INHIBITORS OF SERINE PROTEASES Russian patent published in 2002 - IPC

FIELD: organic chemistry, biochemistry. SUBSTANCE: invention relates to a group of the novel compounds of the general formula 1: R¹-SO₂-B-X-Z-C(O)-Y where R¹ means (1-12C)-alkyl that can be optionally substituted with CF₃, (7-15C)-aralkyl or camphoryl; B means a bond, amino acid of the formula NH-CH[(CH₂)_pC(O)OH]-C(O)- where p = 1, 2 or 3, D-3-Tiq or L- or D-amino acid comprising a hydrophobic or neutral side-chain; X means amino acid with hydrophobic side-chain, glutamine, cyclic amino acid, -NR²-CH₂-C(O)- or the group: or where n = 2, 3 or 4; W means CH; R³ means H, (1-6C)-alkyl; Z means lysine or 4-aminocyclohexyl-glycine; Y means NH-(1-6C)- alkylene-C₆H₅, -OR⁴ where R⁴ means H, (2-6C)-alkyl or NR⁵R⁶; R⁵ and R⁶ mean independently H, (1-6C)- alkoxy- -group or (1-6C)-alkyl optionally substituted with halogen atom; or R⁵ and R⁶ in common mean (3-6C)-alkylene; or R⁵ and R⁶ in common with nitrogen atom to which they are bound mean where V means O, S or SO₂; or its prodrug or a pharmaceutically acceptable salt under condition that compounds: naphthyl-SO₂-Asp-Pro-Lysψ-[COCO] -OH, benzyl-SO₂-norLeu(cyclo)Gly-Lysψ-[COCO] -OH and ethyl-SO₂-D-Phe-Pro-Lysψ-[COCO]-OH showing an anticoagulating activity are excluded; and to a pharmaceutical composition showing thrombin-inhibiting activity. EFFECT: new compounds indicated above, valuable pharmacological properties. 10 cl, 4 tbl, 45 ex _