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    • 9. 发明申请
    • QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONISTS
    • 喹诺酮类衍生物有助于VANILLOID ANTAGONISTS
    • WO2010084050A2
    • 2010-07-29
    • PCT/EP2010/050243
    • 2010-01-12
    • NOVARTIS AGCHEN, WeichunKIM, Hong-YongLIANG, JessicaMUTZ, MichaelPRASHAD, MahavirTOWLER, ChristopherWU, Ruoqiu
    • CHEN, WeichunKIM, Hong-YongLIANG, JessicaMUTZ, MichaelPRASHAD, MahavirTOWLER, ChristopherWU, Ruoqiu
    • A61P11/06C07D239/88A61K31/505
    • C07D239/91A61K31/517
    • 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.
    • 描述了具有结构式I(B)的4-(7-羟基-2-异丙基-4-氧代-4H-喹唑啉-3-基) - 苄腈的新的多晶型物及其制备方法。 还有一种用于制备式(I)的药学活性喹唑啉酮化合物的方法或方法,其中符号具有在说明书中给出的含义,所述方法包括使式(II)化合物(其中R4 * 是R 1 * -C(= O) - 其中R 1 *独立地选自如式(I)化合物所定义的R 1的含义,使得R 1 *和R 1彼此相同或不同,或 R4 *特别是H,并且R 1和R 3,R 5和R 6如式(I)化合物或其盐在与式(III)的苯胺化合物同时或顺序缩合和环化条件下所定义, 其中R 2和m如式(I)化合物所定义。 还要求和公开其他反应和相关实施方案。