Abstract: The present invention relates to compounds of general formula I wherein R1, R2, R3 and X are as defined herein, or to a pharmaceutically acceptable acid addition salt or optical isomers thereof, which are useful to treat CNS disorders.
Type:
Grant
Filed:
September 28, 2015
Date of Patent:
March 7, 2017
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Ravi Jagasia, Roland Jakob-Roetne, Juergen Wichmann
Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine 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:
January 29, 2015
Date of Patent:
March 7, 2017
Assignee:
Warsaw Orthopedic, Inc.
Inventors:
John Myers Zanella, Christopher M. Hobot, Danielle L. Biggs, Katara Shaw, Phillip Edward McDonald, Vanja Margareta King, William F. McKay, Kathy L. Remsen
Abstract: The present invention relates to co-crystals of cyprodinil or pyrimethanil and a co-crystal forming compound which has at least one imide and/or oxime functional group.
Type:
Grant
Filed:
April 6, 2011
Date of Patent:
February 28, 2017
Assignee:
Syngenta Limited
Inventors:
Neil George, James Owen Forrest, Rebecca Claire Burton, Christer Björn Aakeroy
Abstract: The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumor activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.
Type:
Grant
Filed:
October 27, 2014
Date of Patent:
February 21, 2017
Assignee:
Cyclacel Limited
Inventors:
Benjamin Mark Skead, Christopher Peter Worrall, Jonathan Charles Christian Atherton, Julian Scott Northen, Philippe Fernandes
Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
Type:
Grant
Filed:
May 18, 2015
Date of Patent:
January 31, 2017
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Craig Grant, James P. Kanter, Graeme Langlands
Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
Type:
Grant
Filed:
March 9, 2016
Date of Patent:
January 17, 2017
Assignee:
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
Inventors:
Samuel J. Danishefsky, Joan Massague, Manuel Valiente Cortes, Thordur Oskarsson, Malcolm Moore, Nicolas Lecomte, Ouathek Ouerfelli, Guangli Yang
Abstract: A method of forming a compound in a subject can include: providing a composition having a prodrug compound represented by a structure of Formula 1 or stereoisomer thereof or pharmaceutically acceptable salt thereof; and administering the composition to a subject such that the prodrug compound has a phosphoryloxyalkyl prodrug moiety removed therefrom to form the compound in the subject and to form the separate phosphoryloxyalkyl compound. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, various cancers (e.g., bladder, breast, etc.), dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.
Abstract: A method and composition for treatment of bacterial infections caused by gram negative or gram positive bacteria such as Staphylococcus aureus, Rhodococcus equi, Mycobacterium tuberculosis, Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a formulation containing gallium (III), in a pharmaceutically acceptable salt or complex thereof.
Type:
Grant
Filed:
May 3, 2010
Date of Patent:
January 10, 2017
Assignee:
Aridis Pharmaceuticals Inc.
Inventors:
Satoshi Ohtake, Vu Truong-Le, David Lechuga-Ballesteros, Luisa Yee, Binh Pham, Russell Martin, Atul Saxena
Abstract: This invention provides topical localized formulations comprising an isoxazoline compound and a pharmaceutically or veterinary acceptable liquid carrier vehicle comprising N,N-diethyl-3-methylbenzamide as a solvent and an improved method for controlling, and preventing parasite infestation in animals.
Type:
Grant
Filed:
September 28, 2015
Date of Patent:
January 3, 2017
Assignee:
Intervet Inc.
Inventors:
Stefan Fuchs, Anja Regina Heckeroth, Ramona Müller, Heike Williams, Hartmut Zoller
Abstract: The present invention relates generally to the field of lipids and in particular aims at improving lipid absorption, for example under conditions of lipid maldigestion or malabsorption. One embodiment of the present invention relates to a composition comprising a sn-2 monoacylglycerol derivative, wherein the sn-1 and sn-3 positions are blocked by protective groups. The acyl group may be a fatty acid, for example one with anti-inflammatory properties.
Type:
Grant
Filed:
April 14, 2015
Date of Patent:
December 20, 2016
Assignee:
Nestec S.A.
Inventors:
Bruce Bistrian, Frederic Destaillats, Cristina Cruz-Hernandez, Fabiola Dionisi, Isabelle Masserey-Elmelegy, Manuel Oliveira, Julie Celine Moulin
Abstract: The present invention relates to new crystalline forms of the inhibitor, 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazoline-4-one; the present invention also relates to methods for preparing the new crystalline forms of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, pharmaceutical compositions containing the new crystalline forms thereof, and uses thereof for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma.
Abstract: This invention pertains to an anti-microbial, in particular anti-bacterial and/or anti-fungal composition comprising cinnamaldehyde, trans-2-methoxy cinnamaldehyde, cinnamyl acetate and linalool. In particular this composition is intended for preventing and/or treating microbial infection in an animal.
Abstract: A ceramide production enhancer and a moisturizer containing, as an active ingredient, an extract of at least one plant selected from the group consisting of Chenopodium hybridum, Melia toosendan, Indigofera tinctoria, Cirsium japonicum, Catalpa ovate, and Tagetes erecta, or a compound represented by the following Formula (1): wherein, R represents an acyl group having 1 to 5 carbon atom(s).
Abstract: The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
Type:
Grant
Filed:
April 11, 2011
Date of Patent:
September 20, 2016
Assignee:
THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK
Abstract: Described herein are methods of treating a mammal in need of treatment for non-histaminic pruritus by administering to the mammal in need thereof a therapeutically effective amount of RS-norketotifen or a pharmaceutically acceptable salt thereof, thereby reducing the desire to scratch in the mammal. Non-histaminergic types of pruritus are resistant to treatment with selective histamine H-1-, H-2- and H-4-receptor inhibitors. In certain aspects, the non-histaminergic pruritus is associated with diabetes.
Abstract: The present invention relates to novel derivatives of oxazaphosphorines that are pre-activated, to the methods for preparing same, to the pharmaceutical compositions containing same and to the therapeutic use thereof, in particular for treating cancer.
Type:
Grant
Filed:
July 2, 2015
Date of Patent:
August 30, 2016
Assignee:
INSTITUT GUSTAVE ROUSSY
Inventors:
Angelo Paci, Thierry Martens, Michael Rivard, Patrick Couvreur, Didier Desmaele, Joachim Caron
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of malaria.
Type:
Grant
Filed:
June 20, 2014
Date of Patent:
August 30, 2016
Assignees:
The Broad Institute, Inc., President and Fellows of Harvard College
Inventors:
Eamon Comer, Benito Munoz, Jennifer A. Beaudoin, Sebastian T. Le Quement, Christina Scherer, Jeremy Duvall, Nobutaka Kato, Micah Maetani, Bertrand Braibant
Abstract: The present invention provides: a pitavastatin-containing preparation containing pitavastatin or a pharmacologically acceptable salt thereof and at least one kind of a basic additive selected from the group consisting of basic magnesium compounds and basic calcium compounds, and an aqueous solution or an aqueous dispersion of the pitavastatin-containing preparation having a pH of more than 8 and 10 or less; and a method for producing a pitavastatin-containing preparation, including blending at least one kind of a basic additive selected from the group consisting of basic magnesium compounds and basic calcium compounds with pitavastatin or a pharmacologically acceptable salt thereof, to make an aqueous solution or an aqueous dispersion of the pitavastatin-containing preparation have a pH of more than 8 and 10 or less.
Abstract: The present invention relates to the use of triazinones such as triazinediones and triazinetriones for triazinetriones for the preparation of compositions for treating animals, in particular treating animals prophylactically, against parasitic protozoans, and to these compositions.
Abstract: The present invention is a composition and method of treatment for skin disorders, conditions, and severe skin dryness in general through topical systematic and periodic application of a formulation that generally may include salicylic acid, glycolic acid, urea, dimethyl isosorbide, ethoxydiglycol, barrier repair agents, anti-irritants, humectants, and also has an acidic pH formulation.