Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
  • Publication number: 20140336183
    Abstract: A method and composition for the treatment of ischemic neuronal reperfusion injury are provided. The composition may include at least a benzodiazepine class material. In another form, the composition may include at least two components selected from the group consisting of an antagonist of the type 3 ryanodine receptor, an NMDA blocker (antagonist), and a benzodiazepine class material which can be administered for ischemic neuronal reperfusion injury. In one form, all three components may be used.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Inventors: Harpal S. Mangat, Pradeep K. Karla
  • Patent number: 8883777
    Abstract: The present invention provides a composition controlling a pH range of release and/or a release rate, which contains (i) a thienotriazolodiazepine compound of the formula (I) and (ii) at least one kind of ingredient selected from the group consisting of a water-soluble polymer, an enteric polymer, a water-insoluble polymer and a porous polymer and/or a surfactant, as well as a production method thereof.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: November 11, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuyoshi Sagara, Tomoyuki Omura, Hirofumi Samemoto, Hirotsugu Komatsu
  • Patent number: 8883214
    Abstract: The present invention provides compositions and methods for treating ocular disorders such as myopia.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: November 11, 2014
    Assignee: The Regents of the University of California
    Inventors: Christine F. Wildsoet, James Su, Kevin E. Healy
  • Publication number: 20140329804
    Abstract: The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: Donald W. LANDRY, Shixian DENG, Ottavio ARANCIO, Jole FIORITO, Andrew WASMUTH
  • Patent number: 8877746
    Abstract: Compositions and methods of making the same for in vivo delivery of lixivaptan to a subject in need thereof are described. The composition includes a substantially water-insoluble pharmacologically active agent (e.g., lixivaptan) and a substantially water-insoluble matrix forming material (e.g., a Vitamin E semi-ester), wherein the pharmacologically active agent is dispersed in said matrix forming material, and wherein the composition delivers said substantially water-insoluble pharmacologically active agent upon exposure to physiological medium.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: November 4, 2014
    Assignee: Cardioklne, Inc
    Inventors: Hailiang Chen, Andrew Xian Chen, Patricia Frech, Khawla Abu-Izza, Christoph Schmidt
  • Publication number: 20140322242
    Abstract: Methods of treating or preventing cancer, or ameliorating a symptom thereof, by administering a muscarinic receptor inhibitor to inhibit cancer metastasis and/or a ? adrenergic receptor inhibitor to inhibit tumor initiation are provided. Also provided are pharmaceutical compositions for treating or preventing cancer comprising a muscarinic receptor inhibitor and/or a ? adrenergic receptor inhibitor.
    Type: Application
    Filed: November 24, 2011
    Publication date: October 30, 2014
    Applicant: Icahn School of Medicine at Mount Sinai
    Inventors: Paul S. Frenette, Claire Magnon
  • Publication number: 20140323399
    Abstract: Methods and compositions for treating a blood glucose condition involve identifying a suitable subject and administering an effective amount of a composition that contains one or more of an opioid antagonist, an anticonvulsant, and a psychotherapeutic agent. The compositions can include insulin. In some embodiments, such methods and compositions can be used to modulate a blood glucose level. In preferred embodiments, such methods and compositions are useful for increasing a subject's sensitivity to insulin.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Michael A. Cowley, Anthony A. McKinney, Gary Tollefson
  • Publication number: 20140323472
    Abstract: The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Inventor: Sveinbjorn Gizurarson
  • Publication number: 20140315894
    Abstract: The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 23, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
    Inventors: Dan Theodorescu, Michael Fitzpatrick Wempe, David Ross, Samy Meroueh, Martin A. Schwartz, Phillip Reigan
  • 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: 8853203
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: August 22, 2013
    Date of Patent: October 7, 2014
    Assignee: Novartis AG
    Inventors: Dirk Behnke, David Carcache, Peter Ertl, Manuel Koller, David Orain
  • Publication number: 20140296218
    Abstract: The present invention relates in some aspects to super-enhancers and related compositions, methods, and agents that are useful for modulating expression of cell type-specific genes that are required for maintenance of cell identity (e.g., embryonic stem cell identity) or maintenance of a disease state (e.g., cancer).
    Type: Application
    Filed: October 25, 2013
    Publication date: October 2, 2014
    Applicant: Whitehead Institute for Biomedical Research
    Inventors: Richard A. Young, Warren Whyte, Denes Hnisz, Jakob Loven, Heather Hoke, David Orlando, Charles Y. Lin, Tony Lee
  • Publication number: 20140296219
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Application
    Filed: November 14, 2013
    Publication date: October 2, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Patent number: 8846663
    Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: September 30, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra H. Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
  • Patent number: 8846661
    Abstract: The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: September 30, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael R. Schrimpf, Kevin B. Sippy
  • Patent number: 8846662
    Abstract: The invention relates to a pharmaceutical composition characterized in that it comprises a benzodiazapine and/or benzodiazapine derivative, and a non-ionic solubilizer, and induces in said combination an analogous effect to an opiate, described as a Straub phenomenon.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: September 30, 2014
    Assignee: Dr. Franz Koehler Chemie GmbH
    Inventor: Rainer Hoernecke
  • Publication number: 20140288054
    Abstract: This invention relates to genetic markers of mental illness, e.g., schizophrenia (SZ), and methods of use thereof.
    Type: Application
    Filed: October 29, 2013
    Publication date: September 25, 2014
    Applicant: SureGene, LLC
    Inventors: Mark David Brennan, Timothy Lynn Ramsey
  • Publication number: 20140271922
    Abstract: The present invention generally relates to the neuroprotective activity of condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine. These compounds are suitable as co-medicaments for the prevention and/or treatment of drug-induced neurotoxic effects in general and neurotoxic side effects during cancer treatments with cytostatic drugs such as platinum-derivatives, e.g. cis-, carbo- and oxaliplatin, taxanes, bleomycin, cyclophosphamide and vincristine etc. Further, these compounds have an intrinisic anti-cancer activity on their own due to PARP-1 inhibition, which prevents NADH depletion in oxidative metabolism of healthy cells thus preventing the shift to anoxygenic, glycolytic metabolism present in many types of tumour cells thus eliminating this crucial metabolic advantage favouring tumour growth.
    Type: Application
    Filed: October 17, 2013
    Publication date: September 18, 2014
    Applicant: PROTEOSYS AG
    Inventor: Andre SCHRATTENHOLZ
  • Publication number: 20140275042
    Abstract: Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyridine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 18, 2014
    Inventors: YAMILA VERDECIA REYES, Estael Ochoa Rodríguez, Alberto Ruiz Reyes, Yanier Nuñez Figueredo, Carmen Carillo Domínguez, Juan Enrique Tacoronte Morales, Livan Lázaro Alba Gutiérrez, Gilberto Lázaro Pardo Andreu
  • Publication number: 20140275019
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • Patent number: 8835424
    Abstract: In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: September 16, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: James Cook, Shengming Huang, Rahul Edwankar, Ojas A. Namjoshi, Zhi-Jian Wang
  • Publication number: 20140256709
    Abstract: The present invention is directed to CNS pharmaceutical compositions and methods of use. The pharmaceutical compositions comprise a CNS active agent and preferably at least two vagal neuromodulators, one of which is a mechanoreceptor stimulator. The vagal neuromodulators are preferably in an amount sufficient to reduce a somnolence side-effect of the CNS active agent without changing its therapeutic efficacy/activity. The invention further encompasses a method of reducing CNS active agent side-effects. The method typically comprises oral administration of at least one CNS active agent to a patient at the conventionally accepted dose; and administration of at least two vagal neuromodulators to the patient so that at least one neuromodulator is administered or released from dosage form after the CNS active agent is administered and/or released.
    Type: Application
    Filed: May 19, 2014
    Publication date: September 11, 2014
    Applicant: TARGIA PHARMACEUTICALS
    Inventor: Sabina Glozman
  • Patent number: 8828993
    Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: September 9, 2014
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Moshe Portnoy, Irit Gil-Ad, Avraham Weizman
  • Publication number: 20140248378
    Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 4, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
  • Patent number: 8822453
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: September 2, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Takashi Oshiyama, Tsuyoshi Nagase, Masataka Ueda, Kuninori Tai
  • Publication number: 20140243286
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140242063
    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: October 10, 2013
    Publication date: August 28, 2014
    Applicant: VALEANT LABORATORIES INTERNATIONAL BERMUDA
    Inventors: Andrew John DUFFIELD, Graham JACKSON, Steven E. FRISBEE
  • Publication number: 20140243322
    Abstract: Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140243321
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Applicant: Coferon, Inc.
    Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
  • Publication number: 20140234443
    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: March 10, 2014
    Publication date: August 21, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Peter R. GUZZO, David D. MANNING, William EARLEY
  • Publication number: 20140235621
    Abstract: A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lymphoid leukemia is provided.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: Eli Lilly and Company
    Inventor: Marcio Chedid
  • Patent number: 8809321
    Abstract: The present invention provides a compound of general formula A, useful as potential anticancer agents against eleven human cancer cell lines. The present invention further provides a process for the preparation of diaryl ether linked pyrrolo[2,1-c][1,4]benzodi azepine conjugates attached through different alkane spacers of general formula A.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: August 19, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmed Kamal, Arutla Viswanath, Jayanti Naga Srirama Chandra Murty, Earla Vijaya Bharathi, Gadupudi Ramakrishna, Farheen Sulthana
  • Patent number: 8809322
    Abstract: The present invention provides a liquid pharmaceutical composition comprising a therapeutic agent and an alkoxy-polyethylene glycol, for example, methoxy-polyethylene glycol, for administration of the therapeutic agent to the mammal. The compositions can be applied to a membrane, for example, a nasal membrane during intranasal administration. The invention also provides methods of administering such compositions to a mammal.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: August 19, 2014
    Assignees: Hananja EHF, University of Iceland
    Inventor: Sveinbjorn Gizurarson
  • Publication number: 20140228355
    Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 14, 2014
    Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine, University of Medicine and Dentistry New Jersey Medical School
  • Publication number: 20140228320
    Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):
    Type: Application
    Filed: April 15, 2014
    Publication date: August 14, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
  • Patent number: 8802668
    Abstract: A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lymphoid leukemia is provided.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: August 12, 2014
    Assignee: Eli Lilly and Company
    Inventor: Marcio Chedid
  • Publication number: 20140213575
    Abstract: The invention relates to 6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepines, in particular for therapeutic purposes, pharmaceutical agents and use thereof in therapy, in particular for the prevention and treatment of tumour diseases.
    Type: Application
    Filed: August 27, 2012
    Publication date: July 31, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Norbert Schmees, Joachim Kuhnke, Bernard Haendler, Philip Lienau, Amaury Ernesto Fernandez-Montalvan, Pascale Lejeune, Stephan Siegel, William Scott
  • Publication number: 20140206667
    Abstract: The invention relates to methods and compositions for treating schizophrenia or bipolar disorder (in particular, mania) by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an antipsychotic or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In some embodiments, the methods and the compositions are for treating one or more positive and/or negative symptoms, as well as cognitive impairment, associated with schizophrenia or bipolar disorder (in particular, mania).
    Type: Application
    Filed: November 14, 2013
    Publication date: July 24, 2014
    Inventor: Michela Gallagher
  • Publication number: 20140206674
    Abstract: The invention relates to a pharmaceutical combination of 2-aminoethanesulfonic acid with a pharmaceutical agent such as an antihypertensive agent and the use of 2-aminoethanesulfonic acid in a method to lower the bilirubin level in the blood.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Markus ZWICKL
  • Publication number: 20140199260
    Abstract: Compositions and methods for the treatment of HIV are provided.
    Type: Application
    Filed: January 29, 2014
    Publication date: July 17, 2014
    Inventors: Terri H. Finkel, Jiangfang Wang, Gerd Blobel, Stephan Kadauke
  • Publication number: 20140200199
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. 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 and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Patent number: 8778933
    Abstract: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
    Type: Grant
    Filed: June 19, 2013
    Date of Patent: July 15, 2014
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Toshihiro Takahashi, Masatoshi Ushioda, Toshiyasu Imai, Kazuhike Inoue
  • Patent number: 8778932
    Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or an alkyl group; R2 represents an alkyl group; R3 represents an aryl or heteroaryl group. Medicinal products containing the same which are useful in the treatment or prevention of psychiatric and neurological disorders characterized by cognitive deficits.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: July 15, 2014
    Assignees: Les Laboratoires Servier, Egis Gyogyszergyar Nyrt
    Inventors: István Ling, József Barkóczy, Ferenc Antoni, István Gascályi, György Lévay, Michael Spedding, László Hársing
  • Publication number: 20140194388
    Abstract: A pharmaceutical composition comprising a CHK inhibitor, and an Hsp90 inhibitor according to the following formulae or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.
    Type: Application
    Filed: May 25, 2012
    Publication date: July 10, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: David Proia, Suqin He
  • Publication number: 20140194409
    Abstract: The present invention relates to 4-((1R,3S)-6-chloro-3-phenyl-indan-1yl)-1,2,2-trimethyl-piperazine and the salts thereof with activity at dopamine D1 and D2 receptors as well as the serotonin 5HT2 receptor for the treatment of diseases in the central nervous system in a once weekly dosing regime.
    Type: Application
    Filed: June 20, 2012
    Publication date: July 10, 2014
    Applicant: H. Lundbeck A/S
    Inventors: René Holm, Lone Bruun
  • Patent number: 8772281
    Abstract: A method of screening a compound having a hypoglycemic effect (hereinafter referred to as “hypoglycemic compound”), a remedy for diabetes which contains a compound having a novel function mechanism, etc. More specifically speaking, a method of screening a hypoglycemic compound capable of binding to the ? subunit of a trimeric GTP-binding protein, a remedy for diabetes comprising a hypoglycemic compound, which is characterized by being capable of binding to the ? subunit of a trimeric GTP-binding protein, as the active ingredient, etc.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: July 8, 2014
    Assignee: Ajinomoto Co., Inc.
    Inventors: Naoyuki Fukuchi, Satoru Okamoto, Wataru Miyanaga, Sen Takeshita, Masaru Takayanagi, Yumiko Fukuda, Takao Ikenoue, Naoyuki Yamada, Naoko Arashida
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Publication number: 20140170112
    Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.
    Type: Application
    Filed: March 8, 2012
    Publication date: June 19, 2014
    Applicant: VICUS THERAPEUTICS, LLC
    Inventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
  • Publication number: 20140171383
    Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.
    Type: Application
    Filed: June 28, 2013
    Publication date: June 19, 2014
    Inventors: Daniel J. ABRAMS, Raymond Bunch, Tom Anchordoquy