Patents Examined by Golam M M Shameem
  • Identification of stabilizers of multimeric proteins
    Patent number: 9308209
    Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and thereby decreasing aggregate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: April 12, 2016
    Assignee: The Board of Trustees of the Leland Stanford Junio
    Inventors: Isabella A. Graef, Mamoun M. Alhamadsheh
  • Process for preparation of optically pure and optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives and their use in preparing pharmaceuticals
    Patent number: 9309216
    Abstract: The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure optionally substituted 2-(1-hydroxy-alkyl)-chromen-4-one derivatives represented by formula (IA) and (IB), processes for preparing the alcohol derivatives and their use in preparing pharmaceuticals.
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: April 12, 2016
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Jayaraman V. Raman, Swaroop K. Vakkalanka
  • Compositions and methods to treat cardiac diseases
    Patent number: 9303053
    Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba(bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: April 5, 2016
    Assignee: UNIVERSITY OF CONNECTICUT
    Inventors: Bruce Liang, Kenneth A. Jacobson
  • Tetracyclic heteroatom containing derivatives useful as sex steroid hormone receptor modulators
    Patent number: 9303037
    Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.
    Type: Grant
    Filed: November 11, 2013
    Date of Patent: April 5, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
  • Inhibitors of p75 receptor and their uses
    Patent number: 9296691
    Abstract: Novel p75 receptor antagonist compounds and compositions and uses thereof for the prevention and treatment of p75-associated disorders, such as neurodegenerative diseases, are described.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: March 29, 2016
    Assignee: Horacio Uri Saragovi
    Inventors: Horacio Uri Saragovi, Hinyu Nedev
  • Cyclic boronic acid ester derivatives and therapeutic uses thereof
    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
  • Tyrosinase inhibitors
    Patent number: 9289364
    Abstract: The compositions and methods of described herein comprise novel ingredients effective to reduce unwanted pigmentation, such as skin discoloration, freckles, age spots, liver spots, sun damage, tans, pigmented acne marks, scars, pigmented birthmarks, hyperpigmentation, post-inflammatory hyperpigmentation, post-injury hyperpigmentation, melasma, cholasma, after-burn scar, nail stain, yellowing of skin, dark circles under eyes, and the like. The composition may include additional ingredients accordingly for a colored cosmetic, moisturizer, cleanser, toner, and the like.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: March 22, 2016
    Assignee: Avon Products, Inc.
    Inventors: Hong Hu, Sunghan Yim, Uma Santhanam, John W. Lyga
  • Anti-invasive compounds
    Patent number: 9290427
    Abstract: The present invention relates to the field of anti-invasive compounds and methods for predicting the anti-invasive activity of said compounds, as well as their use in the prevention and/or treatment of diseases associated with undesired cell invasion; in particular, this invention relates to the field of anti-invasive chalcone-like compounds.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: March 22, 2016
    Assignee: Universiteit Gent
    Inventors: Marc Bracke, Christian Stevens, Tine De Ryck, Bart Roman, Barbara Vanhoecke
  • 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as Btk inhibitors
    Patent number: 9290504
    Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Petrus Antonius De Adrianus Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan-Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
  • Substituted fused pyrimidine compounds
    Patent number: 9284316
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: March 15, 2016
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Trimethylangelicin as CFTR corrector in bronchial epithelial cells
    Patent number: 9283206
    Abstract: The invention relates to the use of 4,6,4?-trimethylangelicin (TMA) and structural analogs thereof to prepare a medicament for the treatment of cystic fibrosis with the primary objective of correcting the defective CFTR in a sub-group of cystic fibrosis patients consisting of patients carrying the F508del-CFTR mutation.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: March 15, 2016
    Assignees: Azienda Ospedaliera Universitaria Integrata di Verona, Universita' degli Studi di Ferrara, Universita' degli Studi di Bari, Rare Partners S.r.l.
    Inventors: Giulio Cabrini, Valeria Casavola, Roberto Gambari
  • Process for the production of the mixture 2,4 furandicarboxylic acid (FDCA) and 2,5 furandicarboxylic acid via disproportionation reaction
    Patent number: 9284290
    Abstract: The present invention refers to a process for production of a mixture including 2,4-furandicarboxylic acid (2,4-FDCA) and 2,5 furandicarboxylic acid (2,5-FDCA) through the disproportionation route, using as base compounds oxidation products of furfural. This invention also relates to a process for production of 2,4-FDCA as a result of a disproportionation route and the use of 2,4-FDCA as a monomer or comonomer to synthesize esters or any compounds which can generate macromolecules, such as polyesters.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: March 15, 2016
    Assignee: Braskem S.A.
    Inventors: Jacco van Haveren, Shanmugam Thiyagarajan, Augusto Teruo Morita
  • Method for producing tetrahydrofuran
    Patent number: 9284289
    Abstract: The present invention relates to a method for producing tetrahydrofuran, comprising feeding 1,4-butanediol to a reactor and performing a cyclodehydration reaction in the presence of an acid catalyst to obtain tetrahydrofuran, in which a water concentration in a in-reactor liquid phase is within a range of 1.4 to 10 wt %.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: March 15, 2016
    Assignee: MITSUBISHI CHEMICAL CORPORATION
    Inventors: Ryo Yamashita, Seijiro Nishimura, Hisashi Nagahama
  • Methods of using (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione
    Patent number: 9283207
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: March 15, 2016
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Methods for purifying trans-(?)-?-tetrahydrocannabinol and trans-(+)-?-tetrahydrocannabinol
    Patent number: 9278083
    Abstract: Methods for making trans-(?)-?9-tetrahydrocannabinoI and trans-(+)-?9-tetrahydrocannabinol are disclosed herein. In one embodiment, a trans-(?)-?9-tetrahydrocannabinoI composition is prepared by allowing a composition comprising (±)-?9-tetrahydrocannabinol to separate on a chiral stationary phase to provide a trans-(?)-?9-tetrahydrocannabinoI composition comprising at least about 99% by weight of trans-(?)-?9-tetrahydrocannabinol based on the total amount of trans-(?)-?9-tetrahydrocannabinol and trans-(+)-?9-tetrahydrocannabinol. The invention also relates to methods for treating or preventing a condition such as pain comprising administering to a patient in need thereof an effective amount of a trans-(?)-?9-tetrahydrocannabinoI having a purity of at least about 98% based on the total weight of cannabinoids.
    Type: Grant
    Filed: January 13, 2015
    Date of Patent: March 8, 2016
    Assignee: SVC Pharma LP
    Inventors: Arie L. Gutman, Marina Etinger, Irina Fedotev, Ram Khanolkar, Gennady A. Nisnevich, Boris Pertsikov, Igor Rukhman, Boris Tishin
  • Zinc oxide complexes
    Patent number: 9273071
    Abstract: Disclosed are compounds and methods of making said compounds comprising a zinc oxide molecule chemically bound to one or more molecules having an acidic hydrogen, such as an organic acid. The invention also provides compositions comprising such compounds and methods of preparing such compounds. The compounds of the invention may be provided in, for example, topical skin formulations, pharmaceutical compositions, or delivery systems for active ingredients.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: March 1, 2016
    Assignee: Mary Kay Inc.
    Inventor: James Swanzy
  • Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors
    Patent number: 9271962
    Abstract: Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: March 1, 2016
    Assignee: NORTHEASTERN UNIVERSITY
    Inventors: Alexandros Makriyannis, Lakshmipathi Pandarinathan, Nikolai Zvonok, Teija Parkkari, Lauren Chapman
  • Cyclobutyl purine derivative, angiogenesis promoting agent, lumen formation promoting agent, neurocyte growth promoting agent, and drug
    Patent number: 9273050
    Abstract: Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight. A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.
    Type: Grant
    Filed: November 27, 2009
    Date of Patent: March 1, 2016
    Assignee: National University Corporation Kagawa University
    Inventors: Ikuko Tsukamoto, Ryoji Konishi, Masaaki Tokuda, Yasuo Kubota, Tokumi Maruyama, Hiroaki Kosaka, Junsuke Igarashi
  • Combination therapy comprising a CDK4/6 inhibitor and a P13K inhibitor for use in the treatment of cancer
    Patent number: 9271988
    Abstract: A combination of a CDK4/6 inhibitor and a P3Kinase inhibitor for the treatment of cancer.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: March 1, 2016
    Assignee: Novartis AG
    Inventors: Sunkyu Kim, Shivang Doshi, Kristy Haas, Steven Kovats, Alan Xizhong Huang, Yan Chen
  • AMPK—activating heterocyclic compounds and methods for using the same
    Patent number: 9266856
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: February 23, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi