Back to results
US 5,633,263 AGranted
Linear somatostatin analogs
AssigneeThe Administrators of the Tulane Educational Fund
InventorsDavid H. Coy, William A. Murphy
Life of this patent
Estimating the term…
Abstract
Linear peptide analogs of somatostatin having the formula: ##STR1## As an example, D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr is covered by the above formula (i.e., R.sub.1 is H, R.sub.2 is H, A.sup.1 is D-Phe, A.sup.2 is Phe, A.sup.3 is Phe, A.sup.6 is Thr, A.sup.7 is Phe, A.sup.8 is Thr, and R.sub.3 is NH.sub.2).
Claims16
An octapeptide of the formula:
- ##STR3## wherein A.sup.1 is a D-isomer of .beta.-Nal, Phe, 2,4-dichloro-Phe, pentafluoro-Phe, p-X-Phe, or o-X-Phe, wherein X is CH.sub.3, Cl, Br, F, OH, OCH.sub.3, or NO.sub.2 ;
- A.sup.2 is Ala, Phe, .beta.-Nal, 2,4-dichloro-Phe, pentafluoro-Phe, o-X-Phe, or p-X-Phe, wherein X is CH.sub.3, Cl, Br, F, OH, OCH.sub.3, or NO.sub.2 ;
- A.sup.3 is Phe, .beta.-Nal, Trp, 2,4-dichloro-Phe, pentafluoro-Phe, o-X-Phe, or p-X-Phe, wherein X is CH.sub.3, Cl, Br, F, OH, OCH.sub.3, or NO.sub.2 ;
- A.sup.6 is Val, Ala, Leu, Ile, Nle, Thr, or Ser;
- A.sup.7 is Ala, Phe, .beta.-Nal, 2,4-dichloro-Phe, Pentafluoro-Phe, o-X-Phe, or p-X-Phe, wherein X is CH.sub.3, Cl, Br, F, OH, OCH.sub.3, or NO.sub.2 ;
- A.sup.8 is a D- or L-isomer of Thr, Ser, Phe, .beta.-Nal, [pyridyl-Ala, Trp,]2,4-dichloro-Phe, pentafluoro-Phe, p-X-Phe, or o-X-Phe, wherein X is CH.sub.3, Cl, Br, F, OH, OCH.sub.3, or NO.sub.2 ;
- each R.sub.1 and R.sup.2, independently, is H, C.sub.1-5 acyl or C.sub.1-5 alkyl;
- and R.sub.3 is OH or NH.sub.2 ;
- provided that at least one of A.sup.1 and A.sup.2 and one of A.sup.7 and A.sup.8 must be one of the aromatic amino acid assigned thereto;
- and further provided that each of A.sup.1, A.sup.2, A.sup.7, and A.sup.8 cannot all be one of the aromatic amino acids assigned thereto;
- or a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.