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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

WO2006100106A1 3-CARBOXY PYRROLES AS ANTI-VIRAL AGENTS 审中-公开
标题翻译： 3-羧基吡咯烷作为反病毒剂
公开(公告)号：WO2006100106A1
公开(公告)日：2006-09-28
申请号：PCT/EP2006/002833
申请日：2006-03-20
申请人： SMITHKLINE BEECHAM CORPORATION , GRIMES, Richard, Martin , SHAH, Pritom
发明人： GRIMES, Richard, Martin , SHAH, Pritom
IPC分类号： A61K31/40 , C07D405/12 , C07D207/34 , A61K31/4025 , A61P31/12
CPC分类号： C07D405/12 , C07D207/34
摘要： Novel antiviral compounds of Formula (I) : wherein: A represents hydroxy; R 4 represents hydrogen and the other substituents are as defined in the claims; and salts, solvates and esters thereof; processes for their preparation, pharmaceutical compositions comprising them, and their use in HCV treatment are provided. .
摘要翻译：式（I）的新型抗病毒化合物：其中：A表示羟基; R 4表示氢，其它取代基如权利要求中所定义; 及其盐，溶剂化物和酯; 提供其制备方法，包含它们的药物组合物及其在HCV治疗中的用途。。

4. 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。

5. 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。

6. 发明申请

WO2005079799A1 4-ACYL-PIPERAZINES AS ANTI-VIRAL AGENTS 审中-公开
标题翻译： 4-ACYL-PIPERAZINES作为反病毒剂
公开(公告)号：WO2005079799A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001451
申请日：2005-02-10
申请人： GLAXO GROUP LIMITED , CORFIELD, John, Andrew , SHAH, Pritom , SLATER, Martin, John
发明人： CORFIELD, John, Andrew , SHAH, Pritom , SLATER, Martin, John
IPC分类号： A61K31/495
CPC分类号： C07D241/04 , C07D403/04 , C07D417/06 , C07D417/14
摘要： Anti-viral agents of Formula (I) wherein: A represents hydroxy or -NH 2 ; D represents aryl or heteroaryl; E represents hydrogen, straight or branched chain C 1-6 alkyl, -CO 2 R 1 , -C(O)R 1a , -C(O)NR 2 R 3 , -SO 2 R 1 , aryl, arylC 1-3 alkyl, heteroaryl, heteroarylC 1-3 alkyl, heterocyclyl or heterocyclylC 1-3 alkyl; R 1 is selected from the group consisting of C 1-6 alkyl, aryl, arylC 1-3 alkyl, heteroaryl, heteroarylC 1-3 alkyl, heterocyclyl or heterocyclylC 1-3 alkyl; R 1a is selected from the group consisting of C 1-6 alkyl, aryl, arylC 1-3 alkyl, heteroaryl, heteroarylC 1-3 alkyl, heterocyclyl or heterocyclylC 1-3 alkyl; R 2 and R 3 are independently selected from hydrogen, C 1-6 alkyl, aryl and heteroaryl; or R 2 and R 3 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; G represents C 1-6 alkyl, heterocyclylC 1-3 alkyl, arylC 1-3 alkyl or heteroarylC 1-3 alkyl; 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, pharmaceutical compositions comprising them, and methods of using them in HCV treatment are provided.
摘要翻译：式（I）的抗病毒剂，其中：A表示羟基或-NH 2; D表示芳基或杂芳基; E表示氢，直链或支链C 1-6烷基，-CO 2 R 1，-C（O）R 1a，-C（O）NR 2 R 3，-SO 2 R 1，芳基，芳基C 1-3烷基，杂芳基，杂芳基C 1-3烷基，杂环基或杂环基C 1-3烷基; R 1选自C 1-6烷基，芳基，芳基C 1-3烷基，杂芳基，杂芳基C 1-3烷基，杂环基或杂环基C 1-3烷基; R 1a选自C 1-6烷基，芳基，芳基C 1-3烷基，杂芳基，杂芳基C 1-3烷基，杂环基或杂环基C 1-3烷基; R 2和R 3独立地选自氢，C 1-6烷基，芳基和杂芳基; 或R 2和R 3与它们所连接的氮原子一起形成5或6元饱和环基; G表示C 1-6烷基，杂环基C 1-3烷基，芳基C 1-3烷基或杂芳基C 1-3烷基; 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，包含它们的药物组合物，以及在HCV治疗中使用它们的方法。

7. 发明申请

WO1994013648A1 1,4-BENZODIAZEPINE DERIVATIVES AND THEIR USE AS CCK-MODULATORS 审中-公开
标题翻译： 1,4-苯并二恶英衍生物及其作为CCK调节剂的用途
公开(公告)号：WO1994013648A1
公开(公告)日：1994-06-23
申请号：PCT/EP1993003381
申请日：1993-12-02
申请人： GLAXO GROUP LIMITED , ARMOUR, Duncan, Robert , BOX, Philip, Charles , SHAH, Pritom
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D243/14
CPC分类号： C07D413/14 , C07D243/14
摘要： Compounds of general formula (I) and physiologically acceptable salts thereof; wherein R1 represents CH2CONR5R6 or CH2COR7; R2 represents a phenyl group optionally substituted by 1 or 2 substituents selected from halogen, alkyl, nitro, cyano, trifluoromethyl, trifluoromethoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, amino, substituted amino, hydroxy, alkoxy, methylenedioxy, alkoxycarbonyl, oxazolyl or oxadiazolyl; A represents a C1-4 straight or branched alkylene chain; R3 and R4 independently represent hydrogen or C1-4alkyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5-7 membered heterocyclic ring, which ring may contain an additional heteroatom selected from oxygen, sulphur or nitrogen; R5 represents hydrogen or C1-4alkyl; R6 represents C1-4alkyl or phenyl, optionally substituted by halogen, or R5 and R6 together with the nitrogen atom to which they are attached represent a saturated 5 to 7 membered heterocyclic ring which may be optionally substituted by 1 or 2 methyl groups or fused to a benzene ring; R7 represents a group selected from C1-4alkyl, or optionally substituted phenyl; R8 represents hydrogen or a halogen atom; n is zero, 1 or 2, are antagonists of gastrin and CCK.
摘要翻译：通式（I）的化合物及其生理上可接受的盐; 其中R1表示CH2CONR5R6或CH2COR7; R 2表示任选被1或2个选自卤素，烷基，硝基，氰基，三氟甲基，三氟甲氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，氨基，取代的氨基，羟基，烷氧基，亚甲二氧基，烷氧基羰基，恶唑基或恶二唑基的取代基取代的苯基。 A表示C1-4直链或支链亚烷基链; R 3和R 4独立地表示氢或C 1-4烷基，或者R 3和R 4与它们所连接的氮原子一起形成饱和的5-7元杂环，该环可含有选自氧，硫或氮的另外的杂原子; R5代表氢或C1-4烷基; R 6表示任选被卤素取代的C 1-4烷基或苯基，或者R 5和R 6与它们所连接的氮原子一起表示饱和的5至7元杂环，其可任选被1或2个甲基取代或稠合至苯环; R 7表示选自C 1-4烷基或任选取代的苯基的基团; R8表示氢或卤素原子; n为零，1或2是胃泌素和CCK的拮抗剂。

8. 发明申请

WO1993008175A1 BENZODIAZEPINE DERIVATIVES AS ANTAGONISTS OF GASTRIN AND/OR CHOLECYSTOKININ 审中-公开
标题翻译：胆碱衍生物作为胃蛋白酶和/或胆钙蛋白的拮抗剂
公开(公告)号：WO1993008175A1
公开(公告)日：1993-04-29
申请号：PCT/EP1992002385
申请日：1992-10-19
申请人： GLAXO GROUP LIMITED , CARR, Robin, Arthur, Ellis , PASS, Martin , SHAH, Pritom
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D243/24
CPC分类号： C07D403/12 , C07D243/24
摘要： Compounds of general formula (I), wherein R1 represents a group selected from CH¿2?CONR?4R5, XYR6¿, phenyl, C¿3-7?-cycloalkyl or C1-6alkyl, optionally substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl or adamantyl group; R?2¿ represents a group selected from NR7SO2CF3, SO2NR?7COR8, CONR7SO¿2R8, or a tetrazole, carboxamidotetrazole, or 3-trifluoromethyl-1,2,4-triazole group in which the tetrazole or triazole moiety may be substituted on one of the nitrogen atoms by a C¿1-4?alkyl group; R?3¿ is phenyl optionally substituted by one or two halogen atoms; R?4 and R5¿ which may be the same or different each independently represent a hydrogen atom, or a phenyl or C¿1-4?alkyl group or NR?4R5¿ represents a saturated 5- to 7-membered nitrogen containing heterocyclic ring, optionally substituted by 1 or 2 methyl groups; R6 represents a group selected from C¿1-6?alkyl, optionally substituted phenyl, C3-7cycloalkyl or adamantyl; R?7¿ represents hydrogen or a C¿1-4?alkyl group; R?8¿ represents a C¿1-4?alkyl group, X is a C1-3 straight or branched alkylene chain; Y represents a group selected from -C=O,C(OR?9)¿2 or C(SR9)2 wherein R9 is C¿1-3?-alkyl or the two R?9¿ groups together form a C¿2-4?alkylene chain; n is zero or 1; are modulators of gastrin and/or CCK.

9. 发明申请

WO2007147794A1 FURAN DERIVATIVES AND THEIR USE AS ANTIVIRAL AGENTS 审中-公开
标题翻译： FURAN衍生物及其作为抗病毒剂的用途
公开(公告)号：WO2007147794A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/055991
申请日：2007-06-18
申请人： SMITHKLINE BEECHAM CORPORATION , GRIMES, Richard, Martin , SHAH, Pritom
发明人： GRIMES, Richard, Martin , SHAH, Pritom
IPC分类号： C07D307/68 , A61K31/341 , C07D471/04 , C07D493/04 , A61P31/00 , C07D413/10 , C07D498/04 , C07D513/04 , A61K31/4355 , A61K31/437 , A61K31/421 , A61K31/429
CPC分类号： C07D307/68 , C07D413/10 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D498/04 , C07D513/04
摘要： Anti-viral agents of compounds of Formula (Ia) : 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（Ia）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

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。

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