Q Is Acyclic And Benzene Ring In A Substituent E Patents (Class 514/605)
  • Patent number: 9833417
    Abstract: Provided is a felbinac-containing external patch which can exhibit high drug release properties, low skin irritation, and high drug stability, wherein felbinac having an average particle diameter of 5 ?m or more and less than 100 ?m is dispersed and mixed in an adhesive base including a styrene-isoprene-styrene block copolymer, an alicyclic saturated hydrocarbon resin, a softener, and diethyl sebacate, and does not contain L-menthol. Specifically, in the felbinac-containing external patch, 0.1 to 10% by weight of felbinac having an average particle diameter of 5 ?m or more and less than 100 ?m is dispersed and mixed in an adhesive base including 10 to 30% by weight of a styrene-isoprene-styrene block copolymer, 10 to 50% by weight of an alicyclic saturated hydrocarbon resin, 10 to 75% by weight of a softener, and 0.1 to 10% by weight of diethyl sebacate.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: December 5, 2017
    Assignee: Teikoku Seiyaku Co., Ltd.
    Inventor: Katsuyuki Inoo
  • Patent number: 9724297
    Abstract: The present invention provides oral solutions containing sotalol hydrochloride which advantageously avoid swallowing while providing with improved stability. The present invention also relates to methods of using the oral solutions for treatment of diseases and disorders, such as delay in reoccurrence of atrial fibrillation/atrial flutter and/or ventricular arrhythmias.
    Type: Grant
    Filed: April 1, 2014
    Date of Patent: August 8, 2017
    Assignee: ARBOR PHARMACEUTICALS, INC.
    Inventors: H. Greg Thomas, Jeffrey S. Kiel
  • Patent number: 9597302
    Abstract: Effective and safe pharmaceutical composition and method for treating atrial fibrillation are described. The combined use of dofetilide and mexiletine resulted in an enhanced efficacy in the prevention and treatment of atrial fibrillation with markedly reduced risk of the life-threatening ventricular arrhythmia TdP.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: March 21, 2017
    Assignee: Heart Rhythm Solutions, Inc.
    Inventors: Ganxin Yan, Jian-Zeng Dong, Chang-Sheng Ma
  • Patent number: 9376380
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: June 28, 2016
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Xiang-qun Xie, Peng Yang, Rentian Feng
  • Patent number: 9351947
    Abstract: A catecholamine or related compound having (S)-configuration at ?-carbon, a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof and having a lipophilicity greater than (S)-noradrenaline has use as an anti-angiogenic agent. A catecholamine or related compound in which a ?-hydroxy group has been modified are also anti-angiogenic. The anti-angiogenic agent is preferably a compound of formula (I) or (II) a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof.
    Type: Grant
    Filed: January 29, 2008
    Date of Patent: May 31, 2016
    Assignee: National Research Council of Canada
    Inventors: Yasuo Konishi, Joanne Magoon, Suwatchai Jarussophon
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Patent number: 9000045
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity. the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 7, 2015
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Publication number: 20150094362
    Abstract: The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21).
    Type: Application
    Filed: December 10, 2014
    Publication date: April 2, 2015
    Inventors: Max S. Wicha, Christophe Ginestier
  • Publication number: 20150094276
    Abstract: This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 2, 2015
    Inventor: Roger D. Tung
  • Patent number: 8993630
    Abstract: The present invention relates to substituted sulphonamido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 31, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ingo Hartung, Marion Hitchcock, Florian Puhler, Gerhard Siemeister, Roland Neuhaus
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Publication number: 20150080439
    Abstract: Various embodiments of the present invention relate to, among other things, compounds that are inhibitors of Memapsin 1 and, as a result, are effective in the treatment of Alzheimer's disease or diabetes (e.g., Type 2 diabetes).
    Type: Application
    Filed: September 12, 2014
    Publication date: March 19, 2015
    Inventor: Arun K. Ghosh
  • Publication number: 20150064234
    Abstract: It has been discovered that pharmacological inhibition of K+ channels (using the FDA-approved broad-spectrum K+ channel antagonist 4-AP) positively benefitted smn mutant phenotypes, a result that is consistent with the defective excitability of motor circuits by their interneuron or sensory neuron inputs being a critical consequence of SMN depletion. Based on these observations, certain embodiments of the invention are directed to methods of treatment of SMA by administering therapeutically effective amounts of one or more potassium channel antagonists, including 4-aminopyridine, 4-(dimethylamino)pyridine, 4-(methylamino)pyridine, and 4-(aminomethyl)pyridine. Other embodiments are directed to new pharmaceutical formulations comprising two or more potassium channel antagonists.
    Type: Application
    Filed: March 26, 2013
    Publication date: March 5, 2015
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventor: Brian D. Mccabe
  • Publication number: 20150057248
    Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.
    Type: Application
    Filed: September 1, 2014
    Publication date: February 26, 2015
    Applicant: The Board of Regents of The University of Texas System
    Inventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
  • Publication number: 20150056164
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (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: Application
    Filed: April 24, 2014
    Publication date: February 26, 2015
    Applicant: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Publication number: 20150051233
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: February 19, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Sandeep K. Agarwal, Mesias Pedroza
  • Patent number: 8952169
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: February 10, 2015
    Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.
    Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
  • Patent number: 8952031
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: February 10, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Publication number: 20150031714
    Abstract: Embodiments of the invention include methods of preventing and/or reducing the risk or severity of an allergic reaction in an individual. In some embodiments, particular small molecules are employed for prevention and/or reduction in the risk or severity of anaphylaxis. In at least particular cases, the small molecules are inhibitors of STAT3. In some cases, the small molecule comprises N-(1?,2-dihydroxy-1,2?-binaphthalen-4?-yl)-4-methoxybenzenesulfonamide.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 29, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Josh Milner
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20150023921
    Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.
    Type: Application
    Filed: April 3, 2014
    Publication date: January 22, 2015
    Applicant: BIOTRON LIMITED
    Inventors: Gary Dinneen EWART, Carolyn Anne LUSCOMBE, Michelle MILLER
  • Publication number: 20150025042
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 16, 2013
    Publication date: January 22, 2015
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Publication number: 20150011639
    Abstract: The use of sulfonamides of formula (I) wherein R and R1 are as defined in the description, for the preparation of medicaments for the prevention of diabetes, in particular of type-1 diabetes is herein disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 8, 2015
    Inventors: Lorenzo PIEMONTI, Luisa DAFFONCHIO, Marcello ALLEGRETTI
  • Publication number: 20140329833
    Abstract: The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 6, 2014
    Applicant: ORYZON GENOMICS, S.A
    Inventors: Tamara Maes, Marc Martinell Pedemonte, Julio Castro-Palomino Laria
  • Publication number: 20140323502
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Application
    Filed: February 13, 2014
    Publication date: October 30, 2014
    Inventors: Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
  • Publication number: 20140315954
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
  • Patent number: 8859590
    Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: October 14, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Publication number: 20140296294
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Xiang-qun XIE, Peng YANG, Rentian FENG
  • Publication number: 20140296255
    Abstract: The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.
    Type: Application
    Filed: May 21, 2012
    Publication date: October 2, 2014
    Applicant: ORYZONG GENOMICS, S.A.
    Inventors: Tamara Maes, Marc Martinell Pedemonte
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA 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: Application
    Filed: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • Patent number: 8829052
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 9, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8778897
    Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: July 15, 2014
    Assignee: The Regents of the University of California
    Inventor: Paul C. Simpson, Jr.
  • Patent number: 8779197
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: July 15, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
  • Publication number: 20140179686
    Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.
    Type: Application
    Filed: February 25, 2014
    Publication date: June 26, 2014
    Applicant: Gruenenthal GmbH
    Inventors: Jeewoo LEE, Hyung Chul Ryu, Robert FRANK, Gregor BAHRENBERG, Jean DE VRY, Thomas CHRISTOPH, Derek John SAUNDERS, Klaus SCHIENE, Bernd SUNDERMANN
  • Patent number: 8759579
    Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard W. Heidebrecht, Chaomin Li, Benito Munoz, Andrew Rosenau, Laura M. Surdi, Paul Tempest
  • Publication number: 20140163041
    Abstract: The present invention relates to methods and compositions for the treatment or prevention of diseases and disorder associated with myeloproliferative and lymphoproliferative disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing diseases and disorder associated with myeloproliferative and lymphoproliferative disorders.
    Type: Application
    Filed: February 8, 2012
    Publication date: June 12, 2014
    Applicant: ORYZON GENOMICS S.A.
    Inventors: Matthew Colin Thor Fyfe, Tamara Maes, Marc Martinell Pedemonte
  • Publication number: 20140066488
    Abstract: Proteases such as memapsin 2 are important enzymes, playing roles in a variety of diseases including Alzheimer's Disease. The inventors have developed inhibitors of memapsin 2 and methods of use therefore in the treatment of disease.
    Type: Application
    Filed: August 28, 2013
    Publication date: March 6, 2014
    Applicants: Purdue Research Foundation, Oklahoma Medical Research Foundation
    Inventors: Jordan Tang, Venkateswararao Kalapala, Arun K. Ghosh
  • Patent number: 8642657
    Abstract: 4-(methylsulfonylamino)phenyl analogues as potent vanilloid receptor antagonists and pharmaceutical compositions comprising the same. The compounds are useful as analgesics to prevent, alleviate or treat pain diseases or inflammatory disease including pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease and urgent urinary incontinence.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: February 4, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Jee Woo Lee, Young Ho Kim, Hee Kim, Hyun Kyung Choi, Hee Jin Ha
  • Publication number: 20140031363
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R1 and R2 is independently H, alkyl, alkenyl or aralkyl or R1 and R2 taken together form a 5-8 membered ring; R3-R6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO2, CH2, NH, N(alkyl), or NHC(?O); and Z is OH, NR6R7, NR8SO2(alkyl), NR8C(O)NR6R7, NR8C(O)O(alkyl), NR8-dihydrothiazole, or NR8-dihydroimidazole or wherein Z can fuse with Ar2 to form selected heterocycles.
    Type: Application
    Filed: April 15, 2013
    Publication date: January 30, 2014
    Inventors: Dennis C. Liotta, James P. Snyder, Stephen F. Traynelis, Lawrence Wilson, Cara Mosley, Raymond J. Dingledine, Scott Myers, Yesim Altas Tahirovic
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Patent number: 8633237
    Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: January 21, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Kevin J. Gillen, Jonathan Gillespie, Craig Jamieson, John K. F. MacLean, Elizabeth M. Moir, Zoran Rankovic
  • Publication number: 20140011881
    Abstract: This present disclosure relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present disclosure provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: September 10, 2013
    Publication date: January 9, 2014
    Applicant: Amorepacific Corporation
    Inventors: Song Seok SHIN, Jin Kwan KIM, Sun-Young KIM, Ki-Wha LEE, Byoung young WOO, Joo-Hyun MOH, Yeon Su JEONG, Kyung Min LIM, Jin Kyu CHOI, Hyun-Ju KOH, Young-Ho PARK
  • Patent number: 8609897
    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
  • Publication number: 20130331392
    Abstract: The invention provides cycloalkyl guanidine compounds that inhibit F1F0-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 12, 2013
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Publication number: 20130324503
    Abstract: The present invention relates to methods of treatment for Parkinson Disease (PD) in a person by identifying gene variants which may indicate a more favorable response to specific medicaments, thereby allowing for personalized or individualized treatment. The present invention relates to a method of screening for a genetic predisposition to PD in a person. The present invention is also directed to a method of testing a person for the presence of particular gene variants, wherein the presence of a gene variant indicates a higher predisposition to PD, and the absence of a gene variant indicates a lower predisposition to PD, compared to a control sample. The present invention further relates to methods and kits for treating, or inhibiting the development of, PD in a person. The present invention is also directed to a method of identifying the heritage of an individual based on the genetic profile of the individual.
    Type: Application
    Filed: October 19, 2012
    Publication date: December 5, 2013
    Applicants: Health Research Inc., Emory University School of Medicine, National Institute of Environmental Health Sciences, Veterans Affairs Puget Sound Health Care System, Oregon Health & Science University
    Inventors: Haydeh Payami, Taye H. Hamza, Stewart A. Factor, John Nutt, Cyrus Zabetian, Honglei Chen, Erin Hill Burns
  • Publication number: 20130317001
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC.
    Inventors: Jean-Christophe Andrez, Sultan Chowdhury, Shannon Marie Decker, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Jun Li, Daniel F. Ortwine, Brian Safina, Tao Sheng, Shaoyi Sun, Daniel P. Sutherlin, Michael Scott Wilson, Alla Yurevna Zenova
  • Publication number: 20130317000
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 8592629
    Abstract: This invention relates to sulfonamide derivative of formula (I), to their use in medicine, to compositions containing them, to processes for their preparation, and to intermediates used in such processes. These compounds are inhibitors of Nav1.7.
    Type: Grant
    Filed: July 11, 2011
    Date of Patent: November 26, 2013
    Assignee: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Marcel John De Groot, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Nigel Alan Swain, Steven Matthieu Gaulier