Patents Assigned to Nicox S.A.
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Patent number: 7825263Abstract: The present invention relates to ?-adrenergic blockers nitrooxyderivatives of general formula (I): A-(Y—ONO2)s and enantiomers and diastereoisomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them and their use for the treatment of hypertension, cardiovascular diseases, glaucoma, migraine headache and vascular diseases.Type: GrantFiled: December 1, 2004Date of Patent: November 2, 2010Assignee: Nicox S.A.Inventors: Piero Del Soldato, Francesca Benedini, Ennio Ongini
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Publication number: 20100266683Abstract: The present invention claims and discloses a pharmaceutical composition suitable for oral administration, in form of an emulsion pre-concentrate, comprising (i) a compound of the formula (I) (ii) one or more surfactants; (iii) optionally an oil or semi-solid fat; said composition forming an in-situ oil-in-water emulsion upon contact with aqueous media such as gastrointestinal fluids. The composition may optionally also comprise one or more short-chain alcohols. The pharmaceutical composition is useful in the treatment of pain and inflammation.Type: ApplicationFiled: April 28, 2010Publication date: October 21, 2010Applicant: NICOX S.A.Inventors: Christina HOLMBERG, Britta Siekmann
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Patent number: 7815933Abstract: The present invention claims and discloses a pharmaceutical composition suitable for oral administration, in form of an emulsion pre-concentrate, comprising (i) one or more NO-releasing NSAID(s); (ii) one or more surfactants, of which at least one is phospholipid; said composition forming an in-situ oil-in-water emulsion upon contact with gastrointestinal fluids. The composition may optionally also comprise an additional oil or semi-solid fat. Further, one or more short-chain alcohols can optionally be included in the composition. Also within the scope of the invention is a combination with a proton pump inhibitor. The pharmaceutical composition is useful in the treatment of pain and inflammation. Further within the scope of the invention is kit comprising a pharmaceutical composition according to the invention in a unit dosage form, in combination with a proton pump inhibitor, and said proton pump inhibitor is enteric coated.Type: GrantFiled: September 5, 2002Date of Patent: October 19, 2010Assignee: Nicox S.A.Inventor: Christina Holmberg
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Patent number: 7812039Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A-(B)b0-(C)o0-N02 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R-TI-, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from aminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: November 14, 2007Date of Patent: October 12, 2010Assignee: Nicox S.A.Inventors: Piero Del Soldato, Ennio Ongini
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Publication number: 20100256411Abstract: 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: ApplicationFiled: June 18, 2009Publication date: October 7, 2010Applicant: NICOX S.A.Inventors: Pietro Allegrini, Tiziano Scubla, Nicoletta Toniutti, Romano Rivolta, Thierry Delahaique
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Publication number: 20100249189Abstract: The invention relates to nitric oxide donors of the formula (I) and pharmaceutically acceptable salts or stereoisomers thereof: wherein A and A? are independently selected from the group consisting of H and —(X)S—Y with the proviso that at least one of A or A? is not H; wherein s is 0 or 1; X is selected from the group consisting of: —CO—, —COO—, —CONH— and —SO2— or Y is straight or branched C1-C20 alkyl chain, preferably C1-C10 alkyl chain, substituted with one or two —ONO2; or C1-C6 alkylenoxy-C1-C5 alkyl wherein the alkyl group is substituted by one or two —ONO2 groups. The invention also provides novel compositions comprising at least one compound of the invention and at least one therapeutic agent.Type: ApplicationFiled: January 15, 2009Publication date: September 30, 2010Applicant: NICOX S.A.Inventors: Nicoletta Almirante, Silvia Stefanini, Laura Storoni, Fabio Nicoli, Julio Lazaro Padron
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Publication number: 20100240745Abstract: The present invention relates to the use of 4-(nitrooxy)-butyl-(S)-2-(6-methoxy-2-naphthyl)-propanoate (naproxcinod) for the treatment of pain and/or inflammation in patients with hypertension treated with renin-angiotensin system blocking agents.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: NICOX S.A.Inventors: Rosa Rosanna B. FLEMING, Brigitte Duquesroix, William B. White
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Patent number: 7799784Abstract: The present invention relates to alpha2-adrenergic receptor agonist nitrooxyderivatives, including the following structure, having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of ocular diseases, in particular high intraocular pressure and glaucoma.Type: GrantFiled: February 2, 2007Date of Patent: September 21, 2010Assignee: Nicox S.A.Inventors: Francesca Benedini, Francesco Impagnatiello, Stefano Biondi, Ennio Ongini, Wesley Kwan Mung Chong
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Publication number: 20100234334Abstract: The invention relates to nitrooxyderivative of corticosteriods of general formula (I) and pharmaceutical acceptable salts or stereoisomers thereof wherein R is the corticosteriod residue of formulas (II): The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological disease and ocular diseases.Type: ApplicationFiled: January 28, 2008Publication date: September 16, 2010Applicant: NICOX S.A.Inventors: Francesca Benedini, Stefano Biondi, Ennio Ongini
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Publication number: 20100217028Abstract: The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.Type: ApplicationFiled: March 30, 2010Publication date: August 26, 2010Applicant: NICOX S.A.Inventors: Piero DEL SOLDATO, Giancarlo SANTUS, Francesca BENEDINI
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Publication number: 20100210694Abstract: The present invention refers to new NO-donors aspirin derivatives, a process for their preparation and pharmaceutical compositions containing them.Type: ApplicationFiled: September 3, 2008Publication date: August 19, 2010Applicant: NICOX S.A.Inventors: Roberta Fruttero, Alberto Gasco, Loretta Lazzarato, Monica Donnola, Barbara Rolando, Stefano Biondi
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Patent number: 7776902Abstract: New compounds able to release COX-2 inhibitors and NO having formula (I): M-T-YA—NO2??(I) for the treatment and/or prophylaxis of inflammatory processes.Type: GrantFiled: June 20, 2003Date of Patent: August 17, 2010Assignee: Nicox S.A.Inventors: Piero Del Soldato, Giancarlo Santus
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Patent number: 7759392Abstract: Compounds or their salts of general formula (I): A-B—N(O)s wherein: s is an integer equal to 1 or 2; A=R-T1-, wherein R is the drug radical and T1=(CO)t or (X)t?, wherein X?O, S, NR1c, R1c is H or a linear or branched alkyl or a free valence, t and t? are integers and equal to zero or 1, with the proviso that t=1 when t?=0; t=0 when t?=1; B=-TB-X2—O— wherein TB=(CO) when t=0, TB=X when t?=0, X being as above defined; X2 is equal to R1B—X—R2B radical wherein X is as above defined, R1B and R2B, equal to or different from each other, are linear or branched C1-C6 alkylenes, or X2 is a radical wherein two alkylene chains C1-C4 are linked to nonadjacent positions of a central ring having 4 or 6 atoms, said ring being an unsaturated cycloaliphatic ring, or a saturated or aromatic heterocylic ring, containing one or two heteroatoms, equal or different, selected from O, S, N; wherein the unsaturated cycloaliphatic ring does not have aromatic character according to Huckel's rule.Type: GrantFiled: June 3, 2008Date of Patent: July 20, 2010Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Publication number: 20100179192Abstract: The present invention relates to nitrooxyderivative of antioxidant compounds of formula (I) and pharmaceutically acceptable salts or stereoisomers thereof for the treatment of chronic pain, in particular chronic neuropathic pain. The invention also describes composition comprising a nitrooxyderivative of a antioxidant compound of formula (I) and an analgesic drugs.Type: ApplicationFiled: June 24, 2008Publication date: July 15, 2010Applicant: NICOX S.A.Inventors: Francesco Impagnatiello, Daniela Ronchetti, Ennio Ongini, Francesca Benedini
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Patent number: 7754772Abstract: 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: GrantFiled: May 23, 2005Date of Patent: July 13, 2010Assignee: 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
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Publication number: 20100174075Abstract: The present invention relates to the use of nitric oxide-releasing statins of formula (I) for the treatment of pulmonary arterial hypertension.Type: ApplicationFiled: May 12, 2008Publication date: July 8, 2010Applicant: NICOX S.A.Inventors: John Wharton, Angela Monopoli
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Publication number: 20100166839Abstract: Non-peptidic renin inhibitors nitroderivatives of general formula (I): A1-(Xa—ONO2)j ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing cardiovascular, renal and chronic liver diseases, inflammatory processes and metabolic syndrome.Type: ApplicationFiled: March 1, 2007Publication date: July 1, 2010Applicant: Nicox S.AInventors: Nicoletta Almirante, Stefano Biondi, Ennio Ongini
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Patent number: 7745496Abstract: A process for preparing a compound of formula (I) X-(CH2)n-ONO2??(I) wherein: X is a halogen atom selected from Cl, Br, I; n is an integer from 3 to 6; said process comprising the slow addition of a compound of formula (II) X-(CH2)n-OH??(II) wherein X and n are as defined above to a nitrating agent selected from the group consisting of concentrated nitric acid/concentrated sulfuric acid (sulfonitric mixture), nitric acid alone, NaNO2 in trifluoroacetic acid, nitronium salts such as NO2BF4 and an organic solvent selected from the group consisting of CH2Cl2, CHCl3, CCl4, perfluorohexane, perfluoroheptane. The invention refers also to solutions containing: a compound of general formula (I) and a solvent selected from the group consisting of CH2Cl2, CHCl3, CCl4, perfluorohexane, perfluoroheptane, characterized in that the compound of formula (I) is present in a concentration not higher than 20% by weight.Type: GrantFiled: November 9, 2005Date of Patent: June 29, 2010Assignee: Nicox S.A.Inventors: Romano Rivolta, Peter Finlander
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Publication number: 20100152274Abstract: The present invention relates to two crystalline forms designated as form A and form B, of (?R,?R)-2(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbon-yl]-1H-pyrrole-1-heptanoic acid 4-(nitrooxy)butyl ester (atorvastatin 4-(nitrooxy)butyl ester), represented by the formula (I), The invention also relates to processes for the preparation of the forms A and B, to pharmaceutical compositions comprising the two forms, and to their use for treating and/or preventing acute coronary syndromes, stroke, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis.Type: ApplicationFiled: March 19, 2008Publication date: June 17, 2010Applicant: Nicox S.A.Inventors: Francesca Benedini, Stefano Biondi, Annalisa Bonfanti, Fabio Nicoli
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Publication number: 20100152259Abstract: A compound having the structure (Formula I), wherein R an angiotensin receptor antagonist active group, Y is Y1—Y2—Y3—Y4—Y5. Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 11, 2007Publication date: June 17, 2010Applicants: Merck & Co Inc., NICox S.A.Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali, Chris Franklin, Nicoletta Almirante, Laura Storoni, Silvia Stefanini