Abstract: The disclosure provides methods and compositions for treating and preventing cancer using 6-substituted coumarin derivatives. The coumarin derivatives of the disclosure have substituents at the 6-position with five carbon atoms or greater. The coumarin derivatives may be further substituted and may be 3,4-dihydrocoumarins. In preferred embodiments, the coumarin derivatives of the disclosure are used to treat pancreatic cancer.
Abstract: This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.
Type:
Grant
Filed:
May 1, 2013
Date of Patent:
July 19, 2016
Assignee:
Gilead Pharmasset LLC
Inventors:
Adrian S. Ray, John O. Link, David W. Oldach, William E. Delaney, IV, Hongmei Mo, Cheng Yong Yang
Abstract: The disclosure provides methods and compositions for treating and preventing cancer using 6-substituted coumarin derivatives. The coumarin derivatives of the disclosure have substituents at the 6-position with five carbon atoms or greater. The coumarin derivatives may be further substituted and may be 3,4-dihydrocoumarins. In preferred embodiments, the coumarin derivatives of the disclosure are used to treat pancreatic cancer.
Abstract: The present invention relates to substituted benzimidazole compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
March 28, 2012
Date of Patent:
July 12, 2016
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
Type:
Grant
Filed:
December 10, 2013
Date of Patent:
July 5, 2016
Assignee:
Genentech, Inc.
Inventors:
Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.
Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
June 14, 2016
Assignee:
NOVARTIS AG
Inventors:
Tom Yao-Hsiang Wu, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan
Abstract: In certain embodiments this invention pertains to the discovery that inhibition of the expression and/or activity of eukaryotic initiation factor 4A (eIF4A) inhibits the aging process. Accordingly, in certain embodiments, methods are provided for inhibiting/slowing aging. The methods typically involve administering to a mammal an agent that inhibits the expression and/or activity of eukaryotic initiation factor 4A (eIF4A) in an amount sufficient to inhibit expression or activity of EIF4A, where the agent is not resveratrol.
Type:
Grant
Filed:
November 18, 2009
Date of Patent:
June 7, 2016
Assignee:
The Regents of the University of California
Abstract: Provided herein are dihydropyrimidine compounds and their pharmaceutical applications, especially for use in treating and preventing HBV diseases. Specifically, provided herein are compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is the use of the compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof for treating and preventing HBV diseases.
Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine and a gamma-aminobutyric acid compound at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.
Type:
Grant
Filed:
December 2, 2011
Date of Patent:
April 5, 2016
Assignee:
Warsaw Orthopedic, Inc.
Inventors:
Jared T. Wilsey, Danielle L. Biggs, Jeffrey C. Marx, William F. McKay, Josee Roy, John Myers Zanella
Abstract: The present invention relates to compounds of general formula 1 for the treatment of bronchial asthma by inhibition of IL-4 or IL-5 pathway inhibition. The present invention also relates to the use of compound of general formula 1 for the treatment of bronchial by inhibition of IL-4 or IL-5 pathway. The present invention also relates to the method of treating asthma by inhibition of IL-4 or IL-5 pathway by administration of compound or said composition through oral, intranasal, route or by inhalation to a mammal in need thereof. Compound of general formula 1 may be used for reducing perivascular and peribronchial inflammation.
Type:
Grant
Filed:
April 11, 2012
Date of Patent:
April 5, 2016
Assignee:
Council of Scientific & Industrial Research
Abstract: This invention relates to methods of treating T-cell mediated diseases or disorders in human or animal subjects, such as autoimmune diseases and chronic graft versus host disease in humans and animals. In particular, the methods comprise administering to the human or animal patient a pharmaceutical composition comprising a ryanodine receptor inhibitor.
Type:
Grant
Filed:
January 16, 2014
Date of Patent:
April 5, 2016
Assignee:
The Regents of the University of California
Abstract: Provided is a pharmaceutical composition for inhibiting apoptosis of neurons or neurodegeneration. The pharmaceutical composition effectively prevents or treats diseases related to apoptosis of neurons or neurodegeneration.
Type:
Grant
Filed:
July 22, 2014
Date of Patent:
March 22, 2016
Assignee:
SK BIOPHARMACEUTICALS CO., LTD.
Inventors:
Cheol Hyoung Park, Hye Kyung Min, In Suk Park, Mi Jung Lim, Ji Won Lee, Jin Yong Chung, Yeo Jin Yoon, Joo Young Park
Abstract: Methods of treating patients with dyskinesias, by administering a therapeutically effective amount of a dual-action mu-opioid receptor antagonist/kappa-opioid receptor agonist or prodrug thereof to a subject in need thereof, sufficient to mitigate the dyskinesia. Alternatively, a combination of both a mu-opioid receptor antagonist or prodrug thereof, and a kappa-opioid receptor agonist or prodrug thereof can be administered, either together or separately.
Type:
Grant
Filed:
April 26, 2012
Date of Patent:
March 22, 2016
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Inventors:
Mary Maral Mouradian, Steven Braithwaite, Michael Voronkov
Abstract: The invention provides crystalline forms of (R)-3-[N-(3?-chlorobiphenyl-4-ylmethyl)-N?-(3-hydroxyisoxazole-5-carbonyl)hydrazino]-2-hydroxypropionic acid isopropyl ester. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
Type:
Grant
Filed:
March 27, 2013
Date of Patent:
March 1, 2016
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Venkat R. Thalladi, Jerry Nzerem, Miroslav Rapta
Abstract: Disclosed are new colchicine solid-state forms, methods of preparing the solid-state forms, as well as formulations prepared therefrom and uses thereof.
Type:
Grant
Filed:
October 8, 2012
Date of Patent:
February 9, 2016
Assignee:
Takeda Pharmaceuticals U.S.A., Inc.
Inventors:
Tong Sun, Kurt Nielsen, Shawn Watson, Rolf Hilfiker, Andreas Sieber
Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.
Type:
Grant
Filed:
February 12, 2014
Date of Patent:
December 15, 2015
Assignees:
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Inventors:
Catherine Guillou, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
Abstract: An extended regimen for treatment of HER-2/neu overexpressed/amplified cancer is described, with involves delivering a course of neratinib therapy to HER-2/neu overexpressed/amplified cancer patients following the completion of surgical and adjuvant therapy. The neratinib regimen may be continued for upwards of twelve months to five years. Also provided are pharmaceutical kits designed to facilitate compliance with the regimen.
Type:
Grant
Filed:
March 24, 2010
Date of Patent:
December 15, 2015
Assignee:
WYETH LLC
Inventors:
Anna Berkenblit, Florence Marie Helene Binlich, Paul Goss
Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
Type:
Grant
Filed:
October 31, 2013
Date of Patent:
December 8, 2015
Assignee:
GENENTECH, INC.
Inventors:
Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel S. Kintz, Hans Edward Purkey