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1. 发明申请

WO2007036718A3 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的化合物及其在医学中的用途
公开(公告)号：WO2007036718A3
公开(公告)日：2007-05-31
申请号：PCT/GB2006003595
申请日：2006-09-27
申请人： GLAXO GROUP LTD , BUDZIK BRIAN , COOPER DAVID GWYN , FORBES IAN THOMSON , GARZYA VINCENZO , JIN JIAN , SHI DONGCHUAN , SMITH PAUL WILLIAM , WALKER GRAHAM
发明人： BUDZIK BRIAN , COOPER DAVID GWYN , FORBES IAN THOMSON , GARZYA VINCENZO , JIN JIAN , SHI DONGCHUAN , SMITH PAUL WILLIAM , WALKER GRAHAM
IPC分类号： C07D401/14 , A61K31/44 , A61P25/00
CPC分类号： C07D401/14
摘要： Compounds of formula (I) and salts and solvates are provided: In a first aspect therefore, the invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 5 is selected from halogen, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, C 1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R 6 is selected from halogen, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 3-6 cycloalkyl, C 3 - 6 cycloalkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, C 1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C 1-6 alkyl. The compounds are M 1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
摘要翻译：提供式（I）化合物和盐和溶剂化物：因此，在第一方面，本发明提供式（I）化合物或其盐或溶剂化物：其中R 5选自卤素 C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C

2. 发明申请

WO2007036715A3 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的化合物及其在医学中的用途
公开(公告)号：WO2007036715A3
公开(公告)日：2007-05-18
申请号：PCT/GB2006003590
申请日：2006-09-27
申请人： GLAXO GROUP LTD , BUDZIK BRIAN , COOPER DAVID GWYN , FORBES IAN THOMSON , GARZYA VINCENZO , JIN JIAN , SHI DONGCHUAN , SMITH PAUL WILLIAM , WALKER GRAHAM
发明人： BUDZIK BRIAN , COOPER DAVID GWYN , FORBES IAN THOMSON , GARZYA VINCENZO , JIN JIAN , SHI DONGCHUAN , SMITH PAUL WILLIAM , WALKER GRAHAM
IPC分类号： C07D235/26 , A61K31/4184 , A61P25/00 , C07D405/12
CPC分类号： C07D405/12 , C07D235/26
摘要： Compounds which have activity at M 1 receptor and their uses in medicine Compounds of formula (I) and salts and solvates are provided: wherein R 4 is fluoro, R 5 is selected from hydrogen, halogen, cyano, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, and C 1-6 alkoxy substituted with one or more fluorine atoms; and R 6 is selected from halogen, cyano, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 3-6 cycloalkyl, C 3-6 cycloalkyl substituted with one or more fluorine atoms, C 1-6 alkoxy and C 1-6 alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C 1-6 alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
摘要翻译：在M 1受体中具有活性的化合物及其在药物中的用途提供式（I）化合物和盐和溶剂化物：其中R 4是氟，R 4， 5选自氢，卤素，氰基，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C

3. 发明申请

WO2008119720A1 1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE ML RECEPTOR AND THEIR USE IN MEDICINE 审中-公开
标题翻译： 1-（1-环丙基-4-哌啶基）-1,3-二氢-2H-苯并咪唑-2-酮衍生物，其在ML受体上具有活性及其在药物中的用途
公开(公告)号：WO2008119720A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008053600
申请日：2008-03-27
申请人： GLAXO GROUP LTD , COOPER DAVID GWYN , FORBES IAN THOMSON , GARZYA VINCENZO , WALKER GRAHAM , WYMAN PAUL ADRIAN
发明人： COOPER DAVID GWYN , FORBES IAN THOMSON , GARZYA VINCENZO , WALKER GRAHAM , WYMAN PAUL ADRIAN
IPC分类号： C07D401/04 , A61K31/454 , A61P25/00
CPC分类号： C07D401/04
摘要： Compounds of formula I or a salt thereof are provided wherein R 4 , R 5 , R 6 , Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式I化合物或其盐，其中R 4，R 5，R 6，Q，L和R R如说明。公开了化合物作为药物和用于制备治疗精神病和认知障碍的药物的用途。本发明还公开了包含该化合物的药物组合物。

4. 发明申请

WO03068732A2 BENZENESULFONAMIDE DERIVATIVES 审中-公开
标题翻译：苯并呋喃衍生物
公开(公告)号：WO03068732A2
公开(公告)日：2003-08-21
申请号：PCT/EP0301544
申请日：2003-02-13
申请人： GLAXO GROUP LTD , 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： C07D217/02 , A61K31/395 , A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/55 , A61P1/00 , A61P1/08 , A61P3/04 , A61P15/02 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07C307/00 , C07D209/44 , C07D217/22 , C07D223/16 , C07D405/12 , C07D409/12
CPC分类号： C07D223/16 , 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, -(CH2)pC3-6cycloalkyl, -(CH2)pC3-6cycloalkyloxy, -COC1-6alkyl, -SOC1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -COC1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8, -(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; R3 represents hydrogen or C1-6alkyl; R4 represents halogen, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, -(CH2)pC3-6cycloalkyl or -(CH2)pC3-6cycloalkyloxy; R5 and R6 each independently represent hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pC3-6cycloalkyloxy, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8, -(CH2)pNR7COR8, optionally substituted aryl, optionally substituted heteroaryl or a fused bicyclic heterocyclic ring system; 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; 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.
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 - 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， - （CH 2）pC 3-6环烷基， - （CH 2）p C 3-6环烷氧基，-COC 1-6烷基，（C 1-6）烷基，-SOC 1-6烷基，-S-C 1-6烷基，-COC 1-6烷基，-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，任选取代的芳基，任选取代的杂芳基或稠合双环杂环体系; R3表示氢或C1-6烷基; R4代表卤素，三氟甲基，三氟甲氧基，C1-6烷基，C1-6烷氧基， - （CH2）pC3-6环烷基或 - （CH2）pC3-6环烷氧基; R5和R6各自独立地表示氢，卤素，羟基，氰基，硝基，羟基C1-6烷基，三氟甲基，三氟甲氧基，C1-6烷基，C1-6烷氧基， - （CH2）pC3-6环烷基， - （CH2）pC3-6环烷氧基，-COC1 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 7 R 8， - （CH 2）p NR 7 COR 8，任选取代的芳基，任选取代的杂芳基或稠合双环杂环体系; R 7和R 8各自独立地表示氢或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或溶剂合物，条件是化合物4-甲基-N-（1,2,3,4-四氢异喹啉-6-基） - 苯磺酰胺，7-（4-氯苯基）亚磺酰氨基-1， 2,3,4-四氢异喹啉盐酸盐和N-（2-乙基-5-异吲哚啉基） - 对甲苯磺酰胺。该化合物可用于治疗，特别是抗精神病药。

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