TRIPHENYLALKENE DERIVATIVES AND THEIR USE AS SELECTIVE ESTROGEN RECEPTOR MODULATORS Russian patent published in 2005 - IPC

FIELD: organic synthesis.

SUBSTANCE: invention provides compounds of general formula I:

in which R1 represents H, halogen, OCH₃, or OH; R2 represents (a) -X-(CH₂)_n-CH₂-N(R4)R5, where (i) X represents NH or S; n is integer from 1 to 4; R4 and R5, the same or different, represent C₁-C₄-alkyl, H, -CH₂C≡CH, or -CH₂CH₂OH; or R4 and R5, together, form nitrogen-containing five- or six-membered cycle or heteroaromatic cycle; or where (ii) X represents O; n is integer from 1 to 4; one of R4 and R5 is CH₂C≡CH, or -CH₂CH₂OH and the other H or C₁-C₄-alkyl; or R4 and R5, together, form imidazole cycle or nitrogen-containing six-membered cycle or heteroaromatic cycle; or R2 represents (b) -Y-(CH₂)_nCH₂-O-R5, where (i) Y represents O; n is integer from 1 to 4; and R6 represents -CH₂CH₂OH or -CH₂CH₂Cl; or where (ii) Y represents NH or S; n is integer from 1 to 4; and R6 represents H, -CH₂CH₂OH, or -CH₂CH₂Cl; or R2 represents (c) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, or 2,2-diethyl-2-hydroxy-ethoxy; R3 represents H. halogen, OH, or -OCH₃. Claimed compounds are novel selective estrogen receptor modulators. Invention also discloses pharmaceutical composition and a method for production of tissue-specific estrogenic and/or antiestrogenic effect in patient, for whom indicated effect is required.

EFFECT: increased choice of estrogen receptor modulators.

19 cl, 7 tbl, 11 ex