Tropanes (including Nor Or Dehydro Form) Patents (Class 514/304)
  • Patent number: 8796256
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Patent number: 8791134
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: July 29, 2014
    Assignee: Cardioxyl Pharmaceuticals, Inc.
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Publication number: 20140206718
    Abstract: A method of enhancing the activity of lysosomal ?-Galactosidase A (?-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 24, 2014
    Applicant: Mount Sinai School of Medicine of New York University
    Inventors: Jian-Qiang Fan, Satoshi Ishii
  • Patent number: 8784892
    Abstract: The present invention is directed to the use of an agent selected from ethyl alcohol, isopropyl alcohol or a mixture thereof and a topically acceptable polymeric carrier in the preparation of a composition for the treatment of burns.
    Type: Grant
    Filed: July 7, 2010
    Date of Patent: July 22, 2014
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventor: Elka Touitou
  • Publication number: 20140171404
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
  • Publication number: 20140163064
    Abstract: A method for alleviating urinary incontinence, by administering to a subject, including, but not limited to, climacteric women, a therapeutically effective amount of an anticholinergic agent. The anticholinergic agent may be an anti-muscarinic agent, and preferably, the anti-muscarinic agent may be homatropine, including its methylbromide salt.
    Type: Application
    Filed: February 14, 2014
    Publication date: June 12, 2014
    Applicant: Eaton Scientific Systems, Ltd.
    Inventors: Hootan Melamed, Edward W. Withrow, III, Jennifer R. Berman
  • Publication number: 20140163063
    Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: October 1, 2013
    Publication date: June 12, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
  • Publication number: 20140163062
    Abstract: A medicinal preparation for preventing and/or treating psychoneurotic diseases such as integration dysfunction and Alzheimer's disease which contains tropisetron or its pharmaceutically acceptable salt as the active ingredient.
    Type: Application
    Filed: June 24, 2013
    Publication date: June 12, 2014
    Inventors: Kenji Hashimoto, Masaomi Iyo, Kaori Koike
  • Patent number: 8748457
    Abstract: The present invention is related to novel 2-Amino-2-[8-(dimethyl carbamoyl)-8-aza-bicyclo[3.2.1]oct-3-yl]-exo-ethanoyl derivatives of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: June 10, 2014
    Assignee: Lupin Limited
    Inventors: Neelima Sinha, Prathap Nair, Navnath Karche, Nabendu Saha, Rajan Goel, Rajender Kumar Kamboj
  • Publication number: 20140154236
    Abstract: Described here are devices and methods for treating one or more conditions or symptoms associated with a tonsil procedure. In some variations, a drug-releasing device may be at least partially delivered to one or more tonsillar tissues before, during, or after a tonsil procedure. In some variations, the drug-releasing device may be configured to be biodegradable. In other variations, the drug-releasing device may comprise one or more hemostatic materials or one or more adhesives. The drug-releasing device may be configured to release one or more drugs or agents, such as, for example, one or more analgesics, local anesthetics, vasoconstrictors, antibiotics, combinations thereof and the like.
    Type: Application
    Filed: February 6, 2014
    Publication date: June 5, 2014
    Applicant: INTERSECT ENT, INC.
    Inventors: Jerome E. HESTER, Anthony J. ABBATE, Richard E. KAUFMAN, David C. GALE, Gail M. ZALER, Bin HUANG, Lisa EARNHARDT, Vijaykumar RAJASEKHAR
  • Patent number: 8741922
    Abstract: The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: January 28, 2013
    Date of Patent: June 3, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Beili Zhang, Mariusz Krawiec, Brian Luisi, Ales Medek
  • Publication number: 20140135302
    Abstract: Methods, compositions, and kits for predicting whether a subject with chronic obstructive pulmonary disease (COPD) or at risk of developing COPD is likely to have progressive COPD are provided. Methods, compositions, and kits for predicting whether lung function is likely to decline in a subject with COPD or at risk for developing COPD are also provided.
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Applicant: SOMALOGIC, INC.
    Inventors: Malti P. Nikrad, Stuart G. Field, Stephen Alaric Williams, Alex A.E. Stewart, Rachel M. Ostroff, Rosalynn Dianne Gill
  • Publication number: 20140135306
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: June 19, 2012
    Publication date: May 15, 2014
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Publication number: 20140135300
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Publication number: 20140128345
    Abstract: Described are drug delivery systems incorporating electrospun fibers that comprise and deliver physicochemically diverse drug compounds. Such fibers provide significant advantages in drug agent release, such as adaptability for solid dosage delivery to mucosal tissues. This is in addition to allowing for controlled drug release. Systems and methods for large-scale electrospinning productivity are described, including novel microarchitectures allowing for variable pharmacokinetics in drug release.
    Type: Application
    Filed: November 6, 2013
    Publication date: May 8, 2014
    Applicant: UNIVERSITY OF WASHINGTON
    Inventors: Kim A. Woodrow, Cameron Ball, Anna Blakney, Emily Krogstad, Huarong Nie
  • Publication number: 20140121234
    Abstract: The invention relates to inhalant propellant-free aerosol formulations containing at least one inert, non-volatile auxiliary substance for adjusting defined droplet sizes.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph KREHER, Michael SPALLEK
  • Patent number: 8703758
    Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: April 22, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
  • Patent number: 8703184
    Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: April 22, 2014
    Assignee: Wellesley Pharmaceuticals, LLC
    Inventor: David A. Dill
  • Publication number: 20140109245
    Abstract: The present disclosure, in part, is directed to a mammalian prostate cancer cell line comprising at least one or a set of primary mammalian epithelial cells which have been infected with a retroviral vector carrying an oncogene selected from the group consisting of c-Myc, Ha-Ras, NeuT, c-Src and combinations thereof and in which said gene is expressed.
    Type: Application
    Filed: March 9, 2012
    Publication date: April 17, 2014
    Inventor: Richard G. Pestell
  • Publication number: 20140107088
    Abstract: Improved medical devices and methods are provided comprising an anabolic agent for healing an injury. These improved medical devices and methods can enhance healing in injuries from traumatic soft tissue injury, surgical injuries, burn, traumatic brain injuries, musculotendinous injuries, musculoskeletal conditions, bone injury or other injuries or maladies, which can be chronic or non-chronic in origin. In some embodiments, the medical device comprises a drug depot that releases the anabolic agent over at least 2 days to enhance healing of an injury.
    Type: Application
    Filed: November 20, 2013
    Publication date: April 17, 2014
    Applicant: Warsaw Orthopedic, Inc.
    Inventor: Jared T. Wilsey
  • Patent number: 8697691
    Abstract: In one aspect, the invention relates to compounds having a general structure: which are useful as selective allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: April 15, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Michael R. Wood, Rocco D. Gogliotti, Colleen M. Niswender, Bruce J. Melancon, Evan P. Lebois
  • Patent number: 8697721
    Abstract: The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: April 15, 2014
    Assignee: Aniona APS
    Inventors: Dan Peters, Elsebet Østergaard Nielsen, Karin Sandager Nielsen, Gordon Munro
  • Publication number: 20140093518
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Application
    Filed: August 26, 2013
    Publication date: April 3, 2014
    Applicant: The Scripps Research Institute
    Inventor: Carlos F. Barbas, III
  • Publication number: 20140094450
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
  • Patent number: 8685453
    Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: April 1, 2014
    Assignee: Wellesley Pharmaceuticals, LLC
    Inventor: David A. Dill
  • Publication number: 20140080855
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 10, 2013
    Publication date: March 20, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
  • Publication number: 20140080856
    Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Application
    Filed: August 13, 2013
    Publication date: March 20, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Sean Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
  • Patent number: 8673909
    Abstract: The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.
    Type: Grant
    Filed: November 17, 2008
    Date of Patent: March 18, 2014
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi, John S. Andrews, Gabriela Mladenova
  • Publication number: 20140065219
    Abstract: Methods for making inhalable composite particles comprising a pharmaceutically-active agent, the method comprising: a) providing composite particles comprising a millable grinding matrix and a solid pharmaceutically-active agent, wherein the pharmaceutically-active agent has an median particle size on a volume average basis between 50 nm and 3 ?m; and b) milling the composite particles in a mill without milling bodies for a time period sufficient to produce inhalable composite particles having a mass median aerodynamic diameter between 1 ?m and 20 ?m are described.
    Type: Application
    Filed: February 28, 2013
    Publication date: March 6, 2014
    Inventors: William H. Bosch, Matthew Callahan, Felix Meiser, Marck Norret, Adrian Russell
  • Patent number: 8664242
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: March 4, 2014
    Assignee: Theravance, Inc.
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20140057940
    Abstract: The invention provides methods for treating or preventing cardiac and neurological disorders using chemokine receptor antagonists.
    Type: Application
    Filed: January 11, 2012
    Publication date: February 27, 2014
    Inventors: Joseph L. Mankowski, David R. Graham
  • Publication number: 20140056999
    Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.
    Type: Application
    Filed: March 7, 2013
    Publication date: February 27, 2014
    Applicant: MediciNova, Inc.
    Inventor: MediciNova, Inc.
  • Publication number: 20140057939
    Abstract: The invention provides methods for the treatment of cognitive disorders utilizing specific 5-HT4 receptor agonist compounds, in particular, methods utilizing these compounds in combination with other agents, specifically acetylcholinesterase inhibitors, for the treatment of Alzheimer's disease and other cognitive disorders.
    Type: Application
    Filed: February 20, 2013
    Publication date: February 27, 2014
    Applicant: THERAVANCE, INC.
    Inventors: David Beattie, Fei Shen, Jacqueline A.M. Smith
  • Patent number: 8658671
    Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: February 25, 2014
    Assignee: Theravance, Inc.
    Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
  • Publication number: 20140051687
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 20, 2014
    Applicant: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20140051679
    Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERISTY HEALTH NETWORKS
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
  • Publication number: 20140038949
    Abstract: The present invention provides methods of inducing differentiation of oligodendrocyte progenitor cells to a mature myelinating cell fate with a neurotransmitter receptor modulating agent. The present invention also provides methods of stimulating increased myelination in a subject in need thereof by administering said neurotransmitter receptor modulating agent. Methods of treating a subject having a demyelinating disease using a neurotransmitter receptor modulating agent are also provided.
    Type: Application
    Filed: February 17, 2012
    Publication date: February 6, 2014
    Applicants: IRM LLC, The Scripps Research Institute
    Inventors: Peter Schultz, Luke Lairson, Vishal Deshmukh, Costas Lyssiotis
  • Publication number: 20140030191
    Abstract: A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN? groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.
    Type: Application
    Filed: April 20, 2012
    Publication date: January 30, 2014
    Applicant: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Sylvain Routier, Franck Suzenet, Frederic Pin, Sylvie Chalon, Johnny Vercouillie, Denis Guilloteau
  • 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
  • Publication number: 20140024641
    Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 23, 2014
    Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
  • Patent number: 8633218
    Abstract: The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: January 21, 2014
    Assignee: Aniona APS
    Inventors: Dan Peters, David Spencer Jones, Elsebet Østergaard Nielsen
  • Publication number: 20140005135
    Abstract: Disclosed is a stable liquid formulation for parenteral injection comprising a biocompatible non-aqueous solvent and a small molecule drug, or a salt thereof, solubilized within the non-aqueous solvent, wherein the liquid formulation comprises less than 10% by weight residual water, and wherein the volume of the liquid formulation to be parenterally injected is from 0.1 ?l to 3 ml.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 2, 2014
    Applicant: XERIS PHARMACEUTICALS, INC.
    Inventors: Steven J. Prestrelski, Nancy Scott
  • Publication number: 20130345230
    Abstract: The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions).
    Type: Application
    Filed: August 27, 2013
    Publication date: December 26, 2013
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: D. James Surmeier, Michelle Day, Jun Ding, Savio Chan, Jamie Guzman, Jeff Mercer, Tatiana Tkatch, Zhongfeng Wang, Ema Ilijic
  • Publication number: 20130337063
    Abstract: The present disclosure relates to solid dosage forms comprising the CCR5 co-receptor antagonist maraviroc. More particularly, the present disclosure relates to a solid oral dosage form containing maraviroc which has favorable disintegration properties.
    Type: Application
    Filed: February 17, 2012
    Publication date: December 19, 2013
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Podili Khadgapathi, Goli Kamalakar Reddy, Nelluri Rama Rao
  • Patent number: 8609690
    Abstract: The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: December 17, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Stefan Peters
  • Publication number: 20130331349
    Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
    Type: Application
    Filed: November 30, 2011
    Publication date: December 12, 2013
    Inventors: David C. Tully, Paul Vincent Rucker, Phillip B. Alper, Daniel Mutnick, Donatella Chianelli
  • Patent number: 8604195
    Abstract: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Unmesh Shah, Craig D. Boyle, Samuel Chackalamannil
  • Publication number: 20130324572
    Abstract: A medicinal preparation for preventing and/or treating psychoneurotic diseases such as integration dysfunction and Alzheimer's disease which contains tropisetron or its pharmaceutically acceptable salt as the active ingredient.
    Type: Application
    Filed: May 22, 2013
    Publication date: December 5, 2013
    Applicant: National University Corporation Chiba University
    Inventors: Kenji Hashimoto, Masaomi Iyo, Kaori Koike
  • Publication number: 20130317000
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Publication number: 20130317058
    Abstract: The present invention discloses an ophthalmic composition for ophthalmic application(s) inclusive of Eye examination, surgeries carried out in the posterior chamber of the Eye like cataract surgery. The said composition comprises at least three active ingredients. The said ingredients may be inclusive of, but not restricted to, Epinephrine Bitartrate, Atropine Bisulphate, Xylocaine Hydrochloride and additives like, antioxidant compounds, buffers and the like. The said composition comes in a packaging container inclusive of sterile package such as vial/ampoule/prefilled syringes. The said composition can be directly injected in the Eye in order to bring about effective and speedy dilation of the pupil(s), in particular pupil(s) of relatively smaller dimension than normal pupil. The three active ingredients are mixed in a predefined percentage range in a predefined volume and the composition is supplied in a sterile package.
    Type: Application
    Filed: February 17, 2012
    Publication date: November 28, 2013
    Applicant: M/S. APPASAMY ASSOCIATES
    Inventor: Krishnasamy Rengasamy