Somatostatin analogs and intermediates thereto
AssigneeEli Lilly and Company
InventorJames E. Shields
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Abstract
The tetradecapeptides ##STR1## in which Y is L-Cha, L-Leu, or D-Phe are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts inhibit the release of growth hormone.
Claims28
A compound selected from those of the formula ##STR9## and their pharmaceutically acceptable non-toxic acid addition salts, and R-L-Ala-Gly-L-Cys(R.sub.1)-L-Lys(R.sub.2)-L-Asn-L-Phe-L-Phe-L-Trp(R.sub.5) -L-Lys(R.sub.2)-L-Thr(R.sub.3)-Y-L-Thr(R.sub.3)-L-Ser(R.sub.4)-L-Cys(R.sub. 1)-X;
- in which
- Y is D-Phe, L-Cha, or L-Leu;
- R is hydrogen or an .alpha.-amino protecting group;
- R.sub.1 is hydrogen or a thio protecting group;
- R.sub.2 is hydrogen or an .EPSILON.-amino protecting group;
- R.sub.3 and R.sub.4 each are hydrogen or a hydroxy protecting group;
- R.sub.5 is hydrogen or formyl;
- and
- X is hydroxy or ##STR10## in which the resin is polystyrene;
- with the proviso that, when X is hydroxy, each of R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 is hydrogen, and, when X is ##STR11## each of R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is other than hydrogen.
Dependencies are inferred from the claim text.