C=x Bonded Directly To The Piperidine Ring (x Is Chalcogen) Patents (Class 514/330)
  • Patent number: 11191839
    Abstract: A pharmaceutical composition for treating infertility in a female subject substantially consists of local anesthetic of amide type such as lidocaine, human albumin, viscosity controlling agent selected from recombinant hyaluronic acid and combination of recombinant hyaluronic acid and water-soluble cellulose ether, optionally citrate, glucose, and/or amino acid, water optionally comprising one or more ions selected from the group consisting of sodium, potassium, magnesium, calcium, acetate, chloride, sulfate. Also disclosed is a method of treating infertility by administration of the composition to a female subject in need thereof.
    Type: Grant
    Filed: October 11, 2016
    Date of Patent: December 7, 2021
    Assignee: ISIFER AB
    Inventor: Jack Spira
  • Patent number: 11074998
    Abstract: The present invention relates to a system and method for real-time delivery of medical tests and related data from laboratories (12) or similar sources (18) to portable communication devices such as mobile phones (14), text-enabled pagers (14) and web-enabled personal digital assistance (PDA's) (14) and other WAP devices (14). The subject system enables physicians to access test results remotely as soon as they become available. Also, the system allows the physician to develop an electronic prescription and submit the electronic prescription to a pharmacy using the portable communications device (14).
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: July 27, 2021
    Assignee: INSTANTDX, LLC
    Inventors: Lance A. Liotta, Tyson Liotta
  • Patent number: 11058695
    Abstract: A compound having Formula I is an inhibitor of carbapenem-hydrolyzing class D beta-lactamases. The compound inhibits the activities of clinically-important and emerging subgroups of carbapenem-hydrolyzing class D beta-lactamases. A method of treating a bacterial infection includes administering to a subject suffering from a bacterial infection a composition including an effective amount of the compound having Formula I or the pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 8, 2019
    Date of Patent: July 13, 2021
    Assignee: MYONGJI UNIVERSITY INDUSTRY AND ACADEMIA COOPERATION FOUNDATION
    Inventors: Sang Hee Lee, Jung Hun Lee, Jeong Ho Jeon
  • Patent number: 10881649
    Abstract: A therapeutic agent or a preventive agent for alopecia areata has an ROR? antagonistic activity, and, there is a therapeutic agent or a preventive agent for alopecia areata, including a cyclic amine derivative typified by the following compound or a pharmacologically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: January 5, 2021
    Assignee: Toray Industries, Inc.
    Inventors: Rie Sasaki, Shinnosuke Hayashi, Martial Vallet, Shinya Yokosaka, Kazuya Osumi, Takumi Aoki, Hiroyuki Meguro, Mie Kaino, Kozue Takagaki, Takehiro Takahashi
  • Patent number: 10758626
    Abstract: The present invention relates in general to polymer-bioactive agent conjugates for delivering a bioactive agent to a subject. The polymer-bioactive agent conjugates contain triazole moieties in the polymer backbone and a bioactive moiety selected from quinolones, NSAIDs and mixtures thereof. The present invention also relates to methods for preparing the polymer conjugates using click cycloaddition chemical reactions, to monomer-bioactive agent conjugates suitable for preparing the polymer conjugates, and to pharmaceutical products comprising the polymer conjugates for the post-surgical care to treat or prevent infections, provide analgesia and treat inflammation.
    Type: Grant
    Filed: September 9, 2016
    Date of Patent: September 1, 2020
    Assignee: POLYACTIVA PTY LTD
    Inventors: Stephen Lonsdale Birkett, Andrew Craig Donohue, Asha Marina D'Souza, Sarah Man Yee Ng, Adrian Sulistio, Russell John Tait, David Valade, Alan Naylor, Anton Blencowe
  • Patent number: 10716750
    Abstract: The present invention relates to a topical ophthalmic formulation comprising at least one antagonist of the endothelin receptor, preferably selected from sitaxentan, ambrisentan, atrasentran, bosentan, macitentan and tezosentan, or a mixture thereof, more preferably bosentan. It also relates to the use of a topical ophthalmic formulation comprising at least one antagonist of the endothelin receptor, preferably selected from sitaxentan, ambrisentan, atrasentran, bosentan, macitentan and tezosentan, or a mixture thereof, more preferably bosentan, as active ingredient for preventing and/or treating the retinal neurodegeneration induced by diabetes and/or aging.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: July 21, 2020
    Assignee: Retinset, S.L.
    Inventors: Vicente Duran Muiños, Marta Guerrero Martínez, Cristina Hernández Pascual, José Bruno Montoro Ronsano, Rafael Simó Canonge, José Maria Suñé Negre, José Ramón Ticó Grau
  • Patent number: 10660897
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: May 26, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 10383883
    Abstract: A decongestant composition is provided comprising: (a) a safe and effective amount of an adrenergic compound; (b) a safe and effective amount of a steroid; and (c) a pharmaceutically-acceptable carrier. Methods of treating congestion in a human or animal subject are also provided comprising administering to the subject a composition comprising: (a) an adrenergic compound; and (b) a steroid; where the daily dose of the adrenergic compound administered to the subject is from about 1 ?g to about 800 ?g, and the daily dose of the steroid administered to the subject is from about 1 ?g to about 400 ?g.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: August 20, 2019
    Inventor: Richard A. Wandzel
  • Patent number: 10376595
    Abstract: The present invention relates to inhibitors of C5a activity and their use in the treatment of cutaneous, neutrophilic, inflammatory diseases in a subject.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: August 13, 2019
    Assignee: InflaRx GmbH
    Inventors: Renfeng Guo, Niels C. Riedemann
  • Patent number: 10314833
    Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: June 11, 2019
    Assignee: The Children's Medical Center Corporation
    Inventors: Charles Berde, Daniel S. Kohane
  • Patent number: 10206876
    Abstract: The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a local anesthetic in the form of a clear oily solution and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: February 19, 2019
    Assignee: PAINREFORM LTD.
    Inventors: Shimon Amselem, Michael Naveh
  • Patent number: 10149975
    Abstract: A transcutaneous electronic nerve stimulation device configured to provide therapy to a patient includes a control unit assembly, a power source, and a therapy plate electrically coupled to the power source. The therapy plate includes an electrical source configured to deliver electrical stimulation to the patient, a heat source configured to deliver heat to the patient, and a radiation source configured to deliver radiation to the patient. The transcutaneous electronic nerve stimulation device further includes a rigid connector electrically coupling the therapy plate to the power source such that the therapy plate is fixed relative to the power source.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: December 11, 2018
    Assignee: EASYWELL BIOMEDICALS, INC.
    Inventor: Cheng-Lin Chuang
  • Patent number: 10098872
    Abstract: The present invention is an analgesic for pain control not limited to postoperative pain control. The present invention discloses an opioid sparing anesthetic formulation comprising a local anesthetic, an N-methyl-D-aspartate (NMDA) receptor antagonist, and a cyclooxygenase (COX) inhibitor such as Bupivacaine, Ketamine, and Ketorolac, which is effective to significantly reduce postoperative nausea and vomiting and enhance postoperative pain relief as compared to existing prior art anesthetics. The formulation is administered to a mammal in need of pain treatment. The formulation may be used as a preemptive analgesic. The analgesic formulation has a buffer for enhancing its shelf life.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: October 16, 2018
    Inventor: William Bradley Worthington
  • Patent number: 10053450
    Abstract: Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
    Type: Grant
    Filed: July 5, 2016
    Date of Patent: August 21, 2018
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu, Allan S. Wagman
  • Patent number: 9815787
    Abstract: The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: November 14, 2017
    Assignee: University of Tsukuba
    Inventors: Hiroshi Nagase, Takashi Nagahara
  • Patent number: 9737550
    Abstract: A decongestant composition is provided comprising: (a) a safe and effective amount of an adrenergic compound; (b) a safe and effective amount of a steroid; and (c) a pharmaceutically-acceptable carrier. Methods of treating congestion in a human or animal subject are also provided comprising administering to the subject a composition comprising: (a) an adrenergic compound; and (b) a steroid; where the daily dose of the adrenergic compound administered to the subject is from about 1 ?g to about 800 ?g, and the daily dose of the steroid administered to the subject is from about 1 ?g to about 400 ?g.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: August 22, 2017
    Inventor: Richard A. Wandzel
  • Patent number: 9688624
    Abstract: Described herein is the DP2 antagonist 2-(3-(2-((tert-butylthio)methyl)-4-(2,2-dimethyl-propionylamino)phenoxy)-4-methoxyphenyl)acetic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the DP2 antagonist, or a pharmaceutically acceptable salt thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the DP2 antagonist, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory diseases or conditions, allergic diseases or conditions, inflammatory diseases or conditions, as well as other prostaglandin D2-dependent or prostaglandin D2-mediated diseases or conditions.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: June 27, 2017
    Assignee: Brickell Biotech, Inc.
    Inventors: Jason Edward Brittain, Christopher David King, Brian Andrew Stearns
  • Patent number: 9617224
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: April 11, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Patent number: 9617197
    Abstract: The present application discloses compositions and methods useful for treating and preventing inflammation associated with inflammatory diseases and disorders.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: April 11, 2017
    Assignee: University of Virginia Patent Foundation
    Inventors: Yun Michael Shim, Mikell Paige
  • Patent number: 9402838
    Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 13, 2015
    Date of Patent: August 2, 2016
    Assignee: Eli Lilly and Company
    Inventors: Matthew Allen Schiffler, Jeremy Schulenburg York
  • Patent number: 9399194
    Abstract: Draw solutions comprising at least one N-cyclicalkyl-cycloalkylamine and a secondary solvent. The N-cyclicalkyl-cycloalkylamine comprises the chemical structure: wherein n is 0, 1, or 2, n? is 0, 1, or 2, and each of R1-R6 is independently selected from the group consisting of an alkyl group, an alkoxy group, an acetyl group, an aryl group, a hydrogen group, a hydroxyl group, and a phosphorus-containing group. Methods of treating a liquid using the draw solution are also disclosed.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: July 26, 2016
    Assignee: Battelle Energy Alliance, LLC
    Inventors: Aaron D. Wilson, Christopher J. Orme
  • Publication number: 20150147378
    Abstract: Biocompatible, biodegradable copolymer-xerogel nanocomposites contain a biodegradable, biocompatible copolymer, silica nanoparticles and one or more therapeutic agents, that are useful for wound dressings, medical devices and drug delivery applications.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 28, 2015
    Inventors: David Devore, Paul Ducheyne, Marius C. Costache
  • Publication number: 20150148325
    Abstract: The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a hydrophobic active pharmaceutical ingredient (API) of low water solubility but readily dissolved in alcohols and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 28, 2015
    Inventors: Shimon Amselem, Michael Naveh
  • Publication number: 20150148899
    Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.
    Type: Application
    Filed: February 2, 2015
    Publication date: May 28, 2015
    Inventor: Perry ROSENTHAL
  • Publication number: 20150148379
    Abstract: The present invention relates to an acetaminophen injectable aqueous solution for use in the treatment or in the prevention of pain by spinal administration, wherein said acetaminophen injectable solution is supersaturated. In certain embodiments, the acetaminophen injectable aqueous solution is administered simultaneously, separately or sequentially with a local anaesthetic by spinal administration.
    Type: Application
    Filed: June 27, 2013
    Publication date: May 28, 2015
    Inventors: Augusto Mitidieri, Elisabetta Donati, Nicola Caronzolo
  • Publication number: 20150148355
    Abstract: A silicone gel (“silogel”) composition used to deliver pharmaceutical products transdermally as well as a method for producing the silogel composition, which may contain up to 80% additive ingredients. Preferred embodiments of the invention may include silogel compositions which provide high viscosity/no separation due to API. They are not temperature-sensitive, have no shear stress from the ointment mill/EMP, have no gumming up/stickiness, and no hardening.
    Type: Application
    Filed: November 24, 2014
    Publication date: May 28, 2015
    Inventor: John Olin Trimble
  • Publication number: 20150141425
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: November 3, 2014
    Publication date: May 21, 2015
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20150140133
    Abstract: A system is described for long-term controlled release delivery of a drug or a therapeutic agent. According to the invention, one or more drugs or therapeutic agents contained in microspheres are mixed with a temperature sensitive hydrogel which is then introduced directly to the desired situs of the drug or therapeutic agent. The temperature sensitive hydrogel may also contain a drug or a therapeutic agent, for example, a pain relieving drug, for a short-term controlled release. The temperature sensitive hydrogel is in liquid state at room temperature, but upon injection, shortly becomes gelatinous. This system is particularly suitable for treatment of diseases, disorders, or conditions, for example, tumors, discogenic back pain, or arthritis, warranting localized administration of a drug or a therapeutic agent. In addition, the specification provides a method for production of a drug- or therapeutic agent-containing microspheres.
    Type: Application
    Filed: December 4, 2014
    Publication date: May 21, 2015
    Inventor: Tae-Hong Lim
  • Publication number: 20150133502
    Abstract: The disclosure provides for means for a method to facilitate food intake and food retention in a mammal by applying a sufficient dose of a local anesthetic drug in the lumen of the pharyngeal-esophageal-gastric-duodenal tract before or during or after eating. The local anesthetic can be amethocaine, articaine, benzocaine, bupivacaine, chloroprocaine, cinchocaine, cyclomethycaine, dibucaine, diethocaine, etidocaine, larocaine, levobupivacaine, lidocaine, lignocaine, mepivacaine, novocaine, piperocaine, prilocaine, procaine, proparacaine, propoxycaine, QX-222, QX-314, ropivacaine, tetracaine, trimecaine, menthol, eugenol or a safe pharmaceutical formulations of tetrodotoxin, saxitoxin, or neosaxitoxin. The disclosure is useful for patients having problems with food intake or food retention.
    Type: Application
    Filed: May 15, 2013
    Publication date: May 14, 2015
    Applicant: Chardon Group B.V.
    Inventors: Christophorus Louis Eduard Broekkamp, Bernardus Wijnand Mathijs Marie Peeters
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Publication number: 20150126494
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
  • Publication number: 20150126481
    Abstract: The present disclosure is drawn to an adhesive peel-forming formulation for dermal delivery of a drug, comprising a drug, a solvent vehicle, and a polymer peel-forming agent. The solvent vehicle can comprise a volatile solvent system comprising one or more volatile solvent, and a non-volatile solvent system comprising two or more non-volatile solvents. The non-volatile solvent system can have a solubility with respect to the drug that is within a window of operable solubility such that the drug is deliverable at therapeutically effective rates over a sustained period of time.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Inventors: Jie Zhang, Kevin S. Warner, Michael A. Ashburn, Larry D. Rigby, Suyi Niu
  • Publication number: 20150126555
    Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 13, 2015
    Publication date: May 7, 2015
    Inventors: Matthew Allen SCHIFFLER, Jeremy Schulenburg YORK
  • Publication number: 20150126556
    Abstract: The invention generally relates to methods of using adrenergic receptor agonists for the treatment of skin and mucosal superficial wounds. Some of the preferred adrenergic receptor agonists include epinephrine, phenylephrine, norepinephrine, methoxamine, and mixtures thereof. Methods according to the invention are especially effective to control superficial skin and mucosal bleeding and accelerate healing time.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventor: Roman Kelner
  • Publication number: 20150119423
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of local pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of moderate to severe pain, neuropathic pain, post herpetic neuralgia and rheumatic pains.
    Type: Application
    Filed: May 18, 2013
    Publication date: April 30, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150111924
    Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.
    Type: Application
    Filed: August 20, 2014
    Publication date: April 23, 2015
    Applicant: DURECT CORPORATION
    Inventor: Adrian Neil Verity
  • Publication number: 20150111923
    Abstract: The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a local anesthetic in the form of a clear oily solution and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Shimon Amselem, Michael Naveh
  • Publication number: 20150110852
    Abstract: A system for dermal delivery of lidocaine, bupivacaine, diclofenac, or ketoprofen is provided which comprises at least two components, for example, a sheet of a solid and flexible material, and a vehicle liquid comprising a solvent and optionally other ingredients. A drug, selected from group consisting of lidocaine, bupivacaine, diclofenac, and ketoprofen, can be impregnated in the sheet or contained in the vehicle liquid. These two components can be stored separately and joined either shortly before or at the time of application. To use the system, the vehicle liquid may be applied either on the target skin area or on the sheet, and the sheet may then be applied on the target skin area so that the vehicle liquid is positioned between the sheet and the skin and brought into contact with the ingredients impregnated in the sheet.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 23, 2015
    Inventor: Jie Zhang
  • Publication number: 20150111749
    Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.
    Type: Application
    Filed: December 31, 2014
    Publication date: April 23, 2015
    Inventors: Huazhang Huang, Ratnakar Asolkar
  • Patent number: 9012477
    Abstract: A method for treating subjects experiencing neuropathic pain is provided. The method involves the application of a solid-forming local anesthetic formulation to a skin surface of the subject experiencing the neuropathic pain and then maintaining the formulation on the skin surface for a period of time sufficient to allow itself to transdermally deliver the local anesthetic to the subject thereby providing relief from the neuropathic pain within about 45 minutes.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: April 21, 2015
    Assignee: Nuvo Research Inc.
    Inventors: Jie Zhang, Robert Lippert
  • Publication number: 20150105426
    Abstract: The invention relates to novel formulations for topical local anaesthesia and for the use thereof as analgesics, antalgics, or as sexual retardants.
    Type: Application
    Filed: December 4, 2012
    Publication date: April 16, 2015
    Applicant: UNIVERSITE PARIS DESCARTES
    Inventors: Mathieu Lazerges, Philippe Espeau, Sylvie Sophie Crauste-Manciet, Denis Brossard, Yohann Corvis, Florence Agnely, Nicolas Huang
  • Publication number: 20150105425
    Abstract: The present invention is directed to kits and methods for the treatment of a patient suffering from post-traumatic stress disorder (PTSD) and/or hot flashes by an administration of a mixture produced by a combination of a long acting local anesthetic combined with clonidine. The combination of the two pharmaceuticals produces a significant increase in duration and speed of onset of sympathetic blockade, increased intensity of the sympathetic blockage as well as the reduction of local anesthetic absorption locally. The combination significantly improves the efficacy, speed of onset and block intensity of a right sided cervical sympathetic ganglion injection (RCSGI) leading to increased length of resolution of PTSD and hot flashes as well as reducing the potential for complications related to absorption of the local anesthetic.
    Type: Application
    Filed: March 4, 2014
    Publication date: April 16, 2015
    Inventor: Eugene Lipov
  • Patent number: 9006228
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
  • Patent number: 9006249
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: April 14, 2015
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Publication number: 20150086604
    Abstract: Biodegradable polymer-coated surgical meshes formed into pouches are described for use with cardiac rhythm management devices (CRMs) and other implantable medical devices. Such meshes are formed into a receptacle, e.g., a pouch or other covering, capable of encasing, surrounding and/or holding the cardiac rhythm management device or other implantable medical device for the purpose of securing it in position, inhibiting or reducing bacterial growth, providing pain relief and/or inhibiting scarring or fibrosis on or around the CRM or other implantable medical device. Preferred embodiments include surgical mesh pouches coated with one or more biodegradable polymers that can act as a stiffening agent by coating the filaments or fibers of the mesh to temporarily immobilize the contact points of those filaments or fibers and/or by increasing the stiffness of the mesh by at least 1.1 times its original stiffness.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 26, 2015
    Inventors: Fatima Buevich, Frank Do, William McJames, Satish Pulapura, William Edelman, Arikha Moses, Mason Diamond, Shari Timothy
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20150087674
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of severe pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of postoperative pain, cancer pain, kidney stones pain, fractures, local pain, chronic pain, chemotherapy induced pain, neuropathic pain, post herpetic neuralgia, neuralgia, motor neurone disease, diabetic neuropathy, postherpetic neuralgia, injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, cancer pain and lower back pain.
    Type: Application
    Filed: February 23, 2013
    Publication date: March 26, 2015
    Inventor: Mahesh KANDULA
  • Publication number: 20150087629
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat