N-n Containing (e.g., Aminimine, Hydrazine, Etc.) Patents (Class 514/614)
  • Patent number: 11806326
    Abstract: A method of treating Parkinson's Disease, Huntington's Disease and the like, diseases with abnormal dopamine-neuro-transmission, using small molecules administered systemically that penetrate into the central nervous system to inhibit the rate-limiting step of dopamine synthesis in the central nervous system, the conversion of L-tyrosine to L-3, 4-dihydroxyphenylalanine (L-DOPA) by tyrosine hydroxylase along with its cofactors tetrahydrobiopterin and iron (Fe+).
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: November 7, 2023
    Inventor: Jonathan Sackner-Bernstein
  • Patent number: 11058688
    Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: July 13, 2021
    Assignee: Board of Regents, The University of Texas System
    Inventors: Kang Le, Michael J. Soth, Philip Jones, Jason Bryant Cross, Christopher L. Carroll, Timothy Joseph McAfoos, Pijus Kumar Mandal
  • Patent number: 10471028
    Abstract: Small molecule efflux pump inhibitors are provided, as well as methods for their use in treating infections. Also provided herein are methods of using the small molecule efflux pump inhibitors to restore the antibiotic susceptibility of microbes.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: November 12, 2019
    Assignee: UNIVERSITY OF ROCHESTER
    Inventors: Paul M. Dunman, Catlyn E. Blanchard
  • Patent number: 9889129
    Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.
    Type: Grant
    Filed: March 21, 2013
    Date of Patent: February 13, 2018
    Assignee: Case Western Reserve University
    Inventor: Chris Dealwis
  • Patent number: 9744233
    Abstract: Novel methods for treating patients with autoimmune diseases are disclosed. The methods of the invention include first depleting circulating lymphocytes in the mammal, e.g., by administering anti-thymocyte antibody, and then, during the course of repopulation, administering to the mammal a therapeutically effective amount of latent TGF-? and/or another agent that promotes expansion of regulatory T cells. In certain aspects, the disclosed process results in improved kidney function and survival rates.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: August 29, 2017
    Assignee: GENZYME CORPORATION
    Inventors: Johanne Kaplan, John McPherson
  • Patent number: 9555061
    Abstract: The invention relates to low-molecular-weight compounds which are capable of inducing differentiation of mesenchymal stem cell into hepatocytes.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: January 31, 2017
    Assignees: National University Corporation Torrori University, Tokyo Women's Medical University
    Inventors: Goshi Shiota, Yoshiko Hoshikawa, Noriko Matsumoto, Yoshiaki Matsumi, Minoru Morimoto, Takayuki Tonoi, Hiroyuki Saimoto, Kazuo Ohashi, Teruo Okano
  • Patent number: 9233095
    Abstract: Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: January 12, 2016
    Assignees: University of Rochester, Board of Regents of the University of Nebraska, Temple University—Of the Commonwealth System of Higher Education
    Inventors: Paul M. Dunman, Patrick D. Olson, Wayne Childers
  • Patent number: 9211410
    Abstract: Described herein are systems and methods for applying extremely low duty-cycle stimulation sufficient to treat chronic inflammation with progressively longer delays (off periods) from an initial stimulation. In particular, described herein are supra-threshold pulses of electrical stimulation sufficient to result in a long-lasting (e.g., >48 hours) inhibition of pro-inflammatory cytokines and/or effects of chronic inflammation; the delay between initial doses (which may be single-pulse doses) may be extended for subsequent doses, potentially dramatically enhancing battery and device longevity.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: December 15, 2015
    Assignee: SetPoint Medical Corporation
    Inventors: Jacob A. Levine, Michael A. Faltys
  • Patent number: 9169199
    Abstract: The invention provides cycloalkyl guanidine compounds that inhibit F1F0-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: October 27, 2015
    Assignee: Lycera Corporation
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 9156783
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: October 13, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Patent number: 9044442
    Abstract: The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: June 2, 2015
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
  • Publication number: 20150148359
    Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 28, 2015
    Inventors: Uri Ben-David, Nissim Benvenisty, Payal Arora, Qing-Fen Gan, Ralph J. Garippa
  • Publication number: 20150094314
    Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.
    Type: Application
    Filed: March 21, 2013
    Publication date: April 2, 2015
    Inventor: Chris Dealwis
  • Publication number: 20150031771
    Abstract: There is provided a novel use of ramalin for preventing or treating liver diseases, and more specifically, a pharmaceutical composition for preventing or treating hepatic fibrosis or cirrhosis containing ramalin or a pharmaceutically acceptable salt thereof, and a functional food containing the same. It was confirmed that at the time of applying ramalin, which is a compound derived from Ramalina terebrata according to the present invention, to animal models, ramalin may remarkably suppress hepatic fibrosis and lower liver cirrhosis levels as compared to silymarin known as a liver cell protecting ingredient without cytotoxicity to normal liver cells, such that ramalin may be effectively used for preventing or treating hepatic fibrosis and liver cirrhosis.
    Type: Application
    Filed: February 29, 2012
    Publication date: January 29, 2015
    Applicant: KOREA INSTITUTE OF OCEAN SCIENCE AND TECHNOLOGY
    Inventors: Joung Han Yim, Il Chan Kim, Se Jong Han, Hyoung Seok Lee, Hari Datta Bhattarai, Su-Geun Yang, Lee Don Hang
  • Publication number: 20150025042
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 16, 2013
    Publication date: January 22, 2015
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Publication number: 20150018290
    Abstract: The present invention generally relates to compositions containing chemical compounds and compositions and pharmaceutical formulations of the compounds which increase the expression of total hemoglobin or globin protein such as embryonic or fetal globin, or the proliferation of hemoglobin expressing and other blood cells. These compositions can be used to treat or prevent the symptoms associated with anemia, sickle cell diseases, thalassemia, and other blood cell deficiencies and blood disorders. The invention also relates to methods for administering these compositions to subjects and for use as medical aids for the treatment and prevention of blood and other disorders.
    Type: Application
    Filed: December 2, 2011
    Publication date: January 15, 2015
    Applicant: Trustees of Boston University
    Inventors: Susan Perrine, Douglas V. Faller
  • Patent number: 8865641
    Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: October 21, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Valentin A. Pavlov, Kevin J. Tracey
  • Patent number: 8809578
    Abstract: The present invention relates to a novel compound having excellent antioxidant activity, isolated from Ramalina terebrata, and more particularly to a novel compound, RAMALIN™, having excellent antioxidant activity, isolated from the Antarctic lichen Ramalina terebrata, a method for preparing the RAMALIN™, and a pharmaceutical composition, a functional food and a functional cosmetic composition, which contain the RAMALIN™ as an active ingredient. The RAMALIN™ according to the invention has significantly excellent antioxidant effects compared to commercially available antioxidants, and thus can be widely used in agents for treating oxidation-related diseases, anti-aging functional foods, functional cosmetic products for skin whitening and wrinkle reduction, etc.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: August 19, 2014
    Assignee: Korea Ocean Research and Development Institute
    Inventors: Joung Han Yim, Hong Kum Lee, Hari Datta Bhattarai, Paudel Babita, Il Chan Kim, Soon Gyu Hong, Doc Kyu Kim, Yoo Kyung Lee, Sung Gu Lee, Hyun Cheol Oh
  • Patent number: 8809395
    Abstract: The present invention is directed to compounds, intermediates and methods for making valerenic acid and its derivatives as well as the use of such compounds as GABAA receptor ligands.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: August 19, 2014
    Assignee: Valericon GmbH
    Inventors: Johann Mulzer, Jürgen Ramharter, Steffen Hering, Sophia Khom
  • Publication number: 20140221489
    Abstract: A method of eliminating or significantly decreasing shifts between dyskinesia and bradykinesia in a patient suffering from an advanced stage of Parkinson's Disease comprises for a predetermined time period intravenously, subcutaneously or intrathekally administering to the patient by continuous infusion a stable and therapeutically acceptable solution comprising at least 5 mg/ml of Levodopa.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 7, 2014
    Applicant: Dizlin Medical Design AB
    Inventor: Nil Dizdar Segrell
  • Patent number: 8785499
    Abstract: The emergence of multidrug-resistant pathogens necessitates the search for new antibiotics acting on previously unexplored targets. Nicotinate mononucleotide adenylyltransferase of the NadD family, an essential enzyme of NAD biosynthesis in most bacteria, was selected as a target for structure-based inhibitor development. To this end, the inventors have identified small molecule compounds that inhibit bacterial target enzymes by interacting with a novel inhibitory binding site on the enzyme while having no effect on functionally equivalent human enzymes.
    Type: Grant
    Filed: July 12, 2010
    Date of Patent: July 22, 2014
    Assignees: University of Maryland, Baltimore, The Board of Regents of the University of Texas System, Sanford-Burnham Medical Research Institute
    Inventors: Alexander Mackerell, Jr., Hong Zhang, Andrei Osterman, Rohit Kolhatkar
  • Patent number: 8779002
    Abstract: In accordance with the present invention, there are provided novel compounds that have a variety of properties, i.e., antioxidant, anti-inflammatory, antiviral, antibacterial, and antifungal properties. Invention compounds, therefore, have the ability to impart a variety of beneficial physiological effects, e.g., to protect neurons and/or to promote neuroregeneration and/or to promote memory formation and/or to act as protein phosphatase or kinase inhibitors and/or to act as lipoxygenase inhibitors. Such compounds are useful for treatment of a variety of indications, including neurodegenerative diseases and conditions, diabetes, ischemia associated with heart disease, and memory deficit. In another aspect of the present invention, there are also provided formulations containing one or more of the above-described compounds, optionally further containing additional neurologically active compound(s) and/or adjuvants to facilitate delivery thereof across the blood/brain barrier.
    Type: Grant
    Filed: October 14, 2008
    Date of Patent: July 15, 2014
    Assignee: Salk Institute for Biological Studies
    Inventor: David R. Schubert
  • Publication number: 20140179637
    Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.
    Type: Application
    Filed: December 21, 2013
    Publication date: June 26, 2014
    Applicants: The Research Foundation for The State University of New York, Northwestern University
    Inventors: Jonathan Leis, Carol Carter
  • Patent number: 8729129
    Abstract: Disclosed is a method of reducing bleed time in a subject by activation of the cholinergic anti-inflammatory pathway in said subject. The cholinergic anti-inflammatory pathway can be activated by direct or indirect stimulation of the vagus nerve. The cholinergic anti-inflammatory pathway can also be activated by administering an effective amount of cholinergic agonist or acetylcholinesterase inhibitor to the subject.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: May 20, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Kevin J. Tracey, Carol Ann Amella, Christopher Czura
  • Publication number: 20140056952
    Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using polyamines is described.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Richard LOSICK, Illana KOLODKIN-GAL, Jon CLARDY, Shugeng CAO, Matt CABEEN, Roberto KOLTER, Liraz CHAI, Thomas BÖTTCHER
  • Publication number: 20140056951
    Abstract: Methods of treating or reducing biofilms, treating a biofilm-related disorder, and preventing biofilm formation using polyamines is described.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Richard LOSICK, Illana KOLODKIN-GAL, Jon CLARDY, Shugeng CAO, Matt CABEEN, Roberto KOLTER, Liraz CHAI, Thomas BÖTTCHER
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Patent number: 8623921
    Abstract: Disclosed herein are compositions comprising a compound represented by structural formula (I): 2 g of which is reconstitutable in 10 mL of a water in less than 10 minutes, and methods for preparing these compositions. Also disclosed are compositions comprising a compound represented by structural formula (I) and a pharmaceutically acceptable excipient, wherein the molar ratio of said compound to said excipient is from 1:20 to 1:1, and methods for preparing these compositions.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: January 7, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Walter J. Lunsmann, Ninad Deshpanday
  • Patent number: 8618170
    Abstract: Disclosed herein are oral formulations of bis(thio-hydrazide amides) compounds of the following structural formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R7, R8, Z, and Y are defined herein.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: December 31, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Noriaki Tatsuta, Takayo Inoue, Keizo Koya
  • Patent number: 8581004
    Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: November 12, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Teresa Kowalczyk-Przewloka, Lijun Sun
  • Patent number: 8552067
    Abstract: Provided herein are bioactive agents comprising a compound that inhibits the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR) and that is linked to a macromolecule that interacts with a cell that expresses CFTR. The bioactive agents described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: October 8, 2013
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Nitin D. Sonawane
  • Publication number: 20130237580
    Abstract: The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
    Type: Application
    Filed: March 7, 2013
    Publication date: September 12, 2013
    Applicant: AURIGENE DISCOVERY TECHNOLOGIES LIMITED
    Inventors: POTTAYIL GOVINDAN NAIR SASIKUMAR, MURALIDHARA RAMACHANDRA, SEETHARAMAIAH SETTY SUDARSHAN NAREMADDEPALLI
  • Publication number: 20130190296
    Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.
    Type: Application
    Filed: November 20, 2012
    Publication date: July 25, 2013
    Applicant: Dendreon Corporation
    Inventor: Dendreon Corporation
  • Patent number: 8492434
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: February 22, 2012
    Date of Patent: July 23, 2013
    Assignee: Siga Technologies Inc.
    Inventors: Dennis E. Hruby, Tove C. Bolken, Sean Amberg, Dongcheng Dai
  • Publication number: 20130150346
    Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.
    Type: Application
    Filed: January 7, 2011
    Publication date: June 13, 2013
    Applicants: Ironwood Pharmaceutical, Inc.
    Inventors: James Philip Pearson, Todd G. Milne, Thomas Henry Johnston, Jonathan Michael Brotchie
  • Patent number: 8455686
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: June 4, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Weiwen Ying, Teresa Kowalczyk-Przewloka, Lijun Sun
  • Publication number: 20130137774
    Abstract: This application describes pharmaceutical compositions, commercial packages, and methods for inhibiting cell proliferative disorders, especially those disorders, including Her2 related cancers, characterized by overactivity and/or inappropriate activity of a receptor tyrosine kinase, and methods for imaging an HER-2 expressing tumor.
    Type: Application
    Filed: May 26, 2011
    Publication date: May 30, 2013
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: Mark I. Greene, Ramachandran Murali, Hongtao Zhang
  • Publication number: 20130072477
    Abstract: The present invention relates to a therapeutic or prophylactic method for treating Parkinson's disease by administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to a pharmaceutical composition for treatment or prophylaxis of Parkinson's disease comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity. Moreover, the present invention relates to a method for enhancing dopamine signal in the brain, which comprises administering an effective amount of a compound having a phosphodiesterase 10 inhibitory activity; and also relates to pharmaceutical composition for enhancing dopamine signal in brain comprising as an active ingredient a compound having a phosphodiesterase 10 inhibitory activity.
    Type: Application
    Filed: November 16, 2012
    Publication date: March 21, 2013
    Applicant: MITSUBISHI TANABE PHARMA COPORATION
    Inventor: MITSUBISHI TANABE PHARMA COPORATION
  • Publication number: 20130004577
    Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: NIPPON SHINYAKU
    Inventors: Hironobu KATO, Hirokazu SAKAMOTO
  • Publication number: 20120322717
    Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.
    Type: Application
    Filed: May 22, 2009
    Publication date: December 20, 2012
    Inventors: Dakai Liu, Xiaofeng Li, Richard Jin, Yuaxin Liang, Wei Cheng, Riddhi Bhattacharyya, Guangrong Zhang
  • Publication number: 20120322719
    Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 20, 2012
    Applicant: The Feinstein Institute For Medical Research
    Inventors: Valentin A. Pavlov, Kevin J. Tracey
  • Patent number: 8288441
    Abstract: The present invention concerns enhancements in the cooling effects of certain physiological coolant-containing compositions such as topically applied cosmetic, toiletry or pharmaceutical products, wherein the cooling effect of the physiological coolants is enhanced by the addition of a substance according to formula (I) or dermatologically acceptable salts thereof: R1—CR2(OR3)—CO—NR4—CR5R6—X—OR7??(I) It was found that substances represented by formula (I) are capable of bringing about greater cooling effects from reduced concentrations of physiological coolants without behaving as physiological coolants themselves, thereby enabling the preparation of compositions that do not necessarily have the characteristic minty odor of menthol-containing products and/or to allow greater freedom in creating perfumed products.
    Type: Grant
    Filed: March 3, 2008
    Date of Patent: October 16, 2012
    Assignee: Givaudan Nederland Services B.V.
    Inventors: Michael Steven Watson, Stephen David Watkins, Sander Tondeur
  • Publication number: 20120196918
    Abstract: Pancreatic islet dysfunction, in both type 1 and type 2 diabetes results, in part, from cytokine-mediated inflammation leading to iNOS generation and the death of pancreatic islets. The production of pro-inflammatory cytokines involved in the generation of iNOS is facilitated by the availability of the hypusine-containing translational factor eIF5A, necessary for the maturation of antigen-presenting cells. Treatment with agents capable of interfering with the mRNA translating iNOS or with agents that can interfere with the hypusination of eIF5A, prevents the death of islets, lowers blood glucose levels, avoids insulin resistance, and generally avoids the inflammatory response in islets associated with type 1 and type 2 diabetes.
    Type: Application
    Filed: April 8, 2010
    Publication date: August 2, 2012
    Inventors: Raghavendra G. Mirmira, Bernhard Maier
  • Publication number: 20120178697
    Abstract: The Wnt signaling pathways are involved in embryo development as well as in tumorigenesis. Dishevelled (Dvl) tranduces Wnt signals from the receptor Frizzled (Fz) to downstream components in canonical and non-canonical Wnt signaling pathways, and the Dvl PDZ domain plays an essential role in both pathways, and the Dvl PDZ domain binds directly to Fz receptors. In the present invention using NMR-assisted virtual ligand screening, several compounds were identified and were found to bind to the Dvl PDZ domain. Molecular dynamics simulation was used to analyze the binding between the PDZ domain and these compounds in detail. These compounds provide a basis for rational design of high-affinity inhibitors of the PDZ domain, which can block Wnt signaling by interrupting the Fz-Dvl interaction.
    Type: Application
    Filed: April 1, 2005
    Publication date: July 12, 2012
    Inventors: Jie Zheng, Jufang Shan, Dianqing Wu
  • Publication number: 20120122878
    Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.
    Type: Application
    Filed: June 30, 2008
    Publication date: May 17, 2012
    Inventors: Baltazar Gomez-Mancilla, Fabrizio Gasparini
  • Patent number: 8148426
    Abstract: A method of treating a Hsp70-responsive disorder in a subject includes administering to the subject an effective amount of a compound represented by Structural Formula I, or a pharmaceutically acceptable salt or solvate thereof. Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C?Z groups to which it is bonded, is an optionally substituted aromatic group. R1-R4 are independently —H, an optionally substituted aliphatic group, an optionally substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R7-R8 are independently —H, an optionally substituted aliphatic group, or an optionally substituted aryl group. Z is O or S.
    Type: Grant
    Filed: November 17, 2005
    Date of Patent: April 3, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventor: James Barsoum
  • Patent number: 8138182
    Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 20, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Hatayama, Hiroshi Tsuruta, Yasuo Ochi, Haruo Imawaka, Kazuyuki Ohmoto
  • Publication number: 20120065235
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 7, 2008
    Publication date: March 15, 2012
    Inventors: Lijun Sun, Jun Jiang
  • Patent number: 8093425
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: January 10, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Weiwen Ying, Teresa Przewloka, Lijun Sun
  • Publication number: 20110294814
    Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 1, 2011
    Inventors: Teresa Kowalczyk-Prezewloka, Lijun Sun