SERINE PROTEASE INHIBITORS, PHARMACEUTICAL COMPOSITION AND THERAPEUTICAL METHODS BASED ON THE SAME

FIELD: pharmaceutical industry, medicine. ^ SUBSTANCE: invention relates to new compounds of formula ^ , ^ wherein A and B are independently CH or CR3; X is C=O or (CR4aR4b)m, (m = 1 or 2); Y is S(O)n-R2 (n = 1 or 2), S(O)n-NR2R2, or S(O)n-OR2; N1 and N2 are nitrogen atoms; Q and R1 are independentl...

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Hauptverfasser: SUTERLIN DANIEL P, ARTIS DIN R, DZHOU AJE, UIZ KENNET DZH, PASTOR RICHARD, DZHU JAN, OLIVERO ALAN G, FLAJGAR DZHON A, DAJNA MAJKL S, ALIAGAS-MARTIN IGNASIO, ROBARDZH KIRK D, GOLDSMIT RICHARD A, MANROU REDZHAJNA A, ROSON TOMAS I
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: pharmaceutical industry, medicine. ^ SUBSTANCE: invention relates to new compounds of formula ^ , ^ wherein A and B are independently CH or CR3; X is C=O or (CR4aR4b)m, (m = 1 or 2); Y is S(O)n-R2 (n = 1 or 2), S(O)n-NR2R2, or S(O)n-OR2; N1 and N2 are nitrogen atoms; Q and R1 are independently 1) optionally substituted C1-C10-alkyl; 2) optionally substituted aralkyl containing C6-C10-aryl, attached to C1-C10-alkyl; 3) optionally substituted aralkenyl containing C5-C10-aryl, attached to C1-C10-alkenyl; 4) optionally substituted C6-C10-aryl; 5) optionally substituted aryl, containing 5-10 ring atoms, selected from carbon and sulfur; each R2 and R3 are hydrogen; R4a, R4b, R5, and R6, are independently hydrogen; R2 and R3 are independently hydrogen or C1-C6-alkyl; as well as acid and base additive salts thereof. Also disclosed are method for production of claimed compounds, pharmaceutical composition inhibiting serine protease enzymes and therapeutic method based thereon. ^ EFFECT: new compounds and pharmaceutical composition for thrombosis preventing or abnormal thrombosis treatment. ^ 11 cl, 7 tbl, 15 ex