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1. 发明申请

WO2009095377A1 SPIRO COMPOUNDS AS NPY Y5 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： SPIRO化合物作为NPY Y5受体拮抗剂
公开(公告)号：WO2009095377A1
公开(公告)日：2009-08-06
申请号：PCT/EP2009/050867
申请日：2009-01-27
申请人： GLAXO GROUP LIMITED , BIAGETTI, Matteo , CONTINI, Stefania Anne , GENSKI, Thorsten , GUERY, Sebastien , LESLIE, Colin Philip , MAZZALI, Angelica , PIZZI, Domenica Antonia , SABBATINI, Fabio Maria , SERI, Catia
发明人： BIAGETTI, Matteo , CONTINI, Stefania Anne , GENSKI, Thorsten , GUERY, Sebastien , LESLIE, Colin Philip , MAZZALI, Angelica , PIZZI, Domenica Antonia , SABBATINI, Fabio Maria , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , A61K31/423 , A61P3/00
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; Z 1 is H, C 1 -C 4 alkyl or F; Z is CH 2 , CH(C 1 -C 4 alkyl), C(C 1 -C 4 alkyl)2 or a bond; A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or -C(=O)-X; or O(CH 2 ) 0-1 R 1 ; B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom; R 1 is -(C 1 -C 4 )alkyl(C 1 -C 4 )alkoxy; or C 3 -C 8 cycloalkyl; or R 1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; or R 1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 haloalkyl, C 1 -C 4 haloalkoxy, cyano; X is OR 2 or NR 3 R 4 ; R 2 is C 1 -C 4 alkyl; R 3 is hydrogen or together with R 4 and the nitrogen form a 5-6 saturated membered ring; R 4 is C 3 -C 8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐，其中R是芳基或杂芳基，其可被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4 烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; Z 1是H，C 1 -C 4烷基或F; Z是CH 2，CH（C 1 -C 4烷基），C（C 1 -C 4烷基）2或键; A是6-10元芳基或杂芳基，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或-C（= O）-X; 或O（CH 2）0-1R1; B是氢或是5-6元杂芳基或4-6元杂环，或苯基，其可被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C4卤代烷氧基，羟基，氰基; A和B通过任何原子相连; R1是 - （C1-C4）烷基（C1-C4）烷氧基; 或C 3 -C 8环烷基; 或者R 1是可被一个或多个卤素取代的芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 或R 1是4-6元杂环，其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; X为OR2或NR3R4; R2是C1-C4烷基; R3是氢或与R4一起形成5-6饱和的元环; R4是C3-C8环烷基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

2. 发明申请

WO2010142652A1 IMIDAZOBENZAZEPINE COMPOUNDS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM (CNS) DISEASES 审中-公开
标题翻译：用于治疗中枢神经系统（CNS）的IMIDAZOBENZAZEPINE化合物
公开(公告)号：WO2010142652A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/057948
申请日：2010-06-08
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GIANOTTI, Massimo , LESLIE, Colin Philip , STASI, Luigi Piero
发明人： DI FABIO, Romano , GIANOTTI, Massimo , LESLIE, Colin Philip , STASI, Luigi Piero
IPC分类号： C07D487/04 , A61K31/55 , A61P25/00
CPC分类号： C07D487/04 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： This invention relates to novel novel imidazobenzazepine derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.
摘要翻译：本发明涉及用于治疗中枢神经系统（CNS）的疾病和病症，特别是睡眠障碍的式（I）的新颖的咪唑并氮吖庚因衍生物或其药学上可接受的盐。

3. 发明申请

WO2008092891A1 1-OXA-3-AZASPIRO(4.5)DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS 审中-公开
标题翻译： 1-OXA-3-AZASPIRO（4.5）用于治疗排毒障碍的DECAN-2-ONE衍生物
公开(公告)号：WO2008092891A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051116
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BIAGETTI, Matteo , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , A61K31/423 , A61P3/00 , A61P25/00
CPC分类号： C07D413/14
摘要： The present invention relates to novel compounds or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of: (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)3-(2-fluoro-3-pyridinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(3-pyridazinyl)-1-oxa-3- azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(1-methyl-1H-pyrazol-3-yl)- 1-oxa-3-azaspiro[4.5]decan-2-one; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
摘要翻译：本发明涉及选自以下的新的化合物或其药学上可接受的盐或溶剂化物：（反）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基} 甲基）-3-（2-氟-3-吡啶基）-1-氧杂-3-氮杂螺[4.5]癸-2-酮; （反式）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（3-哒嗪基）-1-氧杂-3-氮杂螺[4.5] -2-酮; （反式）-8 - （{[1-（2-氟苯基）-1H-吡唑-3-基]氨基}甲基）-3-（1-甲基-1H-吡唑-3-基）-1-氧杂 - 3-氮杂螺[4.5]癸-2-酮; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

4. 发明申请

WO2008092887A1 I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS 审中-公开
标题翻译： I-OXA-3-AZASPIRO（4.5）Decan-2-ONE和1-OXA-3,8-DIAZASPIRO（4.5）Decan-2-ONE衍生物用于治疗排卵病
公开(公告)号：WO2008092887A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051110
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/423 , A61P3/00 , A61P25/00
CPC分类号： C07D498/10 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1 -C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; W is -CZ 1 or nitrogen; Z 1 is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C 4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ 1 , compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐或溶剂合物，式（I）其中R是芳基或杂芳基; 其可以被一个或多个取代：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; W是-CZ 1 N或氮; Z 1是氢，C 1 -C 4烷基; A是可以被一个或多个卤素取代的5元杂芳基，吡嗪，嘧啶或喹啉或喹唑啉：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; B是氢或可被一个或多个取代基取代的5-10元芳基或杂芳基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，氰基; 是通过任何原子连接的A和B; 条件是当W是-CZ 1时，式（I）的化合物具有反式立体化学; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为NPY Y5受体拮抗剂以及用于治疗和/或预防进食障碍如狂饮病症的药剂。

5. 发明申请

WO2005014552A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 审中-公开
标题翻译：具有5HT1型受体亲和力的喹啉和喹唑啉衍生物
公开(公告)号：WO2005014552A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008000
申请日：2004-07-15
申请人： GLAXO GROUP LIMITED , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong , WARD, Simon, Edward
发明人： BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong , WARD, Simon, Edward
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R 1 , m, X, R 2 , n, W, p, Y, Z, R 3 , R 4 , R 5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中R1，m，X，R2，n，W，p，Y，Z，R3，R4，R5和q具有如说明书中所定义的含义。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁或焦虑症。

6. 发明公开

EP2121673A1 I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS 审中-公开
标题翻译： 1-氧杂-3-氮杂螺[4.5]癸-2-酮和1-氧杂-3,8-二氮杂螺[4.5]癸-2-酮用于治疗进食障碍衍生物
公开(公告)号：EP2121673A1
公开(公告)日：2009-11-25
申请号：EP08708425.7
申请日：2008-01-30
申请人： Glaxo Group Limited
发明人： BENTLEY, Jonathan , BIAGETTI, Matteo , CARDULLO, Francesca , GENSKI, Thorsten , KOPF, Silvia Rosalia , LESLIE, Colin Philip , MELOTTO, Sergio , MENICONI, Mirco , MERLO, Giancarlo , PIZZI, Domenica Antonia , SERI, Catia
IPC分类号： C07D413/12 , C07D413/14 , C07D417/14 , C07D498/10 , A61K31/423 , A61P3/00 , A61P25/00
CPC分类号： C07D498/10 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1 -C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; W is -CZ1 or nitrogen; Z1 is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ1, compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.

7. 发明授权

EP1646613B1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 有权
标题翻译：喹啉和喹唑啉衍生物亲和力受体在来自5HT1-TYPE
公开(公告)号：EP1646613B1
公开(公告)日：2008-03-19
申请号：EP04763307.8
申请日：2004-07-15
申请人： GLAXO GROUP LIMITED
发明人： BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong, GlaxoSmithKline , WARD, Simon, Edward, GlaxoSmithKline
IPC分类号： C07D215/38 , C07D413/12 , C07D409/12 , C07D401/12 , C07D417/12 , C07D405/12 , A61K31/4709
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.

8. 发明公开

EP1646613A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 有权
标题翻译：喹啉和喹唑啉衍生物亲和力受体在来自5HT1-TYPE
公开(公告)号：EP1646613A1
公开(公告)日：2006-04-19
申请号：EP04763307.8
申请日：2004-07-15
申请人： GLAXO GROUP LIMITED
发明人： BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong, GlaxoSmithKline , WARD, Simon, Edward, GlaxoSmithKline
IPC分类号： C07D215/38 , C07D413/12 , C07D409/12 , C07D401/12 , C07D417/12 , C07D405/12 , A61K31/4709
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R1, m, X, R2, n, W, p, Y, Z, R3, R4, R5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.

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