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41. 发明公开

EP0147211A2 4H-3,1-benzoxazin-4-ones and related compounds, pharmaceutical compositions containing them, and processes for their preparation 有权
标题翻译： 4H-3,1-苯并恶嗪-4-酮及相关化合物，含有它们的进程的药物组合物及其制造。
公开(公告)号：EP0147211A2
公开(公告)日：1985-07-03
申请号：EP84309013.5
申请日：1984-12-21
申请人： SYNTEX (U.S.A.) INC.
发明人： Krantz, Alexander , Tam, Tim F. , Spencer, Robin W.
IPC分类号： C07D265/24 , C07K5/06 , C07K5/08 , A61K31/535
CPC分类号： C07K7/06 , A61K38/00 , C07C265/16 , C07C273/1827 , C07D265/24 , C07K5/06043 , C07K5/06165 , C07K5/0823 , C07K5/101 , C07C275/42
摘要： Novel 2-amino-4H-3,1-benzoxazin-4-ones represented by the formula
and the pharmaceutically acceptable esters and salts thereof wherein R' is hydrogen or lower alkyl;

R 2 and R 3 are each independently hydrogen, halo, lower alkyl, hydroxy, lower alkoxy, lower thioalkyl, -N0 2 , -N(R') 2 , -NR'COR', -NHCON(R') 2 or -NHCOOR',
with the proviso that at least one of R 1 , R 2 and R 3 is not hydrogen when X is NHR or NR'COR"; and
X is a radical chosen trom
in which:
R is lower alkyl, lower alkenyl, lower alkynyl, optionally substituted lower cycloalkyl or optionally substituted phenyl lower alkyl;
each R' is independently hydrogen or lower alkyl, or lower alkenyl or lower alkynyl where the unsaturated bond is at least one carbon removed from the O or N atom;
each R" is independently R, lower alkoxy, NHR' or AOR'; and
A is an amino acid residue, or a peptide of 2 to 3 amino acid residues, are useful as enzyme inhibitors in animals.
摘要翻译：新颖的2-氨基-4H-3,1-苯并恶嗪-4-酮由式表示，并且其药学上可接受的盐和酯worin - [R <1>是氢或低级烷基; [R <2>和R <3>各自独立地是氢，卤素，低级烷基，羟基，低级烷氧基，低级硫代烷基，-NO 2，-N（R“）2，-NR COR分钟分钟，-NHCON（R分钟） 2或--NHCOOR分钟，条件做的R的至少一个<1>，R <2>和R <3>不为氢时，X是NHR或NR COR分秒; 并且X是一个基团，从在其中选择的：R是低级烷基，低级烯基，低级炔基，低级环烷基或任选substituiertem OPTIONALLY substituiertem苯基低级烷基; 每个R min是独立地为氢或低级烷基，或低级链烯基或低级炔基，其中不饱和键的至少一个碳从O或N原子除去每个R独立地秒R，低级烷氧基，NHR min或AOR分钟; 而A是一个氨基酸残基，或2至3个氨基酸残基的肽，如在动物酶抑制剂是有用的。

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