Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Containing at least one abnormal peptide link – e.g. – gamma...
Patent
1987-06-12
1990-02-06
Phillips, Delbert R.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Containing at least one abnormal peptide link, e.g., gamma...
530323, 562503, 562507, 560125, 560129, 564159, 548537, C07K 754
Patent
active
048989304
ABSTRACT:
Peptide ester and amide derivatives of the general formula I: ##STR1## in which X is H or an acyl, A and B are structurally defined amino acid residues, n is an integer of from 1 to 3, R.sup.1 is H or a lower alkyl and either R.sup.2 or C is a defined optionally modified amino acid residue and the other is a lower alkoxyl, an amino group or a direct chemical bond, are converted under physiologic conditions, by enzymic hydrolysis in pathologically altered tissues and subsequent spontaneous cyclization, into pharmacodynamically active spirocyclic peptide derivatives of the general formula III: ##STR2## in which R.sup.3 and R.sup.4 are H atoms, optionally substituted alkyl groups or jointly an aliphatic chain forming preferably a 2,5- piperazinedione ring, and hence can act as pro-farmaca (drug precursors) of prolonged biological effect.
REFERENCES:
patent: 4278595 (1981-07-01), Cort
patent: 4620012 (1986-10-01), Henning et al.
patent: 4690936 (1987-09-01), Ryan et al.
Inhibition of Proliferative Activity by Cyclic Dipeptides: Spirocyclic Derivatives of 1-Aminocyclopentane-Carboxylic Acid (Toxicology Letters, 31 (1986) 189-192).
VIIIth International Symposium on Medicinal Chemistry (Proceedings), vol. 2; Swedish Academy of Pharmaceutical Sciences.
Activitas Nservosa Superior--vol. 28, 12/86, Research Institute For Pharmacy and Biochemistry.
Bartik Michal
Kasafirek Evzen
Krejci Ivan
Krepela Evzen
Roubalova Alena
Phillips Delbert R.
Spofa spojene podniky pro
Wessendorf T.
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