Abstract: Disclosed herein are compounds, compositions, and methods for preventing and treating proliferative diseases associated with aberrant receptor tyrosine kinase (RTK) activity. The therapeutic indications described herein more specifically relate to the non-selective inhibition of RTKs associated with vascular and pulmonary disorders.
Abstract: The combination of 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline or a pharmaceutically acceptable salt thereof with a second therapeutic agent, wherein the second therapeutic agent is selected from: (a) a therapeutic agent known to modify cholinergic transmission such as M1 muscarinic receptor agonists or allosteric modulators, M2 muscarinic antagonists, acetylcholinesterase inhibitors, nicotinic receptor agonists or allosteric modulators, 5-HT4 receptor partial agonists or 5HT1A receptor antagonists and NMDA receptor antagonists or modulators, glutamate antagonists, GABA-ergic antagonists, H3 antagonists, putative metabolic/mitochondrial modulators, or disease modifying agents such as ? or ?-secretase inhibitors, Tau-targeted therapeutics, ?-amyloid aggregation inhibitors and ?-amyloid immunotherapies; (b) an antidepressant such as a tricyclic, a MAOI (Monoamine oxidase inhibitor) a SSRI (Selective Serotonin Reuptake Inhibitor), a SNRI (Serotonin and Noradrenaline Reuptake Inhibitor) or a NaSSA (noradrener
Type:
Grant
Filed:
July 17, 2015
Date of Patent:
November 7, 2017
Assignee:
Axovant Sciences GmbH
Inventors:
Tsu Tshen Chuang, Ann Jacqueline Hunter, David John Virley
Abstract: Provided is a novel medicament capable of reducing the side effects of metformin or a pharmaceutically acceptable salt thereof and useful as an anti-malignant tumor agent, in which metformin or a pharmaceutically acceptable salt thereof and dihydroquercetin or a pharmaceutically acceptable salt thereof are combined.
Type:
Grant
Filed:
May 23, 2014
Date of Patent:
November 7, 2017
Assignee:
RESEARCH INSTITUTE FOR NUTRITION AND AGING CO., LTD.
Abstract: The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formula (I)-(XXVI) and (III?) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.
Type:
Grant
Filed:
December 23, 2016
Date of Patent:
October 31, 2017
Assignee:
TRUSTEES OF BOSTON UNIVERISTY
Inventors:
Ulla Hansen, Scott Schaus, Trevor Grant, Joshua Bishop, John Kavouris, Lisa M. Christadore
Abstract: Methods and materials for reducing organ transplant rejection or minimizing ischemia or ischemia/reperfusion injury in a subject are described. The methods include administering a fat emulsion before or after the organ transplant or before, at the onset of, or after the ischemic event.
Type:
Grant
Filed:
September 6, 2013
Date of Patent:
October 24, 2017
Assignee:
Carnegie Mellon University
Inventors:
Chien Ho, Li Liu, Yijen Wu, T. Kevin Hitchens, Qing Ye
Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
Type:
Grant
Filed:
March 18, 2015
Date of Patent:
October 3, 2017
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Jeffery L. Kutok, David G. Winkler, Vito J. Palombella, Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Martin R. Tremblay
Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Abstract: The invention relates inter alia to compounds of the general formula (I) in which the A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
Type:
Grant
Filed:
November 5, 2014
Date of Patent:
September 12, 2017
Assignee:
BAYER CROPSCIENCE AKTIENGESELLSCHAFT
Inventors:
Werner Hallenbach, Hans-Georg Schwarz, Kerstin Ilg, Ulrich Goergens, Johannes Koebberling, Andreas Turgerg, Niels Boehnke, Michael Maue, Robert Velten, Tobias Harschneck, Julia Johanna Hahn, Sebastian Horstmann
Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.
Type:
Grant
Filed:
June 3, 2015
Date of Patent:
September 12, 2017
Assignee:
University of Maryland, Baltimore
Inventors:
Alan E. Tomkinson, Helen Xi Chen, Barbara Dziegielewska, Alexander D. Mackerell, Shijun Zhong, Gerald M. Wilson
Abstract: The present invention relates to pharmaceutical compositions intended to be used in the form of a solid unit such as a tablet, for oral administration, comprising a high content of fexofenadine and/or of at least one pharmaceutically acceptable salt thereof, and also to hot-melt processes for manufacturing solid units.
Type:
Grant
Filed:
December 20, 2013
Date of Patent:
September 12, 2017
Assignee:
SANOFI
Inventors:
Baptiste Merillon, Jean-Yves Lanne, Marie Renouard
Abstract: This invention relates to the treatment of breast cancer in a subject, for example a female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed SERM (tamoxifen, toremifene), aromatase inhibitor, trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), lapatinib, exemestane (Aromasin), bevacizumab (Avastin), and/or fulvestrant treatments; metastasis in a subject suffering from breast cancer; comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound.
Type:
Grant
Filed:
July 13, 2015
Date of Patent:
August 29, 2017
Assignee:
GTX, INC.
Inventors:
James T. Dalton, Mitchell S. Steiner, Ramesh Narayanan, Sunjoo Ahn
Abstract: The present invention relates to compounds as inhibitor of WNT signal transduction pathway, as well as a composition comprising the same. Further, the present invention relates to the use of the compounds in the treatment of fibrosis. Fibrosis is the formation of excess fibrous connective tissue in an organ or tissue in a reparative or reactive process. Fibrosis is the end result of chronic inflammatory reactions induced by a variety of stimuli including persistent infections, autoimmune reactions, allergic responses, chemical insults, radiation, and tissue injury.
Abstract: The present invention relates to compositions and methods for preventing and treating cell proliferation in cancer. More specifically, the present invention relates to compositions and methods for inhibiting tumor growth, and for treating proliferative diseases, particularly colon and breast cancer, with a combined pharmacological approach. Yet more specifically, the compositions for inhibiting tumor growth comprise a combination of: i) a first component which is an ACSL4 inhibitor; and ii) a second component selected from the group consisting of mTOR inhibitor and ER inhibitor.
Type:
Grant
Filed:
March 2, 2016
Date of Patent:
August 22, 2017
Assignee:
Consejo Nacional De Investigaciones Cientificas Y Tecnicas (CONICET)
Inventors:
Ernesto Jorge Podesta, Paula Mariana Maloberti, Ulises Daniel Orlando, Melina Andrea Dattilo, Ana Fernanda Castillo, Angela Rosaria Solano
Abstract: Provided are 5-substituted quinazolinone compounds, for example, of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use for treating angiogenesis or cytokine related disorders, and pharmaceutical compositions of these compounds are disclosed.
Abstract: Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Type:
Grant
Filed:
March 19, 2014
Date of Patent:
August 8, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Matthew Lloyd Childers, Christopher Dinsmore, Peter Fuller, David Guerin, Jason David Katz, Qinglin Pu, Mark E. Scott, Christopher F. Thompson, Hongjun Zhang, Danielle Falcone, Luis Torres, Jason Brubaker, Hongbo Zeng, Jiaqiang Cai, Xiaoxing Du, Chonggang Wang, Yunfeng Bai, Norman Kong, Yumei Liu, Zhixiang Zheng
Abstract: This invention is in the area of tricyclic lactam compounds for and methods of treating selected Rb-positive cancers and other Rb-positive abnormal cellular proliferative disorders while minimizing the deleterious effects on healthy cells, for example healthy Hematopoietic Stem Cells and Progenitor Cells (HSPCs), associated with current treatment modalities. In one aspect, treatment of select Rb-positive cancers is disclosed using specific compounds disclosed herein. In certain embodiments, the compounds described herein act as selective cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects.
Type:
Grant
Filed:
April 17, 2015
Date of Patent:
August 1, 2017
Assignee:
G1 Therapeutics, Inc.
Inventors:
Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Ricky D. Gaston, Robert C. Gadwood
Abstract: Described herein are combination therapies for cancer (such as lymphoid malignancies) and immune diseases (such as autoimmune diseases and inflammatory diseases). The therapies comprise the combined use of inhibitors of BTK, mTOR kinase, and Bcl-2 or their signaling pathways, and immunomodulatory drugs. Also described are pharmaceutical compositions and kits comprising these inhibitors.
Abstract: The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)-mepazine and one of its intermediates.
Type:
Grant
Filed:
June 25, 2014
Date of Patent:
August 1, 2017
Assignees:
Helmholtz Zentrum München—Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH), Ludwig-Maximilians—Universität München
Inventors:
Daniel Krappmann, Daniel Nagel, Florian Schlauderer, Katja Lammens, Karl-Peter Hopfner, Robert A. Chrusciel, Dale L. Kling
Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.
Abstract: The present invention relates to compounds as inhibitor of WNT signal transduction pathway, as well as a composition comprising the same. Further, the present invention relates to the use of the compounds in the treatment of cancer.