The Additional Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/319)
  • Patent number: 10189784
    Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: January 29, 2019
    Assignees: ACADEMISCH MEDISCH CENTRUM, UNIVERSITEIT LEIDEN
    Inventors: Herman Steven Overkleeft, Stan Van Boeckel, Johannes Maria Franciscus Gerardus Aerts, Amar Ghisaidoobe, Richard Van Den Berg
  • Patent number: 10065920
    Abstract: The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
    Type: Grant
    Filed: January 31, 2018
    Date of Patent: September 4, 2018
    Assignee: Aquinox Pharmaceuticals (Canada) Inc.
    Inventors: Lloyd F. Mackenzie, Jeffery R. Raymond, Curtis Harwig, Ana Fernandez Casares
  • Patent number: 10052346
    Abstract: Methods are presented for treating cancers and hematopoietic stem cell disorders, comprising administering to a subject with a cancer or hematopoietic stem cell disorder who is receiving a treatment regimen, a heparin derivative capable of inhibiting, reducing, abrogating or otherwise interfering with the binding of CXCL12 to CXCR4, wherein the cancer or hematopoietic stem cell disorder is one in which interaction of CXCL12 with CXCR4 privileges the cancer or disordered HSCs against therapeutic intervention. In preferred embodiments, the heparin derivative is a substantially 2-O, 3-O-desulfated heparin derivative.
    Type: Grant
    Filed: February 16, 2016
    Date of Patent: August 21, 2018
    Assignee: Cantex Pharmaceuticals, Inc.
    Inventor: Stephen Marcus
  • Patent number: 9944590
    Abstract: The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
    Type: Grant
    Filed: June 23, 2016
    Date of Patent: April 17, 2018
    Assignee: Aquinox Pharmaceuticals (Canada) Inc.
    Inventors: Lloyd F. Mackenzie, Jeffery R. Raymond, Curtis Harwig, Ana Fernandez Casares
  • Patent number: 9764316
    Abstract: Despite significant progress in the synthesis of nanocomposite materials, integration of several components with various functions remains a big challenge, which significantly limits control over nanocomposite properties. The disclosure provides a multifunctional micro particle based on incorporation of titania nanoparticles combined into a porous polylactic acid (PLA) matrix. PLA is used as a biodegradable and biocompatible polymer and titania nanoparticles represent photocatalytically active nanofillers capable of degradation of organic compounds under solar irradiation. Titania nanoparticles are integrated with PLA by using ‘mixed’ and ‘in situ grown’ approaches. The hybrid systems effectively absorbed and degraded organic impurities from water. The sorption capacity, dye degradability, and PLA disintegration were controlled by varying the concentration of incorporated titania.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: September 19, 2017
    Assignee: The UAB Research Foundation
    Inventors: Eugenia P. Kharlampieva, Benjamin Yancey
  • Patent number: 9533052
    Abstract: The invention provides an ophthalmic product containing rebamipide, which has a transparency enough to be agreeable feeling on using it and has neutral so weakly acidic pH not to injury of the keratoconjunctiva of a patient suffering from dry eye. An aqueous suspension of crystalline rebamipide which has an improved transparency is provided by adding an aqueous solution of rebamipide dissolved by a base such as sodium hydroxide or an aqueous solution of a salt of rebamipide to an aqueous acidic solution such as hydrochloric acid containing at least one of the compounds selected from water-soluble polymers and surfactants, and mixing them.
    Type: Grant
    Filed: October 19, 2015
    Date of Patent: January 3, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Takakuni Matsuda, Shogo Hiraoka, Yuso Tomohira, Shinichi Ishikawa
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 9011912
    Abstract: Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: April 21, 2015
    Assignee: Abon Pharmaceuticals, LLC
    Inventors: Yanming Zu, Sudhir Gorukanti, Salah Uddin Ahmed
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Patent number: 9000010
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Patent number: 8993768
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: March 31, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: John A. Beutler, Stuart F. J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Publication number: 20150080378
    Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Caryn TROCME-THIBIERGE, Aurore Sors, Florence Keime-Guibert
  • Publication number: 20150080400
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 19, 2015
    Applicant: TAKEDA GMBH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Publication number: 20150080379
    Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 19, 2015
    Inventors: Caryn TROCME-THIBIERGE, Aurore SORS, Florence KEIME-GUIBERT
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Patent number: 8969402
    Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: March 3, 2015
    Inventor: Steven A. Rich
  • Patent number: 8969326
    Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: March 3, 2015
    Assignee: University of Pittsburgh—Of The Commonwealth System Of Higher Education
    Inventors: Carol A. Feghali-Bostwick, Pamela Anne Hershberger
  • Publication number: 20150051246
    Abstract: Treatment of varying degrees of cognitive impairment associated with Alzheimer's disease with a combination of a phosphodiesterase 4 inhibitor and an acetylcholinestase inhibitor, including roflumilast and donepezil hydrochloride.
    Type: Application
    Filed: August 15, 2014
    Publication date: February 19, 2015
    Inventors: Tadataka Yamada, Jos Prickaerts, Marlies van Duinen, Anke Sambeth, Arjan Blokland
  • Publication number: 20150045389
    Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.
    Type: Application
    Filed: April 9, 2013
    Publication date: February 12, 2015
    Inventors: Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
  • Publication number: 20150025112
    Abstract: The present invention relates to orally disintegrating tablet formulations of donepezil hydrochloride comprising magnesium aluminium silicate, and one or more pharmaceutically acceptable excipient and process for preparing such a formulation.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: Ali Turkyilmaz, Fatih Cengiz Aygul, Devrim Celik
  • Publication number: 20150023950
    Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
  • Patent number: 8933097
    Abstract: The present invention is directed to an aqueous pharmaceutical suspension of fexofenadine zwitterionic dihydrate Form I.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: January 13, 2015
    Assignee: Sanofi-Aventis U.S. LLC
    Inventors: Kazimierz Chrzan, Rajiv Haribhakti, Matthew Mermey, Curtis J. Porcello, Gary Lee Silvey, Vinh Tran, Prafulla Agrawala
  • Publication number: 20150010493
    Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.
    Type: Application
    Filed: June 27, 2014
    Publication date: January 8, 2015
    Inventor: Shou-Wei DING
  • Publication number: 20150005283
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20140378439
    Abstract: The invention provides a method of diagnosing Alzheimer's Disease in a subject, by determining the level of at least one miRNA in a sample derived from the subject, wherein a change in the level of the at least one miRNA relative to a suitable control is indicative of Alzheimer's Disease in the subject. Methods for monitoring the course of Alzheimer's Disease, methods of treating a subject having Alzheimer's Disease, and kits for diagnosing Alzheimer's Disease are also provided.
    Type: Application
    Filed: June 26, 2012
    Publication date: December 25, 2014
    Inventors: Zoltan Dezso, Pavan Kumar
  • Publication number: 20140377328
    Abstract: Provided is an intraoral soluble-type film preparation in which an unpleasant taste of a drug is masked. The intraoral soluble-type film preparation comprises a drug layer containing: a drug having a bitter taste and/or an astringent taste; an alkyl sulfate at a content of ¾ mol or more with respect to 1 mol of the drug; and a water-soluble polymer.
    Type: Application
    Filed: December 12, 2012
    Publication date: December 25, 2014
    Applicant: KYUKYU PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Ishise, Hisanobu Nishikawa
  • Publication number: 20140378440
    Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease, Alzheimer's disease related disorders, amyotrophic lateral sclerosis, multiple sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on baclofen and acamprosate combination.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: DANIEL COHEN, ILYA CHUMAKOV, SERGUEI NABIROCHKIN, EMMANUEL VIAL, MICKAEL GUEDJ
  • Publication number: 20140377351
    Abstract: The invention relates to a pharmacologically active combination and a method of enhancing cognitive performance in a patient suffering from Alzheimer's disease comprising administering to said patient a cognitive performance-enhancing amount of melatonin or a melatonin agonist in a combination therapy with a nicotine receptor agonist.
    Type: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Applicant: NEURIM PHARMACEUTICALS (1991) LTD.
    Inventors: Nava ZISAPEL, Moshe LAUDON
  • Publication number: 20140371209
    Abstract: Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
    Type: Application
    Filed: February 3, 2012
    Publication date: December 18, 2014
    Inventors: Jermaine Thomas, Sha Mi, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Kevin Guckian, Gnanasambandam Kumaravel
  • Publication number: 20140371260
    Abstract: The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
    Type: Application
    Filed: May 16, 2014
    Publication date: December 18, 2014
    Applicant: MERZ PHARMA GmbH & CO. KGaA
    Inventor: Hans-Joerg Moebius
  • Publication number: 20140370076
    Abstract: The present invention provides a transdermal drug delivery system comprising donepezil or its pharmaceutically acceptable salt and method of making the same.
    Type: Application
    Filed: March 12, 2014
    Publication date: December 18, 2014
    Inventors: Hoo-Kyun Choi, Myung-Kwan Chun
  • Publication number: 20140356292
    Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Sumitomo Dainippon Pharma Co., Ltd.
    Inventor: Takeo ISHIYAMA
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20140343000
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20140315952
    Abstract: The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 23, 2014
    Inventor: Ziqiang Gu
  • Patent number: 8865741
    Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
    Type: Grant
    Filed: February 18, 2012
    Date of Patent: October 21, 2014
    Assignee: Asana Biosciences, LLC
    Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
  • Publication number: 20140308335
    Abstract: The present invention provides transdermal absorption preparation having a support, and a drug-containing adhesive layer formed on the support, wherein a drug-containing adhesive layer contains donepezil or a salt thereof, and a higher fatty acid salt.
    Type: Application
    Filed: September 7, 2012
    Publication date: October 16, 2014
    Applicant: KM TRANSDERM LTD.
    Inventors: Atsuyo Hamada, Mitsuji Akazawa, Keiko Yamasaki, Masaoki Goto
  • Publication number: 20140309190
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 16, 2014
    Applicant: BIOGEN IDEC MA INC.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140301999
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20140296211
    Abstract: This invention concerns a dosage form comprising a therapeutically neuroprotective amount of A2-73 and a neuroprotective amount of at least one cooperating acetylcholinesterase inhibitor selected from the group consisting of donepezil, galantamine, rivastigmine, or memantine and method of use.
    Type: Application
    Filed: July 12, 2013
    Publication date: October 2, 2014
    Applicant: ANAVEX LIFE SCIENCES CORP.
    Inventors: Alexandre Vamvakides, Tangui Maurice
  • Patent number: 8841325
    Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 23, 2014
    Assignee: Celgene Corporation
    Inventors: Carole Brosseau, Justin Blake Bartlett, Angus George Dalgleish, Kay Winifred Colston, Christine Galustian
  • Publication number: 20140275036
    Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.
    Type: Application
    Filed: May 29, 2014
    Publication date: September 18, 2014
    Applicant: Chase Pharmaceuticals Corporation
    Inventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
  • Publication number: 20140248353
    Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.
    Type: Application
    Filed: May 16, 2014
    Publication date: September 4, 2014
    Applicant: NAL Pharmaceuticals Ltd.
    Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
  • Publication number: 20140249183
    Abstract: Treatments are described for stress disorders and substance use disorders, for example, substance use disorders associated with use of alcohol, cocaine, amphetamines, and the like.
    Type: Application
    Filed: February 22, 2014
    Publication date: September 4, 2014
    Applicant: Baylor College of Medicine
    Inventors: Thomas F. Newton, Colin N. Haile
  • Publication number: 20140249181
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Application
    Filed: May 10, 2012
    Publication date: September 4, 2014
    Applicant: The united States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: John A. Beutler, Stuart F.J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Publication number: 20140243334
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20140243335
    Abstract: This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Emily F. Calderwood, Kenneth M. Gigstad, Alexandra E. Gould, Sean J. Harrison, He Xu
  • Publication number: 20140243278
    Abstract: Disclosed is an acid addition salt of donepezil, wherein acid counterion is selected from the group consisting of pamoic acid, cypionic acid, camphor sulfonic acid, enanthic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, valeric acid, Dibenzoyl-D-Tartaric acid and terephthalic acid. Disclosed is a process for the preparation and pharmaceutical composition comprising the same. More specifically, disclosed is concerned with the pamoate acid addition salts of donepezil. Disclosed also is long acting formulation comprising the acid addition salt of donepezil and process for the preparation thereof.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 28, 2014
    Inventors: Sunil Sadanand Nadkarni, Arunkumar Gupta, Jaya Abraham, Manish Parikh, Mahesh Suthar, Bipin Manavadariya, Vivek Mishra
  • Publication number: 20140235641
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 21, 2014
    Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi