GB1524747A — Polypeptide

USPTO Abstract

1524747 Polypeptides IMPERIAL CHEMICAL INDUSTRIES Ltd 21 April 1977 [11 May 1976] 19327/76 Heading C3H [Also in Division C2] A polypeptide of the Formula (I) H-Pyroglu- His - Trp - Ser - Tyr - A - B - Arg - Pro - E - F wherein (i) A is D-Tyr, D-Tyr(Me), D-Ser,(But), D-Phe, D-Ala or D-Trp; B is Leu or MeLeu; E is Azgly; F is NH2; (ii) A is Azgly or Azala; B is Leu; E is a direct bond; F is NHEt; and the pharmaceutically-acceptable and veterinarily-acceptable acid addition salts thereof. Peptides (I) prepared are Peptide intermediates isolated are: DECAPEPTIDE: H - Pyroglu - His - Trp - Ser- Tyr(But) - D - Phe - MeLeu - Arg(H<+>) - Pro- Azgly-NH2. OCTAPEPTIDES: Z and H - Trp Ser - Tyr- D - Ala - Leu- Arg(H<+>) - Pro - Azgly - NH2. HEPTAPEPTIDES: Z and H - Trp - Ser- Tyr(Bzl) - Azgly - Leu - Arg(H<+>) Pro - NHEt; Z and H - Trp - Ser - Tyr(Bzl) Azala - Leu- Arg(H<+>) - Pro - NHEt. HEXAPEPTIDES: Z - Tyr(Bzl) D - Ala - Leu- Arg(N02) - Pro - Azgly NH2; H - Tyr D - Ala- Leu - Arg(H<+>) - Pro - Azgly - NH2; Z - Tyr(Bzl)- D Phe - Leu - Arg(NO2) - Pro - Azgly NH2; H Tyr D Phe - Leu - Arg(H<+>) - Pro Azgly- NH2; Z - Tyr(Bzl) D - Trp - Leu - Arg(NO2)- Pro - Azgly - NH2- H - Tyr - D - Trp - Leu- Arg(H<+>) - Pro - Azgly - NH2; Z - Tyr(Bzl) - DTyr(Me) - Leu - Arg(NO2) - Pro - Azgly - NH2; H - Tyr - D - Tyr(Me) Leu - Arg(H<+>) Pro- Azgly - NH2; Z - Tyr(Bzl) D - Ser(But) - Leu- Arg(N02) - Pro - Azgly - NH2; H - Tyr - DSer(But) Leu - Arg(H<+>) - Pro - Azgly - NH2; Z - Tyr(Bzl) - D - Tyr(Me) - MeLeu - Arg(NO2)- Pro - Azgly - NH2; H Tyr - D - Tyr(Me)- MeLeu - Arg(H+) - Pro Azgly - NH2; Z - Tyr(But) - D - Phe - MeLeu - Arg(NO2) - Pro- Azgly - NH2; H - Tyr(But) D - Phe - MeLeu- Arg(H<+>) - Pro - Azgly - NH2. PENTAPEPTIDES: Z - Tyr(Bzl) - Azgly - Leu- Arg(NO2) - Pro - NHEt; H - Tyr(Bzl) - Azgly- Leu - Arg(H<+>) - Pro - NHEt; Z - Tyr(Bzl)- Azala - Leu - Arg(NO2) - Pro - NHEt; H - Tyr- (Bzl) - Azala Leu - Arg(H<+>) - Pro - NHEt. TETRAPEPTIDES: Z - Leu - Arg(NO2) - Pro- Azgly - NH2; H - Leu - Arg(H<+>) Pro - Azgly- NH2; H - Pyroglu His - Trp - Ser - OMe, NHNH2 and N3. TRIPEPTIDES: Z - Tyr(Bzl) Azgly - Leu- OMe, NHNH2 and N3; Z - Tyr(Bzl) - Azala- Leu OMe and OH; Z - Tyr(Bzl) - D - Phe- Leu - OMe, NHNH2 and N3 ; Boc and HArg(NO2) - Pro Azgly - NH2; Z - Tyr(Bzl)- D - Trp - Leu - OMe,NHNH2 and N3; ZTyr(Bzl)-D-Tyr(Me) -Leu-OMe, NHNH2 and N3; Z-Tyr(Bzl) - D - Ser(But) - Leu - OMe, NHNH2 and N3; Z - Tyr(Bzl) D - Tyr(Me) - MeLeu- OMe, NHNH2 and N3; Z - Tyr(But) - D - Phe - MeLeu - OMe, NHNH2 and N3. DIPEPTIDES: Boc and H - Arg(NO2) Pro- NHEt; H - Pyroglu His - OMe, NHNH2 and N3; Z and H - Pro - Azgly - NH2; Z - Leu- Arg(NO2) - OH; Z - Tyr(Bzl) - D - Ala - OMe, NHNH2 and N3 ; Z and H - D - Phe - Leu - OMe; H - Trp-Ser - OMe; Z and H - D - Tyr(Me)- Leu- OMe; Z and H - D - Trp - Leu - OMe ; Z and H - D - Ser(But) - Leu - OMe; Z and H - DTyr - MeLeu - OMe; Z and H D - Phe - MeLeu- OMe. A pharmaceutical composition or veterinary composition, which may be administered parenterally or orally, comprises peptide (I) in association with a pharmaceutically-acceptable or veterinarily acceptable diluent or carrier.