Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
  • Patent number: 10702537
    Abstract: A method of treating a condition of in a human patient comprising pharmacologically activating a translocator protein of 18 kDa (TSPO), wherein the condition is one of a chronic methamphetamine addiction, a medical consequence of methamphetamine use; a behavioral consequence of methamphetamine use, an HIV associated cognitive motor disorder, an HIV-associated neurodegenerative disorder, and a neuroinflammatory response.
    Type: Grant
    Filed: June 4, 2018
    Date of Patent: July 7, 2020
    Assignee: BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY and Agricultural and Mechanical College
    Inventors: Nicholas E. Goeders, Christopher Dalton Schmoutz
  • Patent number: 10669242
    Abstract: The present invention relates to benzodiazepine derivative compounds of formula (I), or pharmaceutically acceptable salts thereof. The present benzodiazepine compounds are useful Clostridium difficile inhibitors in the treatment of Clostridium difficile infection in humans. The present invention provides a pharmaceutical composition containing benzodiazepine compounds of formula (I) and a method of making as well as a method of using the same in treating patients infected with Clostridium difficile infection by administering the same. The compounds of the present invention may be used in combination with additional antibiotics or anti-toxin antibody drugs.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: June 2, 2020
    Assignee: Venenum Biodesign, LLC
    Inventors: Jeffrey J. Letourneau, Andrew G. Cole, Brett A. Marinelli, Jorge G. Quintero
  • Patent number: 10604523
    Abstract: The present invention relates to novel 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]-quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. 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 PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabelled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron-emission tomography (PET).
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: March 31, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Ignacio Andrés-Gil, Peter Jacobus Johannes Antonius Buijnsters, Andrés Avelino Trabanco-Suárez, Meri De Angelis, Greta Constantia Peter Vanhoof, Jérôme Emile Georges Guillemont, Frederik Jan Rita Rombouts, Maarten Vliegen, Guy Maurits R. Bormans, Sofie Jeanne Leopoldine Celen
  • Patent number: 10597367
    Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: March 24, 2020
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Nicholas David Peter Cosford, Dhanya Raveendra-Panickar, Douglas J. Sheffler, John Howard Hutchinson, Reto Andreas Gadient
  • Patent number: 10561668
    Abstract: A method of treating a condition of in a human patient comprising pharmacologically activating a translocator protein of 18 kDa (TSPO), wherein the condition is one of a chronic methamphetamine addiction, a medical consequence of methamphetamine use; a behavioral consequence of methamphetamine use, an HIV associated cognitive motor disorder, an HIV-associated neurodegenerative disorder, and a neuroinflammatory response.
    Type: Grant
    Filed: June 4, 2018
    Date of Patent: February 18, 2020
    Assignee: BOARD OF SUPERVISORS OF LOUISIANA STATE UNIVERSITY
    Inventors: Nicholas E. Goeders, Christopher Dalton Schmoutz
  • Patent number: 10548846
    Abstract: A solid oral dosage form is provided, comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, tenofovir alafenamide or a pharmaceutically acceptable salt thereof, and emtricitabine or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: February 4, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Benjamin Micah Collman, Lei Hong, Joanna M. Koziara
  • Patent number: 10501424
    Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: December 10, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10501481
    Abstract: The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as ?-lactamase inhibitors and/or as antibacterial agents.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: December 10, 2019
    Assignee: MUTABILIS
    Inventors: Julie Brias, Sophie Chasset, Francis Chevreuil, Nicolas Lecointe, Benôit Ledoussal, Frédéric Le Strat, Sophie Vomscheid, Sébastien Richard, Fabien Faivre, Julien Barbion, Audrey Caravano, Géraldine Le Fralliec, Christophe Simon
  • Patent number: 10494353
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 14, 2018
    Date of Patent: December 3, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10494354
    Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 17, 2018
    Date of Patent: December 3, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10478408
    Abstract: A method of reducing the risk of medication-related overdose, death, or other injury associated with inappropriate consumption of alcohol in conjunction with prescription opioid analgesics, comprising: administering a combination medication having an effective amount of one or more opioid medications, and an effective amount of one or more aldehyde dehydrogenase inhibitors, in order to provide the powerful analgesic effects of the opioid in conjunction with a substance that prevents concomitant alcohol consumption, thereby reducing the risk of alcohol mediated opioid overdose or death. A combination medication, including an effective amount of one or more opioid medications, and an effective amount of one or more aldehyde dehydrogenase inhibitors and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: November 19, 2019
    Inventor: Michael Presti
  • Patent number: 10472337
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 14, 2018
    Date of Patent: November 12, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10464910
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 13, 2018
    Date of Patent: November 5, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Heather Davis, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair, David S. Millan, Matthew W. Martin
  • Patent number: 10457652
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 13, 2018
    Date of Patent: October 29, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Heather Davis, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair, David S. Millan, Matthew W. Martin
  • Patent number: 10426786
    Abstract: Provided are compositions comprising a benzodiazepine and a neurosteroid, containing one or both of the benzodiazepine and the neurosteroid in a subtherapeutic dose, and administration of such compositions for mitigation of an epileptic seizure. Further provided are compositions comprising a benzodiazepine, a neurosteroid, and an NMDA blocker, and administration of such compositions for mitigation of an epileptic seizure.
    Type: Grant
    Filed: July 13, 2017
    Date of Patent: October 1, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Michael A. Rogawski, Isaac N. Pessah, Zhengyu Cao, Pamela J. Lein
  • Patent number: 10421731
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: September 24, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin, Kenneth W. Bair
  • Patent number: 10398706
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: These compounds are useful for treating Respiratory Syncytial Virus (RSV) infection. The present invention further relates to pharmaceutical compositions comprising these compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering to the subject a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: January 5, 2018
    Date of Patent: September 3, 2019
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Brian C. Shook, In Jong Kim, Jianming Yu, Thomas P. Blaisdell, Joseph Panarese, Yat Sun Or
  • Patent number: 10272077
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: April 30, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • Patent number: 10272061
    Abstract: The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and/or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.
    Type: Grant
    Filed: November 10, 2016
    Date of Patent: April 30, 2019
    Assignee: ALLERGAN SALES, LLC
    Inventors: Charles D. Ebert, Steven W. Sanders
  • Patent number: 10225017
    Abstract: To improve the signal quality of the optical signal emitted by a reconfigurable transmitter after a reconfiguration event, an optical transmitter includes a modulator, a digital signal processor, and a controller. The modulator is for modulating light by a driving signal with a reconfigurable format. The digital signal processor is for processing digital data to be transmitted by using parameters in order to generate the driving signal. The controller is for controlling the digital signal processor changing the parameters so as to keep the driving signal stable before and after changing the reconfigurable format.
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: March 5, 2019
    Assignee: NEC CORPORATION
    Inventor: Emmanuel Le Taillandier De Gabory
  • Patent number: 10206931
    Abstract: The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: February 19, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: F. Anthony Romero, Steven R. Magnuson, Richard Pastor, Vickie Hsiao-Wei Tsui, Jeremy Murray, Terry Crawford, Daniel J. Burdick, Brian K. Albrecht, Alexandre Cote, Alexander M. Taylor, Christopher G. Nasveschuck, Yves LeBlanc, Michael Charles Hewitt, Kwong Wah Lai, Kevin Chen
  • Patent number: 10047075
    Abstract: The present disclosure provides pyridines and pyrimidines of Formula I and pharmaceutically acceptable salts and solvates thereof: wherein A, G, W1, W2, W3, and R5 are defined as set forth in the specification. The present disclosure also provides uses of the compounds of Formula I and pharmaceutically acceptable salts and solvates thereof. In certain embodiments, Compounds of the present disclosure are useful for treating pain. In another embodiment, Compounds of the present disclosure are useful for treating a disorder responsive to blockade of sodium channels, or alleviating symptoms of the disorder.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: August 14, 2018
    Assignee: Purdue Pharma L.P.
    Inventor: Stephen M. Lynch
  • Patent number: 10034859
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and their uses for the treatment and prophylaxis of visual hallucinations associated with Lewy Body dementia.
    Type: Grant
    Filed: July 15, 2016
    Date of Patent: July 31, 2018
    Assignee: Axovant Sciences GmbH
    Inventors: Lawrence Tim Friedhoff, Shankar Ramaswamy, Yandong Wen
  • Patent number: 10022383
    Abstract: A method of treating a condition of in a human patient comprising pharmacologically activating a translocator protein of 18 kDa (TSPO), wherein the condition is one of a chronic methamphetamine addiction, a medical consequence of methamphetamine use; a behavioral consequence of methamphetamine use, an HIV associated cognitive motor disorder, an HIV-associated neurodegenerative disorder, and a neuroinflammatory response.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: July 17, 2018
    Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
    Inventors: Nicholas E. Goeders, Christopher Dalton Schmoutz
  • Patent number: 10012777
    Abstract: The present invention provides a resin composition capable of forming a film exhibiting a small humidity-dependent variation in optical values; a triazole compound to be incorporated into the resin composition; an optical film and an optical lens, each of which is prepared from the resin composition and exhibits a small humidity-dependent variation in optical values; and a polarizing plate, a circularly polarizing plate, and an image display device, each of which includes the optical film and exhibits excellent moisture resistance. The resin composition of the present invention contains a resin and a compound having a 5-membered or 6-membered aromatic hydrocarbon or heterocyclic ring, wherein the resin is a hygroscopic resin, the compound has at least three specific aromatic rings having a specific NICS value, and the specific aromatic rings are bonded to one another via a single bond or one or two atoms.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: July 3, 2018
    Assignee: KONICA MINOLTA, INC.
    Inventors: Hiroyoshi Kiuchi, Takatugu Suzuki, Kiyoshi Fukusaka, Rie Fujisawa, Hiroshi Kita, Issei Nakahara
  • Patent number: 9994584
    Abstract: The present invention provides a process for producing the compound having the structure: comprising (a) reacting a compound having the structure: with a compound having the structure: in the presence of a first organic solvent under conditions sufficient to produce the compound, wherein the first organic solvent is a substituted benzene.
    Type: Grant
    Filed: October 14, 2015
    Date of Patent: June 12, 2018
    Assignee: Lixte Biotechnology, Inc.
    Inventors: Jason J. Piotrowski, Dumitru Ionescu
  • Patent number: 9890147
    Abstract: What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
    Type: Grant
    Filed: August 13, 2013
    Date of Patent: February 13, 2018
    Assignee: Bayer Pharma Aktiengesellshaft
    Inventors: Stephan Siegel, Stefan Bäurle, Arwed Cleve, Bernard Haendler, Amaury Ernesto Fernandez-Montalvan, Ursula Mönning, Sabine Krause, Pascale Lejeune, Norbert Schmees, Matthias Busemann, Simon Holton, Joachim Kuhnke
  • Patent number: 9868728
    Abstract: The invention relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the invention relates to inhibitors of NADPH-oxidase.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: January 16, 2018
    Assignee: Emory University
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Patent number: 9763876
    Abstract: The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: September 19, 2017
    Assignee: Hale Biopharma Ventures, LLC
    Inventors: Steve Cartt, David Medeiros, Garry Thomas Gwozdz, Andrew Loxley, Mark Mitchnick, David Hale, Edward T. Maggio
  • Patent number: 9730932
    Abstract: The present invention relates to an oral solid dosage form, in particular a tablet, comprising macitentan free base polymorphic form I.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: August 15, 2017
    Assignee: SANDOZ AG
    Inventors: Marijan Stefinovic, Johannes Raneburger, Ludwig Englmeier
  • Patent number: 9695156
    Abstract: Provided herein are compounds of Formula (I) or (II): (I) (II) pharmaceutically acceptable salts, tautomers, prodrugs, and stereoisomers thereof, and pharmaceutical compositions thereof, wherein X, RN, R1, R3, R4, p, and m are as defined herein. Such compounds and compositions have been found useful in the treatment or prevention of viral infections, e.g., polyomaviral infections, and are further envisioned useful in treatment or prevention of other pathogenic conditions associated with endosomal trafficking. Methods of treating or preventing an infection by a pathogen secreting an AB5 toxin is also contemplated.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: July 4, 2017
    Assignee: Brown University
    Inventors: Walter Atwood, Christian Nelson, Jason K. Sello, Daniel William Carney
  • Patent number: 9616123
    Abstract: The subject invention describes a method of use of Ropinirole™ to alleviate and control menopausal symptoms in women, and in particular, hot flashes. The invention describes the use of Ropinirole as a dopamine agonist with affinity for the dopamine D2, D3, or D4 receptors. Ropinirole may also be used to treat menopausal symptoms in conjunction with Tizanidine™ to further reduce the effects menopausal symptoms by providing a sedative and muscle relaxant effect which aids in sleep. The combination of Ropinirole and Tizanidine provides a useful new compound for treatment of menopausal symptoms that are most disruptive to the functioning in activities of daily living.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: April 11, 2017
    Inventor: Robert L. Knobler
  • Patent number: 9545414
    Abstract: In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: January 17, 2017
    Assignee: BRISTOL-MYERS SQUIBB & GILEAD SCIENCES, LLC
    Inventors: Terrence C. Dahl, Munir A. Hussain, Robert A. Lipper, Robert L. Jerzewski, Mark M. Menning, Reza Oliyai, Taiyin Yang
  • Patent number: 9492469
    Abstract: A method of treating a proliferative disease, such as cancer, is disclosed. The method comprises administering to a mammal in need thereof synergistically therapeutically effective amounts of: (i) (2R,3S)—N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-di-hydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide; (ii) 2-deoxy-2,2-difluorocytidine monohydrochloride (beta-isomer); and (iii) optionally, one or more additional anticancer agents.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: November 15, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventor: Francis Y. Lee
  • Patent number: 9468631
    Abstract: The subject invention describes a method of use of Ropinirole™ to alleviate and control menopausal symptoms in women, and in particular, hot flashes. The invention describes the use of Ropinirole as a dopamine agonist with affinity for the dopamine D2, D3, or D4 receptors. Ropinirole may also be used to treat menopausal symptoms in conjunction with Tizanidine™ to further reduce the effects menopausal symptoms by providing a sedative and muscle relaxant effect which aids in sleep. The combination of Ropinirole and Tizanidine provides a useful new compound for treatment of menopausal symptoms that are most disruptive to the functioning in activities of daily living.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: October 18, 2016
    Inventor: Robert L. Knobler
  • Patent number: 9408852
    Abstract: Enantiomerically-pure (S)-tofisopam is administered to lower serum uric acid levels in a mammal.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: August 9, 2016
    Assignee: PHARMOS CORPORATION
    Inventors: Judi Gidner, Karen Raudibaugh, Brian Speicher
  • Patent number: 9399145
    Abstract: The present invention relates to methods and compositions for modulating receptors in postsynaptic neurons of damaged or diseased retinas. The invention also related to methods for using the compositions set forth herein for treatment of diseases of hyperexcitability such as epilepsy.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: July 26, 2016
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: David R. Pepperberg, Karol Bruzik, Lan Yue, Michal Pawlowski, Haohua Qian
  • Patent number: 9382258
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, treat pain; (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: Grant
    Filed: April 22, 2015
    Date of Patent: July 5, 2016
    Assignee: AbbVie Inc.
    Inventors: Pramila A. Bhatia, John T. Randolph, Michael R. Schrimpf, Qingwei I. Zhang
  • Patent number: 9371335
    Abstract: The use of ORL-1 receptor antagonists of the formula: for the treatment of alcohol use disorders is described.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: June 21, 2016
    Assignee: Eli Lilly and Company
    Inventor: Linda Rorick Kehn
  • Patent number: 9346795
    Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: May 24, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
  • Patent number: 9315518
    Abstract: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: April 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hannah D. Fiji, Michael J. Kelly, III, Jeffrey C. Kern, Mark E. Layton, Joseph E. Pero, Alexander J. Reif, Michael A. Rossi
  • Patent number: 9283212
    Abstract: The present invention relates to unique delivery systems and the use of an imidazobenzodiazepine derivative, such as flumazenil either alone or in combination with other receptor antagonists in the treatment of disease or medical disorders.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: March 15, 2016
    Assignee: PALMAYA PTY LTD
    Inventor: Alexander George Brian O'Neil
  • Patent number: 9273304
    Abstract: The present invention relates to the field of thermostable enzymes, methods for their inactivation, and related uses, kits and reagents. In particular, the invention relates to a method for reversible inactivation of thermophilic enzymes by chemical modification under aqueous or non-aqueous conditions.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: March 1, 2016
    Assignee: Thermo Fisher Scientific Baltics UAB
    Inventors: Arunas Lagunavicius, Daiva Tauraite, Jurgita Barkauskaite, Leonas Grinius
  • Patent number: 9266890
    Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, AbI, DCAMKL1, ABL1, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS 1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, AxI, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: February 23, 2016
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Xianming Deng, Nicholas P. Kwiatkowski
  • Patent number: 9248192
    Abstract: A pH sensitive carrier which includes at least one pH sensitive compound selected from the group consisting of deoxycholic acid, cholic acid, ursodeoxycholic acid, chenodeoxycholic acid, hyodeoxycholic acid, C27 bile acid, glycodeoxycholic acid, glycyrrhizic acid, glycyrrhetinic acid and salts thereof, and at least one amphipathic substance selected from the group consisting of a phosphatidylcholine having 10 to 12 carbon atoms, a polyoxyethylene sorbitan monofatty acid ester having 12 to 18 carbon atoms, a sorbitan fatty acid ester having 16 to 18 carbon atoms, glycerol monooleate, glycerol dilaurate, glycerol distearate, glycerol dioleate, polyoxyethylene castor oil and ?-tocopherol, and which is capable of developing a membrane disruptive function promoting effect.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: February 2, 2016
    Assignee: TERUMO KABUSHIKI KAISHA
    Inventor: Naoki Sakaguchi
  • Patent number: 9249100
    Abstract: Organophosphate (OP) nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Though oxime nucleophiles can reactivate an AChE-phosphyl adduct, the adduct can undergo a reaction called aging, leading to an aged-AChE adduct. The invention provides compounds and methods that can be used to reactivate an aged-AChE adduct. Such compounds and methods are useful to counteract organophosphorus poisoning.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: February 2, 2016
    Assignee: University of Iowa Research Foundation
    Inventors: Daniel M. Quinn, Joseph John Topczewski
  • Patent number: 9193710
    Abstract: The present invention relates to novel benzodiazepinone compounds of Formulae (I) wherein R1, R2, R4, R6, R7, R8, R9, and R10 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, methods of use of such compounds and compositions, and methods for preparing the compounds and compositions. The compounds are Group II metabotropic glutamate antagonists or allosteric modulators and are useful for the treatment of a variety of CNS disorders.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: November 24, 2015
    Assignee: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
    Inventors: John Howard Hutchinson, Leo Bleicher, Nick Cosford, Robert John Ardecky, Jiwen Zou
  • Patent number: 9181259
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: November 10, 2015
    Assignee: LEO PHARMA A/S
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
  • Patent number: 9180193
    Abstract: The present invention discloses compounds of Formulae I and II, wherein the variables in Formulae I and II are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formulae I and II in the treatment of HCV infection.
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: November 10, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: John A. Brinkmann, Hongju Li, Ramakanth Sarabu, Sung-Sau So
  • Patent number: RE46397
    Abstract: Particles of an organic acid salt of an amino acid amide or ester local anesthetic are employed as agents for the improved alleviation of pain. Particularly, the particles find use with surgically created wounds, where the particles may be administered directly into the bed of the wound or topically for transdermal transport.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: May 9, 2017
    Assignee: SVIP5 LLC
    Inventors: Samuel P. Sawan, Daniel Jacobs, Tadmor Shalon