Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
  • Patent number: 10881655
    Abstract: The present disclosure relates generally to compositions and methods of treating neoplastic diseases or cancers, such as glioblastoma and non-Hodgkin's lymphomas, or other cancers in which the subject suffers from an advanced solid tumor, comprising a combination of, or administering a combination of, a bromodomain and extra-terminal protein (BET) inhibitor and at least one chemotherapeutic agent, which does not inhibit BET directly. The BET inhibitor/chemotherapeutic agent combination, or combination therapy, can yield synergistic effects, thereby increasing the effectiveness of the cancer treatment as compared with the administration of either the BET inhibitor or the chemotherapeutic agent alone.
    Type: Grant
    Filed: January 23, 2020
    Date of Patent: January 5, 2021
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Robert Cho, Jeffrey Alan Stafford
  • Patent number: 10875831
    Abstract: A method for preparing an alkyl 5,7-dihalo-1,4-dihydro-4-oxoquinoline-2-carboxylate ester is described herein. The method comprises cyclizing a compound of Formula III with Eaton's reagent in heated continuous flow reactor to form a compound of Formula IV wherein in Formula III and Formula IV, each X independently is a halogen atom; and each R independently is C1 to C4 alkyl. Optionally, a cosolvent such as dichloromethane can be included with the Eaton's reagent. A method of preparing a diphenylureido-dihalokynurenic acid alkyl ester of Formula VI from the compound of Formula IV also is described.
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: December 29, 2020
    Assignee: Lohocla Research Corporation
    Inventors: Sergiy Krasutsky, Scott Tweedie, Gurusankar Ramamoorthy
  • Patent number: 10865206
    Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: December 15, 2020
    Assignee: Syros Pharmaceuticals, Inc.
    Inventors: Stephane Ciblat, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Jason J. Marineau, Tom Miller, Stephanie Roy, Darby Schmidt, M. Arshad Siddiqui, Kevin Sprott, Dana K. Winter, Amy Ripka, Dansu Li, Guoli Zhang
  • Patent number: 10851061
    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: December 1, 2020
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Patent number: 10844416
    Abstract: The present invention pertains to a cell culture medium comprising manganese as a media supplement, which was shown to control recombinant protein glycosylation and methods of using thereof. The present invention further pertains to a method of controlling or manipulating glycosylation of a recombinant protein of interest in a large scale cell culture.
    Type: Grant
    Filed: June 1, 2016
    Date of Patent: November 24, 2020
    Assignee: Biogen MA Inc.
    Inventors: Lia Tescione, Thomas Ryll, Alan Gilbert
  • Patent number: 10772865
    Abstract: The present invention relates to methods for treating a disease associated with insulin resistance selected from a nonalcoholic fatty liver disease (NAFLD) and its sequelae, a lipodystrophic syndrome or a combination thereof with the selective PPAR? agonist, INT131 and optionally vitamin E or compositions thereof. NAFLDs that may be treated with methods and compositions of the present invention include, but are not limited to, simple nonalcoholic fatty liver and nonalcoholic steatohepatitis (NASH). Lipodystrophic syndromes that may be treated with the methods and compositions of the present invention include, but are not limited to, generalized lipodystrophy including congenital generalized lipodystrophy and acquired generalized lipodystrophy and/or partial lipodystrophy, including congenital partial lipodystrophy and acquired partial lipodystrophy, all of which may or may not include hyperlipidemia and/or hyperglycemia and may or may not include NAFLD.
    Type: Grant
    Filed: January 16, 2020
    Date of Patent: September 15, 2020
    Assignee: Coherus Biosciences, Inc.
    Inventor: Christos Mantzoros
  • Patent number: 10745390
    Abstract: Methods for improving mitochondrial function, decreasing iron accumulation, and/or decreasing oxidative stress by exposing cells or treating a subject to compounds or compositions of the general formula are described that are beneficial in treating, for example, diseases and conditions such as Friedreich's ataxia, normal aging, and various neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. Furthermore, such compounds are useful as probes for identifying defects in mitochondrial metabolism, mitochondrial iron accumulation, cellular stress among other mitochondrial diseases and helping to identify compounds active in overcoming such defects.
    Type: Grant
    Filed: June 2, 2017
    Date of Patent: August 18, 2020
    Assignee: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Robert B. Wilson, Maria Grazia Cotticelli, Phillip A. Benedetti, Amos Smith, Jason E. Melvin, Donna M Huryn
  • Patent number: 10744127
    Abstract: The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: August 18, 2020
    Assignee: Magyar Tudományos Akadémia Természettudományi Kutatóközpont
    Inventors: Gergely Szakács, Tibor Soós, Roberta Ferenczi-Palkó, András Füredi, Szilárd Tóth, Dóra Türk, Veronika Pape, Ferenc Fülöp, István Szatmári, György Dormán
  • Patent number: 10736886
    Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: August 11, 2020
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Thomas Mueller, Aaron Weitzman, Jaymes Holland
  • Patent number: 10683274
    Abstract: The present invention provides a compound of the following Formula (1) or a pharmaceutically acceptable salt thereof: wherein X is an oxygen atom and the like; Y is —CO—, —SO2— and the like; R1 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkylcarbonyl group and the like; R2 is an optionally-substituted C1-6 alkyl group, an optionally-substituted C1-6 alkoxy group, an optionally-substituted amino group, an optionally-substituted 5- to 12-membered monocyclic or polycyclic saturated heterocyclic group and the like; R3, R4, R5, and R6 are independently a hydrogen atom and the like which exhibits excellent effects in suppressing the proliferation and sphere-forming ability of cancer cells, and can be useful as an antitumor drug or cell growth inhibitor.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: June 16, 2020
    Assignee: Boston Biomedical, Inc.
    Inventors: Toshihiko Sone, Wataru Hirose, Naoaki Shimada, Chiang Li, Wei Li, David Leggett
  • Patent number: 10675366
    Abstract: The present disclosure provides a positron emission tomography (PET)-detectable 1-((2-fluoro-6-[18F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) probe that can selectively bind to the pyruvate kinase variant M2 (PKM2) found in cancer cells, such as of human glioma. Given the importance of PKM2 in the regulation of tumor metabolism, there is an on-going need to non-invasively measure its expression through the development of PKM2-specific radiopharmaceuticals. Precursors useful for the synthesis of the radiolabeled [18F]DASA-23-PKM2-specific probe and related compounds, and their methods of synthesis, are provided. Since the half-life of the 18F isotope is approximately 110 min, it is advantageous for a practitioner to attach the radionuclide to the precursor shortly before administration. Therefore, a precursor compound suitable for receiving the radionuclide and capable of specifically binding to the PKM2 variant can be provided.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: June 9, 2020
    Assignee: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Corrine Gaye Beinat, Israt Shamima Alam, Michelle L. James, Sanjiv S. Gambhir, Ananth Srinivasan
  • Patent number: 10662207
    Abstract: The present disclosure is directed to disclosed compounds that modulate e.g., address underlying defects in cellular processing of CFTR activity.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: May 26, 2020
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Benito Munoz, Daniel Parks, Cecilia M. Bastos
  • Patent number: 10654807
    Abstract: Compounds described herein can be used for therapeutic purposes. The compounds can be TLR agonists, such as TLR8 agonists. The compounds can be included in pharmaceutical compositions and used for therapies were being a TLR8 agonist is useful. The pharmaceutical compositions can include any ingredients, such as carries, diluents, excipients, fillers or the like that are common in pharmaceutical compositions. The compounds can be those illustrated or described herein as well as derivative thereof, prodrug thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combinations thereof. As such, the compounds can be used as adjuvants in vaccines as well as for other therapeutic purposes described herein. The compounds can have any one of the formulae described herein or derivative thereof.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: May 19, 2020
    Assignee: The University of Kansas
    Inventors: Sunil Abraham David, Hari Prasad Kokatla, Diptesh Sil, Subbalakshmi Malladi, Lauren Miranda Fox
  • Patent number: 10639299
    Abstract: Described herein are compounds that can bind CaSR and/or a CaSR extracellular domain and formulations thereof. Also described herein are methods of inhibiting CaSR and/or treating a disease or disorder associated with a mutation in CaSR by administering a compound or formulation thereof described herein. Also described herein are assays that can be used to identify compounds that can bind an extracellular domain of CaSR.
    Type: Grant
    Filed: March 29, 2017
    Date of Patent: May 5, 2020
    Assignees: Georgia State University Research Foundation, Inc., University of Georgia Research Foundation, Inc., Board of Trustees of Michigan State University
    Inventors: Jenny Jie Yang, Jian Hu, Edward Brown, Kelley Moremen
  • Patent number: 10588900
    Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.
    Type: Grant
    Filed: February 7, 2017
    Date of Patent: March 17, 2020
    Assignee: PHARMAKEA, INC.
    Inventors: Martin W. Rowbottom, John Howard Hutchinson
  • Patent number: 10583133
    Abstract: The present invention relates to a pharmaceutical composition comprising lenvatinib mesylate and a stabilizer in an amount of about 10% to about 20% based on the total weight of the composition, wherein the stabilizer is selected from the group consisting of calcium hydroxide and potassium hydroxide; and its process for preparation thereof.
    Type: Grant
    Filed: March 1, 2019
    Date of Patent: March 10, 2020
    Assignee: SHILPA MEDICARE LIMITED
    Inventors: Nijaguni Revansiddayya Rudraswamy Math, Sreenivas Reddy, Ravi Vamsi Peri, Krishnamurthy Toppaladoddi, Shivakumar Pradeep
  • Patent number: 10556883
    Abstract: Compounds having formula (I) are described. Also described, are methods of using these compounds to treat diseases, conditions, and disorders.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: February 11, 2020
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Gilles Ouvry, Craig Steven Harris, Yushma Bhurruth-Alcor
  • Patent number: 10548888
    Abstract: Pharmaceutical compositions and unit dosage forms comprising Compound (I) are disclosed.
    Type: Grant
    Filed: July 3, 2018
    Date of Patent: February 4, 2020
    Assignee: EXELIXIS
    Inventors: Jo Ann Wilson, Khalid Shah
  • Patent number: 10508097
    Abstract: The present invention relates to compounds of formula (I) including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of tuberculosis.
    Type: Grant
    Filed: March 7, 2017
    Date of Patent: December 17, 2019
    Assignees: The Global Alliance for TB Drug Development, Inc., Janssen Pharmaceutica NV
    Inventors: Anna Marie Upton, Christopher Blair Cooper, Koenraad Jozef Lodewijk Marcel Andries, Jerome Emile Georges Guillemont, Walter Marcel Mathilde Van den Broeck, Brian Desmond Palmer, Zhenkun Ma
  • Patent number: 10501438
    Abstract: This application relates to aryl-substituted dihydroquinolinones of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to aryl-substituted dihydroquinolinones and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: December 10, 2019
    Assignee: Neomed Institute
    Inventors: Guillaume Jacquemot, Malken Bayrakdarian, Shawn Johnstone, Jeffrey S. Albert, Andrew Griffin
  • Patent number: 10501418
    Abstract: The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N?-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.
    Type: Grant
    Filed: February 16, 2015
    Date of Patent: December 10, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Nathan Guz, Stephen Lau, Noel Hamill, Tracy Walker, Jana Galbraith, Simon Yau, Khalid Shah
  • Patent number: 10472342
    Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
    Type: Grant
    Filed: April 12, 2019
    Date of Patent: November 12, 2019
    Assignee: FORMA THERAPEUTICS, INC.
    Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
  • Patent number: 10449189
    Abstract: Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: October 22, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Akio Fujioka
  • Patent number: 10450286
    Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: October 22, 2019
    Assignee: FORMA THERAPEUTICS, INC.
    Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
  • Patent number: 10442817
    Abstract: The present invention includes novel RAD52 inhibitors for preventing or treating cancers in a subject in need thereof. The present invention further includes a method of preventing or treating cancers in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In certain embodiments, the subject is further administered at least one additional therapeutic agent.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: October 15, 2019
    Assignee: Drexel University
    Inventor: Alexander V. Mazin
  • Patent number: 10435389
    Abstract: The present invention relates to compounds capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds, and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.
    Type: Grant
    Filed: September 11, 2018
    Date of Patent: October 8, 2019
    Assignee: Krouzon Pharmaccuticals, Inc.
    Inventors: Robert Volkmann, Anthony Marfat, Frederick Nelson, Panayiotis Zagouras
  • Patent number: 10426767
    Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.
    Type: Grant
    Filed: April 5, 2018
    Date of Patent: October 1, 2019
    Assignee: Kura Oncolofy, Inc.
    Inventors: Antonio Gualberto, Catherine Rose Scholz
  • Patent number: 10426780
    Abstract: The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: October 1, 2019
    Assignee: ViiV Healthcare Company
    Inventor: Mark Richard Underwood
  • Patent number: 10406149
    Abstract: A novel technique with which it is possible to suppress chemical degradation of a compound represented by general formula (1) or a salt thereof in an aqueous liquid formulation containing a compound represented by general formula (1) or a salt thereof. A method for suppressing the generation of a compound represented by general formula (2) or a salt thereof including containing a compound represented by general formula (1) or a salt thereof and a magnesium compound in an aqueous liquid formulation.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: September 10, 2019
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Wataru Minagawa, Hitoshi Kozuka, Mizuho Shibata, Takahiro Goto, Chifuyu Toriumi, Norihiro Kanayama
  • Patent number: 10407435
    Abstract: The present invention is a compound having the following formula: (Formula (I)) or a pharmaceutically acceptable salt thereof, wherein e.g. X is C or N; n is 1 to 10; each L is independently a 5- to 12-membered heteroaryl containing at least two nitrogen atoms; and W is a zinc-binding group. The compounds are useful as histone deacetylase (HDAC) inhibitors.
    Type: Grant
    Filed: October 29, 2015
    Date of Patent: September 10, 2019
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Somhairle MacCormick, William John Nodes, Cyrille Davy Tomassi
  • Patent number: 10399951
    Abstract: The present invention relates to compounds and compositions for inhibition of FASN, their synthesis, applications, and antidotes.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: September 3, 2019
    Assignee: FORMA THERAPEUTICS, INC.
    Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
  • Patent number: 10376504
    Abstract: The present invention is directed to azacyanoquinolinone compounds of the general structural formula: (wherein R5 and R6 are defined herein) which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 13, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Antonella Converso, Kevin Rodzinak
  • Patent number: 10351527
    Abstract: This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: July 16, 2019
    Assignees: THE UNIVERSITY OF BRITISH COLUMBIA, SIMON FRASER UNIVERSITY
    Inventors: Paul Rennie, Artem Tcherkassov, Robert N. Young, Christophe M. Andre
  • Patent number: 10351568
    Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: July 16, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: Daniel J. Finley, Randall W. King, Byung-Hoon Lee, Min Jae Lee, Timothy C. Gahman
  • Patent number: 10323029
    Abstract: The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: June 18, 2019
    Assignee: The Scripps Research Institute
    Inventors: Edward Roberts, Hugh Rosen, Mariangela Urbano, Miguel A. Guerrero
  • Patent number: 10323036
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: June 18, 2019
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Silvana Marcel Leit de Moradei, Craig E. Masse, Thomas H. McLean, Sayan Mondal
  • Patent number: 10300052
    Abstract: The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: May 28, 2019
    Assignee: The UAB Research Foundation
    Inventors: Steven M Rowe, Mark Dransfield
  • Patent number: 10287265
    Abstract: Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: May 14, 2019
    Assignees: AVIDIN Co. Ltd., SONEAS Research Co. Ltd., Synaging SAS
    Inventors: László Puskás, István Kanizsai, Thierry Pillot, Márió Gyuris, András Szabó, Ferenc Takács, László Hackler
  • Patent number: 10267796
    Abstract: Embodiments of screening methods for determining test agents effective for modifying the appearance of pigmented skin are provided. The screening method may comprise the steps of contacting a cell, a cell culture, or bulk cells with the test agent, wherein the cell, the cell culture, or the bulk cells comprise ADR?1 receptors, and determining based on the binding interaction of the test agent with the ADR?1 receptors whether the test agent is an effective ADR?1 receptor antagonist suitable for modifying the appearance of pigmented skin, wherein a test agent is considered to be an effective ADR?1 receptor antagonist when it defines a half maximal inhibitory concentration of less than about 1000 ppm.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: April 23, 2019
    Assignee: The Procter & Gamble Company
    Inventors: Leo Timothy Laughlin, II, Tomohiro Hakozaki, Wenzhu Zhao, Jiazhen Wang, John Crist Bierman
  • Patent number: 10251876
    Abstract: The present invention provides 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopro-pylamine used for combating a tumor. Specially, the present invention refers to method for treating tumor, pharmaceutical composition and medicinal kit related to the described compound. Administrating the compound with a suitable dosage regimen can not only make the patient's plasma concentration maintain the level of 100 ng/ml or lower, but also achieve effects of treatments and obtain benefits for various tumours.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: April 9, 2019
    Inventors: Shanchun Wang, Xunqiang Wang, Hongmei Gu, Ping Dong, Hongjiang Xu
  • Patent number: 10246443
    Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
    Type: Grant
    Filed: April 13, 2017
    Date of Patent: April 2, 2019
    Assignee: TIANJIN HEMAY ONCOLOGY PHARMACEUTICAL CO., LTD.
    Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
  • Patent number: 10202367
    Abstract: Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R1, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: February 12, 2019
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of Kansas
    Inventors: Tsanyang Liang, Zongyi Hu, Juan Jose Marugan, Noel Terrence Southall, Shanshan He, Xin Hu, Jingbo Xiao, Marc Ferrer, Wei Zheng, Kevin J. Frankowski, Frank J. Schoenen, Kelin Li
  • Patent number: 10166225
    Abstract: This invention is directed to the treatment of osteoporosis using N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: January 1, 2019
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Douglas Clary
  • Patent number: 10166223
    Abstract: The present invention relates to a pharmaceutical composition for the prevention or treatment of diabetes or fatty liver comprising a CYP4A (cytochrome P450A) inhibitor as an active ingredient. The compound of the present invention has activities of promoting glucose uptake into hepatocytes, inhibiting fat accumulation in liver cells, and inhibiting reactive oxygen production in mitochondria, and thus can be very usefully used for the development of a therapeutic agent for diabetes or fatty liver.
    Type: Grant
    Filed: May 18, 2018
    Date of Patent: January 1, 2019
    Assignee: KOREA BASIC SCIENCE INSTITUTE
    Inventors: Gun Hwa Kim, Joo Hyun Park, Min Ji Lee
  • Patent number: 10159666
    Abstract: The invention relates to administration of various pharmaceutical formulations of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve desirable pharmacokinetic and pharmacodynamic effects.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: December 25, 2018
    Assignee: Exelixis, Inc.
    Inventors: Dana T. Aftab, Sriram Naganathan, Wei Xu, Steven Lacy
  • Patent number: 10160726
    Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: December 25, 2018
    Assignee: Novartis AG
    Inventors: Javier de Vicente Fidalgo, Haiying He, Cheng Hu, Zhigan Jiang, Xiaolin Li, Peichao Lu, Wosenu Mergo, Daniel Mutnick, Folkert Reck, Alexey Rivkin, Colin Keith Skepper, Xiaojing Michael Wang, Jianhua Xia, Yongjin Xu
  • Patent number: 10150764
    Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: July 18, 2014
    Date of Patent: December 11, 2018
    Assignee: Epizyme, Inc.
    Inventor: John Emmerson Campbell
  • Patent number: 10150763
    Abstract: A compound of the formula:(I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: December 11, 2018
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. Cecil, Somhairle MacCormick, William J. Nodes, Franck A. Silva
  • Patent number: 10125112
    Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: November 13, 2018
    Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES
    Inventors: Juan Jose Marugan, Jingbo Xiao, Marc Ferrer-Alegre, Catherine Chen, Noel Southall, Wei Zheng, Alexander Agoulnik, Irina Agoulnik
  • Patent number: 10106502
    Abstract: A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: October 23, 2018
    Assignees: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, THE BROAD INSTITUTE, INC.
    Inventors: Longqin Hu, Sadagopan Magesh, Lin Chen, Timothy Lewis, Ben Munoz, Lili Wang