Coumarins (including Hydrogenated) Patents (Class 514/457)
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PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
Publication number: 20120108592Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol -
Publication number: 20120100223Abstract: Lipid compositions comprising nuts, seeds, oils, legumes, fruits, grains, and dairy useful in specified amounts as dietary supplements and diet plans designed around and including the aforementioned for the prophylaxis and treatment of numerous diseases are disclosed. The compositions include omega-6 and omega-3 fatty acids where the ratio of the omega-6 to the omega-3 fatty acids and their amounts are controlled based on one or more factors including age of the subject, sex of the subject, diet of the subject, the body weight of the subject, medical conditions of the subject, and climate of the subject's living area.Type: ApplicationFiled: December 20, 2011Publication date: April 26, 2012Applicant: ASHA NUTRITION SCIENCES, INC.Inventor: Urvashi BHAGAT
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Patent number: 8163795Abstract: Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.Type: GrantFiled: September 13, 2011Date of Patent: April 24, 2012Assignee: Marshall Edwards, Inc.Inventors: Andrew Heaton, Alan Husband
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Publication number: 20120094977Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: May 25, 2011Publication date: April 19, 2012Applicant: Dendreon CorporationInventors: Sateesh K. Natarajan, Ofir Moreno, Thomas J. Graddis, David F. Duncan, Reiner Laus, Feng Chen
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Patent number: 8158148Abstract: Accurate means of dosing with a compressed, segmented pharmaceutical tablet, and tablettes formed from said tablets, is disclosed.Type: GrantFiled: May 23, 2005Date of Patent: April 17, 2012Assignee: Accu-Break Technologies, Inc.Inventors: Lawrence Solomon, Allan S. Kaplan
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Publication number: 20120039796Abstract: A bio compatible free radical suspension, comprising of oxygen and electronically modified reaction intermediates, where a fluorocarbon is used as an inert medium for stabilization of reaction intermediates. A stabilized bio compatible electronically modified derivative suspension is produced by the subjecting a fluorocarbon to certain stressors, such as oxidizing agents, reactive intermediates, physiological gases, benzo-?-pyrone derivatives, ultrasonic-cavitation, electric fields, magnetic fields, UV radiation, active metal catalyst, surfactant reactants, buffers, electrolytes, glucose, glucose derivatives, for the purpose of inducing a cascading immune response.Type: ApplicationFiled: August 13, 2011Publication date: February 16, 2012Inventor: Demetrios Markou
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Publication number: 20120028912Abstract: The present invention features compounds useful for and methods for preventing or inhibiting the binding of bromodomains to acetyl-lysine residues of proteins and methods for treating HIV infection and HIV related disease.Type: ApplicationFiled: November 2, 2009Publication date: February 2, 2012Inventors: Ming-Ming Zhou, Aneel K. Aggarwal, Melanie Ott, Eric Verdin
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Publication number: 20120015904Abstract: The present invention provides methods and compositions for diagnosing and predicting the risk and cause of transient ischemic attacks (TIA).Type: ApplicationFiled: July 14, 2011Publication date: January 19, 2012Applicant: Regents of the University of CaliforniaInventors: Frank SHARP, Xinhua ZHAN, Glen C. JICKLING, S. Claiborne JOHNSTON
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Patent number: 8093288Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.Type: GrantFiled: November 19, 2009Date of Patent: January 10, 2012Assignees: Beth Israel Deaconess Medical Center, Trustees of Boston UniversityInventors: Chen-Yu Zhang, Bradford B. Lowell, John A Porco, Jr., Ruichao Shen, Cheng T. Lin, Stefan Krauss
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Publication number: 20120003335Abstract: The invention provides a method of controlling obesity or type two diabetes in a human. In accordance with the inventive method, the constitutive androstane receptor (CAR) is agonized within the human, which effectively controls obesity or type two diabetes.Type: ApplicationFiled: November 18, 2009Publication date: January 5, 2012Applicant: UNIVERSITY OF PITTSBURGH-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: Wen Xie, Jie Gao
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Publication number: 20110312984Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.Type: ApplicationFiled: June 3, 2009Publication date: December 22, 2011Inventors: David J. Tweardy, Wanzhi Huang, Moses M. Kasembeli
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Patent number: 8080675Abstract: Novel chroman derivatives and intermediate compounds, compositions containing same, methods for their preparation and uses thereof as therapeutic agents particularly as anti-cancer and chemotherapeutic selective agents are described.Type: GrantFiled: September 21, 2005Date of Patent: December 20, 2011Assignee: Marshall Edwards, Inc.Inventors: Andrew Heaton, Alan Husband
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Publication number: 20110300239Abstract: An object of the present invention to obtain a blood flow improving agent composed of natural components, which increase activity or circulation of blood flow and accelerate decomposition, detoxication and elimination of toxic substances and supplement each other, and the production method thereof. The blood flow improving agent of the present invention is prepared by blending a nano-colloidized marine organic compound, more than one of trace elements containing minerals extracted from a mineral ore and nano-colloidized plant minerals and amino acids derived from a fuvic acid in nano-bubble water containing dissolved oxygen.Type: ApplicationFiled: February 18, 2010Publication date: December 8, 2011Inventor: Yukio Hasegawa
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Patent number: 8067461Abstract: Compounds of Formula I: wherein R1, R2, M, Q and n are as defined herein, are useful as antiproliferative agents including, for example, as anticancer agents.Type: GrantFiled: June 2, 2006Date of Patent: November 29, 2011Assignee: Temple University-Of The Commonwealth System of Higher EducationInventors: M. V. Ramana Reddy, E. Premkumar Reddy
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Publication number: 20110288161Abstract: Certain embodiments in the present invention provide for methods for therapy of lung diseases and other conditions such as infection are provided. In certain embodiments, the methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e., ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments can include the use of agents to modulate transport of thiol-containing compounds from the cell such as thiocyanate. In certain embodiments, therapeutic methods involve the administration of such agents to a patient afflicted with an inflammatory condition or infection responsive to stimulation of thiol-containing compound transport.Type: ApplicationFiled: March 15, 2011Publication date: November 24, 2011Inventor: Brian J. Day
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Publication number: 20110275558Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.Type: ApplicationFiled: May 4, 2011Publication date: November 10, 2011Applicant: Virginia Tech Intellectual Properties, Inc.Inventors: Josep BASSAGANYA-RIERA, Pinyi LU, Raquel HONTECILLAS
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Publication number: 20110271408Abstract: Mutated PYR/PYL receptor polypeptides and methods of making and using mutated PYR/PYL receptor polypeptides are described.Type: ApplicationFiled: April 27, 2011Publication date: November 3, 2011Applicant: Regents of the University of CaliforniaInventors: Sean R. Cutler, Sang-Youl Park
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Publication number: 20110268679Abstract: Described herein are compositions and methods for preventing and/or treating skin diseases including, but not limited to, psoriasis and atopic dermatitis as well as providing anti-aging benefits which results in reduced appearance of wrinkles and aged skin, improved skin color, treatment of photodamaged skin, improvement in skin's radiance and clarity and finish, and an overall healthy and youthful appearance of the skin, involving aberrant angiogenesis and hyperplasia employing one or more benzo[c]chromen-6-one derivatives.Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Inventor: David SHERRIS
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Publication number: 20110268692Abstract: The present invention relates to the combination of an active anticoagulant rodenticidal compound with an analogue of vitamin D, with at least one of the two components being used at a very low concentration.Type: ApplicationFiled: October 7, 2009Publication date: November 3, 2011Applicant: Bayer CropScience AGInventor: Stefan Endepols
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Patent number: 8048889Abstract: The present invention relates to 3,4-disubstituted coumarin and quinolone derivatives and processes for their preparation. The invention also related to methods for treating infection of Hepatitis C virus by administering a 3,4-disubstituted coumarin or quinolone derivative.Type: GrantFiled: March 29, 2005Date of Patent: November 1, 2011Assignee: XTL Biopharmaceuticals Ltd.Inventors: Bin Xu, Qiang Zhu, Hyun-Joon Cho, Reza Fathi, Zhen Yang, Anthony Sandrasagra, Yixin Liu
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Publication number: 20110262362Abstract: The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.Type: ApplicationFiled: October 9, 2009Publication date: October 27, 2011Inventors: Yansong Gu, Hongzhi Li
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Patent number: 8044094Abstract: The present invention refers to coumarin ethers of the formula (I), wherein R1 is H, OH or (E)-3-methyl-but-2-enyl, R2 is selected from the group consisting of methyl, 3-(4,5-dihydro-5,5-dimethyl-4-furanon-2-yl)-2-(E/Z)-butenyl, (E/Z)-3,7-dimethylocta-2,6-dienyl, 7-hydroxy-3,7-dimethyl-2-octen-6-on-yl and (E/Z,E/Z)-11-acetyl-oxy-3,7,11,11-tetramethyl-undeca-2,7-dien-10-on-yl, R3 is H, R1 and R2O together for the group —O—C(C(?CH2)CH3)H—CH2—O— or the group —C(H)?C(H)—C(CH3)2—O— or R2O and R3 together form the group —O—C(H)(C(CH3)2(H)—O—C(O)CH3)—CH2—, preferably to obliquin, for use as medicaments, especially for the treatment and/or prevention of disorders connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions and plant extracts containing such coumarin ethers and their uses.Type: GrantFiled: October 21, 2005Date of Patent: October 25, 2011Assignee: DSM IP Assets B.V.Inventors: Antoine De Saizieu, Ann Fowler, Regina Goralczyk, Goede Schueler, Bernd Mussler
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Publication number: 20110251272Abstract: The present invention relates to methods and compositions for predicting drug responses. In particular, the present invention provides methods and compositions for determining individualized Warfarin dosages based on genotype of DNA polymorphisms and haplotypes derived from them in the VKORC1 gene.Type: ApplicationFiled: January 18, 2011Publication date: October 13, 2011Applicant: UNIVERSITY OF WASHINGTONInventors: Mark J. Rieder, Allan Rettie
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Publication number: 20110243958Abstract: Aspects of the invention relate to a method for inhibiting the growth of a microbe that expresses bacterial vitamin K epoxide reductase (bVKOR). The method involves contacting the bacterial cell with an effective amount of an agent that inhibits bVKOR. Agents include a drug, ligand or portion thereof, protein, polypeptide, small organic molecule, antisense nucleic acid, RNAi, or antibody. Examples of useful agents are a phenylpropanoid, a modified phenylpropanoid, a coumarin or modified coumarin. A particularly useful agents is warfarin or a variant thereof or ferulenol or a variant thereof. The microbe is any microbe carrying a bVKOR gene, such as Mycobacterium tuberculosis.Type: ApplicationFiled: October 14, 2009Publication date: October 6, 2011Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Jonathan Beckwith, Rachel Dutton, Dana Boyd, Mehmet Berkmen
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Publication number: 20110243917Abstract: The present invention relates to a composition comprising PKC agonist as an active ingredient. More precisely, the present inventors confirmed that absence seizure specific SWD was reduced by administrating PKC agonist into an animal model. Therefore, the composition of the present invention comprising PKC agonist as an active ingredient can be effectively used for the prevention and treatment of absence seizure and for the production of health improving functional food.Type: ApplicationFiled: August 5, 2010Publication date: October 6, 2011Inventors: Eunji Cheong, Hee-Sup Shin, Yihong Zheng, Kyoobin Lee, Jungryun Lee, Seongwook Kim, Maryam Sanati, Sukyung Lee, Yeon-Soo Kim
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Publication number: 20110224292Abstract: Methods and apparatus are disclosed for determining new anticoagulant therapy factors for monitoring oral anticoagulant therapy to help prevent excessive bleeding or deleterious blood clots that might otherwise occur before, during or after surgery. The inventive methods and apparatus provide an International Normalization Ratio (INR) based on a coagulation reaction with a blood sample of a living being. Embodiments include methods and apparatus for determining an anticoagulant therapy factor without requiring use of a mean normal prothrombin time determination or an ISI, and may be carried out with the patient sample and a coagulation reagent, where the coagulation reagent may be selected from a number of coagulation reagents.Type: ApplicationFiled: March 7, 2011Publication date: September 15, 2011Inventors: Wallace E. Carroll, R. David Jackson
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Publication number: 20110218209Abstract: The present invention is a hypoallergenic nutrient delivery drug composition, that includes an active drug, a binder with non-genetically engineered and non-chemically treated starches and food powders, a filler with non-genetically engineered and non-chemically treated vegetable powder and/or extracts and a non-genetically engineered and non-chemically treated fruit powder and/or extract and a preservative that includes non-genetically engineered and non-chemically treated fruit juice, fruit oil and vitamins. There is also a sustained nutrient drug delivery composition that includes non-genetically engineered and non-chemically treated oils, starches and vegetable powders and/or extracts and fruit powder and/or extracts. There is also a broad spectrum nutrient delivery drug composition that includes non-genetically engineered and non-chemically treated pepper and oil mixtures or extracts.Type: ApplicationFiled: March 2, 2011Publication date: September 8, 2011Inventor: Paul Daniel Yered
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Publication number: 20110206739Abstract: The disclosure relates to compositions and methods of forming nanoemulsions, e.g., containing an active component, in combination with lipophilic components such as oils, hydrophilic components such as water, and one or more surfactants capable of causing a temperature-dependent phase inversion, such as a nonionic polyethoxylated surfactant. Nanoemulsions containing the active component can be produced having average oil droplet sizes of less than 100 nm, 50 nm, or 25 nm without the need for high energy emulsion forming methods (such as microfluidization) by combining the surfactant and the oil in specified weight ratios (e.g., at least 3:1) prior to forming the nanoemulsion.Type: ApplicationFiled: March 30, 2009Publication date: August 25, 2011Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Robert J. Nicolosi, Fonghsu Kuo, SriKanth Kakumanu, Shawn Konecni, Carl W. Lawton
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Publication number: 20110196029Abstract: New pharmaceutical compositions extracted from Ferula assa-foetida are confirmed to effectively treat influenza A (H1N1) virus. The extraction method of the new pharmaceutical compositions mainly includes steps of (a) extracting F. assa-foetida with methanol to obtain a crude extract; (b) fractioning the crude extract with n-hexane-methanol to obtain a methanol extract; (c) fractioning the methanol extract with chloroform-water to obtain a chloroform extract; and (d) chromatographing the chloroform extract to obtain the pharmaceutical compositions, which can be further fractioned and chromatographed to obtain various sesquiterpene coumarins.Type: ApplicationFiled: August 18, 2010Publication date: August 11, 2011Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventors: Yang-Chang Wu, Fang-Rong Chang, Lien-Chai Chiang
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Publication number: 20110190234Abstract: The present invention is directed to methods and compounds for inhibiting bacterial growth and treating a bacterial infection in a subject. These methods involve providing an inhibitor of intrabacterial pH homeostasis, including inhibitors of the Mycobacterium tuberculosis Rv3671c gene encoded membrane protease. Methods for identifying novel compounds that disrupt intrabacterial pH homeostasis and their use for inhibiting bacterial growth and treating a bacterial infection in a subject are also disclosed.Type: ApplicationFiled: July 20, 2009Publication date: August 4, 2011Applicant: CORNELL UNIVERSITYInventors: Carl Nathan, Sabine Ehrt, Omar Vandal, Crystal Darby
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Publication number: 20110190229Abstract: A method for preventing hyperpigmented skin, undesired pigmentation disorder of skin, or undesired darkening of skin using coumarin compounds, the use of such compounds, and compositions and formulations thereof are disclosed. In a particular embodiment, the coumarin compounds are selected from robustic acid methyl ether, scandenin, and coumophos. The compounds may be prepared as additives to pharmaceutical and cosmetic compositions, and in personal care products such as antiperspirants. In a particular embodiment extends to an antiperspirant product containing a skin darkening inhibitory amount of a compound of the invention. Also, the present skin darkening compounds may be prepared in combination with each other.Type: ApplicationFiled: January 28, 2011Publication date: August 4, 2011Inventors: Seth J. Orlow, Li Ni Komatsu
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Publication number: 20110172234Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.Type: ApplicationFiled: March 28, 2011Publication date: July 14, 2011Applicants: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, UNIVERSITY OF MARYLAND, BALTIMORE A CONSTITUENT INSTITUTION OF THE UNIVERSITYInventors: Rakesh Srivastava, Sharmila Shankar, Alexander D. MacKerell, JR.
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Publication number: 20110171146Abstract: An anti-aging composition comprising a skin-beneficial amount of actives identified in Menyanthes trifoliata leaf, wherein the actives are inhibitors of one or more of MMP-1, 2 and 9 and/or scavengers of peroxynitrite. Also disclosed are methods of using such a composition, which include treating the skin for signs of chronological or pre-mature aging.Type: ApplicationFiled: February 4, 2011Publication date: July 14, 2011Inventors: Hugo Corstjens, Lieve Declercq, Ilse Sente, Annelise Lobstein, Bernard Weniger, Robert Anton
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Publication number: 20110172220Abstract: 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.Type: ApplicationFiled: November 15, 2010Publication date: July 14, 2011Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Amos B. Smith, III, Simon J. Shaw, David C. Myles
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Publication number: 20110144127Abstract: Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating glaucomatous retinopathy or optic neuropathy. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.Type: ApplicationFiled: February 22, 2011Publication date: June 16, 2011Applicant: ALCON INC.Inventors: Robert A. Landers, Iok-Hou Pang
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Publication number: 20110136779Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering a multiple ion channel blocker anti-arrhythmic to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of multiple ion channel blocker and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of the multiple ion channel blocker may also be treated.Type: ApplicationFiled: November 23, 2010Publication date: June 9, 2011Inventors: Peter G. Milner, David Jack Ellis
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Publication number: 20110124504Abstract: Disclosed is a process for preparing an adjuvant for agricultural applications, characterized in that a polyhydric alcohol, polyol, saccharide, or polysaccharide is reacted with a sulfonating agent, such as sulphamic acid.Type: ApplicationFiled: July 11, 2009Publication date: May 26, 2011Applicant: COGNIS IP MANAGEMENT GMBHInventors: Dean Oester, Mike White, Timothy Anderson
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Publication number: 20110123512Abstract: The present invention is directed to method of modulating a heat shock response in a first cell of a multicellular organism comprising stimulating or inhibiting an HSR signaling activity of a second cell, wherein the second cell is a neuronal cell that regulates heat shock response activation in the first cell and that does not directly innervate the first cell.Type: ApplicationFiled: November 8, 2010Publication date: May 26, 2011Inventors: Veena Prahlad, Richard I. Morimoto
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Publication number: 20110117202Abstract: Methods and systems for producing a change in a medium. A first method and system (1) place in a vicinity of the medium at least one upconverter including a gas for plasma ignition, with the upconverter being configured, upon exposure to initiation energy, to generate light for emission into the medium, and (2) apply the initiation energy from an energy source including the first wavelength ?1 to the medium, wherein the emitted light directly or indirectly produces the change in the medium. A second method and system (1) place in a vicinity of the medium an agent receptive to microwave radiation or radiofrequency radiation, and (2) apply as an initiation energy the microwave radiation or radiofrequency radiation by which the agent directly or indirectly generates emitted light in the infrared, visible, or ultraviolet range to produce at least one of physical and biological changes in the medium.Type: ApplicationFiled: November 10, 2010Publication date: May 19, 2011Applicants: Immunolight, LLC, Duke UniversityInventors: Frederic A. Bourke, JR., Zakaryae Fathi, Ian Nicholas Stanton, Michael J. Therien, Paul Rath Stauffer, Paolo MacCarini, Katherine Sarah Hansen, Diane Renee Fels, Cory Robert Wyatt, Mark Wesley Dewhirst
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Publication number: 20110112084Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.Type: ApplicationFiled: November 13, 2009Publication date: May 12, 2011Inventors: Lin Zhi, Christopher Tegley, Barbara Pio, Corneils Arjan Van Oeveren, Mehrnouch Motamedi, Esther Martinborough, Robert Higuchi, Lawrence G. Hamann
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Patent number: 7932405Abstract: The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.Type: GrantFiled: November 10, 2008Date of Patent: April 26, 2011Assignee: Aryx Therapeutics, Inc.Inventors: Pascal Druzgala, Cyrus Becker
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Publication number: 20110091565Abstract: Methods are described for producing non-immunogenic nanoparticles from protein sources by controlling the pH in a nanoprecipitation process. The nanoparticles that are produced by the disclosed methods range in diameter size from about 100 ran to about 400 nm, with a preferred diameter size of from approximately 100 nm to approximately 300 nm, thereby rendering them non-immunogenic. The invention further discloses methods for producing nanoconjugates that are suitable for a variety of therapeutic, diagnostic and other uses.Type: ApplicationFiled: May 11, 2009Publication date: April 21, 2011Inventors: Omathanu P. Perumal, Satheesh K. Podaralla, Radhey S. Kaushik
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Publication number: 20110082098Abstract: Novobiocin analogues are useful in methods of treating, inhibiting, and/or preventing cyst formation in autosomal dominant polycystic kidney disease (ADPKD) in a subject. The disclosure provides methods of treating ADPKD comprising administering a therapeutically effective amount of a coumarin-3-carboxamide novobiocin analogue. Accordingly, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of mTOR pathway phosphoproteins P-mTOR, P-Akt and P-S6K, or combinations thereof. Further, the method can include administering a novobiocin analogue in a therapeutically effective amount for reducing levels of Hsp-90 client proteins CFTR, ErbB2, c-Raf and Cdk4, or combinations thereof.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: UNIVERSITY OF KANSASInventors: James P. Calvet, Brian S.J. Blagg, Shirin V. Sundar, Brenda S. Magenheimer
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Publication number: 20110082071Abstract: The invention relates to a delivery system for an active ingredient. The system provides an encapsulating material for the active ingredient, wherein the encapsulating material is formed by combining a cationic component, an anionic component and the active ingredient. The anionic component is a mixture of carbonate and phosphate moieties, wherein the molar ratio of carbonate to phosphate moieties is from 9:1 to 1:9.Type: ApplicationFiled: May 14, 2009Publication date: April 7, 2011Inventors: Amal Elabbadi, Olivier Haefliger, Lahoussine Ouali
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Publication number: 20110071142Abstract: The present invention relates to methods of identifying small molecule candidate agents capable of modulating transcription factor function such that the function/expression of a target transcription factor and/or proteins downstream of this target protein comprises the screening of small molecule libraries using in silico high throughput docking for candidate small molecules/agents that are selectively identified for their ability to target and disrupt the transcription factor-DNA interface through unique transcription factor and/or DNA descriptors that are defined within a pharmacophore, and then testing/evaluating the candidate agents identified above through one or more in vitro assays for their ability to modulate transcription factor function including expression of this target protein and/or proteins that are downstream of the target transcription factor. The present invention also relates to various compounds described herein (e.g.Type: ApplicationFiled: March 19, 2010Publication date: March 24, 2011Applicant: BETH ISRAEL DEACONESS MEDICAL CENTERInventors: Peter Oettgen, Alan C. Rigby, Towia Libermann
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Publication number: 20110065704Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.Type: ApplicationFiled: June 25, 2010Publication date: March 17, 2011Inventor: Sean RYDER
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Publication number: 20110044999Abstract: The present invention relates to methods of screening for modulators of interleukin 32 (IL-32), to modulators of IL-32 and to their use.Type: ApplicationFiled: October 8, 2010Publication date: February 24, 2011Applicants: YEDA RESEARCH AND DEVELOPMENT CO. LTD, THE REGENTS OF THE UNIVERSITY OF COLORADOInventors: DANIELA NOVICK, MENACHEM RUBINSTEIN, CHARLES A. DINARELLO, SOO-HYUN KIM
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Publication number: 20110038905Abstract: It is an object of the present invention to provide a skin anti-aging agent for external use which comprises highly safe protein nanoparticles having high transparency due to the small particle size and high permeability into skin. The present invention provides a skin anti-aging agent for external use, which comprises protein nanoparticles containing an active ingredient.Type: ApplicationFiled: October 28, 2010Publication date: February 17, 2011Applicant: FUJIFILM CorporationInventors: Makiko AIMI, Kazutaka Ogiwara, Takuo Amano
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Patent number: 7888388Abstract: The present invention easily and efficiently provides a peroxisome proliferator-activated receptor ligand, and a composition for amelioration of insulin resistance or for prevention and/or amelioration of the insulin resistance syndrome containing the same, as an active ingredient. The present invention relates to a peroxisome proliferator-activated receptor ligand which comprises a prenylflavonoid, a chalcone derivative exclusive of prenylflavonoids, a flavonol derivative exclusive of prenylflavonoids, and a salt, a glycoside and/or an esterified substance thereof acceptable as a pharmaceutical preparation or a food or a beverage; a composition containing the above ligand; a plant-derived extract containing the above ligand; and a process for producing the above extract.Type: GrantFiled: September 18, 2008Date of Patent: February 15, 2011Assignee: Kaneka CorporationInventors: Tatsumasa Mae, Misuzu Tsukagawa, Mikio Kitahara, Kaku Nakagawa, Shiro Kitamura, Yasuyoshi Ueda, Minpei Kuroda, Yoshihiro Mimaki, Yutaka Sashida
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Publication number: 20110033397Abstract: An anti-aging composition comprising a skin-beneficial amount of actives identified in Menyanthes trifoliata leaf, wherein the actives are inhibitors of one or more of MMP-1, 2 and 9 and/or scavengers of peroxynitrite. Also disclosed are methods of using such a composition, which include treating the skin for signs of chronological or pre-mature aging.Type: ApplicationFiled: October 25, 2010Publication date: February 10, 2011Inventors: Hugo Corstjens, Lieve Declercq, Ilse Sente, Annelise Lobstein, Bernard Weniger, Robert Anton