Analogs of gonadoliberin with improved solubility, methods...

C - Chemistry – Metallurgy – 07 – K

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530/9, 530/7.2,

C07K 9/00 (2006.01) C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1314656

HOE 86/F 253 Abstract of the disclosure: Analogs of gonadoliberin with improved solubility, methods for their preparation, agents containing them and their use The invention relates to peptides of the formula Image in which X is absent or is hydrogen or acyl; A is Pgl, de- hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally sub- stituted D-Nal(2), D-Phe or D-Trp; .beta. is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg or His; E is D-Ser(R1), .beta.- Asn, .beta.-Asp-OMe, D-Thi or -NH-CH(CH2R2)-CO-; F is Ser(R1), Leu, Trp or Phe; G is Gly-NH2, Aza-Gly-NH2, D-Ala-NH2 or NH- alkyl; R1 is glycosyl and R2 is hydrogen, acyl, aryl or het- eroaryl. The invention also relates to methods for the preparation of these peptides, agents containing them and their use.

548918

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