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Title:
HYDROXYLATED INHIBITOR OF HIV REVERSE TRANSCRIPTASE
Document Type and Number:
Japanese Patent JPH05170740
Kind Code:
A
Abstract:

PURPOSE: To provide an inhibitor of HIV reverse transcriptase, which is comprised of a specific pyridinone derivative, etc., and useful for preventing HIV infection and treating HIV infection, AIDS and/or ARC.

CONSTITUTION: The compound of formula I [X is NR, O, S, C(R)H, SO, SO2, CO, C(OR)H (R is H, an alkyl, alkenyl, etc.); Z is O, S, NRx (Rx is H or an alkyl); (n) is 0-4; R1, R2, R4 are each H, an alkyl, alkenyl, alkylthio, alkoxy, cyano, aryl, etc., or R1 and R4 or R1 and R2 together form a cyclic alkyl ring; R3, R5 are each H, an alkyl, alkenyl, cycloalkyl; formula II is an aryl or heterocycle (except phthalimide) which may have substituents], e.g. 3-[2-(4,7- dichlorobenzoxazol-2-yl)ethyl]-5-ethyl-6-hydroxymethylpyridin-2-(1H)-one. The compound of formula I, wherein R4, R5 are each H and Z is O, is obtained by condensing a compound of formula III with a compound of formula IV.


Inventors:
SHIEE SHIYUNGU TOMU CHIEN
ANJIA FUSU
JIYOOJI EE DOSU
MAAKU II GOORUDOMAN
SURESHIYU KEE BARANI
ANSONII DEE TEOHARAIDO
JIYAKOBU EMU HOFUMAN JIYUNIYA
SUTEIIBUN EMU PITSUTSUENBAAGAA
HARI JII RAMUJITO
ROORA AARU KAUFUMAN
BAIRON ETSUCHI ARISON
UORUFURETSUDO ESU SAARI
KURARENSU ESU RUUNII
JIYON ESU WAI
Application Number:
JP33388991A
Publication Date:
July 09, 1993
Filing Date:
October 18, 1991
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
A61K31/44; A61K31/4418; A61K31/4425; A61K31/443; A61K31/4433; A61K31/47; A61P31/12; A61P31/18; A61P43/00; C07D213/64; C07D213/69; C07D213/70; C07D213/74; C07D401/12; C07D405/06; C07D405/12; C07D409/06; C07D409/12; C07D413/06; C07D413/12; C07D417/06; C07D417/12; C07D498/04; C12N9/99; C12P17/12; C12P17/16; (IPC1-7): A61K31/44; A61K31/47; C07D213/64; C07D213/69; C07D213/70; C07D213/74; C07D405/06; C07D405/12; C07D409/06; C07D409/12; C07D413/06; C07D413/12; C07D417/06; C07D417/12; C07D498/04; C12N9/99
Domestic Patent References:
JPH04253961A1992-09-09
Attorney, Agent or Firm:
Masao Okabe (6 others)