公开(公告)号：WO2008101867A1

公开(公告)日：2008-08-28

申请号：PCT/EP2008/051832

申请日：2008-02-15

Applicant: SMITHKLINE BEECHAM CORPORATION ,  LAZARIDES, Linos ,  SMITH, Stephen, Allan ,  STOCKER, Richard ,  THEOBALD, Colin, Jack

Inventor： LAZARIDES, Linos ,  SMITH, Stephen, Allan ,  STOCKER, Richard ,  THEOBALD, Colin, Jack

IPC: C07D405/12

CPC classification number: C07D473/18 ,  C07D473/16

Abstract: Compounds of formula (I) wherein R 1 is C 1-8 alkylamino, C 1-8 alkoxy, C 3-7 cycloalkylC 1-6 alkylamino, C 3-7 cycloalkylC 1-6 alkoxy, C 1-3 alkoxyC 2-3 alkoxy, or Het b -C 1-3 alkoxy; Het b is a 5- or 6-membered saturated aliphatic heterocyle containing one oxygen atom; R 2 is -(CH 2 ) n -Het; n is an integer having a value of 1 to 4; Het is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen heteroatom, which heterocycle may be substituted by one or two C 1-4 alkyl groups, and salts and solvates thereof, are inducers of human interferon and may be useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.

Abstract translation: 式（I）的化合物，其中R 1是C 1-8烷基氨基，C 1-8烷氧基，C 3-7 C 1 -C 6烷基氨基，C 3-7环烷基C 1-6烷氧基，C 1-3烷基氨基， 烷氧基C 2-3烷氧基或Het-C 1-3烷氧基; Het B是含有一个氧原子的5-或6-元饱和脂族杂环; R 2是 - （CH 2 CH 2）n -Het; n为1〜4的整数， Het是含有一个氧杂原子的5或6元饱和脂族杂环，该杂环可被一个或两个C 1-4烷基取代，其盐和溶剂化物是人的诱导剂 并且可用于治疗各种疾病，特别是感染性疾病，癌症，过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，以及作为疫苗佐剂。

公开(公告)号：WO2007039142A1

公开(公告)日：2007-04-12

申请号：PCT/EP2006/009234

申请日：2006-09-21

Applicant: GLAXO GROUP LIMITED ,  HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  JARVEST, Richard, Lewis ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

Inventor： HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  JARVEST, Richard, Lewis ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

IPC: C07D417/14 ,  A61K31/427 ,  A61P31/14

CPC classification number: C07D417/14 ,  C07D417/04

Abstract: Anti-viral agents of Formula (Ia): wherein A represents hydroxyl; D represents 4- tert -butyl-3-ethenylphenyl or 4-tert-butyl-5-ethenyl-2-fluorophenyl; E represents 1,3-thiazol-2-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.

Abstract translation: 式（Ia）的抗病毒剂：其中A表示羟基; D代表4-叔丁基-3-乙烯基苯基或4-叔丁基-5-乙烯基-2-氟苯基; E表示1,3-噻唑-2-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。

公开(公告)号：WO2010018134A1

公开(公告)日：2010-02-18

申请号：PCT/EP2009/060267

申请日：2009-08-07

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BAZIN-LEE, Helene ,  COE, Diane, Mary ,  LAZARIDES, Linos ,  MITCHELL, Charlotte, Jane ,  SMITH, Stephen, Allan ,  TRIVEDI, Naimisha

Inventor： BAZIN-LEE, Helene ,  COE, Diane, Mary ,  LAZARIDES, Linos ,  MITCHELL, Charlotte, Jane ,  SMITH, Stephen, Allan ,  TRIVEDI, Naimisha

IPC: A61K31/522 ,  C07D473/16 ,  C07D473/18 ,  A61P29/00

CPC classification number: C07D473/16 ,  A61K31/522 ,  C07D473/18

Abstract: Compounds of formula (I) wherein R 1 is C 1-6 alkylamino, or C 1-6 alkoxy; R 2 is a group having the structure (II): n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the -(CH 2 ) n - moiety at any carbon atom of the heterocycle; R 3 is hydrogen, C 1-8 alkyl, or C 3-7 cycloalkylC 0-6 alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

Abstract translation: 其中R 1为C 1-6烷基氨基或C 1-6烷氧基的式（I）化合物; R2是具有结构（II）的基团：n是1至6的整数; Het是含有一个氮原子的6元饱和杂环，其中Het与杂环的任何碳原子连接至 - （CH 2）n - 部分; R3是氢，C1-8烷基或C3-7环烷基C0-6烷基; 其盐是人类干扰素的诱导剂。 诱导人类干扰素的化合物可用于治疗各种疾病，例如治疗过敏性疾病和其它炎性病症，例如过敏性鼻炎和哮喘，治疗感染性疾病和癌症，并且也可用作疫苗佐剂。

公开(公告)号：WO2009046098A1

公开(公告)日：2009-04-09

申请号：PCT/US2008/078439

申请日：2008-10-01

Applicant: SMITHKLINE BEECHAM CORPORATION ,  ANACOR PHARMACEUTICALS, INC. ,  FAN, Dazhong ,  JARVEST, Richard Lewis ,  LAZARIDES, Linos ,  LI, Qun ,  LI, Xianfeng ,  LIU, Yang ,  LIAO, Liang ,  MORDAUNT, Jacqueline Elizabeth ,  NI, Zhi-jie ,  PLATTNER, Jacob ,  QIAN, Xuelei ,  SLATER, Martin John ,  WHITE, Gemma Victoria ,  ZHANG, Yong Kang

Inventor： FAN, Dazhong ,  JARVEST, Richard Lewis ,  LAZARIDES, Linos ,  LI, Qun ,  LI, Xianfeng ,  LIU, Yang ,  LIAO, Liang ,  MORDAUNT, Jacqueline Elizabeth ,  NI, Zhi-jie ,  PLATTNER, Jacob ,  QIAN, Xuelei ,  SLATER, Martin John ,  WHITE, Gemma Victoria ,  ZHANG, Yong Kang

IPC: A61K31/69 ,  C07F5/02 ,  C07K5/08 ,  A61P31/14

CPC classification number: C07F7/10 ,  A61K31/69 ,  A61K38/05 ,  A61K38/21 ,  C07F5/025 ,  C07F7/1844 ,  C07K5/0821 ,  A61K2300/00

Abstract: Compounds of formula (I) or a salt thereof are provided; wherein R 1 , R 2 , R 3 , R 4 , R 6 , R 8 , R 20 , R 30 , Y, Z and n are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicaments for treating viral infection, especially HCV infection are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.

Abstract translation: 提供式（I）化合物或其盐; 其中R 1，R 2，R 3，R 4，R 6，R 8，R 20，R 30，Y，Z和n如说明书中所定义。 还公开了化合物作为药物的用途，以及用于制备用于治疗病毒感染的药物，特别是HCV感染。 本发明还包括制备这些化合物及其药物制剂的方法。

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

Applicant: GLAXO GROUP LIMITED ,  HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  JARVEST, Richard, Lewis ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

Inventor： HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  JARVEST, Richard, Lewis ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

IPC: C07D417/14 ,  A61K31/4025 ,  A61P31/12

CPC classification number: C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2012078915A1

公开(公告)日：2012-06-14

申请号：PCT/US2011/064009

申请日：2011-12-08

Applicant: GILEAD SCIENCES, INC. ,  SELCIA LIMITED ,  APPLEBY, Todd ,  FLIRI, Hans, G. ,  KEATS, Andrew, J. ,  LAZARIDES, Linos ,  MACKMAN, Richard, L. ,  PETTIT, Simon, N. ,  POULLENNEC, Karine, G. ,  SANVOISIN, Jonathan ,  STEADMAN, Victoria, A. ,  WATT, Gregory, M.

Inventor： APPLEBY, Todd ,  FLIRI, Hans, G. ,  KEATS, Andrew, J. ,  LAZARIDES, Linos ,  MACKMAN, Richard, L. ,  PETTIT, Simon, N. ,  POULLENNEC, Karine, G. ,  SANVOISIN, Jonathan ,  STEADMAN, Victoria, A. ,  WATT, Gregory, M.

IPC: C07D487/08 ,  C07D498/08 ,  C07D498/18 ,  A61K31/504 ,  A61P31/14

CPC classification number: A61K38/06 ,  A61K45/06 ,  C07D487/04 ,  C07D487/08 ,  C07D498/08 ,  C07D498/18 ,  C07K5/02 ,  C07K5/06052

Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract translation: 提供式（I）的化合物及其药学上可接受的盐和酯。 所提供的化合物，组合物和方法可用于治疗黄病毒科感染，特别是丙型肝炎感染。

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

Applicant: GLAXO GROUP LIMITED ,  HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

Inventor： HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

IPC: C07D417/14 ,  A61K31/427 ,  A61P31/14

CPC classification number: C07D417/14

Abstract: 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.

Abstract translation: 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。

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

Applicant: GLAXO GROUP LIMITED ,  HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

Inventor： HAIGH, David ,  HARTLEY, Charles, David ,  HOWES, Peter, David ,  LAZARIDES, Linos ,  NEROZZI, Fabrizio ,  SMITH, Stephen, Allan

IPC: C07D417/14 ,  A61K31/4025 ,  A61P31/12

CPC classification number: C07D417/14

Abstract: 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.

Abstract translation: 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。