| 摘要 |
FIELD: organic chemistry, medicine, hematology. ^ SUBSTANCE: invention relates to novel compounds or their salts that inhibit activated X factor of blood coagulation and elicit the strong anti-coagulating effect. Compounds show the following formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 wherein R1 and R2 represent oxygen atom; Q1 represents tetrahydrothienopyridyl group, tetrahydrothiazolpyridyl group, tetrahydrothiazolpyridazinyl group, dihydropyranothiazolyl group, tetrahydrooxazolopyridyl group, dihydropyrrolopyromidinyl group, pyrrolothiazolyl group, dihydropyrrolothiazolyl group, tetrahydrobenzothiazolyl group, dihydrothiazolopyrimidinyl group, 4,5,6,7-tetrahydro-5,6-tetramethylenethiazolopyridazinyl group or 5,6-trimethylene-4,5,6,7-tetrahydrothiazolopyridazinyl group wherein each group can comprise from 1 to 3 substitutes chosen from amino group, (C1-C6)-alkyl groups, di-(C1-C6-alkyl)amino groups; Q2 represents a simple bond; Q3 represents group of the formula: wherein Q5 means alkylene group comprising 1-8 carbon atoms, or group -(CH2)m-CH2-A-CH2-(CH2)n- wherein m and n = 0 independently of one another; A means nitrogen atom; R3 and R4 represent substitutes at carbon ring atom(S) wherein ring comprises Q5 and represent independently of one another hydrogen atom, N,N-dialkylcarbamoyl group or alkoxycarbonylalkyl group; Q4 represents aryl group chosen from phenyl group that can be substituted, heteroaryl group comprising at least one heteroatom chosen from sulfur and nitrogen atoms that can be substituted wherein substitute(s) in Q4 group are represented by 1-3 substituted chosen from hydroxyl group, halogen atoms, halogenalkyl groups, amino group, nitro group, linear or branched alkyl groups comprising 1-6 carbon atoms, linear or branched alkoxy groups comprising 1-6 carbon atoms, linear or branched hydroxyalkyl groups comprising 1-6 carbon atoms, linear or branched alkynyl groups comprising 2-6 carbon atoms, linear or branched N,N-di-(C1-C6-alkyl)-carbamoyl groups, (C1-C6)-alkylamino groups; T0 represents carbonyl group; T1 represents group -C(=O)-C(=O)-N(R')-, group -C(=S)-C(=O)-N(R')-, group -C(=O)-C(=S)-N(R')- wherein R' means hydrogen atom, alkyl group; group -C(=O)-A1-N(R'')- wherein A1 means alkylene group comprising 1-5 carbon atoms that can be substituted; R'' means hydrogen atom, group -C(=O)-NH-, group -C(=O)-NH-NH-, group -C(=O)-A2-C(=O)- wherein A2 means alkylene group comprising 1-5 carbon atoms, group -C(=O)-A3-C(=O)-NH- wherein A3 means alkylene group comprising 1-5 carbon atoms, group -C(=O)-C(=NORa)-N(Rb)- wherein Ra means hydrogen atom, and Rb means hydrogen atom, group -C(=O)-N=N-, or its salt. Also, invention relates to a drug, inhibitor of activated X factor of blood coagulation, anti-coagulant agent, medicinal composition containing indicated compounds, and to their using for preparing a drug, inhibitor and anti-coagulant agent. ^ EFFECT: valuable medicinal properties of compounds and agents. ^ 24 cl, 1 tbl, 748 ex |
