公开(公告)号：US20080318940A1

公开(公告)日：2008-12-25

申请号：US12096139

申请日：2006-12-06

申请人： Edward Karol Dziadulewicz ,  Christopher Thomas Brain ,  Timothy John Ritchie ,  Andrew James Culshaw

发明人： Edward Karol Dziadulewicz ,  Christopher Thomas Brain ,  Timothy John Ritchie ,  Andrew James Culshaw

IPC分类号： A61K31/5383 ,  C07D239/88 ,  A61K31/517 ,  A61P25/04 ,  C07D487/04 ,  C07D498/04 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The invention relates to quinazolinone compounds of the formula wherein the R groups are defined in the specification, processes for their preparation and their use as pharmaceuticals, particularly in the treatment of disorders ameliorated by administration of TRPV1 antagonists.

摘要翻译： 本发明涉及下式的喹唑啉酮化合物，其中R基团在说明书中定义，其制备方法及其作为药物的用途，特别是治疗通过施用TRPV1拮抗剂而改善的疾病。

公开(公告)号：US20080293939A1

公开(公告)日：2008-11-27

申请号：US11950079

申请日：2007-12-04

申请人： Andrew James Culshaw ,  Edward Karol Dziadulewicz ,  Allan Hallett ,  Terance William Hart

发明人： Andrew James Culshaw ,  Edward Karol Dziadulewicz ,  Allan Hallett ,  Terance William Hart

IPC分类号： C07D239/88

CPC分类号： C07D403/14 ,  C07C229/56 ,  C07D239/90 ,  C07D239/95 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04

摘要： The present invention relates to quinazolinones of formula (I) wherein R1 is hal; a); b); or c); X is N or CR8; R2 is hal; nitro; C1-C6alkylcarbonyl; C1-C6alkyl or C3-C6cycloalkyl; R3 is C1-C6alkyl; C1-C6alkoxy or amino; and wherein the further radicals have the meanings as defined in the specification, which compounds exhibit human vanilloid antagonistic activity; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

摘要翻译： 本发明涉及式（I）的喹唑啉酮，其中R 1为卤素; 一个）; b）; 或c）; X为N或CR8; R2是hal; 硝基 C1-C6烷基羰基; C 1 -C 6烷基或C 3 -C 6环烷基; R3是C1-C6烷基; C1-C6烷氧基或氨基; 并且其中所述其它基团具有如说明书中所定义的含义，所述化合物表现出人类香草素拮抗活性; 其制备方法，它们作为药物的用途以及包含它们的药物组合物。