The Nitrogen In R Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Bonding Patents (Class 514/620)
  • Patent number: 10226460
    Abstract: The present invention provides pharmaceutically acceptable salts of enantiomerically pure (R)-pirlindole and (S)-pirlindole compounds having an increased bioavailability profile for use in medicine.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: March 12, 2019
    Assignee: TECNIMEDE SOCIEDADE TECNICO-MEDICINAL S.A.
    Inventors: Augusto Eugenio Pardal Filipe, Pedro Filipe Eufrasio Pedroso, Susana Marques Almeida Pecorelli, Carlos Alberto Eufrasio Casimiro Caixado, Ana Sofia da Conceicao Lopes, Joao Carlos Ramos Damil, Pedro Paulo de Lacerda E Oliveira Santos
  • Patent number: 10045955
    Abstract: The present invention is directed to an aqueous gel composition containing a local anesthetic, a lubricating agent, and a preservative and methods of treating vulvovaginal pain, such as dyspareunia by topically administering said composition.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: August 14, 2018
    Assignee: ELLE PHARMACEUTICAL, LLC
    Inventors: Elias Reichel, Lauren Oshry
  • Patent number: 9814712
    Abstract: (S)-pirlindole or its pharmaceutically acceptable salts, as well as pharmaceutical compositions comprising the same for use in the therapeutic treatment and prevention of pain.
    Type: Grant
    Filed: May 9, 2014
    Date of Patent: November 14, 2017
    Assignee: TECNIMEDE SOCIEDADE TECNICO-MEDICINAL S.A.
    Inventors: Augusto Eugenio Pardal Filipe, Pedro Filipe Eufrasio Pedroso, Susana Marques Almeida Pecorelli, Carlos Alberto Eufrasio Casimiro Caixado, Ana Sofia da Conceicao Lopes, Joao Carlos Damil
  • Patent number: 9308183
    Abstract: The present invention is directed to the use of a class of peptide compounds for treating diseases associated with hyperexcitability. The present invention is also directed to the use of a class of peptide compounds for treating diseases associated with dysfunction of an ion channel.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: April 12, 2016
    Assignee: UCB PHARMA GMBH
    Inventors: Cara Heers, Thomas Stoehr, Bettina Beyreuther
  • Patent number: 9242928
    Abstract: A compound represented by the following General Formula (I): where, in General Formula (I), R1 and R2 each represent an alkyl group which may have a substituent, R3 represents the following General Formula (II) or (III), and R1 and R2 may be identical or different, where, in General Formulas (II) and (III), X represents a hydrogen atom or a halogen atom, R4 represents a methyl group, a dimethyl group or an oxygen atom, and * represents a binding position.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: January 26, 2016
    Assignee: FUJITSU LIMITED
    Inventors: Nozomu Kamiya, Atsushi Tomonaga, Hajime Sugiyama
  • Publication number: 20150148424
    Abstract: The present invention relates to stable dosage forms of levomilnacipran and pharmaceutically acceptable salts thereof. Processes for the preparation of these dosage forms and methods of using these dosage forms are also described.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: Anil Chhettry, Murali Divi, Rahul Surana
  • Publication number: 20150141437
    Abstract: The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.
    Type: Application
    Filed: June 10, 2013
    Publication date: May 21, 2015
    Inventors: Hubert Gstach, Peter Chiba, Matthias Mastalir
  • Publication number: 20150133407
    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 respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 14, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150132358
    Abstract: A method and apparatus for administering an active agent such as a medicine to a subject, uses an ocular implant such as a punctal plug, to which the active agent has been applied. The implant is installed at the eye of the subject for administering the active agent via tissues of the eye.
    Type: Application
    Filed: August 29, 2014
    Publication date: May 14, 2015
    Inventors: Steven A. Odrich, Liane C. Glazer
  • Publication number: 20150087610
    Abstract: The present invention provides methods and compositions for modifying fertility in a male mammalian subject by contacting the subject's testis cells, germ cells or sperm with a sufficient amount of a composition comprising a ligand that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Also described are methods for screening a test molecule for its effect on fertility by examining changes in male germ cells, testis cells or sperm resulting from contact with a molecule that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Compositions for modifying fertility in a mammalian subject, e.g., contraceptive products, include a ligand that binds, inhibits or activates a TAS2R receptor in a pharmaceutically acceptable carrier.
    Type: Application
    Filed: March 18, 2013
    Publication date: March 26, 2015
    Applicant: Monell Chemcial Senses Center
    Inventors: Liquan Huang, Jiang Xu
  • Publication number: 20150038574
    Abstract: Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: February 5, 2015
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Judd Berman, Tan Quach
  • Publication number: 20150038587
    Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Rahul Surana, Mahendra G. Dedhiya
  • Patent number: 8946297
    Abstract: To provide an anthranilamide formulation compound for improving pest controlling effects. A solid composition for pest control which comprises an amorphous anthranilamide compound or its salt as a pesticidal active ingredient, a nonionic surfactant and/or an anionic surfactant and a mineral carrier.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: February 3, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Masayuki Morita, Takao Awazu, Akira Nakagawa, Taku Hamamoto
  • Publication number: 20150017099
    Abstract: The invention provides methods and compositions for the diagnosis, prognosis and treatment of respiratory tract diseases. Specifically, the invention provides diagnosis, prognosis and treatment of respiratory infections using bitter and sweet taste signal transduction pathways. In one aspect, the invention relates to a method for treating a respiratory infection by administering a composition to the respiratory tract of a subject in an amount capable of activating bitter taste signaling and/or inhibiting sweet taste signaling. The composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract. In another aspect, the invention relates to a composition for treatment of a respiratory infection. Such composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 15, 2015
    Inventors: Noam A. Cohen, Robert J. Lee, Danielle R. Reed
  • Publication number: 20140357634
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
  • Patent number: 8901176
    Abstract: New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: December 2, 2014
    Assignee: Newron Pharmaceuticals, S.P.A.
    Inventors: Ruggero Fariello, Carlo Cattaneo, Patricia Salvati, Luca Benatti
  • Publication number: 20140350019
    Abstract: The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 27, 2014
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: John Feutrill, Caroline Leriche, David Middlemiss
  • Publication number: 20140350017
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: November 8, 2013
    Publication date: November 27, 2014
    Applicants: The University of Utah, Curza Global, LLC
    Inventors: Dustin Williams, Ryan Looper, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hari Kanna Reddy
  • Publication number: 20140350116
    Abstract: The invention provides methods for enhancing histone acylation, learning, memory and/or cognition in subjects with compound (I) or compositions comprising compound (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 11, 2012
    Publication date: November 27, 2014
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY INTHE CITY OF NEW YORK
    Inventors: Yitshak Francis, Ottavio Arancio, Mauro Fa
  • Publication number: 20140348774
    Abstract: The present inventions relate to a number of fields including wound healing, a waterless antibacterial disinfectant, a surgical scrub, insect repellant, and methods of treating traumatic injuries, particularly those on the battlefield where there is a need to stabilize the patient and prevent infection.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Aurora Pharmaceutical, LLC
    Inventors: Michael Strobel, Gene Komer
  • Publication number: 20140336262
    Abstract: Disclosed herein are naphthamide and quinoline carboxamide compounds containing two bicyclic moieties, pharmaceutical compositions comprising those compounds and methods of using the compositions in the treatment of cancers mediated by cyclic-AMP (cAMP) response element binding protein (CREB). The disclosed compositions have utility in the treatment of lung, prostate and breast cancers in a human subject.
    Type: Application
    Filed: November 2, 2012
    Publication date: November 13, 2014
    Applicant: OREGON HEALTH & SCIENCE UNIVERSITY
    Inventors: Xiangshu Xiao, Bingbing Li, Fuchun Xie
  • Publication number: 20140323487
    Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
  • Patent number: 8865937
    Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
    Type: Grant
    Filed: November 8, 2010
    Date of Patent: October 21, 2014
    Inventors: Mahendra G. Dedhiya, Rahul Surana
  • Patent number: 8853452
    Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: October 7, 2014
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
  • Patent number: 8853266
    Abstract: This invention provides use of a SARM compound or a composition comprising the same in treating a variety of diseases or conditions in a subject, including, inter-alia, a diabetes disease, and/or disorder such as cardiovascular disease, atherosclerosis, cerebrovascular conditions, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: October 7, 2014
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller
  • Patent number: 8846763
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C1-C5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: September 30, 2014
    Assignee: Newron Pharmaceuticals, S.p.A.
    Inventors: Elena Barbanti, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
  • Publication number: 20140288040
    Abstract: The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyc
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Gianni Chessari, Gilbert Ebai Besong, Maria Grazia Carr, Steven Douglas Hiscock, Michael Alistair O'Brien, David Charles Rees, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson
  • Publication number: 20140271527
    Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 18, 2014
    Applicant: Serina Therapeutics, Inc.
    Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
  • Publication number: 20140256698
    Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Robert Booth, Jeff Dener, Michael Green
  • Publication number: 20140256743
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicants: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
  • Patent number: 8809280
    Abstract: The present invention provides a peptide, peptidomimetic or amino acid derivative having a net positive charge of at least +2 and incorporating a disubstituted ? amino acid, each of the substituting groups in the ? amino acid, which may be the same or different, comprises at least (7) non-hydrogen atoms, is lipophilic and has at least one cyclic group, one or more cyclic groups within a substituting group may be linked or fused to one or more cyclic groups within the other substituting group and where cyclic groups are fused in this way the combined total number of non-hydrogen atoms for the two substituting groups is at least (12), for use as a cytolytic therapeutic agent; as well as non therapeutic uses of these molecules and certain defined novel compounds from within this definition.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 19, 2014
    Assignee: Lytix Biopharma AS
    Inventors: Morten Strom, Terkel Hansen, Martina Havelkova, Veronika Torfoss
  • Publication number: 20140187628
    Abstract: The invention relates to a liquid vehicle that can be used to create suspensions and/or solutions of liquid or powdered medications. The vehicle is thixotropic and has improved stability and rheologic characteristics. Vehicles of the invention include an aqueous medium and a suspending agent comprising a polysaccharide having at least 50% glucose repeating saccharide units and at least 90% alpha linkages. The polysaccharide can be a starch, modified starch, or glycogen. The aqueous medium and individual components of the vehicle provide a palatable and easily ingested drug preparation. The invention also provides a vehicle containing an aqueous medium, suspending agent comprising a polysaccharide having at least 50% glucose repeating saccharide units and at least 90% alpha linkages, buffer, and artificial sweetener, the combined suspending vehicle having a pH of about 3 to about 10 and an osmolality of 300 mOmsol or less.
    Type: Application
    Filed: September 23, 2013
    Publication date: July 3, 2014
    Applicant: Fagron, Inc
    Inventors: Joshua Radke, Michael Jones, Martin Erickson
  • Publication number: 20140170112
    Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.
    Type: Application
    Filed: March 8, 2012
    Publication date: June 19, 2014
    Applicant: VICUS THERAPEUTICS, LLC
    Inventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
  • Patent number: 8748339
    Abstract: The present invention relates to a composition, comprising a 5-amino-3-oxo-2,3-dihydro-pyrazole of the formula I as defined in the claims and the description and at least one active compound II selected from groups A) to I) in a synergistically effective amount.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Egon Haden
  • Publication number: 20140155355
    Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).
    Type: Application
    Filed: April 29, 2013
    Publication date: June 5, 2014
    Inventor: Jenrin Discovery
  • Patent number: 8741957
    Abstract: The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an ?-aminoamide, particularly safinamide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourette's syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimer's Disease, Parkinson's Disease, Down's Syndrome, traumatic brain injury Huntington's Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: June 3, 2014
    Assignee: Newron Pharmaceuticals S.P.A.
    Inventors: Patricia Salvati, Stefano Rossetti, Luca Benatti
  • Patent number: 8722734
    Abstract: The present invention relates to the a method of inhibiting bone resorption in a mammal in need thereof with an oral pharmaceutical composition comprising a cathepsin K inhibitor, or a pharmaceutically acceptable salt thereof, or a mixture thereof, according to a continuous schedule having a dosage interval of once weekly, biweekly, twice monthly or once monthly.
    Type: Grant
    Filed: February 24, 2006
    Date of Patent: May 13, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Anastasia Daifotis, Selwyn Aubrey Stoch, Basil Avery Ince, Cameron Black
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Publication number: 20140086872
    Abstract: Methods are provided for treating a subject for at least one condition that includes inflammation, a blood clotting condition and autonomic nervous system dysfunction such as adrenergia, e.g., simultaneously. Also provided are kits for use in practicing the subject methods.
    Type: Application
    Filed: September 24, 2013
    Publication date: March 27, 2014
    Applicant: PALO ALTO INVESTORS
    Inventors: Anthony Joonkyoo Yun, Patrick Yuarn-Bor Lee
  • Patent number: 8669261
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: March 11, 2014
    Assignee: Congenia SLR
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Publication number: 20140066500
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema BHAT
  • Publication number: 20140056999
    Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.
    Type: Application
    Filed: March 7, 2013
    Publication date: February 27, 2014
    Applicant: MediciNova, Inc.
    Inventor: MediciNova, Inc.
  • Patent number: 8658698
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, L, Q1, and Q2 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: February 25, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Pierre Joseph Marcel Jung, Antoine Daina, Christopher Richard Ayles Godfrey, Peter Renold, Peter Maienfisch
  • Publication number: 20140051758
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C1-C5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 20, 2014
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Elena BARBANTI, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
  • Publication number: 20140051764
    Abstract: The present invention relates to solid forms of (S)—N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 20, 2014
    Inventors: James T. Dalton, Thomas G. Bird, Tai Ahn, David A. Dickason, Seoung-Soo Hong
  • Publication number: 20140023710
    Abstract: The present invention provides formulations comprising milnacipran or pharmaceutically acceptable salts thereof (e.g., milnacipran hydrochloride), including immediate release formulations and modified formulations, such as delayed release and extended release formulations. The present invention provides formulations with improved stability and high bioavailability. Processes for preparing the formulations as well as methods of treating conditions by administering the formulations are also described.
    Type: Application
    Filed: September 16, 2013
    Publication date: January 23, 2014
    Applicant: Forest Laboratories Holdings Ltd.
    Inventors: Mahendra G. Dedhiya, Anil Chhettry, Yan Yang, Yun Mo, Bhaveshkumar H. Kothari
  • Publication number: 20140018433
    Abstract: This invention relates to the treatment of androgen receptor-positive breast cancer in a subject, for example a female subject.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 16, 2014
    Inventors: James T. Dalton, Mitchell S. Steiner, Ramesh Narayanan, Sunjoo Ahn
  • Publication number: 20140005179
    Abstract: The invention provides an oral pharmaceutical composition, optionally in dose unit form, comprising a lipophilic drug substance in dispersion in a physiologically tolerable aqueous carrier, preferably an aqueous gel, wherein said drug substance contains a functional electrostatic group having a pKa value of from 2 to 10, characterised in that said aqueous carrier has a pH at least 0.3 below or above said pKa value, said pH being below said pKa where said group is acidic and above said pKa where said group is basic.
    Type: Application
    Filed: April 11, 2011
    Publication date: January 2, 2014
    Applicant: AYANDA GROUP AS
    Inventors: Kurt Ingar Draget, Ingvild Haug, Magnus N. Hattrem, Tore Seternes, Steinar Johan Engelsen
  • Patent number: 8609684
    Abstract: A composition for increasing the bioavailability of Acetaminophen in humans and animals, comprising Acetaminophen, a first water soluble surfactant having a cloud point greater than about 37° C., a second water soluble surfactant having a cloud point greater than about 37° C., wherein a mixture of the first surfactant and the second surfactant comprises a cloud point less than about 37° C.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: December 17, 2013
    Assignee: PruGen IP Holdings, Inc.
    Inventor: Bhiku G. Patel