基或6元杂芳基; Ar 2是芳基或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基; R4是氢，低级烷基，任选被卤素取代的苯基，或是任选被低级烷基取代的五元杂芳基，或者是被卤素任意取代的芳基; 是六元杂环基，其中X是-N（SO 2 CH 3）; R6是氢; Y是-N（R 7'）-R 7'是任选被氰基或C（O） - 环烷基取代的6元杂芳基，其中环烷基任选被低级烷基取代，n是1; m为1; o is1; p为1; s是0; t为1; 你是1 或其药物活性盐，外消旋混合物，对映体，旋光异构体或其互变异构形式。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

2. 发明申请

WO2009109493A3 2-AMINOQUINOLINE DERIVATIVES AS 5-HT ( 5A) RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT（5A）受体拮抗剂的2-氨基喹啉衍生物
公开(公告)号：WO2009109493A3
公开(公告)日：2009-10-29
申请号：PCT/EP2009052195
申请日：2009-02-25
申请人： HOFFMANN LA ROCHE , 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 , A61K31/47 , A61K31/4709 , A61P25/00 , C07D405/12
CPC分类号： C07D215/38 , C07D405/12
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 R1 and -Z-Ar1 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R1和-Z-Ar1如本文所述。

3. 发明申请

WO2009109493A2 2-AMINOQUINOLINES 审中-公开
标题翻译： 2-氨基喹啉
公开(公告)号：WO2009109493A2
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052195
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 , C07D405/12 , A61K31/47 , A61K31/4709 , A61P25/00
CPC分类号： C07D215/38 , C07D405/12
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 -Z-Ar 1 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R1和-Z-Ar1如本文所述。

4. 发明申请

WO2009109477A1 2-AMINOQUINOLINES 审中-公开
标题翻译： 2-氨基喹啉
公开(公告)号：WO2009109477A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052100
申请日：2009-02-23
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： C07D401/12 , C07D401/14 , C07D405/14 , C07D451/14 , A61K31/4709 , A61P25/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D451/14
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.
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。

5. 发明申请

WO2009049791A2 RADIOLABELED NK3 RECEPTOR ANTAGONIST 审中-公开
标题翻译：放射性NK3受体拮抗剂
公开(公告)号：WO2009049791A2
公开(公告)日：2009-04-23
申请号：PCT/EP2008008439
申请日：2008-10-07
申请人： HOFFMANN LA ROCHE , BISSANTZ CATERINA , MALHERBE PARICHEHR , RIEMER CLAUS , SPOOREN WILL
发明人： BISSANTZ CATERINA , MALHERBE PARICHEHR , RIEMER CLAUS , SPOOREN WILL
IPC分类号： C07D215/52 , A61K31/47
CPC分类号： C07D215/52
摘要： The present invention relates to a radiolabeled Neurokinin 3 receptor antagonist of the general formula (I) wherein R1 is a radiolabeled lower alkyl and a method for identifying a compound that can bind to a NK3R comprising a) contacting a compound of interest with a sample comprising the NK3R in the presence of the radiolabeled NK3R antagonist of any one of claims 1 to 3; and b) monitoring whether the compound of interest influences the binding of said radiolabeled NK3R antagonist to said NK3R. Furthermore, the present invention relates also to a mutant NK3R and uses thereof.
摘要翻译：本发明涉及通式（I）的放射性标记的神经激肽3受体拮抗剂，其中R 1是放射性标记的低级烷基，和鉴定可以结合NK 3 R的化合物的方法，包括a）使目的化合物与样品接触，所述样品包含在权利要求1至3中任一项的放射性标记的NK3R拮抗剂存在下的NK3R; 和b）监测感兴趣的化合物是否影响所述放射性标记的NK3R拮抗剂与所述NK3R的结合。此外，本发明还涉及突变型NK3R及其用途。

6. 发明申请

WO2005000842A1 BENZOTHIAZOLE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：苯并噻唑衍生物作为腺苷受体配体
公开(公告)号：WO2005000842A1
公开(公告)日：2005-01-06
申请号：PCT/EP2004/005178
申请日：2004-05-14
申请人： F. HOFFMAN-LA ROCHE AG , FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： C07D417/14
CPC分类号： C07D417/04 , C07D417/14 , C07D491/10
摘要： The invention relates to compounds of the general formula (I) wherein R 1 is 1,4-dioxepanyl or tetrahydropyran-4-yl; R 2 is -N(R)-(CH 2 ) n ,-5-or 6 membered non aromatic heterocycle, optionally substituted by one or more substituents, selected from the group consisting of lower alkyl or -NR 2 , or is - (CH 2 ) n -5-or 6 membered non aromatic heterocycle, optionally substituted by -(CH 2 ) n -OH, lower alkyl, lower alkoxy, or is -CH 2 ) n -5-or 6 membered aromatic heterocycle, optionally substituted by lower alkyl, lower alkoxy, halogen, halogen-lower alkyl, -CH 2 N(R)(CH 2 ) 2 0CH 3 , -N(R)(CH 2 ) 2 0CH 3 , -CH 2 -morpholinyl or -CH 2 -pyrrolidinyl or is (CH 2 ) n -cycloalkyl, optionally substituted by hydroxy, or is -N(R)-cycloalkyl, optionally substituted by hydroxy or lower alkyl, or is phenyl, optionally substituted by lower alkoxy, halogen, halogen-lower alkyl, lower alkyl, -CH 2 -pyrrolidin-1-yl, -CH 2 -morpholinyl, -CH 2 N(R)(CH 2 ) 2 0CH 3 or -CH 2 -N(R)C(O)-lower alkyl, or is 1,4-dioxa-8-aza-spiro[4,5]decane, or is 2-oxa-5-aza-bicyclo[2.2.1]heptane, or is I-oxa-8-aza-spiro[4,5]decane, or is -N(R)-7-oxa-bicyclo [2.2. 11 hept-2-yl, or is 2-aza-bicyclo[2.2.2]decane; R is hydrogen or lower alkyl; n is 0 or 1; and pharmaceutically acceptable acid addition salts thereof for the treatment of diseases, which relate to the A2A receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是1,4-二氧杂环戊烷基或四氢吡喃-4-基; R 2是-N（R） - （CH 2）n，5-或6-元非芳族杂环，任选地被一个或多个选自低级烷基或-NR 2的取代基取代，或是 - （（CH 2）n -OH，低级烷基，低级烷氧基或-CH 2）n-5-或6元芳族杂环，任选被低级烷基，低级烷氧基，卤素，卤素 - 低级烷基，-CH2N（R）（CH2）20CH3，-N（R）（CH2）20CH3，-CH2-吗啉基或-CH2-吡咯烷基或是（CH2）或被羟基或低级烷基取代的-N（R） - 环烷基，或为任选被低级烷氧基，卤素，卤素 - 低级烷基，低级烷基，-CH 2 - 吡咯烷-1-基，-CH 2 - 吗啉基，-CH 2 N（R）（CH 2）20 CH 3或-CH 2 -N（R）C（O） - 低级烷基，或是1,4-二氧杂-8-氮杂 - 螺[4,5]癸烷或者是2-氧杂-5-氮杂 - 双环[2.2.1]庚烷，或是1-氧杂-8-氮杂 - 螺[4,5]癸烷，或是-N（R）-7-氧杂双环 [2.2。 11庚-2-基，或是2-氮杂 - 双环[2.2.2]癸烷; R是氢或低级烷基; n为0或1; 和其药学上可接受的酸加成盐，用于治疗涉及A2A受体的疾病。

7. 发明申请

WO2011023626A1 PYRROLIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK3受体拮抗剂
公开(公告)号：WO2011023626A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062141
申请日：2010-08-20
申请人： F. HOFFMANN-LA ROCHE AG , JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , PATINY-ADAM, Angélique , RATNI, Hasane , RIEMER, Claus
发明人： JABLONSKI, Philippe , KNUST, Henner , NETTEKOVEN, Matthias , PATINY-ADAM, Angélique , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D401/14 , C07D413/14 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/24 , A61P29/00
CPC分类号： C07D401/14 , C07D413/14
摘要： The present invention relates to a compounds of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen, lower alkyl, lower alkyl substituted by halogen or is halogen or CN, and may be independently from each other if o is 2; Ar 1 is aryl or heteroaryl; Ar 2 is aryl or heteroaryl; R'/R" are independently from each other hydrogen, lower alkyl, lower alkoxy, halogen, C(O)- lower alkyl, cyano or lower alkyl substituted by halogen; m is 0, 1, or 2 when n is 0; or m is 0 or 1 when n is 1; n is 0 or 1; o is 1 or 2; or to pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or to tautomeric forms thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢或低级烷基; R 2是氢，低级烷基，被卤素取代的低级烷基，或者是卤素或CN，如果o是2，可以彼此独立地表示; Ar 1是芳基或杂芳基; Ar2是芳基或杂芳基; R'/ R“彼此独立地为氢，低级烷基，低级烷氧基，卤素，C（O） - 低级烷基，氰基或被卤素取代的低级烷基;当n为0时，m为0,1或2;或当n为1时，m为0或1; n为0或1; o为1或2;或者为药物活性盐，外消旋混合物，对映异构体，光学异构体或其互变异构形式。用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜在NK-3受体拮抗剂。

8. 发明申请

WO2009153179A1 PYRROLIDINE DERIVATIVES AS NK2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吡咯啉衍生物作为NK2受体拮抗剂
公开(公告)号：WO2009153179A1
公开(公告)日：2009-12-23
申请号：PCT/EP2009/056987
申请日：2009-06-08
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , KOBLET, Andreas , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
发明人： BISSANTZ, Caterina , JABLONSKI, Philippe , KNUST, Henner , KOBLET, Andreas , LIMBERG, Anja , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus
IPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10 , A61K31/40 , A61K31/4439 , A61K31/443 , A61P25/24
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/10
摘要： The present invention relates to a compound of Formula (I) wherein R 1 is hydrogen, halogen, cyano or lower alkyl; n is 1, 2 or 3; R 2 is hydrogen or lower alkyl; R 3 is an aryl- or a heteroaryl ring, wherein the rings are optionally substituted by one or two substituents R'; R' is selected from hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen,-S(O) 2 -lower alkyl, CN, -NR 4 R 5 , -C(O)-lower alkyl, heterocyclyl or heteroaryl; R 4 /R 5 are independently from each other hydrogen, -(CO)CF 3 or lower alkyl or is a non aromatic heterocyclic group (II) wherein X is N or CH; Y is -CH(R 7 )-; -N(R 7' )-, or O or can be SO 2 ; R 6 is hydrogen, lower alkyl or hydroxy; R 7 is hydrogen, hydroxy, =0, lower alkyl, lower alkoxy, -S(O) 2 -lower alkyl, -C(O)-lower alkyl, -C(O)CH 2 O-lower alkyl, -CH 2 CN, -C(O)CH 2 CN, -C(O)-cycloalkyl wherein the cycloalkyl group is optionally substituted by cyano, lower alkyl, one or two halogen atoms, =0 or by amino, or is -C(O)O-lower alkyl, -NH-lower alkyl, -NRC(O)O-lower alkyl, -NRC(O)-lower alkyl or -CH 2 O-lower alkyl; and R 7' is hydrogen, lower alkyl, -(CH 2 ) q -S(O) 2 -lower alkyl, -(CH 2 ) q -S(O) 2 -cycloalkyl, -C(O)-lower alkyl, -(CH 2 ) q -cycloalkyl, -C(O)CH 2 -O-lower alkyl, -(CH 2 ) q CN, -C(O)CN, -C(O)CH 2 CN, lower alkyl substituted by halogen, lower alkenyl substituted by halogen, -C(O)-cycloalkyl wherein the cycloalkyl group is optionally substituted by cyano, lower alkyl, one or two halogen atoms, =0 or by amino, or is -C(O)O-lower alkyl or -(CH 2 )qO-lower alkyl and q is O - 3; or R 6 and R 7 may form together with the carbon atoms to which they are attach a five or six- membered non aromatic ring or R 6 and R 7 may form together with the nitrogen and carbon atoms to which they are attach a five or six-membered non aromatic ring; p is 0, 1 or 2; Ar is aryl- or heteroaryl, wherein the rings are optionally substituted by one or two substituents R"; R' ' is selected from hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -O-CH 2 -cycloalkyl, -NR 4 R 5 , -CN, -CH(CH 3 )CN, -CH 2 O-lower alkyl or pyrrolyl; m is 0, 1 or 2 and o is 0; o is 0, 1 or 2 and m is 1 or pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds may be used for the treatment of depression, anxiety or schizophrenia.
摘要翻译：本发明涉及式（I）的化合物，其中R 1是氢，卤素，氰基或低级烷基; n为1,2或3; R2是氢或低级烷基; R3是芳基或杂芳基环，其中环任选地被一个或两个取代基R'取代; R'选自氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，-S（O）2 - 低级烷基，CN，-NR 4 R 5，-C（O） - 低级烷基，杂环基或杂芳基; R 4 / R 5彼此独立地为氢， - （CO）CF 3或低级烷基或为非芳族杂环基团（II），其中X为N或CH; Y是-CH（R 7） - ; -N（R 7'） - 或O或可以是SO 2; R6是氢，低级烷基或羟基; R 7是氢，羟基，= 0，低级烷基，低级烷氧基，-S（O）2 - 低级烷基，-C（O） - 低级烷基，-C（O）CH 2 O-低级烷基，-CH 2 CN，-C O）CH 2 CN，-C（O） - 环烷基，其中环烷基任选被氰基，低级烷基，一个或两个卤素原子取代，= 0或被氨基取代，或者是-C（O）O-低级烷基，-NH - 低级烷基，-NRC（O）O-低级烷基，-NRC（O） - 低级烷基或-CH 2 O-低级烷基; 并且R 7'是氢，低级烷基， - （CH 2）qS（O）2 - 低级烷基， - （CH 2）qS（O）2-环烷基，-C（O） - 低级烷基， - （CH 2），-C（O）CH 2 -O-低级烷基， - （CH 2）q CN，-C（O）CN，-C（O）CH 2 CN，被卤素取代的低级烷基，被卤素取代的低级链烯基，-C（O） - 环烷基，其中环烷基任选被氰基，低级烷基，一个或两个卤素原子，= O或氨基取代，或者是-C（O）O-低级烷基或 - （CH 2）q O-低级烷基，q是 O - 3; 或者R 6和R 7可以与它们所连接的五元或六元非芳香环的碳原子一起形成，或者R 6和R 7可以与它们所连接的五元或六元非芳环的氮和碳原子一起形成，芳香环 p为0,1或2; Ar是芳基或杂芳基，其中环任选地被一个或两个取代基R“取代; R”选自氢，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基， O-CH 2 - 环烷基，-NR 4 R 5，-CN，-CH（CH 3）CN，-CH 2 O-低级烷基或吡咯基; m为0,1或2，o为0; o为0,1或2，m为1 或其药物活性盐，外消旋混合物，对映异构体，旋光异构体或互变异构体形式。化合物可用于治疗抑郁症，焦虑或精神分裂症。

9. 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。

10. 发明申请

WO2011073160A1 PYRROLIDINE DERIVATIVES AS NK - 3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK-3受体拮抗剂的吡咯烷衍生物
公开(公告)号：WO2011073160A1
公开(公告)日：2011-06-23
申请号：PCT/EP2010/069564
申请日：2010-12-14
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , KOBLET, Andreas , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
发明人： KNUST, Henner , KOBLET, Andreas , NETTEKOVEN, Matthias , RATNI, Hasane , RIEMER, Claus , VIFIAN, Walter
IPC分类号： C07D401/06 , C07D401/14 , C07D403/14 , C07D405/14 , A61P25/28 , A61K31/44
CPC分类号： C07D401/14 , C07D207/14 , C07D401/06 , C07D405/14
摘要： The present application relates to compounds of formula (I) wherein R 1 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; n is 1, 2 or 3, if n is 2 or 3, R 1 can be different; R 2 is C 2-7 -alkyl or C 3-6 -cycloalkyl; R 3 is the group (II) wherein X is CH or N; R 5 is hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, S(O) 2 -lower alkyl, -C(O)CH 2 O-lower alkyl, -C(O)-CH 2 -CN, or is - or -C(O)-cycloalkyl, cycloalkyl, or -CH 2 -cycloalkyl, wherein the cycloalkyl groups are optionally substituted by lower alkyl, -CH 2 -O-Iower alkyl, lower alkoxy, CF 3 , halogen or cyano, or is -C(O)-heterocycloalkyl or heterocycloalkyl, or is -C(O)-heteroaryl or is heteroaryl or is -C(O)-aryl or aryl, which heterocycloalkyl, heteroaryl or aryl groups are optionally substituted by halogen, lower alkyl, =O, lower alkoxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -C(O)-CH 2 -N(di-lower alkyl), C(O)NH-lower alkyl, C(O)NH 2 , -O-C(O)- lower alkyl, C(O)-lower alkyl, S(O) 2 -lower alkyl or cyano; R 4 is aryl, which is optionally substituted by halogen, hydroxy, lower alkyl, lower alkyl substituted by halogen, S(O) 2 -lower alkyl, cyano or by lower alkoxy; or to a pharmaceutically active salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
摘要翻译：本申请涉及其中R 1为氢，卤素，氰基，低级烷基或被卤素取代的低级烷基的式（I）化合物; n为1,2或3，如果n为2或3，则R1可以不同; R2是C2-7烷基或C3-6-环烷基; R3是其中X是CH或N的基团（II）; R5是氢，-C（O） - 低级烷基，-C（O）O-低级烷基，S（O）2-低级烷基，-C（O）CH2O-低级烷基，-C（O） CN，或是 - 或-C（O） - 环烷基，环烷基或-CH 2 - 环烷基，其中环烷基任选被低级烷基，-CH 2 -O-低级烷基，低级烷氧基，CF 3，卤素或氰基取代，或是-C（O） - 杂环烷基或杂环烷基，或是-C（O） - 杂芳基或是杂芳基或是-C（O） - 芳基或杂芳基，该杂环烷基，杂芳基或芳基任选被卤素取代，低级烷基，= O，低级烷氧基，被卤素取代的低级烷基，被羟基取代的低级烷基，-C（O）-CH 2 -N（二低级烷基），C（O）NH-低级烷基，C（O），-OC（O） - 低级烷基，C（O） - 低级烷基，S（O）2 - 低级烷基或氰基; R4是芳基，其任选被卤素，羟基，低级烷基，被卤素，S（O）2 - 低级烷基，氰基或低级烷氧基取代的低级烷基取代; 或其药物活性盐。已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

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