Chalcogens Bonded Directly To At Least Two Ring Carbons Of The Six-membered Hetero Ring Patents (Class 514/348)
  • Patent number: 11458103
    Abstract: The invention is directed to pharmaceutical compositions such as tablets that exhibit delayed release properties when administered as either whole or half tablets. The invention is also directed to delayed release tablets comprising deferiprone for oral administration, for which twice daily administration is bioequivalent to the same daily dose of an immediate release tablet administered thrice daily. The invention is also directed to methods of making and using the same.
    Type: Grant
    Filed: December 13, 2019
    Date of Patent: October 4, 2022
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Bernard Charles Sherman, Michael Spino
  • Patent number: 11236090
    Abstract: A compound for inhibiting and degrading cyclin-dependent kinase (CDK) is disclosed. The compound is a substituted glutarimide represented by formula I. The compound can be used in the preparation of drugs for treating diseases related to the activity of the CDK.
    Type: Grant
    Filed: March 17, 2020
    Date of Patent: February 1, 2022
    Assignee: SHANGHAI MEIZER PHARMACEUTICALS CO., LTD.
    Inventor: Yongzhi Shu
  • Patent number: 11155561
    Abstract: A compound for inhibiting and degrading Bruton's tyrosine kinase (Btk) is disclosed. The compound is a substituted glutarimide represented by Formula I?. The compound can be used in the preparation of drugs for treating Btk activity-related diseases.
    Type: Grant
    Filed: March 3, 2020
    Date of Patent: October 26, 2021
    Assignee: SHANGHAI MEIZER PHARMACEUTICALS CO., LTD.
    Inventor: Yongzhi Shu
  • Patent number: 9636333
    Abstract: The present disclosure provides methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, including rheumatoid arthritis, having the structure of Formula (I): wherein R1, R2, R3, R4, R5 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: May 2, 2017
    Assignee: CONFLUENCE LIFE SCIENCES, INC.
    Inventors: Susan L. Hockerman, Joseph B. Monahan, Shaun R. Selness
  • Patent number: 9562019
    Abstract: The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: February 7, 2017
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Hakim Djaballah, Harold E. Varmus, David Shum, Romel Somwar, Alexander Chucholowski, Mohan Santhanam Thiruvazhi
  • Patent number: 9393236
    Abstract: The invention relates to the use of 4-cyclopropylmethoxy-N-(3,5-dichloro-1-oxidopyridin-4-yl)-5-(methoxy)pyridine-2-carboxamide for the preparation of a medicament for use in the treatment of cerebral traumas.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: July 19, 2016
    Assignee: SANOFI
    Inventors: Philippe Delay-Goyet, Corinne Perron
  • Patent number: 9365547
    Abstract: The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, X and Y are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: June 14, 2016
    Assignee: CONFLUENCE LIFE SCIENCES INC.
    Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas
  • Patent number: 9365546
    Abstract: The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, X and Y are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: June 14, 2016
    Assignee: CONFLUENCE LIFE SCIENCES INC.
    Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas
  • Patent number: 9359300
    Abstract: The present disclosure provides methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: June 7, 2016
    Assignee: CONFLUENCE LIFE SCIENCES, INC.
    Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas, Susan L. Hockerman
  • Patent number: 9278930
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: February 22, 2015
    Date of Patent: March 8, 2016
    Assignee: AERPIO THERAPEUTICS, INC.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Patent number: 9247742
    Abstract: A synergistic fungicidal mixture contains a fungicidally effective amount of a compound of Formula I and at least one fungicide selected from the group consisting of tricyclazole, azoxystrobin, carpropamid, probenazole, kasugamycin, and boscalid.
    Type: Grant
    Filed: December 28, 2013
    Date of Patent: February 2, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: David Ouimette, Richard K. Mann, John Todd Mathieson, Olavo Correa da Silva
  • Patent number: 9115089
    Abstract: The present disclosure provides methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, including rheumatoid arthritis, having the structure of Formula (I): wherein R1, R2, R3, R4, R5 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: August 25, 2015
    Assignee: CONFLUENCE LIFE SCIENCES, INC.
    Inventors: Susan L. Hockerman, Joseph B. Monahan, Shaun R. Selness
  • Patent number: 9073865
    Abstract: Provided are compounds of Formula I which are derivatives of 3-Hydroxypyridin-4-ones. The compounds may be used in treatment of a medical condition related to a toxic concentration of iron. The compounds may be used for preparation of a medicament for treatment of a medical condition related to a toxic concentration of iron. The medical condition related to a toxic concentration of iron may be selected from the group consisting of: cancer, pulmonary disease, progressive kidney disease and Frederich's Ataxia.
    Type: Grant
    Filed: July 5, 2010
    Date of Patent: July 7, 2015
    Assignee: Apotex Technologies Inc.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Birenkumar Shah, Blaise N'Zemba, Jolanta Maria Wodzinska, Maryna Premyslova
  • Patent number: 9056110
    Abstract: The present disclosure provides pyrimidinone-phenyl-pyrimidinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4 and R5 are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: June 16, 2015
    Assignee: CONFLUENCE LIFE SCIENCES, INC.
    Inventors: Shaun R. Selness, Balekudru Devadas, Susan L. Hockerman, Joseph B. Monahan
  • 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
  • Patent number: 9024032
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 5, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
  • Publication number: 20150094310
    Abstract: The present invention relates to a corticotropin releasing hormone receptor type 1 (CRHR1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. patients having corticotropin releasing hormone (CRH) overactivity.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventor: Florian Holsboer
  • Publication number: 20150079161
    Abstract: The present invention features methods for stimulating clearance of misfolded or aggregated proteins or peptides in microglia or neurons, and treating neurodegenerative diseases associated with such pathology in brain by selectively inhibiting the expression or activity of Acyl-CoA:Cholesterol Acyltransferase 1, but not Acyl-CoA:Cholesterol Acyltransferase 2.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 19, 2015
    Inventors: Ta-Yuan Chang, Catherine C.Y. Chang, Yohei Shibuya, Zhaoyang Niu
  • Publication number: 20150080362
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 19, 2015
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Tamil Arasu, John David Baird, Wu Du, Olya Ginzburg, Yi Jin Kim Gorske, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Anthony Allan Turpoff, Richard Gerald Wilde, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
  • Patent number: 8962661
    Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: February 24, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Akihiro Nishimura
  • 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
  • Patent number: 8933079
    Abstract: Pyridone and pyridazinone derivatives that are active against the melanin-concentrating hormone (MCH) and useful as anti-obesity pharmaceuticals.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: January 13, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Oost, Ralf Lotz, Dirk Stenkamp
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140336165
    Abstract: Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain.
    Type: Application
    Filed: November 14, 2012
    Publication date: November 13, 2014
    Inventors: Takeshi Hondo, Keita Nakanishi, Tatsuya Niimi, Masaichi Warizaya, Ichiji Namatame, Katsuya Harada
  • Patent number: 8883774
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: November 11, 2014
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Publication number: 20140314676
    Abstract: The current application is directed to methods of treating or ameliorating myocardial ischemia, an acute coronary event, and a myocardial reperfusion injury comprising administering a therapeutically effective amount of deferiprone or a pharmaceutically acceptable salt thereof to a patient in need thereof. The application is also directed to reducing the risk for myocardial reperfusion injury as well as promoting the beneficial remodeling of cardiac tissue in a patient, comprising administering a therapeutically effective amount of deferiprone or a pharmaceutically acceptable salt thereof to a patient before, during or after reperfusion therapy. The application also includes methods of selecting a patient for treatment of reperfusion injury and subsequently treating the selected patient.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 23, 2014
    Inventors: Michael Spino, John Chalmers Connelly, John Charles Wood, Graham Arnold Wright, Nilesh Ramesh Ghugre
  • Publication number: 20140308340
    Abstract: The present invention features methods for stimulating clearance of misfolded or aggregated proteins or peptides in microglia, and treating neurodegenerative diseases associated with such pathology in brain by selectively inhibiting the expression or activity of Acyl-CoA:Cholesterol Acyltransferase 1, but not Acyl-CoA:Cholesterol Acyltransferase 2.
    Type: Application
    Filed: May 29, 2014
    Publication date: October 16, 2014
    Applicant: Trustees of Dartmouth College
    Inventors: Ta-Yuan Chang, Catherine C.Y. Chang, Yohei Shibuya, Zhaoyang Niu
  • Patent number: 8859573
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: October 14, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Publication number: 20140288017
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20140243353
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or fluorine, one of A and B is R2, the other is a group —X—Y—R3. R3 represents a carbocyclic or heterocyclic ring. Further variables are as defined in the specification. Also claimed are—processes for their preparation, pharmaceutical compositions containing them and their use in therapy of diseases such as schizophrenia, cognitive disorders and pain by modulating the D-amino acid oxidase enzyme (DAAO).
    Type: Application
    Filed: July 5, 2012
    Publication date: August 28, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: William Farnaby, Charlotte Fieldhouse, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller, Katherine Hazel
  • Publication number: 20140235673
    Abstract: The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Inventors: Zulan Pi, John Llyod, Jennifer X. Qiao, Tammy C. Wang, George O. Tora
  • Patent number: 8809373
    Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: August 19, 2014
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
  • Publication number: 20140228310
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 14, 2014
    Applicant: InterMune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Publication number: 20140213589
    Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Alexis DENIS, Vincent Gerusz, Yannick Bonvin
  • Publication number: 20140200205
    Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
    Type: Application
    Filed: September 17, 2012
    Publication date: July 17, 2014
    Inventors: Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
  • Publication number: 20140163024
    Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 10, 2013
    Publication date: June 12, 2014
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Patent number: 8716318
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: May 6, 2014
    Assignee: Ardea Biosciences
    Inventors: Shunqi Yan, Jean-Michel Vernier, Zhi Hong, Suetying Chow, Yung-hyo Koh
  • Publication number: 20140113008
    Abstract: The invention is directed to methods for diagnosing reperfusion/non-reperfusion hemorrhage and predicting cardiac arrhythmias and sudden cardiac death in subjects comprising using imaging techniques to detect regional iron oxide deposition. The invention also provides treatment methods for subject at increased risk of sudden cardiac death.
    Type: Application
    Filed: June 13, 2012
    Publication date: April 24, 2014
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Rohan Dharmakumar, Ivan Cokic
  • Patent number: 8686155
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Patent number: 8685955
    Abstract: Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety. The neuroprotective function is imparted to the compound, e.g., by a neuroprotective peptide. A combined antiapoptotic and neuroprotective function is provided by a propargyl group.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: April 1, 2014
    Assignees: Technion Research and Development Foundation Ltd., Yeda Research and Development Co. Ltd.
    Inventors: Moussa B. H. Youdim, Matitiyahu Fridkin, Hailin Zheng, Rivka Warshawsky
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Patent number: 8673943
    Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: March 18, 2014
    Assignee: Apotex Technologies Inc.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao
  • Publication number: 20140073685
    Abstract: Provided are methods for treating a NAD comprising administering to a patient suffering from a NAD a composition comprising an eIF5A inhibitor compound in an amount effective to prevent intracellular hypusination of eIF5A, whereby gene expression of NMD-susceptible mRNA is increased.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 13, 2014
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Tsafi Pe'ery, Michael B. Mathews, Mainul Hoque, Hartmut M. Hanauske-Abel
  • Publication number: 20140038980
    Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: October 1, 2013
    Publication date: February 6, 2014
    Inventors: Alan D. Snow, Beth Nguyen, Gerardo Castillo, Virginia Sanders, Thomas Lake
  • Publication number: 20140031370
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: 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
  • Publication number: 20140031395
    Abstract: 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: Application
    Filed: February 2, 2012
    Publication date: January 30, 2014
    Applicant: Bionomics Limited
    Inventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
  • Patent number: 8603814
    Abstract: Provided are methods for treating a NAD comprising administering to a patient suffering from a NAD a composition comprising an eIF5A inhibitor compound in an amount effective to prevent intracellular hypusination of eIF5A, whereby gene expression of NMD-susceptible mRNA is increased.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: December 10, 2013
    Assignee: Rutgers the State University of New Jersey
    Inventors: Tsafi Pe'ery, Michael B. Mathews, Mainul Hogue, Hartmut Martin Hanauske-Abel
  • Publication number: 20130310346
    Abstract: The present invention provides methods and compositions for treating or preventing bacterial infections, where a pharmaceutically acceptable iron chelator that reduces biological availability of iron for one or more strains of bacteria, such as VK28 or an analog or derivative thereof is administered to a patient in need of treatment. The method also provides methods and compositions where an iron chelator and an antibiotic are administered to a patient in need of treatment for a bacterial infection.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: Government of the United States, as represented by the Secretary of the Army
    Inventor: Daniel Zurawski
  • Publication number: 20130267546
    Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 10, 2013
    Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of Ari
    Inventors: Sidney HECHT, Omar KHDOUR, Jun LU, Pablo ARCE