Octapeptide analogs of somatostatin having threonine at the sixth position

US5506339A · kind A · utility

Assignee

• The Administrators of the Tulane Educational Fund · US

Inventors

• David H. Coy · New Orleans, US
• William A. Murphy · Slidell, US

Key dates

• Filing date: Feb 21, 1992
• Grant date: Apr 9, 1996
• Expiry date: Feb 21, 2012

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y10S930/26
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; PA1 each X.sub.1 and X.sub.2, independently, is H, F, Cl, Br, OH, CH.sub.3, or CF.sub.3, provided that at least one of X.sub.1 and X.sub.2 must be H; PA1 A.sub.3 is Phe or Tyr; and PA1 A.sub.4 is OH, NH.sub.2, or NH-R.sub.3 (wherein R.sub.3 is a saturated aliphatic C.sub.1-8 alkyl); or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.