DERIVATIVES OF INDOLE AS INHIBITORS OF XA FACTOR Russian patent published in 2004 - IPC

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of indole of the formula (I): wherein: two among R^1a, R^1b, R^1c, R^1d mean independently of one another H, F, J, Cl, Br, (C₁-C₄)-alkyl, phenyl, phenyl-(C₁-C₄)-alkyl, (C₁-C₄)- -alkoxy-group, phenyl-(C₁-C₄)-alkoxy-group, phenyloxy-group, OH, -NR^5aR^5b, -SO_n-R^6c; n = 1-2 and they are similar or different and two other mean hydrogen atom; wherein all residues R^5a, R^5b, R^5c if they are present in molecule more one time are independent of one another and each can be similar or different; one of R² and R³ means -(CH₂)_P-CO-R⁸ and another means H, F, Cl, Br or -(CH₂)_P-CO--R⁸; p = 0, 1 or 2; R⁸ means -NR⁹R¹⁰, -OR¹⁰; A means bivalent residue -(C₁-C₄)-alkyl that is unsaturated or comprises triple linkage or -(C₁-C₄)-alkyl- CO-NH- wherein nitrogen atom is bound with R⁴; R⁴ means phenyl that is substituted with one residue R^15b or pyridyl that is unsubstituted or substituted with R¹⁴ by nitrogen atom; all their stereoisomeric forms and their mixtures taken in any ratios and their physiologically acceptable salts. Compounds of the formula (I) inhibit blood coagulant proteins and can be used in pharmaceutical composition for inhibition of Xa factor, for treatment of thrombosis, myocardial infarction, stenocardia and others. Invention describes method for preparing compounds of the formula (I). EFFECT: improved preparing method, valuable medicinal properties of compounds. 16 cl, 2 tbl, 166 ex