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
1985-05-20
1986-06-10
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...
560 16, 560 34, 560 41, 560125, 560153, 560147, 560168, 560169, 562426, 562439, 562450, 562507, 562556, 562557, 562560, 562561, C07K 506, C07C14943, C07C10100, C07C10102, C07C10910, C07C10142, C07C 6108, C07C14702, C07C149243, C07C109106, C07C10124, C07C 6974, C07C14920, C07C10126, C07C14940
Patent
active
045941882
ABSTRACT:
An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;
REFERENCES:
H. Umezawa et al., J. Antibiotics, vol. 29, p. 97 (1976), "Bestatin, An Inhibitor of Aminopeptidase B, Produced by Actinomycetes".
H. Suda et al., J. Antibiotics, vol. 29, p. 100 (1976), "The Structure of Bestatin".
T. Aoyagi et al., J. Antibiotics, vol. 31, p. 636 (1978), "Amastatin, An Inhibitor of Aminopeptidase A, Produced By Actinomycetes".
H. Tobe et al., Agric. Biol. Chem., vol. 43, p. 591 (1979), "Structure and Chemical Synthesis of Amastatin".
G. Wagner et al., J. Neurochem., vol. 37, p. 709 (1980), "Inhibitors of a Rat Brain Enkephalin Aminopeptidase".
R. Meyer et al., J. Med. Chem., vol. 25, p. 996 (1982), "Angiotensin Converting Enzyme Inhibitors: Modifications of a Tripeptide Analogue".
T. Aoyagi et al., J. Antibiotics, vol. 36, p. 1572 (1983), "Arphamenines A and B, New Inhibitors of Aminopeptidaze B, Produced by Bacteria".
H. Umezawa et al., J. Antibiotics, vol. 36, p. 1576 (1983), "The Structure of Arphamenines A and B".
Delaney Norma G.
Gordon Eric M.
Barrack Donald J.
E. R. Squibb & Sons Inc.
Levinson Lawrence S.
Phillips Delbert R.
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