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    PYRIMIDINYL PYRIDONE INHIBITORS OF JNK
    3.
    发明申请
    PYRIMIDINYL PYRIDONE INHIBITORS OF JNK 审中-公开
    吡咯烷酮吡咯烷酮抑制剂

    公开(公告)号：WO2010046273A2

    公开(公告)日：2010-04-29

    申请号：PCT/EP2009/063327

    申请日：2009-10-13

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BOICE, Genevieve N. ,  GONG, Leyi ,  MCCALEB, Kristen Lynn ,  PALMER, Wylie Solang

    Inventor： BOICE, Genevieve N. ,  GONG, Leyi ,  MCCALEB, Kristen Lynn ,  PALMER, Wylie Solang

    IPC: C07D487/04 ,  A61K31/519 ,  A61P29/00

    CPC classification number: C07D471/04

    Abstract: This application discloses novel pyrimidinyl pyridone derivatives according to Formulae I and II, wherein R 1 and R 2 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.

    Abstract translation: 本申请公开了根据式I和II的新型嘧啶基吡啶酮衍生物，其中R1和R2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。

    INHIBITORS OF JNK
    5.
    发明申请
    INHIBITORS OF JNK 审中-公开
    JNK的抑制剂

    公开(公告)号：WO2011018417A1

    公开(公告)日：2011-02-17

    申请号：PCT/EP2010/061476

    申请日：2010-08-06

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GONG, Leyi ,  HAN, Xiaochun ,  MAKRA, Ferenc ,  PALMER, Wylie Solang ,  RAPTOVA, Lubica

    Inventor： GONG, Leyi ,  HAN, Xiaochun ,  MAKRA, Ferenc ,  PALMER, Wylie Solang ,  RAPTOVA, Lubica

    IPC: C07D403/04 ,  C07D401/14 ,  A61K31/506 ,  A61P29/00 ,  A61P25/00 ,  A61P35/00

    CPC classification number: C07D403/04 ,  C07D401/14

    Abstract: 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, R 1 , R 2 , X, X 1 , X 2 , X 3 , and X 4 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.

    Abstract translation: 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，R1，R2，X，X1，X2，X3和X4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介导的病症的方法和制剂，以及与本文公开的化合物，以及制备所述化合物的方法和相应的组合物。

    DIHYDROQUINONE AND DIHYDRONAPHTHRIDINE INHIBITORS OF JNK
    6.
    发明申请
    DIHYDROQUINONE AND DIHYDRONAPHTHRIDINE INHIBITORS OF JNK 审中-公开
    二氢喹啉酮和二氢吲哚啉抑制剂

    公开(公告)号：WO2009015917A2

    公开(公告)日：2009-02-05

    申请号：PCT/EP2008/055470

    申请日：2008-05-05

    Applicant: F. HOFFMANN-LA ROCHE AG ,  ABBOT, Sarah C. ,  BOICE, Genevieve N. ,  GONG, Leyi ,  TAN, Yun-chou

    Inventor： ABBOT, Sarah C. ,  BOICE, Genevieve N. ,  GONG, Leyi ,  TAN, Yun-chou

    CPC classification number: C07D215/48 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04

    Abstract: Compounds fo Formula (I) are effective modulators of INK: wherein X s CR 11 or N; X2 s CH or N; R 1 and R 2 are each independently H, halo, CN, lower alkyl, or -Y 1 -Y 2 -Y 3 -R 8 , or R 1 and R 2 together form -O(CH 2 )nO-, where n is 1 or 2; Y 1 is -O- -C(O)- -C(O)O- -C(O)NR 9 -, -NR 9 C(O)- -S-, or -SO 2 -; Y 2 is lower alkylene or a bond; Y 3 is -O- -C(O)- -C(O)O-, -C(O)NR 9 -, -NR 9 C(O)- -SO 2 -, or a bond; R 8 is H, lower alkyl, cycloalkyl, heterocycloalkyl, or -NR 9 R 10 , wherein R 8 other than H is optionally substituted with lower alkyl, halo or -OH; R 9 and R 10 are each independently H or lower alkyl; R 3 is OH, lower alkyl, lower alkoxy, or -NR 9 R 10 ; R 4 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; R 5 and R 6 are each independently H, halo, cyano, lower alkyl, -CF 3 , lower alkoxy, -OCHF 2 , -NO 2 , or -NR 9 R 10 ; R 11 is H, lower alkyl, lower cycloalkyl, or phenyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 式（I）的化合物是INK的有效调节剂：其中X s CR11或N; X2 s CH或N; 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 - （O）NR9-，-NR9C（O）-S-或-SO2-; Y2是低级亚烷基或键; 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，环烷基，杂环烷基或-NR9R10，其中除H之外的R8任选地被低级烷基，卤素或-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; 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。

    INHIBITORS OF JNK
    9.
    发明申请
    INHIBITORS OF JNK 审中-公开
    JNK的抑制剂

    公开(公告)号：WO2011151357A1

    公开(公告)日：2011-12-08

    申请号：PCT/EP2011/059003

    申请日：2011-06-01

    Applicant: F. HOFFMANN-LA ROCHE AG ,  GONG, Leyi ,  TAN, Yun-chou

    Inventor： GONG, Leyi ,  TAN, Yun-chou

    IPC: C07D487/04 ,  A61K31/4985 ,  A61P19/02 ,  A61P11/06 ,  A61P3/10 ,  A61P29/00

    CPC classification number: C07D487/04

    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein: wherein m, n, p, q, X Y, Z, A, R 1 , R 2 , R 3 , R 4 , R 5 and Y 6 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.

    Abstract translation: 式（I）化合物或其药学上可接受的盐，其中：其中m，n，p，q，X Y，Z，A，R 1，R 2，R 3，R 4，R 5和Y 6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。

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