The Hetero Ring Is Five-membered Patents (Class 514/438)
  • Patent number: 11939285
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: October 29, 2021
    Date of Patent: March 26, 2024
    Assignee: SUN PHARMACEUTICAL INDUSTRIES, INC.
    Inventor: Roger D. Tung
  • Patent number: 11762276
    Abstract: Provided is a compound that is fluidized by light irradiation and reversibly non-fluidized, and is not significantly colored. Provided is a photoresponsive compound represented by the following general formula (1), the photoresponsive compound being fluidized by light irradiation and reversibly non-fluidized: R1—Z1?Z2—R2??General formula (1) wherein Z1 and Z2 are N or CH, while Z1?Z2, R1 contains an aromatic hydrocarbon structure, R2 contains an aromatic heterocyclic structure, and a hydrogen atom is bonded to at least one carbon atom bonded adjacent to a carbon atom in the aromatic heterocyclic structure bonded to the Z2.
    Type: Grant
    Filed: July 15, 2021
    Date of Patent: September 19, 2023
    Assignee: KONICA MINOLTA, INC.
    Inventors: Yukiko Nakai, Kouji Sugama, Haruo Horiguchi, Kazuaki Nakamura, Toyoko Shibata
  • Patent number: 11702398
    Abstract: Disclosed is a compound containing a specific structure having an azomethine part, the compound being reversibly fluidized and non-fluidized by being irradiated with light.
    Type: Grant
    Filed: February 12, 2020
    Date of Patent: July 18, 2023
    Assignee: KONICA MINOLTA, INC.
    Inventors: Yukiko Kusano, Haruo Horiguchi, Kouji Sugama, Seijiro Takahashi, Toyoko Shibata, Hirofumi Hayata, Tomohiro Oshiyama
  • Patent number: 11497731
    Abstract: An object is to provide a compound having ?-lactamase inhibitory activity. The object is achieved by a compound represented by formula (1), typified by a compound in which specific positions of a 5-membered ring having planarity are replaced by sulfamoyl and carboxy groups.
    Type: Grant
    Filed: May 14, 2019
    Date of Patent: November 15, 2022
    Assignee: NATIONAL UNIVERSITY CORPORATION TOKAI NATIONAL HIGHER EDUCATION AND RESEARCH SYSTEM
    Inventors: Yoshichika Arakawa, Jun-ichi Wachino, Kouji Kimura, Wan Chun Jin, Ayato Sato
  • Patent number: 11161798
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: November 2, 2021
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Patent number: 11129801
    Abstract: The present invention relates to methods for treating neurodegenerative diseases and disorders with igmesine.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: September 28, 2021
    Assignee: SigmaThera SAS
    Inventors: François J. Roman, Johann Meunier
  • Patent number: 10786480
    Abstract: The present invention provides methods and pharmaceutical compositions for treating proliferative disorders.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: September 29, 2020
    Assignee: Peloton Therapeutics, Inc.
    Inventors: John A. Josey, Eli M. Wallace, Guangzhou Han
  • Patent number: 10780078
    Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.
    Type: Grant
    Filed: August 17, 2018
    Date of Patent: September 22, 2020
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, FRIEDRICH-ALEXANDER-UNIVERSITÄT, THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Brian K. Shoichet, Anat Levit, Aashish Manglik, Brian Kobilka, Peter Gmeiner, Harald Hübner, Daniela Gisela Dengler
  • Patent number: 10695402
    Abstract: This invention relates to treating gastrointestinal dysfunction with erythropoietin (EPO) or its analog.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: June 30, 2020
    Assignee: UNIVERSITY OF ROCHESTER
    Inventors: John Elfar, Walaa Elfar, Mark Noble
  • Patent number: 10668081
    Abstract: Prostamide-containing biodegradable intraocular implants, prostamide compounds, prostamide-containing pharmaceutical compositions, and methods for making and using such implants and compositions for the immediate and sustained reduction of intraocular pressure and treatment of glaucoma in an eye of a patient are described.
    Type: Grant
    Filed: February 12, 2018
    Date of Patent: June 2, 2020
    Assignee: ALLERGAN, INC.
    Inventors: Patrick M. Hughes, Jie Shen, Michael R. Robinson, David F. Woodward, Robert M. Burk, Hui Liu, Jinping Wan, Chandrasekar Durairaj, Gyorgy F. Ambrus, Ke Wu, Danny T. Dinh
  • Patent number: 10639318
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronic acid ester derivatives and their use as therapeutic agents.
    Type: Grant
    Filed: November 13, 2018
    Date of Patent: May 5, 2020
    Assignee: REMPEX PHARMACEUTICALS, INC.
    Inventors: Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
  • Patent number: 10590105
    Abstract: The present disclosure generally relates to compounds of formula (I), wherein R2 is a phenyl or pyridinyl moiety, useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
    Type: Grant
    Filed: July 5, 2017
    Date of Patent: March 17, 2020
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Kap-Sun Yeung, Katharine A. Grant-Young, Juliang Zhu, Mark G. Saulnier, David B. Frennesson, Zhaoxing Meng, Paul Michael Scola
  • Patent number: 10561675
    Abstract: Method of treating or ameliorating a bacterial infection comprising administering a composition comprising a cyclic boronic acid ester compound in combination with a carbapenem antibacterial agent such as Biapenem, and the pharmacokinetics studies thereof are provided.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 18, 2020
    Assignee: REMPEX PHARMACEUTICALS, INC.
    Inventors: David C. Griffith, Michael N. Dudley, Olga Rodny
  • Patent number: 10550095
    Abstract: The present invention provides a compound of Formula I, II or III or a salt or prodrug or derivative thereof that is useful for skin-whitening by inhibiting melanin formation and removing existing melanin and the inhibition of melanoma growth and/or the removal of existing melanoma cells.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: February 4, 2020
    Assignee: WISYS TECHNOLOGY FOUNDATION, INC.
    Inventors: Cheng-Chen Huang, Aaron P. Monte
  • Patent number: 10532971
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: January 14, 2020
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Patent number: 10464913
    Abstract: A purified acid composition including 2,5-furandicarboxylic acid is prepared in a process, including oxidizing a feedstock containing 5-alkoxymethylfurfural to an oxidation product including 2,5-furandicarboxylic acid (FDCA) and 2-formyl-furan-5-carboxylic acid (FFCA), and esters of FDCA and, optionally, esters of FFCA; hydrolyzing the at least part of the oxidation product in the presence of water, thereby hydrolyzing at least esters of FDCA and, optionally, esters of FFCA to obtain an aqueous solution of an acid composition including FDCA, FFCA and ester of FDCA in an amount below the amount of ester of FDCA in the solution of the oxidation product; contacting at least part of the solution of the acid composition with hydrogen in the presence of a hydrogenation catalyst to hydrogenate FFCA to hydrogenation products, yielding a hydrogenated solution; and separating at least a portion of the FDCA from at least part of the hydrogenated solution by crystallization.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: November 5, 2019
    Assignee: Synvina C.V.
    Inventors: Ana Rita Martins Guerreiro Rocha Almeida, Martinus Mathilda Pieter Zieverink, Ana Sofia Vagueiro De Sousa Dias, Ines Dacil Gonzalez Jimenez
  • Patent number: 10364257
    Abstract: A process for a continuous production of a boronic acid derivative based on a Matteson boronic ester homologation and an apparatus of performing the process are disclosed.
    Type: Grant
    Filed: December 9, 2015
    Date of Patent: July 30, 2019
    Assignee: REMPEX PHARMACEUTICALS, INC.
    Inventors: Ulfried Felfer, Clemens Stueckler, Stefan Steinhofer, Andreas Pelz, Marcus Hanacek, Thomas Heinrich Pabst, George Winkler, Peter Poechlauer, Bas Ritzen, Michel Goldbach
  • Patent number: 10335389
    Abstract: The present invention provides a patch containing beraprost or a pharmacologically acceptable salt thereof, which achieves high transdermal absorption of beraprost or a pharmacologically acceptable salt thereof and has excellent formulation properties.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: July 2, 2019
    Assignee: TEIKOKU SEIYAKU CO., LTD.
    Inventors: Satoshi Kawakami, Manabu Sogabe, Taiki Shibata
  • Patent number: 10323004
    Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
    Type: Grant
    Filed: May 4, 2017
    Date of Patent: June 18, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Weifang Shan, James Aaron Balog
  • Patent number: 10179118
    Abstract: Pharmaceutical compositions and dosage forms of dimethyl fumarate containing low levels of certain impurities are disclosed.
    Type: Grant
    Filed: March 24, 2014
    Date of Patent: January 15, 2019
    Assignee: ARBOR PHARMACEUTICALS, LLC
    Inventors: Sami Karaborni, Wei Chen, Suresh Kumar Manthati
  • Patent number: 10155722
    Abstract: The present application relates to compounds represented by general formula (I), general formula (II) or general formula (III), and pharmaceutically acceptable salts or hydrates thereof, preparation methods thereof, and pharmaceutical compositions thereof. The compounds represented by general formula (I), general formula (II) or general formula (III) have inhibitory activities against isocitrate dehydrogenase 2 (IDH2), thereby being capable of treating IDH2 mutation-induced cancers.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: December 18, 2018
    Assignees: Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd., Centaurus Biopharma Co., Ltd.
    Inventors: Shulong Wang, Na Zhao, Xijie Liu, Yuandong Hu, Hui Zhang, Hong Luo, Yong Peng, Dengming Xiao, Yongxin Han, Xiquan Zhang, Xin Tian
  • Patent number: 10112881
    Abstract: The present invention provides a compound of Formula I, wherein R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is CnH(2n+1)O, wherein n is 1-10, R2 is OH or CnH(2n+1)O, wherein n is 1-10, A, B and R1, R2, R5, R6, and R7 are separately and independently selected from a group consisting of H, alkyl, hydroxyl, halo, nitro and aryl groups, R11 is an alkyl or an aryl group and L is an optional linker or linking group, with x=0 or 1, i.e., if x=0, no linking group is present, or a salt or prodrug or derivative thereof that is a skin-lightening agent useful for the inhibition of melanin synthesis and/or the removal of existing melanin to function as a skin-lightening agent.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: October 30, 2018
    Assignee: WISYS TECHNOLOGY FOUNDATION, INC.
    Inventors: Cheng-Chen Huang, Aaron P. Monte
  • Patent number: 10112920
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: October 30, 2018
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 10040748
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: April 11, 2016
    Date of Patent: August 7, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Adam J. Morgan
  • Patent number: 10010812
    Abstract: Disclosed is an oxidation process to produce a crude carboxylic acid product carboxylic acid product. The process comprises oxidizing a feed stream comprising at least one oxidizable compound to generate a crude carboxylic acid slurry comprising furan-2,5-dicarboxylic acid (FDCA) and compositions thereof. Also disclosed is a process to produce a dry purified carboxylic acid product by utilizing various purification methods on the crude carboxylic acid.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: July 3, 2018
    Assignee: Eastman Chemical Company
    Inventors: Kenny Parker, Mesfin Janka, Ashfaq Shaikh, Lee Partin
  • Patent number: 9944615
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi. A product FDCA composition is produced having a low amount of tetrahydrofuran dicarboxylic acid, a low b*, and a low amount of 5-formyl furan-2-carboxylic acid (FFCA).
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: April 17, 2018
    Assignee: EASTMAN CHEMICAL COMPANY
    Inventors: Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Charles Edwan Sumner, Jr., Shane Kipley Kirk
  • Patent number: 9889142
    Abstract: Prostamide-containing biodegradable intraocular implants, prostamide compounds, prostamide-containing pharmaceutical compositions, and methods for making and using such implants and compositions for the immediate and sustained reduction of intraocular pressure and treatment of glaucoma in an eye of a patient are described.
    Type: Grant
    Filed: March 21, 2016
    Date of Patent: February 13, 2018
    Assignee: Allergan, Inc.
    Inventors: Patrick M. Hughes, Jie Shen, Michael R. Robinson, David F. Woodward, Robert M. Burk, Hui Liu, Jinping Wan, Chandrasekar Durairaj, Gyorgy F. Ambrus, Ke Wu, Danny T. Dinh
  • Patent number: 9884839
    Abstract: Provided herein are non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 and type 2 (17?-HSD1 and 17?-HSD2) inhibitors, their production and use, especially for the treatment and for prophylaxis of hormone-related diseases.
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: February 6, 2018
    Assignee: ElexoPharm GmbH
    Inventors: Rolf Hartmann, Martin Frotscher, Ahmed Saad Abdelsamie Ahmed, Emmanuel Bey, Chris J. van Koppen, Sandrine Oberwinkler-Marchais, Carsten Börger, Lorenz Siebenbürger, Victor Hernández Olmos
  • Patent number: 9815763
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: November 14, 2017
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Patent number: 9637467
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: May 2, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
  • Patent number: 9382188
    Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: July 5, 2016
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata, Akito Shibuya
  • Patent number: 9353079
    Abstract: Provided herein are multiple solid forms of a defined ?,{acute over (?)}-disubstituted dihydroxy cyclopentyl compound, and methods for the preparation and use thereof. In one aspect, there are provided crystalline forms of said cyclopentyl compound, and methods for the preparation and use thereof. In another aspect, there are provided substantially amorphous forms of said dihydroxy cyclopentyl compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: May 31, 2016
    Assignee: ALLERGAN, INC.
    Inventors: Ke Wu, Gyorgy F. Ambrus
  • Patent number: 9296763
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: March 29, 2016
    Assignee: Rempex Pharmaceuticals, Inc.
    Inventors: Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
  • Patent number: 9289413
    Abstract: Prostamide-containing biodegradable intraocular implants, prostamide compounds, prostamide-containing pharmaceutical compositions, and methods for making and using such implants and compositions for the immediate and sustained reduction of intraocular pressure and treatment of glaucoma in an eye of a patient are described.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: March 22, 2016
    Assignee: Allergan, Inc.
    Inventors: Patrick M. Hughes, Jie Shen, Michael R. Robinson, David F. Woodward, Robert M. Burk, Hui Liu, Jinping Wan, Chandrasekar Durairaj, Gyorgy F. Ambrus, Ke Wu, Danny T. Dinh
  • Patent number: 9156810
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: October 13, 2015
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen, Karen M. Kedzie, Daniel W. Gil, John E. Donello, Wha-Bin Im
  • Patent number: 9133157
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: September 15, 2015
    Assignee: Merck Canada Inc.
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Patent number: 9084774
    Abstract: The present invention relates to co-crystals of duloxetine and co-crystal formers selected from COX-INHIBITORS, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: July 21, 2015
    Assignee: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Helmut Heinrich Buschmann, Lluis Sola Carandell, Jordi Benet Buchholz, Jordi Carles Ceron Bertran, Jesus Ramirez Artero
  • Patent number: 9062075
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: June 23, 2015
    Assignees: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn. BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi
  • Patent number: 9051261
    Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: June 9, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Patent number: 9034914
    Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: May 19, 2015
    Assignee: UCB PHARMA GMBH
    Inventors: Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
  • Publication number: 20150126511
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 7, 2015
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Larry R. BUSH, Jianguo MA, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, John E. CAMPBELL
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150119315
    Abstract: This application provides methods of increasing vascularization, muscle performance, muscle rehabilitation, and/or mitochondrial activity in subjects in need thereof, by administering a therapeutically effective amount of one or more agents that increases ERR? activity to the subject. Such agents can include one or more ERR? agonists. In some examples the method does not require that the subject exercise, and as such, the subject may be sedentary (such as bedridden or in a wheelchair).
    Type: Application
    Filed: January 15, 2015
    Publication date: April 30, 2015
    Applicant: Salk Institute for Biological Studies
    Inventors: Vihang A. Narkar, Michael Downes, Ruth T. Yu, Ronald M. Evans
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Publication number: 20150118309
    Abstract: Exemplary embodiments of the present invention relate to a method for preparing a preparation for percutaneous absorption, which includes rotigotine as an active ingredient, and more specifically, to a method for preparing a preparation for percutaneous absorption including mixing rotigotine and an ethylene-vinyl acetate adhesive so as to have a weight ratio of 1:(0.1 to 20), a preparation for percutaneous absorption manufactured by the method, and a percutaneous treatment system. The preparation and the system may prevent separation of the rotigotine, thereby increasing long-term storage stability, and effectively release the rotigotine, and thus can be effectively applied to preparing patch medication containing the rotigotine.
    Type: Application
    Filed: January 6, 2015
    Publication date: April 30, 2015
    Inventors: Hye-Min KIM, Yong-Youn HWANG, Won-No YOUN, Yeo-Jin PARK, Joon-Gyo OH, Jong-Seob IM, Hun-Taek KIM
  • Publication number: 20150118282
    Abstract: A method for preventing the precipitation of rotigotine crystals, including a step of mixing rotigotine and one or more crystallization prevention agents selected from the group consisting of fatty alcohols, fatty acids, fatty acid esters, fatty acid amides, and the derivatives thereof, and to a transdermally absorbable preparation that includes rotigotine and crystallization prevention agents.
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Inventors: Hye-Min KIM, Yong-Youn Hwang, Won-No Youn, Yeo-Jin Park, Joon-Gyo Oh, Jong-Seob Im, Hun-Taek Kim
  • Patent number: 9012491
    Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronate compounds and their use as therapeutic agents.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: April 21, 2015
    Assignee: Rempex Pharmaceuticals, Inc.
    Inventors: Raja K. Reddy, Serge Henri Boyer, Maxim Totrov, Scott Hecker
  • Patent number: 9012493
    Abstract: The present invention provides a pest control agent having a novel skeleton, which can be synthesized industrially, and also has excellent biological activity and residual effects. Specifically, the present invention provides a 1-heterodiene derivative represented by Formula (1) or a salt thereof, and a pest control agent including, as an active ingredient, a 1-heterodiene derivative or a salt thereof.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 21, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Jyun Takahashi, Takehiko Nakamura, Masahiro Miyazawa, Isami Hamamoto, Jyun Kanazawa
  • Publication number: 20150105429
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene