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11. 发明申请

WO2006045615A1 4- (PYRAZINE-2-YL) -PYRROLIDINE-2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 4-（吡嗪-2-基） - 吡咯烷-2-羧酸化合物及其作为丙型肝炎病毒抑制剂的衍生物
公开(公告)号：WO2006045615A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/011542
申请日：2005-10-24
申请人： GLAXO GROUP LIMITED , GUIDETTI, Rossella , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , NEROZZI, Fabrizio , SMITH, Stephen, Allan
发明人： GUIDETTI, Rossella , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , NEROZZI, Fabrizio , SMITH, Stephen, Allan
IPC分类号： C07D417/14 , A61K31/427 , A61P31/12
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia) wherein: A represents hydroxy; B represents C(O)R 3 wherein R 3 is 4-tert-butyl-3-methoxyphenyl; D represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-2-ylmethyl, 1,3-thiazol-4-ylmethyl, 1,2-thiazol-3-ylmethyl, or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl, processes for their preparation and their use in HCV treatment are provided.
摘要翻译：式（Ia）的抗病毒剂，其中：A表示羟基; B表示C（O）R 3，其中R 3是4-叔丁基-3-甲氧基苯基; D代表1,3-噻唑-2-基或5-甲基-1,3-噻唑-2-基; E表示吡嗪-2-基; G表示1,3-噻唑-2-基甲基，1,3-噻唑-4-基甲基，1,2-噻唑-3-基甲基或1H-吡唑-1-基甲基; 及其盐，溶剂化物和酯; 条件是当A被酯化形成-OR时，其中R选自直链或支链烷基，芳烷基，芳氧基烷基或芳基，则R不是叔丁基，提供其制备方法及其在HCV治疗中的用途。

12. 发明申请

WO2002096886A1 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2002096886A1
公开(公告)日：2002-12-05
申请号：PCT/GB2002/002408
申请日：2002-05-23
申请人： GLAXO GROUP LIMITED , GREEN, Jennifer Margaret , BRAVI, Gianpaolo , CARTER, Malcolm , HARTLEY, Charles, David , NAYLOR, Alan , PASS, Martin , PAYNE, Jeremy, John , PEGG, Neil, Anthony
发明人： BRAVI, Gianpaolo , CARTER, Malcolm , HARTLEY, Charles, David , NAYLOR, Alan , PASS, Martin , PAYNE, Jeremy, John , PEGG, Neil, Anthony
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D401/12 , C07D405/12 , C07D409/12
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R 1 and R 2 are independently selected from the group consisting of H, C 1-6 alkyl, C 1-2 alkyl substituted by one to five fluorine atoms, C 3-6 alkenyl, C 3-6 alkynyl, C 3 -cycloalkylC 0-6 alkyl, C 4-12 bridged cycloalkyl, A(CR 7 R 8 ) n and B(CR 7 R 8 ) n ; R 3 is selected from the group consisting of C 1-6 alkyl, NH 2 and R 10 CONH; R 4 is C 1-2 alkyl substituted by one to five fluorine atoms; R 5 is selected from the group consisting of H, C 1-4 alkyl, C 1-2 alkyl substituted with one to five fluorine atoms, halogen and C 3-10 cycloalkylC 0-6 alkyl, with the proviso that when R 6 is H R 5 is not H. R 6 is selected from the group consisting of H, C 1-4 alkyl, C 1-2 alkyl substituted with one to five fluorine atoms, halogen, C 1-4 alkoxy, CN, NO 2 , C 1-6 alkylOCO, NH 2 CO C 1-6 alkylNHCO, NH 2 , C 1-6 alkylNH, (C 1-6 alkyl) 2 N, (C 1-6 alkyl) 2 NCO, C 1-6 alkylCONH, NH 2 SO 2 , C 1-6 alkylNHSO 2 (C 1-6 alkyl) 2 NSO 2 , C 1-6 alkylSO 2 NH, ArSO 2 NH, C 1-6 alkylSO 2 , ArSO 2 , C 3-10cycloalkylC¿0-6 alkyl, C 3-6 alkenyl and C 3-6 alkynyl, with the proviso that when R 5 is H R 6 is not H. R 7 and R 8 are independently selected from H or C 1-6 alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R 9 is selected from the group consisting of hydroxy, halogen, C 1-6 alkyl, C 1-6 alkyl substituted by one mor fluorine atoms, C 1-6 alkoxy, C 1-6 alkoxy substituted by one or more F, NH 2 SO 2 and C 1-6 alkylSO 2 ; R 10 is selected from the group consisting of H, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylOC 1-6 alkyl, phenyl, HO 2 CC 1-6 alkyl, C 1-6 alkylOCOC 1-6 alkyl, C 1-6 alkylOCO, H 2 NC 1-6 alkyl, C 1-6 alkylOCONHC 1-6 alkyl and C 1-6 alkylCONHC 1-6 alkyl; B is selected from the group consisting of (II) and where (III) defines the point of attachmnent of the ring; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of pain, fever and inflammation of a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐，其中：R 1和R 2独立地选自H，C 1-6烷基，被1至5个取代的C 1-2烷基氟原子，C 3-6烯基，C 3-6炔基，C 3-环烷基C 1-6烷基，C 4-12桥环烷基，A（CR 7 R 8）n和B（CR 7 R 8）n; R 3选自C 1-6烷基，NH 2和R 10 CONH; R 4是被1至5个氟原子取代的C 1-2烷基; R 5选自H，C 1-4烷基，被1至5个氟原子取代的C 1-2烷基，卤素和C 3-10环烷基C 1-6烷基，条件是当R 6为HR 5时，不是H.R 6选自H，C 1-4烷基，被1至5个氟原子取代的C 1-2烷基，卤素，C 1-4烷氧基，CN，NO 2，C 1-6烷基COO，NH 2 CO C 1-6烷基NHCO ，C 1-6烷基NH，（C 1-6烷基）2 N，（C 1-6烷基）2 CO，C 1-6烷基CONH，NH 2 SO 2，C 1-6烷基NHSO 2（C 1-6烷基）2 NSO 2，C 1-6烷基SO 2 NH，ArSO 2 NH，C 1-6烷基SO 2，ArSO 2， -10个环烷基C 0-6烷基，C 3-6烯基和C 3-6炔基，条件是当R 5是HR 6不是H. R 7和R 8独立地选自H或C 1-6烷基; A是未取代的5-或6-元杂芳基或未取代的6-元芳基，或被一个或多个R 9取代的5-或6-元杂芳基或6-元芳基选自羟基，卤素，C 1-6烷基，被一个氟原子取代的C 1-6烷基，C 1-6烷氧基，被一个或多个F，NH 2 SO 2和C 1-6烷基SO 2取代的C 1-6烷氧基; R 10选自H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基C 1-6烷基，苯基，HO 2 CCl 1-6烷基，C 1-6烷基COC 1-6烷基，C 1-6烷基COO，H 2 NC 1-6烷基，C 1-6烷基OCONHC 1 -6-烷基和C 1-6烷基CONHC 1-6烷基; B选自（II），其中（III）定义环的附着点; 并且n为0至4.式（I）化合物是COX-2的有效和选择性抑制剂，并且可用于治疗各种病症和疾病的疼痛，发热和炎症。

13. 发明申请

WO1997021666A1 ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS 审中-公开
标题翻译：芳香胺衍生物及其作为原子反应的激动剂使用
公开(公告)号：WO1997021666A1
公开(公告)日：1997-06-19
申请号：PCT/EP1996005470
申请日：1996-12-06
申请人： GLAXO GROUP LIMITED , HARTLEY, Charles, David , CARTER, Malcolm, Clive , FOXTON, Michael, Walter
发明人： GLAXO GROUP LIMITED
IPC分类号： C07C229/42
CPC分类号： C07D257/04 , C07C229/42 , C07C229/46 , C07C237/20 , C07C275/40 , C07C309/24 , C07C311/35 , C07C2601/08 , C07F9/3882
摘要： The present invention relates to phenethanolamine derivatives of formula (I), wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the aromatic ring may be optionally substituted by up to four substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents CO2R , C1-6alkylCO2R , CONR R , NHCONR R , SO2NHR , P(O)(OR )2, SO3H, C1-6alkylSO3H, NHSO2R , NHCOR or tetrazol-5-yl; R and R independently represent hydrogen, C1-6alkyl, trifluoromethyl, CN, OH, CO2R , CH2CO2R , or R and R form a 5-6 membered cycloalkyl ring; R represents hydrogen, or C1-6alkyl; R represents hydrogen, C1-6alkyl, or C1-6alkylOR ; R , R , R , R -R , and R -R each independently represent hydrogen, or C1-6alkyl; R represents C1-6alkyl or trifluoromethyl; R represents C1-6alkyl or trifluoromethyl; with the proviso that when R and R are both hydrogen, R is other than hydrogen; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
摘要翻译：本发明涉及式（I）的苯乙醇胺衍生物，其中R 1表示任选被一个或多个选自卤素，羟基，C 1-6烷氧基，C 1-6烷基，硝基，氰基，羟甲基和三氟甲基的取代基取代的芳基 ; R 2表示氢或C 1-6烷基; R 3表示芳基可以任选被至多四个选自C 1-6烷基，卤素，三氟甲基和C 1-6烷氧基的取代基取代的基团（A）; R 4表示氢或C 1-6烷基; R 5表示CO 2 R 8，C 1-6烷基CO 2 R 16，CONR 9 R 10，NHCONR 11 R 12，SO 2 NHR 13，P（O）（OR 14） 2，SO 3 H，C 1-6烷基SO 3 H，NHSO 2 R 15，NHCOR 17或四唑-5-基; R 6和R 7独立地表示氢，C 1-6烷基，三氟甲基，CN，OH，CO 2 R 18，CH 2 CO 2 R 19或R 6和R 7形成5-6元环烷基环; R 8表示氢或C 1-6烷基; R 9表示氢，C 1-6烷基或C 1-6烷基OR 20; R 10，R 11，R 12，R 14 -R 16和R 18 -R 20各自独立地表示氢或C 1-6烷基; R 13表示C 1-6烷基或三氟甲基; R 17表示C 1-6烷基或三氟甲基; 条件是当R 6和R 7都是氢时，R 8不是氢; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。

14. 发明申请

WO1992012160A1 BRIDGED CYCLIC KETAL DERIVATIVES 审中-公开
标题翻译： BRIDGED循环酮衍生物
公开(公告)号：WO1992012160A1
公开(公告)日：1992-07-23
申请号：PCT/EP1992000019
申请日：1992-01-07
申请人： GLAXO GROUP LIMITED , SIDEBOTTOM, Philip, James , HARTLEY, Charles, David , PROCOPIOU, Panayiotis, Alexandrou , LESTER, Michael, George , WATSON, Nigel, Stephen , KIRK, Barrie, Edward , COX, Brian , ROBERTS, Suzanne, Elaine , ROSS, Barry, Clive
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D493/08
CPC分类号： C07D493/08 , C07H9/04 , C07H19/01 , C12P17/181
摘要： These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

15. 发明申请

WO2009000818A1 3-CARBONYLAMINOTHIOPHENE-2-CARBOXYLIC ACIDS AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译：作为丙型肝炎病毒抑制剂的3-羰基亚氨基二羟基-2-羧酸
公开(公告)号：WO2009000818A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/057984
申请日：2008-06-24
申请人： SMITHKLINE BEECHAM CORPORATION , HARRISON, David , HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SLATER, Martin John
发明人： HARRISON, David , HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SLATER, Martin John
IPC分类号： C07D487/04 , A61K31/381 , A61K31/519 , A61P31/12
CPC分类号： C07D487/02 , C07D333/36 , C07D403/10 , C07D487/12
摘要： The present invention relates to novel 2-carboxy thiophene compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine, as anti-viral agents. Specifically, the present invention relates to compounds as inhibitors of Hepatitis C Virus (HCV) replication.
摘要翻译：本发明涉及式（I）的新型2-羧基噻吩化合物及其盐，其含有它们的药物组合物及其在医药中的用途作为抗病毒剂。具体地，本发明涉及作为丙型肝炎病毒（HCV）复制抑制剂的化合物。

16. 发明申请

WO2007088148A1 DERIVATIVES OF THIOPHENE CARBOXILIC ACID AS ANTIVIRAL AGENT 审中-公开
标题翻译：硫代羧酸作为抗病毒剂的衍生物
公开(公告)号：WO2007088148A1
公开(公告)日：2007-08-09
申请号：PCT/EP2007/050823
申请日：2007-01-29
申请人： SMITHKLINE BEECHAM CORPORATION , HARTLEY, Charles, David , MORDAUNT, Jacqueline, Elizabeth , SHAH, Pritom , SLATER, Martin, John
发明人： HARTLEY, Charles, David , MORDAUNT, Jacqueline, Elizabeth , SHAH, Pritom , SLATER, Martin, John
IPC分类号： C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/04 , A61K31/41 , A61K31/435 , A61K31/495 , A61P31/00
CPC分类号： C07D413/14 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D491/04
摘要： Anti-viral agents of compounds of Formuta (I) : wherein A, R 1 , R 2 and R 3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.
摘要翻译： Formuta（I）化合物的抗病毒剂：其中A，R 1，R 2和R 3如本说明书中所定义提供其制备方法及其在HCV治疗中的应用。

17. 发明申请

WO2002062794A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2002062794A2
公开(公告)日：2002-08-15
申请号：PCT/EP2002/000939
申请日：2002-01-30
申请人： GLAXO GROUP LIMITED , GELLIBERT, Françoise, Jeanne , HARTLEY, Charles, David , MATHEWS, Neil , WOOLVEN, James, Michael
发明人： GELLIBERT, Françoise, Jeanne , HARTLEY, Charles, David , MATHEWS, Neil , WOOLVEN, James, Michael
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Therapeutically active pyrazole derivatives of formula (I) wherein R 1 -R 3 are as defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor β (TGF-β), and pharmaceutical compositions for use in such therapy.
摘要翻译：其中R 1 -R 3如说明书中所定义的式（I）的治疗活性吡唑衍生物，其制备方法，其在治疗中的用途，特别是用于治疗或预防特征在于转化生长因子β（TGF-β）过表达的病症，以及用于这种治疗的药物组合物。

18. 发明申请

WO2002062776A1 2-AMINO-4-(PYRIDIN-2-YL)-THIAZOLE DERIVATIVES AS TRANSFORMING GROWTH FACTOR BETA (TGF-BETA) INHIBITORS 审中-公开
标题翻译：作为转化生长因子β（TGF-βA）抑制剂的2-氨基-4-（吡啶-2-基） - 噻唑衍生物
公开(公告)号：WO2002062776A1
公开(公告)日：2002-08-15
申请号：PCT/EP2002/000940
申请日：2002-01-30
申请人： GLAXO GROUP LIMITED , GELLIBERT, Francoise, Jeanne , HARTLEY, Charles, David , MATHEWS, Neil , WOOLVEN, James, Michael
发明人： GELLIBERT, Francoise, Jeanne , HARTLEY, Charles, David , MATHEWS, Neil , WOOLVEN, James, Michael
IPC分类号： C07D277/42
CPC分类号： C07D417/14 , C07D471/04
摘要： Therapeutically active thiazole derivatives of formula (I) wherein R 1 , R 2 , X and X ' are as defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor β (TGF-β), and pharmaceutical compositions for use in such therapy. (I)
摘要翻译：其中R 1，R 2，X和X'如本说明书中所定义的式（I）的治疗活性噻唑衍生物，其制备方法，其在治疗中的用途，特别是在治疗或预防转化生长因子β（TGF-β）过表达的疾病，以及用于此类治疗的药物组合物。（一世）

19. 发明申请

WO2008017688A1 2-CARBOXY THIOPHENE DERIVATIVES AS ANTI-VIRAL AGENTS 审中-公开
标题翻译： 2-羧基噻吩衍生物作为反病毒剂
公开(公告)号：WO2008017688A1
公开(公告)日：2008-02-14
申请号：PCT/EP2007/058231
申请日：2007-08-08
申请人： SMITHKLINE BEECHAM CORPORATION , HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SHAH, Pritom , SLATER, Martin John
发明人： HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SHAH, Pritom , SLATER, Martin John
IPC分类号： A61K31/519 , C07D487/04 , C07D491/048 , C07D498/04 , C07D513/04 , A61K31/4353 , A61P31/12
CPC分类号： C07D487/04 , C07D491/048 , C07D498/04 , C07D513/04
摘要： Anti-viral agents of compounds of Formula (I) wherein A, R 1 , R 2 and R 3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.
摘要翻译：其中A，R 1，R 2和R 3的式（I）化合物的抗病毒剂如说明书中所定义，提供了其制备方法及其在HCV治疗中的应用。

20. 发明申请

WO2006045613A1 4-METHOXYMETHYL-PYRROLIDINE-2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS 审中-公开
标题翻译： 4-甲氧基甲基 - 吡咯烷-2-羧酸化合物及其作为丙型肝炎病毒抑制剂的衍生物
公开(公告)号：WO2006045613A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/011532
申请日：2005-10-24
申请人： GLAXO GROUP LIMITED , GUIDETTI, Rossella , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , NEROZZI, Fabrizio , SMITH, Stephen, Allan
发明人： GUIDETTI, Rossella , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , NEROZZI, Fabrizio , SMITH, Stephen, Allan
IPC分类号： C07D417/14 , A61K31/427 , A61P31/12
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (la) wherein: A represents hydroxy; D represents 4-tert-butyl-3-methoxyphenyl; E represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl; G represents methoxymethyl; J represents 1,3 thiazol-2-ylmethyl, 1,3-thiazol-4-ylmethyl, 1,2-thiazol-3-ylmethyl, or 1H-pyrazol-1-ylmethyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert- butyl; processes for their preparation and their use in HCV treatment are provided.
摘要翻译：式（Ia）的抗病毒剂其中：A代表羟基; D表示4-叔丁基-3-甲氧基苯基; E表示1,3-噻唑-2-基或5-甲基-1,3-噻唑-2-基; G表示甲氧基甲基; J代表1,3-噻唑-2-基甲基，1,3-噻唑-4-基甲基，1,2-噻唑-3-基甲基或1H-吡唑-1-基甲基; 及其盐，溶剂化物和酯; 条件是当A被酯化形成-OR时，其中R选自直链或支链烷基，芳烷基，芳氧基烷基或芳基，则R不是叔丁基;其制备及其在HCV中的用途提供治疗。

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