C=x Bonded Directly Or Indirectly By An Acyclic Carbon Or Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring (e.g., Tryptophan, Etc.) (x Is Chalcogen) Patents (Class 514/419)
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Patent number: 8901317Abstract: The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized by formation of amide or ester with some known anti oxidant molecules. These derivatives show excellent antioxidant property in vitro. Among all the derivatives the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesized compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and also accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondroial transmembrane potential and dehydrogenase activity.Type: GrantFiled: September 14, 2011Date of Patent: December 2, 2014Assignees: Council of Scientific & Industrial Research, University of CalcuttaInventors: Uday Bandyopadhyay, Chinmay Pal, Samik Bindu, Susanta Sekhar Adhikari
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Publication number: 20140343116Abstract: This invention is to provide multiple specific inhibitors of cytochrome P450 isozyme CYP2C9. These inhibitors can be derived from any combinations with the following compounds including: Tamarixetin, Formononetin, isoliquritigenin, Phloretin, luteolin, Quercitrin, quercetin, myricetin, Wongonin, Puerarin, Genistein, Nordihydroguaiaretic acid, Narigenin, Capillarisin, Chrysin, Fisefin, eriodictyol, 6-Gingerol, Isorhamneti, isoquercitrin, Morin, (+)-Taxifolin, isovitexin, 3-Phenylpropyl Acetate, Oleanolic acid, ursolic acid, ?-Myrcene, cinnamic acid, Luteolin-7-Glucoside, Liquiritin, (+)Limonene, Homoorientin, Swertiamarin, Embelin, Daidzein, Poncirin, (?)-Epicatechin, ergosterol. These natural products can be used to enhance the bioavailability of therapeutic agents (drugs).Type: ApplicationFiled: July 30, 2014Publication date: November 20, 2014Inventors: Oliver Yoa-Pu HU, Hong-Jaan Wang, Cheng-Huei Hsiong, Li-Heng Pao
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Publication number: 20140343001Abstract: The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy.Type: ApplicationFiled: December 19, 2012Publication date: November 20, 2014Applicant: Universita di PisaInventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Valeria Di Bussolo, Gino Giannaccini, Antonio Lucacchini, Paul J. Hergenrother, Emilia C. Calvaresi
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Publication number: 20140343050Abstract: Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.Type: ApplicationFiled: March 30, 2012Publication date: November 20, 2014Applicant: APTOEX TECHNOLOGIES, INC.Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Wanren Li, Jolanta Maria Wodzinska, Vrajlal S. Rabadia, Christopher John Feeney
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Patent number: 8889729Abstract: Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.Type: GrantFiled: June 6, 2010Date of Patent: November 18, 2014Assignee: Tel Aviv University Future Technology Development L.P.Inventors: Ehud Gazit, Tomer Cohen
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Patent number: 8889730Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.Type: GrantFiled: March 15, 2013Date of Patent: November 18, 2014Assignee: Pfizer Inc.Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
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Patent number: 8889194Abstract: Disclosed is a compound and methods for use by an individual attempting to reduce or cease tobacco smoking or one exposed to environmental tobacco smoke. The compound includes a first component blocking nicotine receptor sites to reduce nicotine cravings or withdrawal symptoms, a second component increasing serotonin levels and acting synergistically with the first component to reduce nicotine cravings or withdrawal symptoms, assisting in maintaining body weight and reducing increased stress and anxiety, and a third component acting synergistically with the first and/or second component to reduce nicotine cravings or withdrawal symptoms, maintain body weight, and/or reduce increased stress and anxiety. The third component comprises a supplement that replenishes depleted body substance(s), repairs damaged body substance(s), and/or ameliorates the impaired function of body substance(s). Some combination of the first, second, and third component alters the perceived taste of tobacco smoke.Type: GrantFiled: September 29, 2010Date of Patent: November 18, 2014Inventor: Harlan Clayton Bieley
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Patent number: 8883233Abstract: Disclosed is an animal feed composition that comprises free indole acetic acid (free IAA) or a derivative thereof. Also disclosed is a method for enhancing animal growth by feeding the animal with a composition according to the invention. Further disclosed is the use of free IAA or a derivative thereof in a method of therapy of animals in need of a growth-promoting treatment, such as immunocompromised animals, animals with a growth deficit or slow-growing animals. Disclosed is the use of free IAA or a derivative thereof for the preparation of a therapeutical composition for increasing the growth rate and/or the feed conversion rate and/or the immunity of animals in need of such a treatment, in particular, immunocompromised or slow-growing animals. A composition may be in the form of a food or feed supplement.Type: GrantFiled: July 13, 2012Date of Patent: November 11, 2014Assignee: Veijlen N.V.Inventors: Hurbert Jean Marie Francois Gillessen, Christian Rebiere
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Publication number: 20140329785Abstract: The present embodiments provide for sustained release formulations of antioxidants that are useful in treating afflictions of the eye and tumors.Type: ApplicationFiled: June 11, 2012Publication date: November 6, 2014Applicant: RAMSCOR, INC.Inventor: Carol Wood
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Publication number: 20140323535Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Applicants: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY, FLORIDA INSTITUTE OF TECHNOLOGYInventors: William S. POWELL, Joshua ROKACH
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Publication number: 20140323475Abstract: The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 14, 2012Publication date: October 30, 2014Inventors: Antoni Torrens Jover, Ramon Mercé Vidal, Francesc Xavier Caldentey Frontera, Antonio David Rodríguez Garrido, Elena Carceller González, Jordi Salas Solana
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Patent number: 8859593Abstract: The invention relates to a pharmacologically active combination, having utility in treating insomnia patients, which comprises: (a) at least one first active ingredient selected from melatonin, other melatonergic agents, melatonin agonists and melatonin antagonists; and (b) at least one second active ingredient selected from nicotine and nicotine receptor agonists; to use of a medicament containing component (a) with or without component (b) for alleviation of at least one adverse effect which occurs in a patient in the course of nicotine replacement therapy, or otherwise, selected from impairment of the quality of sleep, impairment of cognition and impairment of memory, as well as to a kit having utility in treating insomnia patients, which comprises components (a) and (b) in unit dosage form.Type: GrantFiled: April 15, 2004Date of Patent: October 14, 2014Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
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Publication number: 20140303227Abstract: The present invention provides a pharmaceutical composition for sublingual or buccal administration of actives with low to poor aqueous solubility, e.g. the hormone melatonin, which contains a solution of the active in a pharmaceutically acceptable solvent adsorbed or absorbed onto particles of a pharmaceutically acceptable carrier and methods of preparing and using the pharmaceutical composition.Type: ApplicationFiled: March 14, 2014Publication date: October 9, 2014Inventor: John McCarty
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Publication number: 20140302170Abstract: Described herein are food formulations and methods, which promote sleep.Type: ApplicationFiled: April 8, 2014Publication date: October 9, 2014Applicant: Scientific Nutrition Products, Inc.Inventors: Robert C. Jones, Caroline Apovian, Bruce R. Bistrian, Judy Phillips
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Publication number: 20140303186Abstract: The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.Type: ApplicationFiled: November 16, 2012Publication date: October 9, 2014Inventors: Yan Zhang, Min Zhang, Hoyin Lo
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Publication number: 20140303228Abstract: The disclosure provides biomarkers of amyotrophic lateral sclerosis (ALS). The disclosure also provides various methods of using the biomarkers, including methods for diagnosis of ALS, methods of determining predisposition to ALS, methods of monitoring progression/regression of ALS, methods of assessing efficacy of compositions for treating ALS, methods of screening compositions for activity in modulating biomarkers of ALS, methods of treating ALS, as well as other methods based on biomarkers of ALS.Type: ApplicationFiled: October 17, 2012Publication date: October 9, 2014Inventors: Kay A. Lawton, Meredith V. Brown, Bruce Neri, Rebecca Caffrey, Michael V. Milburn
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Patent number: 8853254Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: October 16, 2012Date of Patent: October 7, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida Ruah, Anna Hazlewood
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Patent number: 8853229Abstract: A combination is described comprising at least one omega-3 fatty acid, optionally esterified or salified, at least one statin, Coenzyme Q10, resveratrol, at least one policosanol, pantethine, selenium, and zinc. This combination is endowed with a synergistic effect and is useful in the treatment of disease forms due to insulin resistance and in cardiovascular diseases.Type: GrantFiled: July 19, 2005Date of Patent: October 7, 2014Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventor: Claudio Cavazza
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Patent number: 8853209Abstract: Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mdl-1 protein, such as leukemia and lymphoma, are disclosed.Type: GrantFiled: April 15, 2011Date of Patent: October 7, 2014Assignee: AbbVie Inc.Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
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Publication number: 20140294767Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Inventors: David Waugh, Christopher Self, Guangtao Zhang, Yves Pommier, Robert H. Shoemaker, Michael Currens, John Cardellina, Andrew Jobson, George Lountos, Dominic Scudiero
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Publication number: 20140296223Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.Type: ApplicationFiled: August 31, 2012Publication date: October 2, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140288119Abstract: This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(?O)OR8, C(?O)R8, —C(?O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present orType: ApplicationFiled: October 3, 2012Publication date: September 25, 2014Applicants: The Trustees of Columbia University in the City of New York, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Ronald Breslow, Paul A. Marks
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Publication number: 20140275093Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: October 16, 2013Publication date: September 18, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Patent number: 8835486Abstract: An improved pharmaceutical formulation for oral administration includes a therapeutically effective quantity of an active ingredient and a stabilizer. The active ingredient is Fluvastatin, or pharmaceutically acceptable salts thereof, and the stabilizer is a mixture of Carrageenans. The stabilizer inhibits isomerization, and/or elimination, and/or oxidation and/or recrystallization of the active ingredient.Type: GrantFiled: May 12, 2006Date of Patent: September 16, 2014Inventors: Evangelos Karavas, Efthimios Koutris, Elisavet Ioannidou, Eleni Stathaki, Dimitrios Bikiaris
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Publication number: 20140256666Abstract: The present invention describes single drug entities, formed by connecting an antibiotic moiety via a linker with a non-steroidal anti-inflammatory drug (NSAID) moiety. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual antibiotic and NSAID drug.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140249197Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: May 14, 2014Publication date: September 4, 2014Applicant: Janssen Pharmaceutica, NVInventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Publication number: 20140249199Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.Type: ApplicationFiled: July 19, 2012Publication date: September 4, 2014Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITYInventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
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Patent number: 8821915Abstract: The present invention is directed to a method of treating a patient suffering from the metabolic syndrome and/or related disorders including obesity, Type 2 diabetes, pre-diabetes, hypertension, dyslipidemia, insulin resistance, endothelial dysfunction, pro-inflammatory state, and pro-coagulative state, and comprising the steps of (a) providing to the patient a dietary regimen that decreases overactive CNS noradrenergic tone; followed by (b) providing to the patient a dietary regimen that increases dopaminergic tone while maintaining the above decreased overactive CNS noradrenergic tone. The present invention is also directed to food products useful in implementing the dietary regimens.Type: GrantFiled: September 19, 2011Date of Patent: September 2, 2014Assignee: VeroScience, LLCInventor: Anthony Cincotta
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Publication number: 20140242030Abstract: Provided is a novel anti-HCV agent including as an active ingredient a peroxide derivative represented by the general formula (I). In the general formula (I), C represents an alicyclic hydrocarbon ring group which may be substituted, n represents an integer of from 1 to 6, and R represents a hydrogen atom or a hydroxyalkyl group. The peroxide derivative exhibits potent anti-HCV activity by remarkably suppressing HCV-RNA replication.Type: ApplicationFiled: October 2, 2012Publication date: August 28, 2014Applicant: National University Corporation Okayama UniversityInventors: Nobuyuki Kato, Masanori Ikeda, Yusuke Wataya, Hye-Sook Kim, Hiroyuki Doi
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Patent number: 8815908Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: January 4, 2013Date of Patent: August 26, 2014Assignee: Ardelyx, Inc.Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
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Publication number: 20140235605Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment, particularly for reducing the risk of cardiovascular disease, especially coronary heart disease (such as myocardial infarction) and stroke. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents and kits for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents and kits for their detection.Type: ApplicationFiled: March 15, 2013Publication date: August 21, 2014Applicant: CELERA CORPORATIONInventor: CELERA CORPORATION
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Patent number: 8809382Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.Type: GrantFiled: May 4, 2010Date of Patent: August 19, 2014Assignees: The Royal Institution for the Advancement of Learning/McGill University, Florida Institute of TechnologyInventors: William S. Powell, Joshua Rokach
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Patent number: 8802716Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.Type: GrantFiled: June 25, 2013Date of Patent: August 12, 2014Assignee: TetraLogic Pharmaceuticals CorporationInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20140221452Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases.Type: ApplicationFiled: February 5, 2014Publication date: August 7, 2014Applicant: Amarin Pharmaceuticals Ireland LimitedInventor: Joseph S. Zakrzewski
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Publication number: 20140221431Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.Type: ApplicationFiled: June 26, 2012Publication date: August 7, 2014Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., LtdInventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
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Publication number: 20140213615Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.Type: ApplicationFiled: April 7, 2014Publication date: July 31, 2014Applicant: THE UNIVERSITY OF TOLEDOInventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
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Publication number: 20140213627Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.Type: ApplicationFiled: January 30, 2014Publication date: July 31, 2014Applicant: RAMOT AT TEL AVIV UNIVERSITY LTD.Inventors: Roni SCHERZER, Ehud GAZIT, Daniel SEGAL
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Publication number: 20140213586Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.Type: ApplicationFiled: September 26, 2012Publication date: July 31, 2014Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. Leuven R&DInventors: Dorothee Bardiot, Gunter Carlens, Kai Dallmeier, Suzanne Kaptein, Michael McNaughton, Arnaud Marchand, Johan Neyts, Wim Smets, Mohamed Koukni
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Publication number: 20140206757Abstract: This disclosure provides agents, compositions and methods of treating cancer by inhibiting histone lysine specific demethylase 1 (LSD1) and/or and a histone lysine specific demethylase 2 (LSD2). Agents and compositions comprise statins and/or inhibitors of LSD1/2.Type: ApplicationFiled: September 4, 2012Publication date: July 24, 2014Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Yujiang Geno Shi, Christine Guo Lian
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Publication number: 20140206741Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.Type: ApplicationFiled: April 12, 2012Publication date: July 24, 2014Applicant: Sichuan Guokang Pharmaceutical Co., LtdInventors: Luyun Zhang, Fang Yang, Wanqi Shi, Ping Zhang, Ying Li, Shufan Yin
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Patent number: 8785489Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: GrantFiled: October 13, 2009Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Publication number: 20140194388Abstract: A pharmaceutical composition comprising a CHK inhibitor, and an Hsp90 inhibitor according to the following formulae or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.Type: ApplicationFiled: May 25, 2012Publication date: July 10, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Publication number: 20140194423Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.Type: ApplicationFiled: March 4, 2014Publication date: July 10, 2014Inventors: Baltazar Gomez-Mancilla, Fabrizio Gasparini
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Publication number: 20140187600Abstract: The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction.Type: ApplicationFiled: March 7, 2014Publication date: July 3, 2014Inventors: Ralf GLATTHAR, Donald JOHNS, Daniel UMBRICHT
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Patent number: 8765802Abstract: Provided herein are Compounds having the following structure: wherein A, L, X and ring B are as defined herein, compositions comprising an effective amount of a Compound and methods for treating or preventing cancer, hypoxia, diabetes, stroke, autoimmune disease or a condition treatable or preventable by inhibition of Chk2, the ATM-Chk2 pathway or RSK2 comprising administering an effective amount of a Compound to a patient in need thereof.Type: GrantFiled: June 9, 2008Date of Patent: July 1, 2014Assignees: Provid Pharmaceuticals, Inc., United States of America as represented by the Department of Health and Human Resources NIHInventors: Robert Shoemaker, John Cardellina, Michael Currens, Sudhir Kondapaka, Yves Pommier, Andy Jobson, Dominic Scudiero, David Waugh, George Lountos, Guangtao Zhang, Andrew Colasanti, Christopher R. Self, Janet Cicariello Cook
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Publication number: 20140179750Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.Type: ApplicationFiled: June 19, 2012Publication date: June 26, 2014Applicant: EMORY UNIVERSITYInventors: Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
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Publication number: 20140179723Abstract: Statin compositions are disclosed for stimulating neurite growth from spiral ganglion neurons in the inner ear and methods for preventing damage to or treating damage of auditory neurons and/or hair cells of the cochlea following acoustic or toxic insult.Type: ApplicationFiled: December 13, 2013Publication date: June 26, 2014Inventors: Donna S. Whitlon, Claus-Peter Richter
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Publication number: 20140179735Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.Type: ApplicationFiled: April 25, 2012Publication date: June 26, 2014Inventors: Zhong-Yin Zhang, Yantao He, Li-Fan Zeng
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Publication number: 20140165223Abstract: Described are methods and compositions for inhibiting the trimerization of ligands belonging to the TNF superfamily, in particular, inhibiting RANKL trimerization. Accordingly, the methods and compositions provided herein can be used to treat disorders associated with increased RANK signaling, in particular those related to bone loss. Compounds that inhibit trimerization of ligands belonging to the TNF superfamily are also described.Type: ApplicationFiled: February 12, 2014Publication date: June 12, 2014Applicant: B.S.R.C. "Alexander Fleming"Inventors: Eleni Ntouni, Georgios Kollias