PHENYLPYRIMIDONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, METHODS FOR PREPARING AND USING THEM

FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new phenylpyrimidone derivatives of formula I possessing the properties of a phosphodiesterase type 5 (PDE5) inhibitor. The compounds of formula I can be used for treating various vascular disorders, such as erectile dysfunction, pulmonary arterial hypertension, etc. In formulaeach Rand Rindependently means H; C-Calkyl; halogen; CF; CN; OR; NRR; NHCOR; aryl; or C-Calkyl optionally substituted by OR; Z means OR; Rmeans C-Calkyl or C-Calkyl, substituted by C-Calkoxy group; Rmeans SONRR; NRR, providing NRRis other than NH; COR; OR; or Rmeans 5-6-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of OH and C-Calkyl; or Rmeans 5- or 6-merous cyclic monosaccharide group; Rmeans C-Calkyl; C-Calkyl optionally substituted by C-Calkoxy group; each Rand Rindependently means H, OH, C-Calkyl, C-Calkoxy group, C-Calkenyl, C-Ccycloalkyl, adamantyl, C-Clactamyl, aryl, Het or (CHCHO)H, wherein j is 1-3; or each Rand Rindependently means C-Calkyl, optionally substituted by OH, C-Calkoxy group, SOH, SONRR, SO2R, NRR, aryl, Het or 5-6-merous heterocyclyl; or each Rand Rindependently means 5-6-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of C-Calkyl and C-Calkyl substituted by hydroxyl; or Rand Rtogether with a nitrogen atom attached whereto form 5-7-merous heterocyclyl optionally substituted by one or more substitutes specified in a group consisting of OH, COOR, (CHCHO)H, wherein j is 1-3, C-Calkoxy group, Het and C-Calkyl substituted by aryl; or Rand Rtogether with a nitrogen atom attached whereto form a glucosyl amino group, an amino acid residue, a residue of an amino acid ester or an amino amide residue. The other radical values are specified in the patent claim.EFFECT: invention refers to pharmaceutical compositions based on the above compounds, using them, methods for preparing the compounds, and intermediate products.18 cl, 2 tbl, 224 ex Настоящее изобретение относится к новым производным фенилпиримидона формулы I, обладающим свойствами ингибитора фосфодиэстеразы типа V (PDE5). Соединения формулы I могут использоваться для лечения различных сосудистых нарушений, таких как эректильная дисфункция, легочная артериальная гипертензия и т.п. В формуле IRи Rозначают каждый независимо H; C-Cалкил; галоген; CF; CN; OR; NRR; NHCOR; арил; или C-Cалкил, необязательно замещенный OR; Z означает OR; Rозначает