Nitrogen In R Patents (Class 514/619)
  • Patent number: 10329256
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Grant
    Filed: March 5, 2018
    Date of Patent: June 25, 2019
    Assignee: Oryzon Genomics, S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Àngeles Estiarte Martinez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 10265282
    Abstract: The invention relates generally to the treatment of cancer. One embodiment of the invention provides a method of treating cancer in an individual, the method comprising: administering to the individual an effective amount of trichostatin A (TSA).
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: April 23, 2019
    Assignee: Vanda Pharmaceuticals Inc.
    Inventors: Mihael H. Polymeropoulos, Louis William Licamele, Christian Lavedan
  • Patent number: 9968630
    Abstract: The invention is based on a finding that silencing CIP2A (KIAA1524) gene sensitizes cancer cells for apoptosis-inducing activity of certain small molecule chemotherapeutic agents. Thus, the invention is directed to a respective combination therapy, sensitization method and pharmaceutical compositions. The invention further relates to a method of selecting cancer therapy for a subject on the basis of CIP2A and p53 expression and/or protein activity in a sample obtained from said subject.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: May 15, 2018
    Assignee: TURUN YLIOPISTO
    Inventors: Jukka Westermarck, Anna Cvrljevic
  • Patent number: 9610274
    Abstract: The invention is directed to a method of treating bipolar disorder in a subject, comprising administering a therapeutically effective amount of a carbamate compound, or pharmaceutically acceptable salt or amide thereof.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: April 4, 2017
    Assignee: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Sung James Lee, Susan Marie Melnick
  • Patent number: 9487512
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: November 8, 2016
    Assignee: Oryzon Genomics S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martinez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 9464052
    Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X is hydroge
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: October 11, 2016
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Simon David Edwards, Meriel Ruth Kimberley, Richard Edward Armer, Nawaz Mohammed Khan
  • Patent number: 9206125
    Abstract: The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain. The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g.
    Type: Grant
    Filed: February 9, 2011
    Date of Patent: December 8, 2015
    Assignees: PUBLIC UNIVERSITY CORPORATION YOKOHAMA CITY UNIVERSITY, NAGASAKI UNIVERSITY, NAGOYA CITY UNIVERSITY
    Inventors: Yoshifumi Nishimura, Aritaka Nagadoi, Yuuka Hirao, Yoshio Goshima, Naoya Yamashita, Naoki Miyata, Takayoshi Suzuki, Ryuta Hiraishi, Hiroshi Ueda
  • Patent number: 9169198
    Abstract: The present invention relates to a process for preparing 2-amino-5-cyano-N,3-dimethylbenzamide of formula (I) by reacting 2-amino-5-cyano-3-methylbenzoic esters or diesters with methylamine.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: October 27, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Frank Volz, Thomas Himmler, Thomas Norbert Müller, Sandra Lehmann, Sascha Von Morgenstern, Wahed Ahmed Moradi, Sergii Pazenok, Norbert Lui
  • Patent number: 9144609
    Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. An embodiment of said liquid preparation does not include any preservative. Said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: September 29, 2015
    Assignee: SENJU PHARMACEUTICAL CO., LTD.
    Inventors: Shirou Sawa, Shuhei Fujita, George A. Baklayan, Angeliqueo E. Padilla
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150140122
    Abstract: The invention relates to methods for detecting inactivation of the DNA Homologous Recombination pathway in a patient, and in particular for detecting BRCA1 inactivation.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 21, 2015
    Applicant: INSERM (Institut National de la Sante et de la Rec herche)
    Inventors: Marc-Henri Stern, Elodie Manie, Tatiana Popova
  • Publication number: 20150087711
    Abstract: Methods and compositions for using a tetracycline compound to treat bacterial infections are described. In one embodiment, for example, the invention provides a method of treating a subject for an infection, comprising administering to said subject an effective amount of 9-[(2,2-dimethyl-propyl amino)-methyl]-minocycline or a salt thereof, such that said subject is treated, wherein said infection is selected from the group consisting of MSSA, MRSA, B-streptococci, Viridans Streptococci, Enterococcus, or combinations thereof.
    Type: Application
    Filed: April 22, 2014
    Publication date: March 26, 2015
    Applicant: Paratek Pharmaceuticals, Inc.- 124418
    Inventors: Sean M. Johnston, Robert D. Arbeit, Thomas J. Bigger, Dennis P. Molnar, S. Ken Tanaka
  • Publication number: 20150073021
    Abstract: The present invention provides a method of inhibiting the binding of anthrax lethal factor with protective antigen comprising contacting the anthrax lethal factor with a compound having the structure:
    Type: Application
    Filed: September 5, 2014
    Publication date: March 12, 2015
    Applicants: The Research Foundation for The State University of New York, Chem-Master International, Inc.
    Inventors: Anthony ANTONELLI, Sanford R. SIMON, Yu ZHANG, Lorne M. GOLUB, Francis JOHNSON
  • Publication number: 20150072011
    Abstract: The present invention generally relates to suspension compositions having a carboxyvinyl polymer such as a carbomer, a galactomannan such as guar, and a borate compound. A sparingly soluble particulate compound such as nepafenac is also included in the compositions. The sparingly soluble particulate compound has a small particle size to enhance bioavailability of the compound.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 12, 2015
    Inventors: Masood A. CHOWHAN, Malay GHOSH, Bahram ASGHARIAN, Wesley Weshin HAN
  • Patent number: 8951934
    Abstract: The invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a compound of formula (I) and at least one further respiratory chain complex in inhibitor (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: December 5, 2009
    Date of Patent: February 10, 2015
    Assignee: Bayer CropScience AG
    Inventors: Burkhard Schütz, Peter Dahmen, Ulrike Wachendorff-Neumann, Peter Herold
  • Publication number: 20150038492
    Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
    Type: Application
    Filed: August 12, 2014
    Publication date: February 5, 2015
    Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
  • Patent number: 8946295
    Abstract: A method for promoting wound healing and preventing scar formation in a variety of wounds in skin, mucosa, and cornea. The method comprises administering a therapeutically effective amount of a histone deacetylase inhibitor or a hyperacetylating agent. The histone deacetylase inhibitor or hyperacetylating agent is capable of stimulating multiple cytokines/growth factors in the early phase of wound healing, and suppressing fibrogenic cytokines/growth factors in the late phase of tissue remodeling in the wound site, and is useful in promoting epithelial cell re-growth and reducing excessive collagen accumulation, which results in rapid wound closure with reduced scaring.
    Type: Grant
    Filed: May 10, 2004
    Date of Patent: February 3, 2015
    Assignee: Sunny Pharmtech Inc.
    Inventor: Yih-Lin Chung
  • Patent number: 8946296
    Abstract: The invention relates to compounds of Formula (I): (A?)x-(A)-(B)—(Z)-(L)-C(?O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A?), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: February 3, 2015
    Assignee: Oryzon Genomics S.A.
    Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
  • Publication number: 20150023921
    Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
    Type: Application
    Filed: April 3, 2014
    Publication date: January 22, 2015
    Applicant: BIOTRON LIMITED
    Inventors: Gary Dinneen EWART, Carolyn Anne LUSCOMBE, Michelle MILLER
  • Publication number: 20150011628
    Abstract: The invention relates to substituted diphenylamine compounds using as antitumor agents. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) showed potent antitumor activity, especially to cure or alleviate the cancer causing by cancer cells of human tissue or organ. The preferred cancers are: colon cancer, liver cancer, lymph cancer, lung cancer, esophageal cancer, breast cancer, central nervous system cancer, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostatic cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharynx cancer or stomach cancer.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 8, 2015
    Inventors: Changling Liu, Baoshan Chai, Huichao Li, Aiying Guan
  • Patent number: 8927606
    Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
    Type: Grant
    Filed: September 23, 2014
    Date of Patent: January 6, 2015
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Shirou Sawa, Shuhei Fujita
  • Patent number: 8906395
    Abstract: A pharmaceutical composition includes lipid nanoparticles which include two or more of a phospholipid, cholesterol, and an ionic lipid, and a tricyclic derivative, wherein the solubility of the tricyclic derivative is improved. It is possible to solubilize a partially soluble tricyclic derivative in a high concentration even without using a solubilization aid harmful to the human body, to maintain improved solubility even if water is added for the use as an injection, and to show stability even if stored for a long time, by preparing lipid nanoparticles. Therefore, the lipid nanoparticles of the present invention can be used for preparing a pharmaceutical preparation containing a partially soluble tricyclic derivative as an active ingredient.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: December 9, 2014
    Assignee: Jeil Pharmaceutical Co., Ltd.
    Inventors: Myung-Hwa Kim, Kwang-Woo Chun, In-Hae Ye, Jong-Hee Choi
  • Publication number: 20140348819
    Abstract: The present invention provides methods of treating cancer.
    Type: Application
    Filed: June 22, 2012
    Publication date: November 27, 2014
    Applicants: Dana-Farber Cancer Institute, Inc., The Broad Institute, Inc.
    Inventors: Todd Golub, Ravid Straussman
  • Publication number: 20140341891
    Abstract: The present invention is based, at least in part, on the identification of a pharmaceutical container formed, at least in part, of a glass composition which exhibits a reduced propensity to delaminate, i.e., a reduced propensity to shed glass particulates. As a result, the presently claimed containers are particularly suited for storage of pharmaceutical compositions and, specifically, a pharmaceutical solution comprising a pharmaceutically active ingredient, for example, LYXUMIA (lixisenatide), LEMTRADA (alemtuzumab), REGN727/SAR236553 (alirocumab), SAR2405550/BSI-201 (iniparib), OTAMIXABAN (otamixaban), SARILUMAB (sarilumab), LANTUS and LYXUMIA (insulin glargine and lixisenatide) or VISAMERIN/MULSEVO (semuloparin sodium).
    Type: Application
    Filed: April 23, 2014
    Publication date: November 20, 2014
    Applicant: CORNING INCORPORATED
    Inventors: Wendell P. Weeks, Robert Anthony Schaut, Steven Edward DeMartino, John Stephen Peanasky
  • Patent number: 8889742
    Abstract: The present invention provides methods of ameliorating or reducing the extent of ischemic injury, reperfusion injury, and myocardial infarction, by administering an inhibitor of histone deacetylase enzyme (HDAC) or an inhibitor of DNA methyltransferase enzyme (DNMT).
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: November 18, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Peter J. Gruber, Jonathan A. Epstein, Ibrahim Abdullah
  • Publication number: 20140336254
    Abstract: A family of covalent kinetic stabilizer compounds that selectively and covalently react with the prominent plasma protein transthyretin in preference to more than 4000 other human plasma proteins is disclosed. A contemplated compound corresponds in structure to Formula I, below, where the various substituents are defined within, and reacts chemoselectively with one or two of four Lys-15 ?-amino groups within the transthyretin tetramer. The crystal structure confirms the binding orientation of the compound substructure and the conjugating amide bond. A covalent transthyretin kinetic stabilizer exhibits superior amyloid inhibition potency, compared to a non-covalent counterpart, and inhibits cytotoxicity associated with amyloidogenesis.
    Type: Application
    Filed: April 14, 2014
    Publication date: November 13, 2014
    Inventors: Jeffery W. Kelly, Sungwook Choi
  • Publication number: 20140329833
    Abstract: The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 6, 2014
    Applicant: ORYZON GENOMICS, S.A
    Inventors: Tamara Maes, Marc Martinell Pedemonte, Julio Castro-Palomino Laria
  • Patent number: 8877815
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: November 4, 2014
    Assignee: Novartis AG
    Inventors: Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Qian Liu, Muneto Mogi, Nikolaus Schiering, Robert Sun
  • Patent number: 8877816
    Abstract: Compounds of the formula: are disclosed. The compounds act as phosphodiesterase-4 modulators, and useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions. Other embodiments are also disclosed.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 4, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov
  • Patent number: 8871813
    Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: October 28, 2014
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Shirou Sawa, Shuhei Fujita
  • Publication number: 20140316008
    Abstract: Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 23, 2014
    Inventors: Bernard ATTALI, Asher PERETZ
  • Patent number: 8853266
    Abstract: This invention provides use of a SARM compound or a composition comprising the same in treating a variety of diseases or conditions in a subject, including, inter-alia, a diabetes disease, and/or disorder such as cardiovascular disease, atherosclerosis, cerebrovascular conditions, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: October 7, 2014
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller
  • Patent number: 8853281
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Publication number: 20140296255
    Abstract: The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.
    Type: Application
    Filed: May 21, 2012
    Publication date: October 2, 2014
    Applicant: ORYZONG GENOMICS, S.A.
    Inventors: Tamara Maes, Marc Martinell Pedemonte
  • Publication number: 20140294970
    Abstract: The present invention is directed to a pharmaceutical submicron suspension and a method of forming the submicron suspension. The submicron suspension is useful for delivery of relatively hydrophobic and/or low solubility therapeutic agent. The submicron suspension and method of forming the submicron suspension typically employ a polymeric material that aids in preventing aggregation of the therapeutic agent.
    Type: Application
    Filed: June 11, 2014
    Publication date: October 2, 2014
    Inventors: Bahram Asgharian, Ernesto J. Castillo, Masood A. Chowhan
  • Publication number: 20140296191
    Abstract: The present invention relates to pharmaceutical compositions of various pharmaceutical actives, especially lyophilic and hydrophilic actives containing Diethylene glycol monoethyl ether or other alkyl derivatives thereof as a primary vehicle and/or to pharmaceutical compositions utilizing Diethylene glycol monoethyl ether or other alkyl derivatives thereof as a primary vehicle or as a solvent system in preparation of such pharmaceutical compositions. The pharmaceutical compositions of the present invention are safe, non-toxic, exhibits enhanced physical stability compared to conventional formulations containing such pharmaceutical actives and are suitable for use as injectables for intravenous and intramuscular administration, as well as for use as a preformed solution/liquid for filling in and preparation of capsules, tablets, nasal sprays, gargles, dermal applications, gels, topicals, liquid oral dosage forms and other dosage forms.
    Type: Application
    Filed: April 2, 2014
    Publication date: October 2, 2014
    Applicant: THEMIS MEDICARE LIMITED
    Inventors: Dinesh Shantilal PATEL, Sachin Dinesh PATEL, Shashikant Prabhudas KURANI, Madhavlal Govindlal PATEL
  • Patent number: 8841346
    Abstract: The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: September 23, 2014
    Assignees: Massachusetts Institute of Technology, The Broad Institute, Inc., The General Hospital Corporation
    Inventors: Li-Huei Tsai, Ji-Song Guan, Stephen J. Haggarty, Edward Holson, Florence Wagner, Johannes Graeff
  • Publication number: 20140256742
    Abstract: The invention relates to methods and compositions for the treatment or prevention of Flaviviridae infections. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing Flaviviridae infections, including hepatitis C virus infections.
    Type: Application
    Filed: December 4, 2013
    Publication date: September 11, 2014
    Inventors: Jonathan A. BAKER, Matthew Collin Thor Fyfe
  • Publication number: 20140256746
    Abstract: A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed.
    Type: Application
    Filed: September 10, 2013
    Publication date: September 11, 2014
    Applicant: CALOSYN PHARMA, INC.
    Inventor: David D. Waddell
  • Publication number: 20140248236
    Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 4, 2014
    Inventors: Michael G. Natchus, Richard Arrendale
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Publication number: 20140213657
    Abstract: The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A?), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 31, 2014
    Applicant: ORYZON GENOMICS S.A.
    Inventors: Alberto Ortega MUÑOZ, Julio CASTRO-PALOMINO LARIA, Matthew Colin Thor FYFE
  • Patent number: 8791135
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: July 29, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Publication number: 20140206690
    Abstract: The present invention relates to compound (I) wherein R1 and R2 independently represent a hydrogen atom, a (C1-C4)alkoxy group, a fluoro(C1-C4)alkoxy group, a hydroxyl group, a benzyloxy group, a di(C1-C4)alkylamino group, a pyridyl-vinyl group, a pyrimidinyl-vinyl group, a styryl group, or a —NHCOphenyl group; R3, R4 and R5 independently represent a hydrogen atom, a (C1-C4)alkyl group, a CONHR6 group, a —CONR7R8 group, a —SO2NHR6 group, or a heteroaryl group optionally substituted by a halogen atom, a —(CH2)nNR7R8 group or a hydroxy(C1-C4)alkyl group; R6 represents a hydrogen atom, a —(CHR9)m(CH2)nNR7R8 group or a (C1-C6)alkyl group optionally substituted by a hydroxyl group; or anyone of its pharmaceutically acceptable salt, for use in a method for preventing, inhibiting or treating a disease in a patient suffering thereof, said disease involving a deregulated p53. Some of said compounds are new and also form part of the invention.
    Type: Application
    Filed: April 2, 2012
    Publication date: July 24, 2014
    Applicants: SOCIETE SPLICOS, UNIVERSITE DE MONTPELLIER 2, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Didier Scherrer, Jamal Tazi, Romain Najman, Florence Mahuteau, Pierre Roux
  • Publication number: 20140179700
    Abstract: Methods of alleviating the symptoms of hemoglobinopathies, including, but not limited to, sickle cell disease, ?-thalassemia, and hemoglobin H disease are provided. In some embodiments, the methods comprise administering an inhibitor selected from an ERK inhibitor, a MEK inhibitor, and a Raf inhibitor. Methods of inhibiting adhesion of sickle red blood cells to endothelial cells are also provided.
    Type: Application
    Filed: April 30, 2012
    Publication date: June 26, 2014
    Applicant: Duke Univeristy
    Inventor: Rahima Zennadi
  • Publication number: 20140179794
    Abstract: The present invention concerns the use of levomilnacipran as medicinal product in functional recovery after a cerebrovascular accident or traumatic brain injury. The pharmaceutical compositions containing levomilnacipran are exclusively those not containing dextromilnacipran to a proportion of more than 5% by weight of the levomilnacipran/dextromilnacipran mixture, to avoid compromising functional recovery due to the alpha1-blocking property of dextromilnacipran.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 26, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventor: Pierre Sokoloff
  • Patent number: 8754131
    Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: June 17, 2014
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Shirou Sawa, Shuhei Fujita
  • Publication number: 20140163041
    Abstract: The present invention relates to methods and compositions for the treatment or prevention of diseases and disorder associated with myeloproliferative and lymphoproliferative disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing diseases and disorder associated with myeloproliferative and lymphoproliferative disorders.
    Type: Application
    Filed: February 8, 2012
    Publication date: June 12, 2014
    Applicant: ORYZON GENOMICS S.A.
    Inventors: Matthew Colin Thor Fyfe, Tamara Maes, Marc Martinell Pedemonte
  • Publication number: 20140163111
    Abstract: The invention relates to compositions including porous biomolecule-containing metal-organic frameworks and methods for their preparation. The porous biomolecule-containing metal-organic frameworks can include a metal component and a biomolecule component. The pores located within the frameworks have a pore space and said pore space is capable to adsorb materials therein. These compositions of the invention are useful in a wide variety of applications, such as, but not limited to, hydrogen and carbon dioxide sequestration, separation and storage; carbon dioxide uptake; and drug storage and release.
    Type: Application
    Filed: February 13, 2014
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: NATHANIEL LOUIS ROSI, JIHYUN AN
  • Patent number: 8748339
    Abstract: The present invention relates to a composition, comprising a 5-amino-3-oxo-2,3-dihydro-pyrazole of the formula I as defined in the claims and the description and at least one active compound II selected from groups A) to I) in a synergistically effective amount.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Egon Haden