Abstract: The present invention relates to the administration of compositions comprising an antiestrogen, preferably a selective estrogen receptor modulator (SERM) such as trans-clomiphene, for treating cancer and associated diseases. The invention is also directed to methods for reducing IGF-1 levels in a subject in need thereof by administering a composition comprising an antiestrogen, preferably a SERM such as trans-clomiphene.
Type:
Grant
Filed:
October 22, 2013
Date of Patent:
June 27, 2017
Assignee:
Repros Therapeutics Inc.
Inventors:
Joseph S. Podolski, Ronald D. Wiehle, Kuang Hsu, Greg Fontenot
Abstract: Insecticidal, acaricidal, nematicidal or molluscicidal compounds of formula (I) wherein Y is a single bond, C?O, C?S or S(O)q where q is 0, 1 or 2; and R1, R2, R3, R4, R8, R9 are R10 are as defined in the claims or salts or N-oxides thereof, processes for preparing them and compositions containing them.
Type:
Grant
Filed:
September 21, 2015
Date of Patent:
June 27, 2017
Assignee:
Syngenta Participations AG
Inventors:
David John Hughes, Paul Anthony Worthington, Charles Adam Russell, Eric Daniel Clarke, James Edward Peace, Mark Richard Ashton, Thomas Stephen Coulter, Richard Spurring Roberts, Louis-Pierre Molleyres, Fredrik Cederbaum, Jerome Cassayre, Peter Maienfisch
Abstract: The present invention describes methods of treating dementia comprising administering an effective daily dose of N-[2-(6-fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine to improve or augment the effect of an acetylcholinesterase inhibitor.
Abstract: The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
Type:
Grant
Filed:
November 2, 2015
Date of Patent:
June 27, 2017
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Chantal Fürstner, Jörg Keldenich, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Ingo Pluschkell, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
Abstract: The present application discloses strategies to recruit and mobilize stem cells using S1P receptor selective agonists and antagonists as wells as regulators of chemokine receptors. In an in vivo ischemic model, S1P1/S1P3 activation with FTY720 impeded inflammatory cell infiltration and recruited endothelial progenitor cells (EPCs) with the potential to increase microvascular remodeling. S1P3 expression on marrow-derived cells was essential for this remodeling. Concurrent systemic S1P3 and CXCR4 antagonism mobilized hematopoietic stem cells (HSCs) with the ability to engraft and repopulate blood cells. Pre-treatment of donor HSCs with FTY720 increased homing toward SDF-1 and improved engraftment in marrow. FTY720-coated bone allografts coupled with systemic administration of VPC01091 enhanced bone allograft integration and new bone formation in bone defects. MSCs pre-treated with FTY720 exhibited increased migration toward SDF-1, a CXCR4+ ligand.
Type:
Grant
Filed:
March 16, 2012
Date of Patent:
June 20, 2017
Assignee:
University of Virginia Patent Foundation
Inventors:
Edward A. Botchwey, III, Mary J. Laughlin, Kevin R. Lynch, Anusuya Das, Anthony Awojoodu
Abstract: Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.
Type:
Grant
Filed:
March 13, 2015
Date of Patent:
June 20, 2017
Assignee:
GRUNENTHAL GMBH
Inventors:
Mazen Hanna, Ning Shan, Miranda Cheney, David R. Weyna
Abstract: The invention provides combinations comprising a) compound of formula I: (formula I), or a pharmaceutically acceptable salt thereof; and another agent selected from GDC-0973, PD-0325901, or a pharmaceutically acceptable salt thereof. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.
Type:
Grant
Filed:
March 30, 2012
Date of Patent:
June 20, 2017
Assignee:
GENENTECH, INC.
Inventors:
Brian Lee, Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath
Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
Type:
Grant
Filed:
November 17, 2010
Date of Patent:
June 13, 2017
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Volker Schulze, Marcus Koppitz, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Ulf Bömer
Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
Type:
Grant
Filed:
September 2, 2011
Date of Patent:
June 13, 2017
Assignee:
FORMA TM, LLC
Inventors:
Kenneth W. Bair, Alexandre J. Buckmelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
October 15, 2015
Date of Patent:
June 6, 2017
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Daniel D. Long, Robert Murray McKinnell, Lan Jiang, Mandy Loo, Kassandra Lepack, Lori Jean Van Orden, Gavin Ogawa
Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.
Type:
Grant
Filed:
April 28, 2011
Date of Patent:
May 30, 2017
Assignee:
Gachon University of Industry-Academic Cooperation Foundation
Abstract: Described are gel compositions containing active pharmaceutical ingredient such as testosterone, solvent, and thickener, the gel compositions being useful for transdermal administration of the active ingredient to a patient, and related methods. Certain embodiments of the gel composition specifically exclude Hsieh enhancer.
Abstract: Compositions for treating a condition associated with activity of a muscarinic receptor (e.g., one or more of M1, M2, M3, M4, M5) and for anesthetizing a subject include a bitopic muscarinic antagonist or agonist. A bitopic muscarinic antagonist named JB-D4 was discovered. Additional bitopic muscarinic antagonists discovered and described herein include BK-23, HD-42, HD153, HD-185, KH-5, JM-31 and JM-32. These bitopic ligands and their structural analogs, as well as bitopic muscarinic agonists, may be used as neuromuscular blocking agents (e.g., for use in compositions for anesthetizing a subject) and for the treatment of central nervous system disorders (e.g., Parkinson's disease, Schizophrenia, etc.), Overactive Bladder Syndrome, Chronic Obstructive Pulmonary Disease, asthma, and many other diseases associated with the activation or inhibition of M1-M5 acetylcholine receptors.
Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
Type:
Grant
Filed:
October 28, 2016
Date of Patent:
May 23, 2017
Assignee:
Agios Pharmaceuticals, Inc.
Inventors:
Giovanni Cianchetta, Byron DeLaBarre, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan, Tao Guo, Li Zhang
Abstract: The disclosure herein generally relates to methods of treating an overweight or obese condition, and overweight or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MetAp-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.
Abstract: The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-?B for the treatment or prevention of muscular wasting disease, including muscular dystrophy.
Type:
Grant
Filed:
August 5, 2016
Date of Patent:
May 16, 2017
Assignee:
ReveraGen Biopharma, Inc.
Inventors:
John M. McCall, Eric Hoffman, Kanneboyina Nagaraju
Abstract: Described herein are transdermal parasiticidal formulations and methods of treatment and use, wherein the formulation is not only able to deliver an agent or agents through the skin layer, but is able to do so through wool, dirt and/or a sebum layer on the skin if such layers are present. The transdermal parasiticidal formulation may be a solution including a therapeutically effective amount of levamisole anthelmintic agent dissolved in a solution including isopropyl myristate and D-limonene. This base formulation is highly compatible with other compounds and various other actives may be added to this formulation.
Abstract: The Invention relates to the use of antibiotic, tylvalosin, as an anti-viral agent. Tylvalosin is particularly useful for the treatment of PRRSV.
Type:
Grant
Filed:
June 8, 2015
Date of Patent:
May 16, 2017
Assignees:
ECO ANIMAL HEALTH LIMITED, CAMBRIDGE UNIVERSITY TECHNICAL SERVICES
Inventors:
Albert Philip Adrian Mockett, Thomas David Kay Brown, Amanda Denise Stuart
Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
Type:
Grant
Filed:
March 14, 2016
Date of Patent:
May 9, 2017
Assignee:
Almirall, S.A.
Inventors:
Maria Prat Quinones, Silvia Fonquerna Pou, Carlos Puig Duran, Wenceslao Lumeras Amador, Jose Aiguade Bosch, Juan Francisco Caturla Javaloyes