Physiologically active substance well capable of permeating biom

Details Physiologically active substance well capable of permeating biom Physiologically active substance well capable of permeating biom

1994-04-15

1997-07-29

Warden, Jill

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

4 to 5 amino acid residues in defined sequence

530302, 530402, 536 221, 536 284, 536 172, 536 187, 514 43, 514 49, 514 50, 548543, A61K 3800, C07K 500, C07K 700, C07H 1900

Patent

active

056523351

ABSTRACT:
A physiologically active substance well capable of permeating biomembrane according to the present invention is represented by: ##STR1## where R represents a residue of a physiologically active substance comprising a peptide, amino acid, aliphatic amine having a phenol skeleton, amino sugar, nucleoside or lactam compound and a residue of physiologically active derivative thereof. The biomembrane permeability of a substance with poor biomembrane permeability can be improved by introducing an adamantyl group to the physiologically active substance.

REFERENCES:
patent: 4128639 (1978-12-01), Lin et al.
patent: 4273704 (1981-06-01), Mazur et al.
patent: 4661512 (1987-04-01), Laruelle et al.
patent: 4851519 (1989-07-01), Lambert et al.
Tomatis, et al; Amide, 1-Adamantylamide of Leu-Enkephalin and Leu-[D ALA.sup.2 ]Enkephalin; Ed. Scient., vol. 34, pp. 496-506, Il Farmaco, 1978.
Database WPI, Week 8104, 1981, Derwent Publications Ltd., London, GB; AN 81-04915D.

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