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Novel quinazolinones and related compounds for use as anti-inflammatory agents
专利权人:
RESVERLOGIX CORP.
发明人:
HANSEN C. HENRIK
申请号:
NZ59574710
公开号:
NZ595747A
申请日:
2010.03.16
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
Disclosed are 5,7-dimethoxy-2-phenyl-4-oxo-3,4-dihydroquinazolines and analogues thereof or a stereoisomer, tautomer, pharmaceutically acceptable salt, or hydrate thereof, wherein: Q is selected from CR12 and nitrogen; V is selected from CH and nitrogen; U is C=O; -X-(Z)n-G is selected from 1-[(dimethylamino)carbonyl]piperidin-4-yloxy, 1-acetylpiperidin-4-yloxy, 2-(isoindolin-2-yl)ethoxy, (4-acetylpiperazin-1-yl)ethoxy, (1H-imidazol-1-yl)ethoxy, (piperidin-1-yl)ethoxy, 2-(1-isopropyl-2,4-dioxo-imidazolidin-3-yl)-ethoxy, 2-(5-phenyl-2,4-dioxo-imidazolidin-3-yl)-ethoxy, (2,4-dioxo-imidazolidin-3-yl)methyl, 2-(azepan-1-yl)ethoxy, 2-(azetidin-1-yl)ethoxy, 2-(3-(acetylamino)-azetidin-1-yl)ethoxy, (5-oxopyrrolidin-2-yl)methoxy, [4-{ acetyl(isopropyl)amino} piperidin-1-yl]methyl, (4-(isopropylamino)piperidin-1-yl)methyl, 2-(2,5-dioxo-pyrrolidin-1-yl)ethoxy and (1H-tetrazol-5-yl)methyl; R12 is selected from hydrogen, alkoxy, and halogen; Rc is selected from hydrogen and (pyrrolidin-1-yl)propyl; Ra1, Ra2, and Ra3 are independently selected from hydrogen, alkyl, alkoxy, halogen, and heterocycle; Rb2 and Rb6 are hydrogen; and Rb3 and Rb5 are independently selected from hydrogen and alkyl; provided that at least one of Ra1, Ra2, and Ra3 is not hydrogen; if Ra2 or Ra3 is chloro, then Ra1 is not hydrogen; with at least one proviso selected from: Rc is not hydrogen; Rb3 is hydrogen; V is not N; and X-(Z)n is not ethoxy. Representative compounds include 4-(4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenoxy)-N,N-dimethylpiperidine-1-carboxamide; 2-(4-(1-acetylpiperidin-4-yloxy)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one; 3-(4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)benzyl)imidazolidine-2,4-dione; (S)-2-(3,5-dimethyl-4-((5-oxopyrrolidin-2-yl)methoxy)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one; N-(1-(4-(5,7-dimethoxy-4-oxo-3,4-dihydroquinazolin-2-yl)benzyl)piperidin-4-yl)-N-isopropylacetamide; 2-(4-((4-(isopropylamino)piperidin-1-yl)methyl)phenyl)-5,7-dimethoxyquinazolin-4(
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中国工程科技知识中心
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