Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
  • 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: 9181245
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2- a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: May 16, 2013
    Date of Patent: November 10, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Frederik Jan Rita Rombouts, Andrés Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • Patent number: 9096546
    Abstract: The aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepine derivative compounds of the present invention are represented by formulae 1(A-D) having the following structure: where the substituents X and R1-R8 are as defined herein.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 4, 2015
    Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb Company
    Inventors: Peter R. Guzzo, Bruce F. Molino, Wenge Cui, Shuang Liu, Richard E. Olson, Larry Yet
  • Patent number: 9079030
    Abstract: A protocol or procedure is provided for lowering sympathetic nervous system arousal in a person in order to prepare that person for a medical or dental procedure. First, a therapeutic dosage of one or more neurotransmitter supplements, such as a gamma aminobutyric acid formulation, a tryptophan-derived neurotransmitter precursor, and dehydroepiandrosterone are administered to the patient. Concomitantly, gelled electrodes are placed adjacent or below the mastoid. The gelled electrodes are connected to a cranial electrotherapy stimulation device that administers a sub-sensation level current to the patient. Also, a noise dampening headset is placed on the patient and a neuroacoustic entrainment recording or program is played. Next, light is blocked with black out glasses. Then, the medical or dental procedure is performed.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: July 14, 2015
    Inventor: G. Blake Holloway
  • Patent number: 9056857
    Abstract: Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: where X, R1, R2, subscript m, subscript n and subscript v are as defined herein.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: June 16, 2015
    Assignee: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Lei Zhu, Yueming Li
  • Publication number: 20150147282
    Abstract: The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: November 24, 2014
    Publication date: May 28, 2015
    Inventors: Fredrik JOABSSON, Margareta LINDEN, Krister THURESSON, Fredrik TIBERG
  • Publication number: 20150148339
    Abstract: The provided embodiments are based in some aspects on the demonstration herein of a role for gastrin in regulating the aging gut-ovary axis and effects of targeting gastrin activity in reversing gastrin-mediated bone loss. Provided are methods, compositions and agents, including gastrin antagonists, for treatment, amelioration, and prevention of bone diseases and conditions. Methods for treating a bone disease or condition associated with hypergastrinemia in a subject in need thereof may comprise administering to the subject at least one dose of a therapeutically effective amount of a gastrin receptor-targeting agent, thereby treating the bone disease or condition associated with hypergastrinemia.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Irvin Mark Modlin, Mark Kidd
  • Patent number: 9040508
    Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: May 26, 2015
    Assignee: VM Pharma LLC
    Inventors: Jay Jie-Qiang Wu, Ling Wang
  • Publication number: 20150141411
    Abstract: The present invention is concerned with novel substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, R5, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Frederik Jan Rita Rombouts, Andres Avelino Trabanco-Suarez, Henricus Jacobus Maria Gijsen, Gregor James Macdonald, Francois Paul Bischoff, Sergio-Alvar Alonso-de-Diego, Adriana Ingrid Velter, Yves Emiel Maria Van Roosbroeck
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Publication number: 20150140127
    Abstract: Provided is a method for detecting injury to the brain comprising: a) determining the level of a tight junction (TJ) protein in exosomes isolated from a test sample from a subject, wherein the TJ protein is occludin, claudin-3, claudin-5, claudin-12, ZO-1, ZO-2, ZO-3, JAM-A, JAM-B or JAM-C, or any combination thereof; b) comparing the level of the TJ protein in the test sample to the level of the TJ protein in a control sample, wherein an elevated level of the TJ protein in the test sample relative to the level of the TJ protein in the control sample indicates that the subject has an injury to the brain.
    Type: Application
    Filed: June 25, 2013
    Publication date: May 21, 2015
    Applicant: TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Servio H. Ramirez, Slava Rom, Yuri Persidsky
  • Patent number: 9034868
    Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.
    Type: Grant
    Filed: November 19, 2013
    Date of Patent: May 19, 2015
    Assignees: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Daniel Gillet, Julien Barbier, Ludger Johannes, Bahne Stechmann, Siau-Kun Bai
  • Publication number: 20150133437
    Abstract: The invention provides tetrahydro[1,8]naphthyridine and related compounds, methods of promoting RORy activity and/or increasing the amount of iL-17 in a subject, and therapeutic uses of the tetrahydro[1,8]naphthyridine and related compounds. In particular, the invention provides sulfonamide-tetrahydro[1,8]naphthyridine and related compounds, methods of using such compounds to promote RORy activity and/or increase the amount of iL-17 in a subject, and treat medical conditions in which activation of immune response would be beneficial such as in cancer and infections.
    Type: Application
    Filed: May 8, 2013
    Publication date: May 14, 2015
    Inventors: Thomas D. Aicher, Peter L. Toogood, Xiao Hu
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Patent number: 9029361
    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: December 10, 2013
    Date of Patent: May 12, 2015
    Assignee: AbbVie Inc.
    Inventors: Pramila A. Bhatia, John T. Randolph, Michael R. Schrimpf, Qingwei I. Zhang
  • Patent number: 9029366
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: May 12, 2015
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • Publication number: 20150118301
    Abstract: Described are oral dosage forms that contain abuse-deterrent features and that contain core-shell polymers that include an active pharmaceutical ingredient, with particular examples including immediate release dosage forms that contain a drug that is commonly susceptible to abuse.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Inventors: Dinesh K. Haswani, Derek V. Moe, Victoria A. O'Neill, Manuel A. Vega Zepeda
  • Publication number: 20150118302
    Abstract: Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses.
    Type: Application
    Filed: October 29, 2014
    Publication date: April 30, 2015
    Inventors: Dinesh K. Haswani, Derek V. Moe, Victoria A. O'Neill, Manuel A. Vega Zepeda
  • 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