.beta.-amino acid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...


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514 19, 514521, 514522, 514519, 514530, 514531, 514538, 514539, 514541, 514542, 558392, 558393, 558404, 558405, 558414, 558430, 558431, 558432, 558433, 558434, 560 19, 560 45, 560 47, 560 50, 564152, 564155, 564157, 564158, A61K 3116, A61K 31165, C07C25546, C07C25550, C07C23360




Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest of the formula ##STR1## wherein R.sub.1 is selected from cycloalkyl and cycloakylalkyl groups, wherein said cycloalkyl group contains three to about eight carbon atoms and the acyclic alkyl portion of said cycloakylalkyl group contains one to about eight carbon atoms; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; and wherein R.sub.7 is isobutyl or ethyl; or a pharmaceutically-acceptable salt thereof.

patent: 3422104 (1969-01-01), Schroter et al.
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S. Lecolier, Chim. Ther., 3, 34-38 (1968).
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S. M. Rothman and J. W. Olney, "Glutamate and the Pathophysiology of Hypoxic--Ischemic Brain Damage", Annals of Neurology, 19, 105-111 (1986).
P. L. Wood et al, Neuropharm., 21, 1235-1238 (1982).
C. Carter et al, J. Pharm. Exp. Ther., 247 (3), 1222-1232 (1988).


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