DERIVATIVES OF INDOLE AS INHIBITORS OF XA FACTOR

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of indole of the formula (I): wherein: two among R1a, R1b, R1c, R1d mean independently of one another H, F, J, Cl, Br, (C1-C4)-alkyl, phenyl, phenyl-(C1-C4)-alkyl, (C1-C4)- -alkoxy-grou...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: TSOLLER GERKHARD, MATTER KHANS, KLINGLER OTMAR, DEFOSSA EHLIZABET, VAL'ZER ARMIN, AL'-OBAJDI FAKHAD, KHAJNEL'T UVE, VAJLDGUZ PITER
Format: Patent
Sprache:eng ; rus
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of indole of the formula (I): wherein: two among R1a, R1b, R1c, R1d 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, -NR5aR5b, -SOn-R6c; n = 1-2 and they are similar or different and two other mean hydrogen atom; wherein all residues R5a, R5b, R5c 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 R15b 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