Novel LHRH-antagonists, production and use thereof as medicament for hormone-dependant tumors, endometriosis, beign prostate hyperplasia and fertility disorders
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Abstract
A compound of general formula I A-Xxx1- Xxx2- Xxx3- Xxx4- Xxx5- Xxx6- Xxx7- Xxx8- Xxx9- Xxx10- NH2 is describd wherein: A is an acetyl group Xxx1 is D-Nal(2), Xxx2 is D-Cpa, Xxx3 is D-Pal(3), Xxx4 is Ser, Xxx5 is N-Me-Tyr, Xxx6 is D-Cit or D[e-N'-4-(4-amidinophenyl)-amino-1,4-dioxobutyl]Lys (D-Lys(B), Xxx7 is Leu or Nle, Xxx8 is Arg or Lys(iPr), Xxx9 is Pro and Xxx10 is D-Ala or Sar, with the proviso that if Xxx6 is D-Lys(B), then Xxx7 is Nle and Xxx10 is D-Ala. The pharmaceutical compositions comprising the compounds are useful for the treatment of hormone-dependant tumors or for non-malignant indication whose treatment necessitates LH-RH hormone suppression, such as endometriosis and benign prostate hyperplasia, and for the treatment of male or female fertility disorders.
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- last seen: 2026-07-08T06:14:57.058073+00:00