PHOSPHONIC ACID DERIVATIVE ITS PRODUCTION AND USE

PURPOSE:To obtain the subject new compound having an endothelin transferase- inhibiting activity and useful as a therapeutic agent for hypertension, cardiac or cerebral circulation doseases or renal diseases, etc., by reacting a specific organic phosphorus compound and a dipeptide compound, and subs...

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Bibliographic Details
Main Authors MORI MASAAKI, WAKIMASU MITSUHIRO, KAWADA AKIRA
Format Patent
LanguageEnglish
Published 27.04.1993
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:PURPOSE:To obtain the subject new compound having an endothelin transferase- inhibiting activity and useful as a therapeutic agent for hypertension, cardiac or cerebral circulation doseases or renal diseases, etc., by reacting a specific organic phosphorus compound and a dipeptide compound, and subsequently subjecting the reactional product to a protecting group-removing treatment. CONSTITUTION:An organic phosphorus compound of formula I [A is protected hydroxy; R1' is (substituted) hydrocarbon; X is halogen] (e.g. O-benzyl-p- phenetylphosphochloridate) is reacted with a dipeptide compound of formula II [Y is protected carboxyl; R2', R3' are (substituted) hydrocarbon] or its salt (e.g. N-t-butyloxycarbonyl-leucyl-tryptophan benzyl ester) and, if necessary, the reactional product is subjected to a protecting group-removing treatment to obtained the objective phosphonic acid derivative (salt) of formula III [R1-R3 are (substituted)hydrocarbon][e.g. N-(phenethylphosphonyl)-leucyltryptophan disodium salt[.
Bibliography:Application Number: JP19920089111