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51. 发明申请

WO2004026866A1 N-AROYL CYCLIC AMINES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： N-亚油酸环化酶作为OREXIN受体拮抗剂
公开(公告)号：WO2004026866A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010412
申请日：2003-09-17
申请人： GLAXO GROUP LIMITED , BRANCH, Clive, Leslie , COULTON, Steven , JOHNS, Amanda , NASH, David, John , PORTER, Roderick, Alan , STEMP, Geoffrey
发明人： BRANCH, Clive, Leslie , COULTON, Steven , JOHNS, Amanda , NASH, David, John , PORTER, Roderick, Alan , STEMP, Geoffrey
IPC分类号： C07D417/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D417/14
摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及N-芳酰基环胺衍生物及其作为药物的用途。

52. 发明申请

WO2003051872A1 ETHYLENE DIAMINE DERIVATIVES AND THEIR USE AS OREXIN-RECEPTOR ANTAGONISTS 审中-公开
标题翻译：乙烯二胺衍生物及其作为OREXIN-RECEPTOR ANTAGONISTS的用途
公开(公告)号：WO2003051872A1
公开(公告)日：2003-06-26
申请号：PCT/GB2002/005665
申请日：2002-12-13
申请人： SMITHKLINE BEECHAM P.L.C. , COULTON, Steven , JOHNS, Amanda , PORTER, Roderick, Alan
发明人： COULTON, Steven , JOHNS, Amanda , PORTER, Roderick, Alan
IPC分类号： C07D417/12
CPC分类号： C07D403/12 , C07D417/12
摘要： This invention relates to heterocyclic substituted ethylene diamine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及杂环取代的乙二胺衍生物及其作为药物的用途。

53. 发明申请

WO03002559A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO03002559A2
公开(公告)日：2003-01-09
申请号：PCT/EP0207007
申请日：2002-06-25
申请人： SMITHKLINE BEECHAM PLC , CHAN WAI NGOR , JOHNS AMANDA , JOHNSON CHRISTOPHER NORBERT , NOVELLI RICCARDO , PORTER RODERICK ALAN
发明人： CHAN WAI NGOR , JOHNS AMANDA , JOHNSON CHRISTOPHER NORBERT , NOVELLI RICCARDO , PORTER RODERICK ALAN
IPC分类号： A61K31/427 , A61K31/4375 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/10 , A61P5/12 , A61P9/00 , A61P11/00 , A61P15/10 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , A61K31/4545
CPC分类号： C07D413/14 , C07D401/14 , C07D413/06 , C07D417/04 , C07D417/14 , C07D471/04
摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.
摘要翻译：本发明涉及N-芳酰基环胺衍生物及其作为药物的用途，特别是作为食欲素受体拮抗剂。

54. 发明申请

WO2002090355A1 N-AROYL CYCLIC AMINES 审中-公开
标题翻译： N-AROYL循环氨基酸
公开(公告)号：WO2002090355A1
公开(公告)日：2002-11-14
申请号：PCT/GB2002/002042
申请日：2002-05-02
申请人： SMITHKLINE BEECHAM P.L.C. , BRANCH, Clive, Leslie , COULTON, Steven , JOHNS, Amanda , JOHNSON, Christopher, Norbert , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin
发明人： BRANCH, Clive, Leslie , COULTON, Steven , JOHNS, Amanda , JOHNSON, Christopher, Norbert , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin
IPC分类号： C07D417/14
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： This invention relates to N -aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH 2 ) n , wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents O or 1; X is NR, wherein R is H or (C 1-4 )alkyl; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A 2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R 1 and further optional substituents; or Ar 2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R 1 represents hydrogen, optionally substituted (C 1-4 )alkoxy, halo, cyano, optionally substituted (C 1-6 )alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6- membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S; when Ar 1 is aryl p is not 1; or a pharmaceutical acceptable salt thereof.
摘要翻译：本发明涉及N，N-芳酰基环胺衍生物及其作为食欲素拮抗剂的用途，其中：Y表示键，氧或基团（CH 2）n，其中n表示1,2或3; m表示1,2或3; p表示0或1; X是NR，其中R是H或（C 1-4）烷基; Ar 1是芳基或含有至多3个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; A 2表示苯基或含有至多3个选自N，O和S的杂原子的5或6元杂环基，其中苯基或杂环基被R 1和另外任选的取代基取代; 或Ar 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示氢，任选取代的（C 1-4）烷氧基，卤素，氰基，任选取代的（C 1-6）烷基，任选取代的苯基或任选取代的含有至多4个杂原子的5-或6-元杂环基选自N，O和S; 当Ar 1是芳基p不为1时; 或其药学上可接受的盐。

55. 发明申请

WO0047580A3 PHENYL UREA AND PHENYL THIOUREA DERIVATIVES 审中-公开
标题翻译：苯乙酸和苯乙酸衍生物
公开(公告)号：WO0047580A3
公开(公告)日：2000-12-21
申请号：PCT/EP0001142
申请日：2000-02-10
申请人： SMITHKLINE BEECHAM PLC , COULTON STEVEN , JOHNS AMANDA , PORTER RODERICK ALAN
发明人： COULTON STEVEN , JOHNS AMANDA , PORTER RODERICK ALAN
IPC分类号： A61K31/4375 , A61K31/4725 , A61P1/04 , A61P1/08 , A61P3/04 , A61P3/10 , A61P5/06 , A61P5/10 , A61P5/14 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/02 , A61P13/08 , A61P13/12 , A61P15/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P35/00 , A61P37/08 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I) in which: one of X and Y is N and the other is CH; Z represents oxygen or sulfur; and R to R represent various substituent groups; and pharmaceutically acceptable salts thereof.
摘要翻译：式（I）化合物，其中：X和Y之一是N，另一个是CH; Z表示氧或硫; R 1〜R 7表示各种取代基; 及其药学上可接受的盐。

56. 发明申请

WO0008020A3 TRICYCLIC CARBOXAMIDES 审中-公开
标题翻译：三氯碳酰胺
公开(公告)号：WO0008020A3
公开(公告)日：2000-07-13
申请号：PCT/EP9905584
申请日：1999-08-03
申请人： SMITHKLINE BEECHAM PLC , COULTON STEVEN , NOVELLI RICCARDO , PORTER RODERICK ALAN , THOMPSON MERVYN , WARD ROBERT WILLIAM
发明人： COULTON STEVEN , NOVELLI RICCARDO , PORTER RODERICK ALAN , THOMPSON MERVYN , WARD ROBERT WILLIAM
IPC分类号： A61K31/4375 , A61K31/4745 , A61K31/55 , A61P9/10 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/10 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D455/03 , C07D471/04 , C07D471/14 , C07D487/04 , A61K31/437 , C07D455/04
CPC分类号： C07D455/00 , C07D471/04 , C07D471/14 , C07D487/04
摘要： Compounds of formula (I) or salt thereof or solvate thereof, in which: m is 1 or 2; n is 1 or 2; X is CH or N; Y is selected from hydrogen, halogen, cyano, CF3, alkyl or alkoxy; R , which may be at any position within the saturated ring system, is hydrogen or up to two substituents which may be the same or different and each of which is selected from fluoro and C1-6 alkyl; R is hydrogen or up to four substituents selected from halogen, NO2, CN, N3, CF3O-, CF3S-, CF3CO-, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO-, C1-6-alkylCO-, C3-6cycloalkylO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS-, C1-6alkylSO2-, (C1-4alkyl)2NSO2-, (C1-4alkyl)NHSO2-, (C1-4alkyl)2NCO-, oxazolyl, (C1-4alkyl)NHCO-, CONH2; or R CONH- or -NR R , wherein R is hydrogen or C1-4 alkyl; and R is hydrogen, C1-4alkyl, formyl, -CO2C1-4alkyl or -COC1-4alkyl; or two R groups are linked together form a carbocyclic or heterocyclic ring that is saturated or unsaturated and unsubstituted or substituted by -OH or =O are indicated to be useful in the treatment and pophylaxis of epilepsy, migraine, and other disorders.
摘要翻译：式（I）化合物或其盐或其溶剂合物，其中：m为1或2; n为1或2; X是CH或N; Y选自氢，卤素，氰基，CF 3，烷基或烷氧基; 可以在饱和环体系内的任何位置的R 1是氢或最多两个可以相同或不同的取代基，其各自选自氟和C 1-6烷基; R 2是氢或至多四个选自卤素，NO 2，CN，N 3，CF 3 O-，CF 3 S-，CF 3 CO-，C 1-6烷基，C 1-6烯基，C 1-6炔基，C 1-6全氟烷基，C 3-6环烷基， C 3-6烷基-C 1-4烷基 - ，C 1-6烷基O - ，C 1-6 - 烷基CO-，C 3-6环烷基O - ，C 3-6环烷基CO-，C 3-6环烷基-C 1-4烷基O - ，C 3-6环烷基-C 1-4烷基CO-，苯基，苯氧基，苄氧基，苯甲酰基，苯基-C 1-4烷基 - ，C 1-6烷基-S-，C 1-6烷基SO 2 - ，（C 1-4烷基）2NSO 2 - ，（C 1-4烷基）NHSO 2 - ，（C 1-4烷基）2 CO-，恶唑基，（C 1-4烷基）NHCO-，CONH 2; 或R 4 CONH-或-NR 4 R 5，其中R 4是氢或C 1-4烷基; 和R 5是氢，C 1-4烷基，甲酰基，-CO 2 C 1-4烷基或-COC 1-4烷基; 或两个R 2连接在一起形成饱和或不饱和且未被取代或被-OH或= O取代的碳环或杂环，可用于治疗和预防癫痫，偏头痛和其他疾病。

57. 发明申请

WO1993019754A1 PHENOL AND PYRIDINOL DERIVATIVES AS LUSITROPIC AGENTS 审中-公开
标题翻译：苯酚和吡啶衍生物作为助听剂
公开(公告)号：WO1993019754A1
公开(公告)日：1993-10-14
申请号：PCT/GB1993000615
申请日：1993-03-25
申请人： SMITHKLINE BEECHAM PLC , SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES , MURRAY, Kenneth, John , PORTER, Roderick, Alan , WARRINGTON, Brian, Herbert , LAHOURATATE, Philippe
发明人： SMITHKLINE BEECHAM PLC , SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES
IPC分类号： A61K31/44
CPC分类号： A61K31/675 , A61K31/44
摘要： Fused aryl derivatives are described as lusitropic agents for use in the treatment of cardiovascular disease where there is a component of diastolic failure.

58. 发明申请

WO1992006085A1 PHENYLPYRIDINOL DERIVATIVES AS MEDICAMENTS 审中-公开
标题翻译：苯基吡啶衍生物作为药物
公开(公告)号：WO1992006085A1
公开(公告)日：1992-04-16
申请号：PCT/GB1991001663
申请日：1991-09-26
申请人： SMITH KLINE & FRENCH LABORATORIES LIMITED , PORTER, Roderick, Alan , MURRAY, Kenneth, John , WARRINGTON, Brian, Herbert , PRAIN, Hunter, Douglas
发明人： SMITH KLINE & FRENCH LABORATORIES LIMITED
IPC分类号： C07D401/04
CPC分类号： C07D213/64 , C07D213/85 , C07D401/04
摘要： Phenylpyridinol derivatives are disclosed as medicaments.
摘要翻译：公开了苯基吡啶醇衍生物作为药物。

59. 发明申请

WO2010018213A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2010018213A2
公开(公告)日：2010-02-18
申请号：PCT/EP2009060514
申请日：2009-08-13
申请人： GLAXO GROUP LTD , PORTER RODERICK ALAN
发明人： PORTER RODERICK ALAN
CPC分类号： C07D231/20
摘要： The present invention relates to compounds, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of a condition wherein inhibition of GIyT1 would be beneficial, including neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder.
摘要翻译：本发明涉及化合物，其制备方法，药物组合物和含有它们的药物及其用于治疗其中抑制GlyT1将是有益的病症，包括神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷紊乱。

60. 发明申请

WO2009034062A1 COMPOUNDS WHICH INHIBIT THE GLYCINE TRANSPORTER AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：甘氨酸转运蛋白抑制剂及其在医药中的应用
公开(公告)号：WO2009034062A1
公开(公告)日：2009-03-19
申请号：PCT/EP2008/061890
申请日：2008-09-09
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , PORTER, Roderick, Alan
发明人： COOPER, David, Gwyn , PORTER, Roderick, Alan
IPC分类号： C07D401/10 , C07D403/10 , A61K31/4166 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D401/10 , C07D403/10
摘要： Compounds of Formula (I) and salts thereof are provided: wherein the groups are as defined in the specification. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：提供式（I）的化合物及其盐：其中基团如说明书中所定义。还公开了化合物作为药物的用途，以及用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物的制备。本发明还包括制备这些化合物及其药物制剂的方法。

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