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2 196 139

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IPC

(21) (22)

Application

97113753/04, 1996-01-11

(24)

Start date

1996-01-11

(22)

Actual filing date

1996-01-11

(45)

Published

2003-01-10

(72)

Inventor

Ehdams Dzherri LerojGallager Timoti F.Garidzhipati Ravi ShankerBoem Dzheffri Charl'ZSisko DzhozefLi Dzhon Cheung-Lun

(73)

Holder

Smitklajn Bicham Korporejshn

1,4,5-TRISUBSTITUTED IMIDAZOLE DERIVATIVES, METHODS OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2003 - IPC

Abstract RU 2196139 C2

FIELD: organic chemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to method of synthesis of derivatives of imidazole of the formula (A) where R₁ means substituted heterocycle; R₄ means optionally substituted phenyl; R₂ means alkyl-N3, -(CR₁₀R₂₀)_nOR₉ and further as given in description. Method involves interaction of compound of the formula (II) with compound of the formula (III) . Also, invention relates to methods of synthesis of: a) compound of the formula (IV) by interaction of R₄-CHO with formamide, acid catalyst and dehydrogenated agent; b) compound of the formula (IV) involving interaction of compound of the formula (I) with p-toluenesulfinic acid, acid catalyst and organic solvent. By claim 1 compounds exhibit inhibitory activity with respect to cytokines and therefore they can be used as active component in pharmaceutical composition. EFFECT: improved methods of synthesis, valuable biological and medicinal properties. 30 cl

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RU 2 196 139 C2

Authors

Ehdams Dzherri Leroj

Gallager Timoti F.

Garidzhipati Ravi Shanker

Boem Dzheffri Charl'Z

Sisko Dzhozef

Li Dzhon Cheung-Lun

Dates

2003-01-10—Published

1996-01-11—Filed