Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 548/165)
  • Patent number: 8952005
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark E. Layton, Michael J. Kelly, III
  • Patent number: 8933107
    Abstract: The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I).
    Type: Grant
    Filed: September 12, 2006
    Date of Patent: January 13, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Ralf Dunkel, Ronald Ebbert, Eva-Maria Franken, Olga Malsam
  • Patent number: 8933108
    Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
    Type: Grant
    Filed: September 5, 2012
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Jun Cao, Bernhard Erb, Robin Alec Fairhurst, Arnaud Grandeury, Shinji Hatakeyama, Magdalena Koziczak-Holbro, Xinzhong Lai, Philipp Lustenberger, Bernd Riebesehl, Nicola Tufilli, Thomas Ullrich, Xiang Wu, Jianguang Zhou
  • Patent number: 8877751
    Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: November 4, 2014
    Assignee: Merck Patent GmbH
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Patent number: 8809381
    Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: August 19, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
  • Publication number: 20140228321
    Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 14, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
  • Patent number: 8742133
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: August 13, 2008
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk-Przewloka, Hao Li
  • Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • Publication number: 20130316999
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: August 7, 2013
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
  • Patent number: 8513291
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: August 20, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
  • Publication number: 20130035332
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: April 25, 2011
    Publication date: February 7, 2013
    Inventors: Mark E. Layton, Michael J. Kelly
  • Patent number: 8207350
    Abstract: The present invention relates to compounds of formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: June 26, 2012
    Assignee: Abbott Laboratories
    Inventors: Robert F. Keyes, Yu Gui Gu, Hing L. Sham
  • Patent number: 8076489
    Abstract: Compounds of formula (I) in free or salt or solvate form, wherein T has the meaning as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: November 28, 2005
    Date of Patent: December 13, 2011
    Assignee: Novartis AG
    Inventor: Robin A Fairhurst
  • Patent number: 8058294
    Abstract: A pharmaceutically acceptable salt of N-[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propanamide provided it is not the dihydrobromide or dihydrochloride salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: November 15, 2011
    Assignee: AstraZeneca AB
    Inventors: Robert Whittock, Jane Withnall
  • Patent number: 8008331
    Abstract: The invention relates to benzothiazol-2-one derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: August 30, 2011
    Assignee: Sanofi-Aventis
    Inventors: Gerhard Zoller, Stefan Petry, Gunter Müller, Hubert Heuer, Norbert Tennagels
  • Patent number: 7982036
    Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: July 19, 2011
    Assignee: Avila Therapeutics, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
  • Patent number: 7951955
    Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
    Type: Grant
    Filed: May 1, 2008
    Date of Patent: May 31, 2011
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Publication number: 20100210688
    Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: April 27, 2010
    Publication date: August 19, 2010
    Inventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
  • Publication number: 20100184991
    Abstract: The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula wherein R1, R2 and R3, independently of one another, represent hydrogen, halogen or an organic radical, in racemic form or as an enantiomer, a tautomer, an analog thereof or a salt thereof.
    Type: Application
    Filed: March 29, 2010
    Publication date: July 22, 2010
    Inventors: Gottfried Sedelmeier, Valentina Aureggi
  • Patent number: 7723366
    Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to the use of compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, the invention relates to the use of compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the following formulae: (I) and (II) Wherein Y, C, R1, R2, R6, and R7 are defined herein.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: May 25, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Thomas Arrhenius, Jie Fei Cheng, Mark E. Wilson, Rossy Serafimov, Masahiro Nishimoto, David Mark Wallace, Sovouthy Tith, Steve Joel Brown, Charles Stanford Harmon, Gary D. Lopaschuk, Jason R. Dyck
  • Patent number: 7700782
    Abstract: The present invention provides compounds of formula (I) wherein Ra, Rb, R1, R2, R3, R4, R5, R6 and R29 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: April 20, 2010
    Assignee: AstraZeneca AB
    Inventors: Stephen Connolly, Alexander Humphries, Premji Meghani
  • Patent number: 7678810
    Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.
    Type: Grant
    Filed: March 4, 2005
    Date of Patent: March 16, 2010
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Masakazu Sato, Yuko Matsunaga, Hajime Asanuma, Hideaki Amada, Takeshi Koami, Tetsuo Takayama, Tetsuya Yabuuchi, Fumiyasu Shiozawa, Hironori Katakai, Hiroki Umemiya, Akiko Ikeda
  • Patent number: 7642275
    Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: January 5, 2010
    Assignee: Takeda San Diego, Inc.
    Inventors: Jerome C. Bressi, Jason W. Brown, Robert J. Skene, Jeffrey A. Stafford, Phong H. Vu, Anthony R. Gangloff, Andrew J. Jennings, Stephen W. Kaldor
  • Patent number: 7625889
    Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: December 1, 2009
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
  • Publication number: 20090239916
    Abstract: The present invention provides a pharmaceutical composition comprising as an active ingredient a compound that specifically binds to MFP-2 or a functional fragment thereof and a screening method for the compound; the compound and a pharmaceutical composition comprising the same are highly useful as anti-inflammatory agents and anti-allergic agents.
    Type: Application
    Filed: May 26, 2005
    Publication date: September 24, 2009
    Applicant: Reverse Proteomics Research Institute Co., Ltd
    Inventors: Akito Tanaka, Akira Yamazaki, Akinobu Nakanishi, Mikio Takeuchi, Masayuki Haramura
  • Publication number: 20090198054
    Abstract: The present disclosure is directed to a process for the preparation of a compound having the formula: wherein R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a selected leaving group that is not halogen, and may specifically be methylsulfonate, trifluoromethylsulfonate, and p-toluenesulfonate. These compounds are valuable intermediates useful in the synthesis of compounds having pesticidal activity.
    Type: Application
    Filed: April 16, 2009
    Publication date: August 6, 2009
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony Cornelius O'Sullivan
  • Publication number: 20090111794
    Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.
    Type: Application
    Filed: October 30, 2008
    Publication date: April 30, 2009
    Inventors: Genesis M. Bacani, Scott D. Bembenek, Wendy Eccles, James P. Edwards, Matthew T. Epperson, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Kelly J. McClure, Taraneh Mirzadegan, Alejandro Santillan, JR.
  • Publication number: 20090091234
    Abstract: A salt molten at room temperature that does not contain any organic solvent, excelling in stability; and a display device that is improved in the durability in high-temperature environment by virtue of the use thereof. There is provided a salt molten at room temperature characterized by being composed of a silver salt and any of compounds of the following general formula (I) or general formula (II).
    Type: Application
    Filed: April 6, 2006
    Publication date: April 9, 2009
    Applicant: KONICA MINOLTA HOLDINGS, INC.
    Inventor: Noriyuki Kokeguchi
  • Patent number: 7495020
    Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: January 18, 2006
    Date of Patent: February 24, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, A. Brian Jones, Joel P. Berger, James F. Dropinski, Alexander Elbrecht, Kun Liu, Karen Lamb MacNaul, Guo-Qiang Shi, Derek J. Von Langen, Gaochao Zhou
  • Publication number: 20080319031
    Abstract: The present invention relates to novel tyrosine derivatives of formula (I), their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly provides novel tyrosine derivatives of the general formula (I).
    Type: Application
    Filed: March 10, 2006
    Publication date: December 25, 2008
    Inventors: Surendrakumar Satyanarayan Pandey, Shiv Kumar Agarwal, Gajendra Singh, Santhanagopalan Chithra, Sangmesh Badiger, Bishwajit Nag, Debendranath Dey, Abhijeet Nag, Partha Neogi
  • Patent number: 7402598
    Abstract: The present invention relates to compounds of formula (I) as defined herein and salts or solvates thereof. Processes for preparing these compounds and pharmaceutical formulations containing them are also disclosed, as well as methods for the prophylaxis of treatment of a clinical condition using such compounds.
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: July 22, 2008
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Diane Mary Coe, Duncan Stuart Holmes, Brian Edgar Looker
  • Patent number: 7323564
    Abstract: The present invention is directed to a process for preparing a compound having the formula: wherein R is a range of organic groups and X is a leaving group. The process may include reacting a compound of the formula with a water-removing reagent. Also, when X is a halogen, the process may include reacting a compound of the formula with a halogenating agent or a sulfonylating agent. Alternatively, when X is a halogen, the process may be carried out by reacting a compound of the formula IV where R2 and R3 are defined organic groups with a compound of the formula halogen-C(—O)—O—C1 -C8alkyl, halogen-C(—O)—O-aryl or halogen-C(—O)—O-benzyl.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: January 29, 2008
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Henry Szczepanski, Peter Maienfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony O'Sullivan
  • Publication number: 20070281978
    Abstract: This invention relates an inhibitory modulator of AQP4 protein regarding its transmembrane water transport properties, wherein the modulator selectively binds to the AQP4 protein, and inhibits AQP4 mediated water transport.
    Type: Application
    Filed: June 1, 2007
    Publication date: December 6, 2007
    Applicant: NIIGATA UNIVERSITY
    Inventors: Tsutomu Nakada, Vincent J. Huber
  • Patent number: 7235668
    Abstract: The present invention relates to a novel process for the preparation of compounds of the formula (I) by reacting in a first step amino alcohols of the formula (II) with oleum to give sulphuric acid esters of the general formula (III) and by reacting these sulphuric acid esters in a second step with mercaptans or salts thereof of the general formula (IV) RSM ??(IV) wherein in each formula, where applicable, R1, R2, R3, R4, R5, R6, R, n and M have the meanings given in the disclosure, in the presence of a diluent and in the presence of a base.
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: June 26, 2007
    Assignee: Bayer CropScience AG
    Inventor: Jörn Stölting
  • Patent number: 6992228
    Abstract: This disclosure relates to a method for producing and using catalysts in the production of bisphenols, and in particular to a method for producing catalysts which contain poly-sulfur mercaptan promoters, and using these catalysts in the production of bisphenol-A and its derivatives.
    Type: Grant
    Filed: July 25, 2003
    Date of Patent: January 31, 2006
    Assignee: General Electric Company
    Inventors: Jimmy Lynn Webb, James Lawrence Spivack
  • Patent number: 6943170
    Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for making the same.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: September 13, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventor: David J. Carini
  • Patent number: 6900218
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: May 31, 2005
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
  • Publication number: 20040176409
    Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR&ggr;. In particular, the compounds of the invention modulate the function of PPAR&ggr;. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.
    Type: Application
    Filed: November 20, 2003
    Publication date: September 9, 2004
    Applicants: Tularik Inc, Japan Tobacco, Inc.
    Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein, Atsushi Hagiwara, Noboru Furukawa, Hisashi Shinkai
  • Publication number: 20040142878
    Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): 1
    Type: Application
    Filed: October 30, 2003
    Publication date: July 22, 2004
    Inventor: David J. Carini
  • Patent number: 6710045
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which m represents integers from 3 to 10, n represents 0, 1 or 2 and Het represents the following, in each case optionally substituted, groupings: to processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: March 23, 2004
    Assignee: Bayer CropScience AG
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrum, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder
  • Publication number: 20040029937
    Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents.
    Type: Application
    Filed: July 1, 2003
    Publication date: February 12, 2004
    Applicant: NEUROSEARCH A/S.
    Inventors: Lene Teuber, Palle Christophersen, Dorte Strobaek, Bo Skaaning Jensen
  • Patent number: 6683101
    Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: January 27, 2004
    Assignee: Warner-Lambert Company
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030236252
    Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.
    Type: Application
    Filed: November 12, 2002
    Publication date: December 25, 2003
    Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030232810
    Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.
    Type: Application
    Filed: December 3, 2002
    Publication date: December 18, 2003
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030225127
    Abstract: The present invention provides certain heterocyclic sulfonamide derivatives of formula (I): useful for potentiating glutamate receptor function in a patient and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Application
    Filed: April 1, 2003
    Publication date: December 4, 2003
    Inventors: David Michael Bender, Scott Louis Forman, Winton Dennis Jones, Daryl Lynn Smith, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Publication number: 20030220339
    Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.
    Type: Application
    Filed: January 29, 2003
    Publication date: November 27, 2003
    Applicant: Tularik Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • Publication number: 20030220369
    Abstract: The present invention provides certain heterocyclic sulfonamide derivatives of formula I: useful for potentiating glutamate receptor function in a patient and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Application
    Filed: January 13, 2003
    Publication date: November 27, 2003
    Inventors: Scott Louis Forman, Winton Dennis Jones, Daryl Lynn Smith, Hamideh Zarrinmayeh, Dennis MIchael Zimmerman
  • Publication number: 20030208065
    Abstract: A process for the purification of cefixime via a novel tert.octylamine salt of a cefixime intermediate which may be crystalline and which may be produced in a one pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.
    Type: Application
    Filed: September 30, 2002
    Publication date: November 6, 2003
    Inventors: Martin Decristoforo, Johannes Ludescher, Hubert Sturm, Werner Veit
  • Publication number: 20030191166
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Application
    Filed: February 26, 2002
    Publication date: October 9, 2003
    Applicant: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, Joseph J. McDonald
  • Publication number: 20030187259
    Abstract: The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) 1
    Type: Application
    Filed: May 12, 2003
    Publication date: October 2, 2003
    Inventors: Udo Kraatz, Bernd Gallenkamp, Albrecht Marhold, Peter Wolfrim, Wolfram Andersch, Christoph Erdelen, Andreas Turberg, Olaf Hansen, Achim Harder