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Title:
DI-OR TRIPEPTIDE RENIN INHIBITORS CONTAINING LACTAM CONFORMATIONAL RESTRICTION IN ACHPA
Document Type and Number:
Japanese Patent JPH01207300
Kind Code:
A
Abstract:

NEW MATERIAL: The compound of formula [A is H, 1-6C alkyl or the like; B and D are each formula II, III (R12 is H, 1-5C alkyl or the like; R2 is 1-7C alkyl, H or the like) or the like; R1 is H, 3-6C alkyl or the like; X is formula IV or V (R13 or R14 are H, 2-7C alkenyl or the like); E is H, aryl, alkenyl or the like] and its salt.

USE: Antihypertensive agents, remedies of hyperaldosteronism, etc. Having high oral bioavailability and long acting duration.

PROCESS: For example, BOC-protected amino alcohol derivative is obtained by using N-tert-butyloxylcarbonyl-cyclohexylaranyl, etc., after enolate of 2- pyrrolidinone is prepared by allowing a 2-pyrrolidinone derivative to react in the presence of a base such as lithiumisopropylamide, etc. The compound of formula I is obtained by allowing BOC-protected amino alcohol derivative to bond to an amino acid according to a method of synthesis of a peptide after an N protective group is eliminated and again eliminating a protective group.


Inventors:
PEETAA DEE UIRIAMUSU
DANIERU EFU BUEEBAA
UIRIAMU JIEE GURIINRII
JIYAN TEN BUREEKE
Application Number:
JP25929188A
Publication Date:
August 21, 1989
Filing Date:
October 14, 1988
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
C12N9/99; A61K38/55; A61P9/00; A61P29/00; C07D207/267; C07D207/27; C07D207/28; C07D233/54; C07D401/04; C07D403/12; C07D453/02; C07K5/02; C07K5/06; C07K14/81; (IPC1-7): A61K37/64; C07D207/267; C07D207/27; C07D207/28; C07D401/04; C07D453/02; C07K5/06; C12N9/99
Attorney, Agent or Firm:
Masao Okabe (2 outside)