AMINO ACID DERIVATIVE AND ENKEPHALINASE INHIBITOR CONTAINING THE SAME AS AN ACTIVE INGREDIENT
Document Type and Number:
Japanese Patent JP02209861
NEW MATERIAL:A compound of formula I [R1 is H, 1-4C alkyl; R2 is a carbon ring or a heterocyclic ring which may substituted with R3; R3 is halogen, trihalomethyl, hydroxyl, 1-15C alkyl; Z is H, -COR9 (R9 is 1-4C alkyl, substituted phenyl); (A) is phenyl substituted with R13 (R13 is H, halogen) or 4-7C cycloalkyl; when m=0, n is 1 to 4, when n=0, m is 1 to 4], its salt or acid adduct.
EXAMPLE: N-(3-Mercapto-2RS-cyclohexylmethylpropionyl)-α-anilino-L-glutamic acid.
USE: Analgesic, antianxiety or anticonvulsant.
PREPARATION: In accordance with the reaction equations, an amine of formula II (t-Bu is tertiary butyl) is allowed to react with a carboxylic acid to form an amide bond. The reaction 2 is conducted using 2-mercaptoethylamine in a solvent such as methylene chloride to give the subject compound.
August 21, 1990
May 02, 1989
ONO PHARMACEUT CO LTD
A61K31/195; A61K31/19; A61K31/215; A61K31/225; A61K31/265; A61K31/275; A61K31/335; A61K31/34; A61K31/343; A61K31/357; A61K31/425; A61K31/428; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/495; A61K31/505; A61K31/55; A61K31/551; A61P25/04; A61P25/08; A61P25/20; A61P43/00; C07C323/51; C07C323/60; C07C327/06; C07C327/32; C07D213/75; C07D213/83; C07D237/20; C07D239/42; C07D241/20; C07D243/16; C07D277/82; C07D307/88; C07D317/32; C07D417/12; C07D521/00; C07F7/18; C12N9/99; (IPC1-7): A61K31/19; A61K31/225; A61K31/265; A61K31/335; A61K31/34; A61K31/425; A61K31/44; A61K31/495; A61K31/55; C07C323/60; C07C327/06; C07D213/75; C07D239/42; C07D241/20; C07D243/16; C07D277/82; C07D307/88; C07D317/32; C07D417/12; C07D521/00; C12N9/99