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Somatostatin analogs
| Details |
Inventors: Veber, Daniel F.; Holly, Frederick W.; Strachan, Robert G.; Paleveda, William J.; Nutt, Ruth F.; Hirschmann, Ralph F.;
Assignee: Merck & Co., Inc. (Rahway, NJ)
Primary Examiner: Phillips; Delbert R.
Assistant Examiner:
Attorney, Agent or Firm: Patton; Walter, Westlake, Jr.; Harry E.
Somatostatin analogs having the structural formula: ##STR1## are prepared by controlled stepwise procedures starting with individual amino acid components. These peptides have the property of lowering blood glucose, inhibiting gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals. |
|
DETAILED DESCRIPTION What is claimed is: 1.
The peptides having the structure: ##STR55## wherein: X is CH.
sub.
2, S, ##STR56## SO.
sub.
2 and [X].
sub.
n wherein n=0; Y is CH.
sub.
2, S, ##STR57## SO.
sub.
2 and [Y].
sub.
n wherein n=0; R is H, NH.
sub.
2 and R"NH and wherein R" is Ala-Gly-, lower acyl containing 2 to 6 carbon atoms or aroyl containing 7 to 21 carbon atoms; R' is H and CO.
sub.
2 H; wherein X and Y are not both heteroatoms and when R' is H, X and Y are not both --CH.
sub.
2 --; and R'" is asparagine, alanine or .
alpha.
-aminobutyric acid.
2.
The peptides having the structure: ##STR58## wherein X-Y is: ##STR59## R is H, NH.
sub.
2 and R"NH wherein R" is Ala-Gly-, lower acyl containing 2 to 6 carbon atoms or aroyl containing 7 to 21 carbon atoms; R' is H and CO.
sub.
2 H and when R' is H, X and Y are also --CH.
sub.
2 --CH.
sub.
2 -- and --CH.
sub.
2 --; and R'" is asparagine, alanine or .
alpha.
-aminobutyric acid.
3.
The peptide according to claim 2 having the structure: ##STR60## 4.
The peptide according to claim 3 having the structure: ##STR61## 5.
The peptide according to claim 2 having the structure: ##STR62## 6.
The peptide according to claim 2 having the structure: ##STR63## 7.
The peptide according to claim 2 having the structure: ##STR64## 8.
The peptide according to claim 7 having the structure: ##STR65## 9.
The peptide according to claim 2 having the structure: ##STR66## wherein X-Y is --CH.
sub.
2 --S-- and --S--CH.
sub.
2 --.
10.
The peptide according to claim 9 having the structure: ##STR67## wherein X-Y is --CH.
sub.
2 --S-- and --S--CH.
sub.
2 --.
11.
The peptides having the structure: ##STR68## ##STR69## wherein: X is CH.
sub.
2, S and [X].
sub.
n wherein n=0; Y is CH.
sub.
2, S and [Y].
sub.
n wherein n=0; R is H, NH.
sub.
2 or R"NH wherein R" is Ala-Gly-, lower acyl containing 1 to 6 carbon atoms or aroyl containing 7 to 21 carbon atoms; R' is H or CO.
sub.
2 H; wherein X and Y are not both heteroatoms.
12.
The peptide according to claim 11 having the structure: ##STR70## 13.
The peptides having the structure: ##STR71## wherein: X is CH
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Molecular Biology 
