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Title:
SUBSTITUTED NUCLEOSIDE DERIVATIVE, ITS PREPARATION AND MEDICAL COMPOSITION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JPH0692986
Kind Code:
A
Abstract:

PURPOSE: To provide a new compound useful as curing agents of AIDS or AIDS- related diseases owing to its excellent selectively inhibiting activity against human immunodeficiency virus.

CONSTITUTION: The compound of formula I or II, e.g. {1-[2',5-bis-O-(tert. butyldimethylsilyl)-β-D-ribofranosyl]-3-N-methyl-thymine}-3'-spiro-5"-{4"- amino-1",2"-oxathiol-2",2"-dioxide}, which is obtained by converting the 2'-keto group of 3'-ketonucleoside into a spiro group. In the formula I or II, B is a pyrimidine of formula III (X5 is H, an alkyl or the like; X4 is OH, SH or the like; X3 is H, benzyl or the like; X2 is O, S or the like) or a purine of formula IV (X6 is H, OH or the like; X7 is H, monomethoxytrithyl or the like) or the like; R'5, R'2 are each trimethylsilyl, an aryl or the like; R'3 is a side-chain of the formula V (R1 is H, alkenyl or the like), or VI (R1 is H, amino or the like; R2 is amino, mercapto or the like); provided that the saccharides in the formula are ribose, glucose or the like.


Inventors:
YAN MARIA REENE BARUZARIINI
ERITSUKU DEJIRE ARISU DE KURAA
MARIAAHOSE KAMARASAARIUSU
MARIAAHESUSU PERESUUPERESU
ANA SANNFUERITSUKUSUUGARUSHIA
Application Number:
JP23702892A
Publication Date:
April 05, 1994
Filing Date:
September 04, 1992
Export Citation:
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Assignee:
STICHTING REGA V Z W
KONSEHO SUPERIOOLE DE INBESUTE
International Classes:
A61K31/7042; A61K31/7052; A61K31/7056; A61K31/7064; A61K31/7068; A61K31/7072; A61K31/7076; A61K31/70; A61K31/708; A61P31/12; A61P31/18; C07D473/00; C07H19/04; C07H19/052; C07H19/056; C07H19/06; C07H19/16; C07H19/23; (IPC1-7): C07H19/06; A61K31/70; C07H19/052; C07H19/056; C07H19/16; C07H19/23
Attorney, Agent or Firm:
Aoyama Ryo (2 outside people)