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Document Type and Number:
Japanese Patent JPH0440338
Kind Code:
B2
Abstract:
Novel-Z-2-Acylamino-3-monosubstituted propenic acids and their esters and salts of the formula wherein R1 is, by preference, hydrogen, lower alkyl or a pharmaceutically acceptable cation, R2 is, by preference, methyl substituted cyclopropyl, (cycloalkyl)alkyl, straight alkyl with more than 4 C-atoms or ramified alkyl and R3 is, by preference, optionally substituted alkyl, are prepared by reacting compounds of the formula R3-CH2-@-COOR1 with compounds of the formula R2CONH2 or by acylation of esters of the formula with an acid chloride R2@CI and treating the obtained acylated esters to the formula with t-butylhypochlorite and sodium methoxide, followed by treatment of the resultant intermediate with anhydrous hydrochloric acid. The novel compounds selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products, by preference with the thienamycin class of compounds.

Inventors:
DONARUDO DABURYU GURAHAMU
EDOWAADO EFU ROJAASU
FUREDERITSUKU EMU KEEHAN
Application Number:
JP11062288A
Publication Date:
July 02, 1992
Filing Date:
May 09, 1988
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
C07D333/24; A61K31/16; A61K31/195; A61K31/34; A61K31/341; A61K31/38; A61K31/381; A61K31/40; A61K31/43; A61P43/00; C07C9/00; C07C67/00; C07C69/716; C07C231/00; C07C233/18; C07C233/36; C07C233/47; C07C233/48; C07C233/51; C07C233/59; C07C233/60; C07C233/62; C07C233/63; C07C233/85; C07C235/08; C07C235/10; C07C235/12; C07C235/40; C07C235/76; C07C237/12; C07C237/22; C07C321/18; C07D307/16; C07D477/02; C22C38/08