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 present invention relates to triazine derivatives of formula (I) for their use in the treatment of type 1 diabetes mellitus, and to compositions comprising said triazine derivatives.
Type:
Grant
Filed:
June 9, 2011
Date of Patent:
March 1, 2016
Assignee:
POXEL
Inventors:
Pascale Fouqueray, Daniel Cravo, Sophie Hallakou-Bozec, Sébastien Bolze
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
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: A 5?-androstane-3?,5,6?-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-?-cyclodextrin as a solubilizing agent and the active ingredient is present at a weight ratio of 1-20:40-500 to the hydroxypropyl-?-cyclodextrin. The injection may also comprise, by weight, 1-100 parts of at least one isotonic adjusting agent, 0-200 parts of at least one freeze drying filler, and 0-2000 parts of at least one solvent. The preparation method comprises dissolving hydroxypropyl-?-cyclodextrin solution, 5?-androstane-3?,5,6?-triol and at least one additional soluble excipient in water for injection in sequence to obtain a raw injection solution, and subjecting the raw injection solution to decolorization, depyrogenation, filtration and sterilization to obtain the injection. Drying the filtrate yields a solid for injection.
Abstract: An anti-aging composition containing: (a) at least one first active ingredient chosen from phloretin and its derivatives; (b) at least one second active ingredient chosen from cinnamic acid, resveratrol, retinol, ascorbic acid, tocopherol, and their derivatives; and (c) at least one non-aqueous organic solvent, with the proviso that if the composition contains ascorbic acid, water is present as a co-solvent.
Type:
Grant
Filed:
April 15, 2009
Date of Patent:
February 2, 2016
Assignee:
L'OREAL
Inventors:
Sheldon R. Pinnell, Jan Zielinski, Isabelle Hansenne
Abstract: The present invention relates to obeticholic acid: or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.
Type:
Grant
Filed:
June 17, 2013
Date of Patent:
January 19, 2016
Assignee:
Intercept Pharmaceuticals, Inc.
Inventors:
André Steiner, Heidi Waenerlund Poulsen, Emilie Jolibois, Melissa Rewolinski, Ralf Gross, Emma Sharp, Fiona Dubas-Fisher, Alex Eberlin
Abstract: A method of treating a condition chosen from the group consisting of interstitial cystitis, cystitis, chronic nonbacterial prostatitis, chronic cystitis, prostatic hyperplasia, prostatitis, prostatism, bladder neck contracture, bladder inflammation, and overactive bladder by administering an amount of rebamipide or a pharmaceutically acceptable salt thereof to a human.
Abstract: Injectable bone graft material having a biocompatible, resorbable polymer and a biocompatible, resorbable inorganic material exhibiting macro, meso, and microporosities.
Type:
Grant
Filed:
June 23, 2004
Date of Patent:
December 29, 2015
Assignee:
Orthovita, Inc.
Inventors:
Charanpreet S. Bagga, Theodore D. Clineff, Erik M. Erbe, Michael W. Paris, Gina M. Nagvajara, Antony Koblish
Abstract: The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.
Type:
Grant
Filed:
March 18, 2014
Date of Patent:
December 29, 2015
Assignee:
University of Pittsburgh—of the Commonwealth System of Higher Education
Inventors:
Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
Abstract: Composition and method for preventing and/or treating dementia and ameliorating memory impairment and/or improving memory, comprising one or more arylnaphthalene lignan derivatives, namely Justicidin A, 5-methoxyjusticidin A, Chinensinaphthol, and a pharmaceutically-acceptable salt thereof, as active ingredient.
Type:
Grant
Filed:
September 25, 2013
Date of Patent:
December 15, 2015
Assignees:
KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY, CSIR
Inventors:
Hyun Ok Yang, Sung-Kwon Chung, Hak Cheol Kwon, Jin Wook Cha, Young-Joo Kim, Gerda Fouche, Rudzani Nthambeleni, Dashnie Naidoo, Jeremiah Senabe, Vinesh Jaichand Maharaj, Eric Khorombi, Jungyeob Ham, Joon Ki Kim
Abstract: Anhydrous topical gel composition of mupirocin or its salts comprising: a) a lipophilic base selected from the group consisting of petrolatum, medium-chain triglycerides, isopropyl myristate and mixtures thereof; b) a bioadhesive selected from the group comprising polyvinylpyrrolidone and polymethacrylates; and c) a solvent selected from the group comprising ethanol, propanol, and isopropanol; which is stable and shows an increased residence time of the active ingredient in the skin, resulting in an improved clinical effect in the treatment of bacterial skin infections while maintaining the safety profile of the commercial pharmaceutical product.
Type:
Grant
Filed:
October 19, 2011
Date of Patent:
December 8, 2015
Assignee:
LABORATORIOS OJER PHARMA, S.L.
Inventors:
Carlos González Ojer, Beatriz Goñi Allo, Fiona Pastor Fernández, Cayetana Yárnoz De Miguel
Abstract: Polymorphic forms of onapristone and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns and other properties.
Abstract: The present invention is directed to a series of glycerin polysilicones. By glycerin polysilicones in meant polymers that have silicone portions that are functionalized with glycerin groups. The polymers of the present invention can range from relatively low molecular weight (around 600 daltons) to higher molecular weight (of about 2,500 daltons). The presence of the glyceryl groups together with the silicone groups allows for the preparation of molecules uniquely suited to personal care applications, more specifically, skin care products.
Abstract: The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient.
Type:
Grant
Filed:
April 10, 2012
Date of Patent:
November 17, 2015
Assignees:
Helmholtz Zentrum Fuer Infektionsforschung GmbH, Medizinische Hochschule Hannover
Abstract: The present invention provides novel aspirin derivatives useful for preventing and/or treating cancer. The novel compounds of this invention may be particularly useful for the prevention and/or treatment of cancers affecting the gastrointestinal system, such as colorectal cancer.
Type:
Grant
Filed:
June 14, 2013
Date of Patent:
November 17, 2015
Assignee:
North Carolina Agricultural and Technical State University
Abstract: This invention provides new therapeutic potential of nandrolone or a derivative thereof, against protozoal diseases. More specifically, nandrolone or a derivative thereof exhibits anti-protozoal activity against Leishmania major. Anti-protozoal potential of nandrolone derivatives, such as compounds 1-8, can contribute in the development of effective therapies against protozoal diseases, such as leishmaniasis, trypanosomiasis, malaria, toxoplasmosis, babeosis, amoebic dysentery and lambliasis. Another aspect of the invention is a method of testing derivatives of nandrolone for anti-protozoal activity comprising growing Leishmania in the presence of the test derivative and determining the IC50 value.
Type:
Grant
Filed:
May 28, 2014
Date of Patent:
November 3, 2015
Inventors:
Elias Baydoun, Muhammad Iqbal Choudhary, Atia-tul- Wahab, Colin Smith, Martin Karam, Dina Farran, Mahwish Shafi Ahmed Khan, Malik Shoaib Ahmad
Abstract: The present invention relates to adamantyl derivatives and their anti-cancer activity. Compounds of formulae I and II are provided as well as related methods of treatment and methods of synthesis.
Type:
Grant
Filed:
April 16, 2014
Date of Patent:
October 27, 2015
Assignee:
Women & Infants' Hospital of Rhode Island