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1. 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。

2. 发明申请

WO2003068732A3 BENZENESULFONAMIDE DERIVATIVES AND THEIR USE AS DOPAMINE D3 AND D2 RECEPTOR LIGA DS 审中-公开
公开(公告)号：WO2003068732A3
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001544
申请日：2003-02-13
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P
IPC分类号： C07D223/16
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, -(CH 2 ) p C 3 - 6 cycloalkyl, -(CH 2 ) p C 3 - 6 cycloalkyloxy, -COC 1 - 6 alkyl, -SOC 1 - 6 alkyl, -SOC 1 - 6 alkyl, -S-C 1 - 6 alkyl, -COC 1 - 6 alkyl, -CO 2 NR 7 R 8 , -SO 2 NR 7 R 8 , -(CH 2 )pNR 7 R 8 , -(CH 2 )pNR 7 COR 8 , optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R 3 represents hydrogen or C 1 - 6 alkyl; R 4 represents halogen, trifluoromethyl, trifluoromethoxy, C 1 - 6 alkyl, C 1 - 6 alkoxy, -(CH 2 ) p C 3 - 6 cycloalkyl or -(CH 2 ) p C 3 - 6 cycloalkyloxy; R 5 and R 6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC 1 - 6 alkyl, trifluoromethyl, trifluoromethoxy, C 1 - 6 alkyl, C 1 - 6 alkoxy, -(CH 2 ) p C 3 - 6 cycloalkyl, -(CH 2 ) p C 3 - 6 cycloalkyloxy, -COC 1 - 6 alkyl, -SO 2 C 1 - 6 alkyl, -SOC 1 - 6 alkyl, -S-C 1 - 6 alkyl, -CO 2 C 1 - 6 alkyl, -CO 2 NR 7 R 8 , -SO 2 NR 7 R 8 , -(CH 2 ) p NR 7 R 8 , -(CH 2 ) p NR 7 COR 8 , optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R 7 and R 8 each independently represent 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; or a pharmaceutically acceptable salt or solvate thereof,with the proviso that the compounds 4-methyl-N-(1,2,3,4-tetrahydroisoquinolin-6-yl)-benzenesulfonamide, 7-(4-chlorophenyl)sulfonamido-1,2,3,4-tetrahydroisoquinoline hydrochloride and N-(2-ethyl-5-isoindolinyl)-p-toluenesulfonamide are excluded.The compounds are useful in therapy, in particular as antipsychotic agents.

3. 发明申请

WO2005014578A1 PHENYLSULFONYL COMPOUNDS AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：苯甲醚化合物作为抗生素代谢物
公开(公告)号：WO2005014578A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008965
申请日：2004-08-05
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P , PAYNE, Andrew, H , WALKER, Graham
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P , PAYNE, Andrew, H , WALKER, Graham
IPC分类号： C07D401/12
CPC分类号： C04B35/632 , C07D223/16 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , C07D451/06
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 fluoroalkoxy, -(CH 2 ) p C 3-6 cycloalkyl, -(CH 2 ) p OC 3-6 cycloalkyl, -COC 1-6 alkyl, -SO 2 C 1-6 alkyl, -SOC 1-6 alkyl, -S-C 1-6 alkyl, -CO 2 C 1-6 alkyl, -CO 2 NR 5 R 6 , -SO 2 NR 5 R 6 , -(CH 2 ) p NR 5 R 6 , -(CH 2 ) p NR 5 COR 6 , optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring; R 3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; R 4 represents hydrogen, hydroxy, C 1-6 alkyl, C 1-6 alkoxy, trifluoromethyl, trifluoromethoxy, halogen, -OSO 2 CF 3 , -(CH 2 ) p C 3-6 cycloalkyl, -(CH 2 ) q OC 1-6 alkyl or -(CH 2 ) p OC 3-6 cycloalkyl; X represents -CH- or N; Z represents a bond, -O-, -(CH 2 ) r -, -CH 2 O-, -OCH 2 - or CPO; R 5 and R 6 each independently represent hydrogen, C 1-6 alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring; R 7 and R 8 represent hydrogen or C 1-6 alkyl, or R 7 and R 8 together represent -(CH 2 ) s -; 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 selected from 1, 2 and 3; r represents an integer selected from 1, 2 and 3; s represents an integer selected from 2, 3 and 4; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that when X is N, Z is a bond, -(CH 2 ) r - or CPO. The compounds of formula (I) 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分别表示基团 - （CH 2）m-和 - （CH 2）n - R 1表示氢或C 1-6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氟烷氧基， - （CH 2）pC 3-6环烷基， - （CH 2） pOC3-6环烷基，-COC1-6烷基，-SO2C1-6烷基，-SOC1-6烷基，-S-C1-6烷基，-CO2C1-6烷基，-CO2R5R6，-SO2NR5R6 ， - （CH 2）p NR R 5， - （CH 2）p NR 5 COR 6，任选取代的芳基环，任选取代的杂芳基环或任选取代的杂环基环; R 3表示任选取代的芳基环或任选取代的杂芳基环; R 4表示氢，羟基，C 1-6烷基，C 1-6烷氧基，三氟甲基，三氟甲氧基，卤素，-OSO 2 CF 3， - （CH 2）p C 3-6环烷基， - （CH 2）q OC 1-6烷基或 - （CH 2） X表示-CH-或N; Z表示键，-O - ， - （CH 2）r - ， - CH 2 O - ， - OCH 2 - 或CPO; R 5和R 6各自独立地表示氢，C 1-6烷基，或与它们所连接的氮原子或其它原子一起形成氮杂环烷基环或氧代取代的氮杂环烷基环; R 7和R 8代表氢或C 1-6烷基，或R 7和R 8一起表示 - （CH 2）s - ; 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表示选自1,2和3的整数; r表示选自1,2和3的整数; s表示选自2,3和4的整数; 或其药学上可接受的盐或溶剂化物，条件是当X为N时，Z为键， - （CH 2）r - 或CPO。式（I）化合物可用于治疗，特别是抗精神病药。

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