Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
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Publication number: 20140187567Abstract: A composition having a stable and high fungicidal effect against a cultivated crop infected by a plant pathogen is provided. An agricultural or horticultural fungicide composition containing, as active ingredients, (a) fluazinam or its salt and (b) a strobilurin compound or its salt is provided; in addition, a method for controlling a plant pathogen by applying the subject agricultural or horticultural fungicide composition to a plant or a soil is provided; and furthermore, a method for controlling a plant pathogen by applying (a) fluazinam or its salt and (b) a strobilurin compound or its salt to a plant or a soil is provided.Type: ApplicationFiled: May 25, 2012Publication date: July 3, 2014Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Takanori Suzuki, Koudai Yamamoto
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Publication number: 20140187586Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X1, X2, Z, R3, R4, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: March 12, 2014Publication date: July 3, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Zhiqiang Xia, Junyi Zhang, Gary Bohnert, Shoujun Chen, Yu Xie
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Publication number: 20140179518Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: BASF SEInventors: Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang VON DEYN, Matthias POHLMAN, Juergen LANGEWALD, Egon HADEN
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Publication number: 20140179686Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Gruenenthal GmbHInventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
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Patent number: 8754111Abstract: A method for the synthesis of N-substituted 3-acylated pyridinium compounds by reacting a pentamethine precursor with a primary amine.Type: GrantFiled: July 18, 2013Date of Patent: June 17, 2014Assignee: Roche Diagnostics Operations, Inc.Inventors: Peter Gebauer, Dieter Heindl, Carina Horn
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Patent number: 8754110Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.Type: GrantFiled: December 28, 2012Date of Patent: June 17, 2014Assignee: Dow AgroSciences, LLC.Inventors: Jossian Oppenheimer, Mark V. M. Emonds, Christopher W. Derstine, Robert C. Clouse
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Patent number: 8748445Abstract: The present disclosure provides for method of treatment and/or prevention of disease states that require cystine for maintenance or progression of the disease state. In addition, methods for screening and identifying novel therapeutic agents useful in the treatment of such disease states are described. In one embodiment, the disease state is a cancer, such as, but not limited to, glioma. In this embodiment, methods for the treatment and prevention of glioma by inhibiting cystine uptake or decreasing intracellular cystine concentrations are provided. The present disclosure teaches that glioma cells are dependent on system Xc for cystine uptake. Pharmacological inhibition of system Xc causes a rapid depletion of intracellular glutathione, resulting in decreased cell growth. In contrast, non-malignant astrocytes and cortical neurons remain viable in the presence of Xc inhibitors and continue to take up cystine via alternate amino acid transporters.Type: GrantFiled: October 27, 2005Date of Patent: June 10, 2014Assignee: The UAB Research FoundationInventors: W. Joon Chung, Harald Sontheimer
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Publication number: 20140155436Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.Type: ApplicationFiled: November 4, 2013Publication date: June 5, 2014Applicants: CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, INSTITUT CURIEInventors: Jamal TAZI, David GRIERSON, Florence MAHUTEAU-BETZER, Pierre ROUX
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Patent number: 8735394Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents (such as an anti-VEGF antibody), or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.Type: GrantFiled: May 6, 2009Date of Patent: May 27, 2014Assignee: Abraxis BioScience, LLCInventors: Neil P. Desai, Patrick Soon-Shiong
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Patent number: 8729107Abstract: Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol.Type: GrantFiled: September 9, 2010Date of Patent: May 20, 2014Assignee: Purdue Research FoundationInventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
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Publication number: 20140135359Abstract: The present invention provides a computer-assisted method of generating a protonophore requiring the use of a computer including a processor. The method includes: designing the protonophore, calculating, using the processor, an estimated protonophoric activity; producing the protonophore if the estimated protonophoric activity corresponds to an U50 of about 20 ?M or less; and determining the uncoupling activity of the protonophore. The present invention also provides novel protonophores that meet the above requirement and their methods of use.Type: ApplicationFiled: November 12, 2012Publication date: May 15, 2014Inventor: Louis C. Martineau
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Publication number: 20140134262Abstract: The present invention provides a compound of Formula I: for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride level; wherein R1, X1, R7, R5, C, L and p are defined herein. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of diseases and conditions associated with CETP activity, such as atherosclerosis and dyslipidemia, in a subject with high triglyceride levels.Type: ApplicationFiled: July 6, 2012Publication date: May 15, 2014Inventors: Yoshie Arai, Margaret Elizabeth Brousseau, Jessie Gu, Tomoko Hayashi, Hironobu Mitani, Muneto Mogi, Kazuhiko Nonomura, Ken Yamada
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Publication number: 20140135329Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20140135320Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.Type: ApplicationFiled: November 8, 2013Publication date: May 15, 2014Applicant: Jacobus Pharmaceutical Company, Inc.Inventors: Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
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Publication number: 20140128397Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.Type: ApplicationFiled: January 20, 2012Publication date: May 8, 2014Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
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Patent number: 8716527Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.Type: GrantFiled: March 4, 2009Date of Patent: May 6, 2014Assignee: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
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Patent number: 8716486Abstract: Methods of treating or suppressing oxidative stress disorders including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-heterocyclylaminoalkyl-(p-quinone) derivatives.Type: GrantFiled: June 23, 2009Date of Patent: May 6, 2014Assignee: Edison Pharmaceuticals, Inc.Inventors: Andrew W. Hinman, Orion D. Jankowski, Kieron E. Wesson
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Publication number: 20140121166Abstract: Provided are materials and methods for the prevention and treatment of Juvenile Neuronal Ceroid Lipofuscinosis comprising administration of an effective amount of at least one of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor. In some embodiments, the methods comprise administration of an effective amount of each of a hemi-channel inhibitor and a phosphodiesterase-4 inhibitor. Also provided are pharmaceutical compositions comprising a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor, as well as kits comprising at least one effective dose of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor or a combination of both.Type: ApplicationFiled: October 29, 2013Publication date: May 1, 2014Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKAInventor: Tammy Kielian
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Patent number: 8710234Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: GrantFiled: September 20, 2013Date of Patent: April 29, 2014Assignee: Mitsui Chemicals, Inc.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Patent number: 8710233Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.Type: GrantFiled: October 19, 2006Date of Patent: April 29, 2014Assignee: Gruenenthal GmbHInventors: Jeewoo Lee, Hyung Chul Ryu, Robert Frank, Gregor Bahrenberg, Jean De Vry, Thomas Christoph, Derek John Saunders, Klaus Schiene, Bernd Sundermann
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Publication number: 20140107160Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: ApplicationFiled: October 9, 2013Publication date: April 17, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
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Patent number: 8697733Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: June 20, 2013Date of Patent: April 15, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20140100227Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.Type: ApplicationFiled: September 10, 2013Publication date: April 10, 2014Applicant: REATA PHARMACEUTICALS, INC.Inventors: Christopher F. BENDER, Xin JIANG, Eric ANDERSON, Melean VISNICK
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Patent number: 8691847Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: September 12, 2012Date of Patent: April 8, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song
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Patent number: 8691852Abstract: The present disclosure relates to compounds of formula (I): or a pharmaceutically acceptable salt or N-oxide thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds of formula (I), and to their methods of use in therapy.Type: GrantFiled: August 6, 2012Date of Patent: April 8, 2014Assignee: Amirall, S.A.Inventors: Julio Cesar Castro Palomino Laria, Montserrat Erra Sola, Maria Estrella Lozoya Toribio, Eloisa Navarro Romero
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Publication number: 20140094455Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.Type: ApplicationFiled: August 19, 2013Publication date: April 3, 2014Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
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Patent number: 8686003Abstract: Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases.Type: GrantFiled: December 7, 2011Date of Patent: April 1, 2014Assignee: Sanford-Burnham Medical Research InstituteInventors: Jose Luis Millan, Eduard Sergienko
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Publication number: 20140088105Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: ApplicationFiled: November 22, 2013Publication date: March 27, 2014Applicant: NOVARTIS AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Patent number: 8680136Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.Type: GrantFiled: August 8, 2011Date of Patent: March 25, 2014Assignee: Rempex Pharmaceuticals, Inc.Inventors: Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
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Publication number: 20140080768Abstract: The invention generally relates to Pro-Drugs of dihydroorotate dehydrogenase (DHODH) inhibitors and methods of use thereof. In certain embodiments, the invention provides a DHODH inhibitor compound including a cleavable functional group that increases bioavailability as compared to a form of the DHODH inhibitor without the functional group, rendering the former more suitable for therapeutic use.Type: ApplicationFiled: September 19, 2012Publication date: March 20, 2014Inventors: Alan Palmer, Michael J. Hudson, Richard Todd, Patrick Camilleri
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Publication number: 20140080875Abstract: The invention relates to 3,4-diaminopyridine salts, pharmaceutical compositions containing at least one of said salts and uses thereof for the treatment of botulism, myasthenia, myasthenic syndromes or fatigue.Type: ApplicationFiled: November 20, 2013Publication date: March 20, 2014Applicant: ASSISTANCE PUBLIQUE-HOPITAUX DE PARISInventors: Francois GUYON, Dominique PRADEAU, My Dung LE HOANG, Jean-Jacques HOURI
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Patent number: 8673910Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in formula II: or a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: June 30, 2009Date of Patent: March 18, 2014Assignees: H. Lee Moffitt Cancer Center and Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Publication number: 20140073611Abstract: The disclosure relates to a platform of using zebrafish in screening candidates for treating and/or preventing myopia and keratoconus disease. The disclosure is mainly based on that Lumican, one of several SLRPs, plays an important role in the regulation of fibrillogenesis or the genes affecting the size of eyeballs in zebrafish, in addition to playing an important role in clinical myopia. Therefore, the disclosure uses the established zebrafish model to further identify the drugs affecting the expression of lumican and collagen fibrillogenesis, and/or the regulation of eyeball size. These drugs are potential candidates for treating myopia and/or keratoconus disease.Type: ApplicationFiled: May 21, 2013Publication date: March 13, 2014Applicant: National Taiwan UniversityInventors: I-Jong Wang, Wei-Ting Ho, Ting-Hsuan Chiang, I-Tsen Lin
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Patent number: 8669209Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.Type: GrantFiled: November 22, 2010Date of Patent: March 11, 2014Assignee: Dow AgroSciences, LLC.Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
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Publication number: 20140066410Abstract: This disclosure relates generally to compounds and compositions comprising one or more diphenylethylene, diphenylethylyne, and azobenzene analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory disease.Type: ApplicationFiled: February 23, 2012Publication date: March 6, 2014Applicant: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: Ming-Ming Zhou, Michael Ohlmeyer, Shiraz Mujtaba, Alexander Plotnikov, David Kastrinsky, Guangtao Zhang
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Patent number: 8663685Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.Type: GrantFiled: July 20, 2011Date of Patent: March 4, 2014Assignee: Acorda Therapeutics, Inc.Inventors: Andrew R. Blight, Ron Cohen
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Publication number: 20140051686Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: July 11, 2013Publication date: February 20, 2014Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Patent number: 8653086Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.Type: GrantFiled: October 21, 2009Date of Patent: February 18, 2014Assignee: Oregon Health & Science UniversityInventors: Xiangshu Xiao, Bingbing Li
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Patent number: 8648100Abstract: The invention relates to the use of Roflumilast, Roflumilast N-Oxide or a pharmaceutically acceptable salt of either for the treatment of pulmonary hypertension. The invention additionally relates to the use of Roflumilast, Roflumilast N-oxide or a pharmaceutically acceptable salt of either in combination with a PDE5 inhibitor or a pharmaceutically acceptable salt thereof for the treatment of pulmonary hypertension.Type: GrantFiled: April 12, 2006Date of Patent: February 11, 2014Assignee: Takeda GmbHInventors: Rolf Beume, Armin Hatzelmann, Degenhard Marx, Christian Schudt, Hermann Tenor, Saadia Eddahibi, Serge Adnot
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Patent number: 8648102Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.Type: GrantFiled: January 13, 2012Date of Patent: February 11, 2014Assignee: Board of Regents, The University of Texas SystemInventors: Waldemar Priebe, Nicholas Donato, Moshe Talpaz, Slawomir Szymanski, Izabela Fokt, Alexander Levitzki
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Publication number: 20140038948Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: June 25, 2013Publication date: February 6, 2014Applicant: Plexxikon Inc.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20140039015Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at about 12 hours and the use of the composition to treat various neurological diseases, including multiple sclerosis. A method of selecting individuals based on responsiveness to a treatment, including, for example, identifying individuals who responded to treatment with a sustained release fampridine composition.Type: ApplicationFiled: March 14, 2013Publication date: February 6, 2014Applicant: Acorda Therapeutics, Inc.Inventor: Acorda Therapeutics, Inc.
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Patent number: 8642624Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.Type: GrantFiled: November 15, 2011Date of Patent: February 4, 2014Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey A. Adams, Jean E. Bemis, Shon Booker, Guolin Cai, Lucian V. DiPietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael K. Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander S. Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian M. Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael D. Croghan
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Publication number: 20140031396Abstract: Dosage forms for oral administration of a PDE 4 inhibitor whose solubility is slight are described. They contain PVP binder.Type: ApplicationFiled: September 26, 2013Publication date: January 30, 2014Applicant: Takeda GmbHInventors: Rango Dietrich, Klaus Eistetter, Hartmut Ney
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Publication number: 20140031397Abstract: Dosage forms for oral administration of a PDE 4 inhibitor whose solubility is slight are described. They contain PVP as binder.Type: ApplicationFiled: September 26, 2013Publication date: January 30, 2014Applicant: Takeda GmbHInventors: Rango Dietrich, Klaus Eistetter, Hartmut Ney
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Publication number: 20140031348Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: July 9, 2013Publication date: January 30, 2014Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
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Publication number: 20140024608Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: March 14, 2013Publication date: January 23, 2014Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Publication number: 20140024621Abstract: The invention generally relates to aminopyridines and methods of use thereof. In certain embodiments, the invention provides an aminopyridine or a pharmaceutically-acceptable salt thereof, in which the aminopyridine or the salt thereof includes a cleavable functional group that substantially prevents extra-hepatic hydrolysis.Type: ApplicationFiled: July 23, 2012Publication date: January 23, 2014Applicant: MS THERAPEUTICS LIMITEDInventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
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Publication number: 20140024683Abstract: The present invention provides, inter alia, methods and pharmaceutical compositions for preventing, treating, or ameliorating the effects of a disease characterized by altered smooth muscle contractility, such as e.g., asthma and chronic obstructive pulmonary disease.Type: ApplicationFiled: September 24, 2013Publication date: January 23, 2014Inventors: Charles William EMALA, Peter YIM, George GALLOS, Donald LANDRY