Amino acids and peptides having a modified tyrosine residue, the

Details Amino acids and peptides having a modified tyrosine residue, the Amino acids and peptides having a modified tyrosine residue, the

1992-01-24

1993-03-02

Lee, Lester L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 18, 530329, 530330, A61K 3702, C07K 508, C07K 510, C07K 706

Patent

active

051909219

ABSTRACT:
These compounds are represented by formula (I), in which each of R.sub.1 R.sub.2 =H, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, or aromatic; (when R.sub.1 =H, R.sub.2 can be an amine function-protecting radical, amino acid residue or peptide fragment; R.sub.1 and R.sub.2 being capable of forming, with N, a 5-7 component ring); A=carbonyl or methylene; W=hydroxy, phenoxy, C.sub.1 -C.sub.8 alkoxy; phenoxy(C.sub.1 -C.sub.8 alkyl), amino, (C.sub.1 -C.sub.8 alkyl)amino, di(C.sub.1 -C.sub.8 alkyl)amino, (when A=carbonyl, W=amino acid residue or peptide fragment); Y=--OSO.sub.2 OR.sub.3 (II), --OPO(OR.sub.3).sub.2 (III), --(CH.sub.2 (.sub.m --SO.sub.2 OR.sub.3 (IV) or --(CH.sub.2).sub.m --PO(OR.sub.3).sub.2 (V) [R.sub.3 =H, C.sub.1 -C.sub.8 alkyl; m=1 to 4]; Z=cyclohexane, pyridyl or phenyl; n=0 to 4; on the condition that when Y=(II) or (III), -A-W is other than a sequence composed of natural amino acids. They have antipsychotic properties, an effect facilitating the memorization processes, analgesic properties; they are useful as anorexia-producing agents, and they have stimulatory effects on intestinal motility. ##STR1##

REFERENCES:
patent: 4657899 (1987-04-01), Rzeszotarski
Journal of Controlled Release, 13, 147-155, 1990.
Journal of Medicinal Chemistry,32, 445-449, 1989.
Neurology Neurobiology, vol. 46, pp. 231-234, 1988.
Marseigna, J. Org. Chem., vol. 53, No. 15, pp. 3621-3624, Jul. 22, 1988.

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