DERIVATIVES OF BENZONAPHTHOAZULENE, THEIR USING AS INTERMEDIATE SUBSTANCES AND FOR PREPARING PHARMACEUTICAL COMPOSITIONS DESIGNATED FOR INHIBITION OF PRODUCING TNF-α Russian patent published in 2008 - IPC C07D495/04 A61K31/38 A61P19/02 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes derivatives of benzonaphthoazulene of the formula (I): wherein X represents oxygen (O) or sulfur (S) atom; Y and Z mean hydrogen atom; groups of the formula or the formula mean structures of formulae ; R¹ represents compound of the formula (II): wherein R² and R³ can represent simultaneously and independently of one another hydrogen atom (H), (C₁-C₄)-alkyl, or in common with nitrogen atom (N) they mean heterocycle chosen from morpholinyl, piperidinyl or pyrrolidinyl; n means a whole number from 0 to 3; m means a whole number 1; Q₁ and Q₂ represent independently of one another oxygen atom or group of the formula: wherein y₁ and y₂ represent independently of one another hydrogen atom or (C₁-C₄)-alkyl. Also, invention describes derivatives of benzonaphthoazulene of the formula (Ia) given in the invention description and differing from compounds of the formula (I) wherein R¹ represents (C₁-C₇)-alkyl substituted with hydroxyl or (C₁-C₇)-alkyloxycarbonyl. Compounds of the formula (I) inhibit producing TNF-α, and compounds of the formula (Ia) are intermediate substances used in synthesis of compounds of the formula (I). Also, invention describes using compounds of the formula (Ia) wherein R¹ means CO₂Et, CH₂OH for preparing compounds of the formula (I), and using compounds of the formula (I) for preparing pharmaceutical compositions designated for inhibition of production of TNF-α.

EFFECT: valuable properties of compounds and pharmaceutical compositions.

10 cl, 5 tbl, 10 ex