DERIVATIVES OF THIADIAZOLYLPYRIDAZINE INHIBITING ANGIOGENESIS, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING Russian patent published in 2002 - IPC

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention describes derivatives of thiadiazolylpyridazine of the general formula (I) and their N-oxide forms, pharmaceutically acceptable acid-additive salts and stereochemical isomeric forms where R¹ means hydrogen atom, C_1-6-alkyl, di-(C_1-6-alkyl)-amino-group, hydroxymethyl or benzyloxymethyl; R² and R³ mean hydrogen atom; R⁴ means hydrogen, halogen atom, C_1-6-alkyl, C_1-6-alkoxy-group, trifluoromethyl-, nitro-, amino-group. C_1-6-alkyloxycarbonyl or Het¹; R⁵ means hydrogen, halogen atom, C_1-6-alkyl, C_1-6-alkoxy-, trifluoromethyl- or nitro-group; R⁶ means hydrogen or halogen atom; or if R⁴ and R⁵ are in adjacent position each to other they can form in common bivalent radical of the formula: -CH=CH-CH=CH-; A means bivalent radical of structural formula where X means a direct bond in the formula (a-2) , -O-, -S-, C=O, -NR⁸- or Het²; X means O- in formulas (a-3) and (a-6) ; X means in the formula (a-4) -NR⁸-; R⁷ means hydrogen atom, C_1-6-alkyl or Ar² means methyl; R⁸ means hydrogen atom, C_1-6-alkyl or Ar² means methyl; Alk¹ means C_1-6/ -alkanediyl; Alk² means C_1-4-alkane- -diyl; Ar² means phenyl; Het¹ means monocyclic heterocycle taken among oxazolyl, oxazolinyl or oxadiazolyl substituted by carbon atom with C_1-4-alkyl; Het² means dioxolane. Invention relates also to methods of their synthesis, pharmaceutical composition comprising thereof and method of its preparing. New compounds are inhibitors of angiogenesis and can be used for treatment angiogenesis-dependent diseases, for example, neovascular glaucoma, diabetic retinopathy, psoriasis and rheumatic arthritis. EFFECT: improved method of synthesis and preparing, valuable medicinal properties. 11 cl, 7 tbl