Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20140038954Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Applicant: AMGEN INC.Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Human
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Patent number: 8642602Abstract: The present invention relates to the discovery of an epigenetic relay pathway that controls hepatic stellate cell activation and the wound-healing response in fibrogenesis, including fibrogenesis of the injured liver. Methods of inhibiting fibrogenesis, including liver fibrogenesis and secondary disease states and conditions thereof, and in treating liver damage, including cirrhosis of the liver (which may be caused by viruses or chemicals, including alcohol), are aspects of the present invention. The methods utilize certain nucleoside compounds and/or antibodies which are optionally conjugated. Pharmaceutical compositions represent additional aspects of the invention.Type: GrantFiled: February 2, 2010Date of Patent: February 4, 2014Assignees: University of Georgia Research Foundation, Inc., University of Newcastle Upon TyneInventors: Jelena Mann, Chung K. Chu, Derek A. Mann
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Patent number: 8637493Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.Type: GrantFiled: November 10, 2010Date of Patent: January 28, 2014Assignee: University of MassachusettsInventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
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Patent number: 8637496Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.Type: GrantFiled: June 2, 2008Date of Patent: January 28, 2014Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
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Publication number: 20140023699Abstract: The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.Type: ApplicationFiled: July 25, 2013Publication date: January 23, 2014Inventors: James D. McChesney, Gilles H. Tapolsky, David Lloyd Emerson, John Marshall, Tauseef Ahmed, Allen Cohn, Michael Kurman, Manuel R. Modiano
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Patent number: 8633234Abstract: Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.Type: GrantFiled: September 24, 2007Date of Patent: January 21, 2014Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Maruti Ghagare
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Patent number: 8633212Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: GrantFiled: March 12, 2010Date of Patent: January 21, 2014Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbHInventors: Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian McKeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
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Publication number: 20140011798Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: January 24, 2013Publication date: January 9, 2014Applicant: NOVARTIS AGInventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Patent number: 8618150Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, and are defined herein.Type: GrantFiled: December 9, 2011Date of Patent: December 31, 2013Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, Mingde Xia, James J. McNally, Jay M. Matthews
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Publication number: 20130344063Abstract: The use of specific microRNAs (miRNAs) present in CSF as biomarkers for particular brain malignancies and disease activity.Type: ApplicationFiled: November 16, 2011Publication date: December 26, 2013Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Anna M. Krichevsky, Nadiya Teplyuk, Brit Mollenhauer, Santosh Kesari
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Publication number: 20130338104Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.Type: ApplicationFiled: May 24, 2013Publication date: December 19, 2013Applicant: Pharminox LimitedInventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
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Patent number: 8609862Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 13, 2011Date of Patent: December 17, 2013Assignee: Novartis AGInventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
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Publication number: 20130331422Abstract: The present invention provides for a method of treating a disease such as cancer, comprising the step of administering to a patient a therapeutically effective amount of an isomer or analog of monoterpene or sesquiterpene (or its derivative), such as an isoperillyl alcohol. The present invention also provides for a method of treating a disease comprising the step of administering to a patient a therapeutically effective amount of a derivative of an isomer or analog of monoterpene or sesquiterpene, such as an isoperillyl alcohol carbamate. The derivative may be an isoperillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The route of administration may vary, including inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: ApplicationFiled: December 16, 2011Publication date: December 12, 2013Applicant: NEONC Technologies Inc.Inventors: Thomas Chen, Daniel Levin, Satish Puppali, Daniel Anthony Dickman
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Publication number: 20130331384Abstract: The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: The Regents of the University of CaliforniaInventors: Richard L. Gallo, Teruaki Nakatsuji
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Patent number: 8604045Abstract: The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF, and to a method of treating non-cancerous, benign brain tumors, especially for the curative and/or prophylactic treatment of NF.Type: GrantFiled: December 5, 2012Date of Patent: December 10, 2013Assignee: Novartis AGInventor: Paul W. Manley
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Publication number: 20130296311Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: May 26, 2011Publication date: November 7, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20130296355Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20130295198Abstract: Methods for selecting chemotherapeutic agents for treating a cancer are provided that include the steps of providing a cancer cell sample having a population of bulk cancer cells and a population of cancer stem-like cells, culturing a first portion of the cancer cell sample in a hydrodynamic focusing bioreactor under microgravity conditions and for a period of time to selectively enhance the population of cancer stem-like cells and selectively kill the population of bulk cancer cells, contacting the cancer stem-like cells with one or more chemotherapeutic agents, and then selecting the one or more chemotherapeutic agents for treating the cancer if there is an increase in an amount of cytotoxicity. Methods for treating a cancer are also provided in which the identified chemotherapeutic agents are administered to a subject. Further provided are methods for identifying a test compound useful for treating a cancer.Type: ApplicationFiled: March 19, 2013Publication date: November 7, 2013Applicant: Marshall University Research CorporationInventor: Marshall University Research Corporation
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Publication number: 20130296390Abstract: The present invention relates to oral nutritional and therapeutic products which are useful for enhancing the safety of administering and reducing the adverse effects caused by magnesium alpha-lipoate to a warm-blooded mammal, comprising administering magnesium alpha-lipoate with D-biotin.Type: ApplicationFiled: April 30, 2013Publication date: November 7, 2013Applicant: BioLink Life Sciences, Inc.Inventor: Deanna J. Nelson
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Patent number: 8575140Abstract: A decongestant composition is provided comprising: (a) a safe and effective amount of an adrenergic compound; (b) a safe and effective amount of a steroid; and (c) a pharmaceutically-acceptable carrier. Methods of treating congestion in a human or animal subject are also provided comprising administering to the subject a composition comprising: (a) an adrenergic compound; and (b) a steroid; where the daily dose of the adrenergic compound administered to the subject is from about 1 ?g to about 800 ?g, and the daily dose of the steroid administered to the subject is from about 1 ?g to about 400 ?g.Type: GrantFiled: March 7, 2011Date of Patent: November 5, 2013Inventor: Richard A. Wandzel
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Publication number: 20130287789Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.Type: ApplicationFiled: June 26, 2013Publication date: October 31, 2013Applicant: Novartis AGInventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
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Patent number: 8569312Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: April 4, 2013Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Publication number: 20130274256Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.Type: ApplicationFiled: October 11, 2012Publication date: October 17, 2013Applicant: SEQUOIA SCIENCES, INC.Inventor: Sequoia Sciences, Inc.
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Patent number: 8557838Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: October 24, 2011Date of Patent: October 15, 2013Assignee: Medicis Pharmaceutical CorporationInventors: Alexis S. Statham, Robert J. Nelson
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Publication number: 20130267501Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: January 22, 2013Publication date: October 10, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventor: The Board of Trustees of the Leland Stanford Junior University
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Patent number: 8552044Abstract: The present invention relates to coatings for disease control. More particularly, the present invention relates to coatings that are effective against toxins, precursors to these coatings and methods of forming the coatings.Type: GrantFiled: August 19, 2009Date of Patent: October 8, 2013Assignee: The United States of America as represented by the Secretary of the Air ForceInventor: Jeffery R. Owens
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Patent number: 8552045Abstract: This invention is directed to compounds with the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula 1. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula 1. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula 1.Type: GrantFiled: November 18, 2011Date of Patent: October 8, 2013Assignee: H. Lundbeck A/SInventors: Jan Kehler, Jacob Nielsen, Mauro Marigo, John Paul Kilburn, Morten Langgård
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Patent number: 8546440Abstract: The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: December 16, 2009Date of Patent: October 1, 2013Assignee: Janssen Pharmaceuticals, Inc.Inventors: Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
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Patent number: 8524756Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.Type: GrantFiled: October 16, 2012Date of Patent: September 3, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Jun Jiang, Hao Li, David A. James, Dinesh Chimmanamada, Christopher Borella, Lijun Sun, Yu Xie, Mats Holmqvist, Jerome Mahiou, Zhiqiang Xia
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Publication number: 20130224312Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.Type: ApplicationFiled: November 16, 2012Publication date: August 29, 2013Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCHInventor: Mayo Foundation for Medical Education and Research
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Patent number: 8519149Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: GrantFiled: October 28, 2011Date of Patent: August 27, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
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Publication number: 20130209483Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.Type: ApplicationFiled: November 30, 2012Publication date: August 15, 2013Applicant: SUTTER WEST BAY HOSPITALSInventor: SUTTER WEST BAY HOSPITALS
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Publication number: 20130210877Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: ApplicationFiled: August 26, 2011Publication date: August 15, 2013Applicant: NEONC TECHNOLOGIES INC.Inventors: Thomas Chen, Daniel Levin, Satish Puppali
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Publication number: 20130209460Abstract: The invention encompasses methods and kits used in the identification of invasive glioblastoma based upon the expression of TROY. The methods and kits also allow prediction of disease outcome as well as therapeutic outcome.Type: ApplicationFiled: March 18, 2013Publication date: August 15, 2013Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE
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Publication number: 20130203828Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: ApplicationFiled: August 3, 2012Publication date: August 8, 2013Applicant: NEO ONCOLOGY INC.Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Publication number: 20130190290Abstract: The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: January 23, 2013Publication date: July 25, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GmbH
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Patent number: 8492405Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: GrantFiled: October 17, 2007Date of Patent: July 23, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Yasufumi Miyamoto
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Patent number: 8492374Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: GrantFiled: April 28, 2010Date of Patent: July 23, 2013Assignee: Industrial Technology Research InstituteInventors: On Lee, Chih-Hung Chen, Chi-Y Hung, Yow-Lone Chang, Ting-Shou Chen
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Publication number: 20130184240Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.Type: ApplicationFiled: September 8, 2011Publication date: July 18, 2013Applicant: Shionogi & Co., Ltd.Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
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Publication number: 20130183269Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: January 7, 2013Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130183277Abstract: Provided are compositions and methods for increasing patient CD4+ cell count while undergoing treatment for immune-mediated disease, cancer, heart disease, neurodegenerative disease, or infectious disease by administering to the patient a nutrient composition including, inter alia, alpha lipoic acid, acetyl L-carnitine, and N-acetyl-cysteine.Type: ApplicationFiled: December 19, 2012Publication date: July 18, 2013Inventor: Jon D. Kaiser
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Publication number: 20130177632Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.Type: ApplicationFiled: February 27, 2013Publication date: July 11, 2013Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
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Patent number: 8481750Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: May 28, 2010Date of Patent: July 9, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jennifer A. Kowalski, Matt Aaron Tschantz
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Publication number: 20130164218Abstract: This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: EMORY UNIVERSITYInventor: EMORY UNIVERSITY
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Publication number: 20130165454Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: October 18, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: HYDRA BIOSCIENCES, INC.
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Publication number: 20130156853Abstract: A liquid composition of an insoluble medicament and a preparation method thereof are disclosed. The composition includes insoluble medicament, oil for injection, phospholipid, and solvent; the percentage by weight of each component is as follows: insoluble medicament 0.01-10%, oil for injection 0%-20%, phospholipid 10-80%, solvent 20-89%. The preparation method for the composition includes the following steps: dissolving an insoluble medicament into solvent or oil for injection or a mixture thereof firstly, and then adding other components, and mixing uniformly; or dissolving an insoluble medicament into a mixture of other components, and mixing uniformly; or dissolving an insoluble medicament into part of solvent firstly, and then adding into a mixed solvent of other components and the remaining solvent, and mixing uniformly.Type: ApplicationFiled: August 31, 2011Publication date: June 20, 2013Applicant: PEKING UNIVERSITYInventors: Qiang Zhang, Wenbing Dai, Jiancheng Wang, Xuan Zhang
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Patent number: 8461192Abstract: PKCiota inhibitor 1H-imidazole-4-carboxamide, 5-amino-1-[2,3-dihydroxy-4-[(phosphonooxy)methyl]cyclopentyl]-,[1R-(1?,2?,3?,4?)], (ICA-1), targets a unique sequence (amino acid residues 469-475) in the catalytic domain of PKCiota and inhibits PKCiota activity. The data shows suprising and unexpected ability of ICA-1 to selectively inhibit the proliferation of cells that overexpress PKCiota.Type: GrantFiled: September 15, 2008Date of Patent: June 11, 2013Assignees: The University of South Florida, The United States of America Department of Veterans Affairs, The University of Florida Research Foundation, Inc.Inventors: Mildred Acevedo-Duncan, Shraddha R. Desai, Hla Yee Win, David A. Ostrov, Prajit P. Pillai, Diondra D. Hill
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Publication number: 20130142887Abstract: The present invention provides methods for treating cancer comprising inhibiting the activity of p300/CBP histone acetyltransferase (HAT). Also provided are p300/CBP HAT inhibitors for treating a subject having cancer. In addition, the present invention includes biomarkers for p300/CBP HAT inhibition, which are used to i) monitor the effectiveness of cancer therapy, and ii) identify anti-cancer agents for use in combination therapy.Type: ApplicationFiled: July 14, 2011Publication date: June 6, 2013Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Rhoda Myra Alani, Philip A. Cole, Gai Yan, Erin M. Bowers
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Publication number: 20130129841Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase II inhibitor, an antimitotic agent and radiation wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.Type: ApplicationFiled: July 25, 2011Publication date: May 23, 2013Applicant: NERVIANO MEDICAL SCIENCES S.r.l.Inventors: Antonella Ciavolella, Alessia Montagnoli, Enrico Pesenti