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Title:
IRREVERSIBLE HYMAN IMMUNODEFICIENCY VIRUS(HIV) PROTEASE INHIBITOR, ITS INTERMEDIATE, COMPOSITION AND PREPARATION
Document Type and Number:
Japanese Patent JPH072820
Kind Code:
A
Abstract:

PURPOSE: To obtain a cis-epoxide compound useful for the treatment or prevention of diseases caused by HIV infection having a higher inhibitory effect and a lower cyto toxicity than conventional inhibitors.

CONSTITUTION: The compound of formula I [R1 is cycloalkyl or aryl-substituted alkyl; A is functional acyl of formula II (R2 is alkyl or amide-substituted alkyl; R3 is alkoxy, aryloxyalkyl, arylalkoxy, aromatic group containing N or the like; m is 0 or 1); B is functional amino or the like of formula III (R6 is alkyl, arylalkyl or amide-substituted alkyl; R7 is alkoxy, alkylamino, benzylamino, alkoxyamino, heterocyclic amino containing O; m is 1 or 2) or formula IV (R8 and R9 are each alkyl or aromatic group), e.g. N-[5-L-(N-benzyloxycarbonyl- L-asparaginyl)amino-(4R,3S)-epoxy-6-phenylhexanoyl]-L-isoleucine methylester, or the compound of formula V or formula VI.


Inventors:
KIN SEITEN
SAI RAKUKEN
RI MASANOBU
SON EISAN
SAI KOUJITSU
KOU SHIYOUSEI
IN KOUSHIYOKU
BOKU SHIHIYO
KIN SHIYOUSHIYU
Application Number:
JP30306393A
Publication Date:
January 06, 1995
Filing Date:
December 02, 1993
Export Citation:
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Assignee:
LUCKY CO LTD
International Classes:
A61K31/00; A61K31/336; A61K31/335; A61P31/00; A61P31/12; A61P31/18; C07C213/02; C07C217/08; C07C269/04; C07C271/20; C07C271/22; C07D301/02; C07D303/36; C07D303/38; C07D303/40; C07D303/46; C07D405/12; C07D405/14; C07D493/08; C07K5/02; C07K5/06; C07K5/065; C07K5/078; C07K7/02; A61K38/00; (IPC1-7): C07D303/38; A61K31/335
Attorney, Agent or Firm:
Hajime Tsukuni (2 outside)