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1. (WO2006116057) FACILITATED TRANSPORT OF BISPHOSPHONATES BY VITAMIN C

Pub. No.:    WO/2006/116057    International Application No.:    PCT/US2006/015051
Publication Date: Nov 2, 2006 International Filing Date: Apr 21, 2006
IPC: C07F 9/02
A61K 31/4427
Applicants: DUKE UNIVERSITY
KRAUS, Virginia, Byers
MCNULTY, Amy, Lynn
TOONE, Eric, John
Inventors: KRAUS, Virginia, Byers
MCNULTY, Amy, Lynn
TOONE, Eric, John
Title: FACILITATED TRANSPORT OF BISPHOSPHONATES BY VITAMIN C
Abstract:
Compounds of the formula: are described wherein: A1 is ascorbic acid, dehydroascorbic acid, ascorbyl-2-phosphate, an analog thereof, or a salt thereof; L is a linking group coupled to A1 at the C5 or C6 position thereof; and B1 is an active agent such as an imaging agent or therapeutic agent (e.g. a bisphosphonate), along with pharmaceutically acceptable salts and prodrugs thereof. The compounds are useful for, among other things, improving cartilage uptake of active agents administered for joint diseases such as osteoarthritis and rheumatoid arthritis, and for improving gastrointestinal absorption of bisphosphonates.