Piperidines Patents (Class 546/184)
  • Patent number: 8791136
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 29, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 8778969
    Abstract: Nitrone, nitroso, and nitroxide spintraps and spin labels and their reduction products are claimed for the prevention and treatment of fibrocystic disease of breast, premenstrual dysphoric syndrome and associated symptomology, prevention and treatment of migraine headache, cyclic vomiting syndrome, rectal hemorrhoids, trigeminal neuralgia, peripheral vascular disease, influenza, peridontitis and gingivitis, herpes zoster, herpes simplex, and post-herpetic neuralgia.
    Type: Grant
    Filed: November 7, 2010
    Date of Patent: July 15, 2014
    Inventor: Peter H Proctor
  • Patent number: 8772318
    Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: July 8, 2014
    Assignee: The Scripps Research Institute
    Inventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
  • Patent number: 8765959
    Abstract: Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Bernd Nosse, Thorsten Lehmann-Lintz
  • Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Patent number: 8703807
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Werner Neidhart
  • Patent number: 8691993
    Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jefferson Wright Tilley
  • Patent number: 8680102
    Abstract: The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: March 25, 2014
    Assignee: Sanofi
    Inventors: Francis Barth, Daniel Bichon, Murielle Rinaldi-Carmona, Christian Congy
  • Patent number: 8674093
    Abstract: The present invention is directed to processes for preparing a pyridyl piperidine compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: March 18, 2014
    Assignees: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Louis-Charles Campeau, John Y. Chung, Danny Gauvreau, Melina Girardin-Rondeau, Gregory Hughes, Kevin M. Maloney, Christophe Mellon, Jeffrey C. Moore, Paul O'Shea, Stephane Ouellet
  • Patent number: 8669398
    Abstract: The invention relates to novel O-dialkylamino-isoureas and polymerizable compositions comprising these O-dialkylamino-isoureas of compounds of the general formula (I). The invention further relates to the use of O-dialkylamino-isoureas as polymerization initiators, especially to prepare coatings or for controlled degradation of polyolefins.
    Type: Grant
    Filed: December 28, 2009
    Date of Patent: March 11, 2014
    Assignee: BASF SE
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Antoine Carroy, Marc Faller
  • Publication number: 20140046054
    Abstract: The invention relates to a process for preparing amines (A) by alcohol amination of alcohols (Al) by means of an aminating agent (Am) with elimination of water, wherein the alcohol amination is carried out in the presence of a complex catalyst comprising iridium and an amino acid.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 13, 2014
    Applicant: BASF SE
    Inventors: Alexander WETZEL, Michael Limbach, Marion Brinks, Mathias Schelwies
  • Patent number: 8642596
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8637668
    Abstract: Process for preparing a cyclic tertiary methylamine of the formula I where A is a C4-alkylene group, a C5-alkylene group or a —(CH2)2—B—(CH2)2— group, where B is oxygen (O) or an N—R1 radical and R1 is C1-C5-alkyl, aryl or C5-C7-cycloalkyl, wherein an amino alcohol II from the group consisting of 1,4-aminobutanol, 1,5-aminopentanol, aminodiglycol (ADG) or aminoethylethanolamine of the formula IIa where R1 is as defined above or is hydrogen (H), in which case R1?CH3 in the amine I, is reacted with methanol in a reactor at a temperature in the range from 150 to 270° C. in the liquid phase in the presence of a copper-comprising heterogeneous catalyst.
    Type: Grant
    Filed: June 13, 2011
    Date of Patent: January 28, 2014
    Assignee: BASF SE
    Inventors: Christof Wilhelm Wigbers, Johann-Peter Melder, Bernd Stein, Harald Meiβner
  • Patent number: 8624032
    Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: January 7, 2014
    Assignees: The Regents of the University of California, The University of Connecticut
    Inventors: Ohyun Kwon, Gabriel Fenteany
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8604059
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: December 10, 2013
    Assignee: BKG Pharma APS
    Inventor: Birgit Kjældgaard Giwercman
  • Patent number: 8592467
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: November 26, 2013
    Assignee: Abbvie Inc.
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Patent number: 8569313
    Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: October 29, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8557836
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: October 15, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 8546533
    Abstract: The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: October 1, 2013
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Montpellier 1, Universite Jagellone, Universite Montpellier 2—Sciences et Techniques
    Inventors: Jean Martinez, Pawel Zajdel, Maciej Pawlowski, Gilles Subra
  • Patent number: 8546404
    Abstract: Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
    Type: Grant
    Filed: June 5, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, Jr., Neng-Yang Shih, Hugh Y. Zhu, Robert Sun, Joseph M. Kelly, Ronald J. Doll, Yang Nan, Tong Wang, Jagdish A. Desai, James J-S Wang, Youhao Dong, Vincent S. Madison, Li Xiao, Alan W. Hruza, M. Arshad Siddiqui, Ahmed A. Samatar, Sunil Paliwal, Hon-Chung Tsui, Azim Alan Celebi, Yiji Wu, Sobhana Babu Boga, Abdul-Basit Alhassan, Xiaolei Gao, Liang Zhu, Mehul Patel
  • Patent number: 8536341
    Abstract: The invention relates to a process of reacting a primary allylic alcohol with a compound containing a) a metal selected from the group consisting of Ag, Au, Ce, Mn, Ni, Ru, Re, Zn and Co preferably Ag and b) an oxidant like TEMPO (2,2?,6,6?-tetra-methylpiperidin-1-oxyl) or its derivates and c) a co-oxidants selected from the group of peroxodisulfates (PDS), H2SO5, H2O2, NaOCl, O2, KOCl, and air.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: September 17, 2013
    Assignee: DSM IP Assets B.V.
    Inventors: Werner Bonrath, Jean-Francois Eckhard, Manfred L. Eggersdorfer, Ramona Hinze, Wolfgang F. Hölderich, Michael H. Valkenberg
  • Patent number: 8519125
    Abstract: Compositions and methods are disclosed for substantially dry storage at ambient or elevated temperatures of biological samples such as nucleic acids, proteins and cells in a form from which the samples can be substantially recovered, using a dissolvable or dissociable dry storage matrix comprising a borate composition and a stabilizer as disclosed, such as any of a number of zwitterionic stabilizers.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: August 27, 2013
    Assignee: Biomatrica, Inc.
    Inventors: Scott E. Whitney, Sohela De Rozieres, Rolf Muller
  • Patent number: 8518934
    Abstract: The invention relates to oxycarbamoyl compounds of Formula I: The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: June 11, 2009
    Date of Patent: August 27, 2013
    Assignee: Shonogi & Co., Ltd.
    Inventor: Hidenori Mikamiyama
  • Patent number: 8501937
    Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethlamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: August 6, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Dennis J. Hlasta, Mark J. Schulz
  • Patent number: 8501773
    Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhiqiang Yang, David Wisnoski
  • Patent number: 8486971
    Abstract: The invention relates to compounds of the formula (I), where: R1 is: a —NR5R6 group; an unsubstituted or substituted phenyl; R2 is: a (C1-C4)alkyl; an —X—R7 group; R3 and R4 each are independently a substituted phenyl; R5 is a hydrogen atom or a (C1-C4)alkyl; R6 is an unsubstituted or substituted (C1-C4)alkyl; or R5 and R6 together with the nitrogen atom to which they are bonded constitute an unsubstituted or substituted heterocyclic compound; X is a (C1-C5)alkylene; R7 is an —OR8 group, a —NR9R10 group, an —SO2—(C1-C4)alkyl group; R8 is a hydrogen atom or a (C1-C4)alkyl; R9 is a hydrogen atom or a (C1-C4)alkyl; R10 is a hydrogen atom, a —COR11 group, an —SO2R11 group or a —CO(CH2)mOH group; R11 is an unsubstituted or substituted (C1-C4)alkyl; m is 1, 2 or 3. The invention also relates to methods for preparing same and to the therapeutic use thereof.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Jean-Philippe Ducoux, Murielle Rinaldi-Carmona, Arnaud Rouquette
  • Patent number: 8481726
    Abstract: The present invention relates to a novel process for the preparation of specific sterically hindered nitroxyl ethers from their corresponding sterically hindered nitroxyl radicals by reacting it with an aldehyde and a hydroperoxide. This nitroxyl ether formation may be carried out from different starting nitroxyl radicals, which are subsequently further reacted to the desired compounds. The compounds prepared by this process are effective as stabilizers for polymers against harmful effects of light, oxygen and/or heat and as flame-retardants for polymers.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: July 9, 2013
    Assignee: BASF SE
    Inventors: Abdel-Ilah Basbas, Davide Alvisi, Robert Cordova, Michael Peter Difazio, Walter Fischer, Joseph A. Kotrola, Tiziano Nocentini, James Robbins, Kai-Uwe Schöning
  • Patent number: 8471031
    Abstract: The present invention relates to a novel process for the preparation of a sterically hindered nitroxyl ether from the corresponding sterically hindered nitroxyl radical by reacting it with a carbonyl compound and a hydroperoxide. The compounds prepared by this process are effective stabilizers for polymers against harmful effects of light, oxygen and/or heat, as flame-retardants for polymers and as polymerization regulators.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: June 25, 2013
    Assignee: BASF SE
    Inventors: Kai-Uwe Schöning, Walter Fischer, Abdel-Ilah Basbas, Alexander Dichtl
  • Patent number: 8470841
    Abstract: Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: June 25, 2013
    Assignee: Sanofi
    Inventors: Gerhard Zoller, Dieter Schmoll, Marco Mueller, Guido Haschke, Ingo Focken
  • Patent number: 8461184
    Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: June 11, 2013
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Vliet Van
  • Patent number: 8440691
    Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: May 14, 2013
    Assignee: AbbVie Inc.
    Inventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
  • Publication number: 20130109572
    Abstract: Disclosed are compositions and methods of preparing compositions of active herbicidal ingredients. Also disclosed are methods of using the compositions described herein to improve herbicide delivery and efficacy, enhance herbicidal penetration, reduce herbicide volatility and drift, diminish environmental damage from herbicides, decrease water solubility and volatility of herbicides, and introduce additional biological function to herbicides.
    Type: Application
    Filed: July 6, 2011
    Publication date: May 2, 2013
    Applicant: The Board of Trustees of the University of Alabama
    Inventors: Juliusz Pernak, Julia Shamshina, Praczyk Tadeusz, Anna Syguda, Dominika Janiszewska, Marcin Smiglak, Gabriela Gurau, Daniel T. Daly, Robin D. Rogers
  • Publication number: 20130102506
    Abstract: A lubricating base oil includes at least one of ionic liquids containing a compound represented by a formula (1): Z+A?, in which Z+ represents a cation and A? represents an anion, in which Z+ is a cyclic quaternary ammonium ion having two different side chains and A? is a conjugated amide ion.
    Type: Application
    Filed: July 27, 2011
    Publication date: April 25, 2013
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Yukio Yoshida, Yukitoshi Fujinami
  • Patent number: 8426587
    Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: (I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: April 23, 2013
    Assignee: Pharmaxis Ltd.
    Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
  • Patent number: 8410091
    Abstract: The present invention is related to a process of preparing substituted 2-amino-5-(5-(heterocyclemethyl)pyridin-2-yloxy)benzoic acid compound of formula (I) or a salt thereof,
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: April 2, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Magnus Carl Arne Eriksson, Dhileepkumar Krishnamurthy, Xiao-Jun Wang, Li Zhang
  • Patent number: 8410137
    Abstract: The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n?—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: April 2, 2013
    Assignee: Sanofi
    Inventors: Francis Barth, Jean-Philippe Ducoux, Patrick Gueule, Murielle Rinaldi-Carmona, Arnaud Rouquette
  • Patent number: 8404689
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: March 26, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 8404900
    Abstract: An absorbent for separating acidic gases is disclosed. The absorbent or an absorbent composition for separating acidic gases has more than 3 kinds of compounds along with Chemical Formula 1 and 2, and has ability of rapid carbon dioxide elimination, excellent absorption ability, and less energy consumption for regenerating an absorbent due to easy desorption of carbon dioxide.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: March 26, 2013
    Assignee: Korea Electric Power Corporation
    Inventors: Jun-Han Kim, Jae-Goo Shim, Kyung-Ryong Jang, Ji-Hyun Lee
  • Patent number: 8399497
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 8383666
    Abstract: The subject of the invention is Compound of Formula (I): in which R1-R8 and R10 are defined within, its method of preparation, and its therapeutic application.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: February 26, 2013
    Assignee: Sanofi
    Inventors: Francis Barth, Audrey Jeanjean, Murielle Rinaldi-Carmona, Christian Congy
  • Patent number: 8362164
    Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: January 29, 2013
    Assignee: Bridgestone Corporation
    Inventor: Yan Yan-Yong
  • Patent number: 8324250
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: December 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 8324248
    Abstract: The present invention relates to a compounds of formula I wherein A, Ar1, Ar2, R1, R2, R3, R4, R5, R6, m, n, o, p, s, t, and u are as defined herein or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: December 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Publication number: 20120302756
    Abstract: The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
    Type: Application
    Filed: February 17, 2011
    Publication date: November 29, 2012
    Inventors: Rajender Reddy Leleti, Yugang Liu, Mahavir Prashad
  • Patent number: 8288531
    Abstract: A process for preparing compounds of the formula (I) in which R1 and R2 are as defined in the description.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: October 16, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Schnaubelt, Thomas Fachinger, Michael Konrad, Thomas Krueger, Joern Merten, Carsten Reichel, Svenja Renner, Rolf Schmid, Emanuel Stehle, Bianca Werner