Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
  • Patent number: 8835449
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: September 16, 2014
    Assignee: Pfizer Inc.
    Inventors: Edward L. Conn, David Hepworth, Roger B. Ruggeri
  • Publication number: 20140256757
    Abstract: Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof in combination with metformin and in combination with pioglitazone.
    Type: Application
    Filed: May 19, 2014
    Publication date: September 11, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Ronald J. Christopher, Paul Covington
  • Publication number: 20140255348
    Abstract: A pharmaceutical combination comprising a topoisomerase I inhibitor, and an Hsp90 inhibitor according to the following formulae (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 11, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventor: David Proia
  • Publication number: 20140255426
    Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing a viral infection comprising administering an effective amount of a Wnt pathway inhibitor optionally in combination with one or more anti-viral agents. In certain embodiments, the subject is diagnosed with a chronic viral infection such as human immunodeficiency virus (HIV).
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicants: EMORY UNIVERSITY, Children's Healthcare of Atlanta, Inc., The General Hospital Corporation
    Inventors: Guido Silvestri, Ann M. Chahroudi, Mathias Lichterfeld, Maria Jose Buzon, Raymond F. Schinazi
  • Publication number: 20140248378
    Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 4, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
  • Publication number: 20140249127
    Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: February 14, 2014
    Publication date: September 4, 2014
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
  • Publication number: 20140248268
    Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.
    Type: Application
    Filed: May 15, 2014
    Publication date: September 4, 2014
    Inventors: Angela Wandinger-Ness, Larry Sklar, Jacob Agola, Zurab Surviladze, Jeffrey Aube, Jennifer Golden, Chad E. Schroeder, Denise S. Simpson
  • Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • Publication number: 20140249134
    Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
  • Publication number: 20140249100
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: March 3, 2013
    Publication date: September 4, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz Shalwitz, Kevin Gene Peters
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Publication number: 20140243310
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: October 23, 2012
    Publication date: August 28, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tohru Yamashita, Takuya Fujimoto, Ryo Mizojiri, Kazuko Yonemori, Hideki Hirose, Zenichi Ikeda, Ikuo Fujimori, Kyoko Toyofuku, Tsuneo Yasuma, Nobuyuki Matsunaga
  • Publication number: 20140242063
    Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.
    Type: Application
    Filed: October 10, 2013
    Publication date: August 28, 2014
    Applicant: VALEANT LABORATORIES INTERNATIONAL BERMUDA
    Inventors: Andrew John DUFFIELD, Graham JACKSON, Steven E. FRISBEE
  • Patent number: 8815884
    Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: August 26, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
  • Publication number: 20140235582
    Abstract: Compounds of Formula (I) wherein B is selected from the group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl; Y is a linker moiety selected from the group consisting of a direct bond. R, R1, R2, and R3 are each individually selected from the group consisting substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or heterocycle.
    Type: Application
    Filed: August 27, 2012
    Publication date: August 21, 2014
    Applicants: Sanford-Burnham Medical Research Institute, Southern Research Institute
    Inventors: Marintha L. Heil, Nicholas D.P. Cosford, Nicholas Pagano, Peter Teriete
  • Publication number: 20140234295
    Abstract: Provided herein is a pharmaceutical composition comprising at least one isoflavonoid. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions.
    Type: Application
    Filed: November 1, 2011
    Publication date: August 21, 2014
    Applicant: MARSHALL EDWARDS, INC.
    Inventors: George Jeoffreys, Alison Johnson, Andrew Heaton, Ofir Moreno
  • Publication number: 20140234254
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: February 15, 2014
    Publication date: August 21, 2014
    Applicants: SUNSHINE LAKE PHARMA CO., LTD., CALITOR SCIENCES, LLC
    Inventor: Ning Xi
  • Publication number: 20140235640
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20140235661
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Application
    Filed: April 24, 2014
    Publication date: August 21, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Kai GERLACH, Riccardo GIOVANNINI, Christoph HOENKE, Rocco MAZZAFERRO, Marco SANTAGOSTINO, Stefan SCHEUERER, Christofer TAUTERMANN, Thomas TRIESELMANN
  • Publication number: 20140235638
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 21, 2014
    Applicant: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140234245
    Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
    Type: Application
    Filed: November 5, 2012
    Publication date: August 21, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Cédric Poinsard
  • Publication number: 20140234410
    Abstract: A pharmaceutical formulation comprises a plurality of seamless minicapsules having a diameter from 0.5 mm to 5 mm, at least some of the minicapsules containing a methyxanthine as one active ingredient, and at least some of the minicapsules containing a corticosteroid as another active ingredient.
    Type: Application
    Filed: April 23, 2014
    Publication date: August 21, 2014
    Applicant: SIGMOID PHARMA LTD.
    Inventors: Joey Moodley, Ivan Coulter
  • Publication number: 20140235659
    Abstract: Methods are disclosed for treating neoplastic disorders, such as pancreatic cancer, using tocotrienols; namely, gamma-tocotrienol and delta tocotrienol. The antitumorogenic effects of these compounds are shown both in vitro and in vivo using several human pancreatic cancer cell lines and MIA-PACA2 human pancreatic cancer cells xenografted in nude mice. Also disclosed are methods of testing the efficacy of potential chemotherapeutic agents by measuring their effect on surrogate endpoint biomarkers, such as Ki-67 and p27. Associated compounds are also disclosed.
    Type: Application
    Filed: October 16, 2012
    Publication date: August 21, 2014
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventor: UNIVERSITY OF SOUTH FLORIDA
  • Publication number: 20140235660
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
  • Publication number: 20140234415
    Abstract: The present invention features tablet dosage forms comprising two or more different active ingredients. In one embodiment, a tablet dosage form of the invention comprises a first layer and a second layer, wherein the first layer comprises polymer-based solid dispersion particles having a mean particle size of no more than 200 ?m.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Inventors: Todd S. McDermott, Peter T. Mayer, Benjamin M. Collman, Weili Wang, Bei Chen
  • Patent number: 8809562
    Abstract: Metallocene compounds and pharmaceutical compositions containing these metallocene compounds are disclosed and described. Methods of treating cancer employing such metallocene compounds and pharmaceutical compositions also are provided.
    Type: Grant
    Filed: June 5, 2012
    Date of Patent: August 19, 2014
    Assignee: Chevron Phillips Chemical Company LP
    Inventors: Mark L. Hlavinka, Qing Yang, Mandi Michelle Murph
  • Patent number: 8809357
    Abstract: The present invention relates to compounds of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer; methods of preparation of the same; and methods of counducting drug discovery and research by applying the same in an investigation.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: August 19, 2014
    Inventor: Zhen Huang
  • Publication number: 20140227373
    Abstract: A method of improving longevity and/or alleviating a symptom of aging or preventing age related diseases is provided. The method includes a step in which the subject's average and type of daily protein intake, IGF-I, and IGFBP1 levels, and risk factors for overall mortality, cancer and diabetes are determined. With respect to protein consumption, the relative amounts of protein calories from animal and plant sources are determined. A periodic normal calorie or low calorie but low protein fasting mimicking diet with frequencies of every 2 weeks to 2 months is provided to the subject if the subject's average daily protein intake level and type and/or IGF-I levels, and/or IGFBP1 levels is identified as being greater or lower than a predetermined cutoff intake/level and if the subject is younger than a predetermined age. The method is also shown to alleviate symptoms of chemotoxicity.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Inventors: Valter D. LONGO, Sebastian BRANDHORST, Morgan Elyse LEVINE
  • Publication number: 20140227302
    Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: September 4, 2012
    Publication date: August 14, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett
  • Publication number: 20140227260
    Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 21, 2014
    Publication date: August 14, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventor: Chengzhi Zhang
  • Publication number: 20140228368
    Abstract: The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: August 20, 2012
    Publication date: August 14, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
  • Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Patent number: 8802736
    Abstract: The present invention relates to a composition useful for pain relief. The composition is high concentration capsaicinoid topical composition comprising an analgesic agent that eliminates or reduces the burning or stinging sensation or erythema of the capsaicinoid.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: August 12, 2014
    Assignee: API Genesis, LLC
    Inventors: Daniel Bucks, Philip J. Birbara
  • Patent number: 8802240
    Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: August 12, 2014
    Assignee: Nanopharmaceuticals LLC
    Inventors: Paul J. Davis, Shaker A. Mousa
  • Publication number: 20140221401
    Abstract: The present application relates to compounds and methods for treating pain, incontinence and other conditions.
    Type: Application
    Filed: August 14, 2013
    Publication date: August 7, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Magdalene M. Moran, Christopher Fanger, Jayhong A. Chong, Colleen McNamara, Xiaoguang Zhen, Josh Mandel-Brehm
  • Publication number: 20140220141
    Abstract: The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drugs lopinavir and ritonavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof.
    Type: Application
    Filed: September 7, 2012
    Publication date: August 7, 2014
    Applicant: THE UNIVERSITY OF LIVERPOOL
    Inventors: Marco Norman Giardiello, Thomas Oliver McDonald, Andrew Owen, Steven Paul Rannard, Philip John Martin, Darren Lee Smith
  • Publication number: 20140221410
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 7, 2014
    Applicant: SCIFLUOR LIFE SCIENCES, LLC
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Publication number: 20140221409
    Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.
    Type: Application
    Filed: February 5, 2014
    Publication date: August 7, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Naohiro TAKEMOTO, Kenji MURATA, Norihito MURAYAMA, Chikaomi YAMADA
  • Patent number: 8796001
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 5, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
  • Publication number: 20140212501
    Abstract: The present invention relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug lopinavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof.
    Type: Application
    Filed: September 7, 2012
    Publication date: July 31, 2014
    Applicant: THE UNIVERSITY OF LIVERPOOL
    Inventors: Marco Norman Giardiello, Thomas Oliver McDonald, Andrew Owen, Steven Paul Rannard, Philip John Martin, Darren Lee Smith, James Long
  • Publication number: 20140213602
    Abstract: This invention provides a method for predicting a therapeutic effect of chemotherapy that uses an antitumor agent comprising ?,?,?-trifluorothymidine and 5-chloro-6-(1-(2-iminopyrrolidinyl) methyl)uracil hydrochloride at a molar ratio of 1:0.5 on a colorectal cancer patient, the method comprising: (1) detecting the presence or absence of KRAS gene mutation in a biological sample obtained from the patient; and (2) predicting that the patient is likely to sufficiently respond to the chemotherapy, when KRAS gene mutation is detected in Step (1).
    Type: Application
    Filed: August 15, 2012
    Publication date: July 31, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masanobu Ito, Hiroyuki Okabe
  • Patent number: 8791131
    Abstract: The present invention is directed to compounds of Formula (I), and to salts thereof, their synthesis, and their use as PI3-K? inhibitors and/or PI3-K?/mTOR dual inhibitors.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: July 29, 2014
    Assignee: Pfizer Inc.
    Inventors: Hengmiao Cheng, Ted William Johnson, Jacqui Elizabeth Hoffman, Lisa Chen Guo, Zhengyu Liu
  • Patent number: 8791114
    Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
  • Publication number: 20140205567
    Abstract: The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.
    Type: Application
    Filed: June 14, 2012
    Publication date: July 24, 2014
    Applicant: AB Pharma Ltd.
    Inventor: Zheng-yun James Zhan
  • Patent number: 8785444
    Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: August 2, 2012
    Date of Patent: July 22, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
  • Patent number: 8785467
    Abstract: The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Izzat T. Raheem, William D. Shipe, Cory R. Theberge
  • Publication number: 20140199233
    Abstract: The present invention relates to the fabrication and uses of liposomal nanoparticles.
    Type: Application
    Filed: May 11, 2012
    Publication date: July 17, 2014
    Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, NANOVALENT PHARMACEUTICALS, INC.
    Inventors: Jon O. Nagy, Noah Federman, Christopher Denny, James S. Tomlinson
  • Publication number: 20140200212
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Publication number: 20140199263
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 17, 2014
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
  • Patent number: 8778838
    Abstract: The present invention relates to aqueous concentrate formulations for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its anhydrate; N-(phosphonomethyl)glycine in the form of its free acid, in the form of the ammonium salt or a substituted ammonium salt or a mixture thereof; at least two different non-ionic surfactants with at least one of them comprising an ethylene oxide polymer moiety or an ethylene oxide/C3-C4-alkylene oxide block copolymer moiety, and water; wherein the pH-value of the formulation is below 6.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: July 15, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Sven Adam, Klaus Kolb, Juergen Jakob, Bernd Sievernich, Joerg Steuerwald, Steven Bowe, Joseph Zawierucha, Rex Liebl