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1. 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）

2. 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。

3. 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。

4. 发明申请

WO2002096427A1 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：WO2002096427A1
公开(公告)日：2002-12-05
申请号：PCT/GB2002/002414
申请日：2002-05-23
申请人： GLAXO GROUP LIMITED , HARTLEY, Charles, David , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
发明人： HARTLEY, Charles, David , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
IPC分类号： A61K31/505
CPC分类号： C07D239/42
摘要： The invention thus 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 2-6 alkenyl, C 3-6 alkynyl, C 3-10 cycloalkylC 0-6 alkyl and C 4-12 bridged cycloalkyl; R 3 is selected from the group consisting of C 1-6 alkyl, NH 2 and R 5 CONH; R 4 is selected from the group consisting of CH 2 F, CHF 2 , CF 3 CH 2 , CF 3 CHF and CF 3 CF 2 ; and R 5 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. 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：因此，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，C 2-6烯基，C 3-6炔基，C 3-10环烷基C 1-6烷基和C 4-12桥环烷基; R 3选自C 1-6烷基，NH 2和R 5 CONH; R 4选自CH 2 F，CHF 2，CF 3 CH 2，CF 3 CHF和CF 3 CF 2; 和R 5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COOC 1-6烷基，C 1-6烷基COO，H 2 NC 1-6烷基，C 1 1-6烷基OCONHC 1-6烷基和C 1-6烷基CONHC 1-6烷基。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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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