Membrane-permeant second messengers

US5834436A · kind A · utility

Assignee

• The Regents of the University of California · US

Inventors

• Roger Y. Tsien · Village of La Jolla, US
• Carsten Schultz · Heidelberg, DE
• Wenhong Li · Village of La Jolla, US

Key dates

• Filing date: Jun 7, 1995
• Grant date: Nov 10, 1998
• Expiry date: Jun 7, 2015

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/65522
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Acyloxyalkyl esters of phosphate-containing second messengers which are capable of permeating cell membranes. Once inside the cell, the ester derivatives undergo enzymatic conversion to the biologically active form of the second messenger. The acyloxyalkyl esters have the formula: ##STR1## wherein A.sub.1 to A.sub.6 is H, OH, F or ##STR2## wherein R is an alkyl group having from 2 to 6 carbon atoms and R' is H or CH.sub.3 or R is CH.sub.3 and R' is CH.sub.3 and wherein at least one of A.sub.1 to A.sub.6 is a phosphoester having the formula set forth above.