COMPOSÉS LIBÉRANT DE L'OXYDE NITRIQUE POUR LE TRAITEMENT DE DOULEURS NEUROPHATIQUES
N ALMIRANTE, A NICOTRA, V BORGHI… - WO Patent WO/2011/092,065, 2011
... 2011. IPC: C07D 333/20 C07C 271/22 A61K 31/381 A61K 31/325 A61P 29/00. Applicants: NICOX
SA ALMIRANTE, Nicoletta NICOTRA, Alessia BORGHI, Valentina ONGINI, Ennio. Inventors:
ALMIRANTE, Nicoletta NICOTRA, Alessia BORGHI, Valentina ONGINI, Ennio. ...
http://www.wipo.int/patentscope/search/fr/WO2011092065
et...
ncx250
A new approach to antiglaucoma drugs: carbonic anhydrase inhibitors with or without NO donating moieties. Mechanism of action and preliminary pharmacology
Posted online on August 4, 2011. (doi:10.3109/14756366.2011.597749)
HTML
PDF (871 KB)
PDF Plus (872 KB)
Reprints
Permissions
Francesca Fabrizi1, Francesco Mincione2, Teresa Somma1, Gabriele Scozzafava3, Fernando Galassi4, Emanuela Masini1, Francesco Impagnatiello5, Claudiu T. Supuran6
1Università degli Studi di Firenze, Department of Preclinical and Clinical Pharmacology,
Florence
, Italy
2U.O. Oculistica Az. USL 3,
Val di Nievole, Ospedale di Pescia, Pescia
, Italy
3Dipartimento di Economia, Ingegneria, Scienze e Tecnologie Agrarie e Forestali,
Florence
, Italy
4Università degli Studi di Firenze, Dipartimento di Scienze Chirurgiche Specialistiche,
Sezione di Oculistica, Florence
, Italy
5Nicox Research Institute,
Bresso, Milan
, Italy
6Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica,
Florence
, Italy
Address for Correspondence: Emanuela Masini, Università degli Studi di Firenze, Department of Preclinical and Clinical Pharmacology,
Viale Pierracini 6, Florence
, Italy. Tel: +39-055-4271233; Fax: +39-055-4271280; E-mail: emanuela.masini@unifi.it; Claudiu T. Supuran, Università degli Studi di Firenze, Dipartimento di Scienze Chirurgiche Specialistiche,
Sezione di Oculistica, Viale G.B. Morgagni 85, Florence
, Italy. Tel: +39-055-4573005; Fax: +39-055-4573385; E-mail: claudiu.supuran@unifi.it
The clinically used sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitor dorzolamide (DRZ), a new sulfonamide CA inhibitor also incorporating NO-donating moieties, NCX250, and isosorbide mononitrate (ISMN) (an NO-donating compound with no CA inhibitory properties) were investigated for their intraocular pressure (IOP) lowering effects in rabbits with carbomer-induced glaucoma. NCX250 was more effective than DRZ or ISMN on lowering IOP, increasing ocular hemodynamics, decreasing the inflammatory processes and ocular apoptosis in this animal model of glaucoma. NO participate to the regulation of IOP in glaucoma, having also antiapoptotic and anti-inflammatory effects. The ophthalmic artery, both systolic and diastolic velocities, were significantly reduced in NCX250-treated eyes in comparison to DRZ treated ones, suggesting thus a beneficial effect of NCX250 on the blood supply to the optic nerve. Combining CA inhibition with NO-donating moieties in the same compound offers an excellent approach for the management of glaucoma.
Keywords
sulfonamide, carbonic anhydrase, NO donor, dorzolamide, glaucoma, carbomer, intraocular pressure
Read More: http://informahealthcare.com/doi/abs/10.3109/14756366.2011.597749
vu passer aussi un brevet commun avec ferrer
http://www.wipo.int/patentscope/search/fr/WO2011058162