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Galactosylated pro-drugs of non-steroidal anti-inflammatories with improved pharmacokinetic characteristics and reduced toxicity of the starting drug

Rimoli, Maria Grazia and Calignano, Antonio and Cuomo, Rosario and Boatto, Gianpiero and Abignente, Enrico and Melisi, Daniela and Curcio, Annalisa and Luongo, Elvira and La Rana, Giovanna and Sasso, Oscar and Sarnelli, Giovanni and Russo, Roberto and Nieddu, Maria and Cirillo, Carla and De Lucia, Salvatore (2010) Galactosylated pro-drugs of non-steroidal anti-inflammatories with improved pharmacokinetic characteristics and reduced toxicity of the starting drug. WO/2010/013279. Patent.

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Abstract

Pro-drugs of all non-steroidal anti-inflammatories with free acid function derivatized with an ester group, which have the general structural formula given below (I) where A is: aspirin, diflunisal, benorylate, ibufenac, diclofenac, indomethacin, sulindac, ketorolac, ibuprofen, naproxen, ketoprofen, fenoprofen, flurbiprofen, mefenamic acid, meclof enamic acid, flufenamic acid, niflumic acid, and where in the ester group R can be a sugar (amongst which aldose, or ketose pentose, or esose selected from a group of D- and L- enantioiuers of ribose, glucose, galactose, mannose, arabinose, xilose, allose, altrose, gulose, idose and talose and substituted derivatives thereof, such as glucosamine, galactosamine, N-acetyl glucosamine, N-acetyl galactosamine, N-acetyl ribosamine), a disaccharide, a trisaccharide or an oligosaccharide.

Item Type:Patent
ID Code:4449
Status:Published
Uncontrolled Keywords:Galactosylated pro-drugs, pharmacokinetic characteristics, toxicity
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Patent Applicant:M. G. Rimoli, Stewart Italia srl, A. Calignano, R. Cuomo, G. Boatto, E. Abignente, D. Melisi, A. Curcio, E. Luongo, G. La Rana, O. Sasso, G. Sarnelli, R. Russo, M. Nieddu, C. Cirillo, S. De Lucia
International Application Number:PCT/IT2009/000341
International Patent Classification:A61K 47/48 (2006.01), A61P 29/00 (2006.01)
Attorney, Agent, or Firm:Sarpi, Maurizio
Deposited On:31 Aug 2010 15:30

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