AMINO ACID DERIVATIVE AND ITS USE AS MEDICAMENT

Title:

AMINO ACID DERIVATIVE AND ITS USE AS MEDICAMENT

Document Type and Number:

Japanese Patent JP2628820

Kind Code:

B2

Abstract:

PURPOSE: To obtain the subject novel compd. which inhibits the activity of natural enzyme renin and is useful for the suppression, prevention and treatment of high blood pressure and cardiac insufficiency.
CONSTITUTION: A compd. of formula I {R1 is a cycloalkyl, phenyl, etc.; R2 is H, methyl; R3 is H, an alkyl, etc.; R4 is a (substd.) cycloalkyl, etc.; R5 is a cycloalkyl, an alkyl, etc.; B is S, SO2, etc.; A is formula II [R6R8 is H, an alkyl; R9 is H, an alkyl, etc.; X is Y-CO (Y is a cycloalkylamino, etc.), etc.]}. For example, (S)-N[(1S,2R,3S)-1(cyclohexylmethyl)3-cyclopropyl-2,3 dihydroxypropyl]-α[(S)-α-[[[1-[2hydroxy-1(hydroxymethyl)1- methylethyl]carbamoyl]1-methylethy]sulfonyl] methyl]hydrocinnamamide] imizole-4-propioneamide. The compd. of formula I is obtd. by bringing a compd. of formula III and a compd. of formula IV into reaction.

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Inventors:

Chirico Blanca
Marie-Paul Heights
Berner Nighthard
Heinz Stadtler
Eric Huieira
Wolfgang Bostor

Application Number:

JP12139592A

Publication Date:

July 09, 1997

Filing Date:

April 15, 1992

Export Citation:

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Assignee:

F. Hoffman-La Rochille Age

International Classes:

A61K31/165; A61K31/215; A61K31/22; A61K31/415; A61K31/425; A61K31/426; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/4418; A61K31/4427; A61K31/443; A61K31/4433; A61K31/535; A61P9/00; A61P9/04; A61P9/12; C07C317/44; C07C317/50; C07C323/51; C07D207/08; C07D207/12; C07D211/22; A61K31/16; C07D213/40; C07D213/53; C07D213/56; C07D231/12; C07D233/54; C07D233/56; C07D233/58; C07D233/60; C07D233/61; C07D233/64; C07D277/20; C07D277/30; C07D295/088; C07D295/185; C07D295/205; C07D307/54; C07D317/24; C07D333/24; C07D401/12; C07D403/12; C07D405/12; C07D409/12; C07D417/12; C07D521/00; C07H15/12; (IPC1-7): C07C317/44; A61K31/16; A61K31/165; A61K31/215; A61K31/22; A61K31/415; A61K31/425; A61K31/44; A61K31/535; C07C323/51; C07D213/56; C07D231/12; C07D233/58; C07D233/61; C07D233/64; C07D277/30; C07D307/54; C07D333/24; C07D401/12; C07D405/12; C07D409/12; C07D417/12; C07H15/12

Domestic Patent References:

JP1502514A

Attorney, Agent or Firm:

Heiyoshi Odashima

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