SERINE PROTEASE INHIBITOR AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a new serine protease inhibitor of the formula (I):

wherein J means R¹, R¹-SO₂-, R³-OOC-(CHR²)_p- or (R^2aR^2b)-N-CO-(CH²)_p-; D means amino acid of the formula: -NH-CHR¹-C(O)- or -NR⁴-CH[(CH₂)_qC(O)OR¹]-C(O)-; E represents -NR²-CH₂- or fragment of the formula:

R¹ is taken among (1-12C)-alkyl, (3-12C)-cycloalkyl and (3-12C)-cycloalkyl-(1-6C)-alkylene wherein their groups are optionally substituted with (3-12C)-cycloalkyl and among (14-20C)-(bisaryl)-alkyl; each among R², R^2a and R^2b is taken independently among hydrogen atom, (1-8C)-alkyl, (3-8C)-cycloalkyl and (6-14C)-aryl; R³ has the same values that are determined for R²; R⁴ represents hydrogen atom; X and Y represent CH; m = 1 or 2; p = 1, 2 or 3; q = 1, 2 or 3; t = 2, 3 or 4; or to its N-alkoxycarbonyl-substituted derivative; and/or to its pharmaceutically acceptable additive salt and/or solvate. Invention relates also to a pharmaceutical composition eliciting thrombin-inhibitory activity. Invention provides preparing new compounds and medicinal agents based on thereof used for treatment or prophylaxis of thrombin-mediated and thrombin-associated diseases.

EFFECT: valuable medicinal and biochemical properties of inhibitor.

8 cl, 3 tbl, 15 ex