THIENOPYRIMIDINES, METHOD OF THEIR SYNTHESIS (VERSIONS), PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING Russian patent published in 2003 - IPC

Abstract RU 2199541 C2

FIELD: organic chemistry, heterocyclic compounds, medicine, pharmacy. SUBSTANCE: invention relates to novel thienopyrimidines of the general formula (I) or their physiologically acceptable salts comprising properties of inhibitors of activity of phosphodiesterase V. These compounds can be used in pharmaceutical industry for treatment of patients with cardiovascular diseases, in part, cardiac insufficiency and for therapy of potency disorder. In compounds of the general formula (I) R1 and R2 mean independently each of other H, A or Hal being one of residue R1 or R2 does not mean H; R1 and R2 mean in common also alkylene with 3-5 carbon atoms; R3 and R4 mean independently each of other H, OA or Hal; R3 and R4 mean in common also -O-CH2-O- or -O-CH2-CH2-O-; A means alkyl with 1-6 carbon atoms; X means 1-imidazolyl, 2-methyl-imidazolyl, pyrazolyl, 1,2,4-triazolyl-1-yl or 3-pyridyl; Hal means F, Cl, Br or J atoms; n = 1 under condition that if R1 and R2 mean H, A or Hal independently each of other being one of residue R1 and R2 does not mean H always then R3 and R4 do not mean in common H. Invention relates also to method of synthesis of compound of the formula (I) where X is bound through N-atom involves interaction of compound of the formula (II) with imidazole, 2-methylimidazole, pyrazole, 1,2,4-triazole or in the case of synthesis of compounds where X is bound through C-atom by interaction of compound of the formula (III) with compound of the formula (IV) where L means Cl, Br, OH, SCH3 or reactive esterified OH-group; R1-R4 and n have values indicated above with the following if necessary treatment of synthesized base with acid to obtain physiologically acceptable salt. Invention relates also to pharmaceutical composition comprising at least one of the above- mentioned compounds as suitable form for dosing and method of composition preparing. EFFECT: improved method of synthesis, valuable medicinal properties of compounds. 8 cl, 1 tbl, 16 ex

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RU 2 199 541 C2

Authors

Rokhus Jonas

Shelling P'Er

Kluksen Frants-Verner

Kristadler Marija

Dates

2003-02-27Published

1997-07-30Filed