公开(公告)号：US20100197705A1

公开(公告)日：2010-08-05

申请号：US12683317

申请日：2010-01-06

Applicant: Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

Inventor： Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

IPC: A61K31/517 ,  C07D239/88 ,  A61P29/00 ,  A61P21/00 ,  A61P19/02

CPC classification number: C07D239/91 ,  A61K31/517

Abstract: 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 R4* is R1*—C(═O)— wherein R1* is independently selected from the group of meanings of R1 as defined for a compound of the formula I so that R1* and R1 are identical to or different from each other, or R4* is especially H, and R1 and R3, R5 and R6 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 R2 and m are as defined for a compound of the formula I. Further reactions and related embodiments are also claimed and disclosed.

Abstract translation: 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R1 * -C （ΟO） - 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，或者R 4 *特别是H，和 R 1和R 3，R 5和R 6如式I化合物或其盐在同时或连续的缩合和环化条件下与式III的苯胺化合物所定义，其中R 2和m如化合物 其他反应和相关实施方案也被要求保护和公开。

公开(公告)号：US08349852B2

公开(公告)日：2013-01-08

申请号：US12683317

申请日：2010-01-06

Applicant: Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

Inventor： Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

IPC: A61K31/517

CPC classification number: C07D239/91 ,  A61K31/517

Abstract: There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and a method of preparing it.

Abstract translation: 描述了一种新的多晶型形式的4-（7-羟基-2-异丙基-4-氧代-4H-喹唑啉-3-基） - 苄腈及其制备方法。

公开(公告)号：US20130060029A1

公开(公告)日：2013-03-07

申请号：US13612259

申请日：2012-09-12

Applicant: Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

Inventor： Weichun Chen ,  Hong-Yong Kim ,  Jessica Liang ,  Michael Mutz ,  Mahavir Prashad ,  Christopher Towler ,  Ruoqiu Wu

IPC: C07D239/91 ,  C07D401/04

CPC classification number: C07D239/91 ,  A61K31/517

Abstract: There is described a process for the manufacture of compounds of the formula I said process comprising reacting a compound of the formula II as described herein, or a salt thereof, under simultaneous or sequential condensation and cyclisation conditions with an aniline compound of the formula III, wherein R2 and m are as defined for a compound of the formula I. Further reactions and related embodiments are also claimed and disclosed.

Abstract translation: 描述了制备式I化合物的方法，所述方法包括使本文所述的式II化合物或其盐在同时或连续的缩合和环化条件下与式III的苯胺化合物反应， 其中R 2和m如式I化合物所定义。其他反应和相关实施方案也被要求保护和公开。