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Title:
CYCLIC RENIN INHIBITOR CONTAINING 3(S)-AMINO-4 CYCLOHEXYL-2(R)-HYDROXYBUTYLIC ACID OR 4CYCLOHEXYL-(2R,3R)-DIHYDROXYBUTYLIC ACID OR RELATED ANALOGUE
Document Type and Number:
Japanese Patent JPH05222005
Kind Code:
A
Abstract:

PURPOSE: To provide the subject compound which has the ability to inhibit angiotensinogen-cleaving action of the natural proteolytic enzyme, renin and is useful for preventing and treating renin-associated hypertension, hyperaldosteronism, congestive heart failure and glaucoma.

CONSTITUTION: The compound is expressed by formula I [A is H, Het(Het is monocyclic ring having 5-7 ring members or bicyclic ring having 7-10 ring members, which may be substituted and contains 1 or 2 nitrogen atoms), aryl, etc.; B is formulae II-IV (R3 is H, alkyl, aryl, etc.; R11 and A1 are each H or alkyl), etc., or A and B together form formula V, etc.; R1 is alkyl, aryl, cycloalkyl or saturated heterocycle having 5-6 ring members; R15 is alkyl, aryl, imidazol-4-yl, etc.; D is single bond, O, S, CO, etc.; (s) is 0-1; (t) is I-4; W is O, NR23 (R23is H or alkyl); R16 is H, alkyl, aryl, Het, etc.; Y is OCO, CH2CO, etc.; Z is NH2, OH, alkyl, etc.; R24 is H or alkyl], e.g. the compound of formula IV, and shows inhibiting action against HIV protease.


Inventors:
DARUJITO ESU DANOA
AASAA EE PACHIETSUTO
UIRIAMU JIEE GURIINRII
UIRIAMU ETSUCHI PAASONZU
TOMASU EE HARUGUREN
AN II UEEBAA
RIFU YANGU
Application Number:
JP15246092A
Publication Date:
August 31, 1993
Filing Date:
June 11, 1992
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
A61K31/335; A61K31/357; A61K31/39; A61K31/395; A61K31/40; A61K31/435; A61K31/44; A61K31/4427; A61K31/443; A61K31/445; A61K31/495; A61K31/535; A61P5/38; A61P9/00; A61P9/12; A61P27/02; A61P27/06; A61P31/12; A61P43/00; C07D225/02; C07D245/02; C07D267/00; C07D273/00; C07D273/01; C07D273/02; C07D281/00; C07D285/00; C07D291/02; C07D313/00; C07D321/00; C07D323/00; C07D327/00; C07D327/02; C07D401/12; C07D403/12; C07D405/12; C07D411/12; C07D413/12; C07D417/12; C07D419/12; C07D453/02; C07D487/04; C07F9/6527; C07F9/6558; C07F9/6561; C07K5/02; C07K5/065; C07K5/078; C07K5/097; A61K38/00; (IPC1-7): A61K31/335; A61K31/39; A61K31/395; A61K31/40; A61K31/435; A61K31/44; A61K31/445; A61K31/495; A61K31/535; C07; C07D225/02; C07D245/02; C07D267/00; C07D273/01; C07D273/02; C07D281/00; C07D285/00; C07D291/02; C07D313/00; C07D321/00; C07D323/00; C07D327/00; C07D327/02; C07D401/12; C07D403/12; C07D405/12; C07D411/12; C07D417/12
Attorney, Agent or Firm:
Masao Okabe (5 others)