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Title:
PYRIDO(2,3-B)(1,5)BENZOXAZEPIN (AND THIAZEPIN)-5(6H)-ONES AND THIONES AND PHARMACEUTICAL FORMULATOR CONTAING THEM FOR PROPHYLANIS AND TREATMENT OF HIV INFECTIOUS DISEASE
Document Type and Number:
Japanese Patent JPH04178390
Kind Code:
A
Abstract:

NEW MATERIAL: A compound of formula I (X, Z is O or S; R1 is 1-5C alkyl, 1-5C fluoroalkyl with 1-3F, 3-5C cycloalkyl, mono- or dihalovinyl, etc.; one of R2, R3 and R4 is 1-4C alkyl, 2-4C alkenyl, etc., another being H or methyl, and the other being H, or two of R2, R3 and R4 are methyl, chloro, etc., the other being H, or all of R2, R3 and R4 are H; one from R5-R8 is 1-4C alkyl, 2-4C alkenyl, etc., another being H, methyl, etc., and the remaining two being H, or all of R5-R8 are H.

EXAMPLE: 3-Amino-6,9-dimethylpyrido[2,3-b][1,5]benzoxazepin-5(6H)-one.

USE: Prevention and treatment of HIV infection.

PROCESS: A compound of formula II is converted to the corresponding alkali (earth) metal compound of formula III, which is then reacted with a reagent of R1Y (Y stands for a detaching group) under alkylation or acylation conditions.


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Inventors:
GIYUNTAA SHIYUMITSUTO
KAARU DEII HAAGUREIBU
Application Number:
JP22641090A
Publication Date:
June 25, 1992
Filing Date:
August 28, 1990
Export Citation:
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Assignee:
BOEHRINGER INGELHEIM PHARMA
THOMAE GMBH DR K
International Classes:
A61K31/55; A61K31/553; A61K31/554; A61P31/12; C07D498/04; C07D513/04; (IPC1-7): A61K31/55; C07D498/04; C07D513/04
Attorney, Agent or Firm:
Minoru Nakamura (8 outside)