[(BENZODIOXANE, BENZOFURAN OR BENZOPYRANE)-ALKYLAMINO]-ALKYL- -SUBSTITUTED GUANIDINES AS SELECTIVE VASOCONSTRICTORS, METHODS OF THEIR SYNTHESIS, INTERMEDIATES FOR THEIR, PHARMACEUTICAL COMPOSITION AND A METHOD OF ITS PREPARING Russian patent published in 1998 - IPC

FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention relates to [(benzodioxane, benzofuran and benzopyrane)-alkyl- -substituted guanidines of the formula (I) , their pharmaceutically acceptable salts, or their stereochemical isomers where X is O, CH₂ or direct bond; R¹ is H, C₁-C₄-alkyl; R² is H, C₁-C₆-alkyl, C₃-C₆-alkenyl, C₃-C₆-alkynyl; R³ is H, C₁-C₄-alkyl; or R² and R¹ taken together can form bivalent radical of the formula -(CH₂)_m where m = 4 or 5; or R¹ and R² taken together can form bivalent radical of the formula -CH=CH- or -(CH₂)_n where n = 2, 3 or 4; or R³ can means a bond when R¹ and R² taken together form bivalent radical of the formula -CH=CH-CH=, -CH=CH-N= or -CH-N=CH= where one or two hydrogen atoms are substituted with halogen atom, C₁-C₆-alkoxy-group, C₁-C₆-alkyl, CN, NH, mono- or di-(C₁-C₆-alkyl)-amino-group, aminocarbonyl, C₁-C₆-alkylaminocarbonylamino-group; R⁴ is H or C₁-C₆-alkyl; Alk¹ means bivalent C₁-C₃-alkanediyl radical; A means bivalent radical of the formula (A) , (b) , (c) , (d) , (e) where each R⁵ is H or C₁-C₄-alkyl where each R⁶ is H or C₁-C₄-alkyl; Alk² means C₂-C₁₅-alkanediyl or C₅-C₇-cyclo- -alkanediyl and each p = 0, 1, 2; R⁷ and R⁸ each means independently H, halogen atom, C₁-C₆-alkyl, hydroxyl, C₁-C₆-alkyl-hydroxycarbonyl, C₁-C₆-alkoxy-group, cyano-group, amino-C₁-C₆-alkyl, carboxyl, nitro- or amino-group, aminocarbonyl, C₁-C₆-alkylcarbonyl-amino-group or mono- or di-C₁-C₆-alkylamino-group at condition that [2-[(2,3-dihydro-1,4-benzodioxine-2-yl)-methyl]-amino] - -ethylguanidine is excluded. Invention describes pharmaceutical preparations containing the derivatives of guanidine as active components, methods of synthesis of the guanidine derivatives and a new p-cyanoguanidine, and intermediate compounds that can be used as vasoconstrictors. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 14 cl, 10 tbl, 30 ex