Tricyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/220)
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Patent number: 8642588Abstract: 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: GrantFiled: July 10, 2007Date of Patent: February 4, 2014Assignee: PAION UK LimitedInventors: Gary Stuart Tilbrook, Louisa Jane Cubitt
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Publication number: 20140030249Abstract: 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: ApplicationFiled: September 27, 2013Publication date: January 30, 2014Applicant: Valeant International BermudaInventors: Andrew John DUFFIELD, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
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Patent number: 8637664Abstract: 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: GrantFiled: October 5, 2006Date of Patent: January 28, 2014Assignee: Spirogen SARLInventors: Philip Wilson Howard, David Edwin Thurston, Geoffrey Wells
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Publication number: 20140024638Abstract: 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: ApplicationFiled: January 17, 2012Publication date: January 23, 2014Applicant: TARGACEPT, INC.Inventors: Merouane Bencherif, Geoffrey C. Dunbar, David A. Hosford, Gregory J. Gatto, Terry Hauser, Kristen G. Jordan, Anthony Carl Segreti
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Patent number: 8633185Abstract: 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: GrantFiled: November 2, 2009Date of Patent: January 21, 2014Assignee: Spirogen SarlInventors: Philip Wilson Howard, Zhizhi Chen, Stephen John Gregson
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Publication number: 20140018349Abstract: This invention provides an oral dosage regimen for the treatment of depression, a pharmaceutically acceptable medication dispensing package containing multiple dosage units of medicaments comprising an oral dosage regimen of D-cycloserine for the treatment of depression, a pharmaceutical composition comprising D-cycloserine formulated for oral administration providing a dosage of 1000 mg/day alone or in combination with antidepressant agents and uses thereof.Type: ApplicationFiled: January 30, 2012Publication date: January 16, 2014Inventors: Uriel Heresco-Levy, Daniel Javitt
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Publication number: 20140018295Abstract: 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: ApplicationFiled: September 14, 2011Publication date: January 16, 2014Applicant: OPTINOSE ASInventor: Per Gisle Djupesland
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Publication number: 20140018606Abstract: Provided herein is the compound RK-33, or a salt, solvate, stereoisomer, or derivative thereof, which is shown to be an inhibitor if the DEAD box helicase DDX3, in mammalian cells. RK-33 is also provided herein for use as a radiation dose sensitizer in a subject suffering from a proliferative disease and undergoing radiation therapy. Methods of treatment of proliferative diseases, such as cancer with a combination of RK-33 and radiotherapy methods such as stereotactic ablative radiotherapy (SABR) are also provided.Type: ApplicationFiled: March 9, 2012Publication date: January 16, 2014Applicant: The Johns Hopkins UniversityInventors: Venu Raman, Phuoc Tran
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Publication number: 20140018352Abstract: 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: ApplicationFiled: April 26, 2013Publication date: January 16, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francoise Pierard, Jean-Damien Charrier
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Publication number: 20140018353Abstract: A method of treating B-cell malignant cancers or T-cell malignant cancers in a mammal by administering to a patient a pharmaceutically acceptable amount of a composition comprising (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo-[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide. The B-cell malignant cancers include diffuse large B-cell lymphoma and splenic marginal zone lymphoma. The T-cell malignant cancers include anaplastic large T-cell lymphoma.Type: ApplicationFiled: June 25, 2013Publication date: January 16, 2014Inventors: Francesco Bertoni, Paola Bonetti
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Publication number: 20140017199Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: July 3, 2013Publication date: January 16, 2014Inventors: Manoj C. Desai, Allen Yu Hong, Hon Chung Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Publication number: 20140011862Abstract: The invention provides compositions, methods, and kits for the treatment of acute myeloid leukemia in a subject.Type: ApplicationFiled: July 3, 2013Publication date: January 9, 2014Applicants: Cold Spring Harbor Laboratory, Dana-Farber Cancer Institute, Inc.Inventors: James Elliott Bradner, Johannes Zuber, Junwei Shi, Christopher R. Vakoc
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Publication number: 20140005169Abstract: 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: ApplicationFiled: December 2, 2011Publication date: January 2, 2014Applicant: CONSTELLATION PHARMACEUTICALSInventors: Brian K. Albrecht, James Edmund Audia, Alexandre Cote, Victor S. Gehling, Jean-Christophe Harmange, Michael Charles Hewitt, Christopher G. Naveschuk, Alexander M. Taylor, Rishi G. Vaswani
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Publication number: 20140005173Abstract: 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: ApplicationFiled: March 20, 2012Publication date: January 2, 2014Inventor: James Conour
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Publication number: 20130345202Abstract: Soluble complexes of flumazenil, methods for the preparation thereof, pharmaceutical compositions including same and use of the compositions for alleviating or counteracting the various types of hypersomnia, drowsiness, residual effects associated with the administration of sleep/hypnotic drugs, alcohol intoxication or hepatic encephalopathy.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Inventor: Shimon Amselem
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Publication number: 20130345201Abstract: The present invention relates to a pharmaceutical combination for the treatment of schizophrenia and acute manic episodes associated with bipolar disorders, which comprises a compound which is active on a trace amine-associated receptor 1 (TAAR1 agonist) and an antipsychotic drug. This combination can reduce metabolic side effects which appear if using an antipsychotic drug alone.Type: ApplicationFiled: July 19, 2013Publication date: December 26, 2013Applicant: Hoffmann-La Roche Inc.Inventors: Marius Hoener, Susanne Raab, Celine Risterucci, Sabine Sewing
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Publication number: 20130338149Abstract: 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: ApplicationFiled: August 21, 2013Publication date: December 19, 2013Inventor: Walter J. Cukrowski
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Patent number: 8609651Abstract: 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: GrantFiled: August 27, 2007Date of Patent: December 17, 2013Assignee: Jazz Pharmaceuticals, Inc.Inventors: Gene Jamieson, Michael Des Jardin, Clark Allphin, Sigridur Olafsdottir
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Publication number: 20130324520Abstract: The present invention provides methods for treating cancer using modulators of retinoid X receptor gamma (RXRG). The ability of RXRG antagonists to disrupt the association of complexes comprising RXRG is demonstrated.Type: ApplicationFiled: February 14, 2012Publication date: December 5, 2013Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Xiaoliang Xu, Suresh Jhanwar
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Patent number: 8598119Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.Type: GrantFiled: May 27, 2009Date of Patent: December 3, 2013Assignee: Intra-Cellular Therapies, Inc.Inventors: Sharon Mates, Allen Fienberg, Lawrence Wennogle
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Publication number: 20130317011Abstract: 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]benzodiazepine conjugates attached through different alkane spacers of general formula A.Type: ApplicationFiled: March 30, 2011Publication date: November 28, 2013Applicant: COUNCIL OF SCIENCE AND INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Arutla Viswanath, Jayanti Naga Srirama Chandra Murty, Earla Vijaya Bharathi, Gadupudi Ramakrishna, Farheen Sulthana
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Patent number: 8592407Abstract: The present invention provides synthesis and in vitro anticancer activity of novel pyrrolo[2,1-c][1,4]benzodiazepine derivatives with dithiocarbamate side chains. The present invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine derivatives with dithiocarbamate side chains of general formula (A) and a process for the preparation thereof.Type: GrantFiled: March 24, 2009Date of Patent: November 26, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Sreekanth Kokkonda, Praveen K. Pogula, Balakishan Gorre
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Patent number: 8591922Abstract: Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.Type: GrantFiled: January 11, 2013Date of Patent: November 26, 2013Assignee: Jazz Pharmacuticals, Inc.Inventors: Clark P. Allphin, Michael DesJardin
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Publication number: 20130309310Abstract: Described are injectable formulations of particulate olanzapine that produce a prolonged duration of action upon administration, and methods of making and using such formulations. The injectable formulations comprise particulate olanzapine.Type: ApplicationFiled: July 24, 2013Publication date: November 21, 2013Applicant: Alkermes Pharma Ireland LimitedInventors: Stephen B. Ruddy, David Czekai, Gary Liversidge, Scott A. Jenkins, Elaine M. Liversidge
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Publication number: 20130309306Abstract: This invention provides methods for the amelioration, termination and/or abortion of a seizure by the intrapulmonary administration of a benzodiazepine, for example, midazolam.Type: ApplicationFiled: December 1, 2011Publication date: November 21, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Michael A. Rogawski, Ashish Dhir
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Publication number: 20130302282Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: October 21, 2011Publication date: November 14, 2013Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Patent number: 8580764Abstract: The present invention provides methods of treating a cell proliferative disorder, such as lung cancer and breast cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound, such as (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, in combination with a therapeutically effective amount of a second anti-proliferative agent, such as gemcitabine.Type: GrantFiled: July 1, 2011Date of Patent: November 12, 2013Assignee: ArQule, Inc.Inventors: Giovanni Abbadessa, Dennis S. France, Chang-Rung Chen, Thomas C. K. Chan
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Publication number: 20130287854Abstract: According to the invention there is provided a method of treating and/or preventing the symptoms of Parkinson's disease comprising delivering apomorphine, optionally in combination with levodopa and/or a dopamine agonist that is not apomorphine, wherein apomorphine is administered by inhalation.Type: ApplicationFiled: November 15, 2011Publication date: October 31, 2013Applicant: VECTURA LIMITEDInventors: Frazer Giles Morgan, Mark Jonathan Main
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Publication number: 20130289019Abstract: One embodiment of an aspect of the present invention is a method for lessening the symptoms of depression, anxiety, and post-traumatic stress disorder comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of depression, anxiety, and post-traumatic stress disorder. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Applicant: Amazing Grace, Inc.Inventor: David T. Chau
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Patent number: 8569288Abstract: The invention relates to new thienotriazolodiazepine derivatives of the formula (1) wherein R1 is CH3, R2 is CH3 or —(CH2)n—R4 or —(CH2)n—O—R4 or —(CH2)n—S—R4 wherein n is 1, 2, 3 or 4 and R4 is CH3, CH2CH3 or CH2CH2OCH3, and R3 is hydrogen or —OCH2O— or —OCH2CH2O— connected to the ortho/meta position or meta/para position of the phenyl ring; or wherein R1 and R2 are hydrogen and R3 is —OCH2O— Or —OCH2CH2O— connected to the ortho/meta position or meta/para position of the phenyl ring; and pharmaceutically acceptable acid addition salts thereof. These compounds and pharmaceutical compositions containing them are useful in the treatment and prevention of atherosclerotic artery diseases, such as myocardial infarction and stroke, and of Alzheimer's disease.Type: GrantFiled: October 29, 2009Date of Patent: October 29, 2013Assignee: CircoMed LLCInventors: Herman Kempen, Daniel Bellus, Barbara Staehelin
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Publication number: 20130281440Abstract: The invention encompasses methods for treating or preventing diseases and disorders associated abnormal cell growth, for example, treating or preventing cancer or tumor growth, by administering to a subject in need thereof a composition comprising a therapeutically or prophylactically effective amount of a compound that downregulates DDX3, for example a fused diimidazodiazepine ring compound or a pharmaceutically acceptable salt thereof. The invention also encompasses the use of DDX3 as a biomarker for diagnostic and treatment purposes, for example, to identify a hyperproliferative disorder susceptible to treatment by down regulation of DDX3.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Inventor: The Johns Hopkins University
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Publication number: 20130281436Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.Type: ApplicationFiled: June 24, 2013Publication date: October 24, 2013Inventors: Morten JORGENSEN, Peter Hongaard ANDERSEN, Klaus Gjervig JENSEN, Mette Graulund HVENEGAARD, Lassina BADOLO, Mikkel Fog JACOBSEN
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Publication number: 20130281441Abstract: 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: ApplicationFiled: June 19, 2013Publication date: October 24, 2013Inventors: Shogo Sakuma, Toshihiro Takahashi, Masatoshi Ushioda, Toshiyasu Imai, Kazuhike Inoue
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Publication number: 20130281439Abstract: The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy.Type: ApplicationFiled: March 18, 2011Publication date: October 24, 2013Inventors: Andrzej Roman Batt, Rachel Louisa Charlotte Handy, Michael Bryan Roe, Valerie Elizabeth Peal, Timothy John Kenhardt Gibbs, David Raymond Churchley
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Patent number: 8563542Abstract: The present invention relates to a compound of formula (VII)I, or a 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? each independently H 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: GrantFiled: September 29, 2008Date of Patent: October 22, 2013Assignee: Cyclacel LimitedInventors: Jonathan James Hollick, Stuart Donald Jones, Claire June Flynn, Michael George Thomas
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Publication number: 20130274250Abstract: 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 of Formula (I) wherein R1, R2, R3, R4, R5 and R6 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: ApplicationFiled: November 18, 2011Publication date: October 17, 2013Applicant: JANSSEN PHARMACEUTICA NVInventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit
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Publication number: 20130274249Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.Type: ApplicationFiled: March 11, 2013Publication date: October 17, 2013Inventors: Piero MELLONI, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
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Publication number: 20130267504Abstract: The present invention relates to a pharmaceutical composition comprising glycerol esters of a fatty acid, wherein the compositions are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Publication number: 20130267506Abstract: Compositions for therapy of a diabetic symmetrical polyneuropathy a subject in need thereof, the compositions comprising: an effective amount of a muscarinic acetylcholine receptor antagonist exemplified by pirenzepine, telenzepine, atropine, or derivatives thereof or salts thereof or analogs thereof or derivatives thereof, and a pharmacologically acceptable carrier. The composition may be injectable or alternatively, may be applied topically or alternatively, may be delivered orally. A suitable topical composition may comprise a lotion, a cream, a gel, or a viscous fluid. The muscarinic acetylcholine receptor antagonist may be a muscarinic acetylcholine receptor antagonist salt or a muscarinic acetylcholine receptor antagonist derivative or a muscarinic acetylcholine receptor antagonist analog.Type: ApplicationFiled: October 24, 2011Publication date: October 10, 2013Applicant: UNIVERSITY OF MANITOBAInventors: Paul Fernyhough, Nigel A. Calcutt, Lakshmi Kotra
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Publication number: 20130267503Abstract: The present invention relates to an injectable, pharmaceutical composition comprising a C1-6 alkyl ester of a C10-20 fatty acid. In an embodiment, the fatty acid is ethyl oleate, isopropyl oleate, ethyl myristate, or isopropyl myristate. These compositions are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Publication number: 20130267507Abstract: 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 bicyclic benzene derivatives of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 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: ApplicationFiled: December 19, 2011Publication date: October 10, 2013Applicant: JANSSEN PHARMACEUTICA NVInventors: Lieven Meerpoel, Louis Jules Roger Marie Maes, Kelly de Wit
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Publication number: 20130267505Abstract: The present invention relates to a pharmaceutical composition comprising benzyl alcohol and polyoxyethylene derivatives of sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Patent number: 8551986Abstract: In general, the invention provides methods and compositions for treating sequela of weight gain or pain insensitivity, e.g., in a subject suffering from a psychiatric disorder, such as schizophrenia. The combinations employed in the invention include a second generation antipsychotic agent and an opioid receptor antagonist.Type: GrantFiled: December 7, 2006Date of Patent: October 8, 2013Assignee: The McLean Hospital CorporationInventors: Igor Elman, David Borsook, Jan Wasley
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Publication number: 20130261109Abstract: The invention provides a method of inhibiting binding between acetylated histone and a bromodomain-containing protein in a mammal, as well as a method of shrinking or killing of cancer cells expressing a bromodomain-containing protein or inhibiting the growth of cancer cells expressing a bromodomain-containing protein in a mammal. The methods involve administering an effective amount of (S)-2-[4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide or a dihydrate thereof to the mammal.Type: ApplicationFiled: May 28, 2013Publication date: October 3, 2013Inventors: Shinji MIYOSHI, Shinsuke OOIKE, Kazunori IWATA, Hidemasa HIKAWA, Kunio SUGAHARA
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Patent number: 8546377Abstract: 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: GrantFiled: October 21, 2010Date of Patent: October 1, 2013Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
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Publication number: 20130252331Abstract: The invention provides compositions comprising an effective amount of an agent that inhibits a BET protein (e.g., Brd2, Brd3, Brd4), and methods of using such compositions for treating or preventing metabolic syndrome, obesity, type II diabetes, insulin resistance, and related disorders characterized by undesirable alterations in metabolism or fat accumulation.Type: ApplicationFiled: May 16, 2011Publication date: September 26, 2013Inventors: James Elliott Bradner, Jonathan Brown, Jorge Plutzky
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Publication number: 20130245004Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: May 9, 2013Publication date: September 19, 2013Applicant: Synchroneuron Inc.Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong
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Publication number: 20130236573Abstract: The present invention is directed to methods for the treatment of treatment-refractory depression or treatment-resistant depression comprising administering to a patient in need thereof, a therapeutically effective amount of esketamine as mono-therapy or as combination therapy with at least on antidepressant.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Inventors: Jaskaran Singh, Ivo Caers
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Publication number: 20130224289Abstract: 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: ApplicationFiled: April 1, 2013Publication date: August 29, 2013Applicant: Depomed, Inc.Inventor: Depomed, Inc.
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Publication number: 20130224257Abstract: The present invention relates to a method for preparing microsphere and microspheres produced thereby. The method comprises: mixing a water-insoluble organic solvent with a dispersion solvent; mixing a polymer compound, a drug and a water-insoluble organic solvent to prepare a dispersed phase; mixing the dispersed phase with the dispersion solvent mixed with the water-insoluble organic solvent to prepare an emulsion; and adding a base or an acid to the prepared emulsion. With the method, it is possible to prepare a drug-containing polymeric microsphere cost-effectively and conveniently.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicants: Ewha University - Industry Collaboration Foundation, SK Chemicals Co., Ltd.Inventors: SK Chemicals Co., Ltd., Ewha University - Industry Collaboration Foundation