Multi-tyrosinated somatostatin analogs

US5597894A · kind A · utility

Assignees

• Louisiana State University Medical Center Foundation · US
• THE CHILDREN'S HOSPITAL CORPORATION · US
• The Administrators of the Tulane Educational Fund · US
• The Ohio State University Research Foundation · US

Inventors

• David H. Coy · New Orleans, US
• Eugene A. Woltering · Kenner, US
• M. Sue O'Dorisio · Columbus, US
• Thomas M. O'Dorisio · Worthington, US
• William A. Murphy · Slidell, US

Key dates

• Filing date: Jun 5, 1995
• Grant date: Jan 28, 1997
• Expiry date: Jun 5, 2015

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K38/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Disclosed are methods and compositions for the diagnosis and treatment of diseases associated with aberrant expression of a somatostatin receptor (e.g., cancer) or with increased production of a factor regulatable by somatostatin (e.g., acromegaly). The compounds of the invention are of the general formulae: ##STR1## wherein P is a somatostatin peptide analog which binds to a somatostatin receptor, PA1 Y is D-tyrosine, L-tyrosine, or desamino-tyrosine, PA1 n is an integer from 1 to 32, inclusive, PA1 each q, independently, is an integer from 1 to 32, inclusive, and each s, independently, is an integer from 1 to 32, inclusive, where q and s can be the same or different, and PA1 X is of the formula EQU D--NH.sub.2 --CH(CH.sub.2).sub.m NH.sub.2 --CO.sub.2 H or EQU L--NH.sub.2 --CH(CH.sub.2).sub.m NH.sub.2 --CO.sub.2 H, wherein m is an integer from 1 to 10, inclusive.