Abstract: The present invention provides an agent for alleviating side effects caused by use of an anti-tumor agent, which contains 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H-pyrimidi nedione (1) represented by formula (1): or a pharmaceutically acceptable salt thereof. The 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof exhibit an inflammatory-suppressing action in the digestive tract and advantageously alleviate diarrhea and loss of body weight concomitant with administration of a chemical for treating cancer without suppressing the anti-tumor effect. Thus, the compounds of the present invention are of great value as agents for alleviating side effects caused by use of an anti-tumor agent, which enable not only the chemotherapy to be continuedly carried out, but also the body exhaustion to be effectively prevented.
Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
Type:
Grant
Filed:
October 20, 2015
Date of Patent:
May 21, 2019
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
Abstract: The present invention relates to pyrazine derivatives such as those represented by Formulas I and II below. X1 to X4 of the compounds of Formulas I and II may be characterized as electron withdrawing groups. In contrast, Y1 to Y4 of the compounds of Formulas I and II may be characterized as electron donating groups. Pyrazine derivatives of the present invention may be utilized in assessing renal function. In particular, an effective amount of a pyrazine derivative of the invention may be administered into a body of a patient. The pyrazine derivative that is in the body may be exposed to visible and/or infrared light to cause spectral energy to emanate from the pyrazine derivative. This emanating spectral energy may be detected and utilized to determine renal function of the patient.
Type:
Grant
Filed:
August 2, 2017
Date of Patent:
June 4, 2019
Assignee:
MediBeacon, Inc.
Inventors:
Raghavan Rajagopalan, Richard B. Dorshow, William L. Neumann
Abstract: The preparation of chlorinated hydrocarbons, such as pentachloropropanes, such as 1,1,1,2,3-pentachloropropane, from tetrachloropropanes, such as 1,1,1,3-tetrachloropropane, in the presence of a polyvalent antimony compound that includes a pentavalent antimony compound, such as antimony pentachloride, is described. Also described are methods for preparing optionally chlorinated alkenes, such as, tetrachloropropenes, from chlorinated alkanes, such as pentachloropropanes, in the presence of ferric chloride and a polyvalent antimony compound that includes a pentavalent antimony compound.
Type:
Grant
Filed:
August 23, 2016
Date of Patent:
June 11, 2019
Assignee:
EAGLE US 2 LLC
Inventors:
Scott A. Sherwood, Stephen Robert Lester
Abstract: Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an ?-amino acid moiety. The ?-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.
Abstract: The present invention relates to an improved process for the preparation of Linezolid. More specifically, the present invention relates to an improved process for preparing (S)—N-[[3-[3-fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl] phthalimide and (S)-glycidyl phthalimide intermediates, which are used in the preparation of Linezolid.
Abstract: The present invention refers to a red-dyeing acid dye mixture comprising a dye of the formula (I) and at least one dye of the formula (II) a process for its manufacturing and a process for dyeing and printing of natural or synthetic polyamide fiber material in which it used.
Abstract: This invention relates to a compound of formula I wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
Type:
Grant
Filed:
November 30, 2017
Date of Patent:
October 8, 2019
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Viktor Vintonyak, Matthias Grauert, Marc Grundl, Alexander Pautsch
Abstract: Disclosed is a cytoprotective agent for use with respect to ischemic damage, including as an active ingredient a triprenyl phenol compound represented by the following general formula (I), wherein X is —CHY—C(CH3)2Z, Y and Z are each independently —H or —OH, or jointly form a single bond, and R represents a hydrogen atom or a substituent with a molecular weight of 1000 or less.
Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
Type:
Grant
Filed:
March 6, 2018
Date of Patent:
November 19, 2019
Inventors:
Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel
Abstract: There is disclosed aminopyridine- and aminopyrimidinecarboxamide aminopyridinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyridine- and aminopyrimidinecarboxamides aminopyridinecarboxamide compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.
Type:
Grant
Filed:
July 14, 2016
Date of Patent:
November 26, 2019
Assignee:
Syntrix Biosystems Inc.
Inventors:
Dean Y. Maeda, John A. Zebala, Aaron D. Schuler
Abstract: According to an embodiment, two or more sets of knead forging are performed where one set is cold forging processes in directions parallel to and perpendicular to a thickness direction of a columnar titanium material. The titanium material is heated to a temperature of 700° C. or more to induce recrystallization, and thereafter, two or more sets of knead forging are performed where one set is the cold forging processes in the directions parallel to and perpendicular to the thickness direction. Further, the titanium material is cold rolled, and is heat-treated to a temperature of 300° C. or more.
Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
Type:
Grant
Filed:
April 3, 2018
Date of Patent:
January 7, 2020
Assignee:
EISAI R&D MANAGEMENT CO., LTD.
Inventors:
Farid Benayoud, Trevor Lee Calkins, Charles E. Chase, William Christ, Bryan M. Lewis, Matthew Schnaderbeck, Marc Pesant, Brian Austad, Silvio Campagna, Yongbo Hu, Gordon Wilkie, Xiaojie Zhu, Francis G. Fang
Abstract: Methods, compositions and articles of manufacture for assaying a sample for a target polynucleotide are provided. A sample suspected of containing the target polynucleotide is contacted with a polycationic multichromophore and a sensor polynucleotide complementary to the target polynucleotide. The sensor polynucleotide comprises a signaling chromophore to receive energy from the excited multichromophore and increase emission in the presence of the target polynucleotide. The methods can be used in multiplex form. Kits comprising reagents for performing such methods are also provided.
Type:
Grant
Filed:
March 23, 2018
Date of Patent:
February 25, 2020
Assignee:
The Regents of the University of California
Inventors:
Guillermo C. Bazan, Brent S. Gaylord, Shu Wang
Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
Abstract: The present invention relates to use of DHA analogs and their pharmaceutical compositions for treating ototoxicity, by administering these compounds or pharmaceutical compositions to subjects in need thereof. Ototoxicity is defined as damage to the structures of the ear, such as the cochlea and vestibular system, by drugs or toxins. Ototoxicity can result in irreversible hearing loss, tinnitus, dysequilibrium, Meniere's disease, or vertigo.
Abstract: The present invention relates to SiC nanostructures, including SiC nanopowder, SiC nanowires, and composites of SiC nanopowder and nanowires, which can be used as catalyst supports in membrane electrode assemblies and in fuel cells. The present invention also relates to composite catalyst supports comprising nanopowder and one or more inorganic nanowires for a membrane electrode assembly.
Type:
Grant
Filed:
June 25, 2018
Date of Patent:
July 7, 2020
Assignee:
ONED MATERIAL LLC
Inventors:
Yimin Zhu, Jay L. Goldman, Baixin Qian, Ionel C. Stefan
Abstract: Thermoplastic resin foamed particles of the present invention including more than one or more functional additive selected from inorganic powder and inorganic fibers each includes a core layer formed of a thermoplastic resin and a coating layer in a foamed state formed of a thermoplastic resin, the mass ratio of the coating layer to the core layer is 99:1 to 50:50, the content (X) of the functional additive in the core layer is 5 to 90% by mass, and the content of the functional additive in the coating layer is smaller than the content (X) of the functional additive in the core layer. By this way, thermoplastic resin foamed particles from which a homogeneous foamed particle molding having excellent dimension stability, fusibility and appearance can be obtained while containing functional additive are provided.