- Certain N-substituted butyramide derivatives
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Disclosed are compound of the formula STR1 wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, or each said grouping substituted by lower alkyl; R and Ro independently represent lower alkyl, (C3 -C7)-cycloalkyl-lower alkyl, or aryl-lower alkyl; A represents methylene; or A represents methylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by aryl-lower alkylthio-lower alkyl, by arylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by aryl-lower alkyloxy-lower alkyl, by aryloxy-lower alkyl, by amino-lower alkyl, by acylamino-lower alkyl, by guanidino-lower alkyl, by (C3 -C7)-cycloalkyl, by (C3 -C7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl; pharmaceutically acceptable ester and amide derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts; methods for synthesis; pharmaceutical compositions thereof; and use thereof as endopeptidase inhibitors.
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- Enkephalinase Inhibitors. 1. 2,4-Dibenzylglutaric Acid Derivatives
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The synthesis of two new series of dicarboxylic acid dipeptides and two sulfhydryl-containing inhibitors are described.The in vitro enkephalinase inhibition data and some in vivo analgesic data are presented for these compounds.For the dibenzylglutaric ac
- Ksander, Gary M.,Diefenbacher, Clive G.,Yuan, Andrew M.,Clark, F.,Sakane, Yumi,Ghai, R. D.
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p. 2519 - 2526
(2007/10/02)
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