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1.发明申请4-(PYRAZINE-2-YL) -PYRROLIDINE -2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS 审中-公开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：US20090227600A1
公开(公告)日：2009-09-10
申请号：US11577940
申请日：2005-10-24
申请人： Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Fabrizio Nerozzi , Stephen Allan Smith
发明人： Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Fabrizio Nerozzi , Stephen Allan Smith
IPC分类号： A61K31/497 , C07D417/14 , A61P31/12
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia) wherein: A represents hydroxy; B represents C(O)R3 wherein R3 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。
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2.发明授权4-(6-membered)-heteroaryl acyl pyrrolidine derivatives as HCV inhibitors 失效4-（6-元） - 杂芳基酰基吡咯烷衍生物作为HCV抑制剂公开(公告)号：US07259163B2
公开(公告)日：2007-08-21
申请号：US10494127
申请日：2002-10-30
申请人： Gianpaolo Bravi , Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Deborah Lynette Jackson , Victoria Lucy Helen Lovegrove , Pritom Shah , Martin John Slater , Katrina Jane Wareing
发明人： Gianpaolo Bravi , Rossella Guidetti , David Haigh , Charles David Hartley , Peter David Howes , Deborah Lynette Jackson , Victoria Lucy Helen Lovegrove , Pritom Shah , Martin John Slater , Katrina Jane Wareing
IPC分类号： A61K31/4965 , A01N43/54 , C07D239/42 , C07D241/00 , C07D241/02
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14 , C07D417/14
摘要： Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.
摘要翻译： 新型的下式的抗病毒剂，其中：A表示OR 1，NR 1，R 2，或R 1， 其中R 1和R 2是氢，C 1-6烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; B表示C（O）R 3，其中R 3是C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; C表示C 1-6烷基，芳基，杂芳基或杂环基; D表示饱和或不饱和的任选取代的6元杂环; E表示氢或C 1-6烷基; F表示氢，C 1-6烷基，芳基或杂芳基; 和G表示氢，C 1-6烷基，杂环基烷基，芳基烷基或杂芳基烷基; 提供其盐，溶剂合物和酯，其制备方法及其用于HCV治疗的方法。
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3.发明申请4-Methoxy-Pyrrolidine-2-Carboxylic Acid Compounds and Derivatives Thereof as Hepatitis C Virus Inhibitors 审中-公开4-甲氧基 - 吡咯烷-2-羧酸化合物及其衍生物作为丙型肝炎病毒抑制剂公开(公告)号：US20070270475A1
公开(公告)日：2007-11-22
申请号：US11568127
申请日：2005-10-24
申请人： Rossella Guidetti , David Haigh , Charles Hartley , Peter Howes , Fabrizio Nerozzi , Stephen Smith
发明人： Rossella Guidetti , David Haigh , Charles Hartley , Peter Howes , Fabrizio Nerozzi , Stephen Smith
IPC分类号： C07D207/04 , C07D277/02
CPC分类号： C07D417/14
摘要： Anti-viral agents of Formula (Ia) 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表示羟基; 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; 提供了其制备方法及其在HCV治疗中的应用。
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4.发明申请4-(6-membered)-heteroaryl acyl pyrrolidine derivatives as hcv inhibitors 失效4-（6-元） - 杂芳基酰基吡咯烷衍生物作为hcv抑制剂公开(公告)号：US20050043390A1
公开(公告)日：2005-02-24
申请号：US10494127
申请日：2002-10-30
申请人： Gianpaolo Bravi , Rossella Guidetti , David Haigh , Charles Hartley , Peter Howes , Deborah Jackson , Victoria Lovegrove , Pritom Shah , Martin Slater , Katrina Wareing
发明人： Gianpaolo Bravi , Rossella Guidetti , David Haigh , Charles Hartley , Peter Howes , Deborah Jackson , Victoria Lovegrove , Pritom Shah , Martin Slater , Katrina Wareing
IPC分类号： A61K31/4439 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61P1/16 , A61P31/12 , A61P31/14 , C07D401/14 , C07D403/04 , C07D409/14 , C07D417/14 , A61K31/4025 , A61K31/401 , C07D43/02
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14 , C07D417/14
摘要： Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6-alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.
摘要翻译： 新型的式的抗病毒剂其中：A表示OR 1，NR 1 R 2或R 1，其中R 1和R 2是氢，C 1-6烷基，芳基，杂芳基 ，芳基烷基或杂芳基烷基; 或R 1和R 2与它们所连接的氮原子一起形成5或6元饱和环状基团; B表示C（O）R 3，其中R 3是C 1-6烷基，芳基，杂芳基，芳烷基或杂芳基烷基; C代表C 1-6烷基，芳基，杂芳基或杂环基; D表示饱和或不饱和的任选取代的6元杂环; E表示氢或C 1-6 - 烷基; F表示氢，C 1-6烷基，芳基或杂芳基; 和G表示氢，C 1-6烷基，杂环基烷基，芳基烷基或杂芳基烷基; 提供其盐，溶剂合物和酯，其制备方法及其用于HCV治疗的方法。
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公开(公告)号：US08252798B2
公开(公告)日：2012-08-28
申请号：US12633812
申请日：2009-12-09
IPC分类号： C07D473/34 , C07D519/00 , A61K31/52 , A61P25/04 , C07D473/40 , C07D403/12 , C07D407/12 , C07D409/12
CPC分类号： C07D473/34
摘要： A compound of the formula: and pharmaceutical compositions for the treatment of pain.
摘要翻译： 下式的化合物：用于治疗疼痛的药物组合物。
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公开(公告)号：US20070167507A1
公开(公告)日：2007-07-19
申请号：US10599346
申请日：2005-03-22
申请人： Gianpaolo Bravi , John Corfield , Richard Grimes , Rossella Guidetti , Victoria Lucy Lovegrove , Jacqueline Mordaunt , Pritom Shah , Martin Slater
发明人： Gianpaolo Bravi , John Corfield , Richard Grimes , Rossella Guidetti , Victoria Lucy Lovegrove , Jacqueline Mordaunt , Pritom Shah , Martin Slater
IPC分类号： A61K31/416 , A61K31/4152 , C07D405/02 , C07D409/02
CPC分类号： C07D403/12 , C07D231/40 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14
摘要： Novel antiviral compounds of Formula (I): wherein: A represents hydroxy; R1 represents aryl, heteroaryl bonded through a ring carbon atom, or heterocyclyl bonded through a ring carbon atom, C1-6alkyl or —C5-9cycloalkyl, each of which may be optionally substituted; R2 represents substituted phenyl, or —(CH2)nC5-7cycloalkyl optionally substituted on the cycloalkyl; R3 represents heterocyclyl or heteroaryl; optionally substituted phenyl or optionally substituted —C1-6alkyl; R4 represents hydrogen; and salts, solvates and esters thereof processes for their preparation, pharmaceutical compositions comprising them, and methods of using them in HCV treatment are provided.
摘要翻译： 式（I）的新型抗病毒化合物：其中：A表示羟基; R 1表示芳基，通过环碳原子键合的杂芳基，或通过环碳原子键合的杂环基，C 1-6烷基或-C 5-9 其各自可以任选被取代; R 2表示取代的苯基或 - 任选地被取代的苯基或 - （CH 2 CH 2）n C 5 - 环烷基 R 3表示杂环基或杂芳基; 任选取代的苯基或任选取代的C 1-6烷基; R 4表示氢; 及其盐，溶剂化物和酯的制备方法，包含它们的药物组合物及其在HCV治疗中的使用方法。
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公开(公告)号：US08759360B2
公开(公告)日：2014-06-24
申请号：US13072843
申请日：2011-03-28
IPC分类号： A61K31/52 , C07D473/32
CPC分类号： C07D487/04
摘要： A compound of the formula: and pharmaceutical compositions for the treatment or prevention of pain.
摘要翻译： 一种下式的化合物：用于治疗或预防疼痛的药物组合物。
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