Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
  • Publication number: 20140171422
    Abstract: Provided are a compound represented by general formula (I), or the pharmaceutically acceptable salt thereof, (wherein Ra represents a hydrogen atom or the like, R1 and R2 may be the same or different, and each represents a hydrogen atom, optionally substituted lower alkyl or cycloalkyl, or R1 and R2 are combined together with the adjacent nitrogen atom thereto to form nitrogen-containing heterocyclic group, and Z represents a bicyclic heterocyclic group in which optionally substituted two six-membered rings are fused to each other, or the like) and the like.
    Type: Application
    Filed: May 10, 2012
    Publication date: June 19, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Nobumasa Otsubo, Shuko Okazaki, Yukihito Tsukumo, Kyoichiro Iida, Masayoshi Nakoji
  • Publication number: 20140163013
    Abstract: A P2X4 receptor antagonist such as paroxetine, a diazepinedione derivative having the following formula (IX) is used as an agent for preventing or treating neuropathic pain associated with Guillain-Barré syndrome: wherein R1 is hydrogen, a C1-8 alkyl group, or the like; each of R2 and R3 is hydrogen, a C1-8 alkyl group, or the like; each of R4 and R5 is hydrogen or the like; and W is a five-membered or six-membered heterocyclic ring optionally having one or more substituents and comprising one to four nitrogen atoms as the members of the ring.
    Type: Application
    Filed: May 25, 2012
    Publication date: June 12, 2014
    Inventors: Toshiyasu Imai, Toru Kawasaki, Toru Ogawa, Kazuhide Inoue
  • Publication number: 20140162964
    Abstract: Disclosed is a new use for sphingosine-1-phosphate (S1P) receptor agonists in the treatment of progressive dementia or brain degenerative diseases.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 12, 2014
    Applicant: NOVARTIS AG
    Inventors: Volker Brinkmann, Nicole Kaneider, Christian J. Wiedermann
  • Publication number: 20140163014
    Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, 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: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
  • Patent number: 8748419
    Abstract: Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: June 10, 2014
    Assignee: Theracos, Inc.
    Inventors: Brian Seed, Jordan Mechanic
  • Publication number: 20140155388
    Abstract: An abuse deterrent pharmaceutical composition including a pharmaceutically active ingredient; an acid soluble ingredient; and a buffering ingredient; wherein the acid soluble ingredient and the buffering ingredient retard release of the active pharmaceutical ingredient when the composition is ingested in excess of an intended dosage.
    Type: Application
    Filed: November 27, 2013
    Publication date: June 5, 2014
    Applicant: Acura Pharmaceuticals, Inc.
    Inventors: Albert W. BRZECZKO, R. Gary HOLLENBECK
  • Patent number: 8735389
    Abstract: Provided are methods of treating psychological diseases and conditions by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: May 27, 2014
    Assignee: Theracos, Inc.
    Inventors: Brian Seed, Jordan Mechanic
  • Publication number: 20140142090
    Abstract: The present invention is directed to novel pyrrolobenzodiazepine dimers and methods of using the dimers in the treatment of proliferative diseases.
    Type: Application
    Filed: November 13, 2013
    Publication date: May 22, 2014
    Applicant: SPIROGEN SARL
    Inventors: Philip Wilson Howard, Stephen John Gregson, Luke Masterson
  • Patent number: 8729070
    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: Grant
    Filed: August 20, 2010
    Date of Patent: May 20, 2014
    Assignee: Targia Pharmaceuticals
    Inventor: Sabina Glozman
  • Publication number: 20140135316
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: May 4, 2012
    Publication date: May 15, 2014
    Applicant: CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, Victor S. Gehling, Michael C. Hewitt, Alexander M. Taylor, Jean-Christophe Harmange
  • Patent number: 8722665
    Abstract: The present invention provides a compound of general formulae (8a-i), (11a-i), (14a-i), and (17a-i), useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of Cinnamido-pyrrolo[2,1-c][1,4]benzodiazepines of general formulae (8a-i), (11a-i), (14a-i), and (17a-i).
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 13, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Balakishan Gorre, Ramakrishna Gadupudi, Sreekanth Kokkonda, Rajender
  • Patent number: 8722666
    Abstract: A drug for sedating a patient, and especially a smoker, during eye surgery. The drug includes a sedative such as midazolam in a mix with nicotine. The mixture is injected into the patient prior to the eye surgery.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: May 13, 2014
    Inventor: Walter J. Cukrowski
  • Patent number: 8722085
    Abstract: Methods and systems for administration of pharmaceuticals using a unit dosage package that includes a first unit dosage that has a first drug and a second drug, a second unit dosage that has the first drug and the second drug, where the second unit dosage includes a different amount of the second drug than the first unit dosage and a unit dosage package is configured to hold the first unit dosage and the second unit dosage. In preferred embodiments the methods and systems are used for administration of weight loss medications.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: May 13, 2014
    Assignee: Orexigen Therapeutics, Inc.
    Inventors: Anthony McKinney, Gary Tollefson, Eckard Weber, Rick Soltero
  • 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: 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
  • 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
  • Patent number: 8710046
    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: Grant
    Filed: June 30, 2010
    Date of Patent: April 29, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, David D. Manning, William Earley
  • Patent number: 8703764
    Abstract: The invention provides, in part, methods and compositions for treating psychiatric disorders, for example, apathy, dementia, or depression, using combination therapies such a monoamine oxidase inhibitor or a selective serotonin reuptake inhibitor in combination with an anti-psychotic agent.
    Type: Grant
    Filed: May 19, 2006
    Date of Patent: April 22, 2014
    Inventor: Leslie James Sheldon
  • Publication number: 20140107107
    Abstract: A solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein X is a halogen, R1 is C1-C4 alkyl, R2 is C1-C4 alkyl, a is an integer of 1-4, R3 is C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl optionally having substituent(s), or heteroaryl optionally having substituent(s), a pharmaceutically acceptable salt thereof or a hydrate thereof; and a pharmaceutically acceptable polymer. In one embodiment, the pharmaceutically acceptable polymer is HPMCAS. The solid dispersion may be made by spray drying.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 17, 2014
    Inventors: Jeff GAUTSCHI, Ryan MINIKIS
  • Publication number: 20140107108
    Abstract: Disclosed is a composition comprising alprazolam for treating primary insomnia and insomnia associated with anxiety states and the corresponding use and method comprising the administration of alprazolam sublingual tablets having a disintegration time lower than 30 seconds and having the alprazolam preferably in non-crystalline or partially crystalline form according to the X-ray diffraction crystallography expanded for the position delta 9-12.5 (2 theta), to a patient suffering from said disorder. There is also disclosed a method for preparing a composition according to the invention, where the alprazolam is solved in a pharmaceutical acceptable solvent and a binder, preferably polyvinylpyrrolidone, is incorporated to the solution.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 17, 2014
    Applicant: Laboratorios Bago S.A.
    Inventor: Mario Atilio Los
  • 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.
  • Patent number: 8697688
    Abstract: Pyrrolobenzodiazepine dimers I having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: April 15, 2014
    Assignees: Seattle Genetics Inc., Spirogen Sarl
    Inventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien, Scott Jeffrey, Patrick Burke, Peter Senter
  • Publication number: 20140100183
    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: April 12, 2013
    Publication date: April 10, 2014
    Applicant: The Regents of the University of Colorado, a body corporate
    Inventors: Daniel J. ABRAMS, Raymond BUNCH, Tom ANCHORDOQUY, Karen E. STEVENS
  • Patent number: 8691811
    Abstract: The present invention provides a compound of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i.
    Type: Grant
    Filed: July 13, 2009
    Date of Patent: April 8, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Earla V. Bharathi, Dudekula Dastagiri, Jonnala S. Reddy, Arutla Viswanath
  • Publication number: 20140094452
    Abstract: This application discloses liquid compositions for administration to a patient comprising midazolam and a pharmaceutically acceptable carrier, wherein the pH of the composition is about 6 or higher, the composition comprises less than about 200 mg/ml cyclodextrin, and at least about 50% of the midazolam is present in solution. Uses of these compositions are also disclosed.
    Type: Application
    Filed: May 2, 2013
    Publication date: April 3, 2014
    Applicant: Special Products, Ltd.
    Inventor: Special Products, Ltd.
  • Publication number: 20140088089
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds, such as those in formulas (V)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The present invention is further directed to methods of preparing a conjugate of a cell-binding agent and a cytotoxic compound. The methods comprise the use of an imine reactive compound to enable efficient conjugations of cytotoxic compounds with cell binding agents.
    Type: Application
    Filed: February 15, 2012
    Publication date: March 27, 2014
    Applicant: ImmunoGen, INC.
    Inventor: Ravi V.J. Chari
  • Publication number: 20140080815
    Abstract: The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 10 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
    Type: Application
    Filed: November 7, 2011
    Publication date: March 20, 2014
    Applicant: PAION UK LTD.
    Inventors: Karin Wilhelm-Ogunbiyi, Keith Borkett, Gary Stuart Tilbrook, Hugh Wiltshire
  • Publication number: 20140080813
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Inventor: Wilfried Braje
  • Publication number: 20140080816
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margot Bakker, Viktor Lakics, Carolin Hoft, Ruxu Xu, Xiaona Zhao
  • Publication number: 20140080814
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventor: Wilfried Braje
  • Patent number: 8673896
    Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, 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: April 22, 2011
    Date of Patent: March 18, 2014
    Assignee: AbbVie Inc.
    Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
  • 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: 20140073562
    Abstract: A nasal delivery device for and method of delivering a substance, preferably comprising oxytocin, non-peptide agonists thereof and antagonists thereof, preferably as one of a liquid, as a suspension or solution, or a powder to the nasal airway of a subject, preferably the posterior region of the nasal airway, and preferably the upper posterior region of the nasal airway which includes the olfactory bulb and the trigeminal nerve, and preferably in the treatment of neurological conditions and disorders.
    Type: Application
    Filed: March 15, 2012
    Publication date: March 13, 2014
    Applicant: OPTINOSE AS
    Inventor: Per Gisle Djupesland
  • Publication number: 20140066435
    Abstract: Pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: SPIROGEN SARL
    Inventors: Philip Wilson HOWARD, Luke MASTERSON, Arnaud TIBERGHIEN, Scott JEFFREY, Patrick BURKE, Peter SENTER
  • Patent number: 8664216
    Abstract: The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: March 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Erwin Goetschi, Roland Jakob-Roetne, Raffaello Masciadri, Emmanuel Pinard, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • Publication number: 20140057902
    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: Application
    Filed: August 22, 2013
    Publication date: February 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Dirk BEHNKE, David CARCACHE, Peter ERTL, Manuel KOLLER, David ORAIN
  • 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: 20140051689
    Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.
    Type: Application
    Filed: October 24, 2013
    Publication date: February 20, 2014
    Applicant: Biota Scientific Management Pty Ltd.
    Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
  • Publication number: 20140045827
    Abstract: The present invention is concerned with novel antifungal 5,6-dihydro-4H-pyrrolo-[1,2-a][1,4]benzodiazepines and 6H-pyrrolo[1,2-a][1,4]benzodiazepines substituted with heterocyclic derivatives of Formula (I) wherein R1, R2, R3, R4 and Het have the meaning defined in the claims. The compounds according to the present invention are active mainly against dermatophytes and systemic fungal infections. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Application
    Filed: May 3, 2012
    Publication date: February 13, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit, Koen Jan Ludovicus Augustyns
  • Publication number: 20140045915
    Abstract: Disclosed herein are methods for assaying a biological sample from a subject by analyzing components of microvesicle fractions in aid of risk, diagnosis, prognosis or monitoring of or directing treatment of the subject for, a disease or other medical condition in the subject. Also disclosed are methods of treatment and identifying biomarkers using a microvesicle fraction of a subject. Kits, pharmaceutical compositions, and profiles related to the methods are also disclosed.
    Type: Application
    Filed: August 31, 2011
    Publication date: February 13, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Johan Karl Olov Skog, Leonora Balaj, Mikkel Noerholm, Xandra O. Breakefield
  • Patent number: 8648063
    Abstract: An improved method for treating gastric cancer, ovarian cancer, non-small cell lung cancer, or colorectal cancer in a patient is described, as well as pharmaceutical compositions useful for the method and a process for preparing said compositions.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: February 11, 2014
    Assignee: Eli Lilly and Company
    Inventors: Marcio Chedid, Thomas Albert Engler
  • 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
  • Patent number: 8642588
    Abstract: The invention relates to esylate salts of the compound of formula (I): Methods of preparing the salts, and their use as medicaments, in particular for sedative or hypnotic, anxiolytic, muscle relaxant, or anticonvulsant purposes is also described.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: February 4, 2014
    Assignee: PAION UK Limited
    Inventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
  • Patent number: 8642590
    Abstract: The present invention is concerned with alkylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. alkylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene s of formula I wherein R1, R2 and R3 are as described herein, their manufacture, and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The compounds are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: February 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Patrick Schnider
  • 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: 8637664
    Abstract: A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R2 is selected from —H, —OH, =0, ?CH2, —CN, —R, OR, halo, ?CH—R, O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo, where R and R? are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and YRY, where Y is selected from O, S and NH and R is H or C1-7 alkyl or H and SOxM, where x is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and RE is C1-4 alkyl. The compound is useful for the treatment of proliferative diseases.
    Type: Grant
    Filed: October 5, 2006
    Date of Patent: January 28, 2014
    Assignee: Spirogen SARL
    Inventors: Philip Wilson Howard, David Edwin Thurston, Geoffrey Wells
  • Publication number: 20140024638
    Abstract: The present invention relates to (2S,3R)—N-(2-((3-pyridinyl)methyl)-1-azabicyclo[2.2.2]oct-3-yl)benzofuran-2-carboxamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions, and methods for treating schizophrenia.
    Type: Application
    Filed: January 17, 2012
    Publication date: January 23, 2014
    Applicant: TARGACEPT, INC.
    Inventors: Merouane Bencherif, Geoffrey C. Dunbar, David A. Hosford, Gregory J. Gatto, Terry Hauser, Kristen G. Jordan, Anthony Carl Segreti
  • Patent number: 8633185
    Abstract: Compounds of the formula I: or solvate thereof, wherein: R2 is an optionally substituted C5-20 aryl group; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; R? is a C3-12 alkylene group, which chain may be interrupted by one or more heteroatoms and/or aromatic rings; X is selected from O, S, or NH; z is 2 or 3; M is a monovalent pharmaceutically acceptable cation; R2?, R6?, R7?, R9?, X? and M? are selected from the same groups as R2, R6, R7, R9, X and M respectively, or M and M? may together represent a divalent pharmaceutically acceptable cation.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: January 21, 2014
    Assignee: Spirogen Sarl
    Inventors: Philip Wilson Howard, Zhizhi Chen, Stephen John Gregson
  • 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