ADENOSINE DERIVATIVES, METHOD OF PREPARING THEREOF, PHARMACEUTICAL COMPOSITION, AND METHOD OF PREPARING THEREOF Russian patent published in 1999 - IPC

FIELD: pharmaceutical industry. SUBSTANCE: invention describes adenosine derivatives of general formula (I): R₁ wherein R₂ is hydrogen atom, halogen atom, lower alkyl, lower-O-alkyl, lower-S-alkyl or phenyl and is in 2-or 5-position of indole; n is 0.1 or 2; C₃-C₇ is lower alkyl, lower alkenyl, lower alkynyl; -NR₆R₇ cycloalkyl or lower-O-alkyl, phenyl optionally substituted by one to four substituents selected from halogen atom, nitro, lower alkyl or O-alkyl or R₆ wherein R₇ and R₂ are hydrogen atom, lower alkyl, pyridyl, thienyl, naphthyl; and when n is 2, NR₈R₉ is R₈ wherein R₉ and R₃ are simultaneously lower alkyl or together with nitrogen atom to which they are attached, form heterocycle selected from morpholine or piperidine; R₄ and R₁₁, identical or different, are hydrogen atom or lower alkyl, having analgetic and antihypertensive activities. Method of preparing compounds of formula (I) comprises reacting amine of general formula (II): COR₅ with 7-halogenpyrine riboside of general formula (III): R₅ wherein X is halogen atom; CH₂OH is R₁₂ wherein R₁₃ is as defined above, or , and and are protective groups such as acetyl or benzoyl, or together form dioxolane group in solvent such as alcohol or dimethylformamide in the presence of base such as triethyl amine, pyridine or sodium carbonate, or additionally, in the presence of two equivalents of amine at temperatures from 20 C to 140 C, subsequently removing protective groups in basic medium with ammonium hydroxide solution, or in acid medium, with normal hydrochloric acid solution at temperatures between 0 C and 70 C depending on type of protective group. Present invention also describes pharmaceutical compositions based on compound of formula (I) having analgesic and/or antihypertensive activity. EFFECT: improved properties of the pharmaceutical composition. 14, cl, 156 ex, 2 tbl