Chalcogen In The Six-membered Hetero Ring Patents (Class 514/90)
  • Patent number: 8003624
    Abstract: In its many embodiments, the present invention provides a novel class of indolines as inhibitors 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: Grant
    Filed: February 13, 2007
    Date of Patent: August 23, 2011
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    Inventors: Kevin D. McCormick, Christopher W. Boyce, Younong Yu
  • Publication number: 20110195066
    Abstract: The present invention relates to new quinoline inhibitors of tyrosine kinases, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 3, 2011
    Publication date: August 11, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Chengzhi Zhang
  • Publication number: 20110195094
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 13, 2008
    Publication date: August 11, 2011
    Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk Przewloka, Hao Li
  • Publication number: 20110189125
    Abstract: Compositions and methods for modulating HSP70 function, particularly for the targeted killing of cancer cells, are disclosed.
    Type: Application
    Filed: March 18, 2011
    Publication date: August 4, 2011
    Applicants: Trustees of the University of Pennsylvania, Fox Chase Cancer Center
    Inventors: Donna L. George, Julia I-Ju Leu, Maureen Murphy
  • Publication number: 20110189175
    Abstract: Provided herein are methods for identifying a subject afflicted with chronic lymphocytic leukemia who is responsive to treatment with a chemotherapeutic agent by detecting the presence or absence of at least one APOE4 allele in the subject, the presence of an APOE4 allele identifying the subject as responsive to the treatment. Also provided are methods of treating a subject afflicted with chronic lymphocytic leukemia, including administering an estrogenic agent, an androgen withdrawal agent, an apoE4 peptide or mimetic thereof, and/or a chemotherapeutic agent in an amount effective to treat said chronic lymphocytic leukemia. Methods of determining a prognosis for a patient diagnosed with chronic lymphocytic leukemia are also provided. In addition, methods for stratifying a subject into a subgroup of a clinical trial and methods for identifying a patient in a clinical trial of a treatment for chronic lymphocytic leukemia are herein provided.
    Type: Application
    Filed: January 20, 2011
    Publication date: August 4, 2011
    Inventors: J. Brice Weinberg, Warren J. Strittmatter
  • Publication number: 20110171289
    Abstract: The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
    Type: Application
    Filed: November 9, 2010
    Publication date: July 14, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Martin Friedrich STEFANIC, Frank HILBERG, Gerd MUNZERT, Flavio SOLCA, Anke BAUM, Jacobus C.A. van MEEL
  • Publication number: 20110158983
    Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.
    Type: Application
    Filed: March 5, 2009
    Publication date: June 30, 2011
    Inventors: Newell Bascomb, John Maki, Fredric S. Young
  • Publication number: 20110150831
    Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.
    Type: Application
    Filed: November 24, 2010
    Publication date: June 23, 2011
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Tilmann SCHUSTER, Matthias GERLACH, Irene SEIPELT, Emmanuel POLYMEROPOULOS, Gilbert MUELLER, Eckhard GUENTHER, Pascal MARCHAND, Julien DEFAUX
  • Publication number: 20110142794
    Abstract: A method for determining a therapeutically effective amount of suramin for administering to a patient, who is to receive a cytotoxic agent, which comprises the steps of determining the circulating suramin concentration in the patient; administering suramin, if required, to establish a low circulating concentration of suramin in the patient of below about 200 ?M; and administering the chemotherapeutic agent to the patient when the low circulating concentration of suramin is present in the patient. Conveniently a nomogram can be constructed for use in clinical settings with the suramin.
    Type: Application
    Filed: February 21, 2011
    Publication date: June 16, 2011
    Inventors: Jessie L.-S. Au, M. Guillaume Wientjes
  • Publication number: 20110142956
    Abstract: The invention relates to the use of PDE5 inhibitors for treating and/or preventing hypopigmentary disorders.
    Type: Application
    Filed: February 22, 2011
    Publication date: June 16, 2011
    Inventor: Heidemarie PEUKER
  • Publication number: 20110135594
    Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
    Type: Application
    Filed: July 14, 2009
    Publication date: June 9, 2011
    Inventors: Michael Graupe, Chandrasekar Venkataramani
  • Publication number: 20110136764
    Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
    Type: Application
    Filed: June 1, 2010
    Publication date: June 9, 2011
    Applicant: OSI Pharmaceuticals, Inc.
    Inventors: Rama Devi APPARI, Xin CHEN, Ramesh Chllukuri, Andrew P. CREW, Hanqing DONG, Caterina FERRARO, Kenneth FOREMAN, Ramesh C. GUPTA, An-Hu LI, Dan SHERMAN, Kathryn M. STOLZ, Brian VOLK, Robert ZAHLER
  • Publication number: 20110129463
    Abstract: Provided are quinazolin-4(3A)-one derivatives, which are inhibitors of the ubiquitin ligase activity of a human polypeptide, particularly to POSH inhibitors, and to compositions and methods for the treatment RING E3 ubiquitin ligase related diseases.
    Type: Application
    Filed: November 26, 2010
    Publication date: June 2, 2011
    Applicant: Proteologics, Ltd.
    Inventors: Omri EREZ, Philippe NAKACHE
  • Publication number: 20110130366
    Abstract: The present invention generally relates to a process for the preparation of fosaprepitant dimeglumine intermediate and its use in the preparation of fosaprepitant dimeglumine; to a neutral form of fosaprepitant in a solid state and processes for the preparation thereof; and to a stable amorphous fosaprepitant dimeglumine, having a stability at temperatures of about 2° C. to about 8° C. and at a relative humidity below at least 60%; and a process for the preparation thereof.
    Type: Application
    Filed: July 17, 2009
    Publication date: June 2, 2011
    Applicant: GLENMARK GENERICS LMITED
    Inventors: Navin Ganesh Bhatt, Nikhil Rasiklal Trivedi, Mahesh Khedekar, Sukumar Sinha, Mubeen Ahmed Khan, Ramjilal Yadav
  • Publication number: 20110123644
    Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, and HDAC mediated disorders.
    Type: Application
    Filed: April 10, 2009
    Publication date: May 26, 2011
    Applicant: University of Florida Research Foundation
    Inventor: Hendrik Luesch
  • Publication number: 20110123516
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Application
    Filed: July 28, 2009
    Publication date: May 26, 2011
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
  • Publication number: 20110117084
    Abstract: This invention relates to novel quinazoline derivatives and their acceptable acid addition salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibitory activity against the VEGF receptor tyrosine kinase.
    Type: Application
    Filed: January 22, 2009
    Publication date: May 19, 2011
    Applicant: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Publication number: 20110111058
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Application
    Filed: November 5, 2010
    Publication date: May 12, 2011
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Publication number: 20110104249
    Abstract: The subject invention concerns materials and methods for treating oncological disorders in a person or animal using any agent or compound that inhibits uptake of glucose into a cell. The subject invention also concerns methods for inducing apoptosis and inhibiting the proliferation or survival of a cell. In one embodiment, the methods comprise administering an effective amount of an agent or compound that inhibits the activity of one or more glucose transporter proteins, such as Glut-1. An antibody that binds to and inhibits a glucose transporter protein can be used in the present methods.
    Type: Application
    Filed: August 15, 2008
    Publication date: May 5, 2011
    Applicant: University of South Florida
    Inventor: George R. Simon
  • Publication number: 20110104305
    Abstract: Methods for therapy of cystic fibrosis and other conditions such as cancer are provided. The methods comprise one or more agents capable of increasing thiol-containing compound transport via a transporter system (i.e. ABC transporters such as MDR-1 or MRP-2) in cells. Other embodiments include the use of agents to modulate transport of thiol-containing compounds within the cell. Therapeutic methods involve the administration of such agents to a patient afflicted with cystic fibrosis, cancer and/or another condition responsive to stimulation of thiol-containing compound transport.
    Type: Application
    Filed: June 30, 2010
    Publication date: May 5, 2011
    Inventors: Brian J. DAY, Remy KACHADOURIAN
  • Publication number: 20110098237
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: February 23, 2009
    Publication date: April 28, 2011
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan, Sergi Gulnik, John W. Erickson
  • Publication number: 20110097320
    Abstract: This invention relates to novel 4-aminoquinazolines, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2.
    Type: Application
    Filed: September 2, 2010
    Publication date: April 28, 2011
    Applicant: CoNCERT Pharmaceuticals Inc.
    Inventor: Roger TUNG
  • Publication number: 20110098236
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: February 23, 2009
    Publication date: April 28, 2011
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan
  • Publication number: 20110098251
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Application
    Filed: October 26, 2010
    Publication date: April 28, 2011
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Publication number: 20110097426
    Abstract: The present invention provides methods of treating subjects with an oxazaphosphorines, methods of identifying subjects that are suitable for oxazaphosphorine treatment, and systems for ensuring the safety and efficacy of a treatment that includes oxazaphosphorine administration.
    Type: Application
    Filed: May 21, 2010
    Publication date: April 28, 2011
    Applicant: Accentia Biopharmaceuticals, Inc.
    Inventors: FRANCIS O'DONNELL, JR., Carlos Santos
  • Publication number: 20110092462
    Abstract: This disclosure relates, at least in part, to methods of eliminating adverse immune reactions in a subject in need thereof including those associated with autoimmune diseases, allergic reactions and transplant rejection, including administration of a lymphocytotoxic non-myeloablative amount of a oxazaphosphorine drug to the subject.
    Type: Application
    Filed: May 11, 2010
    Publication date: April 21, 2011
    Applicant: The Johns Hopkins University
    Inventors: Robert A. Brodsky, Richard J. Jones
  • Publication number: 20110059074
    Abstract: The present invention provides methods and compositions for predicting patient responses to cancer treatment using a proliferation gene signature. These methods can comprise measuring in a biological sample from a patient the levels of gene expression of a group of the genes designated herein. The present invention also provides for microarrays that can detect expression from a group of genes.
    Type: Application
    Filed: May 2, 2008
    Publication date: March 10, 2011
    Inventors: Maud H.W. Starmans, Balaji Krishnapuram, Ranand G. Seigneuric, Harald Steck, Dimitry S.A. Nuyten, Francesca Buffa, Adrian Lewellyn Harris, Bradly G. Wouters, Philippe Lambin, R. Bharat Rao, Sriram Krishnan
  • Publication number: 20110044940
    Abstract: The present invention relates to novel Heterocyclic Ether or Thioether Derivatives, compositions comprising the Heterocyclic Ether or Thioether Derivatives, and methods for using the Heterocyclic Ether or Thioether Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Application
    Filed: October 27, 2008
    Publication date: February 24, 2011
    Inventors: Gerald W. Shipps, JR., Matthew Richards, Cliff C. Cheng, Xiaohua Huang
  • Publication number: 20110033461
    Abstract: Compositions which act synergistically to inhibit the growth of cancer cells and methods of use thereof are disclosed.
    Type: Application
    Filed: March 12, 2009
    Publication date: February 10, 2011
    Inventors: Vladimir Ratushny, Erica Golemis, Igor Astsaturov, Iiya G. Serebriiskii, Louis M. Weiner
  • Publication number: 20110028415
    Abstract: The present invention relates to the use of a compound of formula (I) wherein R1 is H, C1-C6-alkyl, phenyl-C1-C4-alkyl or phenyl, R2 is a phenyl group which is substituted with 2 or 3 C1-C6-alkoxy groups and R3 is indolyl or azaindolyl which may carry one or two substituents independently selected from C1-C6-alkyl, C1-C6-alkoxy, phenyl, OH, halogen, NH2, C1-C6-alkylamino, di-C1-C6-alkylamino, heteroaryl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S, or heterocyclyl with 5 or 6 ring atoms containing 1 or 2 heteroatoms which are independently selected from O, N, and S, a physiologically acceptable salt thereof, or a solvate of the compound of formula (I) or of the salt thereof, for the prevention or treatment of leukemia.
    Type: Application
    Filed: December 4, 2008
    Publication date: February 3, 2011
    Applicant: Johannes Gutenberg-Universitat Mainz
    Inventors: Gerd Dannhardt, Thomas Fischer, Florian Heidel
  • Publication number: 20110015157
    Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: July 25, 2008
    Publication date: January 20, 2011
    Inventors: David A. Claremon, Wei He, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Wei Zhao, Linghang Zhuang, Salvacion Cacatian, Katerina Leftheris
  • Publication number: 20110008461
    Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.
    Type: Application
    Filed: July 12, 2010
    Publication date: January 13, 2011
    Inventors: Gerald Carlson, Todd Holyoak, Sarah Sullivan, Rose Mary Stiffin
  • Publication number: 20110002879
    Abstract: The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4—; A is a bond, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from fluorine, hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g.
    Type: Application
    Filed: April 1, 2010
    Publication date: January 6, 2011
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Jayne Elizabeth CURRY, John Francis LYONS, Matthew Simon SQUIRES, Neil Thomas THOMPSON, Kyla Merriom THOMPSON, Paul Graham WYATT, Neil James GALLAGHER
  • Publication number: 20110002851
    Abstract: The present invention relates to the use of cationic colloidal compositions for the targeted delivery of an active compound to an inflammatory site or an activated vascular site for the preparation of a medicament for the treatment of MS and in general for all CNS or PNS inflammatory neurodegenerative and demyelinating diseases and for diagnostic applications of such compositions.
    Type: Application
    Filed: October 31, 2007
    Publication date: January 6, 2011
    Applicant: MediGene AG
    Inventors: Heinrich Haas, Paolo Riccio
  • Publication number: 20100323033
    Abstract: The present invention relates to a cancer sensitizer comprising chlorogenic acid or a derivative thereof. In particular, the present invention relates to a cancer sensitizer comprising chlorogenic acid or a derivative thereof, which can make cancer cells sensitive to anticancer agents to increase the therapeutic effect of anticancer agents. In addition, the present invention relates to a composition for inhibiting the chemo-resistance of cancer cells, comprising chlorogenic acid or a derivative thereof in combination with a pharmaceutically acceptable carrier, an anticancer composition comprising an anticancer agent in addition to the composition, and a method for disrupting the chemo-resistance of cancer cells, comprising administration of the cancer sensitizer.
    Type: Application
    Filed: October 1, 2008
    Publication date: December 23, 2010
    Inventors: Soo Youl Kim, Kang-Seo Park, Kyung chae Jeong
  • Publication number: 20100322895
    Abstract: The presently-disclosed subject matter provides methods and compositions for treating or reducing the risk of recurrence of a cancer in a subject. The methods comprise administering an effective amount of a T cell depleting composition to the subject to thereby treat the cancer.
    Type: Application
    Filed: June 20, 2008
    Publication date: December 23, 2010
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventor: Jason Chesney
  • Publication number: 20100310547
    Abstract: The present invention relates generally to the field of inflammatory diseases of the peripheral nervous system. More particularly, it concerns methods for treating inflammatory diseases of the peripheral nervous system by modulating sphingosine-1-phosphate receptor activity. In one embodiment, the present invention provides a method of treating a subject with chronic inflammatory demyelinating polyneuropathy (CIDP) or other autoimmune neuropathies comprising administering to the subject an effective amount of FTY720.
    Type: Application
    Filed: August 17, 2007
    Publication date: December 9, 2010
    Inventor: Betty C. Soliven
  • Publication number: 20100303719
    Abstract: The present invention relates to anti-cancer compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides analogs of the known anti-cancer compound amonafide, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with hyperproliferation.
    Type: Application
    Filed: January 12, 2009
    Publication date: December 2, 2010
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: Sui Huang, John Norton, Daniel Appella, Mark Witschi
  • Publication number: 20100297262
    Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of inflammation and cancer.
    Type: Application
    Filed: April 16, 2010
    Publication date: November 25, 2010
    Applicant: COLBY PHARMACEUTICAL COMPANY
    Inventors: Hirak S. Basu, David A. Zarling
  • Publication number: 20100284915
    Abstract: The invention provides molecular markers that are associated with responsiveness of a cancer patient to a chemotherapy treatment, and methods and computer systems for determining such responsiveness based on measurements of these molecular markers. The present invention also provides methods and compositions for enhancing the efficacy of chemotherapies in patients by modulating the expression or activity of genes encoding these molecular markers and/or their encoded proteins.
    Type: Application
    Filed: June 28, 2007
    Publication date: November 11, 2010
    Inventors: Hongyue Dai, Chunsheng Zhang, Andrey Loboda
  • Publication number: 20100284905
    Abstract: The application is based on the observation that tumor stem cell (TSC) replication involves a replicative intermediate configuration wherein a substantial fraction of the TSC genome is present as single-stranded DNA (ssDNA) when bell-shaped nuclei commence separation into two nuclei. During this replicative intermediate configuration large amounts of ssDNA are thus present in the nuclei of cells which the applicant proposes as target for anti-tumor therapy. A method of screening for anti-tumorigenic agents targeting ssDNA and use of such agents in therapy is claimed.
    Type: Application
    Filed: June 12, 2008
    Publication date: November 11, 2010
    Inventors: Elena V. Gostjeva, William G. Thilly
  • Publication number: 20100273743
    Abstract: The invention is directed to a method of administering hydrogen sulfide (H2S) slowly and sustainably to an individual in need thereof comprising administering an effective amount of a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 24, 2009
    Publication date: October 28, 2010
    Applicant: National University of Singapore
    Inventors: Philip Keith Moore, Choon-Hong Tan, Ling Li, Yan Yi Guan
  • Publication number: 20100260719
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Application
    Filed: April 7, 2010
    Publication date: October 14, 2010
    Inventor: Jerome B. Zeldis
  • Publication number: 20100233164
    Abstract: Combinations of PI3K inhibitor compounds having Formula I and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hematopoietic malignancies. Methods of using such combinations for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: March 11, 2010
    Publication date: September 16, 2010
    Inventors: Allen J. Ebens, JR., Lori Friedman
  • Publication number: 20100233166
    Abstract: Compounds, compositions and methods for the treatment of malignancy are disclosed.
    Type: Application
    Filed: April 13, 2010
    Publication date: September 16, 2010
    Inventors: George C. Prendergast, Alexander J. Muller, James B. Duhadaway, William Malachowski
  • Publication number: 20100221211
    Abstract: The invention relates to a compound of general formula (I-0): wherein R1 means a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, or a C3-C6 cycloalkyl group; R2, R3, R4 and R5 mean a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo-C1-C6 alkoxy group; R6 means a hydrogen atom, or a C1-C6 alkyl group; R7a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxy-C1-C6 alkyl group, -Q2-N(R1c)R1d or a nitrogen-containing heterocyclic group; R8a means a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a C1-C6 alkoxy group or a hydroxy-C1-C6 alkyl group; or R7a and R8a form, as taken together, a C2-C6 alkylene group, or R7a and R8a and the ring atoms to which they bond may form a spiro ring or a bicyclo ring; and X and Y mean a methine group or a nitrogen atom.
    Type: Application
    Filed: October 20, 2008
    Publication date: September 2, 2010
    Inventors: Hidetomo Furuyama, Mikako Kawamura, Toshihiro Sakamoto, Fuyuki Yamamoto, Takashi Yoshizumi
  • Publication number: 20100221251
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.
    Type: Application
    Filed: March 11, 2010
    Publication date: September 2, 2010
    Applicant: ARQULE, INC.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Publication number: 20100203110
    Abstract: The present invention relates to methods of treating a cancerous tumor in a subject comprising administering to the subject an effective amount of 3-bromopyruvate. The 3-bromopyruvate may be administered intraarterially directly to a tumor as a continuous intraarterial infusion. The present invention also relates to methods for identifying agents that inhibit type II hexokinase activity.
    Type: Application
    Filed: December 17, 2007
    Publication date: August 12, 2010
    Applicant: The Johns Hopkins University
    Inventors: Jean-Francois Geschwind, Mustafa Vali
  • Publication number: 20100183603
    Abstract: The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention.
    Type: Application
    Filed: June 19, 2008
    Publication date: July 22, 2010
    Applicant: ARQULE, INC.
    Inventors: Neil Westlund, Jason Hill, Mark A. Ashwell, Nivedita Namdev, Jianqiang Wang, Syed Ali
  • Publication number: 20100183587
    Abstract: The invention provides methods and compositions for minimizing, preventing, or treating damage to corneal nerves by administering to a subject with such damage or at risk of exposure to such damage a composition which blocks an activity of an IL-1 cytokine and/or an IL-17 cytokine.
    Type: Application
    Filed: January 11, 2010
    Publication date: July 22, 2010
    Applicant: Schepens Eye Research Institute
    Inventors: Reza Dana, Mohammad Dastjerdi, Sunil Chauhan