Piperazines (i.e., Fully Hydrogenated 1,4-diazines) Patents (Class 514/252.12)
  • Patent number: 10350207
    Abstract: The invention provides compositions and methods for the induction of cancer cell death. The compositions and methods of using them include use of compositions in therapy for the treatment of cancer and for the selective induction of apoptosis in cancer cells. The drug combinations described herein can be synergistic and can have lower neurotoxicity effects than the same amounts of other compounds and combinations of compounds, and can be effective when a particular cancer has become resistant to previously administered therapies.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: July 16, 2019
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Jessie Peh
  • Patent number: 10195193
    Abstract: The embodiments described herein include methods and formulations for treating viruses and diseases that are exacerbated by inflammatory responses in the body. The methods and formulations include, but are not limited to, methods and formulations for delivering effective concentrations of levocetirizine and montelukast to a patient in need. The methods and formulations can comprise conventional and/or modified-release elements, providing for drug delivery to the patient.
    Type: Grant
    Filed: February 13, 2018
    Date of Patent: February 5, 2019
    Assignee: IRR, Inc.
    Inventor: Bruce Chandler May
  • Patent number: 10166229
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: January 1, 2019
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Karson S. Putt, Quinn P. Peterson, Valerie Fako
  • Patent number: 10085978
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Grant
    Filed: August 22, 2016
    Date of Patent: October 2, 2018
    Assignees: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc., The Johns Hopkins University
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Avadhut Joshi, Gregory J. Riggins, Theodore M. Tarasow
  • Patent number: 10085977
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: October 2, 2018
    Assignees: The Board of Trustees of the Univerity of Illinois, Vanquish Oncology, Inc.
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Howard S. Roth, Theodore M. Tarasow
  • Patent number: 10048272
    Abstract: The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution. The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: August 14, 2018
    Assignees: STC.UNM, Torrey Pines Institute for Molecular Studies
    Inventors: Bruce S. Edwards, Larry A. Sklar, Clemencia Pinilla, Richard A. Houghten, Jon R. Appel, Marc A. Giulianotti, Jose Medina-Franco
  • Patent number: 10004727
    Abstract: The present invention relates to a novel use of a composition containing, as an active ingredient, an amodiaquine compound or a pharmaceutically acceptable salt thereof and specifically, to a metabolic disease prevention, alleviation or treatment use of a composition containing, as an active ingredient, an amodiaquine compound or a pharmaceutically acceptable salt thereof, the composition activating both peroxisome proliferator-activated receptor-gamma (PPAR-?) and peroxisome proliferator-activated receptor-alpha (PPAR-?).
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: June 26, 2018
    Assignees: POSTECH ACADEMY-INDUSTRY FOUNDATION, NOVMETAPHARMA CO., LTD.
    Inventors: Kyong Tai Kim, Hoe Yune Jung
  • Patent number: 9801876
    Abstract: The present invention relates to a complex granule formulation comprising a first granular part comprising levocetirizine or its pharmaceutically acceptable salt, cyclodextrin or its derivative, and an alkalinizing agent; and a second granular part comprising montelukast or its pharmaceutically acceptable salt, cyclodextrin or its derivative, and an alkalinizing agent. This formulation can effectively inhibit the production of related compounds of levocetirizine and montelukast by allowing levocetirizine and montelukast to form clathrate complexes with cyclodextrin, and using an alkalinizing agent. This formulation not only shows increased stability and bioavailability, but also improves patient compliance owing to its effective masking of bitter taste.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: October 31, 2017
    Assignee: HANMI PHARM. CO., LTD
    Inventors: Ho Taek Im, Taek Kwan Kwon, Yong Il Kim, Jae Hyun Park, Jong Soo Woo
  • Patent number: 9777333
    Abstract: The disclosure provides gene fusion variants and novel associations with disease states, as well as kits, probes, and methods of using the same.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: October 3, 2017
    Assignee: Life Technologies Corporation
    Inventors: Daniel Rhodes, Seth Sadis, Peter Wyngaard, Armand Bankhead, Dinesh Cyanam, Nikolay Khazanov
  • Patent number: 9572806
    Abstract: The invention provides a solid preparation which does not undergo the delay of elution of the active ingredient even after long-term storage. The solid preparation independently contains a teneligliptin-containing part containing teneligliptin or a salt thereof, or a solvate of teneligliptin or the salt thereof, in an amount 1.5- to 10-fold larger than that desired for the solid preparation.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: February 21, 2017
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yasuaki Obayashi, Shinichiro Yasui, Hidaka Abe
  • Patent number: 9556142
    Abstract: A method of preparing (R,S)-nicotine, comprising reacting a nicotinate ester with N-vinyl-2-pyrrolidinone in the presence of a base and a solvent to form a first mixture, combining the first mixture with an acid to form a second mixture comprising an aqueous layer, separating the aqueous layer from second mixture, combining the separated aqueous layer with an acid to form a third mixture, combining the third mixture with a base to form a fourth mixture comprising myosamine, reducing myosamine to nornicotine using a reducing agent, and methylating the nornicotine to yield R,S-nicotine.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: January 31, 2017
    Assignee: NEXT GENERATION LABS, LLC
    Inventor: Michael Arnold
  • Patent number: 9522901
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: December 20, 2016
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Karson S. Putt, Quinn P. Peterson, Valerie Fako
  • Patent number: 9464062
    Abstract: Pharmaceutical compositions of the invention comprise disubstituted oxazolidin-2-ones derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 2b activity.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: October 11, 2016
    Assignee: TEMPLE UNIVERSITY—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Daniel J. Canney, Richie R. Bhandare, Benjamin E. Blass, Magid Abou-Gharbia
  • Patent number: 9421202
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: August 23, 2016
    Assignees: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc., The Johns Hopkins University
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael J. Handley, Avadhut Joshi, Gregory J. Riggins, Theodore M. Tarasow
  • Patent number: 9365529
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: June 14, 2016
    Assignee: GALDERMA RESEARCH & DEVLOPMENT
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli-Nollet
  • Patent number: 9199968
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: December 1, 2015
    Assignee: AGIOS PHARMACEUTICALS, INC.
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
  • Patent number: 9095581
    Abstract: This invention concerns combinations of inhibitors of MEK, Raf protein kinases, and other kinases including VEGFR1-3 and PDGFR-?. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer and other hyperproliferative disorders.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: August 4, 2015
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jeffrey N. Miner, Mark S. Chapman, Barry Quart, Alex Adjei, Chunrong Yu
  • Patent number: 9056108
    Abstract: The present invention relates to a method for the treatment or prevention of atrial fibrillation and/or atrial flutter comprising coadministration of a synergistically therapeutic amount of dronedarone or a pharmaceutically acceptable salt or salts thereof and a synergistically therapeutic amount of ranolazine or a pharmaceutically acceptable salt or salts thereof. Also provided are methods for modulating ventricular and atrial rhythm and rate. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: June 16, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Charles Antzelevitch, Luiz Belardinelli, Alexander Burashnikov, John Shryock, Dewan Zeng
  • Patent number: 9051255
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Grant
    Filed: December 27, 2013
    Date of Patent: June 9, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Patent number: 9040539
    Abstract: A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C?N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: May 26, 2015
    Assignee: SANDOZ AG
    Inventors: Michael Oberhuber, Joerg Salchenegger, Dominic De Souza, Martin Albert, Thorsten Wilhelm, Martin Langner, Hubert Sturm, Hans-Peter Spitzenstaetter
  • Patent number: 9034878
    Abstract: The invention provides (i) a method of treating metabolic syndrome in an animal, (ii) a method of suppressing the appetite of an animal, (iii) a method of treating obesity in an animal, (iv) a method of reducing the weight of an animal in need thereof, (v) a method of reducing a blood lipid level in an animal in need thereof, (vi) a method of treating non-alcoholic steatohepatitis in an animal, and (vii) a method of inhibiting adipogenesis. The methods comprise administering an effective amount of an active ingredient, wherein the active ingredient comprises a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them to the animal. The invention also provides a kit comprising a container holding a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them; and instructions for administration. The diketopiperazines have the formula given in the application.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: May 19, 2015
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Patent number: 9012452
    Abstract: Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: April 21, 2015
    Assignee: AstraZeneca AB
    Inventor: Robert Stranne
  • Patent number: 9012453
    Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: April 21, 2015
    Assignee: H. Lundbeck A/S
    Inventors: Morten Jorgensen, Peter Hongaard Andersen, Klaus Gjervig Jensen
  • Publication number: 20150099759
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods the use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Application
    Filed: March 4, 2013
    Publication date: April 9, 2015
    Applicants: The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc.
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Theodore M. Tarasow
  • Publication number: 20150094314
    Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.
    Type: Application
    Filed: March 21, 2013
    Publication date: April 2, 2015
    Inventor: Chris Dealwis
  • Publication number: 20150093365
    Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 2, 2015
    Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
  • Patent number: 8993779
    Abstract: The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • Publication number: 20150087642
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Bronislava GEDULIN, Andrew A. YOUNG, Howard E. GREENE
  • Patent number: 8987263
    Abstract: Basic esters of fatty alcohols of the general formula: R1-O—CO-A or pharmaceutically acceptable salts thereof, wherein R1 is C12-C24 alkyl or C10-C24 alkenyl, and A is a residue containing at least one acyclic or cyclic amino group and/or at least one heteroaromatic ring containing a tertiary or quaternary nitrogen atom, are anti-inflammatory and immunomodulatory agents, useful in the treatment of immunologically-mediated inflammation, as adjuvants for antigens involved in both cellular and humoral responses.
    Type: Grant
    Filed: October 9, 2003
    Date of Patent: March 24, 2015
    Inventors: Meir Shinitzky, Irun R. Cohen, Raanan Margalit, Yaacov Herzig, Jeffrey Sterling, Gyorgy Toth, Istvan Miskolczi, Ferenc Rantal, Tivadar Tamas
  • Patent number: 8980897
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: March 17, 2015
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli-Nollet
  • Patent number: 8975399
    Abstract: A benzene sulphonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for its use in a method for treating a pathology linked to an excessive effect of TNF-alpha and for its use in a method for treating the human or animal body as a direct inhibitor of TNF-alpha.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: March 10, 2015
    Inventors: Jean-Francois Zagury, Matthieu Montes, Hadley Mouhsine, Helene Guillemain
  • Patent number: 8969353
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: March 3, 2015
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 8962022
    Abstract: The present invention is directed to compositions of taste-masked microparticles comprising a substituted benzhydrylpiperazine coated and a taste-masking layer comprising a water-insoluble polymer and a gastrosoluble polymer, and methods of making such taste-masked microparticles. The present invention is also directed to stable orally disintegrating compositions comprising taste-masked microparticles of a substituted benzhydrylpiperazine and rapidly dispersing granules, and methods of making such orally disintegrating compositions.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: February 24, 2015
    Assignee: Aptalis Pharmatech, Inc.
    Inventor: Gopi Venkatesh
  • Publication number: 20150038480
    Abstract: The invention provides methods of preventing, treating or ameliorating autoimmune diseases, such as diabetes and celiac disease, by decreasing the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease by the administration of small organic compounds. The invention also provides pharmaceutical compositions comprising the therapeutically effective small organic compounds and methods of using the same.
    Type: Application
    Filed: May 29, 2012
    Publication date: February 5, 2015
    Applicants: UNIVERSITY OF FLORIDA RESERCH FOUNDATION INCORPORTED, THE REGENTS OF THE UNIVERSITY OF COLORADO, a body corporate
    Inventors: Aaron Michels, Maki Nakayama, David Ostrov
  • Publication number: 20150037410
    Abstract: The present disclosure relates to a solid composition comprising ranolazine and a spray-dried phosphoric acid salt of dronedarone in a bilayer tablet.
    Type: Application
    Filed: July 29, 2014
    Publication date: February 5, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Gerber, Neal Huang, Joanna M. Koziara, Feng Zhang
  • Publication number: 20150031703
    Abstract: [Problem] The present invention aims to elucidate a polynucleotide as a novel responsible gene for cancer and aims to thus provide a method for detecting the polynucleotide and a polypeptide encoded by the polynucleotide and a detection kit, a probe set, and a primer set for the detection. The present invention also aims to provide a pharmaceutical composition for treating cancer. [Means for Solution] The method detects a fusion gene composed of a portion of an FGFR3 gene and a portion of a TACC3 gene or a fusion protein encoded by the fusion gene. The primer set, the probe set, or the detection kit comprises a sense primer and a probe set designed from the portion encoding FGFR3 and an antisense primer and a probe set designed from the portion encoding TACC3. Since an inhibitor of the polypeptide exhibits antitumor effect, a pharmaceutical composition for treating cancer which is positive for either the fusion gene or the polypeptide is provided.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 29, 2015
    Applicant: Astellas Pharma Inc.
    Inventors: Atsushi Suzuki, Makoto Asaumi, Kazuhisa Tsunoyama, Kouichi Nishimura, Akifumi Morinaka, Tomohiro Yamauchi, Masayasu Yoshino, Hiroaki Yoshizaki
  • Publication number: 20150025083
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 22, 2015
    Applicants: THE JOHNS HOPKINS UNIVERSITY, VANQUISH ONCOLOGY, INC.
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael J. Handley, Avadhut Joshi, Gregory J. Riggins, Theodore M. Tarasow
  • Publication number: 20150017264
    Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Applicants: Vanquish Oncology, Inc., TheBoard of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Howard S. Roth, Theodore M. Tarasow
  • Publication number: 20150018371
    Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 15, 2015
    Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
  • Publication number: 20150011559
    Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a compound of formula I: wherein A, B, and X have any of the meanings defined in the specification; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: January 8, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Yongzheng Zhang, Malvika Kaul
  • Publication number: 20150010493
    Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 8, 2015
    Inventor: Shou-Wei DING
  • Publication number: 20150005315
    Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 1, 2015
    Applicant: RESEARCH TRIANGLE INSTITUTE
    Inventors: Frank I. Carroll, James B. Thomas, Hernan A. Navarro, S. Wayne Mascarella, Scott P. Runyon, Chunyang Jin, Chad M. Kormos
  • Publication number: 20150005306
    Abstract: Provided is a pharmaceutical composition for preventing or treating a cognitive impairment-related disease, the pharmaceutical composition including N-(2-hydroxyethyl)piperazine-N?(3-propane sulfonic acid), a pharmaceutically acceptable salt thereof or a derivative thereof, and donepezil, a pharmaceutically acceptable salt thereof or a derivative thereof. The composition may be used in preventing or treating a cognitive impairment-related disease.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 1, 2015
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Dong Jin KIM, Young Soo Kim, Hye Yun Kim, Hyun Jin Kim
  • Publication number: 20140378467
    Abstract: Compositions and therapeutic uses of HEPES and derivatives in the treatment of pain associated with cancers and side-effects including post-chemotherapy cognitive impairment are disclosed herein. HEPES is also used to treat neurodegenerative and neurological diseases, demyelinization injuries, and side-effects and withdrawal symptoms associated with benzodiazepines, anti-depressants, and other neurological agents.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventor: Ivan E. Danhof
  • Publication number: 20140378465
    Abstract: Methods are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 25, 2014
    Inventors: MARKUS JERLING, ANDREW A. WOLFF
  • Publication number: 20140377219
    Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
    Type: Application
    Filed: September 6, 2012
    Publication date: December 25, 2014
    Applicant: New York Blood CEnter, Inc.
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Publication number: 20140378466
    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: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: ARDEA BIOSCIENCES
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Patent number: 8916568
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: December 23, 2014
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas