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1. 发明申请

WO2011045353A1 INDOLE AND AZAINDOLE MODULATORS OF THE ALPHA 7 NACHR 审中-公开
标题翻译： ALPHA 7 NACHR的INDOLE和AZAINDOLE调制器
公开(公告)号：WO2011045353A1
公开(公告)日：2011-04-21
申请号：PCT/EP2010/065368
申请日：2010-10-14
申请人： PROXIMAGEN LIMITED , DINNELL, Kevin , LIGHTFOOT, Andrew , MORTON, Gillian Elizabeth
发明人： DINNELL, Kevin , LIGHTFOOT, Andrew , MORTON, Gillian Elizabeth
IPC分类号： C07D403/12 , C07D471/04 , A61K31/506 , A61P25/00
CPC分类号： C07D471/04 , A61K31/506 , C07D403/12
摘要： This invention relates to modulation of the α7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐调节a7烟碱乙酰胆碱受体（nAChR）。

2. 发明申请

WO2012055942A1 ALPHA-7 NICOTINIC RECEPTOR MODULATORS FOR THE TREATMENT OF PAIN, A PSYCHOTIC DISORDER, COGNITIVE IMPAIRMENT OR ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗疼痛，心理障碍，认知障碍或阿尔茨海默病的ALPHA-7非诺贝特受体调节剂
公开(公告)号：WO2012055942A1
公开(公告)日：2012-05-03
申请号：PCT/EP2011/068807
申请日：2011-10-26
申请人： PROXIMAGEN Limited , DEAN, David , LIGHTFOOT, Andrew , ROOMANS, Susan
发明人： DEAN, David , LIGHTFOOT, Andrew , ROOMANS, Susan
IPC分类号： C07D407/14 , C07D413/14 , A61P25/00 , A61K31/506 , A61K31/55 , A61K31/5377
CPC分类号： C07D413/14 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D405/14 , C07D413/10 , A61K2300/00
摘要： Compounds are disclosed which modulate the α7 nicotinic acetyl choline receptor (nAChR), having the formula (I) wherein the variables are as specified in the description and claims.
摘要翻译：公开了调节具有式（I）的α7烟碱乙酰胆碱受体（nAChR）的化合物，其中变量如说明书和权利要求书中所述。

3. 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。

4. 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.

5. 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。

6. 发明申请

WO2003099792A1 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：WO2003099792A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005728
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
发明人： GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07D209/44 , C07D217/02 , C07D217/04
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 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, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8 or -(CH2)pNR7COR8;R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, 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;R7 and R8 each independently represent 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; or a pharmaceutically acceptable salt or solvate thereof,with the proviso that the compounds 8-hydroxy-3-methyl-7-phenylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 8-hydroxy-7-4-(hydroxyphenyl)sulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline and 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline hydrochloride are excluded.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）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）pOC 3 6-环烷基，-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， - （CH 2）p NR 27 R 8或 - （CH 2）p NR 7 COR 8; R 4表示氢，羟基，C 1-6烷基，C 1-6烷氧基，C 1-6氟烷氧基，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烷基或与氮或它们所连接的其它原子形成氮杂环烷基环或氧代取代的氮杂环烷基环; R7和R8各自独立地表示氢或C1-6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; 或其药学上可接受的盐或溶剂合物，条件是化合物8-羟基-3-甲基-7-苯基磺酰基-2,3,4,5-四氢-1H-3-苯并氮杂-8-羟基-7-4 - （羟基苯基）磺酰基-2,3,4,5-四氢-1H-3-苯并氮杂，7-苯基磺酰基-1,2,3,4-四氢异喹啉和7-苯基磺酰基-1,2,3,4-四氢异喹啉盐酸盐这些化合物可用于治疗，特别是抗精神病药。

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