Non-peptide gnrh antagonists

2005
OA: closed

Abstract

Compounds according to general formula 1, wherein A-Aare selected from Aand Awhere Ais either -CR- or -N- and Ais -NR-, -O- or -S-; Ais either a covalent bond or A, provided that when Ais a covalent bond one of A-Amust be Aand the other two must be Aand when Ais Athen all of A-Amust be A; Ris selected from H, NHY' and COY, in which case Ris H, or Rand R2 may both be methyl or together represent -O; R, Rand Rare each independently selected from H and lower alkyl groups; R, R, R, R, R, Rand Rare each independently selected from H, lower alkyl groups, NH2, halogens (F, CI and Br) O-alkyl, CH2NM2 and CF; Ris selected from H, F, CI Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF; Ris selected from H, methyl and ethyl; W is selected from -CH- and -N-;X is selected from CH2, O, S, SO2, NH and N lower alkyl; Yis selected from CO-lower alkyl, CO(CH2)bY, CO(CH2)bCOYand CO(CH)NHCOY, where b is 1-3; Y2 is selected from OR, NRRand NH(CH2)CCOY, where c is 1-3; Yis selected from ORand NRR; Ris selected from H, lower alkyl and (CH2)aR, where a is 0-4; Rand Rare each independently selected from H, lower alkyl and (CH2)aRor together are -(CH2)2-Z-(CH2)2-; Ris 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 fertilisation.

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europepmc
last seen: 2026-07-08T06:14:57.058073+00:00