PEPTIDYL FLUORODIOL RENIN INHIBITOR

Japanese Patent JPH03148246

A

NEW MATERIAL: A compd. of formula I [where A=H, alkyl, aryl, heterocycle, etc.; W=CO, CH(OH), NR2 (where R2=H, alkyl); U=CO, CH2, NR2; V=CH, COH, etc.; Q=CHR1CC=CHR1a (where R1 = alkyl, phenoxy, etc.; R1a = aryl, a heterocycle); R3 = alkyl, alkenyl, etc.; R4 = alkyl, benzyl, etc.; R5, R6=CH (OH), CO; Z = alkyl, aryl, etc.].

EXAMPLE: 2(R)2-Benzyl-3morpholinocarbonyl propionic acid amide of his-2(S)- amino-1cyclohexyl-4,4difluoro-3(R), 5(R)dihydroxy-6-methylheptane.

USE: A renin inhibitor.

PROCESS: For example, the compd. of formula I is obtd. by reacting a compd. of formula II or its activated ester with an amine of formula III.

HIN ERU SHIYAMU
SOORU EICHI ROOZENBAAGU

JP23548390A

June 25, 1991

September 05, 1990

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ABBOTT LAB

A61K31/195; A61K31/425; A61K31/426; A61K31/44; A61K31/4427; A61K31/535; A61K31/5375; A61K31/5377; A61K38/00; A61P9/00; A61P9/12; A61P13/02; A61P15/00; A61P17/00; A61P43/00; C07C215/10; C07C215/20; C07C229/06; C07C229/36; C07C233/36; C07C233/47; C07C235/08; C07C259/20; C07C265/08; C07C271/16; C07C271/22; C07C271/48; C07C275/24; C07C309/24; C07C309/82; C07C317/28; C07C317/44; C07C323/25; C07C323/41; C07C323/52; C07C323/60; C07C327/22; C07C327/60; C07D205/04; C07D207/12; C07D213/40; C07D231/12; C07D263/20; C07D263/24; C07D277/20; C07D277/30; C07D277/42; C07D277/46; C07D295/145; C07D295/18; C07D295/185; C07D295/205; C07D295/215; C07D401/12; C07D403/12; C07D417/12; C07D513/04; C07D521/00; C07K1/113; C07K5/06; C07K14/81; (IPC1-7): A61K31/195; A61K31/425; A61K31/44; A61K31/535; A61K37/02; C07; C07C215/10; C07C215/20; C07C229/06; C07C229/36; C07C235/08; C07C265/08; C07C271/48; C07C323/25; C07C323/41; C07C323/60; C07C327/22; C07C327/60; C07D207/12; C07D263/24; C07D277/46; C07D295/18; C07D401/12; C07D403/12; C07D417/12; C07D513/04

Yoshio Kawaguchi (4 outside)

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