Abstract: The present invention relates to process for identifying a compound which induces the mitochondrial permeability transition (MPT) in proliferating cells, wherein said process comprises contacting a cell or cell extract with a compound, determining whether the compound binds to adenine nucleotide translocator (ANT), and determining whether the compound selectively induces the MPT in proliferating cells.
Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.
Type:
Grant
Filed:
December 20, 2013
Date of Patent:
May 17, 2016
Assignee:
Pain Therapeutics Inc.
Inventors:
Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
Abstract: The invention relates to a self-emulsifiable liquid composition intended to be diluted in an aqueous intermediate solution and then incorporated into the drinking water of livestock animals, and also to the use of such a composition. The invention is characterized in that the composition comprises at least—between 1% and 12% by weight of the florfenicol active ingredient, relative to the total volume of the composition; —at least 50% by weight, relative to the total volume of the composition (p/v), of a mixture of C8-C10 saturated polyglycosylated glycerides having an HLB (hydrophilic-lipophilic balance) of less than 16; and—at least 5% by weight, relative to the total volume of the composition (p/v), of a surfactant.
Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.
Type:
Grant
Filed:
July 24, 2014
Date of Patent:
May 10, 2016
Assignees:
Ramot at Tel-Aviv University Ltd., Bar-Ilan University
Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. 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 aberrant estrogen receptor activity.
Type:
Grant
Filed:
February 12, 2014
Date of Patent:
April 26, 2016
Assignee:
NOVARTIS AG
Inventors:
Heather Elizabeth Burks, Michael A. Dechantsreiter, Guo He, Jill Nunez, Stefan Peukert, Clayton Springer, Yingchuan Sun, Noel Marie-France Thomsen, George Scott Tria, Bing Yu
Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
Type:
Grant
Filed:
October 13, 2005
Date of Patent:
April 19, 2016
Assignee:
PTC Therapeutics, Inc.
Inventors:
Neil Almstead, Gary M. Karp, Richard Wilde, Ellen Welch, Hongyu Ren
Abstract: A pharmaceutical composition for prophylaxis or treatment of systemic diseases in cats, wherein the composition comprising administration of a therapeutically effective amount of angiotensin II receptor 1 (AT-1) antagonist (sartan) to a cat in need of such a treatment.
Abstract: The present invention relates to a phosphopeptide-stabilized amorphous calcium phosphate and/or amorphous calcium fluoride phosphate complex, wherein the complex is formed at a pH of below 7.0. Methods of making such complexes are also provided. The complexes are useful in dental applications, in particular in dental remineralisation.
Abstract: The invention relates to the use of compounds of general formula (I): CH3(—CH?CH)3—R??(I) wherein R is selected from CO—O—R? or CO—O(?), R? being selected from H, alkyl or alkenyl from C1 to C22, or sugars, and their pharmaceutically acceptable salts, preferably such as sodium, potassium, or lysine salts, each compound of general formula (I) being used as such or mixed with one or more of the others, as active ingredients in a pharmaceutical or cosmetic composition provided with antioxidant activity against free radicals.
Abstract: The invention concerns a pharmaceutical composition characterized in that it contains a combination of a parasympatholytic agent, a sympathomimetic agent and a local anaesthetic. Such a composition may be injected into the anterior chamber of the eye before a cataract operation or instilled on the eye before laser treatment.
Abstract: The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.
Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.
Type:
Grant
Filed:
April 14, 2014
Date of Patent:
March 15, 2016
Assignee:
AERPIO THERAPEUTICS, INC.
Inventors:
Jeffrey Lyle Gray, Kande K. D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.
Type:
Grant
Filed:
March 23, 2014
Date of Patent:
March 15, 2016
Assignee:
University of Tennessee Research Foundation
Inventors:
Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
May 11, 2012
Date of Patent:
March 15, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
Abstract: The present invention relates to compositions, pharmaceutical compositions, and methods for preparing the same, comprising a tetracycline with improved stability and solubility. Some embodiments include a tetracycline with an excess of a divalent or trivalent cation.
Type:
Grant
Filed:
October 17, 2012
Date of Patent:
March 8, 2016
Assignee:
Rempex Pharmaceuticals, Inc.
Inventors:
David C. Griffith, Serge Boyer, Michael N. Dudley, Scott Hecker
Abstract: The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment.
Type:
Grant
Filed:
April 19, 2012
Date of Patent:
March 8, 2016
Assignees:
Exonhit Therapeutics SA, Allergan, Inc.
Inventors:
Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Fabien (Jacques) Schweighoffer
Abstract: The peptidoglycan layer is a vital component of the bacterial cell wall, which comprises 4?3 and 3?3 transpeptide cross-linkages, the formation of which are catalyzed by D,D- and L,D-transpeptidases, respectively. Methods for the treatment of bacterial infections with agents that inhibit L,D-transpeptidases, either alone or in combination with D,D-transpeptidase inhibitors, are provided herein. Also provided are methods for the treatment of chronic stage tuberculosis with agents that inhibit enzyme with L,D-transpeptidase activity.
Type:
Grant
Filed:
March 21, 2014
Date of Patent:
March 1, 2016
Assignees:
The Johns Hopkins University, Institut National de la Sante et de la Recherche Medicale
Inventors:
Gyanu Lamichhane, William R. Bishai, Radhika Gupta, Marie Lavollay, Jean-Luc Mainardi, Michel Arthur
Abstract: Compositions and methods for the dissolution of a microbial biofilm are provided, where the method comprises contacting a microbiofilm with an effective dose of a curcumin derivative as a biofilm inhibitor. In some embodiments the curcumin derivative is dimethoxycurcumin. In some embodiments the biofilm comprises E. coli, e.g. including uropathogenic E. coli. The biofilm can be present in vitro or in vivo. The biofilm inhibitor may be administered alone, or in combination with bacteriocidal agents.
Type:
Grant
Filed:
June 19, 2013
Date of Patent:
March 1, 2016
Assignee:
The Board of Trustees of the Leland Stanford Junior University