THIENOPYRIMIDINES, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION ELICITING EFFECT OF INHIBITORS OF PHOSPHODIESTERASE V Russian patent published in 2003 - IPC

Abstract RU 2217431 C2

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to new thienopyrimidines of the formula (I) , their pharmaceutically acceptable salts eliciting effect of inhibitors of phosphodiesterase V. Invention relates also to method for preparing thienopyrimidines of the formula (I) and their pharmaceutically acceptable salts and pharmaceutical composition based on thereof. In thienopyrimidines of the formula (I) R1 and R2 both in common mean alkylene with 3-5 carbon atoms; R3 and R4 each independently each of other means hydrogen atom, A, OA or Hal; R3 and R4 both in common mean also alkylene with 3-5 carbon atoms, -O-CH2-CH2, -O-CH2-O- or O-CH2-CH2-O-; X means R7 or R5 monosubstituted with R6; R5 means linear or branched alkylene with 1-10 carbon atoms; R6 means cycloalkylalkylene with 6-12 carbon atoms; R7 means COOH, COOA, CONH2, CONHA, CON(A)2 or CN; A means alkyl with 1-6 carbon atoms; Hal means fluorine, chlorine, bromine or iodine atom; m = 1 or 2; n = 1, 2 or 3. Method for preparing compounds of the formula (I) and their salts also involves interaction of compound of the formula (II) wherein R1, R2 and X have above indicated values and L means Cl, Br, OH, SCH3 or reactive esterified OH-group with compound of the formula (III) wherein R3, R4 and n have above indicated value followed by if necessary conversion of one residue X to another residue X in compounds of the formula (I), for example, by hydrolysis of ester group to COOH-group or by conversion of COOH-group to amide or to cyano- group and/or by conversion of compound of the formula (I) to one of its pharmaceutically acceptable salts. Pharmaceutical composition contains at least one compound of the formula (I) and/or one of it physiologically acceptable salts. Prepared compounds can be used for control of cardiovascular system and for treatment and/or therapy in potency disorder, for preparing pharmaceutical composition in form useful for treatment. EFFECT: improved preparing method, valuable medicinal properties. 7 cl, 14 ex

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RU 2 217 431 C2

Authors

Jonas Rokhus

Kluksen Frants-Verner

Shelling P'Er

Kristadler Marija

Dates

2003-11-27Published

1998-11-19Filed