PYRIDONE DERIVATIVES, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 1998 - IPC

Abstract RU 2124004 C1

FIELD: organic chemistry and technology, pharmacy. SUBSTANCE: invention related to derivatives of pyridone of the formula (I') where R1 is C1-C4--alkyl; R2 - hydrogen; R3 is SC6H5,; R4 is CH2OR13 where R13 - hydrogen, benzyl; R′ - tetrazolyl. Method of synthesis of compounds of the formula (I') involves interaction of compound of the formula (II') : AO-CH=C(R3)-C(O)R4 where R3 and R4 have values indicated above with compound of the formula (III'): R1-CH=C(R2)-O-alk where R1 and R2 have values indicated above, and alk - alkyl containing 5 carbon atoms, not more. Synthesized compound of the formula (IV') is saponificated to compound of the formula (V') and oxidized and formed compound of the formula (VI') is subjected for reaction of alkylhydroxy-group elimination to compound of the formula (VII') and the latter is subjected for interaction with compound of the formula (VIII') . Invention proposes also a pharmaceutical composition showing antagonistic activity with respect to receptors of angiotensin-II and containing compound of the formula (I') as an active component at effective dose. These compounds can be used in medicine. EFFECT: improved method of synthesis, enhanced pharmacological activity of compounds. 4 cl, 1 tbl, 4 ex

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RU 2 124 004 C1

Authors

Mishel' Forten

Zhan-Ljuk Aessleen

Bertran Ekkmann

Dates

1998-12-27Published

1993-02-05Filed