Title:
ENZYME INHIBITOR CONTAINING PHOSPHORUS
Document Type and Number:
Japanese Patent JPH02196723
Kind Code:
A
Abstract:
PURPOSE: To obtain an enzyme inhibitor capable of inhibiting renal dehydropeptidase and, in its turn, enhancing antimicrobial activity of carbapenem-based and penem-based antibiotics, comprising a specific phosphorus- containing compound. CONSTITUTION: This enzyme inhibitor comprises a compound of formula I or formula II (R1 is a 2-12C alkyl, a 1-12C substituted alkyl, a 2-12C monoalkenyl, a 2-12C alkynyl, a 7-10C aralkyl, a 4-10C cycloalkylalkyl, a 3-7C cycloalkyl; R2 is H, a 1-12C alkyl, a 2-12C monoalkenyl, a 7-20C aralkyl, a heterocyclic alkyl, a 4-10C cycloalkylalkyl or a 3-7C cycloalkyl; R3 is H, a 2-12C alkyl, a 2-12C monoalkenyl, a 7-20C aralkyl, a heterocyclic alkyl, a 4-10C cycloalkylalkyl or a 3-7C cycloalkyl) such as 1-amino-3-methylbutyl-(2-carboxy-1- hexyl)phosphinic acid. The compound in an amount of 0.1-10mg/kg/day is intravenously or intramuscularly administered together with an antibiotic to enhance the activity of the antibiotic.
Inventors:
UIRIAMU ETSUCHI PAASONZU
AASAA EE PACHIETSUTO
UIRIAMU AARU SHIEEN
AASAA EE PACHIETSUTO
UIRIAMU AARU SHIEEN
Application Number:
JP28002789A
Publication Date:
August 03, 1990
Filing Date:
October 30, 1989
Export Citation:
Assignee:
MERCK & CO INC
International Classes:
C12N9/99; A61K31/40; A61K31/66; A61K31/675; A61P43/00; C07F9/30; C07F9/58; (IPC1-7): A61K31/66; A61K31/675; C12N9/99
Attorney, Agent or Firm:
Masao Okabe (2 outside)
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