Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/279)
  • Patent number: 10238646
    Abstract: The present invention relates to methods for treating pruritus with anti-pruritic compositions.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: March 26, 2019
    Assignee: Trevi Therapeutics Inc.
    Inventor: Thomas Sciascia
  • Patent number: 10183018
    Abstract: The present invention relates to injectable, extended-release, pharmaceutical formulations comprising a nalbuphine ester prodrug homogenously dissolved in a solution comprising a pharmaceutically acceptable oil and an oil-miscible retaining solvent, as well as manufacturing processes and medical uses of the formulations. The invention further provides methods for adjusting the duration of action of the formulations by varying the ratio of the pharmaceutically acceptable oil and the oil-miscible retaining solvent.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: January 22, 2019
    Assignees: Lumosa Therapeutics Co., Ltd., Shanghai Lumosa Therapeutics Co., Ltd.
    Inventors: Chan-Jung Li, David Chih-Kuang Chou, Jin-Ding Huang, Shin-Jr. Tsai, Shu-Wen Kuo, Yu-En Tien
  • Patent number: 10155771
    Abstract: The present disclosure relates to selective reduction of morphinan alkaloids in a continuous flow system. In particular, the present disclosure relates to selective reduction of thebaine or oripavine using hydrazine or a hydrazine-containing compound in a continuous flow system under elevated temperature and pressure condition to form 8,14-dihydrothebaine or 8,14-dihydrooripavine, respectively.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: December 18, 2018
    Assignee: Noramco, Inc.
    Inventors: D. Phillip Cox, C. Oliver Kappe, Bartholomaus Pieber
  • Patent number: 10086114
    Abstract: Provided are antimicrobial solutions, including catheter lock solutions. In some embodiments, the solution contains an antibiotic (e.g., minocycline or trimethoprim), EDTA, and an alcohol (e.g., ethanol), wherein the pH of the solution is adjusted to about 6-8 to reduce precipitation. Methods of using the solutions and kits are also provided.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: October 2, 2018
    Assignee: Board of Regents, The University of Texas System
    Inventors: Joel Rosenblatt, Issam Raad
  • Patent number: 10034871
    Abstract: The invention provides a combination or salt of lipoic acid and a compound of formula (I): The combinations and salts are useful for treating diabetes.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: July 31, 2018
    Assignee: Regents of the University of Minnesota
    Inventor: Philip Portoghese
  • Patent number: 10023584
    Abstract: Drug formulations, methods and their use in treatment of diseases using formulations of pure di-acid salts of tetrandrine family members, especially d-tetrandrine di-hydrochloride, combined with a pharmaceutical diluent or carrier.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: July 17, 2018
    Assignee: CBA Pharma, Inc.
    Inventor: Ron D. Carroll
  • Patent number: 9969727
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: May 15, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Patent number: 9963460
    Abstract: A morphinan derivative represented by the following formula (I), a tautomer or a stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a medicament, an analgesic and an antipruritic drug including the same as an active ingredient: wherein R is selected from hydrogen and C1-6 alkyl, and n represents an integer of 0 to 2.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: May 8, 2018
    Assignees: University of Tsukuba, Nippon Chemiphar Co., Ltd.
    Inventors: Hiroshi Nagase, Naoshi Yamamoto
  • Patent number: 9949958
    Abstract: The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: April 24, 2018
    Assignee: Salix Pharmaceuticals, Ltd
    Inventor: William Forbes
  • Patent number: 9895384
    Abstract: The present disclosure is directed to abuse-resistant transdermal delivery compositions comprising opioid agonists.
    Type: Grant
    Filed: April 1, 2016
    Date of Patent: February 20, 2018
    Assignee: InteguRx Therapeutics, LLC
    Inventors: Agis Kydonieus, Spencer Knapp
  • Patent number: 9890170
    Abstract: The invention provides a method of treating drug and alcohol abuse, depression, anxiety, or a compulsive disorder in a subject comprising administering to the subject a compound having formula 2: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R1, R2, R3, R4, R5, and X are as defined in the specification.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: February 13, 2018
    Assignee: The University of Bath
    Inventors: John Lewis, Stephen Husbands
  • Patent number: 9833492
    Abstract: A compound is provided which has a structure I: A-B-C and a method for administering the compound is also provided for use in the prophylaxis and/or treatment of a viral infection, and in particular for preventing and/or inhibiting viral replication, in which A is a quinoline or quinoline-like group, B is a sole amino acid or a peptide or polypeptide having a given amino acid sequence, and C is an O-phenoxy group. According to one embodiment, the compound is a protease inhibitor such as a caspase inhibitor, and the inhibitor can be Q-VD-OPh (N-(2-(quinolyl)valylaspartyl-(2,6-difluorophenoxyl)methyl ketone), optionally in an O-methylated form. Antiviral compositions and kits are also provided.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: December 5, 2017
    Assignees: Institut Pasteur, Institut National de la Santé et de la Recherche Médicale, Centre National de la Recherche Scientifique, Universite Paris—Sud
    Inventors: Jerome Estaquier, Mireille Laforge, Anna Senik
  • Patent number: 9629829
    Abstract: The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin.
    Type: Grant
    Filed: February 3, 2015
    Date of Patent: April 25, 2017
    Assignee: Salix Pharmaceuticals, Ltd
    Inventor: William Forbes
  • Patent number: 9598431
    Abstract: The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof:
    Type: Grant
    Filed: September 6, 2016
    Date of Patent: March 21, 2017
    Assignee: Eli Lilly and Company
    Inventor: John Richard Morphy
  • Patent number: 9498464
    Abstract: The present invention relates to a pharmaceutical combination composition comprising at least one renin-angiotensin-aldosterone system inhibitor in a subtherapeutic daily dose and at least one HMG-CoA reductase inhibitor in a subtherapeutic daily dose for use in maintaining or improving the functional and morphological properties of the arterial wall in a subject having at least one cardiovascular disorder or having at least one risk factor for cardiovascular disorder.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: November 22, 2016
    Assignee: ARTSKIN D.O.O.
    Inventor: Miso Sabovic
  • Patent number: 9498442
    Abstract: The present invention describes rifaximin powder and to a process for preparing the same. The invention relates also to a pharmaceutical composition in solid form comprising said rifaximin, pharmaceutically acceptable excipients and optionally other ingredients. The compositions according to the invention are suitable for oral administration and are characterized by producing a controlled release of rifaximin, whereby a long-lasting effect is obtained in a patient.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: November 22, 2016
    Assignee: ALFA WASSERMANN S.P.A.
    Inventors: Giuseppe Claudio Viscomi, Paola Maffei, Vittoria Lauro, Maria Barbanti, Donatella Confortini, Dario Braga
  • Patent number: 9480684
    Abstract: The invention provides a method of treating anxiety or a compulsive disorder in a subject comprising administering to the subject a compound having formula 2: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R1, R2, R3, R4, R5, and X are as defined in the specification.
    Type: Grant
    Filed: January 20, 2016
    Date of Patent: November 1, 2016
    Assignee: The University of Bath
    Inventors: John Lewis, Stephen Husbands
  • Patent number: 9481681
    Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: November 1, 2016
    Assignee: EURO-CELTIQUE S.A.
    Inventors: Steve Whitelock, Deborah Phyllis Harding, Carl David Turner
  • Patent number: 9365568
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: June 14, 2016
    Assignee: Array BioPharma Inc.
    Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
  • Patent number: 9266897
    Abstract: Disclosed are derivatives of protoberberine biological alkaloids or physiologically acceptable salts thereof produced by means of a derivative reaction of a source material of biological alkaline quaternary ammonium salts of protoberberine alkaloids, a preparation method for same and pharmaceutical uses thereof. The derivatives of protoberberine biological alkaloids or the physiologically acceptable salts thereof show activity inhibiting ulcerative colitis and can be used in the preparation of drugs for same.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: February 23, 2016
    Assignee: Institute of Materia Medica, Chinese Academy of Medical Sciences
    Inventors: Hailin Qin, Wenjie Wang, Zhihui Zhang, Lianqiu Wu, Anjun Deng, Jinqian Yu, Zhihong Li
  • Patent number: 9259422
    Abstract: The invention provides method of treating depression comprising administering to a subject compounds having formula 2: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R1, R2, R3, R4 , R5, and X are us defined in the specification.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: February 16, 2016
    Assignee: The University of Bath
    Inventors: John Lewis, Stephen Husbands
  • Patent number: 9254323
    Abstract: Enhancing the cellular uptake of a drug or dietary supplement by administering it concurrently with one or more members of the d-tetrandrine family.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: February 9, 2016
    Assignee: CBA Pharma, Inc.
    Inventor: Daryl L. Barnett
  • Patent number: 9249137
    Abstract: The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: February 2, 2016
    Assignee: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Patent number: 9233976
    Abstract: The invention provides novel berbamine derivatives, and compositions or pharmaceutical compositions thereof. These berbamine derivatives have shown higher potency in killing cancer/tumor cells comparing to berbamine, and can be used in cancer/tumor treatments.
    Type: Grant
    Filed: February 5, 2014
    Date of Patent: January 12, 2016
    Assignee: CITY OF HOPE
    Inventors: David Horne, Jun Xie, Angela L. Perkins Harki, Richard Jove, Sangkil Nam, Wendong Huang, Rongzhen Xu
  • Patent number: 9221831
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: December 29, 2015
    Assignee: Purdue Pharma, L.P.
    Inventors: Donald J. Kyle, Laykea Tafesse
  • Patent number: 9216977
    Abstract: The present invention provides compounds of Formula (I-IV): compositions containing the same, and methods of use thereof such as for the treatment of cancer.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: December 22, 2015
    Assignees: The University of North Carolina at Chapel Hill, National Taiwan University
    Inventors: Kuo-Hsiung Lee, Xiaoming Yang, Qian Shi, Kenneth F. Bastow, Che-Ming Teng, Tse-Ming Hong, Pan-Chyr Yang, Shuenn-Chen Yang
  • Patent number: 9211268
    Abstract: A method of reducing the concentration of a chemical or drug substance in the blood plasma comprising titrating an initial peak concentration of the chemical or drug substance in the blood for a predefined dosing period, titrating a lowest concentration level of the chemical or drug substance in the blood immediately before the end of the dosing period, and providing a plurality of subsequent dosing periods where each subsequent dosing period requires administration of a dosing amount of the chemical or drug substance and titrating of the peak concentration and the lowest concentration level to ensure that the lowest concentration level of the chemical or drug substance in the blood plasma for the subsequent dosing period is decreased by not more than five percent of the lowest concentration level of the previous dosing period and where the plurality of dosing periods added together is seventy days or more.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: December 15, 2015
    Inventors: Kenneth C. Slater, Brenda E. Richardson, Scott M. Connors, Wei-wei Chang
  • Patent number: 9206186
    Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.
    Type: Grant
    Filed: August 26, 2013
    Date of Patent: December 8, 2015
    Assignee: AXIKIN PHARMACEUTICALS, INC.
    Inventors: Yingfu Li, Kevin Bacon, Hiromi Sugimoto, Keiko Fukushima, Kentaro Hashimoto, Makiko Marumo, Toshiya Moriwaki, Noriko Nunami, Naoki Tsuno, Klaus Urbahns, Nagahiro Yoshida
  • Patent number: 9206190
    Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: December 8, 2015
    Assignee: EURO-CELTIQUE S.A.
    Inventors: Steve Whitelock, Deborah Phyllis Harding, Carl David Turner
  • Patent number: 9186355
    Abstract: The present invention is directed to methods for preparation of a composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ?. For example, practice of a method of the invention can provide the composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ? wherein the rifaximin ? is present in about 3-12% (w/w) or is present in about 5-8% (w/w). The composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ? is prepared by dissolving raw rifaximin in a water-soluble organic solvent, for example ethanol, at reflux, then adding water to achieve a final mixed solvent of about 7:3 (v/v) solvent to water ratio, then cooling to 35-40° C. until crystallization commences, then further cooling with stirring to 0° C., then recovery of the crystallized material, and drying to a water content of between 2.5% and 5.0%, to provide the composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ?.
    Type: Grant
    Filed: March 30, 2015
    Date of Patent: November 17, 2015
    Assignee: Novel Laboratories
    Inventor: Kishore Kumar Hotha
  • Patent number: 9168298
    Abstract: This invention relates to a novel use of IL-1?-ligand/IL-1 receptor disrupting compounds (herein referred to as “IL-1beta Compounds”); such as small molecular compounds disrupting IL-1? ligand—IL-1 receptor interaction, IL-1? antibodies or IL-1 receptor antibodies, e.g. IL-1? binding molecules described herein, e.g. antibodies disclosed herein, e.g. IL-1? binding compounds or IL-1 receptor binding compounds, and/or RNA compounds decreasing either IL-1? ligands or IL-1 receptor protein levels, in the treatment and/or prevention of auto-inflammatory syndromes, e.g. Juvenile rheumatoid arthritis or adult rheumatoid arthritis syndrome and to methods of treating and/or preventing auto-inflammatory syndromes, e.g. Juvenile rheumatoid arthritis or adult rheumatoid arthritis syndrome, in mammals, particularly humans.
    Type: Grant
    Filed: July 31, 2013
    Date of Patent: October 27, 2015
    Assignee: Novartis AG
    Inventors: Hermann Gram, Thomas Jung
  • Patent number: 9163030
    Abstract: Provided are compounds of the formula: R1; R2, R3; R4; A; X; Y and Z are defined in the present disclosure; pharmaceutically acceptable salts thereof, deuterium forms thereof, isomers thereof, and mixture thereof; and processes for their preparation. The compounds can be used for treating a patient suffering from a condition that is capable of treatment with an agonist and/or antagonist of the opioid receptors and are especially useful a patient suffering from pain, treating a patient in need of an immunosuppressant to prevent rejection in organ transplant and skin graft, in need of an anti-allergic agent, in need of an anti-inflammatory agent, in need of a brain cell protectant, for drug and/or alcohol abuse, to decrease gastric secretion, for diarrhea, for cardiovascular disease, for a respiratory disease, in need of a cough and/or respiratory depressant, for mental illness, for epileptic seizures and other neurologic disorders.
    Type: Grant
    Filed: May 2, 2013
    Date of Patent: October 20, 2015
    Assignee: Southern Research Institute
    Inventor: Subramaniam Ananthan
  • Patent number: 9096606
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R1a, R2, R8, R3a, R3b, G, X, Z, Y, and A® are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: August 4, 2015
    Assignee: Purdue Pharma, L.P.
    Inventor: Donald J. Kyle
  • Patent number: 9085536
    Abstract: Compound derivatives of aconitine are provided, in particular derivatives that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. The subject compounds are useful in treatments, including treatments to modulate neuronal activity or to bring about muscular relaxation. The compounds also find use in the treatment of subjects suffering from a voltage-gated sodium channel-enhanced ailment or from pain. Further methods are provided for the preparation of the aconitine derivatives.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: July 21, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Justin Du Bois, Brian M. Andresen, Frederic Menard, Andrew W. Patterson
  • Patent number: 9078890
    Abstract: The present invention discloses an application of koumine and homologue thereof in preparation of drugs for treating autoimmune diseases involving bones and joints including rheumatoid arthritis, spondylitis ankylopoietica or the like, in particular an application of Gelsemium alkaloid monomer koumine and homologue thereof or pharmaceutically acceptable salt thereof as active ingredient in preparation of drugs for treating autoimmune diseases involving bones and joints including rheumatoid arthritis, spondylitis ankylopoietica or the like.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: July 14, 2015
    Assignee: Fujian Medical University
    Inventors: Changxi Yu, Ying Xu, Jian Yang, Yanping Su, Hongda Cai
  • Patent number: 9051334
    Abstract: The invention provides orvinol and thevinol compounds useful for the treatment of drug and alcohol abuse, the compounds being particularly useful for the prevention of relapse in recovering addicts.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: June 9, 2015
    Assignee: The University of Bath
    Inventors: John Lewis, Stephen Husbands
  • Publication number: 20150141450
    Abstract: Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Inventors: William Forbes, Enoch Bortey
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Patent number: 9034892
    Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: May 19, 2015
    Assignee: Salix Pharmaceuticals, Inc.
    Inventors: Karen S. Gushurst, Donglai Yang, Petinka Vlahova, Jeffrey S. Stults
  • Publication number: 20150133483
    Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
    Type: Application
    Filed: August 29, 2014
    Publication date: May 14, 2015
    Inventors: Steve WHITELOCK, Deborah Phyllis HARDING, Carl David TURNER
  • Publication number: 20150133482
    Abstract: The present invention relates to new rifaximin forms comprising solid dispersions of rifaximin, methods of making same and to their use in medicinal preparations and therapeutic methods.
    Type: Application
    Filed: April 10, 2014
    Publication date: May 14, 2015
    Applicant: SALIX PHARMACEUTICALS, LTD.
    Inventors: Jon Selbo, Jing Teng, Mohammed A. Kabir, Pam Golden
  • Publication number: 20150118307
    Abstract: Embodiments relate to Rifaximin polymorphic, salt, and hydrate forms, methods of producing polymorphic forms and to their use in medicinal preparations and to therapeutic methods using them.
    Type: Application
    Filed: May 27, 2014
    Publication date: April 30, 2015
    Applicant: SALIX PHARMACEUTICALS, LTD
    Inventors: Stephan D. Parent, Lisa Lynn McQueen, Patricia Andres, Paul Schields, Yiduo Wu, Fei Ding, Jared Peters Smit
  • Patent number: 9018225
    Abstract: The present invention is directed to methods for preparation of a composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ?. For example, practice of a method of the invention can provide the composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ? wherein the rifaximin ? is present in about 3-12% (w/w) or is present in about 5-8% (w/w). The composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ? is prepared by dissolving raw rifaximin in a water-soluble organic solvent, for example ethanol, at reflux, then adding water to achieve a final mixed solvent of about 7:3 (v/v) solvent to water ratio, then cooling to 35-40° C. until crystallization commences, then further cooling with stirring to 0° C., then recovery of the crystallized material, and drying to a water content of between 2.5% and 5.0%, to provide the composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ?.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: April 28, 2015
    Assignee: Novel Laboratories
    Inventor: Kishore Kumar Hotha
  • Publication number: 20150111916
    Abstract: This invention relates to the use of a composition comprising opioid/Toll-like receptor 4 (TLR4) antagonists and dextro enantiomers thereof for the treatment of pain, where the opioid antagonists treat pain by blocking TLR4. More preferably, the dextro opioid/TLR4 antagonist enantiomer treats pain by blocking TLR4 while not affecting the opioid receptors and therefore avoiding adverse effects associated with blocking the opioid receptors. Examples of opioid antagonist and their dextro enantiomers include naltrexone, naloxone and nalmefene, and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof and their use in the treatment of pain, particularly neuropathic pain.
    Type: Application
    Filed: March 27, 2013
    Publication date: April 23, 2015
    Inventor: Annette Channa Toledano
  • Patent number: 9006261
    Abstract: The invention relates to a perylene diimide derivative and to an in vitro method for preparing the same. In addition, the invention relates to a method for detecting heparin in a sample using perylene diimide derivatives, wherein the interaction of the perylene diimide derivative with heparin modulates the intensity of the fluorescent signal of the mixture compared to the solution. The invention also comprises a diagnostic kit for detecting heparin in a sample in vitro, comprising the perylene diimide derivative, as well as the use of the perylene diimide derivative for neutralizing the anticoagulant activity of heparin.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: April 14, 2015
    Inventors: Roland Kraemer, Helga Szelke, Job Harenberg, Armin Poeck
  • Publication number: 20150098909
    Abstract: A soluble fiber lozenge provided herein includes a body that is partially or wholly receivable in an oral cavity. The body includes a soluble-fiber matrix and one or more additives dispersed in the soluble-fiber matrix. In some cases, a soluble fiber lozenge provided herein includes at least 40 weight percent of soluble fiber. In some cases, soluble fiber in soluble fiber lozenge provided herein can include maltodextrin. The soluble fiber lozenge is adapted to release one or more additives from the body when the body is received within the oral cavity of a consumer and exposed to saliva. A method of making soluble fiber lozenges provided herein includes forming a molten mixture of at least 40 weight percent soluble fiber, one or more additives, and less than 15 weight percent water while maintaining a mixture temperature of less than 200° C. and portioning the molten mixture into a plurality of soluble fiber lozenges. In some cases, the ingredients can be mixed to form the molten mixture in an extruder.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Feng Gao, Diane L. Gee, Shuzhong Zhuang, Phillip M. Hulan, William J. Burke, Gerd Kobal
  • Patent number: 9000005
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 7, 2015
    Assignee: ArQule, Inc.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Publication number: 20150094324
    Abstract: The present disclosure is concerned with a process for the preparation of the above disclosed compounds, pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, or mixtures thereof which comprises subjecting a 17-substituted-3,14-dihydroxypyridomorphinan to dialkylation at the phenolic hydroxyl at the 3-position and the tertiary alcohol at the 14-position followed by selective dealkylation of the phenolic ether function.
    Type: Application
    Filed: May 2, 2013
    Publication date: April 2, 2015
    Inventor: Subramaniam Ananthan
  • Patent number: 8987289
    Abstract: The present invention relates to methods for treating pruritus with anti-pruritic compositions.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: March 24, 2015
    Assignee: Trevi Therapeutics, Inc.
    Inventor: Thomas Sciascia
  • Patent number: 8987288
    Abstract: The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: March 24, 2015
    Assignee: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Fuwen Xie, Hongxi Lai, Frank Rong