Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/369)
  • Patent number: 10995088
    Abstract: Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.
    Type: Grant
    Filed: June 22, 2020
    Date of Patent: May 4, 2021
    Assignee: THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL
    Inventors: Caroline Springer, Richard Marais, Dan Niculescu-Duvaz, Leo Leung, Deborah Smithen, Cedric Callens, Haoran Tang
  • Patent number: 10960013
    Abstract: Provided is a method of preventing and/or treating a skin disorder and/or an oral disorder including administering to a subject in need thereof an effective amount of a compound of formula (I) or a prodrug or derivative thereof, and salts thereof.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: March 30, 2021
    Assignee: East Carolina University
    Inventor: Rukiyah T. Van Dross
  • Patent number: 10961187
    Abstract: Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: March 30, 2021
    Assignee: Promentis Pharmaceuticals, Inc.
    Inventors: Michael Neary, James Nieman, Steven Tanis, Daniel Lawton, Garry Smith
  • Patent number: 10894054
    Abstract: The present application relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one additional therapeutic agent that lowers the glucose level in the blood, stimulates insulin secretion, and/or increases insulin sensitivity. The present application relates to use of the pharmaceutical composition for the treatment or prevention of a FXR mediated disease or condition, such as NAFLD and NASH, a disease or condition related to an elevated level of glucose in the blood, decreased secretion of insulin, and/or decreased insulin sensitivity such as hyperglycemia, diabetes, obesity, and insulin resistance, or for lowering the glucose level in the blood, stimulating insulin secretion, and/or increasing insulin sensitivity.
    Type: Grant
    Filed: April 6, 2016
    Date of Patent: January 19, 2021
    Assignee: Intercept Pharmaceuticals, Inc.
    Inventors: Mark Pruzanski, Luciano Adorini
  • Patent number: 10869718
    Abstract: Systems, device and methods treat target tissue to provide a therapeutic benefit to the patient. A tissue treatment device comprises a tissue treatment element constructed and arranged to treat target tissue, such as duodenal mucosa tissue.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: December 22, 2020
    Assignee: Fractyl Laboratories, Inc.
    Inventors: Harith Rajagopalan, Jay Caplan, Craig M. Gardner, J. Christopher Flaherty
  • Patent number: 10857134
    Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.
    Type: Grant
    Filed: January 29, 2019
    Date of Patent: December 8, 2020
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Jasper Dingemanse, Matthias Hoch, Andreas Krause
  • Patent number: 10807974
    Abstract: Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: October 20, 2020
    Assignee: The Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Caroline Springer, Richard Marais, Dan Niculescu-Duvaz, Leo Leung, Deborah Smithen, Cedric Callens, Haoran Tang
  • Patent number: 10723728
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Grant
    Filed: August 14, 2019
    Date of Patent: July 28, 2020
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Orn Almarsson, Tarek A. Zeidan
  • Patent number: 10723726
    Abstract: The present invention provides new salts and crystalline forms of leukadherin LA1 [(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid] according to Formula I. Methods for preparation of the salts and crystalline forms are also described, as well as methods for treating 2 integrin-mediated diseases and conditions using the salts and crystalline forms.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: July 28, 2020
    Assignee: GB006, INC.
    Inventor: Antonio J. Barbosa
  • Patent number: 10544113
    Abstract: A pharmaceutical composition containing a compound of Formula (I) for treating an opioid receptor-associated condition. Also disclosed is a method for treating an opioid receptor-associated condition using such a compound. Further disclosed are two sets of thiazolidinone compounds of formula (I): (i) compounds each having an enantiomeric excess greater than 90% and (ii) compounds each being substituted with deuterium.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: January 28, 2020
    Assignees: National Health Research Institute, Regents of the University of Minnesota
    Inventors: Shau-Hua Ueng, Shiu-Hwa Yeh, Shu-Yu Lin, Chuan Shih, Horace Loh
  • Patent number: 10525019
    Abstract: This invention relates to pharmaceutical composition and methods of using vitamin A and/or RAR? agonist for the treatment or prevention of diseases or conditions associated with high fat diet and/or vitamin deficiency.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: January 7, 2020
    Assignee: CORNELL UNIVERSITY
    Inventors: Lorraine J Gudas, Yannick Benoit, Ronald Perez, Xiao-Han Tang, Steven Trasino
  • Patent number: 10517838
    Abstract: The invention refers to novel compositions with at least one prehormone, hormone from group consisting of mevalonate derivatives or from the group consisting of peptides and/or proteohormones and at least one mineral, constituent by preference iodine, selen and at least one Ginkgoloide against alkyl-acyl-GPC (AAGPC), its derivatives (alkyllipids) and/or products (e.g. acetylacyl-CoA). These new hormonal compositions are manufactured with at least one Ginkgoloide and/or acetylcysteine for oral, dietary, oily or local, cosmetic administration. Novel cosmetic preparations without addition of ether/volatile oils contain Ginkgoloides with at least one sun screening agent against impairments of pigmentation. The novel compositions are manufactured with prehormones and constituents to protect against alkylacyl-like destabilization of cells by preference under the conditions of critical lifestyle, critical morning urine samples and/or hypersensitivity syndromes.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: December 31, 2019
    Inventor: Ruth-Maria Korth
  • Patent number: 10501413
    Abstract: Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: December 10, 2019
    Assignees: UNIVERSITY OF MIAMI, UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Anthony J. Capobianco, Alex Mackerell, Jr., Mark Spyvee
  • Patent number: 10478411
    Abstract: Treatment of intrahepatic cholestatic diseases by therapy with seladelpar or a salt thereof.
    Type: Grant
    Filed: March 28, 2019
    Date of Patent: November 19, 2019
    Assignee: CymaBay Therapeutics, Inc.
    Inventors: Pol Boudes, Charles A. McWherter
  • Patent number: 10393733
    Abstract: The present invention provides methods of predicting cell sensitivity or resistance to a therapeutic agent.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: August 27, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Anthony Letai, Juan Jose Montero Boronat, Jeremy Ryan
  • Patent number: 10336760
    Abstract: The present invention provides novel compounds described herein, such as 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 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: July 2, 2019
    Assignee: SYROS PHARMACEUTICALS, INC.
    Inventors: Jason J. Marineau, Kevin Sprott, Darby Schmidt
  • Patent number: 10266870
    Abstract: A method of preparing a sample for cytometry detection of viable biological contaminants includes obtaining a non-aqueous sample, obtaining a suitable solvent, and filtering the suitable solvent creating a filtered solvent. The non-aqueous sample is combined with the filtered solvent creating a mixture for cytometry testing.
    Type: Grant
    Filed: September 7, 2018
    Date of Patent: April 23, 2019
    Assignee: Eagle Analytical Services, Inc.
    Inventor: Ross A. Caputo
  • Patent number: 10239871
    Abstract: A method of treating inflammation, by administering an effective amount of a ?2 integrin agonist to a patient, and reducing inflammation. A method of treating cancer, by administering an effective amount of a ?2 integrin agonist to a patient, and reducing tumor growth. A method of treating a patient exposed to radiation, by administering an effective amount of a ?2 integrin agonist to the patient after radiation exposure, and mitigating the effects of radiation exposure in the patient. A method of preventing effects of radiation, by administering an effective amount of a ?2 integrin agonist to the patient prior to radiation exposure, and preventing the effects of radiation exposure on the patient. A method of treating acquired bone marrow failure (BMF), by administering an effective amount of a ?2 integrin agonist to a patient. Methods of improving the health of damaged vasculature in a patient and activating ?2 integrins.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: March 26, 2019
    Assignee: ADHAERE PHARMACEUTICALS, INC.
    Inventor: Vineet Gupta
  • Patent number: 10206398
    Abstract: Provided are compounds of the formula (I) which are suitable for controlling animal pests including arthropods and in particular insects and acarids and in which the structural elements have the meanings given in the description.
    Type: Grant
    Filed: December 8, 2015
    Date of Patent: February 19, 2019
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Silvia Cerezo-Galvez, Bernd Alig, Reiner Fischer, Julia Johanna Hahn, Tobias Harschneck, David Wilcke, Kerstin Ilg, Olga Malsam, Peter Lösel, Adeline Köhler, Daniela Portz, Ulrich Görgens, Sascha Eilmus
  • Patent number: 10196411
    Abstract: The invention relates to tizoxanide phosphate or alkane sulfonate compounds represented by Formula I, and pharmaceutically acceptable salts thereof, isomers thereof, hydrates thereof or solvates thereof, and pharmaceutical applications of the compounds.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: February 5, 2019
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Xingzhou Li, Wu Zhong, Zhibing Zheng, Junhai Xiao, Xinbo Zhou, Yunde Xie, Xiaokui Wang, Lili Wang, Wei Chen, Fei Xie
  • Patent number: 10045535
    Abstract: The invention relates to novel active substance combinations consisting of heterocyclic trifluorobutenylen of formula (1), wherein X is halogen and n is 0, 1 or 2, and of known insecticide substances. Said novel active substance combinations are suitable for fighting harmful pests like insects and nematodes.
    Type: Grant
    Filed: April 11, 2017
    Date of Patent: August 14, 2018
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: Wolfram Andersch, Anton Kraus, Koichi Ishikawa
  • Patent number: 10010512
    Abstract: This invention relates to pharmaceutical composition and methods of using vitamin A and/or RAR? agonist for the treatment or prevention of diseases or conditions associated with high fat diet and/or vitamin deficiency.
    Type: Grant
    Filed: January 24, 2017
    Date of Patent: July 3, 2018
    Assignee: CORNELL UNIVERSITY
    Inventors: Lorraine J Gudas, Yannick Benoit, Ronald Perez, Xiao-Han Tang, Steven Trasino
  • Patent number: 9999617
    Abstract: The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in S. aureus. The compositions also have the ability to inhibit growth of S. aureus and as such are useful as antibiotic compounds.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: June 19, 2018
    Assignee: TRUSTEES OF DARTMOUTH COLLEGE
    Inventors: Ambrose Cheung, Zhibiao Fu
  • Patent number: 9889124
    Abstract: The present invention relates to the crystalline mono mesylate monohydrate salt of N-[5 -(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide in a definite particle size range, particle size distribution and a specific surface area range, which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions, as well as to pharmaceutical compositions containing said crystalline N-[5-(amino sulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2 -pyridinyl)phenyl]acetamide mono mesylate monohydrate having the afore-mentioned particle size range, particle size distribution and specific surface area range.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: February 13, 2018
    Assignee: AICURIS ANTI-INFECTIVE CURES GMBH
    Inventors: Wilfried Schwab, Alexander Birkmann, Kerstin Paulus, Kurt Vogtli, Dieter Haag, Stephan Maas, Kristian Ruepp
  • Patent number: 9789088
    Abstract: The invention provides methods, compositions, and kits containing phentolamine for improving visual performance. In particular, the invention provides improvement in visual performance, such as improvement in visual acuity, by daily ophthalmic administration of a phentolamine solution to an eye of a patient at or near the bedtime of the patient for an extended duration while minimizing the occurrence of adverse side effects, such as eye redness during the patient's waking hours.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: October 17, 2017
    Assignee: Ocularis Pharma, LLC
    Inventor: Alan Meyer
  • Patent number: 9771430
    Abstract: The present invention relates to methods of treating or preventing a metabolic disorder in a subject, methods of treating or preventing coronary artery disease in a subject with a metabolic disorder, as well as methods of reducing hepatic glucose production in a subject. Such methods include, but are not limited to, the administration to the subject of inhibitors or activators of CaMKII, IP3Rs, calcineurin, p38, MK2/3, HDAC4, Dach1, Dach2, or any combination thereof. The invention also provides methods of identifying a compound that inhibits the activity of CaMKII, IP3Rs, calcineurin, p38, MK2/3, HDAC4, Dach1 or Dach2, or reduces the activity and/or activation of CaMKII, IP3Rs, calcineurin, p38, MK2/3, HDAC4, Dach1 or Dach, or activates CaMKII, IP3Rs, calcineurin, p38, MK2/3, HDAC4, Dach1 or Dach2.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: September 26, 2017
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Ira Tabas, Lale Ozcan
  • Patent number: 9751857
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: September 5, 2017
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Patent number: 9750712
    Abstract: Provided herein are methods for treatment of a neurodegenerative disease, such as neuronal ceroid lipofuscinosis including administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of an agent that mediates upregulation of TPP 1.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: September 5, 2017
    Assignee: Rush University Medical Center
    Inventor: Kalipada Pahan
  • Patent number: 9683002
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: August 3, 2015
    Date of Patent: June 20, 2017
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Patent number: 9642366
    Abstract: Disclosed are novel active substance combinations comprising specific heterocyclic trifluorobutenyls and previously known fungicidal agents. Said active substance combinations have a very good synergistic fungicidal, nematicidal, insecticidal, and/or acaricidal effect.
    Type: Grant
    Filed: June 3, 2015
    Date of Patent: May 9, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: Wolfram Andersch, Ulrike Wachendorff-Neumann, Anton Kraus
  • Patent number: 9622982
    Abstract: A pharmaceutical composition comprising a cancer therapeutic that is capable of inhibiting and/or reducing the ability of a cancer cell to take up and utilize glucose or other energy source, a lipid or other building block of a cell membrane or organelle, and/or cholesterol. The pharmaceutical composition can comprise one or more cancer therapeutics that can be administered individually or in combination to an individual.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: April 18, 2017
    Assignee: HEALTH CLINICS LIMITED
    Inventors: Robin M. Bannister, John Brew, Gregory A. Stoloff
  • Patent number: 9617253
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: April 11, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Natalie C. Giampietro, Gary D. Crouse, Thomas C. Sparks, David A. Demeter
  • Patent number: 9585857
    Abstract: This invention relates to pharmaceutical composition and methods of using vitamin A and/or RARB agonist for the treatment or prevention of diseases or conditions associated with high fat diet and/or vitamin deficiency. After smoking, high fat diet is said to be the second most lethal habit, causing 300,000 deaths each year in the U.S. alone. High fat diet leads to many health problems, including obesity, stroke, cancer, high blood pressure, diabetes, osteoarthritis, rheumatoid arthritis, multiple sclerosis, heart disease, and diseases in other organs such as liver and kidney.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 7, 2017
    Assignee: Cornell University
    Inventors: Lorraine J Gudas, Yannick Benoit, Ronald Perez, Xiao-Han Tang, Steven Trasino
  • Patent number: 9579331
    Abstract: A prodrug having antioxidant activity, including a phosphorylated compound having a thiol group. A method of treating oxidative stress by administering a prodrug of a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug, and treating oxidative stress. A method of increasing bioavailability of a thiol compound by creating a prodrug by phosphorylating a thiol compound, administering the prodrug, preventing first pass metabolism of the prodrug, removing a phosphate group from the prodrug, and providing active drug to a site in need of therapy from oxidative stress. A method of preventing radiation damage to healthy tissue by administering a prodrug comprising a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug to provide active drug, and preventing radiation damage to healthy tissue.
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: February 28, 2017
    Assignee: Board of Trustees of Northern Illinois University
    Inventors: Elizabeth R. Gaillard, James P. Dillon
  • Patent number: 9517230
    Abstract: Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: December 13, 2016
    Assignees: UNIVERSITY OF ROCHESTER, BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA, TEMPLE UNIVERSITY—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Paul M. Dunman, Patrick D. Olson, Wayne Childers
  • Patent number: 9447056
    Abstract: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: September 20, 2016
    Assignee: BIONEVIA PHARMACEUTICALS, INC.
    Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Travis L. Houston
  • Patent number: 9376408
    Abstract: Thiazolidinone compounds, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: June 28, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Revathi Reddy Katipally
  • Patent number: 9340535
    Abstract: The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: May 17, 2016
    Assignee: AICURIS GMBH & CO. KG
    Inventors: Wilfried Schwab, Alexander Birkmann, Kurt Vogtli, Dieter Haag, Andreas Lender, Alfons Grunenberg, Birgit Keil, Joachim Rehse
  • Patent number: 9339458
    Abstract: A method for the treatment and/or prevention of hyperandrogenism and/or polycystic ovary syndrome and/or related disorders comprising the vaginal administration of at least one insulin-sensitizing agent.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: May 17, 2016
    Assignee: ITF RESEARCH PHARMA, S.L.U.
    Inventors: Jaime Moscoso Del Prado, Beatriz Banfi Tosi
  • Patent number: 9309208
    Abstract: The present invention provides methods of making and using 5-(2-(indol-3-yl)-2-oxoethylidene)-3-phenyl-2-thioxothiazolidin-4-one derivatives having HIV-1 or JSP-1 inhibitory activity.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: April 12, 2016
    Assignees: Southern Methodist University, Johns Hopkins University
    Inventors: Edward R. Biehl, Sukanta Kamila, Ted M. Dawson
  • Patent number: 9266872
    Abstract: The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.
    Type: Grant
    Filed: April 18, 2014
    Date of Patent: February 23, 2016
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Semi Kim, Ill Young Lee, Hye-Jin Min, Eun-Hee Nam, Pilho Kim, Chang Soo Yun, Dong Joon Ko
  • Patent number: 9211254
    Abstract: The invention provides an ophthalmic product containing rebamipide, which has a transparency enough to be agreeable feeling on using it and has neutral to weakly acidic pH not to injury of the keratoconjunctiva of a patient suffering from dry eye. An aqueous suspension of crystalline rebamipide which has an improved transparency is provided by adding an aqueous solution of rebamipide dissolved by a base such as sodium hydroxide or an aqueous solution of a salt of rebamipide to an aqueous acidic solution such as hydrochloric acid containing at least one of the compounds selected from water-soluble polymers and surfactants, and mixing them.
    Type: Grant
    Filed: November 11, 2005
    Date of Patent: December 15, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Takakuni Matsuda, Shogo Hiraoka, Yuso Tomohira, Shinichi Ishikawa
  • Patent number: 9174951
    Abstract: Thiazolidinedione compounds and pharmaceutically acceptable salts thereof are described. The compounds can be used in methods of treating cancer in a subject by administering to the subject a therapeutically effective amount of the compound. The compounds can also be used in methods of inhibiting glucose uptake in a cell by contacting the cell with the compound.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: November 3, 2015
    Assignee: OHIO STATE INNOVATION FOUNDATION
    Inventors: Ching-Shih Chen, Dasheng Wang, Samuel K. Kulp
  • Patent number: 9173875
    Abstract: This invention provides pertains to the discovery that that nicotine interrupts molecular signaling between endodermal and mesodermal cells of the lung alveolus. Treatment of the lung with specific molecular agents (e.g., PPAR gamma agonists) can prevent and/or reverse the injury caused by nicotine.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: November 3, 2015
    Assignee: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventors: Virender K. Rehan, John S. Torday
  • Patent number: 9084798
    Abstract: A pharmaceutical composition for treating diabetes is provided in this invention. The composition contains a lanostane compound as a potent component. A suitable source of the lanostane compound is a Poria extract from metabolite, sclerotium, or fermentation product of Poria cocos (Schw) Wolf. The Poria extract contains 1-60% of the lanostane compounds by weight of the extract, and is devoid of secolanostane.
    Type: Grant
    Filed: August 10, 2010
    Date of Patent: July 21, 2015
    Assignee: Sinphar Tian-Li Pharmaceutical Co., Ltd (Hangzhou)
    Inventors: Hang-Ching Lin, Yu-Chuan Huang, Tsu-Chung Chang, Wen-Liang Chang
  • Patent number: 9073853
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: July 7, 2015
    Assignee: SANOFI
    Inventors: Imre Bata, Peter Buzder-Lantos, Attila Vasas, Veronika Bartane Bodor, Gyorgy Ferenczy, Zsuzsanna Tomoskozi, Gabor Szeleczky, Sandor Batori, Martin Smrcina, Marcel Patek, Aleksandra Weichsel, David Squire Thorpe
  • Patent number: 9072300
    Abstract: Disclosed are novel active substance combinations comprising specific heterocyclic trifluorobutenyls and previously known fungicidal agents. Said active substance combinations have a very good synergistic fungicidal, nematicidal, insecticidal, and/or acaricidal effect.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 7, 2015
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: Wolfram Andersch, Ulrike Wachendorff-Neumann, Anton Kraus
  • Publication number: 20150139978
    Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
  • Publication number: 20150139915
    Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Stefan Worgall, Tilla S. Worgall
  • Publication number: 20150133514
    Abstract: Protein disulfide isomerase inhibitors according to formula I are described, wherein R1 is an aryl or cycloalkyl group, R2 is selected from the group consisting of CN, SO2CH3, NO2, CO2R3, CONHR3, NMe2, and CF3, R3 is selected from H or lower alkyl, R4 is H, halogen, CN, or COOH, and X and Y are C—H or heteroatoms selected from the group consisting of N, O, and S. The protein disulfide isomerase inhibitors can be used for the treatment of cancer in a subject.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Frederic J. Reu, Jim Phillips, Sergei Vatolin, Dale Grabowski