FIELD: chemistry.
SUBSTANCE: invention concerns compounds of the formula (1) as inhibitor of activated fibrillation factor FXa and anticoagulant, and their pharmaceutically acceptable salts, medication based on them, as well as new intermediary compounds for obtaining the claimed compounds. The compounds can be applied to treat and prevent diseases caused by activated fibrillation factor FXa, such as infarction, embolism, deep vein thrombosis, etc. In the formula (1) Q1-Q2-T°-N(R1)-Q3-N(R2)-T1-Q4(1) R1 and R2 is hydrogen atom; Q1 is non-saturated 10-membered bicyclic condensed hydrocarbon group, which can be substituted for halogen, or non-saturated 8-10-membered bicyclic 12-13-membered tricyclic group with 1-4 heteroatoms selected out of N, S or O, which can be substituted for C1-C6alkyl, halogen, C2-C6alkinyl, hydroxy-C1-C6alkyl, pyridine, N,N-di(C1-C6alkyl)amine, (C1-C6alkyl)oxycarbonyl group, C1-C6alkoxy-C1-C6alkyl, C1-C6alkoxycarbonyl-C1-C6alkyl, amino-C1-C6alkyl, C1-C6alkylamino-C1-C6alkyl, C1-C6alkylsulfonylamino-C1-C6alkyl, C1-C6alkoxycarbonylamino-C1-C6alkyl, C1-C6alkanoylamino-C1-C6alkyl, C1-C6alkylsulfonyl; Q2 is a direct link; Q3 is 
, where Q5 is an alkylene group containing 1-8 carbon atoms, and both R3 and R4 independently represent a hydrogen atom or 5-membered heterocyclic group including 1-3 heteroatoms selected out of N, S or O, which can be substituted for oxo group, C1-C6alkyl, trifluoromethyl; Q4 is a phenyl group which can be substituted for C1-C6alkyl, pyridine, halogen, trifluoromethyl, hydroxy-C1-C6alkyl, C1-C6alkoxy, C2-C6alkinyl, amino, nitro, cyano, amidino group, hydroxyamidino group, N,N-di(C1-C6alkyl)carbomoyl group, phenyl-C2-C6alkenyl group, which can be substituted for halogen, 5-6-membered heteroaryl group with 1-2 heteroatoms selected out of N or S, which can be substituted for halogen or C1-C6alkyl, 9-membered heteroaryl-C2-C6alkenyl group with 1 heteroatom selected out of N or S, which can be substituted for halogen, saturated or non-saturated 10-membered bicyclic condensed hydrocarbon group, which can be substituted for halogen, or saturated or non-saturated 9-membered bicyclic condensed heterocyclic group with 1-4 heteroatoms selected out of N, S or O, which can be substituted for C1-C6alkyl, halogen, C2-C6alkinyl, hydroxy-C1-C6alkyl, pyridine, N,N-di(C1-C6alkyl) amine, (C1-C6alkyloxycarbonyl group; T0 is a carbonyl group; and T1 is a carbonyl group, -C(=O)-C(=O)-N(R')- group, -C(=S)-C(=O)-N(R')- group or -C(=O)-C(=S)-N(R')- group (where R' is hydrogen atom, C1-C6alkyl group or C1-C6alkoxy group).
EFFECT: obtaining pharmaceutical composition based on diamine derivatives for treatment and prevention of diseases caused by activated fibrillation factor FXa.
15 cl, 1 tbl, 419 ex
| Title | Year | Author | Number |
|---|---|---|---|
| DERIVATIVES OF DIAMINES | 2002 |
|
RU2319699C2 |
| DIAMINE DERIVATIVES | 2002 |
|
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| ETHYLENEDIAMINE DERIVATIVES AND FXa INHIBITOR AND ANTICOAGULANT COMPRISING THEREOF | 2001 |
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| NEW HYDROXAMIC ACID DERIVATIVE | 2011 |
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