C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
530/7.06
C07K 7/56 (2006.01) C07K 7/16 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1216843
CANADIAN PATENT APPLICATION OF PER OLOF RAGNAR MELIN AND JERZY ANDRZEJ TROJNAR FOR VASOTOCIN DERIVATIVES Abstract of the Disclosure Novel vasotocin derivatives having an inhibitory effect on uterine contractions, pharmaceutical compositions con- taining these derivatives, and the use thereof in the thera- peutical treatment of excessive muscle contractions in the uterus are described. The derivatives differ from vasotocin in that the structure of the original hormone has been modified at positions 1, 2 and, optionally, 4 and/or 8. The vasotocin derivatives thus have the formula Image wherein Mpa is a 3-mercaptopropionoyl residue (-S-CH2- CH2-CO-); A is the peptide residue of L- or D-tyrosine-O-ethyl ether (in other words, 4-ethoxy-L or D-phenyl alanine, i.e. L- or D-Tyr(Et)), or of a hydrophobic D-amino acid, such as D-tyrosine(D-Tyr) or D-tryptophane(D-Trp); 1a Ile is the peptide residue of isoleucine; B is the peptide residue of glutamine (Gln), threonine (Thr) or valine (Val); Asn is the peptide residue of asparagine; Cys is the peptide residue of cysteine; Pro is the peptide residue of proline; C is the peptide residue of L- or D-arginine (Arg), ornithine (Orn) or citrulline (Cit); and Gly-NH2 is the peptide residue of glycine amide. 1b
443490
Melin Per O.r.
Trojnar Jerzy A.
Ferring Ab
Gowling Lafleur Henderson Llp
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