PROSTAGLANDIN ANALOGS, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION POSSESSING SELECTIVE AGONISTIC ACTIVITY WITH RESPECT TO EP-RECEPTOR Russian patent published in 2006 - IPC C07D207/27 C07D403/06 C07D405/06 A61K31/4015 A61P19/08 

Abstract RU 2288913 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to analogs of prostaglandin of the formula (I): , wherein A means -CH2-CH2- or -CH=CH-; B is absent or means phenyl; Z means -C(O)OR' or tetrazole-5-yl wherein R' means hydrogen atom or (C1-C6)-alkyl; m = 1, 2, 3, 4, 5 or 6; R1 means (C1-C6)-alkyl, unsubstituted phenyl or phenyl substituted with at least one substitute chosen from the group comprising trifluoromethyl, halogen atom, -Y-Ra, -Y-ORa and -Y-C(O)Ra wherein Y means chemical bond or (C1-C3)-alkylene group; Ra means (C1-C6)-alkyl, unsubstituted phenyl or phenyl substituted with at least one substitute chosen from the group comprising (C1-C6)-alkyl, (C1-C6)-alkoxy-group, trifluoromethyl and halogen atom under condition that B means phenyl and R3, R4, R5 and R6 do not mean hydrogen atom simultaneously; or R1 means unsubstituted phenyl or phenyl substituted with at least one substitute chosen from the group comprising trifluoromethyl, -Y-Ra, -Y-ORa and -Y-C(O)Ra wherein Y means chemical bond or (C1-C)-alkylene group; Ra means (C1-C6)-alkyl, unsubstituted phenyl or phenyl substituted with at least one substitute chosen from the group comprising (C1-C6)-alkyl, (C1-C6)-alkoxy-group, trifluoromethyl and halogen atom under condition that B is absent and R3, R4, R5 and R6 means hydrogen atom simultaneously; R2 means hydrogen atom; each among R3, R4, R5 and R6 means independently of one another hydrogen atom or (C1-C6)-alkyl, or its pharmaceutically acceptable salt or individual isomer. Compounds of the formula (1) possess a selective agonistic activity with respect to ER4-receptors and therefore they can be used in pharmaceutical composition.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds and pharmaceutical composition.

22 cl, 2 tbl, 12 ex

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RU 2 288 913 C2

Authors

Ehluorti Todd Richard

Mirzadegan Taranekh

Ropel Majkl Garret

Smit Dejvid Bernard

Uolker Kejt Adrian Mjurrej

Dates

2006-12-10Published

2002-07-08Filed