Abstract: The invention relates to nitric oxide releasing phosphodiesterase type 5 (PDE5) inhibitors of formula or a stereoisomer or a pharmaceutically acceptable salt thereof: useful for the treatment of ocular condition associated with elevated intraocular pressure such as ocular hypertension, glaucoma or retinopathies.
Type:
Grant
Filed:
July 31, 2019
Date of Patent:
May 14, 2024
Assignee:
NICOX S.A.
Inventors:
Nicoletta Almirante, Stefania Brambilla, Laura Storoni, Francesco Impagnatiello, Elena Bastia
Abstract: This invention provides a method of lowering intraocular pressure in a patient having normal tension glaucoma, comprising contacting an eye of a subject having normal tension glaucoma with a pharmaceutical composition comprising an effective amount of Nitric Oxide releasing prostaglandin derivatives of formula (I).
Type:
Grant
Filed:
November 7, 2017
Date of Patent:
July 13, 2021
Assignees:
Nicox S.A., Bausch & Lomb Incorporated
Inventors:
Jason Lamar Vittitow, Megan Elizabeth Cavet
Abstract: The present invention provides aqueous ophthalmic compositions in the form of solution comprising hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]-3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester and macrogol 15 hydroxystearate as the only solubilizing agent, and a method for their preparation.
Type:
Grant
Filed:
March 11, 2020
Date of Patent:
June 1, 2021
Assignee:
NICOX S.A.
Inventors:
Frédéric Pilotaz, Alan L. Weiner, Marina Do, Julien Saldo
Abstract: The present invention relates to a process for preparing the hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]-3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester of formula (I). In accordance with the present invention, the compound (I) can be efficiently prepared with high purity by coupling bimatoprost in a boronate protected form with 6-(nitrooxy)hexanoyl chloride and removing the boronate protecting group. The 6-(nitrooxy)hexanoyl chloride intermediate is prepared by ring-opening reaction of 2-caprolactone and subsequent nitration of the 6-hydroxyhexanoic acid potassium salt with a mixture of HNO3 and H2SO4 in dichloromethane.
Abstract: The present invention relates to compositions for treating glaucoma and elevated ocular pressure. The compositions comprise a nitric oxide releasing isomannide derivative and a prostaglandin F2? analog.
Type:
Grant
Filed:
November 17, 2015
Date of Patent:
April 7, 2020
Assignee:
NICOX S.A.
Inventors:
Nicoletta Almirante, Laura Storoni, Elena Bastia, Francesco Impagnatiello
Abstract: The present invention relates to 15-nitrooxyderivatives of fluprostenol, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxy derivatives of fluprostenol.
Type:
Grant
Filed:
January 28, 2016
Date of Patent:
May 7, 2019
Assignee:
NICOX S.A.
Inventors:
Nicoletta Almirante, Laura Storoni, Elena Bastia, Stefania Brambilla, Francesco Impagnatiello
Abstract: The present invention relates to a pharmaceutical composition for use as a medicament in the prophylactic or therapeutic topical treatment of viral eye infections caused by adenovirus of subtype D or influenza A virus of subtype H7. The composition in its ready-for-use formulation comprises iota carrageenan as an active antiviral ingredient and is substantially free of a metal halide salt or contains no more than 0.5% w/v of a metal halide salt.
Type:
Grant
Filed:
January 20, 2015
Date of Patent:
March 5, 2019
Assignee:
NICOX S.A.
Inventors:
Eva Prieschl-Grassauer, Martina Morokutti-Kurz, Andreas Grassauer, Sabine Nakowitsch, Angelika Bodenteich, Marielle König-Schuster, Christiane Koller, Frederic Pilotaz
Abstract: The present invention relates to 15-nitrooxyderivatives of latanoprost and 15-nitrooxyderivatives of latanoprost free acid, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxyderivatives of latanoprost and 15-nitrooxyderivatives of latanoprost free acid.
Type:
Grant
Filed:
March 22, 2016
Date of Patent:
August 14, 2018
Assignee:
NICOX S.A.
Inventors:
Nicoletta Almirante, Laura Storoni, Elena Bastia, Stefania Brambilla, Francesco Impagnatiello
Abstract: The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.
Abstract: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx??(I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position ? or ?; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.
Abstract: The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment of pathological conditions where a deficit of NO plays an important role in their pathogenesis.
Type:
Application
Filed:
October 23, 2012
Publication date:
November 20, 2014
Applicant:
NICOX S.A.
Inventors:
Gael Ronsin, Laura Storoni, Francesca Benedini
Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.
Abstract: The present invention relates to the use of nitric oxide releasing compounds for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies.
Abstract: The present invention relates to a pharmaceutical formulation comprising: a) one or more NO-releasing NSAID(s) of formula (I); b) one or more surfactants; c) a carbonyl scavenger compound selected from free acid forms, salts, carboxylic acid esters derivatives of a compound of formula (II) H2N—(CH2)m—(C6H4)—COOH??(II) wherein m=0-10; and d) optionally an oil or semi-solid fat and/or a short-chain alcohol.
Abstract: The present invention relates to the use of nitric oxide releasing compounds for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies.
Abstract: The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.
Abstract: The present invention relates to the use of nitric oxide releasing compounds for retarding or reversing muscular dystrophies such as Duchenne and Becker dystrophies.
Abstract: This invention relates to a new process for preparing 4-nitro-oxy-methyl-benzoic acid, comprising the following steps: a) reaction of 4-chloromethyl-benzoic acid with silver nitrate and in the presence of an acid as a catalyst in acetonitrile at reflux temperature, followed by cooling and adding of a polar aprotic solvent; b) separation of the silver salts by filtration, followed by washout with a polar aprotic solvent; c) precipitation of the 4-nitro-oxy-methyl-benzoic acid with water from the filtrate obtained in step b); and d) drying of the 4-nitro-oxy-methyl-benzoic acid.
Type:
Application
Filed:
November 15, 2010
Publication date:
May 23, 2013
Applicants:
NICOX S.A., FERRER INTERNACIONAL, S.A
Inventors:
Luis Anglada, Albert Palomer, Luis Sobral
Abstract: The present invention relates to a method for purifying naproxcinod comprising the steps of: a) dissolving or dispersing a mixture containing naproxcinod in an amount higher than 90% by weight in a solvent; b) cooling the solution or two phases dispersion under stirring to a temperature ranging from ?20° C. to 10° C. c) optionally seeding the solution with crystals of naproxcinod d) stirring, by maintaining the temperature in the range from ?40° C. to 10° C. e) collecting the formed solid by maintaining the temperature under 15° C. A further object of the invention is a crystalline form of naproxcinod.
Type:
Grant
Filed:
June 18, 2009
Date of Patent:
December 11, 2012
Assignee:
Nicox S.A.
Inventors:
Pietro Allegrini, Tiziano Scubla, Nicoletta Toniutti, Romano Rivolta, Thierry Delahaique
Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
Type:
Grant
Filed:
December 11, 2009
Date of Patent:
November 6, 2012
Assignee:
Nicox S.A.
Inventors:
Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey