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Title:
TUMOR NECROSIS FACTOR PRODUCTION INHIBITOR
Document Type and Number:
Japanese Patent JP2000191659
Kind Code:
A
Abstract:

To obtain the subject new compound consisting of a phthalazine derivative or its prodrug, and having a tumor necrosis factor(TNF) inhibition activity.

This tumor necrosis factor production inhibitor is a compound of formula I [R1 is H or a halogen; R2 to R5 are each H, OH, a halogen, a (substituted) alkyl, an alkoxy, a (substituted) aryl, a (substituted) acyl, a (substituted) acyloxy, nitro, a (substituted) amino or the like; R6 is a substituted alkyl, a (substituted) alkenyl, a (substituted) aryl or the like; R7 is H, a (substituted) alkyl or the like]. For example, 1-[4-(hydroxythienylmethyl) piperidino]phthalazine. The compound of the formula I is obtained as a compound of formula IV, e.g. in the case that R1 is a halogen, by reacting a compound of formula II (X is a halogen) with a piperidine derivative of formula III in an inert organic solvent at temeperatures of preferably 0-200°C.


Inventors:
FUJITA ICHIJI
MURATA SHINOBU
FUJIWARA NORIO
KAWAKAMI HAJIME
Application Number:
JP23899A
Publication Date:
July 11, 2000
Filing Date:
January 04, 1999
Export Citation:
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Assignee:
SUMITOMO PHARMA
International Classes:
C07D401/04; A61K31/00; A61K31/50; A61K31/502; A61P1/00; A61P1/16; A61P3/00; A61P3/10; A61P19/00; A61P19/02; A61P29/00; A61P31/00; A61P31/04; A61P31/18; A61P33/00; A61P33/06; A61P37/00; A61P37/04; A61P43/00; C07D409/14; (IPC1-7): C07D401/04; A61K31/502; A61P1/00; A61P1/16; A61P3/10; A61P19/02; A61P29/00; A61P31/04; A61P31/18; A61P33/06; A61P37/04; A61P43/00; C07D409/14
Attorney, Agent or Firm:
Toshio Nakamura