Polycyclo Ring System Having A 1,2- Or 1,4-diazine As One Of The Cyclos Patents (Class 514/248)
  • Patent number: 10258620
    Abstract: The invention relates to the provision of a new crystalline form for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium, the use of this form for medical purposes, methods for producing the crystalline form according to the invention, as well as pharmaceutical preparations comprising said form.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: April 16, 2019
    Assignee: Metriopharm AG
    Inventors: Thomas Martin, Josef Breu, Wolfgang Brysch, David Kosel, Beate Ludescher, Michael Niedermaier, Jörg Von Wegerer
  • Patent number: 10251885
    Abstract: The present invention relates generally to antifugal compositions. In an embodiment, the antifungal compositions are effective for application to nails and surrounding skin, and comprise at least one volatile solvent, at least one film forming substance, and at least one pyrimidone derivative of formula I, such as albaconazole. These compositions are capable of treating an infection caused by fungi, such as onychomychosis.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: April 9, 2019
    Assignee: ALLERGAN PHARMACEUTICALS INTERNATIONAL LIMITED
    Inventors: Jon Lenn, Hans Hofland, Edward Hsia
  • Patent number: 10253047
    Abstract: Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: April 9, 2019
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Martin R. Tremblay
  • Patent number: 10238630
    Abstract: The invention features methods for treating cancer in a patient in need thereof by administering eribulin, in combination with one or more PARP inhibitors, and, optionally, a platinum-based antineoplastic drug, and kits therefor. The invention is based in part on the observation that combinations of eribulin mesylate, a PARP inhibitor (e.g., E7449), and, optionally, a platinum-based antineo-plastic drug (e.g., carboplatin), show improved (e.g., synergistic) antitumor effects. Therefore, the present invention features methods of preventing and treating cancer (e.g., homologous recombination (HR)-deficient cancer by the use of combinations of eribulin (e.g., eribulin mesylate) and one or more PARP inhibitors (e.g., E7449 or a pharmaceutically acceptable salt thereof (e.g., the tartrate salt), optionally in combination with a platinum-based antineoplastic drug (e.g., carboplatin).
    Type: Grant
    Filed: May 28, 2015
    Date of Patent: March 26, 2019
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: David Cox, Alton Kremer, Sharon McGonigle, Jiayi Wu
  • Patent number: 10226293
    Abstract: The present invention provides a drug eluting surgical screw and a method for manufacturing a drug eluting surgical screw. The drug eluting surgical screw may include a shaft having a threaded portion, a head having a drive recess disposed at a proximal end of the shaft, the drive recess having a reservoir region and a driver engagement region, and at least one or more drug eluting components disposed within the reservoir region of the drive recess in a manner that does not substantially impair a connection between a driver and the surgical screw when the driver is operably disposed within the driver engagement region, each of the at least one or more drug eluting components including a carrier matrix and a therapeutic agent, the therapeutic agent being at least 20 wt % of the drug eluting component prior to any implantation of the drug eluting surgical screw.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: March 12, 2019
    Assignee: DePuy Synthes Products, Inc.
    Inventors: David A. Armbruster, Anurag Pandey
  • Patent number: 10214512
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.
    Type: Grant
    Filed: October 24, 2016
    Date of Patent: February 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiayi Xu, Amjad Ali, Wei Zhou, Ying-Duo Gao, Scott D. Edmondson, Eric Mertz, Santhosh F. Neelamkavil, Weiguo Liu, Wanying Sun, Dong-Ming Shen, Bart Harper, Cheng Zhu, Thomas Bara, Yeon-Hee Lim, Meng Yang
  • Patent number: 10207002
    Abstract: Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: February 19, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, David Monteith
  • Patent number: 10183944
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: January 22, 2019
    Assignee: Asana BioSciences, LLC
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Hosahalli Subramanya, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Patent number: 10167259
    Abstract: The present invention relates generally to novel allosteric regulators of proteasome activity, methods for preparation and use, and pharmaceutical compositions thereof. Specifically piperidine-2-carboxylic acid derivatives containing 1-oxo-aroyl group and a lipophilic ester side chain are disclosed as allosteric inhibitors of proteasome 2S activity, and as therapeutic agents for the treatment of proteasome-associated disorders in a subject.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: January 1, 2019
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Pawel A. Osmulski, Maria E. Gaczynska
  • Patent number: 10159673
    Abstract: Disclosed are methods of alleviating or preventing one or more symptoms associated with fragile X syndrome in an individual in need thereof via administration of a therapeutically effective amount of a GABA(A) alpha 2 and/or 3 partial agonist. The one or more symptoms may include impaired functional communication, anxiety, inattention, hyperactivity, sensory reactivity, autonomic nervous system dysregulation, aberrant eye gaze, self-injury, aggression, seizures, EEG abnormalities, including but not limited to, abnormal spectral analysis, event related potentials which may include auditory and visual responses, abnormalities in cortical responses as evoked by transcranial magnetic stimulation including resting and active motor thresholds and abnormal responses in measures of cortical inhibition and excitation, aberrant impaired cognitive function, compromised daily living skills, or a combination thereof.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: December 25, 2018
    Assignee: Children's Hospital Medical Center
    Inventors: Craig Erickson, Tori Lynn Schaefer
  • Patent number: 10155726
    Abstract: Substituted pyridines that modulate HIF-2a activity, pharmaceutical compositions containing the substituted pyridines, and methods of using these chemical entities for treating proliferative diseases and conditions associated with HIF-2a activity are described herein.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: December 18, 2018
    Assignee: PELOTON THERAPEUTICS, INC.
    Inventors: Paul Wehn, Rui Xu, Hanbiao Yang
  • Patent number: 10149968
    Abstract: A method for treating a subject diagnosed with a cancer or other disorder comprising a hyperproliferative tissue is described herein. The method includes localized delivery of a material which contains a therapeutically effective agent and/or moiety. The localized delivery of the agent is achieved using a catheter-based delivery system and an implant. An implant can include a support component, a cover component, and a valve component. The valve component can be operable to permit flow through the implant. The implant can be delivered on a catheter, with one of the ends of the implant being selectively expanded to permit temporary occlusion of a vessel while delivering a material through the valve component to a downstream target region. The other end of the implant can thereafter be released such that the implant occludes the vessel, or the implant can be removed from the vessel entirely.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: December 11, 2018
    Assignee: ArtVentive Medical Group, Inc.
    Inventor: Leon Rudakov
  • Patent number: 10118916
    Abstract: The present invention provides for compounds of formula (I) wherein R1, m, Z, G1, R2, and R3 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: November 6, 2018
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Robert J. Altenbach, Andrew Bogdan, Vincent Chan, Timothy A. Grieme, John R. Koenig, Philip R. Kym, Bo Liu, Karine Fabienne Malagu, Sachin V. Patel, Marc Scanio, Xenia B. Searle, Shashank Shekhar, Xueqing Wang, Ming C. Yeung
  • Patent number: 10100016
    Abstract: Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.
    Type: Grant
    Filed: May 22, 2018
    Date of Patent: October 16, 2018
    Assignee: SHANGHAI YINGLI PHARMACEUTICAL CO., LTD.
    Inventors: Zusheng Xu, Nong Zhang, Qingrui Sun, Tianzhi Wu
  • Patent number: 10100015
    Abstract: Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: October 16, 2018
    Assignee: SHANGHAI YINGLI PHARMACEUTICAL CO., LTD.
    Inventors: Zusheng Xu, Nong Zhang, Qingrui Sun, Tianzhi Wu
  • Patent number: 10080754
    Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: September 25, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
  • Patent number: 10080749
    Abstract: The present invention is directed to methods of treating tuberculosis by providing a pharmaceutically effective amount of a combination of drug compounds.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: September 25, 2018
    Assignee: The Regents of the University of California
    Inventors: Chih-Ming Ho, Daniel L. Clemens, Bai-Yu Lee Clemens, Marcus Aaron Horwitz, Aleidy Marlene Silva Vite, Theodore Kee, Xianting Ding
  • Patent number: 10077242
    Abstract: Methods of synthesizing the angiotensin II receptor antagonist telmisartan in high yield and purity are provided. The methods involve the coupling of two structurally distinct benzimidazole units via a Suzuki cross-coupling reaction. Methods of regioselectively synthesizing one of the benzimidazole units are also provided.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: September 18, 2018
    Assignee: Virginia Commonwealth University
    Inventors: Frank Gupton, Alex Martin, Ali Siamaki, Katherine Belecki
  • Patent number: 10030015
    Abstract: Amine compounds having activity against inflammation, fungi, unicellular parasitic microorganisms, and cancer are described. The compounds contain a monocyclic, bicyclic, or tricyclic aromatic ring having one, two, or three ring nitrogen atoms.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: July 24, 2018
    Assignee: Wellstat Therapeutics Corporation
    Inventors: David M. Simpson, Dennis Bryan Zerby, Ming Lu, Reid W. von Borstel, Rui Li, Julian Reading, Stephen Wolpe, Nureddin Aman
  • Patent number: 10030027
    Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: July 24, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Yi-Heng Chen, Guoqing Li, Joie Garfunkle, Hong-Dong Li, Shouwu Miao, Subharekha Raghavan, Cameron J. Smith, John Stelmach, Alan Whitehead, Rui Zhang, Yong Zhang, Jianmin Fu, Gang Ji, Falong Jiang
  • Patent number: 10028913
    Abstract: The present invention relates to a liposomal pharmaceutical preparation containing a multivalent ionic drug, a process for the preparation of the liposomal pharmaceutical preparation, and a use thereof in the treatment of diseases, in which the liposome has a size of about 30-80 nm, and the phospholipid bilayer has a phospholipid with a Tm higher than body temperature, so that the phase transition temperature of the liposome is higher than the body temperature.
    Type: Grant
    Filed: April 26, 2016
    Date of Patent: July 24, 2018
    Assignee: CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO., LTD
    Inventors: Chunlei Li, Jinxu Wang, Caixia Wang, Yanhui Li, Dongmin Shen, Wenmin Guo, Li Zhang, Lan Zhang
  • Patent number: 10023541
    Abstract: A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: July 17, 2018
    Assignee: BIAL-PORTELA & Ca, S.A.
    Inventors: Carla Patricia da Costa Pereira Rosa, Rita Gusmao De Noronha, Laszlo Erno Kiss, Patricio Manuel Vieira Araujo Soares Da Silva, Domenico Russo, Jorge Bruno Reis Wahnon, William Maton
  • Patent number: 9988386
    Abstract: The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: June 5, 2018
    Assignee: Kata Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Andrew Good
  • Patent number: 9981916
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: May 29, 2018
    Assignee: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward
  • Patent number: 9968602
    Abstract: Phthalazinediones that function as intracellular redox modulators are useful in treating cells in various disease states where intracellular redox status is impaired. By buffering aberrant redox states, phthalazinediones enable cellular processes essential for survival and augment medical treatments. The phthalazinediones of the invention can modulate functions related to cell growth, differentiation, activity, or death, to correct aberrations and restore homeostasis, and can serve as adjunctive therapy in treating various disease conditions.
    Type: Grant
    Filed: February 11, 2013
    Date of Patent: May 15, 2018
    Assignee: BACH PHARMA, INC.
    Inventors: Mark O. Henry, William S. Lynn
  • Patent number: 9884828
    Abstract: The present invention provides compounds having a structure according to Formula I: (I) or a salt or solvate thereof, wherein R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: February 6, 2018
    Assignee: Imago Pharmaceuticals, Inc.
    Inventors: Danielle L. Aubele, Albert W. Garofalo, Simeon Bowers, Anh P. Truong, Xiaocong Michael Ye, Maurizio Franzini, Marc Adler, R. Jeffrey Neitz, Gary Probst
  • Patent number: 9868742
    Abstract: The invention provides substituted imidazo[1,2-b]pyridazine compounds, substituted imidazo[1,5-b]pyridazine compounds, related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,2-b]pyridazine compounds described herein include substituted imidazo[1,2-b]pyridazine-3-carboxamide compounds and variants thereof.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: January 16, 2018
    Assignee: Lysosomal Therapeutics Inc.
    Inventors: Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury
  • Patent number: 9868749
    Abstract: A series of substituted benzimidazole, imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives, and analogues thereof, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: January 16, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Rikki Peter Alexander, Jonathan Mark Bentley, Gareth Neil Brace, Daniel Christopher Brookings, Prafulkumar Tulshibhai Chovatia, Hervé Jean Claude Deboves, Craig Johnstone, Elizabeth Pearl Jones, Boris Kroeplien, Fabien Claude Lecomte, James Madden, Craig Miller, John Robert Porter, Matthew Duncan Selby, Michael Alan Shaw, Darshan Gunvant Vaidya, Ian Andrew Yule
  • Patent number: 9858761
    Abstract: A real-time betting system includes an event control server enabled to communicate data via a network. The event control server communicates gaming event information to various system components and an event control database for collecting and storing event data. A real-time betting system server communicates in operative communication with the event control server and includes an odds transformation module for transforming probabilities to odds. The system has a bookmaker server and a plurality of betting devices in operative communication with the event control server. The real-time betting system server enables a jackpot payout possibility for each bet enabled by the bookmaker server. The betting devices receive event information, including odds. Bets placed at the betting devices are communicated to the bookmaker server. The events having a short time interval and are selectively communicated to the betting devices to enable bets to be placed.
    Type: Grant
    Filed: February 1, 2014
    Date of Patent: January 2, 2018
    Assignee: Novomatic AG
    Inventor: Martin Zimmerl
  • Patent number: 9839625
    Abstract: Provided herein are compositions and methods for inhibiting cancer cell motility and/or metastasis. In particular embodiments, KBU2046 (or an analog thereof) and one or more additional therapies (e.g., cancer therapies (e.g., hormone therapies and chemotherapies) are provided to inhibit cancer cell motility, inhibit metastasis, and/or treat cancer (e.g., prostate cancer, lung cancer, breast cancer, colon cancer, etc.).
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: December 12, 2017
    Assignee: Northwestern University
    Inventors: Raymond C. Bergan, Karl A. Scheidt, Li Xu
  • Patent number: 9834820
    Abstract: Described herein are methods of the treatment and diagnosis of bone mineral density related disorders. More particularly, described herein are methods of diagnosing or predicting a bone mineral density related disease, or a risk of a bone mineral density related disease, in a subject, which method comprises detecting a mutation in the TBXAS1 gene, wherein the presence of such a mutation is indicative of a bone mineral density related disease or of a risk of a bone mineral density related disease. Also described are compounds such as a thromboxane synthase (TXAS) encoding polynucleotide, a TXAS, thromboxane A2 or an analog thereof for treating or preventing a disease associated with an increased bone mineral density (e.g., Ghosal hematodiaphyseal dysplasia syndrome). Additional aspects describe an inhibitor of TBXAS1 gene expression or a thromboxane inhibitor for treating or preventing a disease associated with a decreased bone mineral density (e.g., osteoporosis).
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: December 5, 2017
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), Universite Paris Descartes, Assistance Publique—Hopitaux de Paris (AP-HP)
    Inventors: Valerie Cormier-Daire, Arnold Munnich
  • Patent number: 9833271
    Abstract: The present invention provides a drug eluting surgical screw and a method for manufacturing a drug eluting surgical screw. The drug eluting surgical screw may include a shaft having a threaded portion, a head having a drive recess disposed at a proximal end of the shaft, the drive recess having a reservoir region and a driver engagement region, and at least one or more drug eluting components disposed within the reservoir region of the drive recess in a manner that does not substantially impair a connection between a driver and the surgical screw when the driver is operably disposed within the driver engagement region, each of the at least one or more drug eluting components including a carrier matrix and a therapeutic agent, the therapeutic agent being at least 20 wt % of the drug eluting component prior to any implantation of the drug eluting surgical screw.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: December 5, 2017
    Assignee: DePuy Synthes Products, Inc.
    Inventors: David Armbruster, Anurag Pandey
  • Patent number: 9828377
    Abstract: Provided herein are compounds of Formula (I?) or (A?), pharmaceutical compositions comprising the compounds, and methods of use thereof. The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including PI3 kinase activity.
    Type: Grant
    Filed: April 24, 2015
    Date of Patent: November 28, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Martin R. Tremblay
  • Patent number: 9820974
    Abstract: The present invention is directed to methods of inhibiting LTA4-h in a human patient and method of treating a condition ameliorated by the inhibition of leukotriene A4 hydrolase activity in a human patient comprising administering to said human patient the compound, 4-{5-[4-(4-Oxazol-2-yl-phenoxy)-benzyl]-2,5-diaza-bicyclo[2.2.1]hept-2-ylmethyl}-benzoic acid.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: November 21, 2017
    Assignee: Celtaxsys, Inc.
    Inventors: Eric B. Springman, Margaret McCrann Pugh, Lopa Bhatt, Ralph Grosswald
  • Patent number: 9802945
    Abstract: The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: October 31, 2017
    Assignee: Pfizer Limited
    Inventors: Robert McKenzie Owen, David Cameron Pryde, Mifune Takeuchi, Christine Anne Louise Watson
  • Patent number: 9801853
    Abstract: In one aspect, the invention provides a method for inhibiting the growth and/or proliferation of a myc-driven tumor cell comprising the step of contacting the tumor cells with a CSNK1? inhibitor. In another aspect, the invention provides a method of treating a subject suffering from a tumor comprising myc-driven tumor cells, comprising administering to the subject an amount of a composition comprising a CSNK1? inhibitor effective to inhibit the growth and/or proliferation of the tumor cells.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: October 31, 2017
    Assignee: Fred Hutchinson Cancer Research Center
    Inventors: Carla Grandori, Masafumi Toyoshima
  • Patent number: 9795568
    Abstract: The invention relates to a solid tablet that is directly-compressed of powder, comprising meloxicam and one or more excipients which are homogenously dispersed within the tablet that can be broken into two, three or four units with each unit containing equal amounts of the active ingredient, meloxicam.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: October 24, 2017
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin A. Folger, Stefan Lehner, Horst Schmitt
  • Patent number: 9795140
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: October 24, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Timothy P. Martin, Joseph D. Eckelbarger, Ronald Ross, Jr., Kyle DeKorver, Ronald J. Heemstra, Daniel I. Knueppel, Peter Vednor, Ricky Hunter, David A. Demeter, Tony K. Trullinger, Erich Baum, Zoltan Benko, Nakyen Choy, Gary Crouse, John F. Daeuble, Sr., Fangzheng Li, Jeff Nissen, Michelle Riener, Tom Sparks, Frank Wessels, Maurice Yap
  • Patent number: 9795139
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: October 24, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Joseph D. Eckelbarger, Daniel I. Knueppel, Ronald J. Heemstra, Ronald Ross, Jr., Kyle A. Dekorver, Kaitlyn Gray, Peter Vednor, Timothy P. Martin, Ricky Hunter, David A. Demeter, Tony K. Trullinger, Erich Baum, Zoltan L. Benko, Nakyen Choy, Gary Crouse, John F. Daeuble, Sr., Fangzheng Li, Jeff Nissen, Michelle Riener, Tom Sparks, Frank Wessels, Maurice Yap
  • Patent number: 9755153
    Abstract: A compound, an organic light emitting diode device, and a display device, the compound being represented by the following Chemical Formula 1:
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: September 5, 2017
    Assignee: SAMSUNG DISPLAY CO., LTD.
    Inventor: Ji Yun Jung
  • Patent number: 9738642
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: August 22, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Lawrence R. Marcin, Mendi A. Higgins, Joanne J. Bronson, F. Christopher Zusi, John E. Macor, Min Ding
  • Patent number: 9732043
    Abstract: The present invention comprises methods of manufacturing a highly purified, pharmaceutical grade phthalazinedione (for example, 5-amino-2,3-dihydrophthalazine-1,4-dione) for administration to a human or animal. The manufacturing methods identify and isolate starting materials (for example, 3-nitrophthalic acid), and prepare intermediate products (for example, 3-nitrophthalhydrazide), which are suitable for the commercial batch process production of highly purified and high-yielding intermediate products and final phthalazinedione products. In an embodiment, a solution of 3-nitrophthalhydrazide and sodium hydroxide in water is prepared and hydrogenated to yield 5-amino-2,3-dihydrophthalazine-1,4-dione.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: August 15, 2017
    Assignee: Bach Pharma, Inc.
    Inventors: Mark O. Henry, William S. Lynn
  • Patent number: 9662330
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: March 3, 2016
    Date of Patent: May 30, 2017
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth C. Deselm, Hui Qiu, Yufang Xiao, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Patent number: 9657034
    Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: January 18, 2016
    Date of Patent: May 23, 2017
    Assignees: AbbVie Deuschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Sean Turner, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob, Lawrence Black, Katja Jantos
  • Patent number: 9650382
    Abstract: The invention relates to novel heteroarylamide derivatives having formula (I) and N-oxides, stereoisomers and pharmaceutically acceptable salts thereof, where RA, RB, R1 1, R?, R?, z and X are as defined in the claims. The arylamide derivatives of formula (I) have antiandrogenic properties. The invention also relates to compounds of formula (I) for use as a medicament and to pharmaceutical compositions comprising them and to their preparation.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: May 16, 2017
    Assignee: ARANDA PHARMA LTD
    Inventors: Jari Ratilainen, Milla Koistinaho, Anu Muona
  • Patent number: 9642823
    Abstract: The treatment options for treating blast-induced and noise-induced traumatic brain injury and tinnitus are limited. Thus, the current invention provides methods for treating traumatic brain injury and tinnitus. The methods involve administering a pharmaceutically effective amount of a composition comprising 2,4-disulfonyl ?-phenyl tertiary butyl nitrone and N-acetylcysteine (NAC).
    Type: Grant
    Filed: February 18, 2016
    Date of Patent: May 9, 2017
    Assignees: Hough Ear Institute, Oklahoma Medical Research Foundation
    Inventors: Richard D. Kopke, Robert A. Floyd, Rheal Towner
  • Patent number: 9624246
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: April 18, 2017
    Assignee: Merck Patent GmbH
    Inventors: Xiaoling Chen, Ruoxi Lan, Catherine Jorand-Lebrun, Henry Yu, Andreas Goutopoulos
  • Patent number: 9561227
    Abstract: The present disclosure provides a method of treating a subject that is resistant to one or more drugs by identifying a subject having one or more drug resistant cells; administering to the subject a pharmaceutically effective amount of an inhibitor compound, and contacting one or more drug resistant cells with the inhibitor compound to reduce the export of the inhibitor compound from the one or more drug resistant tumor cells and to block the transport of drug(s) from the one or more drug resistant cells.
    Type: Grant
    Filed: January 15, 2015
    Date of Patent: February 7, 2017
    Assignee: Southern Methodist University
    Inventors: John G. Wise, Pia D. Vogel, Frances K. Brewer, Courtney A. Follit
  • Patent number: 9562051
    Abstract: The invention provides compounds of formula I: wherein A, B, X, and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds, processes for preparing such compounds, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: February 7, 2017
    Assignee: Rutgers, the State University of New Jersey
    Inventors: Edmond J. LaVoie, Wei Feng, Leroy F. Liu
  • Patent number: 9556147
    Abstract: This application discloses compounds according to generic Formula I: (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: January 31, 2017
    Assignee: HOFFMANN-LA INC.
    Inventors: Christine E. Brotherton-Pleiss, Rama K. Kondru, Francisco Javier Lopez-Tapia, Yan Lou