Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,... – Reduced antigenicity – reduced ability to bind complement – or...
Patent
1980-04-29
1983-01-11
Phillips, Delbert R.
Drug, bio-affecting and body treating compositions
Immunoglobulin, antiserum, antibody, or antibody fragment,...
Reduced antigenicity, reduced ability to bind complement, or...
2601125R, A61K 3700, C07C10352
Patent
active
043681921
ABSTRACT:
Peptides having the carboxyl terminated sequence of the pancreozymin-cholstokinin 25-33 modified such that the amino acid group 25 carries a strongly basic group, the amino acid group 28 exhibits a hydrophilic character similar to that of the hydroxyamino acids and the amino acid group 31 exhibits a strongly hydrophobic character similar to that of amino acids with aliphatic side chains, and in particular nonapeptides having the sequence H--X--Asp--Tyr(SO.sub.3 H)--Y--Gly--Trp--Z--Asp--Phe--NN.sub.2 wherein X is arginine, homoarginine, norarginine, N.sub..epsilon.,N.sub..epsilon. -dialkyllysine, N.sub..delta. or N.sub..delta. -dialkyl-ornithine, Y is threonine, serine or hydroxy-proline and Z is norleucine, leucine, norvaline or .alpha.-amino-butyric acid, possess pronounced pancreozymin activity and can be employed in pharmaceutical preparations for controlling the function of the gall bladder and for controlling the enzyme secretion of the pancreas. Tyrosine-O-sulfate-barium salt and its N-acyl derivatives can be used as intermediate products for the preparation of peptides. For introducing the amino acid group 27 an N-acyl-tyrosine is reacted with an excess of pyridine-SO.sub.3 in a polar organic solvent, the resulting solution is extracted with water, the barium salt of the N-acyl-tyrosine-O-sulfate is precipitated from the aqueous phase by addition of a soluble barium compound, possibly the acyl group is split off in conventional manner, and the resulting tyrosine-O-sulfate-barium salt or its acyl derivative are processed employing the usual methods of peptide synthesis.
REFERENCES:
patent: 3579494 (1971-05-01), Ondetti et al.
patent: 3839315 (1974-10-01), Ondetti et al.
patent: 3892726 (1975-07-01), Ondetti et al.
patent: 3937819 (1976-02-01), Ondetti et al.
Max-Planck-Gesellschaft zur Forderung der Wissenschaften e.v.
Phillips Delbert R.
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