INDOLES WITH ANTIDIABETIC ACTIVITY Russian patent published in 2008 - IPC C07D209/12 C07D209/30 C07D403/12 C07D405/06 C07D413/04 A61K31/404 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to the novel indole derivatives with the common formula I: or its pharmaceutically acceptable salt, where R¹ is (a) -X-aryl-Y-Z and (b) -X-heteroaryl-Y-Z, where aryl and heteroaryl are unsubstituted or substituted with 1-3 groups, chosen independently from A; aryl means phenyl or naphthyl; heteroaryl means the monocyclic or condensed bicyclic aromatic ring structure containing one heteroatom chosen independently from N or O, where the monocyclic ring or each ring of the bicyclic ring structure means the penta- or hexamerous ring; X means the bond CH₂, CH(CH₃) and C(CH₃)₂; Y means -CH=CH-, -CH(OH)CH(OH)-, -OCR⁷R⁸-, -SCR⁷R⁸- and -CH₂CR⁵R⁶-; Z means -CO₂H, tetrazole; A means C_1-4alkyl, -OC_1-4alkyl and halogen, where alkyl, and -Oalkyl, each not necessarily substituted with 1-5 halogens; R⁵, R⁶, R⁷ and R⁸ , each independently means H, C_1-C₅alkyl, -OC_1-C₅alkyl, C_3-6cycloalkyl and phenyl, where C₁-C₅alkyl, -OC₁-C₅alkyl, C_3-6cycloalkyl and phenyl are not necessarily substituted with 1-5 halogens; and C_3-6cycloalkyl and phenyl are additionally not necessarily substituted with 1-3 groups, independently chosen from C₁-C₃alkyl and -OC₁-C₃alkyl, at that, the said C₁-C₃alkyl and -OC₁-C₃alkyl are not necessarily substituted with 1-3 halogens; or alternatively, R⁷ and R⁸ together can form the C₃-C₆cycloalkyl group; or alternatively, when R¹ means -X-phenyl-Y-Z, Y means -OCR⁷R⁸ and R⁷ are chosen from group containing H, C₁-C₅alkyl, -OC₁-C₅alkyl, then R⁸ can, not necessarily , mean the 1-2-hydrocarbon bridge, bound to the phenylic ring by the orthoposition relative to Y, and generating in this way the 5- or 6-membered heterocyclic ring, condensated with the phenylic ring; R² means C₁-C₄alkyl, which is not necessarily substituted with 1-5 halogens; R³ means (a) bensoxazolil, (d) aryl, (e) -C(=O)aryl, (f) -C(=O)heteroaryl, (g) -Oaryl, (i) -S(O)_naryl and where R³ is not necessarily substituted with 1-3 substituting groups, independently chosen from halogen, C_1-3alkyl, -OC_1-3alkyl and -SC_1-3alkyl, where C_1-3alkyl, -OC_1-3alkyl and -SC_1-3alkyl are not necessarily substituted with 1-5 halogens; each R⁴ means from H, halogen, C_1-C₅alkyl and -OC₁-C₅alkyl, where C₁-C₅alkyl and -OC₁-C₅alkyl are not necessarily substituted with 1-5 halogens; n is the even number 0-2 and p is the even number 1-3.

EFFECT: composition I reveals agonistic activity considering PPAR, that allows to use them in pharmaceutical composition, in means to fix PPAR and production of medication to fix PPAR.

33 cl, 8 tbl, 32 ex