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91. 发明申请

WO2002096907A1 BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES FOR USE AS ANTIBACTERIALS 审中-公开
标题翻译：用作抗菌剂的含二氧化氮的杂环衍生物
公开(公告)号：WO2002096907A1
公开(公告)日：2002-12-05
申请号：PCT/EP2002/005709
申请日：2002-05-24
申请人： SMITHKLINE BEECHAM P.L.C. , DARTOIS, Catherine, Genevieve, Yvette , MARKWELL, Roger, Edward , MADLER, Guy, Marguerite, Marie, Gerard , PEARSON, Neil, David
发明人： DARTOIS, Catherine, Genevieve, Yvette , MARKWELL, Roger, Edward , MADLER, Guy, Marguerite, Marie, Gerard , PEARSON, Neil, David
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
摘要翻译：哌啶衍生物及其药学上可接受的衍生物可用于哺乳动物，特别是人的细菌感染治疗方法。

92. 发明申请

WO2002094808A1 IMIDAZOLE-2-CARBOXAMIDE DERIVATIVES AS RAF KINASE INHIBITORS 审中-公开
标题翻译：咪唑-2-羧酰胺衍生物作为RAF激酶抑制剂
公开(公告)号：WO2002094808A1
公开(公告)日：2002-11-28
申请号：PCT/GB2002/002353
申请日：2002-05-20
申请人： SMITHKLINE BEECHAM P.L.C. , DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
发明人： DEAN, David, Kenneth , TAKLE, Andrew, Kenneth , WILSON, David, Matthew
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of formula (I): wherein X is O, CH 2 , S or NH, or the moiety X-R 1 is hydrogen; Y 1 and Y 2 independently represent CH or N; R 1 is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, arylC 1-6 alkyl, heterocyclyl, heterocyclylC 1-6 alkyl, heteroaryl, or heteroarylC 1-6 alkyl, any of which except hydrogen may be optionally substituted; R 2 and R 3 independently represent hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, arylC 1-6 alkyl, heteroaryl, heteroarylC 1-6 alkyl, heterocyclyl, or heterocyclylC 1-6 alkyl, or R 2 and R 3 together with the nitrogen atom to which they are attached form a 4- to 10-membered monocyclic or bicyclic ring; Ar is a group of the formula a) or b), wherein A represents a fused 5- to 7-membered ring optionally containing up to two heteroatoms selected from O, S and NR 5 , wherein R 5 is hydrogen or C 1-6 alkyl, which ring is optionally substituted by up to 2 substituents selected from halogen, C 1-6 alkyl, hydroxy, C 1-6 alkoxy or keto ; R a and R 4 are independently selected from hydrogen, halogen, C 1-6 alkyl, aryl, arylC 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, haloC 1-6 alkyl, arylC 1-6 alkoxy, hydroxy, nitro, cyano, azido, amino, mono- and di- N -)C 1-6 alkylamino, acylamino, arylcarbonylamino, acyloxy, carboxy, carboxy salts, carboxy esters, carbamoyl, mono- and di- N -C 1-6 alkylcarbamoyl, C 1-6 alkoxycarbonyl,aryloxycarbonyl, ureido, guanidino, C 1-6 alkylguanidino, amidino, C 1-6 alkylamidino, sulphonylamino, aminosulphonyl, C 1-6 alkylthio, C 1-6 alkyl sulphinyl or C 1-6 alkylsulphonyl; and one of X 1 and X 2 is N and the other is NR 6 , wherein R 6 is hydrogen, C 1-6 alkyl, or arylC 1-6 alkyl; or pharmaceutically acceptable salts thereof.
摘要翻译：式（I）化合物：其中X是O，CH 2，S或NH，或X-R 1部分是氢; Y1和Y2独立地表示CH或N; R 1是氢，C 1-6烷基，C 3-7环烷基，芳基，芳基C 1-6烷基，杂环基，杂环基C 1-6烷基，杂芳基或杂芳基C 1-6烷基，除氢之外的任何一个可以是任选取代的; R 2和R 3独立地表示氢，C 1-6烷基，C 3-7环烷基，芳基，芳基C 1-6烷基，杂芳基，杂芳基C 1-6烷基，杂环基或杂环基C 1-6烷基，或R 2和R 3 与它们所连接的氮原子一起形成4-至10-元单环或双环; Ar是式a）或b）的基团，其中A表示稠合的5-至7-元环，任选地含有至多两个选自O，S和NR 5的杂原子，其中R 5是氢或 C 1-6烷基，该环任选被至多2个选自卤素，C 1-6烷基，羟基，C 1-6烷氧基或酮的取代基取代; R a和R 4独立地选自氢，卤素，C 1-6烷基，芳基，芳基C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，卤代C 1-6烷基，芳基C 1-6烷氧基，羟基，硝基，氰基，叠氮基，氨基，单 - 和二 - N - C 1-6烷基氨基，酰氨基，芳基羰基氨基，酰氧基，羧基，羧基盐，羧基酯，氨基甲酰基，单 - 和二 - C 1-6烷基氨基甲酰基，C 1-6烷氧基羰基，芳氧基羰基，脲基，胍基，C 1-6烷基胍基，脒基，C 1-6烷基脒基，磺酰基氨基，氨基磺酰基，C 1-6烷硫基，C 1-6烷基亚磺酰基或C 1-6烷基磺酰基; X 1和X 2之一是N，另一个是NR 6，其中R 6是氢，C 1-6烷基或芳基C 1-6烷基; 或其药学上可接受的盐。

93. 发明申请

WO2002089800A3 N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2002089800A3
公开(公告)日：2002-11-14
申请号：PCT/EP2002/004874
申请日：2002-05-03
申请人： SMITHKLINE BEECHAM P.L.C. , GAILLARD, Pascale , JOHNSON, Christopher, Norbert , NOVELLI, Riccardo , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin, Michael
发明人： GAILLARD, Pascale , JOHNSON, Christopher, Norbert , NOVELLI, Riccardo , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin, Michael
IPC分类号： A61K31/445
摘要： This invention relates to N -aroyl cyclic amine derivatives of formula (I), 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 0 or 1; X is O, S C=O, SO 2 , or -CH=CH-; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 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 heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical acceptable salt thereof; and their use as pharmaceuticals, specifically as orexin receptor antagonists.

94. 发明申请

WO2002079151A1 3-SUBSTITUTED INDOELS OR FUSED PYRROLES AS ANTAGONISTS OF THE CHEMOKINE MCP-1 (CCR2B) RECEPTOR 审中-公开
标题翻译：作为化合物MCP-1（CCR2B）受体拮抗剂的3-取代的内含物或熔融的吡咯
公开(公告)号：WO2002079151A1
公开(公告)日：2002-10-10
申请号：PCT/EP2002/003570
申请日：2002-03-28
申请人： SMITHKLINE BEECHAM P.L.C. , GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , WITHERINGTON, Jason
发明人： GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , WITHERINGTON, Jason
IPC分类号： C07D209/14
CPC分类号： C07D451/02 , C07D401/04
摘要： Compounds of the formula (I) are antagonists of the chemokine MCP-1 (CCR2B) receptor and are of use in treating in inflammatory conditions with monocyte and/or lymphocyte involvement.
摘要翻译：式（I）的化合物是趋化因子MCP-1（CCR2B）受体的拮抗剂，并且可用于在单核细胞和/或淋巴细胞受累的炎性病症中治疗。

95. 发明申请

WO2002075474A2 COMPUTER APPLICATION FRAMEWORK 审中-公开
标题翻译：计算机应用框架
公开(公告)号：WO2002075474A2
公开(公告)日：2002-09-26
申请号：PCT/EP2002/002766
申请日：2002-03-13
申请人： SMITHKLINE BEECHAM P.L.C. , HUNTER, John, Robin
发明人： HUNTER, John, Robin
IPC分类号： G06F
CPC分类号： G06F9/547 , G06F9/465
摘要： An application framework supports at least one application that includes one or more application components. The framework includes a directory providing a logical definition of the application. The logical definition is referenced by an application context identifier and provides logical definitions of the application components that make ap the application. It further includes references to physical instances of the application components. An application component includes a harness that contains an application component code segment for a predetermined application context. The harness forms an interface between the application component code segment and an exterior of the application component. The harness is operable to apply a predetermined mapping for the application context to map between an external format for communication external to the application component and an internal format understandable to the application component code segment. In a particular example, LDAP is used as the directory protocol and XML is used to communicate between the framework and the application components and between application components.
摘要翻译：应用程序框架至少支持一个包含一个或多个应用程序组件的应用程序。该框架包括提供应用程序逻辑定义的目录。逻辑定义由应用程序上下文标识符引用，并提供使应用程序成为应用程序组件的逻辑定义。它还包括对应用程序组件的物理实例的引用。应用程序组件包括一个线束，其包含用于预定应用程序上下文的应用程序组件代码段。该线束形成应用程序组件代码段和应用程序组件外部之间的接口。该线束可操作以对应用上下文应用预定映射以在用于应用组件外部的通信的外部格式与可应用于应用组件代码段的内部格式之间进行映射。在一个特定示例中，LDAP用作目录协议，XML用于在框架和应用程序组件之间以及应用程序组件之间进行通信。

96. 发明申请

WO2002072536A1 UREA DERIVATIVES HAVING VANILLOID RECEPTOR (VR1) ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有VANILLOID受体（VR1）拮抗剂活性的尿素衍生物
公开(公告)号：WO2002072536A1
公开(公告)日：2002-09-19
申请号：PCT/GB2002/001046
申请日：2002-03-07
申请人： SMITHKLINE BEECHAM P.L.C. , RAMI, Harshad, Kantilal , THOMPSON, Mervyn , WYMAN, Paul, Adrian
发明人： RAMI, Harshad, Kantilal , THOMPSON, Mervyn , WYMAN, Paul, Adrian
IPC分类号： C07C275/40
CPC分类号： C07J63/008 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/42 , C07C323/44
摘要： The invention relates to novel compounds having Vanilloid Receptor (VR1) antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
摘要翻译：本发明涉及具有香草素受体（VR1）拮抗剂活性的新化合物，其制备方法，含有它们的组合物及其在治疗各种疾病中的用途。

97. 发明申请

WO2002040471A3 TETRAHYDROBENZAZEPINE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS (ANTIPSYCHOTIC AGENTS) 审中-公开
公开(公告)号：WO2002040471A3
公开(公告)日：2002-05-23
申请号：PCT/EP2001/013140
申请日：2001-11-12
申请人： SMITHKLINE BEECHAM P.L.C. , HADLEY, Michael, Stewart , LIGHTFOOT, Andrew, P. , MACDONALD, Gregor, James , STEMP, Geoffrey
发明人： HADLEY, Michael, Stewart , LIGHTFOOT, Andrew, P. , MACDONALD, Gregor, James , STEMP, Geoffrey
IPC分类号： C07D403/12
摘要： The invention provides compounds of formula (I), wherein R 1 -R 4 , A, B and t are as defined in claim 1. The compounds are modulators of dopamine D 3 receptors and have potential in the treatment of psychotic conditions (e.g. schizophrenia) or substance abuse.

98. 发明申请

WO2002040020A1 NOVEL USE OF CERTAIN INSULIN SENSITIZERS OR PPAR-GAMMA AGONISTS 审中-公开
标题翻译：某些胰岛素敏化剂或PPAR-GAMMA AGONISTS的新用途
公开(公告)号：WO2002040020A1
公开(公告)日：2002-05-23
申请号：PCT/GB2001/005044
申请日：2001-11-14
申请人： SMITHKLINE BEECHAM P.L.C. , BUCKINGHAM, Robin, Edwin
发明人： BUCKINGHAM, Robin, Edwin
IPC分类号： A61K31/427
CPC分类号： A61K31/427
摘要： A use of certain insulin sensitiser or a PPARγ agonist such as a compound of formula (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A 1 represents a substituted or unsubstituted aromatic heterocyclyl group; R 1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R 2 and R 3 each represent hydrogen, or R 2 and R 3 together represent a bond; A 2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6, for the manufacture of a medicament for treatment and/or prophylaxis of diseases associated with loss of bone mass, such as osteoporosis and related osteopenic diseases, Paget's disease, hyperparathyroidism and related diseases.
摘要翻译：使用某些胰岛素敏化剂或PPARγ激动剂如式（I）化合物或其互变异构体形式和/或其药学上可接受的盐，和/或其药学上可接受的盐，其中：A 1表示取代或未取代的芳族杂环基; R 1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; R 2和R 3各自表示氢，或者R 2和R 3一起表示键; A 2代表总共有五个取代基的苯环; 并且n表示2至6的整数，用于制备用于治疗和/或预防与骨量丧失相关的疾病如骨质疏松症和相关的骨质疏松症，佩吉特氏病，甲状旁腺功能亢进和相关疾病的药物。

99. 发明申请

WO2002036817A3 METHOD AND KIT TO DETERMINE LP-PLA2 POLYMORPHIC VARIANTS ASSOCIATED WITH SUSCEPTIBILITY TO ATHEROSCLEROSIS 审中-公开
公开(公告)号：WO2002036817A3
公开(公告)日：2002-05-10
申请号：PCT/GB2001/004876
申请日：2001-11-02
申请人： SMITHKLINE BEECHAM P.L.C. , CAMPBELL, David , MCGINNINS, Ralph , SPURR, Nigel, , VALDES, Ana, Maria
发明人： CAMPBELL, David , MCGINNINS, Ralph , SPURR, Nigel, , VALDES, Ana, Maria
IPC分类号： C12Q1/68
摘要： The invention relates to diagnostic methods and kits which are suitable for determining the presence, in a subject, of Lp-PLA 2 polymorphic variants which are assoicated with a higher incidence of atherosclerosis, and to the use of such methods and kits.

100. 发明申请

WO1998011067A1 PREPARATION OF 1-BUTYL-4-PIPERIDINYLMETHYLAMINE 审中-公开
标题翻译： 1-丁基-4-哌啶基甲基胺的制备
公开(公告)号：WO1998011067A1
公开(公告)日：1998-03-19
申请号：PCT/EP1997005167
申请日：1997-09-09
申请人： SMITHKLINE BEECHAM P.L.C. , FEDOULOFF, Michael , GUEST, David, William , SMITH, Gillian, Elizabeth
发明人： SMITHKLINE BEECHAM P.L.C.
IPC分类号： C07D211/26
CPC分类号： C07D211/26
摘要： A process for the preparation of 1-butyl-4-piperidinylmethylamine, which process comprises: i) the reaction of isonipecotamide and 1-bromobutane to give the N-butyl derivative of isonipecotamide; followed by ii) reduction with LiAlH4, characterised in that the reactions i) and ii) are carried out in toluene as solvent.
摘要翻译：一种制备1-丁基-4-哌啶基甲胺的方法，该方法包括：i）异壬酰胺与1-溴丁烷的反应得到异烟酰胺的N-丁基衍生物; 随后ii）用LiAlH 4还原，其特征在于反应i）和ii）在甲苯中作为溶剂进行。

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