CONDENSED THIENOPYRIMIDINES INHIBITING ACTIVITY OF PHOSPHODIESTERASE V, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION Russian patent published in 2004 - IPC

Abstract RU 2224760 C2

FIELD: organic chemistry, biochemistry, chemical technology, pharmacy. SUBSTANCE: invention relates to new condensed thienopyrimidines of the formula (I) and their physiologically acceptable salts acting as inhibitors of activity of phosphodiesterase V (PDE V) that can be used for treatment of cardiovascular system and for treatment and/or therapy of disorder of sexual potency. In compounds of the formula (I) R1, R2 each means independently of one another hydrogen atom, OA or Hal; R1 and R2 in common mean also alkylene with 3-5 carbon atoms, -O-CH2-CH2-, -CH2-O-CH2-, -O-CH2-O- or -O-CH2-CH2-O-; X means R4, R5 or R6 substituted once with substituent R7; R4 means linear or branched alkylene with 1-10 carbon atoms; R5 means cycloalkyl or cycloalkylalkylene with 5-12 carbon atoms; R6 means phenyl or phenylmethyl; R7 means COOH or COOA wherein A means alkyl with 1-6 carbon atoms; Hal means fluorine, chlorine, bromine or iodine atom. Invention relates also to method for preparing compounds of the formula (I). Method for preparing involves interaction of compound of the formula (II) wherein X has above indicated values and L means Cl, Br, OH, SCH3 or reaction esterified OH-group with compound of the formula (III) wherein R1 and R2 have above indicated values followed by if necessary conversion of one residue X in the prepared compound of the formula (I) to another residue X by, for example, hydrolysis of ester group to COOH-group and/or conversion of compound of the formula (I) to one of its physiologically acceptable salts. EFFECT: improved preparing method, valuable medicinal and biochemical properties of compounds. 6 cl, 1 tbl, 14 ex

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RU 2 224 760 C2

Authors

Jonas Rokhus

Shelling P'Er

Kluksen Frants-Verner

Kristadler Marija

Dates

2004-02-27Published

1999-04-23Filed