Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/244)
  • Patent number: 10577384
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: March 3, 2020
    Assignee: Helsinn Healthcare SA
    Inventors: Claudio Giuliano, Silvina Garcia Rubio, Antoine Daina, Angelo Guainazzi, Claudio Pietra
  • Patent number: 10287305
    Abstract: Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: May 14, 2019
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tatsuhiko Fujimoto, Kentaro Rikimaru, Hiromichi Sugimoto, Takahiro Matsumoto
  • Patent number: 9096523
    Abstract: A cyclic amine compound having a prescribed configuration can be efficiently prepared by reducing an imine derivative in the presence of a sulfonic acid. Specifically, a cyclic amine compound which is substituted with an amino group and a carboxyl group in which both groups are arranged in the trans configuration can be prepared efficiently.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: August 4, 2015
    Assignee: KANEKA CORPORATION
    Inventors: Yoshinori Hirai, Akira Nishiyama
  • Patent number: 9034903
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: May 19, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
  • Patent number: 9035062
    Abstract: A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.
    Type: Grant
    Filed: May 27, 2014
    Date of Patent: May 19, 2015
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Publication number: 20150065718
    Abstract: A method for preparing 1-adamantyltrimethylammonium methylcarbonate or N,N-dimethyl-3,5-dimethylpiperidinium methylcarbonate is disclosed. The method comprises reacting dimethyl carbonate and 3,5-dimethylpiperidine or a 1-adamantylamine compound and in the presence of water in a sealed vessel at a temperature of from 80 to 200° C. The 1-adamantylamine compound is 1-adamantylamine, 1-adamantylmethylamine, or mixtures thereof.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Inventor: RICHARD CHARLES BRYAN
  • Publication number: 20150011586
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 8, 2015
    Inventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
  • Publication number: 20140303375
    Abstract: A process for preparing the compound of the following formula (E): wherein Bn represents a benzyl group, and tBu represents a tert-butyl group, the process including: (a) subjecting the following compound (B) to trifluoroacetylation, wherein tBu represents a tert-butyl group to produce the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; (b) reacting the compound (C) with benzyloxyamine in the presence of a hydroxyl group activating agent to produce the following compound (D): wherein Bn represents a benzyl group, tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group; and (c) subjecting the compound (D) to detrifluoroacetylation.
    Type: Application
    Filed: May 27, 2014
    Publication date: October 9, 2014
    Applicant: Meiji Seika Pharma. Co., Ltd.
    Inventors: Takao ABE, Masayuki OKUE, Yoshiaki SAKAMAKI
  • Publication number: 20140296526
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: May 10, 2014
    Publication date: October 2, 2014
    Applicant: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Publication number: 20140275126
    Abstract: Disclosed is a process for the preparation of the following compounds: where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesise downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Philip PYE, Cyril BEN HAIM, Matteo CONZA, Ioannis Nicolaos HOUPIS
  • Patent number: 8829191
    Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: September 9, 2014
    Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew John Phillips, Mahendra G. Dedhiya
  • Publication number: 20140235636
    Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20140221428
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 7, 2014
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei LY, Garrett Thomas POTTER, Jared Andrew FORRESTER
  • Patent number: 8791264
    Abstract: The invention relates to piperidinyl and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z and q are defined as set forth in the specification. 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: April 13, 2007
    Date of Patent: July 29, 2014
    Assignee: Purdue Pharma L.P.
    Inventors: Zhengming Chen, Bin Shao, Jiangchao Yao, Xiaoming Zhou
  • Publication number: 20140203226
    Abstract: A photochromic curable composition that contains a (meth)acrylate compound represented by the following formula (1-X1); (wherein Y is an oxygen atom or a divalent group represented by —NH—, R1 and R2 are hydrogen atoms or methyl groups, R3 is an alkylene group having 1 to 6 carbon atoms, R4 is an alkylene group having 1 to 6 carbon atoms, a cycloalkylene group having 3 to 8 carbon atoms and which may include a double bond, or an arylene group having 6 to 10 carbon atoms, and a is a positive number of 1 to 20), other radically polymerizable monomers and a photochromic compound. The invention provides a lens that features excellent durability and high photochromic property free of the problems of turbidity in the surfaces of the lens caused by bleed out or the peeling in the step of production.
    Type: Application
    Filed: October 15, 2012
    Publication date: July 24, 2014
    Applicant: Tokuyama Corporation
    Inventors: Junji Takenaka, Junji Momoda
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8748617
    Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: June 10, 2014
    Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.
    Inventors: Hiroaki Suga, Jun Igarashi
  • Patent number: 8741894
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 3, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter, Jared Andrew Forrester
  • Patent number: 8669257
    Abstract: The present invention provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein each of W, Q, R1, R2, R3, R4, R5, m, and n is as defined herein, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: March 11, 2014
    Assignee: The Johns Hopkins University
    Inventors: Jun O. Liu, Yunzhao Ren, Fan Pan, Curtis R. Chong, Reinhold Penner, Jonathan R. Behr
  • Publication number: 20140018317
    Abstract: A compound having a structure of:
    Type: Application
    Filed: February 17, 2012
    Publication date: January 16, 2014
    Applicant: University of Pittsburgh-Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Patent number: 8624022
    Abstract: The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: January 7, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Andrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
  • Patent number: 8623887
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, Rg, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephan Karl Zahn, Bojan Bister, Guido Boehmelt, Ulrich Guertler, Andreas Mantoulidis, Ulrich Reiser, Andreas Schoop, Flavio Solca, Ulrike Tontsch-Grunt, Matthias Treu
  • 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
  • Publication number: 20130281702
    Abstract: A method and an intermediate are provided for preparing fentanyl. Aniline and 1-phenylethyl-4-piperidone are reacted with a borane complex, in a lower C1-C4 alcoholic solvent, in the presence of an alkanoic acid. The reaction mixture is then treated with a hydrohalic acid to precipitate 4-anilino-N-phenethyl-4-piperidine (ANPP) as the bis-hydrohalide salt in high yield and purity. This ANPP salt may be directly treated with propionyl halide to produce fentanyl, or the ANPP salt may be converted to the free base of ANPP and similarly treated with propionyl halide to produce fentanyl.
    Type: Application
    Filed: April 23, 2013
    Publication date: October 24, 2013
    Inventors: Jonathan P. Pease, Anthony J. LePine, Catherine M. Smith
  • Publication number: 20130274475
    Abstract: Substituted bicyclic beta-lactams of Formula I: are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 17, 2013
    Inventors: Ian MANGION, Nelo Rivera, Rebecca T. Ruck, Michael Shelvin
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Patent number: 8492111
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: July 23, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
  • Publication number: 20130158050
    Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: February 14, 2013
    Publication date: June 20, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8466238
    Abstract: The invention aims to provide latent curing agents which exert high low-temperature curing properties when used together with ionically polymerizable compounds and which exhibit high storage stability at room temperature. Latent curing agents for ionically polymerizable compounds which agents each contain a hydroxyl-free amine imide compound having an N—N bond energy of 100 to 210 kJ/mol as determined by B3LYP functional theory method.
    Type: Grant
    Filed: December 26, 2008
    Date of Patent: June 18, 2013
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Hiroaki Tamatani, Mitsuaki Chida, Yugo Yamamoto, Yuichi Ito, Takashi Nakano, Naritoshi Yoshimura
  • Publication number: 20130116216
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 9, 2013
    Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
  • Patent number: 8399486
    Abstract: The invention relates to pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, Z and m are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat 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: April 8, 2008
    Date of Patent: March 19, 2013
    Assignee: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Jiangchao Yao
  • Publication number: 20130065756
    Abstract: Compounds of the formula I wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Application
    Filed: November 22, 2010
    Publication date: March 14, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Publication number: 20130012712
    Abstract: The disclosure relates to a method for preparing a compound of formula (I), wherein P1 and P2 are groups protecting the carboxylic acid and oxyamine functions, starting from pyroglutamic acid (S). The disclosure also relates to novel intermediates.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: FOREST LABORATORIES HOLDINGS LTD.
    Inventors: Alain Priour, Alain Bonnet, Gilles Oddon, Alain Mazurie
  • Patent number: 8350042
    Abstract: Disclosed are compounds and methods of synthesis of Formula I for the development of antiviral drugs for the treatment of HCV infection.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: January 8, 2013
    Assignee: The Regents of the University of California
    Inventors: Thomas C. Hermann, Maia Carnevali
  • Patent number: 8338439
    Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same. In some embodiments, the present invention provides a compound of formula I-a or I-b: wherein each of Ring A, Ring B, W1, W2, Ry, Rv, Rx, m, p, and R1 is described herein.
    Type: Grant
    Filed: December 29, 2009
    Date of Patent: December 25, 2012
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Publication number: 20120323010
    Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
    Type: Application
    Filed: June 15, 2012
    Publication date: December 20, 2012
    Applicant: FOREST LABORATORIES HOLDINGS LTD.
    Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew John Phillips, Mahendra G. Dedhiya
  • Publication number: 20120296094
    Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
    Type: Application
    Filed: August 6, 2012
    Publication date: November 22, 2012
    Applicants: OTSUKA CHEMICAL CO., LTD., UNIVERSITY OF TOKYO
    Inventors: Hiroaki SUGA, Jun Igarashi
  • Publication number: 20120289548
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Application
    Filed: June 29, 2012
    Publication date: November 15, 2012
    Applicant: Nektar Therapeutics
    Inventors: Jennifer RIGGS-SAUTHIER, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 8304403
    Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: November 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120277250
    Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 1, 2012
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
  • Patent number: 8288553
    Abstract: The disclosure relates to a method for preparing a compound of formula (I), wherein P1 and P2 are groups protecting the carboxylic acid and oxyamine functions, starting from pyroglutamic acid (S). The disclosure also relates to novel intermediates.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: October 16, 2012
    Inventors: Alain Priour, Alain Bonnet, Gilles Oddon, Alain Mazurie
  • Publication number: 20120245026
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as pesticides.
    Type: Application
    Filed: November 30, 2010
    Publication date: September 27, 2012
    Applicant: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Publication number: 20120238452
    Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1, are useful as a pesticides.
    Type: Application
    Filed: November 29, 2010
    Publication date: September 20, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Michel Muehlebach, Jurgen Harry Schaetzer
  • Patent number: 8258307
    Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: September 4, 2012
    Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.
    Inventors: Hiroaki Suga, Jun Igarashi
  • Patent number: 8252934
    Abstract: 4-amino-2,2,6,6-tetramethylpiperidine is prepared by reacting 2,2,6,6-tetramethylpiperidine-4-one with ammonia and hydrogen in the presence of nickel and/or cobalt catalyst and water. The main reaction is carried out at a pressure of at most 50 bar and a temperature of at most 120° C. up to a conversion of the 2,2,6,6-tetramethylpiperidine-4-one of at least 80%. Then, an after-reaction takes place at a higher temperature and at a higher pressure compared to the pressure and temperature of the main reaction.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: August 28, 2012
    Assignee: Evonik Degussa GmbH
    Inventors: Volker Brehme, Daniel Dembkowski
  • Publication number: 20120136073
    Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.
    Type: Application
    Filed: November 15, 2011
    Publication date: May 31, 2012
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Zhiwei Yang, Parul Angrish, Xavier de Mollerat du Jeu, Kristin Wiederholt
  • Patent number: 8188277
    Abstract: The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.
    Type: Grant
    Filed: August 3, 2005
    Date of Patent: May 29, 2012
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Tae Fukushima, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
  • Publication number: 20120071659
    Abstract: The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques.
    Type: Application
    Filed: September 15, 2011
    Publication date: March 22, 2012
    Applicant: Mallinckrodt LLC
    Inventors: Brian ORR, Joseph P. HAAR, JR., George H. KLEMM, Keith G. TOMAZI