DERIVATIVES OF DECAPEPTIDES AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF

FIELD: chemistry of peptides. SUBSTANCE: invention relates to decapeptides of the formula (I): X-X1-X2-X3-Ser-Tyr--X6=-Leu--X8-Pro-X10 where X - acyl; X1 is D-Nal; X2 is D-Cpa; X3 is D-Pal; X6 is D-Cit, D-Hei, D-Orn, D-Lys, D-Neu; X8 is Orn, Arg, Lys, L-Neu; X10 is D-Ala-NH2; Neu is a residue of the...

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Bibliographische Detailangaben
Hauptverfasser:	ALESSANDRO LOBBIA, JOKHANN MUL'TSER, URSULA KHABENIKHT, TOMAS BRUMBI, PAUL' TAMM, FRIDTIOF SHREDER
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Beschreibung
Zusammenfassung:	FIELD: chemistry of peptides. SUBSTANCE: invention relates to decapeptides of the formula (I): X-X1-X2-X3-Ser-Tyr--X6=-Leu--X8-Pro-X10 where X - acyl; X1 is D-Nal; X2 is D-Cpa; X3 is D-Pal; X6 is D-Cit, D-Hei, D-Orn, D-Lys, D-Neu; X8 is Orn, Arg, Lys, L-Neu; X10 is D-Ala-NH2; Neu is a residue of the formula (IX) or (IV) ; Z - a group -O- or -S-; n = 1-6. Pharmaceutical composition shows LHRH-antagonistic activity. Synthesized compounds of the formula (I) show very high pharmacological activity in combination with low level of histamine release. EFFECT: enhanced activity, low adverse effect. 6 cl, 22 exN