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1. 发明申请

WO2008059042A1 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：WO2008059042A1
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062431
申请日：2007-11-15
申请人： SMITHKLINE BEECHAM CORPORATION , GRIMES, Richard Martin , HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SHAH, Pritom , SLATER, Martin John , WHITE, Gemma Victoria
发明人： GRIMES, Richard Martin , HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SHAH, Pritom , SLATER, Martin John , WHITE, Gemma Victoria
IPC分类号： C07D409/04 , C07D409/10 , C07D409/12
CPC分类号： C07D417/12 , C07D333/38 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
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：式（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。

2. 发明申请

WO2008043791A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2008043791A2
公开(公告)日：2008-04-17
申请号：PCT/EP2007/060779
申请日：2007-10-10
申请人： SMITHKLINE BEECHAM CORPORATION , HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SHAH, Pritom , SLATER, Martin John , WHITE, Gemma Victoria
发明人： HARTLEY, Charles David , MORDAUNT, Jacqueline Elizabeth , SHAH, Pritom , SLATER, Martin John , WHITE, Gemma Victoria
IPC分类号： C07D409/12 , C07D471/04 , C07D491/04 , C07D513/04 , A61K31/381 , A61K31/395 , A61P31/12
CPC分类号： C07D409/12 , C07D471/04 , C07D491/04 , 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：式（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。

3. 发明申请

WO2007039145A1 C (2) -HETEROARYLMETHYL-C (4) -PYRAZINYL-2-YL ACYL PYRROLIDINE COMPOUNDS AND THEIR USE FOR TREATING VIRAL INFECTIONS, ESPECIALLY HEPATITIS C VIRUS 审中-公开
标题翻译： C（2）-HETEROARYLMETHYL-C（4） - 吡嗪-2-基乙酰吡咯烷酮化合物及其用于治疗病毒性感染，特别是丙型肝炎病毒
公开(公告)号：WO2007039145A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009237
申请日：2006-09-21
申请人： GLAXO GROUP LIMITED , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , LAZARIDES, Linos , NEROZZI, Fabrizio , SMITH, Stephen, Allan
发明人： HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , LAZARIDES, Linos , NEROZZI, Fabrizio , SMITH, Stephen, Allan
IPC分类号： C07D417/14 , A61K31/427 , A61P31/14
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia) : wherein A represents hydroxy; B represents -C(O)R 3 ; D represents 1,3-thiazol-2-yl or 5-methylisoxazol-3-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-4-ylmethyl or 1H-pyrazol-1-ylmethyl; R 3 represents 3-bromo-4-tert-butylphenyl or 5-bromo-4- tert -butyl-2-fluorophenyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from branched chain alkyl, 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; D代表1,3-噻唑-2-基或5-甲基异恶唑-3-基; E表示吡嗪-2-基; G表示1,3-噻唑-4-基甲基或1H-吡唑-1-基甲基; R 3表示3-溴-4-叔丁基苯基或5-溴-4-叔丁基-2-氟苯基; 及其盐，溶剂化物和酯; 条件是当A被酯化形成-OR时，其中R选自支链烷基，则R不是叔丁基，提供其制备方法及其在HCV治疗中的用途。

4. 发明申请

WO2007039143A1 C (2) -HETEROARYLMETHYL-C (4) -PYRAZIN-2-YL ACYL PYRROLIDINE COMPOUNDS AND THEIR USER FOR TREATING VIRAL INFECTIONS, ESPECIALLY HEPATITICS C (HCV) 审中-公开
标题翻译： C（2）-HETEROARYLMETHYL-C（4）-PYRAZIN-2-YL ACYL吡咯啉化合物及其用于治疗病毒感染的用户，特别是丙型肝炎病毒（HCV）
公开(公告)号：WO2007039143A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009235
申请日：2006-09-21
申请人： GLAXO GROUP LIMITED , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , LAZARIDES, Linos , NEROZZI, Fabrizio , SMITH, Stephen, Allan
发明人： HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , LAZARIDES, Linos , NEROZZI, Fabrizio , SMITH, Stephen, Allan
IPC分类号： C07D417/14 , A61K31/4025 , 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 ; D represents 1,3-thiazol-2-yl; E represents pyrazin-2-yl; G represents 1,3-thiazol-4-ylmethyl or 1H-pyrazol-1-ylmethyl; R 3 represents 4- tert -butyl-3-ethenylphenyl or 4-tert-butyl-5-ethenyl-2-fluorophenyl; and salts, solvates and esters thereof; provided that when A is esterified to form -OR where R is selected from branched chain alkyl, 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; D表示1,3-噻唑-2-基; E表示吡嗪-2-基; G表示1,3-噻唑-4-基甲基或1H-吡唑-1-基甲基; R 3表示4-叔丁基-3-乙烯基苯基或4-叔丁基-5-乙烯基-2-氟苯基; 及其盐，溶剂化物和酯; 条件是当A被酯化形成-OR，其中R选自支链烷基时，则R不是叔丁基，提供其制备方法及其在HCV治疗中的用途。

5. 发明申请

WO2004096210A1 ACYLATED INDOLINE AND TETRAHYDROQUINOLINE DERIVATIVES AS HCV INHIBITORS 审中-公开
标题翻译：作为HCV抑制剂的ACYLATED INDOLINE ANDTETRAHYDROQUINOLINE DERIVITIVES
公开(公告)号：WO2004096210A1
公开(公告)日：2004-11-11
申请号：PCT/EP2004/004663
申请日：2004-04-29
申请人： GLAXO GROUP LIMITED , BRAVI, Gianpaolo , GRIMES, Richard, Martin , GUIDETTI, Rossella , HAIGH, David , HARTLEY, Charles, David , MORDAUNT, Jacqueline, Elizabeth , SHAH, Pritom , SLATER, Martin, John
发明人： BRAVI, Gianpaolo , GRIMES, Richard, Martin , GUIDETTI, Rossella , HAIGH, David , HARTLEY, Charles, David , MORDAUNT, Jacqueline, Elizabeth , SHAH, Pritom , SLATER, Martin, John
IPC分类号： A61K31/404
CPC分类号： C07D401/04 , C07D209/42 , C07D215/48 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12
摘要： Use of a compound of Formula (I) : wherein: R 1 represents hydroxy or NR B R C ; R 2 represents C 1-6 alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; R 3 represents aryl or heteroaryl; R 4 represents one or two substituents independently selected from hydrogen, C 1-6 alkyl, halo, OR A , C(O)NR B R C , C(O)R D , CO 2 H , CO 2 R D , NR B R C , NR E C(O)R D , NR E CO 2 R D , NR E C(O)NR F R G , NR E SO 2 R D , SO 2 NR F R G , SO 2 R D , nitro, cyano, heterocyclyl, heteroaryl, aryl, arylalkyl heteroarylalkyl or CF 3 ; R 5 and R 6 independently represent hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R 7 and R 8 independently represent hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n represents 0 or 1; R A represents hydrogen, C 1-6 alkyl, arylalkyl, heteroarylalkyl, aryl or heteroaryl; R B and R C independently represent hydrogen, C 1-6 alkyl, aryl or heteroaryl; or R B and R C together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; R D is selected from the group consisting of C 1-6 alkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; R E represents hydrogen or C 1-6 alkyl; R F and R G are independently selected from the group consisting of hydrogen, C 1-6 alkyl, aryl, heteroaryl, arylalkyl, and heteroarylalkyl; or R F and R G together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; and salts, solvates and esters thereof; provided that when R 1 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; in the manufacture of a medicament for the treatment of viral infection is provided. Also provided are certain novel compounds of Formula (I) represented by Formula (Ib). Further provided are processes for the preparation of compounds of Formula (I), pharmaceutical compositions comprising them, and methods of using them in HCV treatment.
摘要翻译：式（I）化合物的用途：其中：R 1表示羟基或NR B; R 2表示C 1-6烷基，杂环基烷基，芳烷基或杂芳基烷基; R 3表示芳基或杂芳基; R 4表示一个或两个独立地选自氢，C 1-6烷基，卤素，OR A，C（O）NR B，C（O）R D，CO 2 H，CO 2 R NR（R）R C，NR C（O）R D，NR E 2 CO 2 R D，NR C（O）NR F SO 2 R D，SO 2 R R，SO 2 R 6，硝基，氰基，杂环基，杂芳基，芳基，芳基烷基杂芳基烷基或CF 3; R 5和R 6独立地表示氢，C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; R 7和R 8独立地表示氢，C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; n表示0或1; R A表示氢，C 1-6烷基，芳基烷基，杂芳基烷基，芳基或杂芳基; R B和R C独立地表示氢，C 1-6烷基，芳基或杂芳基; 或R B和R C与它们所连接的氮原子一起形成5或6元饱和的环状基团; R D选自C 1-6烷基，芳基，杂芳基，芳基烷基和杂芳基烷基; R E表示氢或C 1-6烷基; R F和R G独立地选自氢，C 1-6烷基，芳基，杂芳基，芳基烷基和杂芳基烷基; 或R F和R G与它们所连接的氮原子一起形成5或6元饱和的环状基团; 及其盐，溶剂化物和酯; 条件是当R 1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; 在制备用于治疗病毒感染的药物中。还提供某些由式（Ib）表示的式（I）的新化合物。还提供了制备式（I）化合物，包含它们的药物组合物的方法和在HCV治疗中使用它们的方法。

6. 发明申请

WO02062794A3 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO02062794A3
公开(公告)日：2002-10-03
申请号：PCT/EP0200939
申请日：2002-01-30
申请人： GLAXO GROUP LTD , 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： A61K31/444 , A61P1/16 , A61P13/12 , A61P19/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D471/04 , A61K31/4375
CPC分类号： C07D471/04
摘要： Therapeutically active pyrazole derivatives of formula (I) wherein R -R 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 beta (TGF- beta ), and pharmaceutical compositions for use in such therapy.
摘要翻译：式（I）的治疗活性吡唑衍生物，其中R 1 -R 3如说明书中所定义，其制备方法，其在治疗中的用途，特别是在治疗或预防特征为过表达的转化生长因子β（TGF-β）和用于这种治疗的药物组合物。

7. 发明申请

WO0138311A3 PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITORS OF COX-2 审中-公开
标题翻译：作为COX-2的选择性抑制剂的吡嗪衍生物
公开(公告)号：WO0138311A3
公开(公告)日：2001-11-01
申请号：PCT/EP0011673
申请日：2000-11-23
申请人： GLAXO GROUP LTD , GREEN RICHARD HOWARD , HARTLEY CHARLES DAVID , NAYLOR ALAN , PAYNE JEREMY JOHN , PEGG NEIL ANTHONY
发明人： GREEN RICHARD HOWARD , HARTLEY CHARLES DAVID , NAYLOR ALAN , PAYNE JEREMY JOHN , PEGG NEIL ANTHONY
IPC分类号： A61K31/505 , A61P1/00 , A61P1/02 , A61P1/04 , A61P3/02 , A61P3/10 , A61P5/00 , A61P5/14 , A61P9/00 , A61P9/10 , A61P11/16 , A61P13/12 , A61P15/06 , A61P15/08 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/02 , A61P29/00 , A61P29/02 , A61P31/12 , A61P31/16 , A61P31/18 , A61P35/00 , A61P35/04 , A61P43/00 , C07D239/42
CPC分类号： C07D239/42
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R and R are independently selected from H, C1-6alkyl, C2-6alkenyl, C3-6alkynyl, C3-10cycloalkylC0-6alkyl or C4-12bridged cycloalkane; and R is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, 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衍生物，其中：R 1和R 2独立地选自H，C 1-6烷基，C 2-6烯基，C 3-6炔基，C 3-10环烷基C 0〜 C6烷基或C4-12桥连环烷烃; 和R 3是C 1-6烷基或NH 2。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

8. 发明申请

WO1995001170A2 USE OF PHENETHANOLAMINE DERIVATIVES IN THE TREATMENT OF GASTROINTESTINAL DISORDERS 审中-公开
标题翻译：苯乙醇胺衍生物在治疗胃肠疾病中的应用
公开(公告)号：WO1995001170A2
公开(公告)日：1995-01-12
申请号：PCT/EP1994002106
申请日：1994-06-29
申请人： GLAXO GROUP LIMITED , STORER, Richard , FOXTON, Michael, Walter , HARTLEY, Charles, David , GREEN, Richard, Howard , TRAVERS, Stuart
发明人： GLAXO GROUP LIMITED
IPC分类号： A61K31/165
CPC分类号： A61K31/195 , A61K31/135
摘要： The use of compounds of formula (I) in which: R is hydrogen, methyl or hydroxymethyl; R is substituted alkyl; R and R are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl group, or substituted alkyl; X is oxygen or sulphur; and Ar is optionally substituted phenyl or naphtyl; and pharmaceutically acceptable salts thereof in the treatment of gastrointestinal disorders is described.
摘要翻译：式（I）化合物的用途，其中：R 0是氢，甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自为氢，卤素，羟基，烷氧基，羧基，烷氧基羰基，烷基，硝基，卤代烷基或取代的烷基; X是氧或硫; 和Ar是任选取代的苯基或萘基; 和其药学上可接受的盐在治疗胃肠道疾病中的用途。

9. 发明申请

WO2007071434A1 ANTIVIRAL 2-CARBOXY-THIOPHENE COMPOUNDS 审中-公开
标题翻译：有害的2-羧基 - 噻吩化合物
公开(公告)号：WO2007071434A1
公开(公告)日：2007-06-28
申请号：PCT/EP2006/012442
申请日：2006-12-20
申请人： SMITHKLINE BEECHAM CORPORATION , CORFIELD, John, Andrew , GRIMES, Richard, Martin , HARRISON, David , HARTLEY, Charles, David , HOWES, Peter, David , LE, Joelle , MEESON, Malcolm, Lees , MORDAUNT, Jacqueline, Elizabeth , SHAH, Pritom , SLATER, Martin, John , WHITE, Gemma, Victoria
发明人： CORFIELD, John, Andrew , GRIMES, Richard, Martin , HARRISON, David , HARTLEY, Charles, David , HOWES, Peter, David , LE, Joelle , MEESON, Malcolm, Lees , MORDAUNT, Jacqueline, Elizabeth , SHAH, Pritom , SLATER, Martin, John , WHITE, Gemma, Victoria
IPC分类号： C07D409/10 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D498/04 , C07D513/04 , A61K31/423 , A61K31/429 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/4355
CPC分类号： C07D409/10 , C07D333/70 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04 , 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：式（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。

10. 发明申请

WO2007039144A1 PYRROLIDINE DERIVATIVES FOR TREATING VIRAL INFECTIONS 审中-公开
标题翻译：吡咯啉衍生物用于治疗病毒感染
公开(公告)号：WO2007039144A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009236
申请日：2006-09-21
申请人： GLAXO GROUP LIMITED , HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , JARVEST, Richard, Lewis , LAZARIDES, Linos , NEROZZI, Fabrizio , SMITH, Stephen, Allan
发明人： HAIGH, David , HARTLEY, Charles, David , HOWES, Peter, David , JARVEST, Richard, Lewis , LAZARIDES, Linos , NEROZZI, Fabrizio , SMITH, Stephen, Allan
IPC分类号： C07D417/14 , A61K31/4025 , A61P31/12
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia): wherein A represents hydroxy; D represents 3-bromo-4-tert-butylphenyl or 5-bromo-4-tert-butyl-2-fluorophenyl; E represents 1,3-thiazol-2-yl or 5-methylisoxazol-3-yl; G represents methoxymethyl; J represents 1,3-thiazol-4-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 branched chain alkyl, 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; D代表3-溴-4-叔丁基苯基或5-溴-4-叔丁基-2-氟苯基; E表示1,3-噻唑-2-基或5-甲基异恶唑-3-基; G表示甲氧基甲基; J代表1,3-噻唑-4-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选自支链烷基，则R不是叔丁基，提供其制备方法及其在HCV治疗中的用途。

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