FLUORINATED DERIVATIVES OF 4-AZASTEROID AS ANDROGEN RECEPTOR MODULATORS Russian patent published in 2008 - IPC C07J73/00 A61K31/473 A61K31/56 A61P5/26 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention describes compound of the formula (I) or its pharmaceutically acceptable salt, or an enantiomer wherein n = 0 or 1; a - b means -CF=CH or -CHFCH₂; R¹ represents (C₁-C₃)-alkyl wherein alkyl is unsubstituted; R² represents hydrogen atom; R³ is chosen from (C₁-C₄)-alkyl, (CH₂)_n-cycloheteroalkyl and (CH₂)_n-aryl; or R² and R³ form in common 6-membered saturated ring condensed with 5-membered aromatic ring system comprising 2 heteroatoms chosen from nitrogen atom (N), and pharmaceutical compositions. Compounds of the formula (I) represent modulators of androgen receptors (AR) possessing tissue-selective effect. Proposed compounds are useful as androgen receptors agonists in osseous and/or muscle tissue in antagonizing AR in male patient prostate or in female patient uterus.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

36 cl, 2 tbl, 72 ex