Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Patent number: 8993542Abstract: The present invention provides methods of treating human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, including administering a compound described in the invention in an amount effective treat the HIV and/or HBV infection and at least substantially inhibit the development of resistance to said antiviral compounds in the subject. Pharmaceutical compositions are also provided.Type: GrantFiled: January 23, 2009Date of Patent: March 31, 2015Assignee: Chimerix Inc.Inventors: Ernest Randall Lanier, Merrick R. Almond, George R. Painter
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Publication number: 20150086628Abstract: The present invention provides a pharmaceutical solid oral sprinkle composition comprising one or more antiretroviral drugs, and a method of manufacturing the same. The present invention is particularly useful for treatment of an HIV infection, AIDS related complex, or AIDS.Type: ApplicationFiled: May 3, 2013Publication date: March 26, 2015Inventors: Shrinivas Madhukar Purandare, Geena Malhotra
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Publication number: 20150087610Abstract: The present invention provides methods and compositions for modifying fertility in a male mammalian subject by contacting the subject's testis cells, germ cells or sperm with a sufficient amount of a composition comprising a ligand that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Also described are methods for screening a test molecule for its effect on fertility by examining changes in male germ cells, testis cells or sperm resulting from contact with a molecule that binds, activates, or inhibits activation of, a TAS2R receptor expressed on the cells. Compositions for modifying fertility in a mammalian subject, e.g., contraceptive products, include a ligand that binds, inhibits or activates a TAS2R receptor in a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 18, 2013Publication date: March 26, 2015Applicant: Monell Chemcial Senses CenterInventors: Liquan Huang, Jiang Xu
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150079154Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.Type: ApplicationFiled: July 9, 2012Publication date: March 19, 2015Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBHInventors: Lars Zender, Ramona Rudalska, Daniel Dauch
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Publication number: 20150080372Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.Type: ApplicationFiled: October 14, 2014Publication date: March 19, 2015Inventors: Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
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Publication number: 20150079036Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: Chung K. Chu
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Publication number: 20150080398Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
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Publication number: 20150080420Abstract: The present invention relates to a novel amorphous Form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it.Type: ApplicationFiled: June 30, 2014Publication date: March 19, 2015Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
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Publication number: 20150080393Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.Type: ApplicationFiled: September 5, 2014Publication date: March 19, 2015Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
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Publication number: 20150080370Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: March 17, 2014Publication date: March 19, 2015Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Patent number: 8980888Abstract: It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.Type: GrantFiled: September 4, 2014Date of Patent: March 17, 2015Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Muneyoshi Makabe, Kouki Ogawa
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Publication number: 20150072939Abstract: The present invention relates to the use of 5-HT2 receptor antagonists and in particular of 8-?-ergolines such as lisuride, terguride and the derivatives thereof as 5-HT2B and 5-HT2A receptor antagonists and antioxidants in preferably higher-dosed and preferably continuous use for the treatment, progression prophylaxis and general prophylaxis of organ fibroses and other pathological organ remodeling caused by mesenchymal proliferationType: ApplicationFiled: September 22, 2014Publication date: March 12, 2015Applicant: SINOXA PHARMA GMBHInventors: Reinhard HOROWSKI, Heinz PALLA, Johannes TACK
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Publication number: 20150073004Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.Type: ApplicationFiled: November 18, 2014Publication date: March 12, 2015Inventors: Imre BATA, Veronika BARTONE BODOR, Attila VASAS, Peter BUZDER-LANTOS, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Zsuzsanna SZAMOSVOLGYI
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Publication number: 20150072949Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice for treating pancreatic cancer.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Ilan ZIV, Hagit GRIMBERG
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Publication number: 20150073003Abstract: The present invention provides new ceramide analogs indicated as the compounds of formula (II). These novel analogs exhibit a significant anti cancerous effect and are therefore provided as a pharmaceutical composition for treating cell proliferative diseases, neurodegenerative disorders, metabolism-associated conditions, infectious diseases, and immune-related disorders. The invention further provides combined compositions and kits combining the novel ceramide analogs of formula (II) with an additional therapeutic agent.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Arie DAGAN, Shimon SLAVIN, Shimon GATT, Jeremy ZAHAVY
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Publication number: 20150064282Abstract: Use of Neul sialidase inhibitors for the treatment of cancer as a monotherapy or in combination with known chemotherapeutics. Preferably, Neul sialidase inhibitors are oseltamivir phosphate or 2-deoxy-2,3-dehydro-N-acetylneuraminic acid (DANA) or analogues thereof.Type: ApplicationFiled: November 4, 2011Publication date: March 5, 2015Inventors: Paul Zachary Josefowitz, Myron R. Szewczuk
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Publication number: 20150064234Abstract: It has been discovered that pharmacological inhibition of K+ channels (using the FDA-approved broad-spectrum K+ channel antagonist 4-AP) positively benefitted smn mutant phenotypes, a result that is consistent with the defective excitability of motor circuits by their interneuron or sensory neuron inputs being a critical consequence of SMN depletion. Based on these observations, certain embodiments of the invention are directed to methods of treatment of SMA by administering therapeutically effective amounts of one or more potassium channel antagonists, including 4-aminopyridine, 4-(dimethylamino)pyridine, 4-(methylamino)pyridine, and 4-(aminomethyl)pyridine. Other embodiments are directed to new pharmaceutical formulations comprising two or more potassium channel antagonists.Type: ApplicationFiled: March 26, 2013Publication date: March 5, 2015Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventor: Brian D. Mccabe
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Publication number: 20150065500Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: September 11, 2014Publication date: March 5, 2015Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou, Frederick van Goor
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Publication number: 20150064175Abstract: A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one, is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) with surprisingly superior efficacy and pharmacodynamic properties in vitro and in vivo. Also provided are pharmaceutical compositions including the compound and methods of use of the compound in treating cancer and tumors in vivo, as well as inhibiting glycolytic flux and PFKFB3 enzymatic activity in cells.Type: ApplicationFiled: March 14, 2013Publication date: March 5, 2015Inventors: Gilles H. Tapolsky, Pooran Chand
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Publication number: 20150065532Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
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Publication number: 20150065531Abstract: Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.Type: ApplicationFiled: August 15, 2012Publication date: March 5, 2015Inventors: James R. Connor, Sang Yong Lee, Thomas James Brown, Phillip Martin Cowley
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Publication number: 20150065505Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: March 29, 2013Publication date: March 5, 2015Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
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Publication number: 20150065516Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: October 29, 2014Publication date: March 5, 2015Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Halyan Wang
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Patent number: 8969365Abstract: There is disclosed a pyrimidinecarboxamide compound useful as a pharmaceutical agent, synthetic processes, and pharmaceutical compositions which include the pyrimidinecarboxamide compound. More specifically, there is disclosed a CXCR1/2 inhibitor useful for treating a variety of inflammatory and neoplastic disorders.Type: GrantFiled: August 2, 2013Date of Patent: March 3, 2015Assignee: Syntrix Biosystems, Inc.Inventors: Dean Y. Maeda, John A. Zebala, Aaron D. Schuler
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Publication number: 20150057262Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: October 30, 2014Publication date: February 26, 2015Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
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Publication number: 20150056164Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: April 24, 2014Publication date: February 26, 2015Applicant: AbbVie Inc.Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
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Publication number: 20150057300Abstract: The present disclosure provides substituted piperidines or pyrrolidines having Formula IA: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R6, A, X, m and n are defined as set forth in the specification. In certain embodiments, Compounds of the present disclosure are useful for treating pain. The present disclosure is also directed to the use of Compounds of the present disclosure to treat a disorder responsive to blockade of one or more sodium channels.Type: ApplicationFiled: August 26, 2014Publication date: February 26, 2015Inventors: Laykea Tafesse, Jae Hyun Park
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Patent number: 8962614Abstract: The invention includes compositions and methods of treatment of cancers susceptible to treatment with nucleotide analog chemotherapeutic agent, including cancers in which nucleotide analog resistant tumors have developed, including identifying a subject having cancer susceptible to treatment with a nucleotide analog chemotherapeutic agent and a mitotic disruptor/polo-like kinase (Plk) pathway inhibitor to a subject; and monitoring the subject for a reduction or stabilization of at least one sign or symptom of cancer.Type: GrantFiled: April 17, 2008Date of Patent: February 24, 2015Assignee: The Johns Hopkins UniversityInventors: Antonio Jimeno, Manuel Medina Hidalgo
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Patent number: 8962642Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: August 7, 2013Date of Patent: February 24, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
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Patent number: 8962646Abstract: The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:Type: GrantFiled: June 29, 2012Date of Patent: February 24, 2015Assignee: Alkermes, Inc.Inventors: Laura Cook Blumberg, Derrick Arnelle
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Patent number: 8962641Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: April 7, 2014Date of Patent: February 24, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Annekatrin Heimann, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
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Publication number: 20150050241Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.Type: ApplicationFiled: October 30, 2014Publication date: February 19, 2015Inventors: Fred VOLINSKY, Steven Daniel DONG
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Publication number: 20150051234Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelia A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.Type: ApplicationFiled: September 19, 2014Publication date: February 19, 2015Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Publication number: 20150051196Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: October 29, 2014Publication date: February 19, 2015Inventors: CARL R. ILLIG, SHELLEY K. BALLENTINE, JINSHENG CHEN, RENEE LOUISE DESJARLAIS, SANATH K. MEEGALLA, MARK WALL, KENNETH J. WILSON
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Publication number: 20150051209Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.Type: ApplicationFiled: August 5, 2014Publication date: February 19, 2015Applicant: NOVARTIS AGInventors: Mark Gary BOCK, Henrik MOEBITZ, Sunil Kumar PANIGRAHI, Ramulu PODDUTOORI, Susanta SAMAJDAR
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Publication number: 20150050239Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 19, 2015Applicants: Calitor Sciences, LLC, Sunshine Lake Pharma Co., Ltd.Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Publication number: 20150051233Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.Type: ApplicationFiled: July 18, 2014Publication date: February 19, 2015Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Sandeep K. Agarwal, Mesias Pedroza
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Patent number: 8957215Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Navidea Biopharmaceuticals, Inc.Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Publication number: 20150045375Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.Type: ApplicationFiled: October 24, 2014Publication date: February 12, 2015Inventors: Deirdre Mary Bernadette HICKEY, Robert John IFE, Colin Andrew LEACH, Ivan Leo PINTO, Stephen Allan SMITH, Steven James STANWAY
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Publication number: 20150045344Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Inventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, Sonja ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG, Jens SCHAMBERGER
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Publication number: 20150044239Abstract: The present invention relates to compositions and methods for diagnosing, preventing and treating intracranial aneurysm.Type: ApplicationFiled: March 30, 2012Publication date: February 12, 2015Applicant: YALE UNIVERSITYInventors: Richard Lifton, Murat Gunel
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Publication number: 20150045378Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.Type: ApplicationFiled: February 12, 2013Publication date: February 12, 2015Inventors: Seiji Miwatashi, Hideo Suzuki, Tomohiro Okawa, Yasufumi Miyamoto, Takeshi Yamasaki, Yuko Hitomi, Yasuhiro Hirata
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Publication number: 20150044184Abstract: Provided herein are, inter alia, methods and compositions for treating or preventing diseases using SIRT1 inhibitors. The methods provided herein are particularly useful for treating or preventing age-related hematological diseases as well as cancerous hematological diseases. Further provided herein are hematopoietic cells useful for treating or preventing hematological diseases.Type: ApplicationFiled: August 11, 2014Publication date: February 12, 2015Inventors: WenYong Chen, Zhiqiang Wang
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Publication number: 20150045289Abstract: The present invention relates to the method of pre-preparing pharmaceutical compositions for therapeutic uses, particularly pre-preparing medications for treating patients (e.g., cancer patients and the like) by intravenous infusion.Type: ApplicationFiled: July 14, 2014Publication date: February 12, 2015Inventors: MICHAEL L. WEST, Tracey J. BROWN
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Patent number: 8952028Abstract: Methods of treating or preventing chemoresistance or relapse growth of cancer cells are provided. Methods of treating or preventing resistance to tyrosine kinase based chemotherapeutic treatment in hematologic and solid tumors are provided. BCR-ABL drug resistance in chronic myelogenous leukemia (CML) and models for conducting further study on the same are presented. The methods comprise administering a therapeutically effective amount of one or more SIRT1 modulators to the cells or subject in need thereof. The methods may be administered in combination with, prior to or subsequent to chemotherapy or may be administered to counteract the effect of a spontaneous genetic mutation. Methods of using SIRT1 inhibitors to treat or prevent insulin and transferrin-induced resistance are also presented. A novel cell model to study mechanisms of acquired chemoresistance is also provided.Type: GrantFiled: February 5, 2008Date of Patent: February 10, 2015Assignee: City of HopeInventor: Wenyong Chen
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Publication number: 20150038446Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.Type: ApplicationFiled: August 1, 2014Publication date: February 5, 2015Inventors: Jayakrishna Ambati, Benjamin Fowler
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Publication number: 20150038522Abstract: To provide an anti-cancer agent sensitivity determination marker, which marker can determine whether or not the patient has a therapeutic response to the anti-cancer agent, and novel cancer therapeutic means employing the marker. The anti-cancer agent sensitivity determination marker, the anti-cancer agent including oxaliplatin or a salt thereof and fluorouracil or a salt thereof, contains one or more substances selected from among an amino-acid-metabolism-related substance, a nucleic-acid-metabolism-related substance, a substance in the pentose phosphate pathway, a substance in the glycolytic pathway, a substance in the TCA cycle, a polyamine-metabolism-related substance, 7,8-dihydrobiopterin, 6-phosphogluconic acid, butyric acid, triethanolamine, 1-methylnicotinamide, NADH, NAD+, and a substance involved in the metabolism of any of these substances.Type: ApplicationFiled: February 22, 2013Publication date: February 5, 2015Applicants: KEIO UNIVERSITY, KABUSHIKI KAISHA YAKULT HONSHAInventors: Yusuke Tanigawara, Akito Nishimuta, Junya Tsuzaki, Hiroyuki Takahashi
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Publication number: 20150037280Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: July 19, 2013Publication date: February 5, 2015Applicants: Sunshine Lake Pharma Co., Ltd., Calitor Sciences, LLCInventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
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Patent number: 8946242Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.Type: GrantFiled: January 23, 2014Date of Patent: February 3, 2015Assignee: University of Georgia Research Foundation, Inc.Inventor: Chung K. Chu