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1. (WO2010013279) GALACTOSYLATED PRO-DRUGS OF NON-STEROIDAL ANTI-INFLAMMATORIES WITH IMPROVED PHARMACOKINETIC CHARACTERISTICS AND REDUCED TOXICITY OF THE STARTING DRUG
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2010/013279    International Application No.:    PCT/IT2009/000341
Publication Date: 04.02.2010 International Filing Date: 29.07.2009
IPC:
A61K 47/48 (2006.01), A61P 29/00 (2006.01)
Applicants: RIMOLI, Maria Grazia [IT/IT]; (IT).
STEWART ITALIA SRL [IT/IT]; Corso G. Matteotti, 10 I-20121 Milano (IT) (For All Designated States Except US).
CALIGNANO, Antonio [IT/IT]; (IT).
CUOMO, Rosario [IT/IT]; (IT).
BOATTO, Gianpiero [IT/IT]; (IT).
ABIGNENTE, Enrico [IT/IT]; (IT) (For US Only).
MELISI, Daniela [IT/IT]; (IT) (For US Only).
CURCIO, Annalisa [IT/IT]; (IT) (For US Only).
LUONGO, Elvira [IT/IT]; (IT) (For US Only).
LA RANA, Giovanna [IT/IT]; (IT) (For US Only).
SASSO, Oscar [IT/IT]; (IT) (For US Only).
SARNELLI, Giovanni [IT/IT]; (IT) (For US Only).
RUSSO, Roberto [IT/IT]; (IT) (For US Only).
NIEDDU, Maria [IT/IT]; (IT) (For US Only).
CIRILLO, Carla [IT/IT]; (IT) (For US Only).
DE LUCIA, Salvatore [IT/IT]; (IT) (For US Only)
Inventors: RIMOLI, Maria Grazia; (IT).
CALIGNANO, Antonio; (IT).
CUOMO, Rosario; (IT).
BOATTO, Gianpiero; (IT).
ABIGNENTE, Enrico; (IT).
MELISI, Daniela; (IT).
CURCIO, Annalisa; (IT).
LUONGO, Elvira; (IT).
LA RANA, Giovanna; (IT).
SASSO, Oscar; (IT).
SARNELLI, Giovanni; (IT).
RUSSO, Roberto; (IT).
NIEDDU, Maria; (IT).
CIRILLO, Carla; (IT).
DE LUCIA, Salvatore; (IT)
Agent: SARPI, Maurizio; Studio Ferrario Via Collina, 36 I-00187 Roma (IT)
Priority Data:
NA2008A000047 29.07.2008 IT
Title (EN) GALACTOSYLATED PRO-DRUGS OF NON-STEROIDAL ANTI-INFLAMMATORIES WITH IMPROVED PHARMACOKINETIC CHARACTERISTICS AND REDUCED TOXICITY OF THE STARTING DRUG
(FR) PROMÉDICAMENTS GALACTOSYLÉS D'ANTI-INFLAMMATOIRES NON STÉROÏDIENS PRÉSENTANT DES CARACTÉRISTIQUES PHARMACOCINÉTIQUES AMÉLIORÉES ET UNE TOXICITÉ RÉDUITE DU MÉDICAMENT DE DÉPART
Abstract: front page image
(EN)Pro-drugs of all non-steroidal anti-inf lammatories 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.
(FR)La présente invention concerne des promédicaments de tous les anti-inflammatoires non stéroïdiens à fonction acide libre dérivatisés avec un groupe ester, de formule générale développée (I) ci-dessous où A est l'aspirine, le diflunisal, le bénorilate, l'ibufénac, le diclofénac, l'indométacine, le sulindac, le kétorolac, l'ibuprofène, le naproxène, le kétoprofène, le fénoprofène, le flurbiprofène, l'acide méfénamique, l'acide méclofénamique, l'acide flufénamique, l'acide niflumique, et où dans le groupe ester, R peut être un sucre (dont l'aldose ou le cétose pentose ou l'ose choisi dans un groupe d'énantiomères D- et L- du ribose, glucose, galactose, mannose, arabinose, xylose, allose, altrose, gulose, idose et talose, ainsi que parmi leurs dérivés substitués, comme la glucosamine, la galactosamine, la N-acétylglucosamine, la N-acétylgalactosamine, la N-acétylribosamine), un disaccharide, un trisaccharide ou un oligosaccharide.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Org. (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (EAPO) (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (OAPI) (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: Italian (IT)