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1. 发明申请

WO2008119720A8 1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE 审中-公开
公开(公告)号：WO2008119720A8
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053600
申请日：2008-03-27
申请人： GLAXO GROUP LIMITED , 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
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.

2. 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。

3. 发明申请

WO02074764A3 PIPERAZINE DERIVATIVES AND THEIR USE AS 5-HT1B LIGANDS 审中-公开
标题翻译：哌嗪衍生物及其作为5-HT1B配体使用
公开(公告)号：WO02074764A3
公开(公告)日：2002-11-14
申请号：PCT/EP0202632
申请日：2002-03-11
申请人： SMITHKLINE BEECHAM PLC , THOMPSON MERVYN , WYMAN PAUL ADRIAN
发明人： THOMPSON MERVYN , WYMAN PAUL ADRIAN
IPC分类号： C07D403/14 , A61K31/496 , A61P25/24 , A61P43/00 , C07D209/08 , C07D401/10 , C07D403/04 , A61K31/495
CPC分类号： C07D401/10 , C07D209/08
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof are disclosed: in which R is a group of formula (i), wherein P is phenyl, napththyl heteroaryl or a 5 to 7 membered heterocyclic ring; P is phenyl, naphthyl or heteroaryl; R is NR COR , NR SO2R , CH2NR SO2R , CH2NR COR or CH2NR CO2R where R and R are independently hydrogen or C1-6alkyl; R and R are independently halogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkoxy, COC1-6alkyl, haloC1-6alkyl, cyano or NR R where R and R are independently hydrogen or C1-6alkyl; b and c are independently 0, 1, 2 or 3; Y is a single bond, CH2 or NH; W is -(CR R )t- where t is 2, 3 or 4 and R and R are independently hydrogen or C1-6alkyl or W is a group CH=CH; R is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, COC1-6alkyl, cyano or C1-6alkoxy; and R is hydrogen or C1-6alkyl. Processes for preparation of the compounds and their uses in therapy, particularly depression, are also disclosed.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐：其中R a为式（ⅰ）基团，其中P 2为苯基，萘乙基杂芳基或5至7元杂环; P 3是苯基，萘基或杂芳基; R 1是NR 4 COR 5，NR 4 SO 2 R 5，CH 2 NR 4 SO 2 R 5，CH 2 NR 4 COR 5或CH 2 NR 4 CO 2 R 5，其中 R 4和R 5独立地是氢或C 1-6烷基; R 2和R 3独立地是卤素，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，COC 1-6烷基，卤代C 1-6烷基，氰基或NR 6 R 7，其中R 6和R <7>独立地是氢或C 1-6烷基; b和c独立地为0,1,2或3; Y是单键，CH2或NH; W是 - （CR 9 R 10）t - ，其中t是2,3或4，R 9和R 10独立地是氢或C 1-6烷基或W是基团CH = CH; R b是氢，卤素，C 1-6烷基，卤代C 1-6烷基，COC 1-6烷基，氰基或C 1-6烷氧基; 并且R c是氢或C 1-6烷基。还公开了用于制备化合物及其用于治疗，特别是抑郁症的方法。

4. 发明申请

WO1996023769A2 HETEROCYCLIC COMPOUNDS POSSESSING 5HT2C RECEPTOR ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有5HT2C受体拮抗剂活性的杂环化合物
公开(公告)号：WO1996023769A2
公开(公告)日：1996-08-08
申请号：PCT/EP1996000369
申请日：1996-01-24
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian , MULHOLLAND, Keith, Raymond , DAVIES, David, Thomas
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D209/08
CPC分类号： C07D409/12 , C07D209/08
摘要： The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT2C receptor antagonist activity processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.
摘要翻译：本发明涉及具有药理学活性的化合物的杂环族，特别是其具有5HT 2C受体拮抗剂活性的制备方法，含有它们的组合物及其在治疗CNS病症中的用途。

5. 发明申请

WO1995026328A1 BIPHENYL DERIVATIVES AS 5HT1D ANTAGONISTS 审中-公开
标题翻译： BIPHENYL衍生物作为5HT1D拮抗剂
公开(公告)号：WO1995026328A1
公开(公告)日：1995-10-05
申请号：PCT/EP1995000900
申请日：1995-03-09
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07C233/75
CPC分类号： C07C255/57 , C07C233/75 , C07C235/84 , C07C251/48
摘要： Compounds of formula (I), processes for their preparation and their use as CNS agents are disclosed, in which R is hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, COC1-6alkyl, C1-6alkoxy, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxy C1-6alkoxy, acyl, nitro, trifluoromethyl, cyano, SR , SOR , SO2R , SO2NR R , CO2R , CONR R , CO2NR R , CONR (CH2)pCO2R , (CH2)pNR R , (CH2)pCONR R , (CH2)pCO2C1-6alkyl, NR R , NR CO2R , NR CONR R , CR =NOR , CNR =NOR , where R and R are independently hydrogen or C1-6alkyl and p is 1 to 3; R and R are independently hydrogen, halogen, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkenyl, C1-6alkoxy, acyl, aryl, acyloxy, hydroxy, nitro, trifluoromethyl, cyano, CO2R , CONR R , NR R where R and R are independently hydrogen or C1-6alkyl; R and R are independently hydrogen or C1-6alkyl; R is hydrogen, halogen, hydroxy, C1-6alkyl or C1-6alkoxy; R and R are independently hydrogen, C1-6alkyl, aralkyl, or together with the nitrogen atom to which they are attached form an optionally substituted 5-7-membered heterocyclic ring containing one or two heteroatoms selected from oxygen, nitrogen or sulphur; A is CONH or NHCO; B is oxygen, S(O)p where p is 0, 1 or 2, or B is NR where R 1-6
摘要翻译：公开了式（I）化合物及其制备方法及其作为CNS剂的用途，其中R 1为氢，卤素，C 1-6烷基，C 3-6环烷基，COC 1-6烷基，C 1-6烷氧基，羟基，羟基C 1 -6-烷基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，酰基，硝基，三氟甲基，氰基，SR 9，SOR 9，SO 2 R 9，SO 2 NR 10 R 11，CO 2 R 10，，CONR 10 R 11，CO 2 NR 10 R 11，CONR 10（CH 2）p CO 2 R 11，（CH 2）p NR R 10，（CH 2）p CONR 10， R 11，（CH 2）p CO 2 C 1-6烷基，NR 10 R 11，NR 10 CO 2 R 11，NR 10 CONR 10 R 11，CR 10 = 11 CN，CNR 10 = NOR 11，其中R 10和R 11独立地是氢或C 1-6烷基，p是1至3; R 2和R 3独立地是氢，卤素，C 1-6烷基，C 3-6环烷基，C 3-6环烯基，C 1-6烷氧基，酰基，芳基，酰氧基，羟基，硝基，三氟甲基，氰基，CO 2 R 10， CONR 10 R 11，NR 10 R 11，其中R 10和R 11独立地是氢或C 1-6烷基; R 4和R 5独立地是氢或C 1-6烷基; R 6是氢，卤素，羟基，C 1-6烷基或C 1-6烷氧基; R 7和R 8独立地是氢，C 1-6烷基，芳烷基或与它们所连接的氮原子一起形成任选取代的含有一个或两个选自氧的杂原子的5-7元杂环，氮或硫; A是CONH或NHCO; B是氧，S（O）p，其中p是0,1或2，或B是NR 12，其中R 12是氢或C 1-6>烷基; m为2〜4; n为1或2。

6. 发明申请

WO1995006644A1 AMIDE DERIVATIVES AS 5HT1D RECEPTOR ANTAGONISTS 审中-公开
标题翻译： AMT衍生物作为5HT1D受体拮抗剂
公开(公告)号：WO1995006644A1
公开(公告)日：1995-03-09
申请号：PCT/EP1994002661
申请日：1994-08-09
申请人： SMITHKLINE BEECHAM PLC , DUCKWORTH, David, Malcolm , GASTER, Laramie, Mary , MULHOLLAND, Keith, Raymond , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D295/14
CPC分类号： C07D213/40 , C07C2601/14 , C07D271/06 , C07D295/155
摘要： Novel amide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.
摘要翻译：公开了新型酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。

7. 发明申请

WO1995004737A1 CONDENSED INDOLE DERIVATIVES AS 5-HT4-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT4受体拮抗剂的浓缩型吲哚衍生物
公开(公告)号：WO1995004737A1
公开(公告)日：1995-02-16
申请号：PCT/EP1994002514
申请日：1994-07-28
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： A compound of formula (IA) or a pharmaceutically acceptable salt thereof, wherein X is O, S, SO, SO2, CH2, CH or NR wherein R is hydrogen or C1-6 alkyl; A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms; R1 and R2 are hydrogen or C1-6 alkyl; R3 is hydrogen, halo, C1-6 alkyl, amino, nitro or C1-6 alkyl; R4 is hydrogen, halo, C1-6 alkyl or C1-6 alkoxy; Y is O or NH; Z is of sub-formula (a), wherein N is 1, 2, 3 or 4; q is 0, 1, 2 or 3; R5 is 3-phenoxypropyl; or a compound of formula (IA) wherein the CO-Y linkage is replaced by a heterocyclic bioisostere; having 5-HT4 receptor antagonist activity.
摘要翻译：式（IA）化合物或其药学上可接受的盐，其中X为O，S，SO，SO 2，CH 2，CH或NR，其中R为氢或C 1-6烷基; A是2-4个碳原子的饱和或不饱和多亚甲基链; R1和R2是氢或C1-6烷基; R3是氢，卤素，C1-6烷基，氨基，硝基或C1-6烷基; R4是氢，卤素，C1-6烷基或C1-6烷氧基; Y是O或NH; Z为亚式（a），其中N 1为1,2,3或4; q为0,1,2或3; R5是3-苯氧基丙基; 或其中CO-Y键被杂环生物电子等排体代替的式（IA）化合物; 具有5-HT 4受体拮抗剂活性。

8. 发明申请

WO1994008965A1 N-ALKYLPIPERIDINYL-4-METHYL CARBOXYLIC ESTERS/AMIDES OF CONDENSED RING SYSTEMS AS 5-HT4 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为5-HT4受体拮抗剂的缩合环系的N-烷基哌啶-4-基甲基羧酸酯/氨基酸
公开(公告)号：WO1994008965A1
公开(公告)日：1994-04-28
申请号：PCT/GB1993002130
申请日：1993-10-14
申请人： SMITHKLINE BEECHAM PLC , GASTER, Laramie, Mary , JOINER, Graham, Francis , MULHOLLAND, Keith, Raymond , WYMAN, Paul, Adrian
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/22
CPC分类号： C07D401/12 , C07D211/22 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I), wherein formula (I) consists of formulae (I-1) to (I-5), and pharmaceutically acceptable salts thereof, and the use of compound of formula (I) or a pharmaceutically acceptable salt thereof and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.
摘要翻译：式（I）化合物，其中式（I）由式（I-1）至（I-5）组成，及其药学上可接受的盐，以及式（I）化合物或其药学上可接受的盐和它们作为药物用于治疗胃肠道疾病，心血管疾病和CNS疾病。

9. 发明申请

WO2008119715A1 1- (1-CYCLOHEXYL-4-PIPERIDINYL) -1, 3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的1-（1-环辛基-4-哌啶基）-1,3-二氢-2H-苯并咪唑-2-酮衍生物及其在医药中的用途
公开(公告)号：WO2008119715A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053594
申请日：2008-03-27
申请人： GLAXO GROUP LIMITED , 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 , C07D211/58
摘要： Compounds of formula (I) or a salt thereof are provided, wherein R 4 , R 5 , R 6 , Q 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和R如上定义在说明中。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。

10. 发明申请

WO2008119713A1 1- (1-CYCLOHEXYL-4-PIPERIDINYL) -1, 3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的1-（1-环辛基-4-哌啶基）-1,3-二氢-2H-苯并咪唑-2-酮衍生物及其在医药中的用途
公开(公告)号：WO2008119713A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053591
申请日：2008-03-27
申请人： GLAXO GROUP LIMITED , COOPER, David Gwyn , FORBES, Ian Thomson , GARZYA, Vincenzo , JIN, Jian , WYMAN, Paul Adrian
发明人： COOPER, David Gwyn , FORBES, Ian Thomson , GARZYA, Vincenzo , JIN, Jian , WYMAN, Paul Adrian
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4985 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of formula (I) or a salt thereof are provided, wherein X 1 , X 2 , X 3 , R 6 , Q 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X 1，X 2，X 3，R 6， / SUP>，Q和R如说明书中所定义。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。

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