Process for the preparation of backbone cyclic peptides

US5723575A · kind A · utility

Assignee

• YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD. · IL

Inventors

• Chaim Gilon · Jerusalem, IL
• Zvi Zelinger · Jerusalem, IL
• Gerardo Byk · Créteil, FR

Key dates

• Filing date: May 18, 1995
• Grant date: Mar 3, 1998
• Expiry date: May 18, 2015

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Biologically active, backbone-cyclized peptides of the formula: ##STR1## wherein AA! or A.sup.1 A.sup.1 ! is a naturally occurring or synthetic amino acid residue, n or e is an integer of 1-10, m or d is 0 or an integer of 1-10, R is a naturally occurring or synthetic amino acid side-chain, E is a hydroxyl moiety or a carboxyl protecting group of a blocking group, optionally covalently attached to an insoluble polymeric support, and the circled line designates a spacer group of ##STR2## for formula I wherein M is --S--S--, --CO--NH-- or --S-- and p and q each is an integer of 2-10, or EQU --(CH.sub.2).sub.p --(M).sub.x --Y (IV) for formula II wherein M is an amino or carboxyl group or a sulfur atom, p is an integer of 2-10, x is 0 or 1 and Y is a side-chain of a backbone amino acid. Also, processes for the preparation of these peptides and pharmaceutical compositions containing them.