| abstract |
Compounds of the invention according to formula (1) are novel:n n n [Formula 1]n n n n n n n n Wherein A 1 to A 3 are each selected from A 5 and A 6 , A 5 is = CR 13 -or = N-, and A 6 is -NR 14- , -O-, or S; A 4 is a covalent bond or A 5 ; When A 4 is a covalent bond, one of A 1 to A 3 must be A 6 , the other two must be A 5 , and when A 4 is A 5 , all A 1 to A 3 must be A 5 ; R 1 is selected from a hydrogen atom, NHY ′ and COY 2 , wherein R 2 is H; Alternatively, R 1 and R 2 are both methyl groups or both together represent = O; R 3 , R 4 and R 5 are each independently selected from H, lower alkyl groups; R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 are each independently H, lower alkyl group, NH 2 , halogen (F, Cl and Br), O-alkyl, CH 2 NMe 2 and Is selected from CF 2 ; R 13 is selected from H, F, Cl, Br, NO 2 , NH 2 , OH, Me, Et, OMe, NMe 2 and CF 2 ; R 14 is selected from H, methyl and ethyl; W is selected from = CH- and = N-; X is selected from CH 2 , O, S, SO 2 , NH and N-lower alkyl; Y 1 is selected from CO-lower alkyl, CO (CH 2 ) b Y 3 , CO (CH 2 ) b COY 3 and CO (CH 2 ) b NHCOY 3 , wherein b is 1 to 3; Y 2 is selected from OR 15 , NR 16 R 17 and NH (CH 2 ) c COY 3 , wherein c is 1 to 3; Y 3 is selected from OR 15 and NR 16 R 17 ; R 15 is selected from hydrogen, lower alkyl and (CH 2 ) a R 16 , wherein a is 0 to 4; R 16 and R 17 are each independently selected from H, lower alkyl, (CH 2 ) a R 18 , or together are (CH 2 ) 2 -Z- (CH 2 ) 2 ; R 18 is OH, phenyl or pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrole, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxa Aromatic heterocycles selected from diazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; Z is selected from O, CH 2 , S, SO 2 , NH and N-loweralkyl. The compounds are useful for the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, pregnancy control and in vitro fertilization. |