Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring (e.g., Adrenochrome, Etc.) Patents (Class 548/512)
  • Patent number: 9708261
    Abstract: The present invention relates to crystalline forms of (1R,5S)-1-(naphthalen-2-yl)-3-azabicyclo[3.1.0]hexane hydrochloride and compositions comprising the same and methods of making and using the same.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: July 18, 2017
    Assignee: NEUROVANCE, INC.
    Inventors: Anthony Alexander McKinney, Franklin Bymaster, Walter Piskorski, Fred J. Fleitz, Yonglai Yang, David A. Engers, Valeriya Smolenskaya, Venkat Kusukuntla
  • Patent number: 8980338
    Abstract: A composition including as an active ingredient an extract of a plant of the family Mesembryanthemaceae with mesembrenol and mesembrenone as the two major alkaloids present. The invention also relates to the use of the composition as a PDE4 inhibitor and as a serotonin-uptake inhibitor, preferably applied in formulations for the use of the composition as a dual serotonin-uptake inhibitor and PDE4 inhibitor. The invention extends to compositions, such as pharmaceutical compositions or compositions used as dietary supplements, the total alkaloid content of which includes at least 80% (w/w) combined content of mesembrenol and mesembrenone, less than 5% (w/w) mesembrine, and at least 7% (w/w) mesembranol.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: March 17, 2015
    Assignee: H.L. Hall & Sons Limited
    Inventors: Nigel Gericke, Alan Harvey, Alvaro Viljoen, Deon Hofmeyr
  • Publication number: 20140256782
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Gregory J. Larosa, Jeremy R. Greenwood, Leah L. Frye, Tan Quach, Jamie B. Cote, Judd Berman
  • Patent number: 8742134
    Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: June 3, 2014
    Assignee: Theron Pharmaceuticals, Inc.
    Inventors: Jurg R. Pfister, Gwenaella Rescourio, Meenakshi S. Venkatraman, Xiaoming Zhang
  • Patent number: 8742121
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: June 3, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Guoping Wang
  • Patent number: 8703809
    Abstract: The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: April 22, 2014
    Assignee: Novartis AG
    Inventors: Baltazar Gomez-Mancilla, Fabrizio Gasparini
  • Publication number: 20140094616
    Abstract: Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.
    Type: Application
    Filed: May 17, 2012
    Publication date: April 3, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tetsuya Ikemoto, Leopold Mpaka Lutete, Toshiaki Aikawa
  • Patent number: 8563763
    Abstract: The present invention relates to isonitrile compounds, methods of synthesis, and uses in a variety of fields. In one aspect, the present invention includes sulfinyl methyl isonitriles and methods for their preparation. In another aspect, the present invention includes the use of sulfinyl methyl isonitriles to prepare various other isonitrile compounds and derivatives thereof. In yet another aspect, the present invention includes a relatively simple and routine synthesis of sulfinyl methyl isonitrile compounds, other isonitrile compounds and derivatives thereof.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: October 22, 2013
    Assignee: Duquesne University of the Holy Ghost
    Inventors: Fraser Ferguson Fleming, Bhaskar Reddy Pitta
  • Publication number: 20130237514
    Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 12, 2013
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
  • Publication number: 20130197011
    Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
  • Publication number: 20130157989
    Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 20, 2013
    Applicant: Theron Pharmaceuticals, Inc.
    Inventor: Theron Pharmaceuticals, Inc.
  • Publication number: 20130116293
    Abstract: Described herein are high-throughput methods of monitoring D-serine levels in plasma. The assay involves the use of strong cation solid phase extraction (SPE) to isolate D-serine from plasma, followed by quantitation of D-serine using the D-amino acid oxidase-(DAAO-) catalyzed reaction. Also described are methods of screening for compounds that act as DAAO inhibitors.
    Type: Application
    Filed: November 8, 2012
    Publication date: May 9, 2013
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventor: THE JOHNS HOPKINS UNIVERSITY
  • Publication number: 20120295934
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
    Type: Application
    Filed: May 4, 2012
    Publication date: November 22, 2012
    Inventors: Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch
  • Patent number: 8242285
    Abstract: N-tert-butoxycarbonyl-2-pyrrolidinones represented by the following formula (1). In the formula (1), R1, R2, R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom, a cyano group, a linear, branched or cyclic alkyl group having 1 to 10 carbon atoms, which may have a substituent, a linear, branched or cyclic alkenyl group having 2 to 10 carbon atoms, which may have a substituent, or the like, R1 and R2 may be linked to form a >C?O group along with the carbon atom to which both are attached, R3 and R4 may be linked to form a >C?O group along with the carbon atom to which both are attached, R5 and R6 may be linked to form a >C?O group along with the carbon atom to which both are attached, or any two among R1, R2, R3, R4, R5 and R6 may be linked to form a polymethylene group having 1 to 4 carbon atoms which may have a substituent.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Norihiko Hirata, Toshitsugi Uemura
  • Publication number: 20120130087
    Abstract: The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M?, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
    Type: Application
    Filed: November 11, 2011
    Publication date: May 24, 2012
    Applicant: CODEXIS, INC.
    Inventors: Benjamin Mijts, Sheela Muley, Jack Liang, Lisa M. Newman, Xiyun Zhang, James Lalonde, Michael D. Clay, Jun Zhu, John M. Gruber, Jeffrey Colbeck, John D. Munger, JR., Jagadeesh Mavinahalli, Roger Sheldon
  • Patent number: 8163793
    Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: April 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Patent number: 8158807
    Abstract: The present invention provides for a process for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate, an intermediate useful in the efficient preparation of (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof, processes for preparing (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof from the sulfonate intermediate and processes for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: April 17, 2012
    Assignee: Schering Corporation
    Inventors: Thierry Berranger, Patrice Demonchaux
  • Publication number: 20120083495
    Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.
    Type: Application
    Filed: December 5, 2011
    Publication date: April 5, 2012
    Applicants: SCIENCE APPLICATIONS INTERNATIONAL INC. (SAIC), ALBANY MOLECULAR RESEARCH, INC., DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
  • Publication number: 20120064034
    Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: November 10, 2011
    Publication date: March 15, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: ROBERT EDWARD BABINE, SHU HUI CHEN, IVAN COLLADO, CRISTINA GARCIA-PAREDES, JOHN IRVIN GLASS, DEQI GUO, LING JIN, JASON ERIC LAMAR, RAYMOND SAMUEL PARKER, III, NANCY JUNE SNYDER, XICHENG DAVID SUN, YVONNE YEE MAI YIP, Q. MAY WANG, FRANTZ VICTOR, MARK JOSEPH TEBBE, ROBERT B. PERNI, LUC FARMER
  • Publication number: 20120041045
    Abstract: The use of mesembrenone and medicaments and dietary supplements containing mesembrenone. The applicant has surprisingly found that mesembrenone exhibits potent PDE-4 inhibition properties and, in addition to being useful in treating conditions that respond to treatment with a PDE-4 inhibitor, has dual activity on account of its serotonin-uptake inhibition properties. Mesembrenone is extracted and isolated, for example as a pure compound, from plant material of the plant family Mesembryan-themaceae. Preferably a plant or plants from the genus Sceletium, more preferably, Sceletium tortuosum(L) N.E.Br is used.
    Type: Application
    Filed: March 16, 2010
    Publication date: February 16, 2012
    Applicant: H.L. HALL & SONS LIMITED
    Inventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen
  • Publication number: 20110319287
    Abstract: The present invention relates inter alia to methods for identifying modulators of tumour necrosis factor (TNF) signalling. In one aspect, the method involves identifying an agent that modulates a signalling pathway mediated by TNF, comprising the steps of providing a host cell comprising TNF receptor 1 (TNFR1)-associated death domain (TRADD) linked to a reporter molecule, and determining at least one cellular characteristic detectable by the reporter molecule in the host cell in the presence of TNF and in the presence and absence of a candidate modulator. The invention is suitable for high-throughput screening (HTS) and high-content screening (HCS), or a combination of HTS and HCS.
    Type: Application
    Filed: January 19, 2010
    Publication date: December 29, 2011
    Applicant: ADDEX PHARMA S.A.
    Inventors: Aurelie Florence Chedal-bornu goiller, Vincent Mutel, Robert Johannes Luetjens
  • Patent number: 8039484
    Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: October 18, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
  • Publication number: 20110082172
    Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.
    Type: Application
    Filed: September 21, 2010
    Publication date: April 7, 2011
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
  • Publication number: 20100267722
    Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 16, 2010
    Publication date: October 21, 2010
    Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Publication number: 20100152416
    Abstract: Disclosed herein is a method for producing a purified 2-aryl-3,3-bis(4-hydroxyaryl) phthalimidine of formula (I) wherein R1 is hydrogen or a C1-25 hydrocarbyl group and R2 is a hydrogen, a C1-25 hydrocarbyl group, or a halogen, and wherein the method comprises dissolving a crude phthalimidine compound in an aqueous base solution; precipitating the dissolved, crude phthalimidine compound from the aqueous base solution by adding an acid in an amount effective to lower the pH of the solution to 9.0 to 12.0, to provide a semicrude phthalimidine compound; and isolating the semicrude phthalimidine compound from the aqueous base solution, to provide the purified 2-aryl-3,3-bis(4-hydroxyaryl)phthalimidine of formula (I), and having a phenolphthalein compound content of less than 2,500 ppm, based on the weight of the purified 2-aryl-3,3-bis(4-hydroxyaryl)phthalimidine.
    Type: Application
    Filed: December 12, 2008
    Publication date: June 17, 2010
    Inventors: Venkata Rama Narayanan Ganapathy BHOTLA, Balakrishnan GANESAN, Kishan Gurram, Salkod Parameshwar MALLIKA, Kumar Arun Satyanarayana, Swaminathan SHUBASHREE
  • Publication number: 20100145069
    Abstract: The present invention provides for a process for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate, an intermediateuseful in the efficient preparation of (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof, processes for preparing (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof from the sulfonate intermediate and processes for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate.
    Type: Application
    Filed: December 18, 2007
    Publication date: June 10, 2010
    Applicant: Schering Corporation
    Inventors: Thierry Berranger, Patrice Demonchaux
  • Patent number: 7732480
    Abstract: There are disclosed bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X and n are defined herein.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 8, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: James J. Li, Lawrence Hamann, Haixia Wang
  • Publication number: 20100130498
    Abstract: The present invention relates to agonists of the human bitter-taste receptors hTAS2R14, hTAS2R10 and hTAS2R4 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R14, hTAS2R10 and hTAS2R4 bitter taste transduction or bitter taste response.
    Type: Application
    Filed: March 31, 2008
    Publication date: May 27, 2010
    Applicant: Deutshes Institut Fur Ernahrungsforschung Potsdam- Rehbrucke
    Inventors: Maik Behrens, Anne Brockhoff, Christina Kuhn, Wolfgang Meyerhof, Giovanni Appendino
  • Publication number: 20100105725
    Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
    Type: Application
    Filed: October 26, 2007
    Publication date: April 29, 2010
    Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
  • Patent number: 7696241
    Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X and n are defined herein.
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: April 13, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: James J. Li, Lawrence Hamann, Haixia Wang
  • Patent number: 7645790
    Abstract: The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: January 12, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
  • Publication number: 20090312323
    Abstract: Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.
    Type: Application
    Filed: March 16, 2007
    Publication date: December 17, 2009
    Applicants: The Government of the United States of America, as represented by the Secretary, Department of HHS, Albany Molecular Research, Inc., Science Applications International Corporation
    Inventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
  • Patent number: 7612213
    Abstract: A compound represented by the general formula (I): (I) wherein R represents linear, branched, or cyclic alkyl or aryl; a process for producing the compound; and an antitumor agent containing the compound as an active ingredient.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: November 3, 2009
    Assignee: Riken
    Inventors: Hiroyuki Osada, Hideaki Kakeya, Yujiro Hayashi
  • Patent number: 7598250
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.
    Type: Grant
    Filed: August 4, 2004
    Date of Patent: October 6, 2009
    Assignee: Schering Corporation
    Inventors: Jared N. Cumming, Ying Huang, Guoqing Li, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Jianping Pan, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie
  • Publication number: 20090182029
    Abstract: Provided herein are isolated compounds of formula 1: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.
    Type: Application
    Filed: January 14, 2009
    Publication date: July 16, 2009
    Applicant: Chipscreen Biosciences, Ltd.
    Inventors: Xian-Ping Lu, Zhi-bin Li, Zhi-Qiang Ning
  • Patent number: 7544815
    Abstract: The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Grant
    Filed: July 11, 2006
    Date of Patent: June 9, 2009
    Assignee: Merck & Co, Inc.
    Inventors: Jeffrey T. Kuethe, Jingjun Yin, Mark A. Huffman, Michel Journet
  • Patent number: 7514468
    Abstract: The present invention relates to indolinone derivatives substituted in the 6 position of general formula wherein R1 to R6 and X are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: April 7, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Armin Heckel, Frank Hilberg, Thorsten Lehmann-Lintz, Guenter Linz, Joerg Kley, Jacobus C. A. Van Meel, Werner Rall, Gerald Juergen Roth, Peter Sieger, Ulrike Tontsch-Grunt
  • Publication number: 20090042854
    Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Application
    Filed: January 19, 2007
    Publication date: February 12, 2009
    Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
  • Publication number: 20090012120
    Abstract: An ylide-based aza-Payne rearrangement of 2,3-aziridin-1-ols leads to an efficient process for the preparation of pyrrolidines. The aza-Payne rearrangement under the basic reaction conditions favors the formation of epoxy amines. Subsequent nucleophilic attack of the epoxide by the ylide yields a bis-anion, which upon a 5-exo-tet ring closure yields the desired pyrrolidine, thus completing the relay of the 3-membered the 5-membered nitrogen containing ring system. This process takes place with complete transfer of stereochemical fidelity, and can be applied to sterically hindered aziridinols.
    Type: Application
    Filed: May 9, 2007
    Publication date: January 8, 2009
    Applicant: Board of Trustees of Michigan State University
    Inventors: Babak Borhan, Jennifer M. Schomaker, Somnath Bhattacharjee, Keith Korthals
  • Publication number: 20080249110
    Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.
    Type: Application
    Filed: May 25, 2004
    Publication date: October 9, 2008
    Inventors: Roger Bonnert, Rukhsana Mohammed
  • Publication number: 20080221192
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC kinases.
    Type: Application
    Filed: November 7, 2005
    Publication date: September 11, 2008
    Applicant: IRM LLC
    Inventors: Yongqin Wan, Yuan Mi, Yi Fan, Dai Cheng, Yi Liu, Nathanael S. Gray, Pamela Albaugh
  • Patent number: 7388027
    Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R2? R5, G, n and W are defined herein.
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: June 17, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: James J. Li, Lawrence Hamann, David Augeri, Yingzhi Bi
  • Patent number: 7375237
    Abstract: Pyrrolizine compounds having the formula (I), or pharmaceutically-acceptable salts thereof, are effective in treating inflammatory or immune diseases, where A is a four- to seven-membered saturated ring, K is O or S, and R1, R2, R3 n, and M are defined in the specification.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: May 20, 2008
    Assignees: Bristol-Myers Squibb Company, Cerep SA
    Inventors: T. G. Murali Dhar, Dharmpal S. Dodd, Dominique Potin, Michele Launay
  • Patent number: 7345083
    Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: March 18, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
  • Patent number: 7217731
    Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: May 15, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
  • Patent number: 7094800
    Abstract: The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional derivatives and process for their preparation. The compounds are suitable for the treatment of disorders of metabolism, such as type 2 diabetes.
    Type: Grant
    Filed: July 26, 2004
    Date of Patent: August 22, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Holger Wagner, Gerhard Jaehne, Holger Gaul, Christian Buning, Georg Tschank, Ulrich Werner
  • Patent number: 7078534
    Abstract: The present invention relates to a cost effective and commercially viable process for the preparation of crystalline N-formimidoyl thienamycin monohydrate (Imipenem monohydrate) of Formula I.
    Type: Grant
    Filed: November 5, 2001
    Date of Patent: July 18, 2006
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Yatendra Kumar, Neera Tewari, Ran Chander Aryan, Bishwa Prakash Rai, Seema Ahuja
  • Patent number: RE39128
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: June 13, 2006
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt
  • Patent number: RE43038
    Abstract: A compound represented by the general formula (I): (I) wherein R represents linear, branched, or cyclic alkyl or aryl; a process for producing the compound; and an antitumor agent containing the compound as an active ingredient.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: December 20, 2011
    Assignee: Riken
    Inventors: Hiroyuki Osada, Hideaki Kakeya, Yujiro Hayashi
  • Patent number: RE43390
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt