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, ring Z, m and p 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:
September 2, 2014
Assignee:
Amgen Inc.
Inventors:
Nick A. Paras, Yuan Cheng, Timothy Powers, James Brown, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Qiufen Xue, Bryant Yang
Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
Type:
Grant
Filed:
July 13, 2012
Date of Patent:
September 2, 2014
Assignee:
Bristol-Myers Squibb Company
Inventors:
Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
Type:
Grant
Filed:
January 14, 2011
Date of Patent:
September 2, 2014
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Peter Wipf, Natalia A. Belikova, Jianfei Jiang, Joshua Pierce, Joel Greenberger, Michael Epperly, Valerian Kagan
Abstract: There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.
Abstract: A process for improving the health of a subject, the process comprising orally administering a composition comprising hydroxytyrosol to the subject to provide the subject with a daily dose of about 0.1 to about 750 ?g hydroxytyrosol per kg of body weight, and a dietary supplement in dosage unit form for oral administration, the dosage unit form comprising a composition containing about 1 microgram to about 50 milligrams hydroxytyrosol or an ester or salt thereof.
Abstract: The present invention relates to the field of oil thickeners and in particular oil gels. Embodiments of the present invention relate for example to a an oil composition containing at least one complex comprising an oil dispersible emulsifier and protein fibers and preparations comprising such oil compositions; the use of such complexes as oil thickeners, and a method to produce the complexes.
Abstract: A method for inhibiting the production of cytokines of T helper cell type II (Th2 cell) and/or inhibiting the production of chemokines in a mammal is provided, wherein the method comprises administrating to the mammal an effective amount of an active component selected from a group consisting of a compound of formula (I), pharmaceutically acceptable salts and esters of the compound, and combinations thereof:
Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.
Type:
Grant
Filed:
June 17, 2011
Date of Patent:
August 5, 2014
Assignees:
California Institute of Technology, The Regents of the University of California, The United States of America as represented by the Department of Veterans Affairs
Inventors:
William A. Goddard, III, Mark Menna, Stephen Pandol, Ravinder Abrol
Abstract: This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.
Type:
Grant
Filed:
July 8, 2011
Date of Patent:
August 5, 2014
Assignees:
AbbVie B.V., AbbVie Inc.
Inventors:
Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.
Abstract: The present invention provides a novel biphenyl compound or pharmaceutically acceptable salts thereof, methods for preparing the same, and pharmaceutical compositions for preventing or treating diabetic complications containing the same as an active ingredient. Novel biphenyl compounds, according to the present invention, effectively suppress generation activity of advanced glycation end products, which cause diabetic complications and are a criterion for evaluating the effectiveness of a treating agent for diabetic complications, and show an excellent therapeutic effect on retina blood vessels, increased occludin, and decreased angiogenic growth factor in actual diabetic retinopathy induced retina. Thus, novel biphenyl compounds according to the present invention can be used effectively as an active ingredient in compositions for preventing or treating diabetic complications such as diabetic retinopathy.
Type:
Grant
Filed:
August 11, 2011
Date of Patent:
July 22, 2014
Assignee:
Korea Institute of Oriental Medicine
Inventors:
Jin Sook Kim, Young Sook Kim, Jung Hyun Kim, Eun Jin Shon, Ki Mo Kim, Chan-Sik Kim, Dong Ho Jung, Yun Mi Lee, Kyu Hyung Jo, Ohn Soon Kim, Nam-Hee Yoo
Abstract: The present invention provides a water-in-oil emulsion cosmetic that is excellent in the resilient and supple (in other words, firm and tensional) feels and also excellent in the moisturizing effect and feeling in use. The water-in-oil emulsion cosmetic of the present invention is characterized by comprising the following (A) to (D): (A) 0.5 to 10 mass % of bis-diglyceryl polyacyladipate-2 (B) an oil containing (b1) (b1) a volatile oil of low compatibility with (A) (C) an emulsifying agent and (D) 60 to 90 mass % of an aqueous component, wherein the percentage of component (b1) is 40 to 85% with respect to component (A) and component (B).
Abstract: The disclosure provides compositions and systems for topical ophthalmic application, which include an aqueous mixture of bromfenac and flowable mucoadhesive polymer, for treating inflammation and inflammatory conditions of the eye.
Type:
Grant
Filed:
March 5, 2009
Date of Patent:
July 15, 2014
Assignee:
Insite Vision Incorporated
Inventors:
Kamran Hosseini, Lyle Bowman, Erwin C. Si, Stephen Pham
Abstract: The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used.
Type:
Grant
Filed:
February 25, 2010
Date of Patent:
July 15, 2014
Assignee:
Council of Scientific & Industrial Research
Abstract: Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.
Type:
Grant
Filed:
January 24, 2011
Date of Patent:
July 15, 2014
Assignees:
Sutter West Bay Hospital, Catholic Healthcare West
Abstract: A compound represented by the following general formula (1) or a salt thereof, which has superior inhibitory activity against type 4 PLA2, and thus has prostaglandin and/or leucotriene production suppressing action [X represents a halogen atom, an alkyl group which may be substituted, or the like, Y represents hydrogen atom or an alkyl group which may be substituted, and Z represents hydrogen atom or an alkyl group which may be substituted].
Abstract: A compound represented by the following general formula (I) which has ADAM17 inhibitory activity, or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents a hydrogen atom, —(CH2)mR1 or the like; R1 represents —NR5COR2, —NR5SO2R2 or —NR3R4; R2 represents a C1-C6 alkyl group, an aryl group, or a C1-C6 alkoxy group; R3 and R4 represent a C1-C6 alkyl group and the like; R5 represents a hydrogen atom or a C1-C6 alkyl group or the like; m indicates an integer of from 0 to 4; and Z represents a hydrogen atom or a C1-C6 alkyl group.
Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Abstract: Quinazoline derivatives are provided that specifically inhibit proliferation of T cells without affecting the level of IL-2 secreted from said T cells. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of indications mediated by T cell proliferation.
Type:
Grant
Filed:
January 27, 2011
Date of Patent:
June 24, 2014
Assignee:
Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.