| abstract |
FIELD: chemistry. n SUBSTANCE: invention pertains to non-peptide antagonists GnRH, with general formula 1 , where each of A 1 , A 2 and A 3 are independently chosen from A 5 and A 6 ; and A 4 represents either a covalent bond, or A 5 ; under the condition that, if A 4 is a covalent bond, then one of A 1 -A 3 represent A 6 , and the other two represent A 5 , and that, if A 4 represents A 5 , then all of A 1 -A 3 represent A 5 ; A 5 is chosen from C-R 13 and N; A 6 is chosen from N-R 14 , S and O; R 1 is chosen from H, NHY 1 and COY 2 , and R 2 represents H; or and R 1 , and R 2 represents methyl or together represent =O; each of R 3 , R 4 and R 5 independently represents H or low alkyl; each of R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are independently chosen from H, NH 2 , F, CI, Br, O-alkyl and CH 2 NMe 2 ; R 13 is chosen from H, F, CI, Br, NO 2 , NH 2 , OH, Me, Et, OMe and NMe 2 ; R 14 is chosen from H, methyl and ethyl; W is chosen from CH and N; X is chosen from CH 2 , O and NH; Y 1 is chosen from CO-low alkyl, CO(CH 2 ) b Y 3 , CO(CH 2 ) b COY 3 and CO(CH 2 ) b NHCOY 3 ; Y 2 is chosen from OR 15 , NR I6 R 17 and NH(CH 2 ) c COY 3 ; Y 3 is chosen from alkyl, OR 15 and NR 16 R 17 ; R 15 represents H; each of R 16 and R 17 is independently chosen from H, low alkyl and (CH 2 ) a R 18 , or together represent -(CH 2 ) 2 -Z-(CH 2 ) 2 -; R 18 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. n EFFECT: obtaining new compounds, with useful biological properties. n 27 cl, 70 ex |