FIELD: organic chemistry, heterocyclic compounds, biochemistry. SUBSTANCE: invention describes novel five-membered heterocyclic amidines of the formula (I) where A, B, D and E have the following values: A of the formula (II)
where m = n = 0, 1 or 2; R1 means groups: hydroxyl, carboxyl, C1-6-alkyl-OOC; R2 = R3 mean hydrogen atom, alkyl with 1-4 carbon atoms; B of the formula (III)
where R4 means hydrogen atom, alkyl with 1-4 carbon atoms or R1 - means (CH)m - (in this case R1 and m have the above indicated values); p = 0 or 1; R5 - means hydrogen atom or alkyl with 1-4 carbon atoms; R6 means hydrogen atom, alkyl with 1-6 carbon atoms, cycloalkyl with 3-8 carbon atoms; R4 and R6 in common can mean ethylene group; R7 means hydrogen atom, alkyl with 1-8 carbon atoms; R8 means hydrogen atom, alkyl with 1-4 carbon atoms; E of the formula (IV)
where q = 0 or 1; D of the formulas
,
,
where R9 means hydrogen atom, alkyl with 1-3 carbon atoms; R10 = R11 mean hydrogen atom, alkyl with 1-4 carbon atoms; X means oxygen, sulfur atom, NR12 (R12 is hydrogen atom, alkyl with 1-6 carbon atoms); Y means nitrogen or -CR13 R13 is hydrogen atom, alkyl with 1-4 carbon atoms; Z means nitrogen or -CR13= where R13 has the above indicated value and also their salts with physiologically tolerated acids. Said compounds elicite properties of inhibitors of thrombin. Invention describes also compounds containing derivatives of five-membered heterocyclic amidine as a component of inhibitors of serine proteases and intermediate compounds. EFFECT: valuable medicinal, biochemical and pharmacological properties. 4 cl, 1 tbl, 29 ex
Title | Year | Author | Number |
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SERINE PROTEASE INHIBITORS | 1997 |
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DERIVATIVES OF AMIDINES, COMPOUNDS, PHARMACEUTICAL COMPOSITION | 1999 |
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Authors
Dates
2001-10-27—Published
1997-07-29—Filed