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US 4,061,608 AGranted
Arg .sup.4 -somatostatin and analogues thereof
AssigneeAmerican Home Products Corporation
InventorDimitrois Sarantakis
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Abstract
Polypeptides of the formula: ##STR1## THE LINEAR PRECURSORS, INTERMEDIATES AND NON-TOXIC ACID ADDITION SALTS THEREOF, WHEREIN R is hydrogen or Ala-Gly And X.sub.8 is L-Trp or D-Trp Are described. These polypeptides inhibit the secretion of growth hormone and, at low doses, excel in their higher glucagon to insulin lowering ratio.
Claims9
A polypeptide of the formula:
- ##STR4## its linear precursor or a non-toxic acid addition salt thereof, in which R is hydrogen or Ala-Gly-
- and
- X.sub.8 is L-Trp or D-Trp.
A polypeptide of the formula:
- R.sup.1 --Arg(N.sup.g --R.sup.2)--Asn--Phe--Phe--X.sub.8 --Lys(R.sup.3)--Thr(R.sup.4)--Phe--Thr(R.sup.5)--Ser(R.sup.6)--Cys(R.sup.7 )--OR.sup.8
- wherein
- X.sub.8 is L-tryptophyl or D-tryptophyl;
- R.sup.1 is hydrogen or an .alpha.-amino protecting group;
- R.sup.2 is hydrogen, nitro, tosyl, benzyloxycarbonyl, adamantyloxycarbonyl or tert-butyloxycarbonyl;
- R.sup.3 is hydrogen, tosyl, t-amyloxycarbonyl, t-butyloxycarbonyl, diisopropyloxycarbonyl, benzyloxycarbonyl, halobenzyloxycarbonyl or nitrobenzyloxycarbonyl;
- R.sup.4, r.sup.5 and R.sup.6 are hydrogen or, independently, acetyl, benzoyl, tert-butyl, benzyl;
- R.sup.7 is benzyl, trityl, benzyloxycarbonyl, benzhydryl, tetrahydropyranyl, acetamidomethyl, benzoyl, benzylthiomethyl, ethylcarbamoyl, thioethyl, S-sulfonate salt, 3,4-dimethylbenzyl, p-methoxybenzyl or p-nitrobenzyl;
- and
- R.sup.8 is hydrogen or --CH.sub.2 -[polystyrene resin support].
7 more elements
Dependencies are inferred from the claim text.