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1. 发明申请

WO2010026110A2 6-SUBSTITUTED BENZOXAZINES 审中-公开
标题翻译： 6-取代苯并噻唑
公开(公告)号：WO2010026110A2
公开(公告)日：2010-03-11
申请号：PCT/EP2009/061152
申请日：2009-08-28
申请人： F. HOFFMANN-LA ROCHE AG , KOLCZEWSKI, Sabine , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
发明人： KOLCZEWSKI, Sabine , ROCHE, Olivier , STEWARD, Lucinda , WICHMANN, Juergen , WOLTERING, Thomas
IPC分类号： C07D265/18
CPC分类号： C07D265/18 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/02 , C07D498/08
摘要： The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I), wherein X, Y, R 1 and R 2 are as described herein, as well as their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are 5-HT 5A receptor antagonists, 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, Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
摘要翻译：本发明涉及式（I）的6-取代苯并恶嗪衍生物，其中X，Y，R 1和R 2如本文所述，以及它们的制备，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是可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，惊恐障碍，广场恐怖症，社交恐惧症，强迫症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆，饮食行为障碍，性功能障碍，睡眠障碍，药物滥用，运动障碍，帕金森病，精神病或胃肠疾病。

2. 发明申请

WO2010006938A1 NOVEL HETEROCYCLYL COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISEASE 审中-公开
标题翻译：用于治疗心血管疾病的新型杂环化合物
公开(公告)号：WO2010006938A1
公开(公告)日：2010-01-21
申请号：PCT/EP2009/058467
申请日：2009-07-06
申请人： F. HOFFMANN-LA ROCHE AG , AEBI, Johannes , BINGGELI, Alfred , GREEN, Luke , HARTMANN, Guido , MAERKI, Hans, P. , MATTEI, Patrizio , RICKLIN, Fabienne , ROCHE, Olivier
发明人： AEBI, Johannes , BINGGELI, Alfred , GREEN, Luke , HARTMANN, Guido , MAERKI, Hans, P. , MATTEI, Patrizio , RICKLIN, Fabienne , ROCHE, Olivier
IPC分类号： C07D241/08 , C07D243/08 , C07D285/36 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/14 , A61K31/4965 , A61K31/497 , A61K31/551 , A61P9/10
CPC分类号： C07D403/06 , C07D241/08 , C07D243/08 , C07D285/36 , C07D401/06 , C07D401/12 , C07D405/14
摘要： The invention is concerned with novel heterocyclyl compounds of formula (I); wherein A, X, Y 1 , Y 2 , Y 3 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型杂环基化合物; 其中A，X，Y 1，Y 2，Y 3，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，m，n和p如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物是CCR2受体，CCR5受体和/或CCR3受体的拮抗剂，可用作药物。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO2009092642A1 SULFONAMIDES AS OREXIN ANTAGONISTS 审中-公开
标题翻译： SULFONAMIDES作为OREXIN拮抗剂
公开(公告)号：WO2009092642A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/050272
申请日：2009-01-12
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D207/06 , C07D207/08 , C07D211/16 , A61P25/00 , A61K31/4015
CPC分类号： C07D207/06 , C07D207/08 , C07D211/16
摘要： The present invention is concerned with novel sulfonamides of formula wherein R 1 , R 2 , R 3 and n are as described in the description and claims. The compounds are orexin receptor antagonists may be useful in the treatment of disorders, in which orexin pathways are involved.
摘要翻译：本发明涉及新型的具有下式的磺酰胺，其中R1，R2，R3和n如说明书和权利要求中所述。化合物是食欲素受体拮抗剂可用于治疗其中涉及食欲素途径的病症。

7. 发明申请

WO2009080533A1 HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：异丙肾上腺素衍生物作为OREXIN受体拮抗剂
公开(公告)号：WO2009080533A1
公开(公告)日：2009-07-02
申请号：PCT/EP2008/067273
申请日：2008-12-11
申请人： F. HOFFMANN-LA ROCHE AG , KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： KNUST, Henner , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07D401/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04 , A61K31/4025 , A61P25/00
CPC分类号： C07D413/12 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present invention relates to compounds of Formula (I), wherein Ar is an unsubstituted or substituted aryl or heteroaryl group, wherein the aryl and the heteroaryl group may be substituted by one or more substituents R 2 ; R 2 is hydroxy, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, C(O)-lower alkyl, nitro, NR , R ,, , cyano, S-lower alkyl, SO 2 -lower alkyl, cycloalkyl, heterocycloalkyl, phenyloxy, benzyloxy, phenyl, NH-phenyl or heteroaryl, wherein the phenyl and heteroaryl group is unsubstituted or substituted by one or more substituents selected from lower alkyl or halogen; R , /R ,, are independently from each other hydrogen or lower alkyl; R 1 is hydrogen or lower alkyl; Het is a heteroaryl group, unsubstituted or substituted by one or more substituents selected from R 3 ; R 3 is hydroxy, halogen, =O, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, phenyl, lower alkoxy substituted by halogen, nitro, cyano, SO 2 -lower alkyl, cycloalkyl or heterocycloalkyl; n is 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula (I) are orexin receptor antagonists and the related compounds may be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
摘要翻译：本发明涉及式（I）化合物，其中Ar为未取代或取代的芳基或杂芳基，其中芳基和杂芳基可被一个或多个取代基R2取代; R 2是羟基，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，C（O） - 低级烷基，硝基，NR，R'，氰基，S-低级烷基，SO 2 - 烷基，环烷基，杂环烷基，苯氧基，苄氧基，苯基，NH-苯基或杂芳基，其中苯基和杂芳基是未取代的或被一个或多个选自低级烷基或卤素的取代基取代; R 1 / R 3彼此独立地为氢或低级烷基; R1是氢或低级烷基; Het是未取代或被一个或多个选自R 3的取代基取代的杂芳基; R 3是羟基，卤素，= O，低级烷基，被卤素取代的低级烷基，低级烷氧基，苯基，被卤素，硝基，氰基，SO 2 - 低级烷基，环烷基或杂环烷基取代的低级烷氧基; n为1或2; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。已经发现，式（I）化合物是食欲肽受体拮抗剂，相关化合物可用于治疗睡眠呼吸暂停，发作性睡病，失眠，睡眠，时差综合征，昼夜节律障碍或与神经系统疾病相关的睡眠障碍。

8. 发明申请

WO2008151957A9 CYCLOHEXYL DERIVATIVES 审中-公开
标题翻译：环辛基衍生物
公开(公告)号：WO2008151957A9
公开(公告)日：2009-03-05
申请号：PCT/EP2008056743
申请日：2008-06-02
申请人： HOFFMANN LA ROCHE , GAUFRETEAU DELPHINE , NETTEKOVEN MATTHIAS , PLANCHER JEAN-MARC , ROCHE OLIVIER , SCHMITT SEBASTIEN , TAKAHASHI TADAKATSU
发明人： GAUFRETEAU DELPHINE , NETTEKOVEN MATTHIAS , PLANCHER JEAN-MARC , ROCHE OLIVIER , SCHMITT SEBASTIEN , TAKAHASHI TADAKATSU
IPC分类号： C07D295/185
CPC分类号： C07D403/12 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及其中R 1和R 2如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

9. 发明申请

WO2008151957A1 CYCLOHEXYL DERIVATIVES 审中-公开
标题翻译：环辛基衍生物
公开(公告)号：WO2008151957A1
公开(公告)日：2008-12-18
申请号：PCT/EP2008/056743
申请日：2008-06-02
申请人： F. HOFFMANN-LA ROCHE AG , GAUFRETEAU, Delphine , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , ROCHE, Olivier , SCHMITT, Sébastien , TAKAHASHI, Tadakatsu
发明人： GAUFRETEAU, Delphine , NETTEKOVEN, Matthias , PLANCHER, Jean-Marc , ROCHE, Olivier , SCHMITT, Sébastien , TAKAHASHI, Tadakatsu
IPC分类号： C07D295/185
CPC分类号： C07D403/12 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
摘要翻译：本发明涉及其中R 1和R 2如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

10. 发明申请

WO2008110488A1 MALONAMIDES AS OREXIN ANTAGONISTS 审中-公开
标题翻译：马洛康作为OREXIN ANTAGONISTS
公开(公告)号：WO2008110488A1
公开(公告)日：2008-09-18
申请号：PCT/EP2008/052639
申请日：2008-03-05
申请人： F. HOFFMANN-LA ROCHE AG , GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
发明人： GOBBI, Luca , KNUST, Henner , MALHERBE, Parichehr , NETTEKOVEN, Matthias , PINARD, Emmanuel , ROCHE, Olivier , ROGERS-EVANS, Mark
IPC分类号： C07C233/08 , C07C233/15 , C07C233/22 , A61K31/167
CPC分类号： C07C233/29 , C07C233/15 , C07C233/32 , C07C233/88 , C07C2601/02 , C07C2601/08 , C07D211/16 , C07D211/46 , C07D213/40 , C07D213/75 , C07D295/185 , C07D309/14
摘要： The present invention relates to compounds of formula wherein Ar 1 and Ar 2 are independently from each other unsubstituted or substituted aryl or heteroaryl; R 1 /R 2 are independently from each other hydrogen, lower alkyl, lower alkyl substituted by halogen, -(CH 2 ) o -O-lower alkyl, -(CH 2 ) o -N-(lower alkyl) 2 , (CH 2 )p -cycloalkyl, (CH 2 ) p -heterocycloalkyl, (CH 2 ) p -aryl, (CH 2 ) p -heteroaryl, which rings may be substituted by R, or R 1 and R 2 may form together with the N-atom to which they are attached a heterocyclic ring, optionally with further ring-heteroatoms selected from N, O or S, which ring may be substituted by R; R is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or lower alkoxy substituted by halogen; R 3 is hydrogen or lower alkyl; n is O, 1, 2, 3 or 4; o is 1, 2 or 3; P is 0, 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula I are orexin receptor antagonists and the related compounds may be useful in the treatment of disorders, in which orexin pathways are involved like sleep disorders.
摘要翻译：本发明涉及下式的化合物，其中Ar 1和Ar 2 2彼此独立地为未取代或取代的芳基或杂芳基; R 1和R 2彼此独立地为氢，低级烷基，被卤素取代的低级烷基， - （CH 2 CH 2） -O-低级烷基， - （CH 2）2 - （低级烷基）2 - ， - （CH 3） SUB> 2

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