Bicyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/221)
  • Publication number: 20140128378
    Abstract: The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: UCB Pharma GmbH
    Inventor: Thomas STÖHR
  • Publication number: 20140128379
    Abstract: The present invention provides pharmaceutical compositions for intranasal delivery of a benzodiazepine. The composition may contain a therapeutically effective amount of a benzodiazepine or a pharmaceutically acceptable salt thereof, and a permeation enhancer. The permeation enhancer may be propylene glycol or a Hsieh permeation enhancer. The present compositions have excellent bioavailability. After administration of the present compositions, therapeutically effective plasma levels of the benzodiazepine may be achieved rapidly. The present pharmaceutical composition may be used to treat a patient suffering from anxiety, epilepsy, insomnia, agitation, seizures, muscular disorders, alcohol dependence, and drug withdrawal.
    Type: Application
    Filed: March 29, 2012
    Publication date: May 8, 2014
    Applicant: CPEX Pharmaceuticals, Inc.
    Inventors: Nils Bergenhem, Carl Reppucci, Zhengmao Li
  • Publication number: 20140128381
    Abstract: The present invention generally relates to intranasal pharmaceutical compositions comprising a benzodiazepine and methods of use thereof that can provide a therapeutic effect without a decrease in blood pressure and/or pulse after administration of the pharmaceutical composition.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Inventors: Gary Bream, Moise A. Khayrallah, Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
  • Publication number: 20140128377
    Abstract: The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: UCB Pharma GmbH
    Inventor: Thomas STÖHR
  • Publication number: 20140128380
    Abstract: The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: Mimetica Pty Ltd
    Inventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
  • Patent number: 8716492
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: May 6, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Patent number: 8716279
    Abstract: The present invention includes benzodiazepine compositions formulated for intranasal administration, comprising a binary solvent system comprising a first solvent in which the benzodiazepine is soluble, the first solvent capable of penetrating nasal mucosal tissue, and a second solvent in which the benzodiazepine in less soluble. The compositions of the present invention may be used to treat a variety of disorders including, but not limited to, panic attacks, muscle spasms, anxiety, and seizures. In one aspect, the present invention relates to a fast-acting, clonazepam composition for transnasal administration that can be used for the treatment of seizure clusters.
    Type: Grant
    Filed: August 27, 2007
    Date of Patent: May 6, 2014
    Assignee: Jazz Pharmaceuticals, Inc.
    Inventors: Gene Jamieson, Michael Des Jardin, Clark Allphin, Sigridur Olafsdottir
  • Publication number: 20140120185
    Abstract: The present invention provides a medicament having a wider treatment spectrum, causing a fewer side effects and superior in tolerability and safety, as compared to known typical antipsychotic agents and atypical antipsychotic agents. The present invention related to a medicament containing (I) a compound which is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and (II) at least one drug selected from the group consisting of a mood stabilizer, a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a serotonin and norepinephrine reuptake inhibitor, a noradrenergic and specific serotonergic antidepressant, an antianxiety drug, a tricyclic antidepressant, a tetracyclic antidepressant, an antipsychotic drug and an anti-ADHD drug, in combination.
    Type: Application
    Filed: April 4, 2012
    Publication date: May 1, 2014
    Inventors: Tsuyoshi Hirose, Kenji Maeda, Tetsuro Kikuchi, Masafumi Toda
  • Publication number: 20140107106
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 17, 2014
    Applicant: Affinium Pharmaceuticals, Inc.
    Inventor: Affinium Pharmaceuticals, Inc.
  • Publication number: 20140105852
    Abstract: A process for making cross-linked polysaccharide gels, particularly cross-linked hyaluronic acid gels, under basic conditions. The resulting gels possess improved degradation characteristics, and are useful in a variety of medical and cosmetic applications.
    Type: Application
    Filed: December 26, 2013
    Publication date: April 17, 2014
    Applicant: Ultraceuticals R&D Pty. Limited
    Inventors: Simone Charlotte Vonwiller, Geoffrey Kenneth Heber
  • Patent number: 8697673
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: April 15, 2014
    Assignee: Pfizer Inc.
    Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
  • Publication number: 20140093559
    Abstract: A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.
    Type: Application
    Filed: November 1, 2013
    Publication date: April 3, 2014
    Applicant: GRUNENTHAL GMBH
    Inventors: JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
  • Patent number: 8685962
    Abstract: Articles of manufacturing (such as tobacco products), methods, devices and compositions for preventing or reducing tobacco-associated damage and/or disorders associated with oxidative stress in a subject, and which utilize a TSPO receptor ligand (such as diazepam), are disclosed.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: April 1, 2014
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Moshe Gavish, Rafael M. Nagler
  • Patent number: 8685451
    Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: April 1, 2014
    Assignee: Osmotica Kereskedelmi és Szolgáltató KFT
    Inventors: Fernando G. Toneguzzo, Glenn A. Meyer, Marcelo A. Ricci, Marcelo A. Coppari, Ana C. Pastini, Gustavo A. Fischbein
  • Publication number: 20140087992
    Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.
    Type: Application
    Filed: September 20, 2013
    Publication date: March 27, 2014
    Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
  • Publication number: 20140088085
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.
    Type: Application
    Filed: January 12, 2012
    Publication date: March 27, 2014
    Applicants: ARRAY BIOPHARMA, INC, VENTIRX PHARMACEUTICALS, INC
    Inventors: Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones, James Jeffry Howbert, Robert Hershberg, Joseph P. Lyssikatos, Hong Woon Yang
  • Publication number: 20140088091
    Abstract: The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as neuromuscular blocker or skeletal muscle relaxant.
    Type: Application
    Filed: April 11, 2012
    Publication date: March 27, 2014
    Applicant: KING SAUD UNIVERSITY
    Inventors: Adel S. El-Azab, Hussein I. El-Subbagh, Khalid A. Al-Rashood, Kamal E. H. El-Taher, Mohamed A. Al-Omar, Ghada S. Hassan, Fatmah A. Al-Omary, Alaa A.-M. Abdelaziz, Mohamed M. Hefnawy
  • Publication number: 20140088090
    Abstract: The present invention relates to a compound of formula 1, a pharmaceutical composition containing the compound, a method for its preparation as well as the use of the compound as hypnotic agent or anesthetic agent.
    Type: Application
    Filed: April 4, 2012
    Publication date: March 27, 2014
    Applicant: King Saud University
    Inventors: Ghada S. Hassan, Hussein I. El-Subbagh, Mohamed A. Al-Omar, Kamal E.H. El-Taher, Khalid A. Al-Rashood, Abdulrahman M. Al-Obaid, Adel S. El-Azab, Alaa A.M. Abdelaziz, Fatmah A. Al-Omary, Mohamed M. Hefnawy
  • Publication number: 20140079812
    Abstract: Compositions and methods for the treatment of cancer are provided.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 20, 2014
    Applicant: Lankenau Institute for Medical Research
    Inventors: Iraimoudi S. Ayene, George C. Prendergast
  • Publication number: 20140080780
    Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.
    Type: Application
    Filed: May 21, 2012
    Publication date: March 20, 2014
    Inventor: Benjamin WOLOZIN
  • Publication number: 20140079666
    Abstract: In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: May 5, 2012
    Publication date: March 20, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Thomas R. Webb, Vincent A. Boyd
  • Patent number: 8673897
    Abstract: The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: March 18, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Alexander Ross Hurd, Chad Alan Van Huis
  • Patent number: 8673898
    Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: March 18, 2014
    Assignee: Array BioPharma Inc.
    Inventors: George A. Doherty, Zachary Jones
  • Publication number: 20140073633
    Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 13, 2014
    Applicants: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENE ALT., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE
    Inventors: Daniel GILLET, Julien BARBIER, Ludger JOHANNES, Bahne STECHMANN, Siau-Kun BAI
  • Publication number: 20140072623
    Abstract: A method of treatment for epilepsy and other disease states is described, which comprises the delivery of gabapentin in a gastric retained dosage form.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 13, 2014
    Applicant: DEPOMED, INC.
    Inventors: Bret Berner, Sui Yuen Eddie Hou
  • Publication number: 20140072536
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of Nevada
    Inventors: Ryan Wuebbles, Dean Burkin
  • Publication number: 20140073574
    Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
  • Publication number: 20140066436
    Abstract: The present invention relates to a compound of formula (VII)I, or pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4? are each independently H or alkyl; or R4 and R4? together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.
    Type: Application
    Filed: June 5, 2013
    Publication date: March 6, 2014
    Inventors: Jonathan James HOLLICK, Stuart Donald JONES, Claire June FLYNN, Michael George THOMAS
  • Patent number: 8664217
    Abstract: The present invention provides a novel benzodiazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The benzodiazepine compound of the invention is represented by General Formula (1) wherein R1, R2, R3, and R4 are each independently hydrogen or lower alkyl; R2 and R3 may be linked to form lower alkylene; Al is lower alkylene optionally substituted with one or more hydroxy; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; XA and XB are each independently bond, lower alkylene, etc.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: March 4, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Kunio Oshima, Takashi Oshiyama, Shinichi Taira, Yasuhiro Menjo, Hokuto Yamabe, Shuuji Matsumura, Masataka Ueda, Yasuo Koga, Kuninori Tai, Sunao Nakayama, Toshiyuki Onogawa, Kenji Tsujimae
  • Publication number: 20140057903
    Abstract: This invention provides methods for identifying genes associated with cognitive impairment and for identifying compounds useful in the treatment of cognitive impairment. The methods can in particular be used to identify genes associated with, and compounds useful in treating, cognitive impairment in aging.
    Type: Application
    Filed: July 10, 2013
    Publication date: February 27, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Michela Gallagher, Rebecca Haberman
  • Publication number: 20140050789
    Abstract: Provided are compositions comprising a benzodiazepine and a neurosteroid, containing one or both of the benzodiazepine and the neurosteroid in a subtherapeutic dose, and administration of such compositions for mitigation of an epileptic seizure. Further provided are compositions comprising a benzodiazepine, a neurosteroid, and an NMDA blocker, and administration of such compositions for mitigation of an epileptic seizure.
    Type: Application
    Filed: August 12, 2013
    Publication date: February 20, 2014
    Applicant: The Regents of the University of California
    Inventors: Michael A. ROGAWSKI, Isaac N. PESSAH, Zhengyu CAO, Pamela J. LEIN
  • Publication number: 20140051681
    Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.
    Type: Application
    Filed: May 3, 2013
    Publication date: February 20, 2014
    Inventors: David John AUGERI, Jeffrey Thomas BAGDANOFF, Simon David Peter BAUGH, Marianne CARLSEN, Kenneth Gordon CARSON, John Anthony GILLERAN, Wei HE, Tamas ORAVECZ, Konstantin SALOJIN, Leonard SUNG
  • Publication number: 20140050797
    Abstract: The present invention is directed to pharmaceutical compositions and dosage forms comprising TPR beads, wherein said TPR beads comprise a solid dispersion of at least one active pharmaceutical ingredient in at least one solubility-enhancing polymer, and a TPR coating comprising a water insoluble polymer and an enteric polymer, wherein the active pharmaceutical ingredient comprises a weakly basic active pharmaceutical ingredient having a solubility of not more than 100 ?g/mL at pH 6.8.
    Type: Application
    Filed: June 6, 2013
    Publication date: February 20, 2014
    Inventors: Gopi VENKATESH, Luigi BOLTRI, Italo COLOMBO, Jin-Wang LAI, Flavio FABIANI, Luigi MAPELLI
  • Publication number: 20140051690
    Abstract: There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anticonvulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: SK Biopharmaceuticals Co., Ltd.
    Inventors: Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
  • Publication number: 20140051679
    Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERISTY HEALTH NETWORKS
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
  • Publication number: 20140038935
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: January 21, 2013
    Publication date: February 6, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20140038947
    Abstract: Benzodiazepine compounds, and methods for using those compounds are provided. Some of the benzodiazepine compounds include 1,4-benzodiazepine-2-one and 1,4-benzodiazepine-2,5-dione compounds of structures: wherein R1, R2, R3 and R4 are as defined. The invention also includes enantiomers, pharmaceutically acceptable salts, prodrugs or derivatives of the benzodiazepine compounds. Any one or more of these benzodiazepine compounds can be used to treat a variety of dysregulatory disorders related to cellular death. Such disorders include autoimmune disorders, inflammatory conditions, hyperproliferative conditions, viral infections, and atherosclerosis. In addition, the above compounds can be used to prepare medicaments to treat the above-described dysregulatory disorders. The benzodiazepines can also be used in drugs screening assays and other diagnostic methods.
    Type: Application
    Filed: May 17, 2013
    Publication date: February 6, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Anthony W. Opipari, JR.
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • 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
  • Patent number: 8637502
    Abstract: The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: January 28, 2014
    Assignees: Purde Pharma L.P., Shionogi & Co., Ltd.
    Inventors: Kevin C. Brown, R. Richard Goehring
  • Publication number: 20140024641
    Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 23, 2014
    Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
  • Publication number: 20140018352
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: April 26, 2013
    Publication date: January 16, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Francoise Pierard, Jean-Damien Charrier
  • Patent number: 8629136
    Abstract: Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: January 14, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Claude A. Quesnelle, Soong-Hoon Kim, Francis Y. Lee
  • Patent number: 8629137
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: October 2, 2012
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp
  • Publication number: 20140011772
    Abstract: The present invention relates to compositions and methods for the treating and empirically investigating conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity). In particular, the present invention provides compositions and methods for using flufenamic acid in the treatment and empirical investigation of conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity).
    Type: Application
    Filed: June 13, 2013
    Publication date: January 9, 2014
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: Marco Martina, A. Vania Apkarian
  • Publication number: 20140011770
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: September 10, 2013
    Publication date: January 9, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Patent number: 8623857
    Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: January 7, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
  • Publication number: 20140005135
    Abstract: Disclosed is a stable liquid formulation for parenteral injection comprising a biocompatible non-aqueous solvent and a small molecule drug, or a salt thereof, solubilized within the non-aqueous solvent, wherein the liquid formulation comprises less than 10% by weight residual water, and wherein the volume of the liquid formulation to be parenterally injected is from 0.1 ?l to 3 ml.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 2, 2014
    Applicant: XERIS PHARMACEUTICALS, INC.
    Inventors: Steven J. Prestrelski, Nancy Scott
  • Publication number: 20140005173
    Abstract: Compositions and methods for treating psychotic and neurological disorders in a subject are disclosed. The compositions and methods utilize a pharmaceutical compound that reverses or negates the effects of an NMDA receptor antagonist. The compositions and methods are effective in reducing at least catatonic features in the subject.
    Type: Application
    Filed: March 20, 2012
    Publication date: January 2, 2014
    Inventor: James Conour
  • Publication number: 20140004082
    Abstract: A method for treating core binding factor (CBF) leukemia in a subject, comprising administering to a subject having CBF leukemia a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt or ester thereof, that inhibits CBF? and RUNX1 binding in the subject, thereby treating the CBF leukemia.
    Type: Application
    Filed: March 15, 2012
    Publication date: January 2, 2014
    Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Pu Liu, Wei Zheng, Juan Marugan, Noel T. Southall, Lea Cunningham