Chalcogen And Acyclic Nitrogen Bonded Directly To The Same Carbon Patents (Class 514/346)
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Publication number: 20140179700Abstract: Methods of alleviating the symptoms of hemoglobinopathies, including, but not limited to, sickle cell disease, ?-thalassemia, and hemoglobin H disease are provided. In some embodiments, the methods comprise administering an inhibitor selected from an ERK inhibitor, a MEK inhibitor, and a Raf inhibitor. Methods of inhibiting adhesion of sickle red blood cells to endothelial cells are also provided.Type: ApplicationFiled: April 30, 2012Publication date: June 26, 2014Applicant: Duke UniveristyInventor: Rahima Zennadi
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Patent number: 8747837Abstract: Embodiments of the invention are directed methods that include a thymidine kinase deficient vaccinia virus. The methods include evaluating a tumor for reperfusion after treatment with vaccinia virus and administering an anti-angiogenic agent if reperfusion is detected.Type: GrantFiled: September 14, 2010Date of Patent: June 10, 2014Assignee: Jennerex, Inc.Inventors: David Kirn, Caroline Breitbach
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Publication number: 20140148468Abstract: The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.Type: ApplicationFiled: November 27, 2013Publication date: May 29, 2014Applicant: GRÜNENTHAL GMBHInventors: Simon LUCAS, Sven Kühnert, Gregor Bahrenberg, Wolfgang Schröder
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Publication number: 20140127157Abstract: Antiviral activity of Nilotinib against Hepatitis C virus.Type: ApplicationFiled: November 4, 2013Publication date: May 8, 2014Inventors: Erica Canino, Adam Feire, Christopher Jones, Paul W. Manley
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Publication number: 20140113913Abstract: Some embodiments are based on the discovery that proliferative diseases (e.g., neoplastic diseases, for example, tumors or cancers) having an FBW7 mutation or other FBW7 deficiency are sensitive to Mcl1 inhibiting agents, but resistant to pro-apoptotic drugs that do not inhibit Mcl1. Some embodiments provide methods of treating a proliferative disease based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of classifying a hyperproliferative cell or cell population, for example, a malignant cell or cell population based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of selecting a treatment regimen for treating a proliferative disease, for example, a malignant disorder, based on an assessment of FBW7 expression level or mutation status.Type: ApplicationFiled: March 2, 2012Publication date: April 24, 2014Applicant: Beth Israel Deaconess Medical Center, Inc.Inventor: Wenyi Wei
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Publication number: 20140113898Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.Type: ApplicationFiled: November 4, 2011Publication date: April 24, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
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SYNERGISTIC PHARMACEUTICAL COMBINATION FOR THE TREATMENT OF SQUAMOUS CELL CARCINOMA OF HEAD AND NECK
Publication number: 20140112918Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.Type: ApplicationFiled: May 30, 2012Publication date: April 24, 2014Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy -
Patent number: 8703801Abstract: New chiral and achiral oxy-substituted cyclopentyl pyridinone diketocarboxamides and their derivatives and methods for their preparations are disclosed. The compounds include tautomers, regioisomers and geometric isomers. These complex carboxamides are designed as inhibitors of HIV replication through inhibition of HIV integrase. The compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.Type: GrantFiled: December 7, 2010Date of Patent: April 22, 2014Assignee: University of Georgia Research Foundation, Inc.Inventors: Vasu Nair, Maurice O. Okello, Abdumalik A. Nishonov, Sanjaykumar Mishra
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Publication number: 20140088157Abstract: Provided are an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient, and a method for controlling endoparasites, comprising orally or parenterally administering the endoparasite control agent.Type: ApplicationFiled: March 1, 2012Publication date: March 27, 2014Applicants: NIHON NOHYAKU CO., LTD., THE UNIVERSITY OF TOKYOInventors: Kiyoshi Kita, Akiyuki Suwa
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Publication number: 20140088156Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: ApplicationFiled: February 14, 2012Publication date: March 27, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Publication number: 20140073574Abstract: 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 endothelin 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: November 13, 2013Publication date: March 13, 2014Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
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Publication number: 20140051727Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 8, 2011Publication date: February 20, 2014Applicant: Lycera CorporationInventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
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Publication number: 20140044757Abstract: The present invention features methods for stimulating clearance of amyloid beta in microglia, decreasing cognitive decline associated with amyloid pathology, and treating Alzheimer's disease by selectively inhibiting the expression or activity of Acyl-CoA:Cholesterol Acyltransferase 1, but not Acyl-CoA:Cholesterol Acyltransferase 2.Type: ApplicationFiled: September 11, 2013Publication date: February 13, 2014Applicant: Trustees of Dartmouth CollegeInventors: Ta-Yuan Chang, Catherine C.Y. Chang, Yohei Shibuya, Elena Bryleva, Stephanie Murphy, Maximillian A. Rogers
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Publication number: 20140045899Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: October 24, 2013Publication date: February 13, 2014Applicant: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Publication number: 20140045903Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: July 30, 2013Publication date: February 13, 2014Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20140031376Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: October 3, 2013Publication date: January 30, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Shigeyuki ITOH, Atsushi IWATA
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Publication number: 20140011822Abstract: This document provides methods and materials for reducing venous stenosis formation of an arteriovenous fistula or graft. For example, methods and materials for using VEGF inhibitors to reduce venous stenosis formation of arteriovenous fistulas or grafts are provided.Type: ApplicationFiled: March 16, 2012Publication date: January 9, 2014Inventor: Sanjay Misra
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Patent number: 8618141Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.Type: GrantFiled: July 18, 2012Date of Patent: December 31, 2013Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
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Patent number: 8609854Abstract: The present invention provides a process for the preparation of sorafenib tosylate, comprising contacting sorafenib free base with p-toluenesulphonic acid in water.Type: GrantFiled: September 24, 2010Date of Patent: December 17, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
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Publication number: 20130317020Abstract: 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: ApplicationFiled: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20130310347Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.Type: ApplicationFiled: May 21, 2013Publication date: November 21, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
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Publication number: 20130303461Abstract: The technology described herein is directed to methods of determining oligonucleotide sequences, e.g. by enriching target sequences prior to sequencing the sequences.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Anthony John Iafrate, Long Phi Le, Zongli Zheng
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Publication number: 20130261082Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-I or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-I in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-I and another therapeutic agent.Type: ApplicationFiled: March 6, 2013Publication date: October 3, 2013Applicant: ZIOPHARM ONCOLOGY, INC.Inventors: Barbara WALLNER, Philip B. KOMARNITSKY
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Publication number: 20130251702Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: SNU R&DB FOUNDATIONInventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
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Publication number: 20130252957Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.Type: ApplicationFiled: December 28, 2012Publication date: September 26, 2013Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Ying-Zi Xu, Shendong Yuan, David Wone, Andrei Konradi
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Patent number: 8541402Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: May 3, 2012Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Publication number: 20130245037Abstract: The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided.Type: ApplicationFiled: May 17, 2013Publication date: September 19, 2013Applicant: FibroGen, Inc.Inventors: Volkmar Guenzler-Pukall, Thomas B. Neff, Qingjian Wang, Michael P. Arend, Lee A. Flippin, Alex Melekhov
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Publication number: 20130237546Abstract: The present invention provides a method for determining a response of a mammalian subject having melanoma tumor cells to treatment with a melanoma inhibitory agent. In one aspect, the method comprises (a) determining a first concentration of melanoma inhibitory activity protein (MIA) in a first biological sample taken from the mammalian subject before treatment with the melanoma inhibitory agent; (b) determining a second concentration of MIA in a second biological sample from the mammalian subject taken after treatment with the melanoma, inhibitory agent; and (c) comparing the first and second concentrations of MIA, wherein a decrease in the second concentration of MIA measured in the second biological sample as compared to the first concentration of MIA measured in the first biological sample indicates a positive response to the treatment with the melanoma inhibitory agent.Type: ApplicationFiled: October 4, 2012Publication date: September 12, 2013Applicant: Novartis AGInventors: Nguyen Tan, Eleni Venetsanakos, Michel Faure, Carla Heise
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Publication number: 20130230542Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicants: CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER, UNIVERSITY OF CINCINNATIInventors: Edward J. Merino, James C. Mulloy, Guorui Li, Tiffany Bell-Horwath
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130225605Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 22, 2013Publication date: August 29, 2013Applicant: SANOFIInventor: SANOFI -
Publication number: 20130225641Abstract: Two new compounds with anticancer effects of N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridyloxy)phenyl]-thiourea and N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridylthio)phenyl]-thiourea, and salts thereof are disclosed. Preparation methods of the two new compounds and pharmaceutical compositions containing the new compounds are further disclosed. Experimental studies show that the two new compounds can effectively inhibit the activity of Raf and VEGFR protein kinase, widely inhibit growth of various types of human tumor cell lines and further induce apoptosis of tumor cells. Human tumor heterograft model investigation proves that the two new compounds are effective antineoplastic agents, and can sharply inhibit growth of human liver cancer cells, lung cancer cells and intestinal cancer cells in vivo. Furthermore, the anticancer effects of the compounds are much better than that of Sorafenib.Type: ApplicationFiled: August 30, 2010Publication date: August 29, 2013Inventors: Banghe Pharmaceutical Co., Ltd., Nan Zhang, Rong Zhong, Suzhou Maidixian Pharmaceutical Inc.,
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Publication number: 20130225487Abstract: Compounds of Formula (A) and (B) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).Type: ApplicationFiled: March 12, 2013Publication date: August 29, 2013Applicant: Pfizer Inc.Inventor: Pfizer Inc.
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Publication number: 20130225642Abstract: The present invention provides a prophylactic or therapeutic agent for amyotrophic lateral sclerosis, containing a 1,3-diphenylurea derivative or multikinase inhibitor.Type: ApplicationFiled: September 2, 2011Publication date: August 29, 2013Applicant: KYOTO UNIVERSITYInventor: Ayako Asai
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Publication number: 20130217660Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: ApplicationFiled: May 12, 2011Publication date: August 22, 2013Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
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Publication number: 20130216531Abstract: Inhibition of CXCR4 can inhibit tumor growth and metastasis during certain therapeutic windows. Disclosed are novel methods for treating and preventing cancer in a subject related to administration of CXCR4 inhibitors during a therapeutic window following treatment with another anti-tumor therapy.Type: ApplicationFiled: June 28, 2011Publication date: August 22, 2013Inventors: Rakesh K. Jain, Dan G. Duda, Sergey V. Kozin, Dai Fukumura
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Publication number: 20130210865Abstract: The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N2-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib.Type: ApplicationFiled: January 28, 2011Publication date: August 15, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad, Sachin Deorao Zade, Ajay Shankar Sinch
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Publication number: 20130202573Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: August 8, 2013Applicant: Ardea Biosciences, Inc.Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
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Publication number: 20130202587Abstract: The present disclosure provides a method for identifying whether a subject is more or less likely to be responsive to VEGF-based therapy, comprising screening a nucleic acid sample obtained from the subject to provide output information which identifies the presence or absence of an allelic variant, wherein the presence or absence of an allelic variant indicates whether the subject is more or less likely to be responsive to VEGF-based therapy.Type: ApplicationFiled: August 24, 2012Publication date: August 8, 2013Applicant: Randox Laboratories Ltd.Inventor: John Lamont
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Publication number: 20130195988Abstract: A vascular embolization gelling agent for sustained release of drugs for treating tumors having a drug and a drug carrier. The drugs are antitumor drugs. The drug carrier includes poloxamer polymer and polyvinylpyrrolidone or gel made of the combination, and may be purified before use. The drug carrier accounts for 5-65% of the gel. The particle size of the gel is in the range of 10 nm-150 ?m. The embolization agent is a liquid gel at normal temperature, to facilitate direct transcatheter injection, and is rapidly solidified to the gel state in body with the increase of the temperature; it is used to encapsulate different drugs on demand, and can achieve dual efficacy of embolization and drug treatment through local sustained release of the drug. The present invention can be used as the embolization agent for endovascular interventional therapy for transcatheter arterial chemoembolization of various benign and malignant tumors.Type: ApplicationFiled: March 8, 2013Publication date: August 1, 2013Applicant: Shanghai Cancer InstituteInventor: Shanghai Cancer Institute
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Publication number: 20130190325Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X.Type: ApplicationFiled: June 21, 2011Publication date: July 25, 2013Applicant: ITEK VENTURES PTY LTDInventors: Shudong Wang, Osama Chahrour, Tiangong Lu, Anran Hu
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Publication number: 20130184227Abstract: 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: November 30, 2009Publication date: July 18, 2013Inventors: Oliver Yoa-Pu HU, Hong-Jaan Wang, Cheng-Huei Hsiong, Li-Heng Pao
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Publication number: 20130183297Abstract: The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130178424Abstract: 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 endothelin 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: February 13, 2013Publication date: July 11, 2013Applicant: AbbVie Deutschland GmbH & Co. KGInventor: AbbVie Deutschland GmbH & Co. KG
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Patent number: 8476269Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Publication number: 20130150367Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: September 12, 2012Publication date: June 13, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20130150372Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: February 15, 2013Publication date: June 13, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130136794Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.Type: ApplicationFiled: April 21, 2011Publication date: May 30, 2013Applicant: PEKING UNIVERSITYInventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
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Publication number: 20130121919Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.Type: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
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Publication number: 20130116274Abstract: Disclosed is a method of treating melanoma in a mammal comprising administering (a) a therapeutically effective amount of an inhibitor of metabotropic glutamate receptor 1 (GRM1); and (b) a therapeutically effective amount of an inhibitor of at least one downstream signaling target of GRM1. Also disclosed are compositions and kits for treating melanoma comprising (a) a therapeutically effective amount of an inhibitor of GRM1; and (b) a therapeutically effective amount of an inhibitor of at least one downstream signaling target of GRM1.Type: ApplicationFiled: November 9, 2012Publication date: May 9, 2013Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventor: Rutgers, The State University of New Jersey
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Publication number: 20130116286Abstract: The present invention is directed to methods of treating neurally mediated hypotension. In particular, the invention provides pharmaceutical compositions comprising droxidopa alone, or in combination with one or more further active ingredients, that can be administered to a patient for the treatment of neurally mediated hypotension.Type: ApplicationFiled: October 4, 2012Publication date: May 9, 2013Applicant: Chelsea Therapeutics, Inc.Inventor: Chelsea Therapeutics, Inc.