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1. 发明申请

WO2003068751A1 7-ARYLSULFONAMIDO-2,3,4,5-TETRAHYDRO-1H-BENZO'DIAZEPINE DERIVATIVES WITH 5-HT6 RECEPTOR AFFINITY FOR THE REATMENT OF CNS DISORDERS 审中-公开
标题翻译：具有5-HT6受体亲和力的7-ARYLSULFONAMIDO-2,3,4,5-四氢-1H-苯并恶唑衍生物用于中枢神经系统疾病
公开(公告)号：WO2003068751A1
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001543
申请日：2003-02-13
申请人： GLAXO GROUP LIMITED , BROMIDGE, Steven, Mark , JOHNSON, Christopher, Norbert , MOSS, Stephen, Frederick , RAHMAN, Shahzad, Sharooq , WITTY, David, R
发明人： BROMIDGE, Steven, Mark , JOHNSON, Christopher, Norbert , MOSS, Stephen, Frederick , RAHMAN, Shahzad, Sharooq , WITTY, David, R
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , A61K31/40 , A61K31/47 , A61K31/55 , C07D209/44 , C07D217/02 , C07D217/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The present invention relates to novel sulfonamide compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.
摘要翻译：本发明涉及具有药理学活性的新型磺酰胺化合物，其制备方法，含有它们的组合物及其在治疗CNS和其它疾病中的用途。

2. 发明申请

WO2003068752A1 BENZENESULFONAMIDE DERIVATIVES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：苯并呋喃衍生物作为抗生素代谢物
公开(公告)号：WO2003068752A1
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001545
申请日：2003-02-13
申请人： GLAXO GROUP LIMITED , BROMIDGE, Steven, Mark , COOPER, David, Gwyn , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , JOHNSON, Christopher, Norbert , LIGHTFOOT, Andrew, P. , MOSS, Stephen, Frederick , PAYNE, Andrew, H. , RAHMAN, Shahzad, Sharooq , WITTY, David, R.
发明人： BROMIDGE, Steven, Mark , COOPER, David, Gwyn , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , JOHNSON, Christopher, Norbert , LIGHTFOOT, Andrew, P. , MOSS, Stephen, Frederick , PAYNE, Andrew, H. , RAHMAN, Shahzad, Sharooq , WITTY, David, R.
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , A61K31/40 , A61K31/47 , A61K31/55 , C07D209/44 , C07D217/02 , C07D217/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： The invention provides compounds of formula (I)wherein A and B represent the groups -(CH 2 )m- and -(CH 2 )n-respectively; R 1 represents hydrogen or C 1-6 alkyl; R 2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC 1-6 alkyl, trifluoromethyl, trifluoromethoxy, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 3-7 cycloalkylC 1-6 alkoxy, -(CH 2 )pC 3-6 cycloalkyl, -(CH 2 )pC 3-6 cycloalkyloxy, -COC 1-6 alkyl, -SO 2 C 1-6 alkyl, -SOC 1-6 alkyl, -S-C 1-6 alkyl, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfonylC 1-6 alkyl, -CO 2 C 1-6 alkyl, -CO 2 NR 7 R 8 , -SO 2 NR 7 R 8 , C 1-6 alkylsulfonamido, C 1-6 alkylsulfonamidoC 1-6 alkyl, -(CH 2 ) p NR 7 R 8 , C 1-6 alkylamidoC 1-6 alkyl, -(CH 2 )pNR 7 COR 8 , arylsulfonyl, arylsulfonyloxy, arylsulfonylC 1-6 alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC 1-6 alkyl, arylcarboxamidoC 1-6 alkyl, aroyl, aroylC 1-6 alkyl, arylC 1-6 alkanoyl, -SO 2 NR 7 R 8 , optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl, or a group CONR 7 R 8 or SO 2 NR 7 R 8 wherein R 7 and R 8 together may be fused to form a 5- 7-membered aromatic or non-aromatic heterocyclic ring optionally interrupted by an O or S atom; R 3 represents hydrogen or C 1-6 alkyl; Ar represents optionally substituted phenyl or optionally substituted monocyclic heteroaryl group; R 4 represents optionally substituted aryl or optionally substituted heteroaryl; R 7 and R 8 each independently represent hydrogen, C 1-6 alkyl or together form a 5- to 7-membered heterocyclic ring; Z represents a bond, an oxygen atom or C 1-6 alkyl:Y represents hydrogen or C 1-6 alkyl; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; q represents an integer from 1 to 3; r represents an integer from 1 to 4; or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful in therapy, in particular as antipsychotic agents.
摘要翻译：本发明提供式（I）化合物，其中A和B分别表示 - （CH 2）m-和 - （CH 2）n - 基团; R1表示氢或C1-6烷基; R 2表示氢，卤素，羟基，氰基，硝基，羟基C 1-6烷基，三氟甲基，三氟甲氧基，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，C 3-7环烷基C 1-6烷氧基， - （CH 2）p C 3-6环烷基， - CH2）pC3-6环烷氧基，-COC1-6烷基，-SO2C1-6烷基，-SOC1-6烷基，-S-C1-6烷基，C1-6烷基磺酰氧基，C1-6烷基磺酰基C 1-6烷基，-CO 2 C 1-6烷基，-CO 2 NR 7 R 8，-SO 2 NR 7 R 8，C 1 （CH 2）pNR 7 COR 8，芳基磺酰基，芳基磺酰氧基，芳基磺酰基C 1-6烷基，芳基磺酰氨基，芳基羧酰氨基，芳基亚磺酰氨基C 1-6烷基，芳基羧酰胺基C 1-6烷基，芳酰基，芳酰基C 1 -C 6烷基烷基，芳基C 1-6烷酰基，-SO 2 NR 7 R 8，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基，或CONR 7 R 8或SO 2 NR 7 R 8基团，其中R 7和R 8可以一起稠合形成5-7元芳族或非芳族杂环环任选地被O或S原子中断; R3表示氢或C1-6烷基; Ar表示任选取代的苯基或任选取代的单环杂芳基; R4表示任选取代的芳基或任选取代的杂芳基; R 7和R 8各自独立地表示氢，C 1-6烷基或一起形成5-至7-元杂环; Z表示键，氧原子或C 1-6烷基：Y表示氢或C 1-6烷基; m和n独立地表示选自1和2的整数; p独立地表示选自0,1,2和3的整数; q表示1〜3的整数， r表示1〜4的整数，或其药学上可接受的盐或溶剂合物。该化合物可用于治疗，特别是抗精神病药。

3. 发明申请

WO2003062205A1 7-SULFONYL-3-BENZAZEPINE DERIVATIVES AS MODULATORS OF THE DOPAMINE RECEPTOR AND THEIR USE FOR THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：作为多巴胺受体的调节剂及其用于治疗中枢神经系统疾病的7-磺酰基-3-苄胆碱衍生物
公开(公告)号：WO2003062205A1
公开(公告)日：2003-07-31
申请号：PCT/EP2002/014824
申请日：2002-12-20
申请人： SMITHKLINE BEECHAM P.L.C. , AHMED, Mahmood , BROMIDGE, Steven, Mark , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , JOHNSON, Christopher, Norbert , KING, Francis, David , LIGHTFOOT, Andrew, P , MACDONALD, Gregor, James , MOSS, Stephen, Frederick , THOMPSON, Mervyn , WITTY, David, R
发明人： AHMED, Mahmood , BROMIDGE, Steven, Mark , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , JOHNSON, Christopher, Norbert , KING, Francis, David , LIGHTFOOT, Andrew, P , MACDONALD, Gregor, James , MOSS, Stephen, Frederick , THOMPSON, Mervyn , WITTY, David, R
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07D401/12 , C07D403/12
摘要： The present invention relates to novel sulfone compounds of formula (I) or a pharmaceutically acceptable salt thereof: having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders such as psychotic disorders.
摘要翻译：本发明涉及式（I）的新型砜化合物或其药学上可接受的盐：具有药理学活性，其制备方法，含有它们的组合物及其在治疗CNS和其它疾病如精神病性障碍中的用途。

4. 发明申请

WO2004096771A1 BIARYL COMPOUNDS HAVING ACTIVITY AT THE 5HT5A RECEPTOR 审中-公开
标题翻译：在5HT5A受体中具有活性的BIARYL化合物
公开(公告)号：WO2004096771A1
公开(公告)日：2004-11-11
申请号：PCT/EP2004/004658
申请日：2004-04-28
申请人： GLAXO GROUP LIMITED , BROMIDGE, Steven, Mark , CORBETT, David, Francis , HEIGHTMAN, Thomas, Daniel , MOSS, Stephen, Frederick
发明人： BROMIDGE, Steven, Mark , CORBETT, David, Francis , HEIGHTMAN, Thomas, Daniel , MOSS, Stephen, Frederick
IPC分类号： C07D213/40
CPC分类号： C07D213/40 , C07C211/27 , C07C217/58 , C07C233/37 , C07C233/40 , C07C233/62 , C07C235/20 , C07C275/28 , C07C311/13 , C07C2601/02 , C07C2601/08 , C07C2602/08 , C07D211/56 , C07D211/58 , C07D213/38 , C07D241/12 , C07D295/13 , C07D317/50 , C07D401/12 , C07D405/12 , C07D405/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed, wherein one of Ar 1 and Ar 2 is phenyl linked in a 1,4-relationship, and the other is phenyl linked in a 1,4-relationship or a 6 membered heteroaryl ring linked in a 1,4-relationship; R1 is hydrogen, or a group of formula (a), wherein X is C=O or SO 2 ; Y is a single bond, -CH 2 -, -(CH 2 ) 2 -, -CH=CH-, -CH 2 O-, -OCH 2 -, C 3-7 cycloalkylene or NH; and R4 is optionally substituted phenyl or C 3-7 cycloalkyl; Z is a single bond, -CH 2 -, -(CH 2 ) 2 - or -(CH 2 ) 3 -; R7 is NR 8 R 9 where R 8 and R 9 are independently hydrogen or C 1-6 alkyl, or R7 is optionally substituted phenyl, optionally substituted 5- or 6- membered heteroaryl ring or optionally substituted 5- or 6- membered heteroalicyclic ring; A is a single bond, -CH 2 -, -(CH 2 ) 2 -, -CH 2 CH 2 O-, or -CH 2 OCH 2 -; and E is optionally substituted phenyl, indanyl, methylenedioxyphenyl, or a 5- or 6-membered heteroaryl ring. Methods of preparation and uses thereof in medicine, for example for the treatment of CNS disorders such as depression, anxiety, sleep disorders or schizophrenia, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐，其中Ar1和Ar2中的一个是1,4-连接的苯基，另一个是以1,4-关系连接的苯基或6元杂芳基环联系在一个1,4关系; R1是氢或式（a）的基团，其中X是C = O或SO2; Y是单键，-CH 2 - ， - （CH 2）2 - ， - CH = CH - ， - CH 2 O - ， - OCH 2 - ，C 3-7亚环烷基或NH; 并且R 4是任选取代的苯基或C 3-7环烷基; Z是单键，-CH 2 - ， - （CH 2）2 - 或 - （CH 2）3 - ; R 7是NR 8 R 9，其中R 8和R 9独立地是氢或C 1-6烷基，或R 7是任选取代的苯基，任选取代的5-或6-元杂芳基环或任选取代的5- 或6-元杂脂环; A是单键，-CH 2 - ， - （CH 2）2 - ， - CH 2 CH 2 O-或-CH 2 OCH 2 - ; - 并且E是任选取代的苯基，二氢化茚基，亚甲二氧基苯基或5或6元杂芳基环。还公开了其在药物中的制备方法及其用途，例如用于治疗中枢神经系统疾病如抑郁症，焦虑症，睡眠障碍或精神分裂症。

5. 发明申请

WO2003013510A1 3-ARYLSULFONYL-7-PIPERAZINYL- INDOLES, -BENZOFURANS AND -BENZOTHIOPHENES WITH 5-HT6 RECEPTOR AFFINITY FOR TREATING CNS DISORDERS 审中-公开
标题翻译：具有5-HT6受体亲和力的3-ARYLSULFONY-7-PIPERAZINY- INDOLES，苯并呋喃和苯并噻吩治疗CNS疾病
公开(公告)号：WO2003013510A1
公开(公告)日：2003-02-20
申请号：PCT/EP2002/008719
申请日：2002-08-05
申请人： SMITHKLINE BEECHAM P.L.C. , BROMIDGE, Steven, Mark , JOHNSON, Christopher, Norbert , MACDONALD, Gregor, James , THOMPSON, Mervyn , WITTY, David, R.
发明人： BROMIDGE, Steven, Mark , JOHNSON, Christopher, Norbert , MACDONALD, Gregor, James , THOMPSON, Mervyn , WITTY, David, R.
IPC分类号： A61K31/404
CPC分类号： C07D307/82 , C07D209/40 , C07D333/66
摘要： The invention relates to novel compounds of formula (I) having affinity for the 5-HT 6 receptor preparation, to compositions containing them and their use in the treatment of various disorders, including CNS disoders.
摘要翻译：本发明涉及对5-HT> 6受体制剂具有亲和力的新型式（I）化合物，含有它们的组合物及其在治疗各种疾病（包括CNS解码器）中的用途。

6. 发明申请

WO2002089811A1 BENZO[D]AZEPINE DERIVATIVES AS 5-HT6 RECEPTOR ANTAGONISTS. 审中-公开
标题翻译： BENZO [D] AZEPINE衍生物作为5-HT6受体拮抗剂。
公开(公告)号：WO2002089811A1
公开(公告)日：2002-11-14
申请号：PCT/EP2002/004804
申请日：2002-05-02
申请人： SMITHKLINE BEECHAM P.L.C. , BROMIDGE, Steven, Mark , MOSS, Stephen, Frederick
发明人： BROMIDGE, Steven, Mark , MOSS, Stephen, Frederick
IPC分类号： A61K31/55
CPC分类号： C07D403/12
摘要： The invention relates to novel compounds (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of disorders such like depression, anxiety and Alzheimers disease.
摘要翻译：本发明涉及具有药理活性的新化合物（I），其制备方法，含有它们的组合物及其在治疗诸如抑郁，焦虑和阿尔茨海默病的疾病中的用途。

7. 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。

8. 发明申请

WO2006024517A1 FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS 审中-公开
标题翻译：用于治疗心理障碍的融合三聚体衍生物
公开(公告)号：WO2006024517A1
公开(公告)日：2006-03-09
申请号：PCT/EP2005/009379
申请日：2005-08-29
申请人： GLAXO GROUP LIMITED , BENTLEY, Jonathan , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BORRIELLO, Manuela , BROMIDGE, Steven, Mark , GIANOTTI, Massimo , GRANCI, Enrica , LESLIE, Colin, Philip , PASQUARELLO, Alessandra , ZUCCHELLI, Valeria
发明人： BENTLEY, Jonathan , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BORRIELLO, Manuela , BROMIDGE, Steven, Mark , GIANOTTI, Massimo , GRANCI, Enrica , LESLIE, Colin, Philip , PASQUARELLO, Alessandra , ZUCCHELLI, Valeria
IPC分类号： C07D498/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I) wherein R 1 , R 2 , X, A, Y, B, Z 1 , Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.
摘要翻译：式（I）化合物，其中R

9. 发明申请

WO2004046124A1 BENZOXAZINONE DERIVATIVES, PREPARATION THEREOF AND USES IN THE TREATMENT OF CNS AND OTHER DISORDERS 审中-公开
标题翻译：苄唑胺酮衍生物，其制备方法和用于治疗CNS和其他疾病的用途
公开(公告)号：WO2004046124A1
公开(公告)日：2004-06-03
申请号：PCT/EP2003/013085
申请日：2003-11-20
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , BORRIELLO, Manuela , BOZZOLI, Andrea , BROMIDGE, Steven, Mark , GRANCI, Enrica , LESLIE, Colin , SERAFINOWSKA, Halina , STASI, Luigi , VONG, Antonio , ZUCCHELLI, Valeria
发明人： BERTANI, Barbara , BORRIELLO, Manuela , BOZZOLI, Andrea , BROMIDGE, Steven, Mark , GRANCI, Enrica , LESLIE, Colin , SERAFINOWSKA, Halina , STASI, Luigi , VONG, Antonio , ZUCCHELLI, Valeria
IPC分类号： C07D265/36
CPC分类号： C07D413/12 , C07D265/36 , C07D413/14 , C07D471/04 , C07D495/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:wherein A, R1, R2, R3, p, q, A and X are as defined in the specification. Preparation of the compounds and uses in the treatment of CNS and other disorders, including depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中A，R1，R2，R3，p，q，A和X如说明书中所定义。还公开了化合物的制备和用于治疗CNS和其它疾病，包括抑郁和焦虑的用途。

10. 发明申请

WO2003057220A1 CYCLIC UREA DERIVATIVES WITH 5-HT2C RECEPTOR ACTIVITY 审中-公开
标题翻译：具有5-HT2C受体活性的循环尿素衍生物
公开(公告)号：WO2003057220A1
公开(公告)日：2003-07-17
申请号：PCT/GB2003/000020
申请日：2003-01-07
申请人： GLAXO GROUP LIMITED , BROMIDGE, Steven, Mark , LOVELL, Peter, John , GOODACRE, Caroline
发明人： BROMIDGE, Steven, Mark , LOVELL, Peter, John , GOODACRE, Caroline
IPC分类号： A61K31/4453
CPC分类号： C07D401/10 , C07D233/70 , C07D233/78 , C07D413/10 , C07D413/14 , C07D491/08
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof, having 5HT 2C receptor activity, are disclosed: wherein a is 0, 1, 2, 3, 4 or 5; b is 1, 2 or 3; Y is nitrogen or carbon; A is oxygen, nitrogen, -CONH-, -NHCO- or together with R 2 form a benzoxazolone group; R 1 is halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, hydroxy, amino, mono- or di-C 1-6 alkylamino, nitro, CN, CF 3 , OCF 3 , aryl, arylC 1-6 alkyl, arylC 1-6 alkyloxy or arylC 1-6 alkylthio; R 2 is hydrogen, halogen, C 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkyl or haloC 1-6 alkoxy; R 3 is: (i) -NR 4 R 5 where R 4 and R 5 are independently hydrogen, C 1-6 alkyl or arylC 1-6 alkyl; or (ii) an optionally substituted N-linked heterocycle; or (iii) an optionally substituted C-linked heterocycle; ======= is a single bond or a double bond; and X is CH 2 or C = O (when ======= is a single bond) or X is CH (when ======= is a double bond). The preparation of these compounds and their use in therapy, especially for a CNS disorder such as depression or anxiety, are also disclosed.
摘要翻译：公开了具有5HT> 2C <受体活性的式（I）化合物或其药学上可接受的盐，其中a为0,1,2,3,4或5; b为1,2或3; Y是氮或碳; A是氧，氮，-CONH-，-NHCO-或与R 2一起形成苯并恶唑酮基团; R 1是卤素，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，羟基，氨基，单或二-C 1-6烷基氨基，硝基，CN，CF 3，OCF 3，芳基，芳基C 1-6烷基，芳基C 1-6烷氧基或 arylC1-6alkylthio; R 2是氢，卤素，C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷基或卤代C 1-6烷氧基; R 3是：（i）-NR 4 R 5，其中R 4和R 5独立地是氢，C 1-6烷基或芳基C 1-6烷基; 或（ii）任选取代的N-连接的杂环; 或（iii）任选取代的C连接的杂环; =======是单一债券或双重债券; X为CH 2或C = O（当=======为单键时）或X为CH（当=======为双键时）。还公开了这些化合物的制备及其在治疗中的用途，特别是用于抑制或焦虑等CNS病症。

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