Tricyclo Ring System Having The Seven-membered Hetero Ring A One Of The Cyclos Patents (Class 514/217)
  • Patent number: 8835421
    Abstract: The present invention provides a compounds of general formula (8), (11) and (14), 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 formula (8), (11) and (14).
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: September 16, 2014
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmen Kamal, Pogula Praveen Kumar, Bobburi Naga Seshadri, Kokkonda Sreekanth
  • Publication number: 20140255517
    Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 11, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Kerry J. Ressler, Paul J. Marvar
  • Publication number: 20140248378
    Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 4, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
  • Publication number: 20140243319
    Abstract: A combination treatment taking advantage of the synergistic effect of inhibiting ?-synuclein expression and chemotherapeutic agents to provide improved treatment of cancers, preferably stage III/IV cancers. A method for identifying improved cancer treatments.
    Type: Application
    Filed: March 16, 2012
    Publication date: August 28, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventor: Anita Sidhu
  • Patent number: 8815844
    Abstract: The present invention relates to the compounds useful in the prevention and/or treatment of tumors. More specifically the present invention relates to inhibitors of the activity of the electron transport chains and/or the mitochondrial TCA cycle in glioma-initiating cells (GICs) for use in a method for preventing and/or treating tumors presenting glioma-initiating cells (GICs) in a subject who has undergone a prior removal of a tumor glioma bulk. The present invention further provides a pharmaceutical composition containing the inhibitors of the invention and a screening method for identifying the inhibitors of the invention.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: August 26, 2014
    Assignees: Universite de Geneve, Hopitaux Universitaires de Geneve
    Inventors: Virginie Clement, Ivan Radovanovic
  • Publication number: 20140234443
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: March 10, 2014
    Publication date: August 21, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Peter R. GUZZO, David D. MANNING, William EARLEY
  • Publication number: 20140213578
    Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 31, 2014
    Applicant: MT. SINAI SCHOOL OF MEDICINE
    Inventors: Michael Ohlmeyer, Goutham Narla, Neil Dhawan, David Kastrinsky
  • Publication number: 20140200210
    Abstract: The present invention relates to a pharmaceutical composition for treating, preventing or improving premature ejaculation, which is taken on demand prior to sexual activity, the composition comprising clomipramine hydrochloride in an amount of 14 to 16 mg, preferably about 15 mg, as an active ingredient. More preferably, the composition of the present invention further comprises pregelatinized starch and sodium starch glycolate. The pharmaceutical composition of the present invention can provide rapid onset of efficacy, reduce a dissolution (absorption) deviation according to the patient's gastrointestinal pH conditions and minimize side effects.
    Type: Application
    Filed: June 28, 2012
    Publication date: July 17, 2014
    Applicant: CTC BIO, INC.
    Inventors: Hong-Ryeol Jeon, Do-Woo Kwon, Bong-Sang Lee, Seong-Shin Kwak, Sun-Ahe Lee, Hyun-Jung Park, Jeong-Hwa Yoo
  • Publication number: 20140194411
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are benzazepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).
    Type: Application
    Filed: December 23, 2013
    Publication date: July 10, 2014
    Applicant: ABT Holding Company
    Inventors: Mike Robarge, John Harrington, David Gerrish, John Mecom
  • Patent number: 8765960
    Abstract: A TARP ?8 dependant AMPA receptor antagonist of the formula: its pharmaceutically acceptable salts, uses, and methods for its preparation are described.
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: July 1, 2014
    Assignee: Eli Lilly and Company
    Inventors: Jon Kevin Reel, Warren Jaye Porter
  • Publication number: 20140178503
    Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 26, 2014
    Publication date: June 26, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Ronald C. Newbold, Chengzhi Zhang
  • Publication number: 20140178479
    Abstract: Formulations of a neuroprotective agent for parenteral administration are described herein. The formulation is in the form of a concentrated (supersaturated) solution or a concentrated suspension of microparticles. The suspension medium or the solution solvent carrier may also contain dissolved neuroprotective agent. For the supersaturated solutions, the agent is dissolved at high concentrations of at least about 1% by weight, 5% by weight, 10% by weight, 15% by weight, or 20% by weight in a solvent suitable for parenteral administration. For the concentrated suspension, the microparticles have an effective particle size from about 100 nm to about 5 microns, preferably from about 50 nm to about 3 microns, more preferably from about 10 nm to about 2 microns. The formulations described herein can be used to treat a variety of neurological diseases/disorders and/or neurological injury or trauma.
    Type: Application
    Filed: April 9, 2012
    Publication date: June 26, 2014
    Applicant: PEROSPHERE, INC.
    Inventors: Sasha H. Bakhru, Bryan E. Laulicht, Edith Mathiowitz, Solomon S. Steiner
  • Publication number: 20140171383
    Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.
    Type: Application
    Filed: June 28, 2013
    Publication date: June 19, 2014
    Inventors: Daniel J. ABRAMS, Raymond Bunch, Tom Anchordoquy
  • Publication number: 20140162989
    Abstract: The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.
    Type: Application
    Filed: February 13, 2014
    Publication date: June 12, 2014
    Applicants: The Regents of the University of Michigan, University of South Florida
    Inventors: Michael J. Zaworotko, Nair Rodriguez-Hornedo, Brian Moulton
  • Publication number: 20140148441
    Abstract: A TARP ?8 dependant AMPA receptor antagonist of the formula: its pharmaceutically acceptable salts, uses, and methods for its preparation are described.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 29, 2014
    Applicant: Eli Lilly and Company
    Inventors: Jon Kevin REEL, Warren Jaye PORTER
  • Publication number: 20140142087
    Abstract: Compounds and combinations of them that inhibit phosphatidic phosphohydrolase (PAP) enzymatic activity are formulated into pharmaceuticals useful in cancer treatment. Inhibitors of PAP can be used for blocking the progression of cancers that depend on the epidermal growth factor receptor (EGFR), its oncogenic variants and other members of its ErbB tyrosine kinase receptor family, through induction of their endocytosis, thus making them inaccessible to the extracellular stimuli that promote maintenance and progression of cancer.
    Type: Application
    Filed: February 6, 2012
    Publication date: May 22, 2014
    Applicant: PONTIFICIA UNIVERSIDAD CATÓLICA DE CHILE
    Inventors: Alfonso Gonzalez, Andrea Soza, Claudia Metz
  • Patent number: 8729120
    Abstract: This invention is directed to a method of treating depression in a subject, comprising the step of administering a therapeutically effective amount of a conventional antidepressant and, in addition, administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member Rx selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected f
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: May 20, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventor: Jonathan Sporn
  • Patent number: 8716278
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: May 6, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • 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: 20140113890
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
    Type: Application
    Filed: December 23, 2013
    Publication date: April 24, 2014
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
  • Publication number: 20140107104
    Abstract: The present invention provides a combination medicine for treatment of depression, comprising a combination of (A1) an antidepressant and either (B1) a dopamine D1 receptor agonist or (C1) a dopamine D1 receptor antagonist; and a method for screening for an antidepressant that in combination with a dopamine D1 receptor agonist provides an improvement in treatment of depression, the method comprising the steps of: administering, to a mammal, (A2) a compound having an antidepressant action and (B1) a dopamine D1 receptor agonist, and detecting a greater increase in depression-related gene expression, dopamine D1 receptor expression and/or dopamine D1 receptor signaling in comparison with the case where (A2) the compound having an antidepressant action or (B1) the dopamine D1 receptor agonist is administered.
    Type: Application
    Filed: March 22, 2012
    Publication date: April 17, 2014
    Inventors: Akinori Nishi, Katsunori Kobayashi, Tsuyoshi Miyakawa, Paul Greengard
  • Patent number: 8697685
    Abstract: The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R1-R4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: April 15, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Michael Axten, Charles William Blackledge, Jr., Gerald Patrick Brady, Jr., Yanhong Feng, Seth W. Grant, Jesus Raul Medina, William H. Miller, Stuart P. Romeril
  • Publication number: 20140100219
    Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 10, 2014
    Applicant: Supernus Pharmaceuticals, Inc.
    Inventors: Padmanabh P. Bhatt, Argaw Kidane, Kevin Edwards
  • 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
  • Publication number: 20140094449
    Abstract: The invention relates to sulphur- and/or selenium-containing compounds that can inhibit the enzyme inositol mono-phosphatase (IMPase), and which can be used in treating conditions that are treatable through inhibition of this enzyme, such as bi-polar disorder, the compounds having a structure of Formula (I), or is a pharmaceutically acceptable salt thereof; Formula (I); in which: E is S or Se and each of phenyl rings A and B is optionally substituted with one or more substituents, in which each substituent is selected independently from: (1) a halogen, which is preferably selected from F, Cl and Br; (2) C1-C4 alkyl, such as C1-C2 alkyl or C1 alkyl, optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br; and (3) C1-C4 alkoxy, such as C1-C2 alkoxy or C1 alkoxy; optionally substituted with one or more halogen atoms, each of which is preferably selected from F, Cl and Br.
    Type: Application
    Filed: January 18, 2012
    Publication date: April 3, 2014
    Applicant: ISIS INNOVATION LTD.
    Inventors: Grant C. Churchill, Sridhar R. Vasudevan, Nisha Singh
  • Publication number: 20140093592
    Abstract: 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: Application
    Filed: December 5, 2013
    Publication date: April 3, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Jaskaran Singh, Lodewijk Ivo Caers
  • Publication number: 20140079780
    Abstract: The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 20, 2014
    Applicant: GRUENENTHAL GMBH
    Inventors: Elisabeth ARKENAU MARIC, Johannes BARTHOLOMÄUS, Heinrich KUGELMANN
  • Publication number: 20140080812
    Abstract: The present invention is directed to a carbamazepine-cyclodextrin inclusion complex useful for the parenteral administration of carbamazepine. The carbamazepine-cyclodextrin inclusion complex is prepared by the admixture of a modified cyclodextrin and carbamazepine in a physiologically acceptable fluid. Modified cyclodextrins include 2-hydroxypropyl-beta-cyclodextrin and sulfoalkyl cyclodextrins. More particularly, the sulfoalkyl cyclodextrins are those described and disclosed in U.S. Pat. Nos. 5,134,127 and 5,376,645. A physiologically acceptable fluid includes sterile isotonic water, Ringer's lactate, D5W (5% dextrose in water), physiological saline, and similar fluids suitable for parenteral administration.
    Type: Application
    Filed: October 11, 2013
    Publication date: March 20, 2014
    Applicant: LUNDBECK LLC
    Inventors: James CLOYD, Angela BIRNBAUM, Ilo LEPPIK, Stephen D. COLLINS
  • Publication number: 20140079667
    Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 20, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140057900
    Abstract: Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Application
    Filed: August 23, 2013
    Publication date: February 27, 2014
    Applicant: Board of Regents of The University of Texas System
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Enrique Fernandez
  • Patent number: 8653065
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: February 18, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Publication number: 20140044787
    Abstract: The present application discloses a sustained release composition in pellet form, wherein the core of the pellet comprises: (a) a therapeutically effective amount of a medicament; (b) 0.5 to 50% by weight of a water-soluble polymer; and (c) 1 to 25% by weight of a water-insoluble polymer applied as an aqueous latex dispersion and subsequently the water is removed, wherein the sum of the percentages of the medicament, the water-insoluble polymer and the water-soluble polymer is equal to or less than 100%. It also discloses methods of making this composition.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: NOSTRUM PHARMACEUTICALS, LLC
    Inventor: Nirmal MULYE
  • Publication number: 20140045824
    Abstract: The present invention relates to a method for producing a complex crystal composed of two or more different compounds, comprising crystallizing the two or more different compounds under a condition at which menthol is heat melted, and a method for screening a complex crystal. In accordance with the method for producing a complex crystal of the present invention, a complex crystal capable of being used as a drug material can be produced rapidly, simply and efficiently. In addition, in accordance with the method for screening a complex crystal of the present invention, a stable complex crystal can be searched, which is industrially useful.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Inventors: Akinori Goto, Mamoru Fukuda
  • 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
  • Publication number: 20140030340
    Abstract: A method for preparing poorly water soluble drug particles is disclosed. The method comprises dissolving a drug in at least one organic solvent to form a drug/organic mixture, spraying the drug/organic mixture into an aqueous solution and concurrently evaporating the organic solvent in the presence of the aqueous solution to form an aqueous dispersion of the drug particles. The resulting drug particles are in the nanometer to micrometer size range and show enhanced dissolution rates and reduced crystallinity when compared to the unprocessed drug. The present invention additionally contemplates products and processes for new drug formulations of insoluble drug particles having high dissolution rates and extremely high drug-to-excipient ratios.
    Type: Application
    Filed: October 3, 2013
    Publication date: January 30, 2014
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Keith P. Johnston, Robert O. Williams, III, Xiaoxia Chen
  • Patent number: 8637087
    Abstract: The present invention relates to non-psychoactive derivatives of tetrahydrocannabinol, which are useful in treating interstitial cystitis and relieving symptoms thereof. The invention uses (6aR,10aR)-?8-tetrahydrocannabinol-11-oic acids (hereinafter referred to as (6aR,10aR)-?8-THC-11-oic acid), as well as pharmaceutical compositions containing the (6aR,10aR)-?8-THC-11-oic acids, for treatment of interstitial cystitis in a mammal. The invention further covers methods of formulating and administering the compounds and pharmaceutical compositions as therapeutic agents in the treatment of interstitial cystitis, with particularly preferred administration routes being oral and via intravesicular instillation.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: January 28, 2014
    Assignee: JB Therapeutics Inc.
    Inventors: Bobby W. Sandage, Jr., Glenn L. Cooper
  • Patent number: 8632763
    Abstract: The use of copolymers obtained by free-radical polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the total of components i), ii) and iii) equals 100% by weight, as solubilizers for slightly water-soluble substances.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: January 21, 2014
    Assignee: BASF SE
    Inventors: Nathalie Bouillo, Marianna Pierobon, Ralf Widmaier, Rainer Dobrawa, Kathrin Meyer-Böhm, Ronald Frans-Maria Lange
  • Publication number: 20140018338
    Abstract: Methods and assays for treating a subject with a filovirus infection using an agent that inhibits Niemann-Pick CI (NPCI), VPSII, VPSI6, VPSI8, VPS33A, VPS39, VPS41, BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4. Methods for screening for an agent that treats and/or prevents infection of a subject with a filovirus, where the methods comprise determining whether the agent inhibits one or more of Niemann-Pick CI (NPCI), VPSII, VPSI6, VPSI8, VPS33A, VPS39, VPS41. BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4, wherein an agent that inhibits one or more of NPCI, VPSII, VPSI6, VPSI8, VPS33A, VPS39, VPS41, BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4 is a candidate for treating and/or preventing an infection with a filovirus and wherein an agent that does not inhibit NPCI, VPSII, VPSI6, VPSI8, VPS33A. VPS39, VPS41, BLOCISI, BLOCIS2, GNPTAB, PIKFYVE, ARHGAP23 or FIG4 is not a candidate for treating and/or preventing an infection with a filovirus.
    Type: Application
    Filed: January 24, 2012
    Publication date: January 16, 2014
    Inventors: Kartik Chandran, Sean Whelan, Thijn Brummelkamp, Jan Carette, Matthijs Raaben
  • Patent number: 8629135
    Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumor cells.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: January 14, 2014
    Assignee: Queen's University at Kingston
    Inventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
  • 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: 20130345198
    Abstract: The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(?)-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-(?)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(?)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J1, J2, J3, J4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof.
    Type: Application
    Filed: March 6, 2012
    Publication date: December 26, 2013
    Applicant: JUBILANT LIFE SCIENCES LIMITED
    Inventors: Sujay Biswas, Shailendra Kumar Dubey, Vikas Bansal, Mukesh Masand, Dharam Vir
  • Publication number: 20130338143
    Abstract: Disclosed herein are compositions that are useful in effecting the transdermal delivery of therapeutic agents. More particularly, the disclosed transdermal compositions may include a fatty alcohol (for example, octanol), a terpene (for example, limonene), and an active agent comprising an amine moiety.
    Type: Application
    Filed: November 15, 2011
    Publication date: December 19, 2013
    Applicant: Neuroderm, Ltd.
    Inventors: Oron Yacoby-Zeevi, Mara Nemas, Eduardo Zawozink
  • Patent number: 8598119
    Abstract: 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: Grant
    Filed: May 27, 2009
    Date of Patent: December 3, 2013
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Sharon Mates, Allen Fienberg, Lawrence Wennogle
  • Patent number: 8597666
    Abstract: A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: December 3, 2013
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Ilan Zalit, Fanny Leska, Mali Kadosh, Dorit Marco, Yonit Messer-Triger
  • Publication number: 20130317009
    Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient which is an anticonvulsant selected from the group consisting of retigabin, lamotrigine, lacosamide, levetiracetam, carbamazepine, sultiame, phenacemide, felbamate, topiramate, pheneturide, brivaracetam, selectracetam, zonisamide, stiripentol, beclamide, mexiletin, ralfinamide, methylphenobarbital, phenobarbital, primidone, barbexaclone, metharbital, ethotoin, phenyloin, amino(diphenylhydantoin) valeric acid, mephenyloin, fosphenyloin, paramethadione, trimethadione, ethadione, ethosuximide, phensuximide, mesuximide, clonazepam, lorazepam, diazepam, clobazam, oxcarbazepine, eslicarbazepine, rufinamide, valproic acid, valpromide, aminobutyric acid, progabide, tiagabine, and the physiolo
    Type: Application
    Filed: May 13, 2013
    Publication date: November 28, 2013
    Applicant: Gruenenthal GmbH
    Inventor: Gruenenthal GmbH
  • Publication number: 20130310348
    Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).
    Type: Application
    Filed: July 25, 2013
    Publication date: November 21, 2013
    Applicants: State University
    Inventors: David H. Peyton, Steven Burgess
  • Patent number: 8586608
    Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetra-hydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetra-hydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: November 19, 2013
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca
  • Patent number: 8586575
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8580776
    Abstract: This invention provides agents, compositions, pharmaceutical compositions and methods for treating or slowing the progression of a neurodegenerating disease, such as Alzheimer's disease and a demyelinating disease.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: November 12, 2013
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Douglas L. Feinstein, Maria Vittoria Simonini, Sergey Kalinin, Paul E. Polak
  • Publication number: 20130280330
    Abstract: A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).
    Type: Application
    Filed: July 30, 2010
    Publication date: October 24, 2013
    Applicant: XI'AN LIBANG MEDICAL TECHNOLOGY CO., LTD.
    Inventors: Renle Hu, Jiucheng Wang, Tao Chen, Hua Liang, Duohao Ding, Yaqi Jiao