The Additional Hetero Ring Consists Of One Nitrogen And Four Carbons (e.g., Nicotine, Etc.) Patents (Class 514/343)
  • Publication number: 20140343083
    Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Patent number: 8889715
    Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: November 18, 2014
    Assignee: Alcobra Ltd.
    Inventors: Rina Yamin, Dalia Megiddo
  • Patent number: 8883774
    Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: November 11, 2014
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Joseph H. Gardner
  • Publication number: 20140329797
    Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: October 16, 2012
    Publication date: November 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
  • Publication number: 20140329835
    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: June 19, 2014
    Publication date: November 6, 2014
    Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
  • Publication number: 20140328915
    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: June 19, 2014
    Publication date: November 6, 2014
    Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
  • Publication number: 20140323423
    Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.
    Type: Application
    Filed: May 2, 2014
    Publication date: October 30, 2014
    Applicant: Chrono Therapeutics, Inc.
    Inventors: Guy DiPierro, Steven A. Giannos
  • Patent number: 8871208
    Abstract: A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: October 28, 2014
    Assignee: AbbVie Inc.
    Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
  • Patent number: 8871263
    Abstract: The present invention features a process for making a tablet by (i) compacting a powder blend in a die to form a tablet shape, wherein the powder blend contains a pharmaceutically active agent and a meltable binder and (ii) applying radiofrequency energy to the tablet shape for a sufficient period of time to soften or melt the binder within said tablet shape to form the tablet.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: October 28, 2014
    Assignee: McNeil-PPC, Inc.
    Inventors: Frank J. Bunick, Harry S. Sowden, Joseph R. Luber, Leo B. Kriksunov, Christopher E. Szymczak
  • Publication number: 20140315903
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: HASSAN JULIEN IMOGAI, JOSE MARIA CID-NUNEZ, JOSE IGNACIO ANDRES-GIL, ANDRES AVELINO TRABANCO-SUAREZ, JULEN OYARZABAL SANTAMARINA, FRANK MATTHIAS DAUTZENBERG, GREGOR JAMES MACDONALD, SHRILEY ELIZABETH PULLAN, ROBERT JOHANNES LUTJENS, GUILLAUME ALBERT JACQUES DUVEY, VANTHEA NHEM, TERRY PATRICK FINN, GAGIK MELIKYAN
  • Publication number: 20140315893
    Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi
    Type: Application
    Filed: November 22, 2012
    Publication date: October 23, 2014
    Inventors: Ferenc Fülöp, László Vígh, Zsolt Török, Botond Penke, Ibolya Horváth, Gábor Balogh, Sándor Bernáth, Ákos Hunya
  • Patent number: 8865204
    Abstract: The present invention features a process for making a lozenge product including the steps of forming a powder blend containing an amorphous carbohydrate polymer into the desired shape of the lozenge product and applying radiofrequency energy to the shape for a sufficient period of time to soften or melt said amorphous carbohydrate polymer to fuse the shape into said lozenge product.
    Type: Grant
    Filed: December 18, 2012
    Date of Patent: October 21, 2014
    Assignee: McNeil-PPC, Inc.
    Inventors: Jen-Chi Chen, Harry S. Sowden, Joseph R. Luber, Leo B. Kriksunov, Frank J. Bunick, Christopher E. Szymczak, Gregory E. Koll
  • Publication number: 20140309228
    Abstract: The present disclosure provides substituted pyridine and pyrimidine compounds of Formula (I): A1-X-A2-Z-R1 (I) and the pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein A, X, A, Z, and R are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 16, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: John J. Engel
  • Patent number: 8859593
    Abstract: The invention relates to a pharmacologically active combination, having utility in treating insomnia patients, which comprises: (a) at least one first active ingredient selected from melatonin, other melatonergic agents, melatonin agonists and melatonin antagonists; and (b) at least one second active ingredient selected from nicotine and nicotine receptor agonists; to use of a medicament containing component (a) with or without component (b) for alleviation of at least one adverse effect which occurs in a patient in the course of nicotine replacement therapy, or otherwise, selected from impairment of the quality of sleep, impairment of cognition and impairment of memory, as well as to a kit having utility in treating insomnia patients, which comprises components (a) and (b) in unit dosage form.
    Type: Grant
    Filed: April 15, 2004
    Date of Patent: October 14, 2014
    Assignee: Neurim Pharmaceuticals (1991) Ltd.
    Inventors: Nava Zisapel, Moshe Laudon
  • Patent number: 8859588
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: October 14, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Daniel Hall, David Stefany
  • Publication number: 20140299125
    Abstract: The present disclosure relates to an inhaler component for producing a steam/air mixture or/and condensation aerosol in an intermittent and inhalation- or pull-synchronous manner, the inhaler component including: a housing; a chamber arranged in the housing; an air inlet opening for the supply of air from the surroundings to the chamber; an electrical heating element for evaporating a portion of a liquid material; and a wick having a capillary structure, which wick forms a composite structure with the heating element and automatically supplies the heating element with fresh liquid material after evaporation.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 9, 2014
    Inventor: Helmut BUCHBERGER
  • Publication number: 20140303214
    Abstract: Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 9, 2014
    Inventor: John McCarty
  • Publication number: 20140296237
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: June 12, 2014
    Publication date: October 2, 2014
    Inventors: Hirohide NOGUCHI, Tadashi INOUE, Mikio MORITA, Yoshimasa ARANO
  • Publication number: 20140296287
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specification
    Type: Application
    Filed: March 18, 2014
    Publication date: October 2, 2014
    Applicant: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Publication number: 20140296196
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Patent number: 8846721
    Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer?s Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: January 22, 2011
    Date of Patent: September 30, 2014
    Assignee: Kareus Therapeutics SA
    Inventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
  • Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Patent number: 8841329
    Abstract: The present invention relates to methods of treating and/or ameliorating the severity of inflammation and autoimmunity in the central nervous system (CNS). In one embodiment, the present invention provides a method of treating multiple sclerosis by administering a therapeutically effective dosage of nicotine, or a pharmaceutical equivalent, analog, derivative, or salt thereof.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: September 23, 2014
    Assignee: Dignity Health
    Inventors: Fu-Dong Shi, Ronald J. Lukas, Timothy Vollmer
  • Patent number: 8841287
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
  • Publication number: 20140275086
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140275181
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Jason R. Harris, Qing Xu, Zhe Li
  • Publication number: 20140275087
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Publication number: 20140274940
    Abstract: The use of pectins and/or polymers to prevent nicotine oxidation in tobacco containing products is disclosed. These polymers may be naturally occurring anionic polymers or synthetic polymers. These pectins and/or polymers prevent nicotine from oxidizing into cotinine, nicotine-cis-N-oxide, nicotine-trans-N-oxide, and/or nicotine-1,1-di-N-oxide. Molluscicides, algaecides, pesticides, and stabilized nicotine compositions comprising nicotine and pectin, anionic polymers, or combinations thereof are disclosed.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Altria Client Services Inc.
    Inventors: Munmaya K. Mishra, Jason Flora, Georgios D. Karles, Christophe Claude Galopin, Diane Gee, John B. Paine, III, Douglas Antonio Fernandez
  • Publication number: 20140275182
    Abstract: The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Michael P. Winters
  • Publication number: 20140275079
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Publication number: 20140274957
    Abstract: The present invention includes compositions and methods for treating certain conditions, the composition comprising a choline compound; a cholinesterase inhibitor; and Acetyl-L-Carnitine, wherein the composition is used to treat at least one of autonomic dysfunctions or vascular diseases.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventor: Diana Driscoll
  • Patent number: 8835466
    Abstract: Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumors, bacterial, fungal or viral infections, or autoimmune diseases.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: September 16, 2014
    Assignee: Prodimed, S.A.
    Inventors: Julio Álvarez Builla Gómez, José Luis Novella Robisco, Ma Paz Matía Martín, Sonia Serna Pereda
  • Patent number: 8835464
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: September 16, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140256773
    Abstract: Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III).
    Type: Application
    Filed: May 14, 2014
    Publication date: September 11, 2014
    Inventor: Paresh T. Gandhi
  • Publication number: 20140256734
    Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 11, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
  • Publication number: 20140256728
    Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
  • Publication number: 20140255452
    Abstract: A nicotine-containing pharmaceutical product configured for insertion into the mouth of a user of that product is provided. The product can have an outer water-permeable pouch, a nicotine-containing pharmaceutical composition situated within the outer water-permeable pouch, and product identifying information relating to the nicotine-containing pharmaceutical composition. The information can be presented such that a user of the product can discern the identifying information by visually inspecting the product and thereby differentiate or identify certain nicotine-containing pharmaceutical products. The product identifying can be, for example, printed, imprinted or dyed on the outer water-permeable pouch, positioned within the outer water-permeable pouch, or attached to the outer water-permeable pouch.
    Type: Application
    Filed: March 11, 2013
    Publication date: September 11, 2014
    Applicant: NICONOVUM USA, INC.
    Inventors: Edwin Matthew Reddick, Stephen Taylor Armstrong
  • Patent number: 8829195
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: September 9, 2014
    Assignee: Novartis AG
    Inventors: Stephanie Kay Dodd, Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20140249188
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.
    Type: Application
    Filed: May 16, 2014
    Publication date: September 4, 2014
    Applicant: NERRE THERAPEUTICS LIMITED
    Inventors: Giuseppe ALVARO, Agostino MARASCO
  • Publication number: 20140249125
    Abstract: A polyacrylate formulation suitable for delivery of drug to through a body surface of an individual. By loading the drug and permeation enhancers at a high concentration into a polyacrylate proadhesive that has inadequate adhesive properties for typical adhesive application on the skin, a formulation with desirable adhesive characteristics and effective therapeutic properties can be made. The proadhesive has higher glass transition temperature than typical pressure sensitive adhesives.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: ALZA Corporation
    Inventors: Jay Audett, Jianye Wen, Eli J. Goldman, Robert M. Gale, Allison Luciano, Paul B. Foreman, Eric N. Silverberg
  • 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
  • Patent number: 8822463
    Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: September 2, 2014
    Assignee: Sk Biopharmaceuticals Co., Ltd.
    Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
  • Patent number: 8822504
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: September 2, 2014
    Assignee: Nerre Therapeutics Limited
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Patent number: 8822505
    Abstract: The invention relates to a compound of formula (I) wherein A1, A2 and R1 to R8 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: September 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Lilli Anselm, David Banner, Wolfgang Haap, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Beat Spinnler
  • Patent number: 8822503
    Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: September 2, 2014
    Assignees: Taisho Pharmaceutical Co., Ltd, Nissan Chemical Industries, Ltd.
    Inventors: Takanori Kawaguchi, Kengo Watatani, Keiko Fusegi, Masahiro Bohno, Hajime Asanuma, Shoichi Kuroda, Yudai Imai, Tomomichi Chonan, Nagaaki Sato, Shigeru Tokita, Shigetada Sasako, Takumi Okada, Keishi Hayashi, Shin Itoh, Noriko Saito, Rui Jibiki, Seishi Ishiyama, Hirofumi Ota
  • Patent number: 8822442
    Abstract: The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: September 2, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Zheng Xin Dong, Michael Dewitt Culler, Yeelena Shen
  • 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: 20140243337
    Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup