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QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONITS
专利权人:
NOVARTIS AG
发明人:
CHEN WEICHUN,KIM HONG-YONG,LIANG JESSICA,MUTZ MICHAEL,PRASHAD MAHAVIR,TOWLER CHRISTOPHER,WU RUOQIU
申请号:
TN2011000326
公开号:
TN2011000326A1
申请日:
2011.07.29
申请国别(地区):
TN
年份:
2012
代理人:
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 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.
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