Irreversible peptide ligands for bombesin receptors, their use, and process for making the same

US5100873A · kind A · utility

Assignee

• Farmitalia Carlo Erba S.p.A. · IT

Inventors

• Roberto de Castiglione · Milano, IT
• Mauro Galantino · Milano, IT
• Fabio Corradi · Milano, IT
• Luigia Gozzini · Milano, IT
• Marina Ciomei · Corsico, IT
• Isabella Molinari · Milano, IT

Key dates

• Filing date: Jul 17, 1989
• Grant date: Mar 31, 1992
• Expiry date: Jul 17, 2009

Classification

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

Abstract

A peptide of formula (I): EQU A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (I) wherein either: PA0 (i) A represents a hydrogen atom, a Boc group or an acetyl group, one of B and C represents a pMel or mMel residue, and the other of B and C represents a sigma bond or a Gly, Leu-Gly, E-Leu-Gly or Gln-E-Leu-Gly, E, or E-Gly residue with E=Arg(A), arg(A), Lys(A), lys(A), Orn(A) and orn(A); or PA0 (ii) A represents a hydrogen atom; PA0 B represents a Glp-Arg-Leu-Gly residue; PA0 C represents a pMel or mMel residue; PA0 D represents a sigma bond or an Asn or Thr residue; PA0 X represents a Gly or ala residue; PA0 Y represents a sigma bond or a His(R.sub.1); PA0 his(R.sub.1), Phe, phe, Ser, ser, Ala or ala residue, PA0 T represents a sigma bond or a Leu, leu, Phe or phe residue; PA0 W represents an OH, amino, pentylamino or phenethyl-amino group or a Met-R.sub.2, Leu-R.sub.2, Ile-R.sub.2 or Nle-R.sub.2 residue; PA0 R.sub.1 represents a hydrogen atom or a Tos, Dnp or Bzl group; and PA0 R.sub.2 represents an amino, hydroxy, methoxy or hydrazino group; and its pharmaceutically acceptable salts are disclosed.