Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein ring A, B1, B2, B3, L, R1, R4, R5 and m of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
Type:
Grant
Filed:
November 19, 2010
Date of Patent:
March 29, 2016
Assignee:
Amgen Inc.
Inventors:
Yuan Cheng, Timothy Powers, Kate Ashton, James Brown, Scott Harried, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Thomas Nixey, Nick A. Paras, Steve F. Poon, David J. St. Jean, Jr., Qiufen Xue, Wenge Zhong
Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an electrophile containing biocide, and its use for the control of microorganisms in aqueous and water-containing systems.
Abstract: Polymorphs of chemical compounds 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 P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
March 22, 2016
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
Type:
Grant
Filed:
August 10, 2011
Date of Patent:
March 22, 2016
Assignees:
Drexel University, Rutgers, The State University of New Jersey
Inventors:
Sandhya Kortagere, Eldo V. Kuzhikandahil
Abstract: Highly acidic, stabilized peroxycarboxylic acid compositions are disclosed as having both improved antimicrobial efficacy in comparison to conventional peroxyoctanoic acid and peroxyacetic acid compositions for sanitizing applications, and improved transport and shipping stability. In particular, low odor and low/no VOC compositions having dual functionality as both acid wash and sanitizing compositions are disclosed.
Type:
Grant
Filed:
December 29, 2014
Date of Patent:
March 22, 2016
Assignee:
Ecolab USA, Inc.
Inventors:
Junzhong Li, David D. McSherry, Richard Staub
Abstract: The present invention provides pharmaceutical formulations of levorotatory-epinephrine, l-epinephrine, more potent and less toxic than existing pharmaceutical formulations of epinephrine, along with methods of producing and using these pharmaceutical formulations of l-epinephrine.
Abstract: The present invention relates to a method for treating skin diseases and skin conditions in a patient in need thereof which comprises of administering a therapeutically effective amount of a pharmaceutical composition comprising a therapeutically effective amount of 7-(1H-Imidazol-4-ylmethyl)-5,6,7,8-tetrahydro-quinoline, or its individual enantiomers or the tautomers thereof, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
March 15, 2016
Assignee:
Allergan, Inc.
Inventors:
Mohammed I. Dibas, Edward C. Hsia, John E. Donello, Daniel W. Gil
Abstract: Compounds selected from the group of N-unsubstituted or N-alkylated or N-acylated 14-O-[(amino(C0-4)alkyl-hydroxy-cycloalkyl- or bicycloalkylsulfanyl)-acetyl]-mutilins which are 14-O-[(amino(C0-4)alkyl-hydroxy-cyclobutylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclopentylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cycloheptylsulfanyl)-acetyl]-mutilins, 14-O-[(amino(C0-4)alkyl-hydroxy-cyclooctylsulfanyl)-acetyl]-mutilins, or 14-O-[(amino(C0-4)alkyl-hydroxy-bicycloalkylsulfanyl)-acetyl]-mutilins, optionally in the form of a salt and/or a solvate, a pharmaceutical compositions comprising such compounds and their use as pharmaceuticals, e.g. for the treatment of microbial infections and for the treatment of acne, optionally in combination with other pharmaceutically active agents.
Type:
Grant
Filed:
August 11, 2011
Date of Patent:
March 8, 2016
Assignee:
Nabriva Therapeutics AG
Inventors:
Rosemarie Riedl, Klaus Thirring, Werner Heilmayer
Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. The oral bioavailabilty of zoledronic acid can be enhanced by administering the zoledronic acid in the disodium salt form.
Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
Type:
Grant
Filed:
December 6, 2011
Date of Patent:
March 1, 2016
Assignee:
AMIRA PHARMACEUTICALS, INC.
Inventors:
Thomas Jon Seiders, Bowei Wang, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
Abstract: Provided is a water-based patch that contains ketoprofen as an active ingredient, provides high transdermal absorbability of the ketoprofen, and has high safety and high storage stability. The water-based patch contains the ketoprofen, an amine, and polyethylene glycol. In the water-based patch, the added amount of the ketoprofen in a paste is 0.1 to 5% by weight, the added amount of the amine in the paste is 0.5 to 10% by weight, and the added amount of the polyethylene glycol in the paste is 5 to 30% by weight. Particularly, in the water-based patch, diisopropanolamine is used as the amine.
Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
Abstract: Disclosed are azaindazole compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein: Q is: (i) 5-membered heteroaryl comprising at least one nitrogen heteroatom and substituted with zero to 2 Rg; or (ii) 9- to 10-membered bicyclic heteroaryl selected from Formula (II) and; wherein Ring A is a 5- to 6-membered aryl or heteroaryl fused ring substituted with zero to 2 Rg; and R1, R2, R3, and Rg are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
Type:
Grant
Filed:
November 9, 2011
Date of Patent:
February 23, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Joel F. Austin, David B. Frennesson, Mark G. Saulnier
Abstract: A stable galenic composition of a compound of general formula (I) wherein R1 and R2 both represent independently of each other an alkyl, aryl, arylalkyl group, optionally substituted with one or more linear or branched groups, optionally bearing one or more heteroatoms, comprising said compound of formula I in an amount ranging from 0.01 to 15% by weight based on the total weight of the final composition; at least one anhydrous ester, the main chain and/or optionally the branched chains of which are free from free and/or reactive groups or functions, in an amount ranging from 0.1 to 99.9% by weight based on the total weight of the cosmetically and pharmaceutically acceptable composition; and optionally a cosmetically and pharmaceutically acceptable excipient for completing the 100% of the total weight of the composition.
Type:
Grant
Filed:
July 19, 2011
Date of Patent:
February 9, 2016
Assignee:
AURIGA INTERNATIONAL
Inventors:
Jacques Dubois, Alfred Marchal, Damien Lacroix, Jérôme Cabou
Abstract: A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.
Abstract: An occlusive dressing made with an elastomeric gel and one or more active agents is described. The elastomeric gel contains a plasticizing oil phase and a block copolymer agent. Methods of preventing, treating, curing or mitigating an infectious disease and methods of making the dressings are also disclosed.
Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
Abstract: The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
Type:
Grant
Filed:
January 12, 2012
Date of Patent:
January 26, 2016
Assignees:
SIENA BIOTECH S.P.A., HOFFMANN-LA ROCHE INC.
Inventors:
Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl, Harald Mauser