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1. 发明申请

WO2009016084A1 SPIRO CYCLOPENTANE COMPOUNDS USEFUL AS ANTAGONISTS OF THE H1-RECEPTOR 审中-公开
标题翻译：螺旋环化合物可用作H1受体拮抗剂
公开(公告)号：WO2009016084A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059682
申请日：2008-07-24
申请人： GLAXO GROUP LIMITED , CASTIGLIONI, Emiliano , DI FABIO, Romano , GIANOTTI, Massimo , MESIC, Milan , PAVONE, Francesca , RAST, Slavko , STASI, Luigi, Piero
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , GIANOTTI, Massimo , MESIC, Milan , PAVONE, Francesca , RAST, Slavko , STASI, Luigi, Piero
IPC分类号： C07C211/38 , A61K31/131 , A61P25/00
CPC分类号： C07C211/38 , C07C2603/94
摘要： This invention relates to novel spiro cyclopentane 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：本发明涉及式（I）的新型螺环戊烷衍生物或其药学上可接受的盐，用于治疗中枢神经系统（CNS）的疾病和病症，特别是睡眠障碍。

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

WO2010063663A1 N-{[(IR,4S,6R-3-(2-PYRIDINYLCARBONYL)-3-AZABICYCLO [4.1.0]HEPT-4-YL] METHYL}-2-HETEROARYLAMINE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： N - {[（1R，4S，6R-3-（2-吡啶基]苄基] -3-亚氨基] [4.1.0] HEPT-4-YL]甲基} -2-叔丁基胺衍生物及其用途
公开(公告)号：WO2010063663A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/066017
申请日：2009-11-30
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
发明人： ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/55 , A61P25/22 , A61P25/24 , A61P3/04
CPC分类号： C07D401/14
摘要： This invention relates to N -{[(1 R ,4 S ,6 R )-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及N - {[（1R，4S，6R）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-杂芳基胺衍生物及其作为药物。

4. 发明申请

WO2010063662A1 N-{[(IR,4S,6R-3-(2-PYRIDINYLCARBONYL)-3-AZABICYCLO [4.1.0] HEPT-4-YL] METHYL}-2-HETEROARYLAMINE DERIVATIVES AND USES THEREOF 审中-公开
标题翻译： N - {[（1R，4S，6R-3-（2-吡啶基]苄基] -3-亚氨基] [4.1.0] HEPT-4-YL]甲基} -2-叔丁基胺衍生物及其用途
公开(公告)号：WO2010063662A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/066016
申请日：2009-11-30
申请人： GLAXO GROUP LIMITED , ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
发明人： ALVARO, Giuseppe , AMANTINI, David , CASTIGLIONI, Emiliano , DI FABIO, Romano , PAVONE, Francesca
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/55 , A61P25/22 , A61P25/24 , A61P3/04
CPC分类号： C07D401/06 , C07D401/14
摘要： This invention relates to N -{[(1 S ,4 S ,6 S )-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及N - {[（1S，4S，6S）-3-（2-吡啶基羰基）-3-氮杂双环[4.1.0]庚-4-基]甲基} -2-杂芳基胺衍生物及其作为药物。

5. 发明申请

WO2009016085A1 SPIRO COMPOUNDS USEFUL AS ANTAGONISTS OF THE H1 RECEPTOR 审中-公开
标题翻译： SPIRO化合物作为H1受体拮抗剂有效
公开(公告)号：WO2009016085A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059683
申请日：2008-07-24
申请人： GLAXO GROUP LIMITED , BOTTA, Maurizio , CASTIGLIONI, Emiliano , DI FABIO, Romano , SPINOSA, Raffaella , TOGNINELLI, Andrea
发明人： BOTTA, Maurizio , CASTIGLIONI, Emiliano , DI FABIO, Romano , SPINOSA, Raffaella , TOGNINELLI, Andrea
IPC分类号： C07C211/38 , C07D498/10 , C07D491/10 , C07D295/02 , C07D205/04 , A61K31/131 , A61P25/00
CPC分类号： C07C211/42 , C07C2603/94 , C07D221/20 , C07D295/00 , C07D295/027 , C07D295/03 , C07D295/033 , C07D491/10 , C07D498/10
摘要： The invention provides a compound 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：本发明提供了用于治疗中枢神经系统（CNS）的疾病和病症的式（I）化合物或其药学上可接受的盐，特别是睡眠障碍。

6. 发明申请

WO2004062665A1 HETEROARYL- SUBSTITUTED PYRROLO` 2, 3- B! PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译： HETEROARYL-替代PYRROLO` 2，3-B！吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：WO2004062665A1
公开(公告)日：2004-07-29
申请号：PCT/EP2004/000409
申请日：2004-01-14
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , GLAXO GROUP LIMITED , CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437
CPC分类号： C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供了包括其立体异构体，前体药物和药学上可接受的盐或溶剂合物的式（I）化合物，其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症）。

7. 发明申请

WO2008148853A1 N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR 审中-公开
标题翻译：作为GHRELIN受体的调节剂的N-苯基水杨酸
公开(公告)号：WO2008148853A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057018
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D213/54 , C07D239/26 , C07D307/79 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/72 , C07D333/76 , C07D405/06 , C07D471/04 , C07D487/04 , C07D295/15 , A61K31/498
CPC分类号： C07D333/76 , C07D211/34 , C07D213/56 , C07D213/61 , C07D239/26 , C07D295/15 , C07D307/81 , C07D307/85 , C07D307/91 , C07D317/46 , C07D317/60 , C07D319/18 , C07D333/60 , C07D405/06 , C07D471/04 , C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: each R 1 is independently selected from the group consisting of Cl, Br, CH 3 and CF 3 ; X is carbon or nitrogen; R 1a is H or a straight C 1-3 alkyl group; R 2a is H or a methyl group R 2 is selected from the group consisting of C 1-3 alkyl, H and -(CH 2 ) n -, wherein n is 3 or 4 and the terminal carbon of the chain is bonded to the carbon atom adjacent to the nitrogen bearing the R 2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed. Y is selected from the group consisting of: phenyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, C 1-3 alkoxy, halogen, C 1-3 alkyl substituted by 1 to 7 fluoro atoms and C 1-3 alkoxy substituted by 1 to 7 fluoro atoms; pyridyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C 1-3 alkyl, OCH 3 , CF 3 , CN, and halogen; naphthyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of F and OCH 3 ; pyrimidinyl; imidazo[1,2-a]pyridine-6-yl; benzothiophen-2-yl; benzothiophen-5-yl; benzofuran-2-yl; dibenzo[b,d]furan-3-yl; dibenzo[b,d]thiophen-2-yl; dibenzo[b,d]thiophen-4-yl; 1,3- benzodioxol-5-yl; 2,3-dihydro-1,4-benzodioxin-5-yl; 2,3-dihydro-1,4-benzodioxin-6-yl; 2,3- dihydro-1-benzofuran-4-yl; 2,2-difluoro-1,3-benzodiox-4-yl; pyridazinyl; imidazolyl; oxazolyl; pyrazolyl; thiazolyl; and triazolyl; with the proviso that when Y is 2,3-dihydro-1,4-benzodioxin-6-yl, R 1 is not Cl; processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
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化物，其中：每个R 1独立地选自Cl，Br，CH 3和CF 3; X是碳或氮; R 1a是H或直链C 1-3烷基; R2a是H或甲基R2选自C1-3烷基，H和 - （CH2）n-，其中n是3或4，并且该链的末端碳键合到邻近的碳原子上含有R2基团的氮，使得形成稠合的6,5或6,6-双环。 Y选自：可以是未取代的或被一个或多个独立地选自C 1-3烷基，C 1-3烷氧基，卤素，被1至7个氟原子取代的C 1-3烷基和C 1 由1-7个氟原子取代的3-烷氧基; 吡啶基，其可以是未取代的或被一个或多个独立地选自C 1-3烷基，OCH 3，CF 3，CN和卤素的取代基取代; 萘基，其可以是未取代的或被一个或多个独立地选自F和OCH 3的取代基取代; 嘧啶; 咪唑并[1,2-a]吡啶-6-基; 苯并噻吩-2-基; 苯并噻吩-5-基; 苯并呋喃-2-基; 二苯并[b，d]呋喃-3-基; 二苯并[b，D]噻吩-2-基; 二苯并[b，D]噻吩-4-基; 1,3-苯并间二氧杂环戊烯-5-基; 2,3-二氢-1,4-苯并二恶英-5-基; 2,3-二氢-1,4-苯并二恶英-6-基; 2,3-二氢-1-苯并呋喃-4-基; 2,2-二氟-1,3- benzodiox -4-基; 哒嗪; 咪唑; 恶唑; 吡唑; 噻唑基; 和三唑基; 条件是当Y是2,3-二氢-1,4-苯并二恶英-6-基时，R 1不是Cl; 其制备方法，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，例如作为生长激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）的调节剂和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

8. 发明申请

WO2008148854A1 GHRELIN MODULATORS 审中-公开
标题翻译： GHRELIN调制器
公开(公告)号：WO2008148854A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/057019
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
发明人： BERNASCONI, Giovanni , BROMIDGE, Steven, Mark , CARPENTER, Andrew, James , D'ADAMO, Lucilla , DI FABIO, Romano , GUERY, Sebastien , PAVONE, Francesca , POZZAN, Alfonso , RINALDI, Marilisa , SABBATINI, Fabio, Maria , ST-DENIS, Yves
IPC分类号： C07D401/06
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
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化物，其制备方法，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，例如作为生长调节剂激素促分泌素受体（也称为生长素释放肽受体或GHSR1a受体）和/或用于治疗和/或预防由生长素释放肽受体介导的病症。

9. 发明申请

WO2004094420A1 CONDENSED N-HETEROCYCLIC COMPOUNDS AND THEIR USE AS CRF RECEPTOR ANTAGONISTS 审中-公开
标题翻译：简便的N-杂环化合物及其作为CRF受体拮抗剂的用途
公开(公告)号：WO2004094420A1
公开(公告)日：2004-11-04
申请号：PCT/IB2004/001350
申请日：2004-04-07
申请人： SB PHARMCO PUERTO RICO INC , NEUROCRINE BIOSCIENCES INC , ANDREOTTI, Daniele , BERNASCONI, Giovanni , CASTIGLIONI, Emiliano , CONTINI, Stefania , DI FABIO, Romano , FAZZOLARI, Elettra , FERIANI, Aldo , GENTILE, Gabriella , MATTIOLI, Mario , MINGARDI, Anna , SABBATINI, Fabio , ST-DENIS, Yves
发明人： ANDREOTTI, Daniele , BERNASCONI, Giovanni , CASTIGLIONI, Emiliano , CONTINI, Stefania , DI FABIO, Romano , FAZZOLARI, Elettra , FERIANI, Aldo , GENTILE, Gabriella , MATTIOLI, Mario , MINGARDI, Anna , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof (Formula (I)) wherein the dashed line may represent a double bond; R is aryl or heteroaryl, each of which may be substituted by 1 to 4 groups J selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 lkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, -C(O)R 2 , nitro, hydroxy, -NR 3 R 4 , cyano and or a group Z; R 1 is hydrogen, C3-C7 cycloalkyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo Cl-C6 alkoxy, halogen, NR 3 R 4 or cyano; D, G is . -C- optionally substituted; X is carbon or nitrogen; Y is nitrogen or -C- optionally substituted; W is a 4-8 membered ring, which may be saturated or may contain one to three double bonds, and in which: - one carbon atom is replaced by a carbonyl or S(O) m ; and - one to four carbon atoms may optionally be replaced by oxygen, nitrogen or NR 12 , S(O) m , carbonyl, and such ring may be further substituted by 1 to 8 substituents; Z is a 5-6 membered heterocycle, which may be substituted by 1 to 8 R 5 groups or a phenyl ring, which may be substituted by 1 to 4 substituents; m is an integer from 0 to 2. to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供了包括立体异构体，前体药物和药学上可接受的盐或溶剂合物（式（I））的式（I）化合物，其中虚线可以表示双键; R是芳基或杂芳基，其各自可以被1-4个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤素 C 1 -C 6烷氧基，-C（O）R 2，硝基，羟基，-NR 3 R 4，氰基和/或Z; R 1是氢，C 3 -C 7环烷基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6硫代烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; D，G为-C-任选取代的; X是碳或氮; Y是氮或-C-任选取代的; W是4-8元环，其可以是饱和的或可以含有一至三个双键，其中： - 一个碳原子被羰基或S（O）m取代; 和 - 1-4个碳原子可以任选被氧，氮或NR 12，S（O）m，羰基取代，并且这样的环可进一步被1至8个取代基取代; Z是5-6元杂环，其可以被1至8个R5基团取代或可被1至4个取代基取代的苯基环; m为0至2的整数。其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

10. 发明申请

WO2009130232A1 PYRAZOLO [1, 5 -A] PYRAZINE DERIVATIVES AS ANTAGONISTS OF V1B RECEPTORS 审中-公开
标题翻译：吡咯并[1,5-A]吡嗪衍生物作为V1B受体的拮抗剂
公开(公告)号：WO2009130232A1
公开(公告)日：2009-10-29
申请号：PCT/EP2009/054780
申请日：2009-04-22
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GENTILE, Gabriella , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
发明人： DI FABIO, Romano , GENTILE, Gabriella , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or salts thereof: wherein R is -X-[CH 2 ] n CR 4 R 5 -Y; or a group G; G is one of the groups selected form the list consisting of G1, G2, G3, G4, G5, G6, G7, G8, G9, G10, G11 and G12, and the rest of the variables are as specified in the claims, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as antagonists of V1b receptors, e.g. to treat depression and anxiety.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R是-X- [CH2] nCR4R5-Y; 或G组; G是从由G1，G2，G3，G4，G5，G6，G7，G8，G9，G10，G11和G12组成的列表中选择的组之一，其余变量如权利要求中所述，对于它们的制备，在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V1b受体的拮抗剂，例如治疗抑郁症和焦虑症。

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