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13 条记录 (耗时 0.016 秒)

    Pyrazines and Pyridines and Derivatives Thereof as Therapeutic Compounds
    13.
    发明申请
    Pyrazines and Pyridines and Derivatives Thereof as Therapeutic Compounds 失效

    公开(公告)号：US20080015191A1

    公开(公告)日：2008-01-17

    申请号：US11722612

    申请日：2005-12-22

    申请人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Esteban Vela ,  Adrian Gill ,  Richard Taylor ,  Richard Marais

    发明人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Esteban Vela ,  Adrian Gill ,  Richard Taylor ,  Richard Marais

    IPC分类号： A61K31/4965 ,  A61K31/497 ,  A61K31/5377 ,  A61P35/00 ,  C07D241/16 ,  C07D241/18 ,  C07D241/20 ,  C07D413/12

    CPC分类号： C07D213/74 ,  C07D241/20 ,  C07D317/46 ,  C07D319/18 ,  C07D321/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： The present invention pertains to certain pyrazines and pyridines, and derivatives thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: (I) wherein: Q is independently —N═ or —CH═; one of RP2 and RP3 is independently a group of the formula -J1-L1-Z; wherein: if Q is —N═, then -J1-L1-Z is independently: —NH-Z; —O-Z; or S-Z; if Q is —CH═, then -J1-L1-Z is independently: —NH—(CH2)n-Z, wherein n is independently 0 or 1; —O-Z; or —S-Z; Z is independently: C6-14 carboaryl, C5-14 heteroaryl, C3-12carbocyclic, C3-12 heterocyclic; and is independently unsubstituted or substituted; the other of RP2 and RP3 is independently —H, —NHRN1, or —NHC(═O)RN2; wherein: RN1, if present, is independently —H or aliphatic saturated C1-4alkyl; RN2, if present, is independently —H or aliphatic saturated C1-4alkyl; one of RP5 and RP6 is independently a group of the formula —W—Y; wherein: W is independently: a covalent bond; —NRN4—, —O—, —S—, —C(═O)—, —CH2—; —NRN4—CH2—, —O—CH2—, —S—CH2—, —C(═O)—CH2—, —(CH2)2—; —CH2—NRN4—, —CH2—O—, —CH2—S—, or —CH2—C(═O)—; wherein RN4, if present, is independently —H or aliphatic saturated C1-4alkyl; Y is independently: C6-14carboaryl, C5-14heteroaryl, C3-12carbocyclic, C3-12heterocyclic; and is independently unsubstituted or substituted; the other of RP5 and RP6 is independently —H; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, e.g., both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.