Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
  • Patent number: 10130611
    Abstract: This application relates to a novel benzo-heterocycle derivative and more particularly, it relates a composition for preventing and treating cancer or for inhibiting metastasis comprising benzo-heterocycle derivative or pharmaceutically acceptable salts thereof as an active ingredient. The present inventors confirmed that KRS has an effect on cancer metastasis by facilitating cancer (or tumor) cell migration through interaction with 67LR, and also found that a substance inhibiting the interaction between KRS and 67LR can prevent and treat cancer by inhibiting cancer cell metastasis. Accordingly, the composition of the present invention can inhibit cancer metastasis, and thus provide a novel means for prevention and treatment of cancer.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 20, 2018
    Assignee: MEDICINAL BIOCONVERGENCE RESEARCH CENTER
    Inventors: Sunghoon Kim, Jin Woo Choi, Jin Young Lee, Dae Gyu Kim, Gyoon Hee Han, Jee Sun Yang, Chul Ho Lee
  • Patent number: 10105353
    Abstract: New compounds, namely, (7aS,2?S)-2-oxoclopidogrel and its pharmaceutically acceptable salts thereof are disclosed for treatment or prophylaxis of thrombo-embolism and/or cardiovascular diseases.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: October 23, 2018
    Assignee: IPCA LABORATORIES LIMITED
    Inventors: Ashok Kumar, Satish Rajanikant Soudagar, Nellithanath Thankachen Byju, Gaurav Sahal, Arpana Prashant Mathur, Sanjay Pandurang Gawade, Dinesh Kanji Bhadra, Devki Moje
  • Patent number: 10064848
    Abstract: Compounds for the preparation of pyridone derivatives are provided. In particular, compounds of formula (IA) are provided, wherein the variable groups are as defined in the specification. The compounds of formula (IA) can be used as intermediates in the preparation of pyridone derivatives useful as mitogen-activated protein kinase kinase (MEK) inhibitors and therapeutic agents for treating cancer.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: September 4, 2018
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Wangyang Tu, Haitang Zhang, Guoji Xu, Jiangtao Chi
  • Patent number: 9937160
    Abstract: The present invention relates to methods of treatment of hepatitis C using prasugrel. The methods of the present invention can be used in patients with hepatitis C administering prasugrel in combination with one or more anti-hepatitis C drugs.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: April 10, 2018
    Assignee: Cipla (UK) Limited
    Inventors: Karl Roberts, Geena Malhotra, Dhiraj Abhyankar, Kalpana Joshi, Jeevan Ghosalkar
  • Patent number: 9938289
    Abstract: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGF?-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: April 10, 2018
    Assignee: FBM THERAPEUTICS, LLC
    Inventors: Stephen D. Barrett, James B. Kramer, Mark L. Boys, Huifen Chen
  • Patent number: 9913831
    Abstract: Disclosed is a treatment of diabetes insipidus. Methods of treating diabetes insipidus disorders associated with P2Y receptors using the compounds and compositions are also disclosed.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: March 13, 2018
    Assignee: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Bellamkonda K. Kishore, Noel G. Carlson, Yue Zhang
  • Patent number: 9815848
    Abstract: This invention provides a new preparation method of Clopidogrel Hydrogen Sulfate spherical crystal form I, using single 2-butanol as solvent, controlling the concentration, addition way and addition speed of sulfuric acid used to salify to shorten the process time, thus separating out Clopidogrel Hydrogen Sulfate from solution system stably with spherality. And the Clopidogrel Hydrogen Sulfate obtained complies with the requirements of the follow-up process on residual solvent, bulk density and mobility.
    Type: Grant
    Filed: December 31, 2014
    Date of Patent: November 14, 2017
    Assignees: TIANJIN UNIVERSITY, SHENZHEN SALUBRIS PHARMACEUTICALS CO., LTD
    Inventors: Junbo Gong, Qi Wang, Qiuxiang Yin, Jingkang Wang, Xiaopeng Song, Baohong Hou, Liting Liao, Duanming Tan, Ziyuan Di
  • Patent number: 9778248
    Abstract: With a method for measurement of thrombocyte function, a solution is created, by which the sensitivity of individual thrombocytes can be measured with the least possible apparatus effort, with high throughput, by passing a liquid thrombocyte solution, in which the thrombocytes are present in isolated form, into a microfluidic chamber and brought into contact with at least one stimulant, wherein an electrical field directed transverse to the entry direction of the thrombocyte solution is applied to the chamber, and the movement path of the thrombocytes in the electrical field is observed and evaluated, in such a manner that thrombocytes having a movement path directed in the direction toward the minus pole of the electrical field are classified as non-activated thrombocytes, and thrombocytes having a movement path directed in the direction toward the plus pole of the electrical field are classified as activated thrombocytes.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: October 3, 2017
    Assignee: Leibniz—Institut fuer Analytische Wissenschaften—ISAS—e.V.
    Inventors: Jonathan West, Dirk Janasek, Albert Sickmann
  • Patent number: 9657014
    Abstract: The present invention relates to the use of compounds of general formula I wherein R?, R1, R2 and R3 are as defined herein, or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, and for methods to treat a variety of neurodegenerative and neuropsychiatric diseases.
    Type: Grant
    Filed: May 20, 2015
    Date of Patent: May 23, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Ravi Jagasia, Roland Jakob-Roetne, Rainer E. Martin, Jens-Uwe Peters, Juergen Wichmann
  • Patent number: 9562015
    Abstract: The present invention comprises compounds and compositions thereof for enhanced drug delivery. Pro-drug and double pro-drug derivatives of corticosteroids non-steroid anti-inflammatory drugs (NSAIDs), and ruboxistaurin for delivery to the eye are provided. The compounds and compositions are useful for treating various ocular diseases, including ocular diseases effecting the posterior segments of the eye. In addition, the present invention is directed to particle in particle carrier formulations for sustained release of therapeutic agents.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: February 7, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY
    Inventors: Uday B. Kompella, Ashish Thakur
  • Patent number: 9539246
    Abstract: Disclosed is a treatment of diabetes insipidus. Methods of treating diabetes insipidus disorders associated with P2Y receptors using the compounds and compositions are also disclosed.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: January 10, 2017
    Assignee: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Bellamkonda K. Kishore, Noel G. Carlson, Yue Zhang
  • Patent number: 9512118
    Abstract: The present invention relates to a crystal of 1-ethyl-7-methyl-3-{4-[(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)oxy]phenyl}-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one useful as a prophylactic or therapeutic agent for schizophrenia and the like, which shows an X-ray powder diffraction pattern having characteristic peaks at interplaner spacings (d) of 13.59 plus or minus 0.2 and 6.76 plus or minus 0.2 Angstroms in powder X-ray diffraction.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: December 6, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: Katsuhiko Yamamoto
  • Patent number: 9504678
    Abstract: The present disclosure provides oral dosage forms comprising an antiplatelet agent and an acid inhibitor, as well as methods of treating subjects with an antiplatelet agent and an acid inhibitor.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: November 29, 2016
    Assignee: KG ACQUISITION LLC
    Inventors: Mark A. Goldsmith, Elizabeth Vadas
  • Patent number: 9480680
    Abstract: The present disclosure provides ready-to-use, oil/water emulsion compositions with mean droplet size (intensity-average, m) of 100-500 nm, wherein the oil phase comprises clopidogrel free base dispersed in pharmaceutical acceptable oil(s). The emulsion uses clopidogrel free base or premix of clopidogrel free base in oil(s) as the starting materials and may also contain one or more excipients such as surfactant and or co-surfactant, osmotic agent, pH adjustment agent, antioxidant, preservative, sweetener, and/or suspending agent, etc. The emulsion formulations and method of manufacturing significantly improves the stability of clopidogrel over other aqueous based formulations (such as cyclodextrin-based formulations and emulsion made using clopidogrel salt as the starting materials) with respect to chiral degradation, hydrolytic, and thermal degradation.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: November 1, 2016
    Inventor: Jingjun Huang
  • Patent number: 9402907
    Abstract: An object of the present invention is to provide a pharmaceutical composition containing compound I or a pharmacologically acceptable salt thereof, or a solvate thereof as an active ingredient, which is favorably dissolved in the neutral region. The present invention relates to a pharmaceutical composition containing (A) N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide or a pharmacologically acceptable salt thereof, or a solvate thereof, and (B) an acid or a salt thereof.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: August 2, 2016
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Koichi Ishidoh, Kazuhiro Matsuura
  • Patent number: 9403842
    Abstract: The present invention relates to prasugrel or a pharmaceutically compatible salt thereof, compositions that contain this active substance and pharmaceutical compositions that contain this active substance or a composition containing this active substance. The present invention further relates to methods for producing the novel compositions.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: August 2, 2016
    Assignee: ratiopharm GmbH
    Inventors: Sandra Brueck, Jana Paetz
  • Patent number: 9271972
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: March 1, 2016
    Assignee: University of Massachusetts
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Patent number: 9248122
    Abstract: The invention relates to substituted heteroquinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: February 2, 2016
    Assignee: GRÜNENTHAL GMBH
    Inventors: Sven Kühnert, Simon Lucas, Gregor Bahrenberg, Wolfgang Schröder
  • Patent number: 9193713
    Abstract: The present invention relates compounds of formula (I) wherein A and R1 are as defined in the specification, pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: November 24, 2015
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Derek W. Nelson, Tongmei Li, Sridhar Peddi, Jennifer Frost, Teodozyj Kolasa, Bo Liu, Steven P. Latshaw, Xueqing Wang
  • Patent number: 9170126
    Abstract: An electronic device is described that includes a range indicator for conveying a range of travel until the electronic device ceases operation due to loss of power. In implementations, the electronic device includes a display device, a memory operable to store one or more modules, and at least one processor coupled to the display device and the memory. The processor is operable to execute the one or more modules to cause display of navigation information at the display device. The navigation information includes a map graphic representing an area an aircraft is traversing. The navigation information also includes an end of use situation that represents a range of travel for the aircraft until the electronic device ceases operation due to a loss of power.
    Type: Grant
    Filed: August 22, 2013
    Date of Patent: October 27, 2015
    Assignee: Garmin International, Inc.
    Inventors: Christopher E. P. Schulte, Douglas E. Leeper, Jr.
  • Patent number: 9138392
    Abstract: Provided is a nontherapeutic cosmetic process for depigmenting, lightening and/or whitening keratin materials applying an effective amount of at least one compound of formula (I): or a tautomer thereof of formula (I?): to a keratin material, where the structural variables are as defined herein.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: September 22, 2015
    Assignee: L'OREAL
    Inventor: Xavier Marat
  • Patent number: 9133186
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Grant
    Filed: September 8, 2011
    Date of Patent: September 15, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • Publication number: 20150148308
    Abstract: A harmful arthropod control composition comprising a compound represented by the following Formula (1) wherein each symbol represents definitions described in the specification, and one or more fungicidal compounds, which are selected from among azoles, strobilurins, phenylamides, rice blast controlling compounds, rice sheath blight disease controlling compounds, and other fungicidal compounds. The composition has an excellent controlling effect against harmful arthropods.
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Tatsuya Suzuki, Atsushi Iwata, Yoshihiko Nokura
  • Patent number: 9040707
    Abstract: The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 26, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gregor James MacDonald, Andrés Avelino Trabanco-Suárez, Susana Conde-Ceide, Gary John Tresadern, José Manuel Bartolomé-Nebreda, Joaquin Pastor-Fernández
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Patent number: 9034896
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 21, 2014
    Date of Patent: May 19, 2015
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Patent number: 9029390
    Abstract: The invention relates to non hemolytic compositions containing an antiplatelet agent such as clopidogrel or ticlopidine; these compositions being characterized in that the antiplatelet agent is in the form of free base, and the composition contains at least one hydrophilic non ionic surfactant. The invention relates also a galenic form, a method of preparation of thereof, as well as therapeutic uses of thereof, especially in patients who suffer from undesirable effects related to hemolysis and/or gastrointestinal acidity.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: May 12, 2015
    Assignee: CLL Pharma
    Inventors: Thierry Breul, Claude Laruelle
  • Publication number: 20150126529
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Upender Velaparthi, Peiying Liu
  • Publication number: 20150126545
    Abstract: A composition comprises a kinase inhibitory compound, e.g., N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea, in a mixture comprising (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. The composition is suitable for dilution with an IV solution for administration to a subject in need thereof for treatment of a cancer.
    Type: Application
    Filed: December 14, 2012
    Publication date: May 7, 2015
    Applicant: AbbVie Inc.
    Inventors: Yi Shi, Josh M. Lipari, Brian E. Padden, Lloyd S. Dias, Julie K. Spence
  • Patent number: 9018207
    Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: April 28, 2015
    Assignee: Spinifex Pharmaceuticals Pty Ltd
    Inventors: Maree Therese Smith, Bruce Douglas Wyse
  • Patent number: 9012641
    Abstract: Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydro bromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: April 21, 2015
    Assignee: Teva Pharmaceuticals Industries Ltd.
    Inventors: Mihaela Tuksar, Tomislav Biljan, Miroslav Zegarac
  • Publication number: 20150105419
    Abstract: Methods for inhibiting the growth of pancreatic cancer cells or other cancer cells driven by Sonic hedgehog are disclosed.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Marilyn D. Resh, Joseph Fraser Glickman, Elissaveta Petrova, Ouathek Ouerfelli
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Patent number: 8999975
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
  • Patent number: 9000006
    Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).
    Type: Grant
    Filed: April 9, 2014
    Date of Patent: April 7, 2015
    Assignee: Fibrogen, Inc.
    Inventors: Eric D. Turtle, Lee A. Flippin, Michael P. Arend, Heng Cheng
  • Publication number: 20150094329
    Abstract: A compound represented by formula (1) and an N-oxide thereof have excellent pest control effect. (In the formula, Het to which R1—S(O)n is bonded represents a five-membered aromatic heterocyclic ring represented by formula H1, H2, H3 or H4 (wherein Y1 represents an oxygen atom or the like; Y2 represents an oxygen atom or the like; G1, G2 and G3 may be the same or different and each represents a nitrogen atom or the like; R1 represents a C1-C6 alkyl group which may have one or more atoms or groups selected from the group X, or the like; and n represents 0, 1 or 2); A1 represents an oxygen atom or the like; A2 represents a nitrogen atom or the like; A3 represents a nitrogen atom or the like; and R2 and R3 may be the same or different and each represents a C1-C6 chain hydrocarbon group which may have one or more atoms or groups selected from the group X, or the like.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 2, 2015
    Inventors: Yoshihiko Nokura, Mai Ito, Chie Shimizu, Hajime Mizuno
  • Publication number: 20150094315
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Application
    Filed: July 1, 2014
    Publication date: April 2, 2015
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
  • Publication number: 20150087512
    Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.
    Type: Application
    Filed: September 26, 2014
    Publication date: March 26, 2015
    Inventors: Nian WANG, Nagaraju AKULA
  • Patent number: 8987249
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Publication number: 20150079169
    Abstract: The present invention provides for novel formulations of clopidogrel in combination with proton pump inhibitors (PPI) and optionally with NSAIDs, for use as improved antiplatelet therapies in stroke and cardiovascular indications. The invention provides the delivery of clopidogrel in pulses or waves, such that the total dose is phased/spread out over time and, advantageously, combined with omeprazole in a way to minimize the conflicting actions these two drugs may have on each other. In addition, the invention also provides the delivery of clopidogrel and a PPI, and optionally aspirin, in a sequential (orderly) manner that would allow for the delivery and metabolism of clopidogrel first, followed by the PPI, and thereafter optionally aspirin. A particular mode of the invention involves the combination of clopidogrel with coformulated immediate release omeprazole+enteric coated aspirin.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 19, 2015
    Applicant: POZEN INC.
    Inventor: John R. Plachetka
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Publication number: 20150072993
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Zengyun AN, Liang CHEN, Shuhui CHEN, Jean Marie DEFAUW, Scott Dale HOLMSTROM, Ping HU, Chongzhi TANG, William Hunter WHITE, Wentao WU, Yang ZHANG
  • Publication number: 20150072998
    Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
    Type: Application
    Filed: April 16, 2013
    Publication date: March 12, 2015
    Inventors: Sanford Markowitz, James K.V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Melissa Moss, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
  • Publication number: 20150065501
    Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Publication number: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Publication number: 20150065456
    Abstract: The invention provides methods of treating or preventing in a subject a cancer, tumor, or neoplasm, including malignancies or metastases thereof, using a direct Factor Xa inhibitor. The methods particularly involve the treatment of human patients afflicted with a malignant cancer, tumor, or neoplasm with an effective amount of the Factor Xa inhibitor. In an embodiment, the Factor Xa inhibitor is the small molecule edoxaban p-toluenesulfonate monohydrate, also termed “DU-176b”. The invention provides methods of administering a Factor Xa inhibitor to effectively reduce or suppress, or otherwise abrogate, the growth of cancers, tumors, or neoplasms in a subject who has, or is at risk for, cancer and, optionally, who also has, or is at risk for, thrombotic disease or embolism. The methods of the invention can also reduce the incidence of migration or invasion of metastatic or malignant cancers in a human subject by administration of a Factor Xa inhibitor.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Inventor: Michele Mercuri
  • Publication number: 20150057265
    Abstract: The present disclosure describes furo- and thieno-pyridine carboxamide compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Taisheng Huang, Song Mei, Jun Pan, Oleg Vechorkin, Hai-Fen Ye, Wenyu Zhu, Maria Rafalski, Anlai Wang, Chu-Biao Xue
  • Patent number: 8962574
    Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Paul Anthony Reilly