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    QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONISTS
    1.
    发明公开
    QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONISTS 有权
    喹唑啉酮衍生物作为香草素拮抗剂

    公开(公告)号：EP2387440A2

    公开(公告)日：2011-11-23

    申请号：EP10701640.4

    申请日：2010-01-12

    申请人： Novartis AG

    发明人： CHEN, Weichun ,  KIM, Hong-Yong ,  LIANG, Jessica ,  MUTZ, Michael ,  PRASHAD, Mahavir ,  TOWLER, Christopher ,  WU, Ruoqiu

    IPC分类号： A61P11/06 ,  C07D239/88 ,  A61K31/505

    CPC分类号： C07D239/91 ,  A61K31/517

    摘要： There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin- 3-yl)-benzonitrile having structural formula I(B) and to a method of preparing it. There is further a process or method for the manufacture of a pharmaceutically active quinazolinone compounds of the formula (I), wherein the symbols have the meanings given in the description, said process comprising reacting a compound of the formula (II), wherein R
    4 * is R
    1 *-C(=O)- wherein R
    1 * is independently selected from the group of meanings of R
    1 as defined for a compound of the formula (I) so that R
    1 * and R
    1 are identical to or different from each other, or R
    4 *is especially H, and R
    1 and R
    3 , R
    5 and R
    6 are as defined for a compound of the formula (I), or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula (III), wherein R
    2 and m are as defined for a compound of the formula (I). Further reactions and related embodiments are also claimed and disclosed.