Plural Six-membered Hetero Rings Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/332)
  • Patent number: 10688087
    Abstract: A pharmaceutical composition for treatment of a pathological condition in a patient comprises, as a first component, a manganese complex of Formula I( ), and, as a second component, a non-manganese complex compound of Formula (I), optionally together with one or more physiologically acceptable carriers and/or excipients, wherein X, R, R, R, and R are as defined herein. Methods for treatment of a pathological condition in a patient, for example, a pathological condition caused by the presence of oxygen-derived free radicals, comprises administering to said patient the first component and the second component.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: June 23, 2020
    Assignee: PLEDPHARMA AB
    Inventors: Jan-Olof Karlsson, Rolf Andersson
  • Patent number: 10653685
    Abstract: A pharmaceutical composition including N,N,N?,N?-tetrakis-(2-pyridylmethyl)-ethylenediamine (TPEN) or a pharmaceutically acceptable salt thereof, an alginate compound, and a pharmaceutically acceptable carrier. The pharmaceutical composition is useful for the treatment of hypoxia-related diseases.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: May 19, 2020
    Inventor: Jerachmiel Yori Appelbaum
  • Patent number: 10383849
    Abstract: The present invention relates to the use of an acetylcholinesterase inhibitor and idalopirdine for reducing falls in patients suffering from a CNS disease, in particular patients with Parkinson's disease, wherein balance, gait or movement is impaired.
    Type: Grant
    Filed: April 25, 2017
    Date of Patent: August 20, 2019
    Assignee: H. LUNDBECK A/S
    Inventors: Inge E. M. de Jong, Aaron Kucinski, Martin Sarter
  • Patent number: 10034889
    Abstract: The purpose of the present invention is to identify a migratory factor that guides pluripotent stem cells (Muse cells) useful in new medical applications to damage, and to provide a pharmaceutical composition that includes the migratory factor for promoting tissue regeneration in regenerative medicine that makes use of Muse cells. In the present invention, a receptor that is specifically expressed in Muse cells rather than non-Muse cells was identified, and it was confirmed that a ligand for this receptor can function as a migratory factor. In the present invention, sphingosine-1-phosphate (S1P) was identified as a migratory factor, and thus, the present invention pertains to a pharmaceutical composition for guiding pluripotent stem cells to damage, the composition including S1P as an active ingredient.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: July 31, 2018
    Assignees: CLIO, INC., TOHOKU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Mari Dezawa, Yoshinori Fujiyoshi, Masanori Yoshida
  • Patent number: 10011594
    Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
    Type: Grant
    Filed: June 2, 2016
    Date of Patent: July 3, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Soong-Hoon Kim, R. Michael Lawrence, Michael C. Myers, Hannguang J. Chao, Monique Phillips, Ji Jiang
  • Patent number: 9988355
    Abstract: The invention discloses a form A of mesylate for nicotinamide derivatives and preparation method and application thereof, wherein the XRPD pattern of the form A of mesylate for nicotinamide derivatives has a diffraction peak at 2?=5.34, 10.341, 14.438, 15.841, 17.32, 18.301, 18.68, 19.005, 19.577, 20.26, 21.161, 21.859, 22.379, 23.04, 23.5, 24.177, 24.959, 25.881, 26.641, 27.18, 28.3, 28.999, 29.501, 31.96, 32.258, 33.999, 36.798, 37.38 and 41.297 with the error range of the 2? values being ±0.2. The form A of mesylate for nicotinamide derivatives provided by the present invention has excellent high-temperature stability, high-humidity stability and illumination stability, and it can be applied to drugs for treating advanced non-small cell lung cancers, gastric cancers, liver cancer or breast cancer. It has preferable bioavailability, and meanwhile the provided qualitative and quantitative information has great significance on further study of the efficacy of such solid drugs.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: June 5, 2018
    Assignee: SHANGHAI SUNTRONG BIOTECHNOLOGY CO., LTD.
    Inventors: Yinglu Yu, Jinyao Chen, Dongxu Yi
  • Patent number: 9908878
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: March 6, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, Michael J. Boyd, Ioana Davies, Hongbo Deng, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Brian Ledford, Mark W. Ledeboer, Francois Maltais, Emanuele Perola, Tiansheng Wang
  • Patent number: 9877954
    Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: April 3, 2017
    Date of Patent: January 30, 2018
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Lücking, Niels Böhnke, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Dirk Kosemund, Rolf Bohlmann, Ludwig Zorn
  • Patent number: 9856242
    Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: January 2, 2018
    Assignee: Bayer Pharma Aktiengesellscaft
    Inventors: Dirk Kosemund, Ulrich Lücking, Arne Scholz, Gerhard Siemeister, Philip Lienau
  • Patent number: 9770444
    Abstract: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: September 26, 2017
    Assignee: MAX-PLANCK-GESELLSCHAFT-ZUR-FÖRDERUNG DER WISSENSCHAFTEN E.V
    Inventors: Gregor Eichele, Henrik Oster, Silke Kiessling
  • Patent number: 9750731
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: September 5, 2017
    Assignee: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos Petasis
  • Patent number: 9701660
    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: Grant
    Filed: September 30, 2014
    Date of Patent: July 11, 2017
    Assignee: AC Immune S.A.
    Inventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
  • Patent number: 9656991
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: May 23, 2017
    Assignee: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, André J. Niestroj, Robert Sommer
  • Patent number: 9540323
    Abstract: The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments.
    Type: Grant
    Filed: July 30, 2013
    Date of Patent: January 10, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alexandre L'Heureux, Sheldon Hiebert, Carol Hu, Patrick Y. S. Lam, John Lloyd, Zulan Pi, Jennifer X. Qiao, Carl Thibeault, George O. Tora, Wu Yang, Yufeng Wang, Tammy C. Wang, Michael S. Bowsher, Ruel Rejean
  • Patent number: 9458151
    Abstract: PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, multi drug resistance, and inflammatory bowel disease. Also provided are methods for preparing and using the compounds represented by Formula I.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: October 4, 2016
    Assignee: Jikai Biosciences, Inc.
    Inventor: Yu Ge
  • Patent number: 9453003
    Abstract: PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, multi drug resistance, and inflammatory bowel disease. Also provided are methods for preparing and using the compounds represented by Formula I.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: September 27, 2016
    Assignee: Jikai Biosciences, Inc.
    Inventor: Yu Ge
  • Patent number: 9446033
    Abstract: The purpose of the present invention is to identify a migratory factor that guides pluripotent stem cells (Muse cells) useful in new medical applications to damage, and to provide a pharmaceutical composition that includes the migratory factor for promoting tissue regeneration in regenerative medicine that makes use of Muse cells. In the present invention, a receptor that is specifically expressed in Muse cells rather than non-Muse cells was identified, and it was confirmed that a ligand for this receptor can function as a migratory factor. In the present invention, sphingosine-1-phosphate (S1P) was identified as a migratory factor, and thus, the present invention pertains to a pharmaceutical composition for guiding pluripotent stem cells to damage, the composition including S1P as an active ingredient.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: September 20, 2016
    Assignees: CLIO, INC., TOHOKU UNIVERSITY, NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Mari Dezawa, Yoshinori Fujiyoshi, Masanori Yoshida
  • Patent number: 9447023
    Abstract: The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: September 20, 2016
    Assignee: Research Foundation of the City University of New York
    Inventors: Krishnaswami Raja, Probal Banerjee, Andrew Auerbach, Wei Shi, William L'Amoreaux
  • Patent number: 9187397
    Abstract: Curcumin analogues and methods are provided for treatment of disease.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: November 17, 2015
    Assignee: STC.UNM
    Inventors: David L. Vander Jagt, Lorraine M. Deck, Steve F. Abcouwer, Robert A. Orlando, Robert E. Royer, Waylon M. Weber, Ekaterina V. Bobrovnikova-Marjon, Lucy A. Hunsaker
  • Patent number: 9156788
    Abstract: Disclosed herein are modulators of TRPV3 of formula (I) wherein G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: October 13, 2015
    Assignee: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Eric A. Voight
  • Patent number: 9096525
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: August 4, 2015
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Patent number: 9095582
    Abstract: The present application relates to novel substituted aryloxazole derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: August 4, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Jorg Keldenich, Alexandros Vakalopoulos, Frank Süssmeier, Katja Zimmermann, Dieter Lang, Daniel Meibom
  • Patent number: 9090561
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: July 28, 2015
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
  • Patent number: 9079889
    Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: July 14, 2015
    Assignee: NOVARTIS AG
    Inventors: Matthew T. Burger, Wooseok Han, Jiong Lan, Gisele Nishiguchi
  • Publication number: 20150141433
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 21, 2015
    Inventors: David R. Anderson, Robert A. Volkmann
  • Publication number: 20150141462
    Abstract: The present invention relates to pharmaceutical compositions comprising (a) a pharmaceutically effective amount of an mGluR5 positive allosteric modulator, derivative, prodrug or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically effective amount of an agent selected from an NMDA partial agonist or a GlyT1 inhibitor, derivative, prodrug or a pharmaceutically acceptable salt thereof; and (c) a pharmaceutically acceptable carrier. The present invention also relates to methods for treating drug addiction and preventing a drug relapse in a patient.
    Type: Application
    Filed: June 11, 2013
    Publication date: May 21, 2015
    Inventor: M. Foster Olive
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Patent number: 9028873
    Abstract: The present disclosure relates to compositions and methods for producing nanoparticles to provide relatively more rapid delivery of such particles across the blood-brain barrier. The nanoparticles may be formed from bis-quaternary pyridinium-aldoxime salts that may also be of a specific polymorphic structure and which may be formed in either hydrophobic or hydrophilic type liquid media. In addition, the nanoparticle for transport across the blood-brain barrier may comprise a polymeric resin encapsulating a bis-quaternary pyridinium-2-aldoxime salt.
    Type: Grant
    Filed: February 8, 2010
    Date of Patent: May 12, 2015
    Assignee: Southwest Research Institute
    Inventors: Joseph A. McDonough, Hong Dixon, Larry A. Cabell
  • Publication number: 20150126557
    Abstract: The invention relates to octenidine or a pharmaceutical salt thereof, in particular octenidine dihydrochloride, which is intended for mutual therapeutic administration of the octenidine in solution with a polyalcohol of formula (1a) or (1b): (H—C—OH)a(HO—C—OH)b(H—C—H)c(CHO)??(1a), (H—C—OH)a(HO—C—OH)b(H—C—H)c(CO)??(1b), wherein a, b, c are whole numbers, where a+b is at least 2, preferably at least 3, c is selected from 0, 1 or a number from 2 to a+b, provided that the aldehyde group of formula (1a) is in a form of an acetal with one of the hydroxy groups or the keto group of formula (1b) is in a form of an acetal with one of the hydroxy groups. The invention also relates to kits containing these ingredients, and use thereof for treating infections and wounds.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: ARTAN HOLDING AG
    Inventor: Ahmet Melih AYDINOGLU
  • Patent number: 9017735
    Abstract: Disclosed herein are compositions and methods for treating a psychiatric disorder or symptoms thereof in a patient. The compositions comprise a compound that modulates KCNQ (Kv7) potassium channel activity and the methods include administering an effective amount of the compound that modulates KCNQ (Kv7) potassium channel activity.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: April 28, 2015
    Assignee: Marquette University
    Inventor: Mohammadhossein Behnam Ghasemzadeh
  • Patent number: 9018233
    Abstract: The invention relates to diaminoaryl derivatives substituted by carbamate, salts thereof and a pesticidal composition containing the same, which exhibit superior pest control effects against various insect pests of insect species, in particular against moths such as the diamondback moth or Spodoptera litura.
    Type: Grant
    Filed: May 7, 2013
    Date of Patent: April 28, 2015
    Assignees: Kyung Nong Corporation, Korea Research Institute of Chemical Technology
    Inventors: Sung Youn Chang, Jung Nyoung Heo, Hyuk Lee, Hwan Jung Lim, Bum Tae Kim, Joo Kyung Kim, Jong-Kwan Kim
  • Publication number: 20150111879
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 24, 2014
    Publication date: April 23, 2015
    Applicants: CURIS, INC., GENENTECH, INC.
    Inventors: Janet L. GUNZNER, Daniel P. SUTHERLIN, Mark S. STANLEY, Liang BAO, Georgette M. CASTANEDO, Rebecca L. LALONDE, Shumei WANG, Mark E. REYNOLDS, Scott J. SAVAGE, Kimberly MALESKY, Michael S. DINA, Michael F.T. KOEHLER
  • Publication number: 20150105428
    Abstract: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Gregor Eichele, Henrik Oster, Silke Kiessling
  • Publication number: 20150105427
    Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Shinzo KAGABU, Masaaki MITOMI, Shigeki KITSUDA, Ryo HORIKOSHI, Masahiro NOMURA, Yasumichi ONOZAKI
  • Publication number: 20150104496
    Abstract: The present invention relates to a composition containing at least one nutritive, at least one disinfecting or decontaminating and/or at least one protease-inhibiting active compound and/or active compound complex for the external care and/or treatment of wounds of the human or animal body.
    Type: Application
    Filed: October 21, 2014
    Publication date: April 16, 2015
    Inventor: Birgit RIESINGER
  • Patent number: 9006269
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: April 14, 2015
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Publication number: 20150094338
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 2, 2015
    Applicant: PFIZER INC.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8980925
    Abstract: The present invention is directed to compositions useful for antimicrobial applications. These compositions comprise amphiphilic compounds.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: March 17, 2015
    Assignee: James Madison Innovations, Inc.
    Inventors: Kevin P. Minbiole, Kevin L. Caran, Kyle N. Seifert
  • Publication number: 20150073021
    Abstract: The present invention provides a method of inhibiting the binding of anthrax lethal factor with protective antigen comprising contacting the anthrax lethal factor with a compound having the structure:
    Type: Application
    Filed: September 5, 2014
    Publication date: March 12, 2015
    Applicants: The Research Foundation for The State University of New York, Chem-Master International, Inc.
    Inventors: Anthony ANTONELLI, Sanford R. SIMON, Yu ZHANG, Lorne M. GOLUB, Francis JOHNSON
  • Publication number: 20150057280
    Abstract: The invention relates to pyridylidene compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted pyridylidene compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Applicant: BASF SE
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
  • Publication number: 20150057288
    Abstract: A pest control method for honeybee parasitic pests has been found, which is highly safe to honeybees and demonstrates excellent pest control effects against honeybee parasitic pests by using a honeybee parasitic pest control agent containing at least one of a compound represented by Formula (I) and acid addition salts thereof.
    Type: Application
    Filed: November 10, 2014
    Publication date: February 26, 2015
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Ryo HORIKOSHI, Masaaki MITOMI
  • Publication number: 20150057289
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Application
    Filed: November 4, 2014
    Publication date: February 26, 2015
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Patent number: 8956589
    Abstract: Disclosed are a curcumin derivative or a salt thereof, which contains a fluorine atom, represented by formula (I): (wherein R1a and R1b are each independently a hydrogen atom, alkyl, acetyl, or methoxycarbonyl; R2s are each independently a fluorine atom, CHF2—, CF3—, CHF2O—, or CF3O—; R3s are each independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxyl, alkoxycarbonyl, or R4—(CH2)m—; R4 is hydroxy, carboxy, cyano, acetyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR5R6; R5 and R6 are each independently a hydrogen atom or alkyl; and m is an integer from 1 to 5), and a diagnostic imaging agent for diagnosing a disease in which an amyloid ? peptide aggregate accumulates, the diagnostic imaging agent containing a compound having a 1,3-dicarbonyl structure, wherein the compound exists in a keto form and an enol form, and the keto form and the enol form have different affinities, respectively, to the amyloid ? peptide aggregate.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: February 17, 2015
    Assignee: Shiga University of Medical Science
    Inventors: Ikuo Tooyama, Hiroyasu Taguchi, Shigehiro Morikawa, Makoto Urushitani, Daijiro Yanagisawa, Tomone Nagae, Nobuaki Shirai, Koichi Hirao, Masanari Kato, Hirohiko Kimura, Takashi Okada
  • Patent number: 8957214
    Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: February 17, 2015
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Ryo Horikoshi, Masahiro Nomura, Yasumichi Onozaki
  • Publication number: 20150037397
    Abstract: The present invention relates to pharmaceutical compositions comprising a compound of formula (I) and a cyclodextrin or a liposome, to the process of preparing said compositions and their use for antitumor, antiviral, antiparasitic and antifungal treatment.
    Type: Application
    Filed: December 22, 2011
    Publication date: February 5, 2015
    Applicant: TRASLATIONAL CANCER DRUGS PHARMA, S.L.
    Inventors: Beatriz Palacios Izquierdo, Peter Van HoogeVest, Mathew L.S. Leigh
  • Patent number: 8946263
    Abstract: The present invention relates to a modulator of glucocorticoid biosynthesis, degradation and/or receptor activation for use in preventing or treating symptoms and/or diseases associated with jet lag. The compositions of the invention may be used as a lead compound for developing a drug for preventing or treating symptoms and/or diseases associated with jet lag. The invention relates to the discovery that administration of the modulator(s) to a subject results in a directional change of the time point of maximum amounts of glucocorticoids in the subject as compared to the time point of maximum amounts of glucocorticoids in a subject not treated with the modulator(s).
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: February 3, 2015
    Assignee: Max-Planck-Gesellchaft zur Forderung der Wissenschaften E.V.
    Inventors: Gregor Eichele, Henrik Oster, Silke Kiessling
  • Patent number: 8940324
    Abstract: The invention relates to octenidine or a pharmaceutical salt thereof, in particular octenidine dihydrochloride, which is intended for mutual therapeutic administration of the octenidine in solution with a polyalcohol of formula 1: (H—C—OH)a(HO—C—OH)b(H—C—H)c, where a, b, c are whole numbers, where a+b is at least 2, preferably at least 3, c is selected from 0, 1 or a number from 2 to a+b, optionally in addition to one or more aldehyde groups provided that they form (cyclic) acetals with one of the hydroxy groups or one or more keto groups optionally as acetal with one of the hydroxy groups, optionally in addition to one or more carboxylic acid groups if the polyalcohol is a cyclic acetal or acetal, preferably with ring sizes of 5 to 7 atoms, or a polymer, polyether or polyester thereof, provided that the polyalcohol exists as a polymer, polyether or polyester with at least two units of formula 1 if a+b is 2 or 3.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: January 27, 2015
    Assignee: Artan Holding AG
    Inventor: Ahmet Melih Aydinoglu
  • 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
  • Publication number: 20150018321
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 15, 2015
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
  • Patent number: 8933103
    Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: January 13, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu