Cyclopeptide derivatives usable as selective inhibitors with res

Details Cyclopeptide derivatives usable as selective inhibitors with res Cyclopeptide derivatives usable as selective inhibitors with res

1990-06-01

1992-08-11

Cashion, Jr., Merrell C.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

C07K 512, A61K 3700

Patent

active

051380358

ABSTRACT:
The invention relates to cyclopeptide derivative usable as protease inhibitors and complying with formula: ##STR1## in which R.sup.1 is a halogen atom, e.g. bromine or a radical such as S.sup.+ R.sub.2.sup.4 X.sub.1/v.sup.v-, R.sup.2 is a hydrogen atom, an alkyl radical, a halogen atom or other groups, R.sup.3 is NH, O or S, Z comprises a peptide sequence Z.sup.1 and a group such that CO has one end connected to the aromatic nucleus and CO-AA is a radical derived fropm an amino acid having a specificity with respect to the protease to be inhibited.

REFERENCES:
Wakselmann et al., Chemical Abstracts, vol. 113, 1990 p. 721, Abst. No. 132827m.
Connert et al., Chem. Abst. vol. 114, 1990, Abst. No. 77553n.
Mor et al., Thrombosis Research, supplement VIII, 1988. pp. 35-44.
Chemical Abstracts, vol. 111, No. 11 Sep. 11, 1989, J. P. Mazaleyrat et al: "Directed enzymic hydrolysis of cyclopeptides containing an aminobenzoic acid residue", p. 319.
Chemical Abstract, vol. 109, No. 3, Jul. 18, 1988, J. P. Mazaleyrate et al.: "Synthesis and enzymic hydrolysis of cyclic peptides containing an anthranilic acid residue", p. 662.
Chemical Abstracts, vol. 109, No. 17, Oct. 24, 1988, M. Reboud-Ravaux et al: "Structural factors in the enzymic hydrolysis of cyclopeptides containing an o-or m-aminobenzoic acid residue", p. 320.
Chemical Abstracts, vol. 110, No. 5, Jan. 30, 1989, A. Mor et al.: "Susceptibility of plasminogen activators to suicide inactivation", p. 259.

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