Chalcogen Double Bonded Directly To A Ring Carbon Of The Four-membered Hetero Ring Which Is Adjacent To The Ring Nitrogen Patents (Class 514/210.02)
  • Patent number: 10309937
    Abstract: Provided is a method for detecting impurities in ammonium hydroxide. The method for detecting impurities in ammonium hydroxide includes preparing a potassium permanganate solution, preparing ammonium hydroxide, and adding the potassium permanganate solution several times to the ammonium hydroxide so as to detect impurities in the ammonium hydroxide. Potassium permanganate contained in the potassium permanganate solution is added for each time in the range of 0.0001 mol to 0.01 mol per 1 g of ammonia contained in the ammonium hydroxide.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: June 4, 2019
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Kihyun Kim, Sooyeon Kim, JungDae Park, Min Soo Suh, Hyang Bong Lee, Kwangshin Lim
  • Patent number: 10196394
    Abstract: Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: February 5, 2019
    Assignee: OPKO Health, Inc.
    Inventors: Mengwei Hu, Sunil Paliwal, Neng-Yang Shih, Frank Bruno Guenter, Ingrid Mergelsberg
  • Patent number: 10195179
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: February 5, 2019
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Patent number: 10188654
    Abstract: Disclosed are methods of treating cancer, which include administering a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, to a subject in need thereof. Also disclosed are methods of inhibiting growth and proliferation of cancer cells in vitro or in vivo, which include contacting the cells with an amount of the compound of formula (I) effective to inhibit the growth or proliferation of the cancer cells. Further disclosed are methods of inhibiting tumor growth, which include contacting the tumor with an amount of the compound of formula (I) effective to inhibit the growth of the tumor.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: January 29, 2019
    Assignee: Asana BioSciences, LLC
    Inventors: Sanjeeva P. Reddy, Sandeep Gupta, Roger Astbury Smith
  • Patent number: 10155753
    Abstract: Disclosed are 4-substituted-2-(5-substituted-1H-indol-2-yl)phenol derivatives for controlling the proliferation and migration of kinase-overexpressed cells. The phenol derivatives are represented by Formula 1: wherein X is selected from the group consisting of hydrogen, halogen, a cyano group, a trifluoromethyl (CF3) group, an amidine (C(?NH)NH2) group, and a 5-methyl-1,2,4-oxadiazole group, Y is selected from the group consisting of hydrogen, halogen, a phenyl group substituted with one or two substituents selected from the group consisting of halogen, methoxy, nitro, trifluoromethyl, and aminomethyl, CO—R?, COOR?, OH, O—R?, and NH—R?, each R? is independently selected from the group consisting of C1-C18 alkyl, alkenyl, alkynyl, and —Z-alkyl (wherein Z is a heteroatom selected from the group consisting of O, S, and N or is —(CH2)m—), and m is an integer from 0 to 5.
    Type: Grant
    Filed: October 17, 2016
    Date of Patent: December 18, 2018
    Assignees: Korea University Research and Business Foundation, Dongguk University Industry-Academic Cooperation Foundation
    Inventors: Youngjoo Byun, Chang Hoon Lee
  • Patent number: 9994614
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: June 12, 2018
    Assignee: Naurex, Inc.
    Inventor: M. Amin Khan
  • Patent number: 9987265
    Abstract: Compounds and compositions are described herein for treating post traumatic stress disorder.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: June 5, 2018
    Assignee: AZEVAN PHARMACEUTICALS, INC.
    Inventor: Michael J. Brownstein
  • Patent number: 9974757
    Abstract: The invention relates to a method of treating or preventing a condition in a subject, comprising administering to the subject an acceptable composition comprising meglumine or a salt thereof. The invention further relates to a method of improving a physiological function in a subject, comprising administering to the subject an acceptable composition comprising meglumine or a salt thereof.
    Type: Grant
    Filed: January 24, 2017
    Date of Patent: May 22, 2018
    Assignee: Dynamics Therapeutics, Inc.
    Inventor: Annette Tobia
  • Patent number: 9925169
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: March 27, 2018
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Patent number: 9845302
    Abstract: The invention disclosed herein relates to novel Peribysin E analogs of general formula-I. Further the invention provides simple, economical and short synthesis of Peribysin E and its analogs of Formula I, in good yield and purity leading to the identification of more potent cell adhesion inhibitors.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: December 19, 2017
    Assignee: Council of Scientific and Industrial Research
    Inventors: Dumbala Srinivasa Reddy, Kishor Laxman Handore
  • Patent number: 9797938
    Abstract: Functionality for estimating characteristics of an on-chip noise signal can be implemented on a processing module. An on-chip noise signal is determined at an on-chip determination point of a computer chip. The on-chip noise signal is converted to a frequency-varying signal using a voltage-controlled oscillator implemented on the computer chip. The frequency-varying signal is measured at an off-chip measurement point and frequency information is extracted from the frequency-varying signal. The frequency information is converted to a voltage level associated with the on-chip noise signal based on the relationship between an input voltage provided to the voltage-controlled oscillator and an output frequency generated by the voltage-controlled oscillator.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: October 24, 2017
    Assignee: International Business Machines Corporation
    Inventors: Jose A. Hejase, Nanju Na, Nam H. Pham, Lloyd A. Walls
  • Patent number: 9701860
    Abstract: This invention discloses a radiation curable barrier coating composition for application to paper or paperboard substrates that can be applied using a conventional flexographic printing process. The coating composition includes one or more hydrophobic cycloaliphatic radiation curable monomers, one or more alcohol-functional waxes or sterols, and one or more other hydrophobic wax materials. The incorporation of these materials together lowers the MVTR of the coating compared to other radiation curable compositions while also generating improved, higher gloss. This invention also discloses a method to manufacture the coating composition and a preferred method to print the coating composition.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: July 11, 2017
    Assignee: Sun Chemical Corporation
    Inventor: Carl Weisbecker
  • Patent number: 9693984
    Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.
    Type: Grant
    Filed: January 18, 2017
    Date of Patent: July 4, 2017
    Assignee: AMARIN PHARMACEUTICALS IRELAND LIMITED
    Inventor: Paresh Soni
  • Patent number: 9623001
    Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: April 18, 2017
    Assignee: AMARIN PHARMACEUTICALS IRELAND LIMITED
    Inventor: Paresh Soni
  • Patent number: 9610272
    Abstract: In various embodiments, the present invention provides methods of reducing the risk of a cardiovascular event in a subject on statin therapy and, in particular, a method of reducing the risk of a cardiovascular event in a subject on statin therapy having a fasting baseline triglyceride level of about 135 mg/dL to about 500 mg/dL, and administering to the subject a pharmaceutical composition comprising about 1 g to about 4 g of eicosapentaenoic acid ethyl ester or a derivative thereof.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: April 4, 2017
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventor: Paresh Soni
  • Patent number: 9399636
    Abstract: The present invention provides for compounds of Formula I and various embodiments thereof, and compositions comprising compounds of Formula I and various embodiments thereof. In compounds of Formula I, the groups R1, R2, R3, R4, R5, R6, m, n and the C-linked Ring have the meaning as described herein. The present invention also provides for methods of using compounds of Formula I and compositions comprising compounds of Formula I as DLK inhibitors and for treating neurodegeneration diseases and disorders.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: July 26, 2016
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Malcolm Huestis, Cuong Ly, Snahel Patel, Michael Siu, Xianrui Zhao
  • Patent number: 9376401
    Abstract: The invention in this document is related to the field of preparation of 1,3-(substituted-diaryl)-1,2,4-triazoles and certain intermediates derived therefrom, where said intermediates are useful in the preparation of certain pesticides disclosed in U.S. Pat. No. 8,178,658.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: June 28, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Natalie C. Giampietro, Gary D. Crouse
  • Patent number: 9353089
    Abstract: The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: May 31, 2016
    Assignees: Saint Louis University, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences
    Inventors: Xiaoping Chen, Ke Ding, Marvin J. Meyers, Micky D. Tortorella, Jing Xu
  • Patent number: 9198890
    Abstract: The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: December 1, 2015
    Assignee: Boston Heart Diagnostics Corporation
    Inventors: Ernst J. Schaefer, Eliana Polisecki
  • Patent number: 9174988
    Abstract: The invention provides derivatives and analogs of triazatetracyclo[7.7.0.01,13.02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6.012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: November 3, 2015
    Assignees: TRUSTEES OF BOSTON UNIVERSITY, THE SCRIPPS RESEARCH INSTITUTE
    Inventors: John K. Snyder, Wanguo Wei, Feng Ni, Arthur Donny Strosberg, Eliane Leuwenkroon, Smitha Kota, Virginia Ngocthanh Takahashi
  • Patent number: 9090586
    Abstract: The present invention provides a compound represented by the formula (1): wherein each symbol is as defined in the specification, or a salt thereof, a prodrug of the compound or a salt thereof, a medicament containing the compound or a salt thereof, the medicament which is a phosphodiesterase 10A inhibitor, and a medicament which is for preventing or treating schizophrenia.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: July 28, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masato Yoshikawa, Shinkichi Suzuki, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo, Haruhi Kamisaki, Takahiko Taniguchi
  • Patent number: 9072735
    Abstract: A proteinase therapy has been invented to eliminate solid tumors by destroying tumors' solid structure and killing cancer cells by cleaving vital extracellular matrix proteins C-terminally, N-terminally or both with cell membrane intact and limited adverse effects. The micro-scale intratumoral proteinase K therapy is tumor specific but not cancer type specific. Proteinase K therapy can be operated on multiple tumors on multiple occasions, if necessary. It may be employed to eliminate any solid tumor to prolong a cancer patient's life span.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: July 7, 2015
    Inventor: Yong Qian
  • Patent number: 9045399
    Abstract: An aromatic organic solvent solution of a methanesulfonic acid alkyl ester having high thermal stability is obtained by reacting an alkyl alcohol with methanesulfonyl chloride in an aromatic organic solvent in the presence of a tertiary amine, and washing the resulting aromatic organic solvent solution of a crude methanesulfonic acid alkyl ester with an aqueous alkali metal carbonate solution. The washing is performed using the aqueous alkali metal carbonate solution having a concentration of 1 to 3 mass % in an amount of 4 to 6 parts by mass per 1 part by mass of the alkyl alcohol.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: June 2, 2015
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Shinobu Maruno, Koichi Nakazawa
  • Patent number: 9034863
    Abstract: The present invention embraces Niemann-Pick C1-like 1 protein antagonists and agents that inhibit hepatic virus infection for use in the prevention and treatment of a hepatic virus infection.
    Type: Grant
    Filed: March 19, 2013
    Date of Patent: May 19, 2015
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Susan L. Uprichard, Bruno Sainz, Jr.
  • Publication number: 20150133422
    Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
  • Publication number: 20150126371
    Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 7, 2015
    Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
  • Publication number: 20150119368
    Abstract: A composition and a method of treatment for the reduction of risk factors for cardiovascular disease utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught.
    Type: Application
    Filed: January 2, 2015
    Publication date: April 30, 2015
    Applicant: PIVOTAL THERAPEUTICS INC.
    Inventors: George JACKOWSKI, Rachelle MACSWEENEY, Nisar Ahmad SHAIKH, Jason YANTHA, Valerie B. SCHINI-KERTH
  • Publication number: 20150111865
    Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 23, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Jun Takeuchi, Masahiro Ikura, Masato Higashino, Maki Iwahashi, Kazuya Hashimura
  • Publication number: 20150105365
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7 R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150105364
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Application
    Filed: October 10, 2013
    Publication date: April 16, 2015
    Applicant: Northwestern University
    Inventors: M. Amin Khan, Joseph Moskal, Paul Wood
  • Publication number: 20150056274
    Abstract: Compositions, methods, and kits useful for treating hyperlipidemic conditions are provided herein. Such compositions can contain synergizing amounts of nicotinic acid, nicotinamide riboside and/or nicotinic acid metabolites in combination with leucine and/or a leucine metabolite, with or without resveratrol.
    Type: Application
    Filed: August 28, 2014
    Publication date: February 26, 2015
    Inventors: Michael Zemel, Antje Bruckbauer
  • Patent number: 8952000
    Abstract: A composition and a method of treatment utilizing a combination of lipid lowering cholesterol absorption inhibitors, e.g. azetidinones, with mixtures of an omega-3 fatty acid formulation containing about 90% or more omega 3 fatty acids by weight including a combination of Eicosapentaenoic acid (EPA), Docosapentaenoic acid (DPA) and Docosahexaenoic acid (DHA) in a weight ratio of EPA:DHA of from 5.7 to 6.3, wherein the sum of the EPA, DHA and DPA represent about 82% by weight of the total formulation and about 92% of the total omega 3 fatty acid content of the composition are taught. EPA+DHA are about 80% of the total formulation and about 89% of the total omega 3 fatty acid content of the composition. The formulation may further contain specific amounts of arachidonic acid (AA), stearidonic acid (SDA), and alpha-linolenic acid (ALA).
    Type: Grant
    Filed: August 13, 2012
    Date of Patent: February 10, 2015
    Assignee: Pivotal Therapeutics Inc.
    Inventors: George Jackowski, Rachelle MacSweeney, Nisar Shaikh, Jason Yantha, Valerie Schini-Kerth
  • Patent number: 8940724
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: January 27, 2015
    Assignee: Amgen Inc.
    Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez de Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
  • Publication number: 20150018329
    Abstract: The present invention relates to pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said pyrazolo[1,5-a][1,3,5]triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors for a protein kinase.
    Type: Application
    Filed: March 1, 2013
    Publication date: January 15, 2015
    Applicant: LEAD DISCOVERY CENTER GMBH
    Inventors: Jan Eickhoff, Gunther Zischinsky, Uwe Koch
  • Publication number: 20150011525
    Abstract: A stable ternary solid dispersion composition with enhanced physical stability and/or bioavailability comprising: (a) about 1% wt. to about 50% wt. of one or more poorly soluble active pharmaceutical ingredient (API) which belongs to Biopharmaceutics Classification System (BCS) class II and/or IV; (b) about 11% wt. to about 50% wt. of at least one water-soluble polymer; and (c) about 20% wt. to about 99% wt. of crosslinked polyvinylpyrrolidone (crospovidone, a water-insoluble polymer). The solid dispersion is capable of inhibiting crystallization of API in solid state and/or aqueous gastrointestinal tract (GIT) medium. Also disclosed is a method of preparation of such solid dispersion composition by fusion or solvent or fusion-solvent method.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 8, 2015
    Applicant: ISP Investments Inc.
    Inventors: Yunxia Bi, Mohammed Abdul Rahman, James David Lester
  • Patent number: 8927533
    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: Grant
    Filed: September 17, 2012
    Date of Patent: January 6, 2015
    Assignee: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
  • Patent number: 8927021
    Abstract: The present invention relates to a process for manufacturing microcrystalline ezetimibe containing granulate, wherein a) ezetimibe is dissolved; b) the dissolved ezetimibe is precipitated with water, which if necessary contains pharmaceutical excipients, preferably lauryl-sulfate derivatives, and c) granulates are formed from the obtained suspension by spraying the suspension onto pharmaceutical excipients. A further aspect of the present invention is the granulate obtained by the present process and the pharmaceutical composition containing such granulate.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: January 6, 2015
    Assignee: Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszventarsasag
    Inventors: Zoltan Toelgyesi, Zsolt Zsigmond, Gyoergy Ujfalussy, Magdolna Leventiszne Huszar, Peter Tonka-Nagy, Monika Agyagos
  • Publication number: 20150005232
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 1, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
  • Patent number: 8921352
    Abstract: The present invention relates to the field of pharmaceutical technology and in particular to novel dosage forms of medicaments containing as active ingredients simvastatin and ezetimibe, or pharmaceutically acceptable salts thereof. The present pharmaceutical compositions are characterized in that the contact of the compositions with oxygen is substantially reduced, such as by coating the composition, providing a medicament useful for the treatment and prevention of atherosclerosis and related conditions, in an environment having an essentially reduced oxygen or humidity, respectively, content.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: December 30, 2014
    Assignee: KRKA
    Inventors: Vesna Kroselj, Renata Lakse, Rebeka Toporisic, Joze Kastelic
  • Patent number: 8889663
    Abstract: The invention relates to a formulation for delivering by oral transmucosal administration at least one lipid-lowering active principle, preferably from the statin family, said formulation including said active principle in the base or salt form, an aqueous alcohol solution titrating at least 30° alcohol, and optionally a pH correcting agent and/or an antioxidant, said active principle being in a stable and completely dissolved state in the aqueous alcohol solution. The invention also relates to a method of preparing said formulation and to the use thereof, preferably in single-dose packaging, for treating and preventing hyperlipemia and/or cardiovascular conditions.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: November 18, 2014
    Inventors: Philippe Perovitch, Marc Maury
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Publication number: 20140315876
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 12, 2014
    Publication date: October 23, 2014
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20140296196
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Publication number: 20140287042
    Abstract: The present invention is an orally consumed fixed combination formulation of both rosuvastatin and ezetimibe in one tablet that is expected to have the same Area Under Curve as two active ingredients taken together individually orally, and pharmaceutically acceptable additives suitable for the preparation. In preferred embodiments of this invention, the rosuvastatin is in the form of rosuvastatin calcium and the pharmaceutically acceptable additives are selected from diluents, disintegrants, glidants, lubric ants, colorants and combinations thereof.
    Type: Application
    Filed: May 1, 2013
    Publication date: September 25, 2014
    Inventor: Marie Charmaine Dias
  • Publication number: 20140275004
    Abstract: Disclosed are compound of Formula (Ia), wherein R1, R2, and R3 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Andrew J. Souers, Rajeev Goswami
  • Publication number: 20140243302
    Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 28, 2014
    Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
  • Publication number: 20140235607
    Abstract: The invention pertains to a method of determining a statin dosage for an individual in need of treatment with a statin, comprising determining a SLCO1B1 genotype from a nucleic acid sample of the individual, said genotype comprising the presence or absence of the SLCO1B1-056 polymorphism, and determining an ApoE genotype or phenotype identifying an ApoE polymorphism selected from the group consisting of ApoE2, ApoE3, ApoE4, and any combination thereof, wherein the combination of a SLCO1B1 genotype identifying the presence of the SLCO1B1-056 C polymorphism and the ApoE genotype or phenotype identifying one of the ApoE3/4 or ApoE4/4 genotypes indicates the statin dosage.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: BOSTON HEART DIAGNOSTICS CORPORATION
    Inventors: Ernst J. Schaefer, Eliana Polisecki
  • Publication number: 20140235605
    Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 21, 2014
    Applicant: CELERA CORPORATION
    Inventor: CELERA CORPORATION
  • Patent number: 8809315
    Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: August 19, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Eric Desarbre, Malcolm G. P. Page