Plural Ring Nitrogens In The Tricyclo Ring System Patents (Class 514/292)
Three or more hetero atoms in the tricyclo ring system (Class 514/293)
  • 17a-HYDROXYLASE/C17,20-LYASE INHIBITORS
    Publication number: 20140045872
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: NOVARTIS AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Carboxamide, Sulfonamide and Amine Compounds and Methods for Using The Same
    Publication number: 20140045882
    Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, D, E, J, T, p, q and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: October 14, 2013
    Publication date: February 13, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Ihab S. Darwish, Jiaxin Yu, Hui Hong, Rajinder Singh, Sambaiah Thota, Xiang Xu
  • NOVEL MICROBIOCIDES
    Publication number: 20140045873
    Abstract: The present invention provides compounds of formula (I) wherein A1, A2, R1, D1, D2, Y3 and X are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: November 10, 2011
    Publication date: February 13, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Stephan Trah, Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato
  • QUINOLONE COMPOUND AND PHARMACEUTICAL COMPOSITION
    Publication number: 20140045793
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
  • DIHYDROPYRIDONE P1 AS FACTOR XIA INHIBITORS
    Publication number: 20140038969
    Abstract: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Inventors: Wu Yang, James R. Corte, Paul J. Gilligan, Donald J.P. Pinto, William R. Ewing, Yufeng Wang
  • TFEB PHOSPHORYLATION INHIBITORS AND USES THEREOF
    Publication number: 20140038920
    Abstract: The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases.
    Type: Application
    Filed: March 7, 2012
    Publication date: February 6, 2014
    Applicant: FONDAZIONE TELETHON
    Inventors: Andrea Ballabio, Carmine Settembre, Diego Luis Medina Sanabria
  • Aryl Lactam Kinase Inhibitors
    Publication number: 20140038999
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 6, 2014
    Inventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu, Tarun Kumar Maishal, Jonathan L. Ditta, Carolyn Diane Dzierba, Joanne J. Bronson, John E. Macor
  • Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
    Patent number: 8642834
    Abstract: The present invention provides tumor cell preparations for use as models of the EMT process for use in the identification of anti-cancer agents, wherein said tumor cell preparations comprise cells of the epithelial tumor cell line CFPAC-1, which are stimulated by receptor ligands to induce EMT, or which have been engineered to inducibly express a protein that stimulates EMT. The present invention also provides methods of identifying potential anti-cancer agents by using such tumor cell preparations to identify agents that inhibit EMT, stimulate MET, or inhibit the growth of mesenchymal-like cells. Such agents should be particularly useful when used in conjunction with other anti-cancer drugs such as EGFR and IGF-1R kinase inhibitors, which appear to be less effective at inhibiting tumor cells that have undergone an EMT.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: February 4, 2014
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Julie Kan, Salam A. Shaaban, Joseph S. Krueger, Maryland Franklin, Robert C. Wild
  • Pharmaceutical Compositions
    Publication number: 20140030249
    Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 30, 2014
    Applicant: Valeant International Bermuda
    Inventors: Andrew John DUFFIELD, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
  • AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF
    Publication number: 20140023636
    Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.
    Type: Application
    Filed: September 23, 2013
    Publication date: January 23, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Haruto KURATA, Shinji NAKADE
  • Thienyl-and furanyl-isoquinolinones and methods for using them
    Patent number: 8633215
    Abstract: The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: January 21, 2014
    Inventors: Roberto Pellicciari, Flavio Moroni, Eric Christian Hansen, Adam Matthew Gilbert, Peter John Larkin
  • INHIBITORS OF MTOR KINASE AS ANTI-VIRAL AGENTS
    Publication number: 20140018354
    Abstract: The present invention provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR. The invention also provides methods and compositions for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR and modulators of the unfolded protein response.
    Type: Application
    Filed: July 23, 2010
    Publication date: January 16, 2014
    Inventors: Nathaniel Moorman, Thomas Shenk
  • [1,10]-PHENANTHROLINE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE OR HAEMATOLOGICAL DISEASES
    Publication number: 20140011835
    Abstract: The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or prophylaxis of a neurodegenerative or hematological disease or condition, their use as a medicament, especially for treating a neurodegenerative or hematological disease or condition, and a pharmaceutical composition comprising the compounds.
    Type: Application
    Filed: September 15, 2013
    Publication date: January 9, 2014
    Applicant: Noscira, S.A.
    Inventors: Ana MARTINEZ GIL, Ana Castro Morera, Miguel Medina Padilla, Jorge Sanchez-Quesada, Mercedes Alonso Cascon, Laura Rubio Arrieta, Esther Garcia Palomero, Paola Usan Egea
  • BETA CARBOLINE DERIVATIVES USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS
    Publication number: 20140005220
    Abstract: The invention provides novel beta-carboline derivatives of formulae (Ia) and (Ib) useful in the treatment of proliferative disorders including cancer, intermediates used in their preparation, processes for preparing the same and uses thereof.
    Type: Application
    Filed: June 24, 2011
    Publication date: January 2, 2014
    Applicants: UNIVERSITE LIBRE DE BRUXELLES, FACULTES UNIVERSITAIRES NOTRE DAME DE LA PAIX
    Inventors: Raphael Frederick, Bernard Masereel, Jeremy Reniers, Johan Wouters, Celine Bruyere, Robert Kiss
  • POLYCYCLIC AGENTS FOR THE TREATMENT OF RESPIRATORY SYNCYTIAL VIRUS INFECTIONS
    Publication number: 20140004111
    Abstract: The present invention relates to polycyclic antiviral compounds, and salts thereof, methods for their preparation and compositions containing them, and the use of the compounds and composition in the treatment of viral infections.
    Type: Application
    Filed: August 30, 2013
    Publication date: January 2, 2014
    Applicant: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Alistair George Draffan, Vanessa Anne Sanford, Silas Bond, Chin Yu Lim, Anne Mayes
  • USE OF IDE AS A BIOMARKER FOR A SCALP CONDITION
    Publication number: 20130337085
    Abstract: The subject matter of the present invention is in particular the use of an amino acid sequence of IDE, or of an analogue or fragment thereof, or of at least one nucleic acid sequence encoding this sequence, as a biomarker, or as an active agent, with regard to a dandruff condition of the scalp.
    Type: Application
    Filed: December 12, 2011
    Publication date: December 19, 2013
    Applicant: L'oreal
    Inventors: Caroline Delattre, Philemon Sirven, Dominique Bernard
  • Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as Axl inhibitors
    Patent number: 8609650
    Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: December 17, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak
  • Hydroxylamine substituted imidazoquinolines
    Patent number: 8598192
    Abstract: Imidazo ring compounds (e.g., imidazoquinolines, 6,7,8,9-tetrahydroimidazoquinolines, imidazonaphthyridines, and imidazopyridines) with a hydroxylamine substituent at the 2-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: December 3, 2013
    Assignee: 3M Innovative Properties Company
    Inventors: Tushar A. Kshirsagar, Gregory D. Lundquist, Jr., David T. Amos, Joseph F. Dellaria, Jr., Bernhard M. Zimmermann, Philip D. Heppner
  • 1,2-dihydro-2-oxoquinoline compounds as 5-HTreceptor ligands
    Patent number: 8598204
    Abstract: The present invention relates to novel 1,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: December 3, 2013
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Ishtiyaque Ahmad, Pradeep Jayarajan, Nagaraj Vishwottam Kandikere, Anil Karbhari Shinde, Rama Sastri Kambhampati, Gopinadh Bhyrapuneni, Jyothsna Ravula, Sriramachandra Murthy Patnala, Venkateswarlu Jasti
  • HARMINE DERIVATIVES FOR PROMOTING BONE GROWTH
    Publication number: 20130315965
    Abstract: The present invention provides compositions comprising a compound of Formula I, and salts, hydrates, and isomers thereof. Methods of promoting bone growth, treating renal disease, and treating cancer in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I, are also provided. Medical devices comprising compound of Formula I are also provided.
    Type: Application
    Filed: May 15, 2013
    Publication date: November 28, 2013
    Inventors: Debra Ellies, Ferris Scott Kimball, Jean-Philippe Rey
  • 5-HT3 RECEPTOR MODULATORS, METHODS OF MAKING, AND USE THEREOF
    Publication number: 20130310366
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 21, 2013
    Applicant: Albany Molecular Research, Inc.
    Inventors: David D. MANNING, Christopher L. CIOFFI
  • Androgen receptor modulator methods
    Patent number: 8580811
    Abstract: Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: November 12, 2013
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Bijan Pedram, Cornelis Arjan Van Oeveren, Lin Zhi, Shuo Zhao, Yixing Shen
  • Use Of Chloroquine To Treat Metabolic Syndrome
    Publication number: 20130296237
    Abstract: The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 7, 2013
    Inventors: Michael B. Kastan, Clay F. Semenkovich, Jochen Schneider
  • Method of preventing or ameliorating psoriasis using pyrroloquinoline quinone compounds
    Patent number: 8575190
    Abstract: The present invention provides a method for preventing or ameliorating skin psoriasis by applying as an active ingredient, a compound represented by general formula (I) or a salt thereof: (wherein R1, R2, and R3 simultaneously or separately represent a lower alkyl, lower alkenyl, lower alkynyl, aralkyl, araryl, or phenyl group, or a hydrogen atom).
    Type: Grant
    Filed: November 12, 2008
    Date of Patent: November 5, 2013
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Ayako Kamimura, Toshikazu Kamiya, Masahiko Nakano, Kazutoshi Kikkawa
  • Inhibition of quorum sensing-mediated processes in bacteria
    Patent number: 8568756
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: October 29, 2013
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • HDAC Inhibitors and Therapeutic Methods of Using Same
    Publication number: 20130281484
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
    Type: Application
    Filed: April 22, 2013
    Publication date: October 24, 2013
    Inventors: Alan Kozikowski, Kyle Vincent Butler, Jay Hans Kalin
  • CARBAZOLE AND CARBOLINE DERIVATIVES, AND PREPARATION AND THERAPEUTIC APPLICATIONS THEREOF
    Publication number: 20130274258
    Abstract: Compounds of general formula (I), wherein A, Y, R1 and R2 are defined herein are useful in the treatment or prevention of proliferative diseases including cancer or infectious or parasitic diseases.
    Type: Application
    Filed: November 3, 2011
    Publication date: October 17, 2013
    Applicant: PHILIP MORRIS PRODUCTS S.A.
    Inventors: Stephane Demotz, Gerhard Lang, Damian McHugh, Axel Teichert, Fernando Goffman, Paul M. Doyle, Paul M. Blaney, Raymond Fisher, Andrew Smith, Emma L. Blaney, Simon Foster
  • Heterocyclic fused phenanthrolinone M1 receptor positive allosteric modulators
    Patent number: 8557992
    Abstract: The present invention is directed to heterocyclic fused phenanthrolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: June 10, 2011
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Azaindole derivatives as CRTH2 receptor antagonists
    Patent number: 8546422
    Abstract: Compounds of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: October 1, 2013
    Assignee: Merck Canada Inc.
    Inventors: Yves Leblanc, Carl Berthelette, Daniel Simard, Mohamed Helmi Zaghdane
  • Oncogenic-RAS-signal dependent lethal compounds
    Patent number: 8546421
    Abstract: Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: October 1, 2013
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Brent R. Stockwell, Wan Seok Yang, Rohitha Sriramaratnam
  • 4, 5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
    Patent number: 8546420
    Abstract: The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Yueheng Jiang, Stuart B. Rosenblum, Srikanth Venkatraman, Francisco Velazquez, Neng-Yang Shih, F. George Njoroge, Joseph A. Kozlowski
  • HIGHLY SOLUBLE SALT OF PYRROLOQUINOLINE QUINONE AND METHOD FOR PRODUCING THE SAME
    Publication number: 20130253001
    Abstract: An object of the present invention is to provide a salt of pyrroloquinoline quinone having a high solubility in water and in an organic solvent and a method for producing the same. According to the present invention, there are provided an ammonium salt of pyrroloquinoline quinone having a high solubility in water and in an organic solvent, consisting of a pyrroloquinoline quinone ion and an ammonium salt having a hydroxyl group.
    Type: Application
    Filed: November 25, 2011
    Publication date: September 26, 2013
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY INC.
    Inventor: Kazuto Ikemoto
  • COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS
    Publication number: 20130253002
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is —CR4?CR5.
    Type: Application
    Filed: April 22, 2013
    Publication date: September 26, 2013
    Inventors: TOM YAO-HSIANG WU, YONGKAI LI, ALEX CORTEZ, YEFEN ZOU, PRANAB MISHRA, XIAOYUE ZHANG, NICHOLAS VALIANTE
  • NOVEL COMPOSITION
    Publication number: 20130245060
    Abstract: This invention relates to topical pharmaceutical compositions comprising the active agent 4-methyl-1-(2-phenylethyl)-8-phenoxy-2,3-dihydro-1H-pyrrolo[3,2-c]-quinoline or a pharmaceutically acceptable derivative thereof and a hydrophobic excipient, to a process for preparing such compositions, and to the use of such compositions for the treatment of microbial infections.
    Type: Application
    Filed: October 7, 2011
    Publication date: September 19, 2013
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Yanmin Hu, Anthony Rm Coates
  • NEURONAL CIRCUIT-DEPENDENT NEUROPROTECTION BY INTERACTION BETWEEN NICOTINIC RECEPTORS
    Publication number: 20130237560
    Abstract: A method of inhibiting excitotoxicity by indirectly activating ?4?2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of ?7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate ?4?2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 12, 2013
    Inventors: Peter Andrew Ferchmin, Vesna Ana Eterovic De Ferchmin, Hector Manuel Maldonado
  • NOVEL FORMULATIONS FOR TREATMENT OF MIGRAINE
    Publication number: 20130231311
    Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.
    Type: Application
    Filed: April 16, 2013
    Publication date: September 5, 2013
    Inventors: Stephen J. FARR, John TURANIN, Roger HAWLEY, Jeffrey A. SCHUSTER
  • Beta-Carbolines as Inhibitors of Haspin and DYRK Kinases
    Publication number: 20130231360
    Abstract: The present disclosure is directed to compounds of Formula (I) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.
    Type: Application
    Filed: April 21, 2011
    Publication date: September 5, 2013
    Applicant: THE BRIGHAM AND WOMEN S HOSPITAL, INC.
    Inventors: Jonathan Higgins, Debasis Patnaik, Natalia Ulyanova, Ross L. Stein, Jun Xian, Marcie Glicksman, Gregory D. Cuny
  • HDAC INHIBITORS TO TREAT CHARCOT-MARIE-TOOTH DISEASE
    Publication number: 20130227717
    Abstract: The present application relates to diseases in the peripheral nervous system, particularly hereditary neuropathies, most particularly, Charcot-Marie-Tooth (CMT) disease. It is shown that this disease is associated with decreased acetylated tubulin levels, which can be overcome by inhibition of histone deacetylases (HDACs). Using HDAC inhibitors, it is shown herein that the symptoms of the CMT phenotype can be overcome both in vitro and in vivo. Also provided herein are two different mouse models of CMT disease.
    Type: Application
    Filed: October 6, 2011
    Publication date: August 29, 2013
    Applicant: Life Sciences Research Partners VZW
    Inventors: Ludo Van Den Bosch, Constantin Van Outryve d'Ydewalle, Wim Robberecht
  • CALCIUM SALT OF PYRROLOQUINOLINE QUINONE
    Publication number: 20130225632
    Abstract: An object of the present invention is to provide an industrially useful method for producing a calcium salt of pyrroloquinoline quinone, without using large amounts of organic solvents, and highly pure crystals produced thereby. According to the present invention, a highly pure calcium salt of pyrroloquinoline quinone can be produced by reacting an alkali metal salt of pyrroloquinoline quinone with a source of calcium ions.
    Type: Application
    Filed: September 22, 2011
    Publication date: August 29, 2013
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Kazuto Ikemoto, Masahiko Nakano
  • Tricyclic compounds useful as inhibitors of kinases
    Patent number: 8518964
    Abstract: The present invention provides inhibitors of kinases, specifically I?B kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-?B-mediated diseases.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: August 27, 2013
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Jean-Francois Truchon, Nicolas Lachance, Cheuk Lau, Yves Leblanc, Christophe Mellon, Patrick Roy, Elise Isabel, Ryan D Otte, Jonathan R Young
  • TREATING ATTENTION DEFICIT HYPERACTIVITY DISORDER WITH NHE INHIBITORS
    Publication number: 20130217707
    Abstract: The present invention relates to a method of treating attention deficit hyperactivity disorder in a subject. This method includes selecting a subject with attention deficit hyperactivity disorder and administering to the selected subject a sodium/hydrogen exchanger inhibitor under conditions effective to treat the subject for attention deficit hyperactivity disorder. Methods of identifying compounds suitable to treat attention deficit hyperactivity disorder are also disclosed.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 22, 2013
    Applicant: The Research Foundation of State University of New York
    Inventor: The Research Foundation of State University of New York
  • SUSTITUTED 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES, METHODS FOR USE THEREOF
    Publication number: 20130217703
    Abstract: The present invention relates to a method of antagonizing a 5-HT6 serotonin receptor and simultaneously regulating Ca+2 ion homeostasis in a cell, comprising administering to the cell a compound of formula 1, or a pharmaceutically acceptable salt thereof, wherein: R1 is a C1-C5 alkyl; R2i is independently hydrogen, halogen, a C1-C3 alkyl, CF3, OCF3 or OCH3; i is 1, 2, 3 or 4; Ar is an unsubstituted phenyl or a substituted phenyl substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle with one or two nitrogen atoms in the heterocycle; and W is an ethylene group —CH2—CH2—, ethenyl group —CH?CH—, or ethynyl group —C?C—.
    Type: Application
    Filed: March 16, 2013
    Publication date: August 22, 2013
    Applicant: ALLA CHEM, LLC
    Inventor: Alla Chem, LLC
  • PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE
    Publication number: 20130217675
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 22, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • TETRACYCLIC COMPOUNDS
    Publication number: 20130203746
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: November 16, 2012
    Publication date: August 8, 2013
    Inventor: Medivation Technologies Inc.
  • METHOD FOR DETECTING NON-TRANSFERRIN BOUND IRON
    Publication number: 20130203800
    Abstract: A method of quantifying non-transferrin bound iron (NTBI) in a biological fluid is provided, the method comprising: (a) contacting a sample of the biological fluid with a reducing agent to obtain redox-active iron; (b) contacting the sample of the biological fluid with a nitrilotriacetate (NTA) at a concentration of 0.4-2 mM to mobilize non-transferrin bound iron including redox inactive and the redox active iron in the sample; (c) contacting the sample of the biological fluid of step (b) with an indicator including an iron binding moiety and fluorophore; and (d) detecting and quantifying a fluorescent signal of the fluorophore thereby quantifying the NTBI in the biological sample.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 8, 2013
    Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Ioav Zvi CABANTCHIK, William Breuer
  • NEUROPROTECTION BY PHARMACOLOGICAL CHAPERONING OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20130197023
    Abstract: A method of ameliorating an endoplasmic reticulum (ER) stress response and/or unfolded protein response (UPR) in cells expressing nicotinic acetylcholine receptors (nAChRs) comprises contacting a cell expressing nAChRs with an effective amount of a ligand for nAChRs. The contacting results in attenuating endogenously expressed ATF6 translocation, expression of XBP1, phosphorylation of eukaryotic initiation factor 2? (peIF2?), increased numbers of ER exit sites, increased trafficking of known associated proteins as well as other proteins such as growth factors and their receptors, changes in abundance of selected mRNA species, and phosphorylation, abundance, or subcellular compartmentalization of other proteins involved with ER stress and/or the UPR, and inhibiting upregulation of CCAAT/Enhancer-Binding Protein Homologous Protein (CHOP) levels in the cells.
    Type: Application
    Filed: January 28, 2013
    Publication date: August 1, 2013
    Applicant: California Institute of Technology
    Inventors: Henry A. Lester, Rahul Srinivasan, Christopher I. Richards, Brandon J. Henderson
  • TETRACYCLIC COMPOUNDS
    Publication number: 20130190304
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 12, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • COMPOUNDS AND METHODS FOR TREATING DIABETES
    Publication number: 20130190294
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: March 7, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc
  • PYRIDO[4,3-B]INDOLES AND METHODS OF USE
    Publication number: 20130190328
    Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • MATRINIC ACID/MATRINE DERIVATIVES AND PREPARATION METHODS AND USES THEREOF
    Publication number: 20130190345
    Abstract: The present invention relates to a N-substituted matrinic acid derivative or matrine derivative, and its preparation method and uses. Specifically, the present invention relates to a compound of Formula (I) or (II) (wherein all the definitions of substituted groups are those mentioned in the specification), or a pharmaceutically acceptable salt, geometric isomer, stereoisomer, solvate, ester or prodrug thereof. The present invention further relates to a method for preparing the compound of the present invention, a pharmaceutical composition containing the compound, and uses thereof in manufacture of a medicament. The compound of the present invention can be used for prophylaxis and/or treatment of a disease or disorder associated with viral infection such as hepatitis B and/orhepatitis C and/or AIDS.
    Type: Application
    Filed: April 29, 2011
    Publication date: July 25, 2013
    Applicants: CSPC Zongqi Pharmaceutical Technology (Shijiahuang) Co., Ltd., Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences
    Inventors: Jiandong Jiang, Danqing Song, Nana Du, Zonggen Peng, Yuping Wang, Limei Gao, Yanxing Han, Xin Li, Chunxin Li