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.
WO/1994/021651 | TAXANES HAVING FURYL OR THIENYL SUBSTITUTED SIDE-CHAIN |
JP2008501767 | Indole derivative as an antiviral agent |
MURATA SHINOBU
FUJIWARA NORIO
KAWAKAMI HAJIME
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