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    Inhibitors of C-FMS kinase
    3.
    发明申请
    Inhibitors of C-FMS kinase 审中-公开

    公开(公告)号：US20050113566A1

    公开(公告)日：2005-05-26

    申请号：US10970903

    申请日：2004-10-22

    申请人： Mark Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond Patch ,  Davoud Asgari ,  Taxiarchis Georgiadis

    发明人： Mark Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond Patch ,  Davoud Asgari ,  Taxiarchis Georgiadis

    IPC分类号： A61K31/16 ,  A61K31/195 ,  A61K31/452 ,  A61K31/4545 ,  C07D223/12 ,  C07D265/30 ,  C07D279/12 ,  C07D307/68 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D405/12 ,  C07D307/68 ,  C07D409/12

    摘要： The invention relates to compounds of Formula I: wherein A is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoalkyl, heteroaryl, halogen, hydroxy, —CF3, alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, —OCF3, —OCO-alkyl, —CORA, —CN, —C(NH)NH2, —COORa, —CONRaRb, —N(Ra)CORb, —NO2, —SO2Ra, —SO3Ra or —SO2NRaRb; or a 5- to 7-membered mono- or a 8- to 10-membered bicyclic heteroaromatic ring having from one to four heteroatoms selected from N, O or S, and may be optionally substituted with one or more of -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, sulfonamidoalkyl, guanidinoalkyl, heteroaryl, halogen, hydroxy, —CF3, alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, —OCF3, —OCO-alkyl, —CORa, —CN, —C(NH)NH2, —COORa, —CONRaRb, —N(Ra)CORb, —NO2, —SO2Ra, —SO3Ra or —SO2NRaRb; R1 is —H, aryl, —CORa, —CORa, —COORa, —CONRaRb, —SO2Ra or —SO2NRaRb; X is —CO—, —C(═NH)—, —CS—, —CON(Ra)—, —CS(NRa)—, —SO2— or —CRaRb—; Y is —S—, —SO—, —SO2—, —O— or direct link; R2 is alkyl, cycloalkyl, heterocyclyl, aryl or heteroaryl, each of which may be optionally substituted with one or more halogens; and W is phenyl, naphthyl or biphenyl, each of which may be optionally substituted with one or more of C1-4 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, halogen, hydroxy, —CF3, alkoxy, aryloxy, arylalkoxy, —OCF3, —CORa, —CN, —C(NH)NH2, —COORa, —CONRaRb, —NHCORaRb, —NHSO2Ra, —NO2, —SORa, —SO3Ra or —SO2NRaRb; or a 5- to 6-membered mono- or a 8- to 10-membered bicyclic heterocyclic or heteroaromatic ring having from one to four heteroatoms selected from N, O or S, and may be optionally substituted with -C1-6 alkyl, amino, aminoalkyl, hydroxyalkyl, alkoxyalkyl, heteroaryl, halogen, hydroxy, —CF3, alkoxy, aryl, aralkyl, heteroaralkyl, aryloxy, arylalkoxy, —OCF3, —OCO-alkyl, —OCO-alkylamino, —OCO-alkylamido, CORa, —CN, —C(NH)NH2, —COORa, —CONRaRb, —N(Ra)CORb, —NO2, —SO2Ra, —SO3Ra or —SO2NRaRb; as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

    Stabilizing ligands for regulation of protein function
    9.
    发明授权
    Stabilizing ligands for regulation of protein function 失效
    稳定配体调节蛋白质功能

    公开(公告)号：US08153785B2

    公开(公告)日：2012-04-10

    申请号：US12754707

    申请日：2010-04-06

    申请人： Uday Khire ,  Davoud Asgari

    发明人： Uday Khire ,  Davoud Asgari

    IPC分类号： C07D413/12

    CPC分类号： C07D211/60

    摘要： The invention pertains to novel compounds of Formula (I) wherein R1, R2, R3, W, Y, Z, A, m, n, p, and q are defined herein. Such compounds are useful as stabilizing ligands in systems that assist in the determination of protein function.

    摘要翻译： 本发明涉及式（I）的新化合物，其中R 1，R 2，R 3，W，Y，Z，A，m，n，p和q在本文中定义。 这些化合物可用作有助于测定蛋白质功能的体系中的稳定配体。