Patents Assigned to Nicox S.A.
  • Patent number: 7825263
    Abstract: 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: Grant
    Filed: December 1, 2004
    Date of Patent: November 2, 2010
    Assignee: Nicox S.A.
    Inventors: Piero Del Soldato, Francesca Benedini, Ennio Ongini
  • Publication number: 20100266683
    Abstract: 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: Application
    Filed: April 28, 2010
    Publication date: October 21, 2010
    Applicant: NICOX S.A.
    Inventors: Christina HOLMBERG, Britta Siekmann
  • Patent number: 7815933
    Abstract: 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: Grant
    Filed: September 5, 2002
    Date of Patent: October 19, 2010
    Assignee: Nicox S.A.
    Inventor: Christina Holmberg
  • Patent number: 7812039
    Abstract: 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: Grant
    Filed: November 14, 2007
    Date of Patent: October 12, 2010
    Assignee: Nicox S.A.
    Inventors: Piero Del Soldato, Ennio Ongini
  • Publication number: 20100256411
    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: Application
    Filed: June 18, 2009
    Publication date: October 7, 2010
    Applicant: NICOX S.A.
    Inventors: Pietro Allegrini, Tiziano Scubla, Nicoletta Toniutti, Romano Rivolta, Thierry Delahaique
  • Publication number: 20100249189
    Abstract: 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: Application
    Filed: January 15, 2009
    Publication date: September 30, 2010
    Applicant: NICOX S.A.
    Inventors: Nicoletta Almirante, Silvia Stefanini, Laura Storoni, Fabio Nicoli, Julio Lazaro Padron
  • Publication number: 20100240745
    Abstract: 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: Application
    Filed: March 19, 2010
    Publication date: September 23, 2010
    Applicant: NICOX S.A.
    Inventors: Rosa Rosanna B. FLEMING, Brigitte Duquesroix, William B. White
  • Patent number: 7799784
    Abstract: 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: Grant
    Filed: February 2, 2007
    Date of Patent: September 21, 2010
    Assignee: Nicox S.A.
    Inventors: Francesca Benedini, Francesco Impagnatiello, Stefano Biondi, Ennio Ongini, Wesley Kwan Mung Chong
  • Publication number: 20100234334
    Abstract: 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: Application
    Filed: January 28, 2008
    Publication date: September 16, 2010
    Applicant: NICOX S.A.
    Inventors: Francesca Benedini, Stefano Biondi, Ennio Ongini
  • Publication number: 20100217028
    Abstract: 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: Application
    Filed: March 30, 2010
    Publication date: August 26, 2010
    Applicant: NICOX S.A.
    Inventors: Piero DEL SOLDATO, Giancarlo SANTUS, Francesca BENEDINI
  • Publication number: 20100210694
    Abstract: The present invention refers to new NO-donors aspirin derivatives, a process for their preparation and pharmaceutical compositions containing them.
    Type: Application
    Filed: September 3, 2008
    Publication date: August 19, 2010
    Applicant: NICOX S.A.
    Inventors: Roberta Fruttero, Alberto Gasco, Loretta Lazzarato, Monica Donnola, Barbara Rolando, Stefano Biondi
  • Patent number: 7776902
    Abstract: 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: Grant
    Filed: June 20, 2003
    Date of Patent: August 17, 2010
    Assignee: Nicox S.A.
    Inventors: Piero Del Soldato, Giancarlo Santus
  • Patent number: 7759392
    Abstract: 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: Grant
    Filed: June 3, 2008
    Date of Patent: July 20, 2010
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Publication number: 20100179192
    Abstract: 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: Application
    Filed: June 24, 2008
    Publication date: July 15, 2010
    Applicant: NICOX S.A.
    Inventors: Francesco Impagnatiello, Daniela Ronchetti, Ennio Ongini, Francesca Benedini
  • Patent number: 7754772
    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: May 23, 2005
    Date of Patent: July 13, 2010
    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
  • Publication number: 20100174075
    Abstract: The present invention relates to the use of nitric oxide-releasing statins of formula (I) for the treatment of pulmonary arterial hypertension.
    Type: Application
    Filed: May 12, 2008
    Publication date: July 8, 2010
    Applicant: NICOX S.A.
    Inventors: John Wharton, Angela Monopoli
  • Publication number: 20100166839
    Abstract: 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: Application
    Filed: March 1, 2007
    Publication date: July 1, 2010
    Applicant: Nicox S.A
    Inventors: Nicoletta Almirante, Stefano Biondi, Ennio Ongini
  • Patent number: 7745496
    Abstract: 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: Grant
    Filed: November 9, 2005
    Date of Patent: June 29, 2010
    Assignee: Nicox S.A.
    Inventors: Romano Rivolta, Peter Finlander
  • Publication number: 20100152274
    Abstract: 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: Application
    Filed: March 19, 2008
    Publication date: June 17, 2010
    Applicant: Nicox S.A.
    Inventors: Francesca Benedini, Stefano Biondi, Annalisa Bonfanti, Fabio Nicoli
  • Publication number: 20100152259
    Abstract: 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: Application
    Filed: December 11, 2007
    Publication date: June 17, 2010
    Applicants: 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