Analogs of gonadoliberin with improved solubility, methods for their preparation, agents containing them and their use

US5091367A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Wolfgang Konig · Hofheim, DE
• Jurgen K. Sandow · Königstein, DE
• Cenek Kolar · Marburg, DE

Key dates

• Filing date: Jun 28, 1991
• Grant date: Feb 25, 1992
• Expiry date: Jun 28, 2011

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to peptides of the formula ##STR1## 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 substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R.sup.1), .beta.-Asn, .beta.-Asp-OMe, D-Thi or --NH--CH(CH.sub.2 R.sup.2)--CO--; F is Ser(R.sup.1), Leu, Trp or Phe; G is Gly-NH.sub.2, Aza-Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-alkyl; R.sup.1 is glycosyl and R.sup.2 is hydrogen, acyl, aryl or heteroaryl. The invention also relates to methods for the preparation of these peptides, agents containing them and their use.