NON-PEPTIDE GnRH ANTAGONISTS

2003
OA: closed

Abstract

Compounds according to general formula 1, wherein A - A are selected from A and A where A is either =CR- or =N- and A is -NR -,-O-or -S-; A is either a covalent bond or A, provided that when A is a covalent bond one of A - A must be A and the other two must be A and when A is A then all of A - A must be A; R is selected from H, NHY' and COY, in which case R is H, or R and R2 may both be methyl or together represent =O; R, R and R are each independently selected from H and lower alkyl groups; R, R, R, R, R, Rand R are each independently selected from H, lower alkyl groups, NH2, halogens (F, CI and Br) O-alkyl, CH2NM2 and CF; R is selected from H, F, CI Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF; R is selected from H, methyl and ethyl;; W is selected from =CH- and =N-; X is selected from CH2, O, S, SO2, NH and Nlower alkyl; Y is selected from CO-lower alkyl, CO(CH2)bY, CO(CH2)bCOY and CO(CH2)bNHCOY, where b is 1-3; Y2 is selected from OR , NR Rand NH(CH2)CCOY, where c is 1-3; Y is selected from OR and NRR; R is selected from H, lower alkyl and (CH2)aR, where a is 0-4; R and R are each independently selected from H, lower alkyl and (CH2)aR or together are -(CH2)2-Z-(CH2)2-; R is OH a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH2, S, SO2, NH and N-lower alkyl, are new.; They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisatio

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last seen: 2026-07-06T06:10:23.601157+00:00