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1. 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）。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明授权

EP1583531B1 HETEROARYL-SUBSTITUTED PYRROLO[2, 3- B]PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 有权
标题翻译：杂芳基取代吡咯并[2,3-b]吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：EP1583531B1
公开(公告)日：2007-04-18
申请号：EP04701955.9
申请日：2004-01-14
申请人： SB Pharmco Puerto Rico Inc , NEUROCRINE BIOSCIENCES, INC.
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437 , A61P1/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07D471/04
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).

8. 发明公开

EP1583531A1 HETEROARYL- SUBSTITUTED PYRROLO' 2, 3- B! PYRIDINE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS 有权
标题翻译：杂芳基取代吡咯并[2,3-b]吡啶衍生物作为CRF受体拮抗剂
公开(公告)号：EP1583531A1
公开(公告)日：2005-10-12
申请号：EP04701955.9
申请日：2004-01-14
申请人： SB Pharmco Puerto Rico Inc , NEUROCRINE BIOSCIENCES, INC.
发明人： CASTIGLIONI, Emiliano , DI FABIO, Romano , FERIANI, Aldo , MICHELI, Fabrizio , SABBATINI, Fabio , ST-DENIS, Yves
IPC分类号： A61K31/437 , A61P1/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07D471/04
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).

9. 发明申请

WO2010007032A1 PIPERIDINE BASED UREAS AS NK1 ANTAGONISTS 审中-公开
标题翻译：作为NK1拮抗剂的基于哌啶的UREAS
公开(公告)号：WO2010007032A1
公开(公告)日：2010-01-21
申请号：PCT/EP2009/058937
申请日：2009-07-13
申请人： GLAXO WELLCOME MANUFACTURING PTE LTD , ALVARO, Giuseppe , CARDULLO, Francesca , CASTIGLIONI, Emiliano
发明人： ALVARO, Giuseppe , CARDULLO, Francesca , CASTIGLIONI, Emiliano
IPC分类号： C07D401/04 , A61K31/454 , A61P1/08 , A61P25/20 , A61P25/22 , A61P25/24
CPC分类号： C07D401/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein n is 1 or 2; useful in the treatment of conditions for which antagonism of NK1 receptor is beneficial.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中n为1或2; 可用于治疗NK1受体的拮抗作用有利的条件。

10. 发明申请

WO2009133135A1 SPIRO (PIPERIDINE-4, 2 ' -PYRROLIDINE) -1- (3, 5- TRIFLUOROMETHYL PHENYL) METHYLCARBOXAMIDES AS NK1 TACHIKYNIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为NK1 TACHIKYNIN受体拮抗剂的SPIRO（哌啶-4，2'-吡咯烷）-1-（3,5-二氟甲基苯基）甲基氨基甲酰胺
公开(公告)号：WO2009133135A1
公开(公告)日：2009-11-05
申请号：PCT/EP2009/055190
申请日：2009-04-29
申请人： GLAXO WELLCOME MANUFACTURING PTE LTD , ALVARO, Giuseppe , CASTIGLIONI, Emiliano , MARASCO, Agostino
发明人： ALVARO, Giuseppe , CASTIGLIONI, Emiliano , MARASCO, Agostino
IPC分类号： C07D471/10 , C07D498/20 , A61P25/22 , A61P25/24 , A61P29/00
CPC分类号： C07D471/10 , C07D498/20
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R is hydrogen or C 1-4 alkyl; R 1 is hydrogen, C 1-4 alkyl, C(O)OH, C(O)NH 2 or (C 1-4 alkylene)R 10 ; R 2 and R 3 are independently hydrogen, C 1-4 alkyl or R 2 together with R 3 and together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group; R 4 is C 1-4 alkyl, C 1-4 alkoxy or halogen; R 5 and R 7 are independently hydrogen, hydroxy, halogen, C(O)NH 2 , C(O)OH or (C 1-4 alkylene) R 10 ; R 6 and R 8 are independently hydrogen or halogen; R 9 is hydrogen, (C 1-4 alkylene)R 10 , C(O)NH 2 , C(O)OH or R 9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R 10 is hydrogen, halogen, hydroxy, C(O)NH 2 , C(O)NH(C 1-4 alkyl), C(O)N(C 1-4 alkyl) 2 or C(O)OH; n is O, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R是氢或C 1-4烷基; R 1是氢，C 1-4烷基，C（O）OH，C（O）NH 2或（C 1-4亚烷基）R 10; R 2和R 3独立地是氢，C 1-4烷基或R 2与R 3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C 1-4烷基，C 1-4烷氧基或卤素; R 5和R 7独立地是氢，羟基，卤素，C（O）NH 2，C（O）OH或（C 1-4亚烷基）R 10; R6和R8独立地是氢或卤素; R 9是氢，（C 1-4亚烷基）R 10，C（O）NH 2，C（O）OH或R 9与R一起形成任选地含有另外选自氧，硫或氮的杂原子的6元杂环; R 10是氢，卤素，羟基，C（O）NH 2，C（O）NH（C 1-4烷基），C（O）N（C 1-4烷基）2或C（O） n为O，1或2.制备方法，含有它们的组合物及其用于治疗NK1拮抗作用的疾病和病症的用途。

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