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Title:
CYCLIC RENIN INHIBITOR CONTAINING 2-SUBSTITUTED (3S,4S)-4-AMINO-5-CYCLOHEXYL-3-HYDROXY PENTANOIC ACID, 2-SUBSTITUTUED (3S,4S)-5-CYCLO-HEXYL-3,4-DIHYDROXY PENTANOIC ACID OR 2-SUBSTITUTED (4S,5S)-5-AMINO-6-CYCLOHEXYL-4-HYDROXYHEXANOIC ACID OR ITS ANALOGS
Document Type and Number:
Japanese Patent JPH06157481
Kind Code:
A
Abstract:

PURPOSE: To prepare a novel compound inhibiting the angiotensinogen-cleaving action of renin.

CONSTITUTION: The compound has the formula I [wherein A is H, aryl or the like; B is -CH2-, the formula II (wherein R3 is H, 1-4C alkyl or the like; R11 is H, 1-4C alkyl; r is of from 0 to 2); D is a single bond, -NH-CO-NH- or the like; Z is -NH2, -OH or the like; W is -O-, -NR23 (wherein R23 is H, 1-4C alkyl); V is the formula III (Y is O, NH or the like; R5 is H, 1-4C alkyl or the like; R10 is H or OH; x and y are each 0 or 1; z is of from 0 to 4) or the like; R15 is 1-4C alkyl, aryl or the like; R1 is 1-4C alkyl, aryl or the like; n is 0 or 1; s is 0 or 1; t is of from 1 to 4]. For example, the compound is the formula IV (wherein A-B is the formula V, V is the formula VI). The compound of the formula I is produced by starting with for example chirarity oxazolidinon and optical active aldehyde to produce 2-substituted ACHPA analogs, then converting to amide derivative and protected amino derivative, obtaining a cyclic precursor, cyclizing them, removing the protect group, and coupling with carbonic acid or the like.


Inventors:
UIRIAMU JIEE GURIINRII
AN II UEEBAA
RARUFU EE RIBUERO
RIFU YANGU
Application Number:
JP15208892A
Publication Date:
June 03, 1994
Filing Date:
June 11, 1992
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
A61K31/335; A61K31/357; A61K31/395; A61K31/40; A61K31/41; A61K31/435; A61K31/445; A61K31/535; A61K38/00; A61P5/38; A61P9/00; A61P9/12; A61P27/02; A61P31/12; A61P43/00; C07D243/00; C07D245/02; C07D267/00; C07D281/00; C07D321/00; C07D327/02; C07D401/12; C07D403/12; C07D405/12; C07D413/12; C07D417/12; C07D453/02; C07D487/04; C07F9/655; C07F9/6558; C07F9/6561; C07K5/02; C07K5/06; C07K5/065; C07K5/078; C07K14/81; (IPC1-7): C07D245/02; A61K31/335; A61K31/395; A61K31/40; A61K31/41; A61K31/435; A61K31/445; A61K31/535; A61K37/02; C07D267/00; C07D281/00; C07D321/00; C07D413/12; C07D417/12; C07D453/02; C07K5/06
Attorney, Agent or Firm:
Masao Okabe (5 others)



 
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