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公开(公告)号:US20090318484A1
公开(公告)日:2009-12-24
申请号:US12454210
申请日:2009-05-14
申请人: Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmanhaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
发明人: Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmanhaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
IPC分类号: A61K31/506 , C07D413/14 , A61P19/02 , A61P3/04 , A61P25/16 , A61P25/28
CPC分类号: C07D401/14
摘要: The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 areas defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译: 本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法,制剂和组合物。 本申请公开了如下式I所述的JNK抑制剂的前药:其中m,n,p,q,Q,r,R1,R2,R3,X,X1,X2,X3,X4,X5,Y1, Z1和Z2区域。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂,以及本文公开的化合物,以及制备所述化合物的方法和相应的组合物。
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公开(公告)号:US08183254B2
公开(公告)日:2012-05-22
申请号:US12454210
申请日:2009-05-14
申请人: Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
发明人: Humberto Bartolome Arzeno , James Patrick Dunn , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Alam Jahangir , Wylie Solang Palmer , Deborah Carol Reuter , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Shao-Yong Wu
IPC分类号: C07D401/14 , A61K31/506
CPC分类号: C07D401/14
摘要: The invention relates to prodrugs of JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses prodrugs of JNK inhibitors, as described below in formula I: wherein m, n, p, q, Q, r, R1, R2, R3, X, X1, X2, X3, X4, X5, Y1, Y2, Z1 and Z2 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
摘要翻译: 本发明涉及JNK抑制剂的前药以及用于抑制JNK和治疗JNK介导的病症的相应方法,制剂和组合物。 本申请公开了如下式I所述的JNK抑制剂的前药:其中m,n,p,q,Q,r,R1,R2,R3,X,X1,X2,X3,X4,X5,Y1, Z1和Z2如本文所定义。 本文公开的化合物和组合物可用于调节JNK的活性并治疗与JNK活性相关的疾病。 公开了用于抑制JNK和治疗JNK介导的病症等的方法和制剂,以及本文公开的化合物,以及制备所述化合物的方法和相应的组合物。
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公开(公告)号:US20080146565A1
公开(公告)日:2008-06-19
申请号:US12001021
申请日:2007-12-07
申请人: James Patrick Dunn , Leyi Gong , David Michael Goldstein , Xiaochun Han , Joan Heather Hogg , Wylie Solang Palmer , Lubica Raptova , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Christophe Michoud , Achyutharao Sidduri
发明人: James Patrick Dunn , Leyi Gong , David Michael Goldstein , Xiaochun Han , Joan Heather Hogg , Wylie Solang Palmer , Lubica Raptova , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Christophe Michoud , Achyutharao Sidduri
IPC分类号: A61K31/506 , A61P29/00 , C07D413/04 , A61K31/5377 , C07D413/14 , C07D471/04 , C07D403/04
CPC分类号: C07D403/04 , C07D471/04 , C07D487/04
摘要: Compounds of formula I modulate JNK: wherein the variables are as defined herein.
摘要翻译: 式I的化合物调节JNK:其中变量如本文所定义。
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公开(公告)号:US08399462B2
公开(公告)日:2013-03-19
申请号:US12001021
申请日:2007-12-07
申请人: James Patrick Dunn , Leyi Gong , David Michael Goldstein , Xiaochun Han , Joan Heather Hogg , Wylie Solang Palmer , Lubica Raptova , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Christophe Michoud , Achyutharao Sidduri
发明人: James Patrick Dunn , Leyi Gong , David Michael Goldstein , Xiaochun Han , Joan Heather Hogg , Wylie Solang Palmer , Lubica Raptova , Tania Silva , Parcharee Tivitmahaisoon , Teresa Alejandra Trejo-Martin , Christophe Michoud , Achyutharao Sidduri
IPC分类号: C07D403/04 , A61K31/506
CPC分类号: C07D403/04 , C07D471/04 , C07D487/04
摘要: Compounds of formula I modulate JNK: wherein the variables are as defined herein.
摘要翻译: 式I的化合物调节JNK:其中变量如本文所定义。
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公开(公告)号:US07238698B2
公开(公告)日:2007-07-03
申请号:US10824731
申请日:2004-04-15
申请人: James Patrick Dunn , David Michael Goldstein , Christoph Martin Stahl , Teresa Alejandra Trejo-Martin
发明人: James Patrick Dunn , David Michael Goldstein , Christoph Martin Stahl , Teresa Alejandra Trejo-Martin
IPC分类号: A61K31/505 , C07D239/72
CPC分类号: C07D239/84 , C07D401/12 , C07D405/12
摘要: Compounds having the formula (I), are useful as p38 kinase inhibitors, wherein R4 and R5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R6 and R7 are optional substituents, and Q is a non-aromatic moiety as defined in the specification.
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6.
公开(公告)号:US07456185B2
公开(公告)日:2008-11-25
申请号:US11728644
申请日:2007-03-27
申请人: James Patrick Dunn , David Michael Goldstein , Christoph Martin Stahl , Teresa Alejandra Trejo-Martin
发明人: James Patrick Dunn , David Michael Goldstein , Christoph Martin Stahl , Teresa Alejandra Trejo-Martin
IPC分类号: A61K31/505 , C07D239/72
CPC分类号: C07D239/84 , C07D401/12 , C07D405/12
摘要: Compounds having the formula (I), are useful as p38 kinase inhibitors, wherein R4 and R5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R6 and R7 are optional substituents, and Q is a non-aromatic moiety as defined in the specification.
摘要翻译: 具有式(I)的化合物可用作p38激酶抑制剂,其中R 4和R 5是氢,卤素,氰基,卤代烷基或卤代烷氧基,但不是 氢; R 6和R 7是任选的取代基,Q是说明书中定义的非芳族部分。
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公开(公告)号:US06753427B2
公开(公告)日:2004-06-22
申请号:US10315633
申请日:2002-12-10
申请人: Humberto Bartolome Arzeno , Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Julie Anne Lim
发明人: Humberto Bartolome Arzeno , Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Julie Anne Lim
IPC分类号: A61K31519
CPC分类号: C07D471/04 , C07D239/47
摘要: The present invention provides compounds of the formula: a prodrug or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and Ar1 are those defined herein, and methods for preparation and uses thereof.
摘要翻译: 本发明提供下式的化合物:其前体药物或其药学上可接受的盐,其中R 1,R 2,R 3和Ar 1为本文定义的化合物及其制备方法及用途 。
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公开(公告)号:US06518276B2
公开(公告)日:2003-02-11
申请号:US09943338
申请日:2001-08-30
申请人: Humberto Bartolome Arzeno , Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Julie Anne Lim
发明人: Humberto Bartolome Arzeno , Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Julie Anne Lim
IPC分类号: A61K31519
CPC分类号: C07D471/04 , C07D239/47
摘要: The present invention provides compounds of the formula: wherein R1, R3, and Ar1 are those defined herein, and R2 is —CR′R″—Ra (where R′ and R″ are hydrogen, hydroxyalkyl or alkyl with at least one being alkyl or hydroxyalkyl and Ra is hydroxyalkyl), Rx—S—Ry— (where Rx is alkyl and Ry is alkylene), alkoxy-substituted alkyl, heterocyclylalkyl or C4-C5 cycloalkyl, wherein each of the hydroxy group present in R2 can be independently Ra—C(═O)—O, RaRbN—C(═O)—O, or Ra—S(O)2—O—, wherein Ra and Rb are independently hydrogen, alkyl, aryl, or aralkyl, and methods for preparation and uses thereof.
摘要翻译: 本发明提供下式的化合物:其中R1,R3和Ar1是本文定义的,R2是-CR'R'-Ra(其中R'和R“是氢,羟基烷基或具有至少一个 (其中R x是烷基,R y是亚烷基),烷氧基取代的烷基,杂环基烷基或C 4 -C 5环烷基,其中R 2中存在的每个羟基可以是 独立地是R a -C(= O)-O,R a R b N-C(= O)-O或R a -S(O)2-O-,其中R a和R b独立地是氢,烷基,芳基或芳烷基, 用于其制备和使用。
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公开(公告)号:US07241794B2
公开(公告)日:2007-07-10
申请号:US10781373
申请日:2004-02-18
IPC分类号: A61K31/415 , C07D231/18
CPC分类号: C07D231/20 , C07D403/06 , C07D409/06
摘要: This invention relates to novel pyrazole derivatives of formula I wherein R1 to R4 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I and pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient. The compounds are useful for treating disorders in which HIV and genetically related viruses are implicated
摘要翻译: 本发明涉及式I的新型吡唑衍生物,其中R 1至R 4如概述中所定义及其药学上可接受的盐和溶剂合物,用式I化合物抑制或调节人类免疫缺陷病毒(HIV)逆转录酶的方法和含有 式I与至少一种溶剂,载体或赋形剂混合。 该化合物可用于治疗涉及HIV和遗传相关病毒的疾病
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公开(公告)号:US07288542B2
公开(公告)日:2007-10-30
申请号:US11085869
申请日:2005-03-22
IPC分类号: A01N43/58 , C07D401/00 , C07D403/00
CPC分类号: C07D237/14 , Y10S514/85
摘要: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein
摘要翻译: 本发明涉及式I化合物,通过给予式I化合物治疗由人类免疫缺陷病毒介导的疾病的方法和用于治疗由含有式I化合物的人类免疫缺陷病毒介导的疾病的药物组合物,其中R R 1,R 2,R 3,R 4,R 5,R 5,R 5, R 6,R 7和R 8如本文所定义
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