Addition Salts Of Morpholine Which Is Unsubstituted Or Hydrocarbyl Substituted Only Patents (Class 544/107)
  • Patent number: 10669496
    Abstract: The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: June 2, 2020
    Assignee: The Lubrizol Corporation
    Inventors: James H. Bush, Robert H. Barbour, David J. Moreton, Hannah Greenfield, Paul R. Stevenson, David C. Arters
  • Patent number: 10411301
    Abstract: The present disclosure provides an ionic liquid and a preparation method thereof, in particular, the present disclosure provides an ionic liquid whose halogen anions content and moisture content are low, and a method for preparing the same. The total content of halogen anions in the ionic liquid is less than 10 ppm, and moisture content in the ionic liquid is less than 50 ppm. The ionic liquid prepared by the method of the present disclosure is suitable for electrochemical systems which have high requirements for moisture content, such as lithium ion secondary batteries and electrochemical supercapacitors.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: September 10, 2019
    Assignee: MICROVAST POWER SYSTEMS CO., LTD.
    Inventors: Zhuoqun Zheng, Dawei Shen, Zhenyu Fei
  • Patent number: 10160850
    Abstract: A quaternary ammonium salt detergent made from the reaction product of the reaction of: (a) polyalkene-substituted amine having at least one tertiary amino group; and (b) a quaternizing agent suitable for converting the tertiary amino group to a quaternary nitrogen and the use of such quaternary ammonium salt detergents in a fuel composition to reduce intake valve deposits.
    Type: Grant
    Filed: November 19, 2014
    Date of Patent: December 25, 2018
    Assignee: The Lubrizol Corporation
    Inventors: David J. Moreton, Paul R. Stevenson, Dean Thetford, Jonathan S. Vilardo
  • Patent number: 10093607
    Abstract: The present invention relates to a process for providing a compound of formula (I): wherein R is hydrogen or R?, wherein R? is —(C1-C4)alkyl, and Hal is a halogen, the process comprising the step of: reacting a compound of formula (II) wherein Hal is defined as above, with an alkali metal alkoxide of the formula XOR?, wherein X is an alkali metal, and R? is defined as above.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: October 9, 2018
    Assignee: BASF SE
    Inventors: Eric George Klauber, Michael Rack, Thomas Zierke, Nicole Holub, David Cortes, Gerald Schmelebeck, Junmin Ji
  • Patent number: 10011552
    Abstract: A process for preparing a herbicidally active carboxylic acid salt is disclosed. The process comprises the steps of: i) combining a carboxylic acid with a high-boiling, water-immiscible organic solvent to obtain a solution or slurry; ii) treating the solution or slurry produced in step (i) with a base to form a carboxylic acid salt; iii) removing solvent from the mixture produced in step (ii) to obtain a carboxylic acid salt cake; and v) drying the cake obtained in step (iii). The process is particularly suitable for preparing a salt of dicamba.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: July 3, 2018
    Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITED
    Inventor: James Timothy Bristow
  • Patent number: 9988341
    Abstract: The present invention provides novel compounds as bacterial topoisomerase inhibitors with antibacterial activity. The present invention also provides pharmaceutical compositions comprising at least one of the compounds and methods of using the compounds and pharmaceutical compositions as antibacterial agents for treating infectious diseases.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: June 5, 2018
    Assignees: THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES, TORREY PINES INSTITUTE FOR MOLECULAR STUDIES
    Inventors: Yuk-Ching Tse-Dinh, Marcello Angelo Giulianotti, Richard Allen Houghten
  • Patent number: 9147919
    Abstract: Methods of preparing sulfate salts of heteroatomic compounds using dialkyl sulfates as a primary reactant are disclosed. Also disclosed are methods of making ionic liquids from the sulfate salts of the heteroatomic compound, and electrochemical cells comprising the ionic liquids.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: September 29, 2015
    Assignee: FLUIDIC, INC.
    Inventors: Cody A. Friesen, Derek Wolfe, Paul Bryan Johnson
  • Publication number: 20150057218
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: November 3, 2014
    Publication date: February 26, 2015
    Inventors: Min ZHONG, Leping LI
  • Patent number: 8822461
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: September 2, 2014
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • Patent number: 8664218
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: March 4, 2014
    Assignee: Astex Therapeutics Ltd.
    Inventors: Brian John Williams, Martyn Frederickson
  • Publication number: 20130210820
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
    Type: Application
    Filed: January 30, 2013
    Publication date: August 15, 2013
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventor: ASTEX THERAPEUTICS LIMITED
  • Patent number: 8481535
    Abstract: The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.
    Type: Grant
    Filed: May 17, 2007
    Date of Patent: July 9, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Tawfik Gharbaoui, Dipanjan Sengupta, Ashwin M. Krishnan, Nainesh Shah, Ryan M. Hart, Mark Macias, Edward A. Lally, Jonathan Duffield
  • Publication number: 20130143876
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 3, 2012
    Publication date: June 6, 2013
    Inventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Bernd NOSSE
  • Patent number: 8222247
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4; provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Z is selected from alkyl, CF3, OH, cycloalkyl, heterocyclo, aryl, heteroaryl, —C(?O)NR8R9, —C(?O)R8, —C(NCN)NR8R9, —C(?O)OR8, —SO2R8, and —SO2NR8R9.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: July 17, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko
  • Publication number: 20120077677
    Abstract: The invention relates to the use of 4-phenylbutyric acid and/or salts thereof, of the formula (I) for enhancing stress tolerance in plants to abiotic stress, preferably drought stress, and to the associated enhancement in plant growth and/or increase in plant yield.
    Type: Application
    Filed: April 5, 2011
    Publication date: March 29, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Lothar Willms, Stefan Lehr, Marco Busch, Gunter Donn, Christopher Hugh Rosinger, Ines Heinemann, Isolde Haeuser-Hahn, Martin Jeffrey Hills
  • Publication number: 20110300074
    Abstract: This invention pertains generally to processes, uses, methods and materials utilising particular xanthylium compounds, including compounds of formula (I) and (II), as further defined herein. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease.
    Type: Application
    Filed: December 10, 2009
    Publication date: December 8, 2011
    Inventors: Scott Clunas, John Mervyn David Storey, Janet Elizabeth Rickard, David Horsley, Charles Robert Harrington, Claude Michel Wischik
  • Patent number: 7998957
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: August 16, 2011
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • Publication number: 20110183967
    Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.
    Type: Application
    Filed: September 25, 2009
    Publication date: July 28, 2011
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
  • Publication number: 20110172215
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: May 4, 2009
    Publication date: July 14, 2011
    Inventors: George Adjabeng, Jeffrey Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
  • Patent number: 7829702
    Abstract: A process for preparing optically active trans-2,6-dimethylmorpholine by (i) reacting racemic trans-2,6-dimethylmorpholine with D-mandelic acid, (ii) removing the salt formed from D-mandelic acid and one enantiomer of trans-2,6-dimethylmorpholine from the other enantiomer of trans-2,6-dimethylmorpholine and (iii) isolating the desired optically active trans-2,6-dimethylmorpholine.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: November 9, 2010
    Assignee: BASF SE
    Inventors: Klaus Ditrich, Frank Haese
  • Publication number: 20100256097
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Application
    Filed: June 16, 2008
    Publication date: October 7, 2010
    Inventors: Michael Altman, Matthew Christopher, Jonathan B. Grimm, Andrew Haidle, Kaleen Konrad, Jongwon Lim, Rachel N. MacCoss, Michelle Machacek, Ekundayo Osimboni, Ryan D. Otte, Tony Siu, Kerrie Spencer, Brandon Taoka, Paul Tempest, Kevin Wilson, Hyan Chong Woo, Jonathan Young, Anna Zabierek
  • Patent number: 7763608
    Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Grant
    Filed: May 4, 2007
    Date of Patent: July 27, 2010
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Yonghong Song, Zhaozhong J. Jia, Anjali Pandey
  • Patent number: 7750004
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds and methods of treating diseases during which are expressed the Mcl-1 protein are disclosed.
    Type: Grant
    Filed: July 7, 2006
    Date of Patent: July 6, 2010
    Assignee: Abbott Laboratories
    Inventors: Michael D. Wendt, Hong Ding, Sheela A. Thomas, Steven W. Elmore, Wang Shen, Daniel A. Dickman, David Augeri
  • Publication number: 20100130465
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Application
    Filed: October 29, 2007
    Publication date: May 27, 2010
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga A. Reddy, Lianyun Zhao, Shuyi Tang, Tzu T. Wong, Praveen K. Tadikonda, Luis E. Torres, M. Arshad Siddiqui, Michael P. Dwyer, Kartik M. Keertikar, Timothy J. Guzi
  • Patent number: 7696205
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: April 13, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventor: Robert J. Cherney
  • Publication number: 20100009961
    Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
    Type: Application
    Filed: June 26, 2009
    Publication date: January 14, 2010
    Applicant: Alantos Pharmaceuticals Holding, Inc.
    Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jurgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
  • Publication number: 20090317360
    Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: June 11, 2008
    Publication date: December 24, 2009
    Inventors: Roopa Rai, Franz Ulrich Schmitz, Christopher Don Roberts, Irina Slobodov, Martin Robert Leivers
  • Publication number: 20090215765
    Abstract: Neuroprotective compounds for treating optic neuropathies and screening methods for identifying neuroprotective compounds.
    Type: Application
    Filed: April 24, 2006
    Publication date: August 27, 2009
    Applicant: The Johns Hopkins University
    Inventors: John Barnwell Kerrison, Donald J. Zack
  • Patent number: 7531651
    Abstract: Compounds of formula (I): wherein A? represents the benzenesulphonate (besylate) anion;. R represents H or C1-6 alkyl; and n is a number from 0.8 to 2.2 are CCR3 antagonists and are therefore indicated to be useful in therapy are described.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: May 12, 2009
    Assignee: Glaxo Group Limited
    Inventors: John Spencer Cook, Robert Philip Landon, Andrew John Walker, Mark Wilkinson
  • Patent number: 7482344
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart disease, hypertension, rheumatoid arthritis or inflammation, comprising administering to a patient in thereof an effective amount of a compound of Formula (I).
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: January 27, 2009
    Assignee: Eli Lilly and Company
    Inventors: Michael Joseph Coghlan, Prabhakar Kondaji Jadhav, James Joseph Droste, Jonathan Edward Green, Donald Paul Matthews
  • Patent number: 7462714
    Abstract: Process for the industrial synthesis of the compound of formula (I): Application to the synthesis of bivalent salts of ranelic acid and more especially strontium ranelate and its hydrates.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: December 9, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Lucile Vaysse-Ludot, Jean-Pierre Lecouve, Pascal Langlois
  • Patent number: 7358248
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Grant
    Filed: April 30, 2004
    Date of Patent: April 15, 2008
    Assignee: The Institute for Pharmaceutical Discovery LLC
    Inventors: Darren Whitehouse, Shaojing Hu, Michael C. Van Zandt, Garrett Parker, Thomas G. Meskill
  • Patent number: 7291615
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: November 6, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventor: Robert J. Cherney
  • Publication number: 20070255057
    Abstract: A method of nitrating a compound selected from the group consisting of is provided.
    Type: Application
    Filed: February 27, 2007
    Publication date: November 1, 2007
    Inventors: Miall Cedilote, Thomas Patrick Cleary, Pingsheng Zhang
  • Patent number: 7265110
    Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: September 4, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Duncan Edward Shaw, Brian John Williams
  • Patent number: 7241759
    Abstract: Certain amidophenyl-sulfanylamino-benzo[1,2,5]thiadiazole compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
    Type: Grant
    Filed: March 26, 2004
    Date of Patent: July 10, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Brett Allison, Laura C. McAtee, Victor K. Phuong, Michael H. Rabinowitz, Nigel P. Shankley
  • Patent number: 7176330
    Abstract: A novel fluorescent group-containing carbodiimide compound having at least one group selected from a carboxyl group, a sulfo group, a phosphono group and a phospho group which have substitution of an alkali metal, an alkaline earth metal or a basic group containing a nitrogen or phosphorus atom, which is prepared by using a novel fluorescent group-containing carbodiimide compound precursor having a halogen atom or a sulfonic acid group; and a method for detecting a nucleic acid by hybridization utilizing a nucleic acid labeled with a labeling substance, which utilizes the fluorescent group-containing carbodiimide compound as the labeling substance.
    Type: Grant
    Filed: September 2, 2003
    Date of Patent: February 13, 2007
    Assignee: Nisshingo Industries, Inc.
    Inventors: Naoki Kimura, Namiko Shiohata, Yoko Yoshikawa
  • Patent number: 7045521
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: May 16, 2006
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Robert Cherney
  • Patent number: 6908918
    Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.
    Type: Grant
    Filed: April 14, 2003
    Date of Patent: June 21, 2005
    Assignee: Regents of the University of California
    Inventors: Trevor C. McMorris, Michael J. Kelner
  • Patent number: 6780858
    Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.
    Type: Grant
    Filed: January 12, 2001
    Date of Patent: August 24, 2004
    Assignee: Tularik Inc.
    Inventors: Leping Li, Xiaoqi Chen, Pingchen Fan, Jeffrey Thomas Mihalic, Serena Cutler
  • Patent number: 6768024
    Abstract: The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R1 to R8 and n have the meanings provided herein. The invention further provides methods of using the ligands to alter or regulate the activity of a melanocortin receptor.
    Type: Grant
    Filed: August 4, 2000
    Date of Patent: July 27, 2004
    Assignee: Lion Bioscience AG
    Inventors: Karen J. Watson-Straughan, Timothy C. Gahman, Ming Qi, Christa Hamashin, James E. Macdonald, Michael J. Green, Kevin R. Holme, Michael C. Griffith
  • Patent number: 6734177
    Abstract: The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said salts.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: May 11, 2004
    Assignee: Novartis AG
    Inventors: Frederick R. Kinder, Jr., Prasad K. Kapa, Eric M. Loeser
  • Patent number: 6706712
    Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: March 16, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Robert Cherney
  • Patent number: 6656946
    Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases and their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6653305
    Abstract: A compound of formula (I) wherein: Ra is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R1 and R2, wherein: R1 is a hydrogen, fluorine, chlorine, or bromine atom, or a methyl, trifluoromethyl, cyano, or ethynyl group, and R2 is a hydrogen or fluorine atom; Rb is an R3O—CO—CH2—N—CH2—CH2—OH group optionally substituted at the methylene groups by 1 or 2 methyl or ethyl groups, wherein R3 is a hydrogen atom or a C1-4-alkyl group, a 2-oxomorpholin-4-yl group optionally substituted by 1 or 2 methyl or ethyl groups, or a N-[(1,3-dioxolan-2-yl)methyl]methylamino group; Rc is a hydrogen atom, or a methoxy, ethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranylmethoxy, or tetrahydropyranylmethoxy group; and n is 1, 2, or 3
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: November 25, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6635761
    Abstract: This invention relates to the use as catalyst for the cyclotrimerization reaction of isocyanates of a hydrogencarbonate of a cation which either as it is or in the form complexed with a complexing agent has an average molecular or ionic radius of more than 1 Å, preferably greater than 1.5 Å, and which is at least partially soluble in the reaction medium. The invention also relates to a method of preparing (poly)isocyanurate polyisocyanates by catalytic cyclotrimerization of isocyanates, in which a catalytic system is used which comprises a cyclotrimerization catalyst based on a quaternary ammonium salt as catalyst and imidazole as cocatalyst.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: October 21, 2003
    Assignee: Rhodia Chimie
    Inventors: Denis Revelant, Jean-Marie Bernard
  • Patent number: 6599901
    Abstract: The present invention relates to compounds of the formula wherein R is as defined herewithin. The compounds of formula I have a good affinity to the A2A receptor and therefore they may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, aniticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure.
    Type: Grant
    Filed: November 5, 2002
    Date of Patent: July 29, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
  • Patent number: 6593345
    Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.
    Type: Grant
    Filed: August 27, 1997
    Date of Patent: July 15, 2003
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
  • Patent number: 6531472
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory activity which is useful in cancer treatment. Also provided is a process for making a compound of formula I by reacting a compound of formula III with a compound of formula IV wherein A is a displaceable group and PG is a protecting group.
    Type: Grant
    Filed: December 4, 2001
    Date of Patent: March 11, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Guy Georges, Adelbert Grossmann, Tim Sattelkau, Wolfgang Schaefer, Ulrich Tibes
  • Publication number: 20030022893
    Abstract: The subject invention concerns methods and compounds that have utility in the treatment of a condition associated with matrix metalloproteinase, ADAM or ADAM-TS enzymes, a condition that is mediated by TNF &agr; or a condition involving a membrane-shedding event that is mediated by a metalloproteinase.
    Type: Application
    Filed: August 29, 2002
    Publication date: January 30, 2003
    Inventors: Andrew Douglas Baxter, David Alan Owen, Duncan Batty, Robert John Watson