NON-PEPTIDE ANTAGONISTS GnRH Russian patent published in 2008 - IPC C07D215/08 C07D241/44 C07D401/06 C07D405/06 C07D409/06 C07D413/14 C07D417/00 C07D498/04 A61K31/47 A61P15/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention pertains to non-peptide antagonists GnRH, with general formula 1 , where each of A¹, A² and A³ are independently chosen from A⁵ and A⁶; and A⁴ represents either a covalent bond, or A⁵; under the condition that, if A⁴ is a covalent bond, then one of A¹-A³ represent A⁶, and the other two represent A⁵, and that, if A⁴ represents A⁵, then all of A¹-A³ represent A⁵; A⁵ is chosen from C-R¹³ and N; A⁶ is chosen from N-R¹⁴, S and O; R¹ is chosen from H, NHY¹ and COY², and R² represents H; or and R¹, and R² represents methyl or together represent =O; each of R³, R⁴ and R⁵ independently represents H or low alkyl; each of R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹ and R¹² are independently chosen from H, NH₂, F, CI, Br, O-alkyl and CH₂NMe₂; R¹³ is chosen from H, F, CI, Br, NO₂, NH₂, OH, Me, Et, OMe and NMe₂; R¹⁴ is chosen from H, methyl and ethyl; W is chosen from CH and N; X is chosen from CH₂, O and NH; Y¹ is chosen from CO-low alkyl, CO(CH₂)_bY³, CO(CH₂)_bCOY³ and CO(CH₂)_bNHCOY³; Y² is chosen from OR¹⁵, NR^I6R¹⁷ and NH(CH₂)_cCOY³; Y³ is chosen from alkyl, OR¹⁵ and NR¹⁶R¹⁷; R¹⁵ represents H; each of R¹⁶ and R¹⁷ is independently chosen from H, low alkyl and (CH₂)_aR¹⁸, or together represent -(CH₂)₂-Z-(CH₂)₂-; R¹⁸ is chosen from OH, pyridyl, pyrizinyl and oxadiazolyl; Z represents NH; a represents 0-4; and b and c represent 1-3. The invention also relates to use of formula 1 a compound as a therapeutic agent and pharmaceutical composition, with antagonistic effect to GnRH receptor. Description is also given of the method of obtaining compounds with the given formula.

EFFECT: obtaining new compounds, with useful biological properties.

27 cl, 70 ex