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1. 发明申请

US20090270389A1 Pyrimidinyl pyridone inhibitors of kinases 失效
标题翻译：嘧啶嘧啶激酶抑制剂
公开(公告)号：US20090270389A1
公开(公告)日：2009-10-29
申请号：US12387181
申请日：2009-04-29
申请人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译：本申请公开了根据式I的新型嘧啶基吡啶酮衍生物，其中A，R1，R2，R3和m如本文所述限定，其抑制JNK。本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。

2. 发明授权

US08268840B2 Pyrimidinyl pyridone inhibitors of kinases 失效
标题翻译：嘧啶嘧啶激酶抑制剂
公开(公告)号：US08268840B2
公开(公告)日：2012-09-18
申请号：US12387181
申请日：2009-04-29
申请人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
发明人： Frederick Brookfield , Florence Eustache , Michael Patrick Dillon , David Michael Goldstein , Leyi Gong , Xiaochun Han , Joan Heather Hogg , Jaehyeon Park , Deborah Carol Reuter , Eric Brian Sjogren
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of formula I to a subject in need thereof.
摘要翻译：本申请公开了根据式I的新型嘧啶基吡啶酮衍生物，其中A，R1，R2，R3和m如本文所述限定，其抑制JNK。本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。

3. 发明授权

US08183254B2 Inhibitors of JNK 失效
标题翻译： JNK抑制剂
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。

4. 发明授权

US08163906B2 Dihydroquinone and dihydronaphthridine inhibitors of JNK 有权
标题翻译：二氢醌和二氢萘并吡嗪类抑制剂
公开(公告)号：US08163906B2
公开(公告)日：2012-04-24
申请号：US12152432
申请日：2008-05-14
申请人： Sarah C. Abbot , Geneviève N. Boice , Bernd Buettelmann , David Michael Goldstein , Leyi Gong , Joan Heather Hogg , Pravin Iyer , Kristen Lynn McCaleb , Yun-chou Tan
发明人： Sarah C. Abbot , Geneviève N. Boice , Bernd Buettelmann , David Michael Goldstein , Leyi Gong , Joan Heather Hogg , Pravin Iyer , Kristen Lynn McCaleb , Yun-chou Tan
IPC分类号： C07D471/04
CPC分类号： C07D215/48 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D471/04
摘要： Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl; Z is phenyl, cycloalkyl, heterocyclyl or heteroaryl, and is substituted with R1 and R2; R1 and R2 are each independently H, halo, CN, lower alkyl, or —Y1—Y2—Y3—R8, or R1 and R2 together form —O(CH2)nO—, where n is 1 or 2; Y1 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —S—, —SO2—, or a bond; Y2 is cycloalkylene, heterocycloalkylene, lower alkylene or a bond; Y3 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —SO2—, or a bond; R8 is H, lower alkyl, lower alkoxy, cycloalkyl, heterocycloalkyl, or —NR9R10, wherein R8 other than H is optionally substituted with lower alkyl, halo, —CF3, or —OH; R9 and R10 are each independently H or lower alkyl; R3 is OH, lower alkyl, lower alkoxy, (lower alkoxy)-lower alkoxy, or —NR9R10; R4 is lower alkyl, phenyl, heterocyclyl, cycloalkyl, heterocycloalkyl, or heteroaryl, and is optionally substituted with lower alkyl, hydroxy, lower alkoxy, halo, nitro, amino, cyano, or halo-lower alkyl; R5 and R6 are each independently H, halo, cyano, lower alkyl, —CF3, lower alkoxy, —OCHF2, —NO2, or —NR9R10; R7 is H, F, Cl, methyl, or OH; R11 is H, lower alkyl, lower cycloalkyl, or phenyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：式I化合物是JNK的有效调节剂：其中X是CR11或N; Y是-C（O）R 3，5元杂芳基或5元杂环基; Z是苯基，环烷基，杂环基或杂芳基，并被R1和R2取代; R1和R2各自独立地为H，卤素，CN，低级烷基或-Y1-Y2-Y3-R8，或R1和R2一起形成-O（CH 2）n O-，其中n为1或2; Y1是-O - ， - C（O） - ， - C（O）O - ， - C（O）NR 9 - ， - NR 9 C（O） - ， - S - ， - SO 2 - 或键; Y2是亚环烷基，杂环亚烷基，低级亚烷基或键; Y 3是-O - ， - C（O） - ， - C（O）O-，-C（O）NR 9 - ， - NR 9 C（O） - ， - SO 2 - 或键; R8是H，低级烷基，低级烷氧基，环烷基，杂环烷基或-NR9R10，其中R8以外的R8任选被低级烷基，卤素，-CF 3或-OH取代; R9和R10各自独立地为H或低级烷基; R3是OH，低级烷基，低级烷氧基，（低级烷氧基） - 低级烷氧基或-NR9R10; R 4是低级烷基，苯基，杂环基，环烷基，杂环烷基或杂芳基，并且任选被低级烷基，羟基，低级烷氧基，卤素，硝基，氨基，氰基或卤代低级烷基取代。 R 5和R 6各自独立地为H，卤素，氰基，低级烷基，-CF 3，低级烷氧基，-OCHF 2，-NO 2或-NR 9 R 10; R7是H，F，Cl，甲基或OH; R11是H，低级烷基，低级环烷基或苯基; 或其药学上可接受的盐。

5. 发明申请

US20090318484A1 Inhibitors of JNK 失效
标题翻译： JNK抑制剂
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。

6. 发明申请

US20080287458A1 Dihydroquinone and dihydronaphthridine inhibitors of JNK 有权
公开(公告)号：US20080287458A1
公开(公告)日：2008-11-20
申请号：US12152432
申请日：2008-05-14
申请人： Sarah C. Abbot , Genevieve N. Boice , Bernd Buettelmann , David Michael Goldstein , Leyi Gong , Joan Heather Hogg , Pravin Iyer , Kristen Lynn McCaleb , Yun-chou Tan
发明人： Sarah C. Abbot , Genevieve N. Boice , Bernd Buettelmann , David Michael Goldstein , Leyi Gong , Joan Heather Hogg , Pravin Iyer , Kristen Lynn McCaleb , Yun-chou Tan
IPC分类号： A61K31/496 , C07D471/04 , A61P19/02 , A61K31/4375
CPC分类号： C07D215/48 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D471/04
摘要： Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl; Z is phenyl, cycloalkyl, heterocyclyl or heteroaryl, and is substituted with R1 and R2; R1 and R2 are each independently H, halo, CN, lower alkyl, or —Y1—Y2—Y3—R8, or R1 and R2 together form —O(CH2)nO—, where n is 1 or 2; Y1 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —S—, —SO2—, or a bond; Y2 is cycloalkylene, heterocycloalkylene, lower alkylene or a bond; Y3 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —SO2—, or a bond; R8 is H, lower alkyl, lower alkoxy, cycloalkyl, heterocycloalkyl, or —NR9R10, wherein R8 other than H is optionally substituted with lower alkyl, halo, —CF3, or —OH; R9 and R10 are each independently H or lower alkyl; R3 is OH, lower alkyl, lower alkoxy, (lower alkoxy)-lower alkoxy, or —NR9R10; R4 is lower alkyl, phenyl, heterocyclyl, cycloalkyl, heterocycloalkyl, or heteroaryl, and is optionally substituted with lower alkyl, hydroxy, lower alkoxy, halo, nitro, amino, cyano, or halo-lower alkyl; R5 and R6 are each independently H, halo, cyano, lower alkyl, —CF3, lower alkoxy, —OCHF2, —NO2, or —NR9R10; R7 is H, F, Cl, methyl, or OH; R11 is H, lower alkyl, lower cycloalkyl, or phenyl; or a pharmaceutically acceptable salt thereof.

7. 发明授权

US07947709B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US07947709B2
公开(公告)日：2011-05-24
申请号：US12214651
申请日：2008-06-20
申请人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
发明人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
IPC分类号： A61K31/708 , A61K31/4184 , A61K31/437 , A61K31/5025 , A61P31/18 , C07D235/26 , C07D471/04 , C07D487/04
CPC分类号： C07D235/26 , C07D471/04 , C07D487/04
摘要： Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
摘要翻译：其中R 1，R 2，R 3，X和Ar如本文所定义的式I化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染和治疗AIDS的方法和/或ARC。本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式I化合物的组合物。

8. 发明申请

US20090012034A1 Non-Nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US20090012034A1
公开(公告)日：2009-01-08
申请号：US12214651
申请日：2008-06-20
申请人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
发明人： Todd Richard Elworthy , Joan Heather Hogg , Joshua Kennedy-Smith , Counde O'Yang , Mark Smith , Zachary Kevin Sweeney , Jeffrey Wu
IPC分类号： A61K31/708 , C07D235/26 , A61K31/4184 , C07D471/04 , A61P31/18 , A61K31/437 , A61K31/5025 , C07D487/04
CPC分类号： C07D235/26 , C07D471/04 , C07D487/04
摘要： Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
摘要翻译：其中R 1，R 2，R 3，X和Ar如本文所定义的式I化合物或其药学上可接受的盐抑制HIV-1逆转录酶，并提供预防和治疗HIV-1感染和治疗AIDS的方法和/或ARC。本发明还涉及含有用于预防和治疗HIV-1感染和治疗AIDS和/或ARC的式I化合物的组合物。

9. 发明申请

US20080146565A1 JNK modulators 失效
标题翻译： JNK调制器
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。

10. 发明授权

US07288542B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US07288542B2
公开(公告)日：2007-10-30
申请号：US11085869
申请日：2005-03-22
申请人： James Patrick Dunn , Todd Richard Elworthy , Joan Heather Hogg , Dimitrios Stefanidis
发明人： James Patrick Dunn , Todd Richard Elworthy , Joan Heather Hogg , Dimitrios Stefanidis
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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