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1. 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。

2. 发明申请

WO2005025576A1 7-HETEROARYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE DERIVATIVES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：作为抗感染剂的7-异氟烷基四氢吡喃-3-胆碱衍生物
公开(公告)号：WO2005025576A1
公开(公告)日：2005-03-24
申请号：PCT/EP2004/010131
申请日：2004-09-09
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H. , SMITH, Alexander, Baxter
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H. , SMITH, Alexander, Baxter
IPC分类号： A61K31/55
CPC分类号： C04B35/632 , C07D401/12 , C07D409/12
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 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 3 R 4 , -SO 2 NR 3 R 4 , -(CH 2 ) p NR 3 R 4 , -(CH 2 ) p NR 3 COR 4 , optionally substituted aryl ring, optionally substituted heteroaryl ring, a fused bicyclic heteroaromatic ring system or optionally substituted heterocyclyl ring; Ar 1 represents optionally substituted heteroaryl ring; Ar 2 represents optionally substituted aryl ring or optionally substituted heteroaryl ring; Z represents -(CH 2 ) q X- wherein the -(CH 2 ) q - group is attached to Ar 2 , or -X(CH 2 ) q - wherein X is attached to Ar 2 , and wherein any of the -CH 2 - groups may be optionally substituted by one or more C 1-6 alkyl groups; X represents oxygen, -CH(OR 5 )-, -NR 5 - or -CH 2 - wherein the -CH 2 - group may be optionally substituted by one or more C 1-6 alkyl groups; R 3 and R 4 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 5 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 independently represents an integer selected from 0, 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof, with the proviso that when Ar 1 is a pyridyl group, and Z is -CH 2 X- where X is attached to the Ar 1 group, X is selected from -CH(OR 5 )-, -NR 5 - and -CH 2 - wherein the -CH 2 - group may be optionally substituted by one or more C 1-6 alkyl groups. 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）p C 3-6环烷基， - （CH 2），-COC 1-6烷基，-SO 2 C 1-6烷基，-SOC 1-6烷基，-S-C 1-6烷基，-CO 2 C 1-6烷基，-CO 2 NR 3 R 4，-SO 2 NR 3 R 4，（CH 2）p NR R 3， - （CH 2）p NR 3 COR 4，任选取代的芳基环，任选取代的杂芳基环，稠合双环杂芳环系统或任选取代的杂环基环; Ar 1表示任选取代的杂芳基环; Ar 2表示任选取代的芳基环或任选取代的杂芳基环; Z表示 - （CH2）qX-，其中 - （CH2）q-基团连接到Ar 2或-X（CH 2）q-，其中X连接到Ar 2上，并且其中-CH 2 - 基团可以任选被一个或多个C 1-6烷基取代; X表示氧，-CH（OR 5） - ， - NR 5 - 或-CH 2 - ，其中-CH 2 - 基可以任选被一个或多个C 1-6烷基取代; R 3和R 4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 5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独立地表示选自0,1,2和3的整数; 或其药学上可接受的盐或溶剂化物，条件是当Ar 1是吡啶基，Z是-CH 2 X-，其中X连接到Ar 1基团时，X选自-CH 5 - ） - ，-NR 5 - 和-CH 2 - ，其中-CH 2 - 基团可以任选被一个或多个C 1-6烷基取代。式（I）化合物可用于治疗，特别是抗精神病药。

3. 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。

4. 发明申请

WO2003099786A2 COMPOUNDS 审中-公开
标题翻译：芳香硫磺及其医疗用途
公开(公告)号：WO2003099786A2
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005727
申请日：2003-05-28
申请人： GLAXO GROUP LIMITED , GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham , GARZYA, Vincenzo
发明人： GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham , GARZYA, Vincenzo
IPC分类号： C07D209/44
CPC分类号： C07D223/16 , C07D209/44 , C07D217/02
摘要： The invention provides compounds of formula (I): wherein A and B represent the groups -(CH2)m- and -(CH2)n- respectively;R1 represents hydrogen or C1-6alkyl;R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR5R6, -SO2NR5R6, -(CH2)pNR5R6, -(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring;R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring;R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, -OSO2CF3, -(CH2)pC3-6cycloalkyl, -(CH2)qOC1-6alkyl or -(CH2)pOC3-6cycloalkyl;R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring;Z represents -(CH2)rX- wherein the -(CH2)r- group is attached to R3, or -X(CH2)r- wherein X is attached to R3, and wherein any of the -CH2- groups may be optionally substituted by one or more C1-6alkyl groups;X represents oxygen, -NR7 or -CH2- wherein the -CH2- group may be optionally substituted by one or more C1-6alkyl groups;R7 represents hydrogen or C1-6alkyl;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 independently represents an integer selected from 1, 2 and 3; r independently represents an integer selected from 0, 1, and 2; 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分别代表 - （CH 2）m-和 - （CH 2）n - 基团; R 1代表氢或C 1-6烷基; R 2代表氢，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）p C 3-6环烷基， - （CH 2）pOC 3 6-环烷基，-COC 1-6烷基，-SO 2 C 1-6烷基，（CH2）pNR5R6， - （CH2）pNR5COR6，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代表（C 1 -C 6）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）pOC 3 -6-环烷基; R 5和R 6各自独立地表示氢，C 1-6烷基，或者与它们所连接的氮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; Z表示 - （CH2）rX-，其中 - （CH2）r-基团连接到R3或-X（CH2）r-，其中X连接到R3，其中任何-CH 2 - 基可任选被一个或多个C 1-6烷基取代; X代表氧，-NR 7或-CH 2 - ，其中-CH 2 - 基可以任选地被一个或多个C 1-6烷基取代; R 7 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独立地表示选自1,2和3的整数; r独立地表示选自0,1和2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。

5. 发明申请

WO2005051397A1 7-PHENYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE DERIVATIVES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：作为抗菌剂的7-苯基磺酰基四氢吡喃-3-胆碱衍生物
公开(公告)号：WO2005051397A1
公开(公告)日：2005-06-09
申请号：PCT/EP2004/013417
申请日：2004-11-25
申请人： GLAXO GROUP LIMITED , FORBES, Ian, Thomson , GENTILE, Gabriella , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H. , WALKER, Graham
发明人： FORBES, Ian, Thomson , GENTILE, Gabriella , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H. , WALKER, Graham
IPC分类号： A61K31/55
CPC分类号： C07D223/16
摘要： The invention provides one or more chemical entities selected from a compound of formula (I): (I) wherein R1 represents C1-6alkyl, trifluoromethoxy or halo; R2 represents hydrogen, C1-6alkyl or halo; or when R1 and R2 are positioned at the 3- and 4-positions, R1 and R2 together with the carbon atoms to which they are attached may form a 1,4-dioxane ring; and a pharmaceutically acceptable salt and solvate thereof. The compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof are useful in therapy, in particular as antipsychotic agents.
摘要翻译：本发明提供一种或多种选自式（I）化合物的化学实体：（I）其中R 1表示C 1-6烷基，三氟甲氧基或卤素; R 2表示氢，C 1-6烷基或卤素; 或当R1和R2位于3-和4-位时，R1和R2与它们所连接的碳原子一起可以形成1,4-二恶烷环; 及其药学上可接受的盐和溶剂合物。式（I）化合物及其药学上可接受的盐和溶剂合物可用于治疗，特别是抗精神病药。

6. 发明申请

WO2003099786A3 AROMATIC SULFONES AND THEIR MEDICAL USE 审中-公开
公开(公告)号：WO2003099786A3
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005727
申请日：2003-05-28
申请人： GLAXO GROUP LIMITED , GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham , GARZYA, Vincenzo
发明人： GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham , GARZYA, Vincenzo
IPC分类号： C07D209/44
摘要： The invention provides compounds of formula (I): wherein A and B represent the groups -(CH2)m- and -(CH2)n- respectively;R1 represents hydrogen or C1-6alkyl;R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR5R6, -SO2NR5R6, -(CH2)pNR5R6, -(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring;R3 represents optionally substituted aryl ring or optionally substituted heteroaryl ring;R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, trifluoromethyl, trifluoromethoxy, halogen, -OSO2CF3, -(CH2)pC3-6cycloalkyl, -(CH2)qOC1-6alkyl or -(CH2)pOC3-6cycloalkyl;R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring;Z represents -(CH2)rX- wherein the -(CH2)r- group is attached to R3, or -X(CH2)r- wherein X is attached to R3, and wherein any of the -CH2- groups may be optionally substituted by one or more C1-6alkyl groups;X represents oxygen, -NR7 or -CH2- wherein the -CH2- group may be optionally substituted by one or more C1-6alkyl groups;R7 represents hydrogen or C1-6alkyl;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 independently represents an integer selected from 1, 2 and 3; r independently represents an integer selected from 0, 1, and 2; or a pharmaceutically acceptable salt or solvate thereof.The compounds are useful in therapy, in particular as antipsychotic agents.

7. 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.

8. 发明申请

WO2003095428A1 DOPAMINE RECEPTOR MODULATORS AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：多巴胺受体调节剂作为抗感染剂
公开(公告)号：WO2003095428A1
公开(公告)日：2003-11-20
申请号：PCT/GB2003/001983
申请日：2003-05-09
申请人： GLAXO GROUP LIMITED , GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H. , COOPER, David, Gwyn
发明人： GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H. , COOPER, David, Gwyn
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07D217/04
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 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 optionally substituted heterocyclyl; R 3 represents hydrogen or C 1-6 alkyl; R 4 represents optionally substituted aryl or optionally substituted heteroaryl; 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 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 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 optionally substituted heterocyclyl; R 7 and R 8 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; m and n independently represent an integer selected from 1 and 2; p independently represents an integer selected from 0, 1, 2 and 3; and either: Z represents -CR 9 R 10 X- or -XCR 9 R 10 - and X represents oxygen, sulfur, -SO- or -SO 2 , or Z represents -CONR 11 - or -NR 9 CO- and X represents -CH 2 -, oxygen, sulfur, -SO- or -SO 2 ; R 9 and R 10 each independently represent hydrogen, C 1-6 alkyl or fluoro; R 11 represents hydrogen or C 1-6 alkyl;or a pharmaceutically acceptable salt or solvate thereof.The compounds of the invention 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）p C 3-6环烷基， - （CH 2），-COC 1-6烷基，-SO 2 C 1-6烷基，-SOC 1-6烷基，-S-C 1-6烷基，-CO 2 C 1-6烷基，-CO 2 NR 7 R 8，-SO 2 NR 7 R 8， - （ CH2）pNR7R8， - （CH2）pNR7 COR8，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基; R 3表示氢或C 1-6烷基; R 4表示任选取代的芳基或任选取代的杂芳基; R 5和R 6各自独立地表示氢，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， - （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，-CO2NR7R8，-SO2NR7R8，， - （CH2）pNR7R8， - （CH2）pNR7 COR8，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基; R 7和R 8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; 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; 并且：Z表示-CR 9 R 10或-XCR 9 R 10 - ，X表示氧，硫，-SO-或-SO 2，或Z表示-CONR 11 - 或-NR 9 CO-，X代表-CH 2 - ，氧，硫，-SO-或-SO 2; R 9和R 10各自独立地表示氢，C 1-6烷基或氟; R 11表示氢或C 1-6烷基;或其药学上可接受的盐或溶剂合物。本发明的化合物可用于治疗，特别是抗精神病药。

9. 发明申请

WO2005051398A1 7-PHENYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE DERIVATIVES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：作为抗菌剂的7-苯基磺酰基四氢吡喃-3-胆碱衍生物
公开(公告)号：WO2005051398A1
公开(公告)日：2005-06-09
申请号：PCT/EP2004/013418
申请日：2004-11-25
申请人： GLAXO GROUP LIMITED , FORBES, Ian, Thomson , GENTILE, Gabriella , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H. , SMITH, Alexander, Baxter
发明人： FORBES, Ian, Thomson , GENTILE, Gabriella , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H. , SMITH, Alexander, Baxter
IPC分类号： A61K31/55
CPC分类号： C07D223/16 , C07D413/12
摘要： The invention provides one or more chemical entities selected from a compound of formula (I): wherein R 1 represents C 1-6 alkyl, C 1-6 alkoxy, trifluoromethyl, trifluoromethoxy, halo, cyano, 5-methyl-1,2,4-oxadiazol-3-yl or a group -SO 2 X; R 2 represents hydrogen, C 1-6 alkyl, C 1-6 alkoxy, halo or cyano; X is C 1-6 alkyl, -NR 3 R 4 or morpholino; R 3 and R 4 independently represent hydrogen or C 1-6 alkyl; and a pharmaceutically acceptable salt and solvate thereof; with the proviso that the compound {8-[4-(4-fluoro-benzyl)-benzenesulfonyl]-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl}-dimethyl-amine is excluded. The compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof are useful in therapy, in particular as antipsychotic agents.
摘要翻译：本发明提供一种或多种选自式（I）化合物的化学实体：其中R 1表示C 1-6烷基，C 1-6烷氧基，三氟甲基，三氟甲氧基，卤素，氰基，5-甲基-1,2,4- 恶二唑-3-基或基团-SO 2 X; R 2表示氢，C 1-6烷基，C 1-6烷氧基，卤素或氰基; X是C 1-6烷基，-NR 3 R 4或吗啉代; R 3和R 4独立地表示氢或C 1-6烷基; 及其药学上可接受的盐和溶剂合物; 条件是化合物{8- [4-（4-氟 - 苄基） - 苯磺酰基] -3-甲基-2,3,4,5-四氢-1H-3-苯并吖庚因-7-基} - 二甲基 - 胺被排除。式（I）化合物及其药学上可接受的盐和溶剂合物可用于治疗，特别是抗精神病药。

10. 发明申请

WO2004031181A1 SULFONAMIDE DERIVATIVES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：磺酰胺衍生物作为抗生素代谢物
公开(公告)号：WO2004031181A1
公开(公告)日：2004-04-15
申请号：PCT/EP2003/011174
申请日：2003-10-06
申请人： GLAXO GROUP LIMITED , FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H.
发明人： FORBES, Ian, Thomson , GRIBBLE, Andrew, Derrick , LIGHTFOOT, Andrew, P. , PAYNE, Andrew, H.
IPC分类号： C07D409/12
CPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
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 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 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 4 R 5 , -SO 2 NR 4 R 5 , -(CH 2 ) p NR 4 R 5 , -(CH 2 ) p NR 4 COR 5 , an optionally substituted aryl group, an optionally substituted heteroaryl group or an optionally substituted heterocyclyl group; R 3 represents hydrogen or C 1-6 alkyl; Ar 1 represents an optionally substituted heteroaryl group; Ar 2 represents an optionally substituted phenyl or an optionally substituted heteroaryl group; Y represents a bond, -O-, -C 1-6 alkyl-, -CR 6 R 7 X-, -XCR 6 R 7 -, -NR 8 CO- or -CONR 8 -; X represents oxygen, sulfur, -SO- or -SO 2 -; R 4 and R 5 each independently represent hydrogen or 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 6 and R 7 each independently represent hydrogen, C 1-6 alkyl or fluoro; R 8 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; or a pharmaceutically acceptable salt, solvate or pharmaceutically acceptable derivative 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分别表示基团 - （CH 2）m - 和 - （CH 2）n - R 1表示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， - （CH 2）pC 3-6环烷基， - （CH 2）pOC 3 6-环烷基， C 1-6烷基，-SO 2 C 1-6烷基，-SOC 1-6烷基，-S-C 1-6烷基，-CO 2 C 1-6烷基，-CO 2 NR 4 R 5，-SO 2 NR 4 R 5， - （CH 2）p NR R 5， - （CH 2）p NR R 4 COR 5，任选取代的芳基，任选取代的杂芳基或任选取代的杂环基; R 3表示氢或C 1-6烷基; Ar 1表示任选取代的杂芳基; Ar 2表示任选取代的苯基或任选取代的杂芳基; Y表示键，-O - ， - C 1-6烷基 - ， - CR 6 R 7，-XCR 6 R 7 - ，-NR 8 CO-或-CONR 8 > - ; X表示氧，硫，-SO-或-SO 2 - ; R 4和R 5各自独立地表示氢或C 1-6烷基，或者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 6和R 7各自独立地表示氢，C 1-6烷基或氟; R 8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; 或其药学上可接受的盐，溶剂化物或药学上可接受的衍生物。该化合物可用于治疗，特别是抗精神病药。

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