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公开(公告)号:US08536172B2
公开(公告)日:2013-09-17
申请号:US12852540
申请日:2010-08-09
申请人: Leyi Gong , Xiaochun Han , Ferenc Makra , Wylie Solang Palmer , Lubica Raptova
发明人: Leyi Gong , Xiaochun Han , Ferenc Makra , Wylie Solang Palmer , Lubica Raptova
IPC分类号: A61K31/495
CPC分类号: C07D403/04 , C07D401/14
摘要: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y′, r, R1, R2, X, X1, X2, X3, and X4 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抑制剂和用于抑制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:其中p,q,Y',r,R 1,R 2,X,X 1,X 2,X 3和X 4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:US20110034470A1
公开(公告)日:2011-02-10
申请号:US12852540
申请日:2010-08-09
申请人: Leyi Gong , Xiaochun Han , Ferenc Makra , Wylie Solang Palmer , Lubica Raptova
发明人: Leyi Gong , Xiaochun Han , Ferenc Makra , Wylie Solang Palmer , Lubica Raptova
IPC分类号: A61K31/506 , C07D403/14 , C07D401/14 , A61P3/10 , A61P3/00 , A61P11/06 , A61P25/28 , A61P35/00 , A61P13/12
CPC分类号: C07D403/04 , C07D401/14
摘要: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y′, r, R1, R2, X, X1, X2, X3, and X4 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抑制剂和用于抑制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:其中p,q,Y',r,R 1,R 2,X,X 1,X 2,X 3和X 4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:US07638517B2
公开(公告)日:2009-12-29
申请号:US11605729
申请日:2006-11-29
申请人: Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
发明人: Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
IPC分类号: A61K31/519 , A61K31/506 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号: C07D471/04 , C07D487/04 , C07D487/14
摘要: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译: 本发明提供下式的化合物或其药学上可接受的盐,溶剂合物或前药,其中p,Ar,R 1,R 2,R 3,R a,R b,R c,R d和R Re如本文所定义。 还提供药物组合物,使用方法和制备化合物的方法。
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公开(公告)号:US20100056499A1
公开(公告)日:2010-03-04
申请号:US12619275
申请日:2009-11-16
申请人: Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
发明人: Robert Greenhouse , Saul Jaime-Figueroa , Stephen M. Lynch , Lubica Raptova , Karin Ann Stein , Robert James Weikert
IPC分类号: A61K31/519 , C07D487/04 , C07D471/04 , C07D471/16 , A61K31/551 , A61K31/437 , A61P25/24 , A61P25/22
CPC分类号: C07D471/04 , C07D487/04 , C07D487/14
摘要: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译: 本发明提供下式的化合物或其药学上可接受的盐,溶剂合物或前药,其中p,Ar,R 1,R 2,R 3,R a,R b,R c,R d和R Re如本文所定义。 还提供药物组合物,使用方法和制备化合物的方法。
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公开(公告)号:US20070123535A1
公开(公告)日:2007-05-31
申请号:US11605729
申请日:2006-11-29
申请人: Robert Greenhouse , Saul Jamie-Figueroa , Stephen Lynch , Lubica Raptova , Karin Stein , Robert Weikert
发明人: Robert Greenhouse , Saul Jamie-Figueroa , Stephen Lynch , Lubica Raptova , Karin Stein , Robert Weikert
IPC分类号: A61K31/519 , A61K31/506 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号: C07D471/04 , C07D487/04 , C07D487/14
摘要: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译: 本发明提供下式的化合物或其药学上可接受的盐,溶剂合物或前药,其中p,Ar,R 1,R 2,R 3, R SUP,R,B,R,C,R,D, / SUP>。 还提供药物组合物,使用方法和制备化合物的方法。
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8.
公开(公告)号:US07863305B2
公开(公告)日:2011-01-04
申请号:US11142076
申请日:2005-06-01
申请人: Robert Greenhouse , Saul Jaime-Figueroa , Lubica Raptova , Deborah Carol Reuter , Karin Ann Stein , Robert Weikert
发明人: Robert Greenhouse , Saul Jaime-Figueroa , Lubica Raptova , Deborah Carol Reuter , Karin Ann Stein , Robert Weikert
IPC分类号: A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , C07D209/04 , C07D231/56 , C07D235/04 , C07D263/54 , C07D277/64
CPC分类号: C07D401/06 , C07D209/08 , C07D209/14 , C07D231/56 , C07D307/14
摘要: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译: 式I化合物或其药学上可接受的盐,溶剂合物或前药,其中p,Ar,R 1,R 2,R 3,R a,R b,R c,R d和R e定义如下。 还提供药物组合物,使用方法和制备化合物的方法。
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9.
公开(公告)号:US20060025467A1
公开(公告)日:2006-02-02
申请号:US11142076
申请日:2005-06-01
申请人: Robert Greenhouse , Saul-Jaime Figueroa , Lubica Raptova , Deborah Reuter , Karin Stein , Robert Weikert
发明人: Robert Greenhouse , Saul-Jaime Figueroa , Lubica Raptova , Deborah Reuter , Karin Stein , Robert Weikert
IPC分类号: A61K31/416 , A61K31/405 , C07D209/18 , C07D231/56
CPC分类号: C07D401/06 , C07D209/08 , C07D209/14 , C07D231/56 , C07D307/14
摘要: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
摘要翻译: 式I化合物或其药学上可接受的盐,溶剂合物或前药,其中p,Ar,R 1,R 2,R 3, R< a>,< b< b>,R< c>,< d>和< 本文定义。 还提供药物组合物,使用方法和制备化合物的方法。
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公开(公告)号:US06852726B2
公开(公告)日:2005-02-08
申请号:US10355588
申请日:2003-01-31
IPC分类号: C07D209/00 , A61K31/4178 , A61K31/506 , A61K31/5377 , A61P1/14 , A61P7/12 , A61P11/02 , A61P13/00 , A61P13/02 , A61P15/10 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/16 , A61P29/00 , A61P43/00 , C07D403/06 , C07D495/04
CPC分类号: C07D403/06 , C07D495/04
摘要: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein X is —S(O)n— or —C(O)—, A is C1-6alkyl, aryl, heteroaryl, hydroxyalkyl, or —(CH2)p—NRaRb, and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译: 本发明涉及作为α-1受体激动剂,优选α-1A / L受体激动剂的化合物,其由式I表示:其中X是-S(O)n - 或-C(O) - ,A是 C 1-6烷基,芳基,杂芳基,羟烷基或 - (CH 2)p -NR a R a R b,其它取代基如说明书中所定义; 或各异构体,异构体的外消旋或非外消旋混合物,或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物,其用作治疗剂的方法及其制备方法。
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