Chalcogen Bonded Directly At 2-position Of The Oxazole Ring Patents (Class 548/229)
  • Publication number: 20080119476
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Application
    Filed: July 1, 2005
    Publication date: May 22, 2008
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Publication number: 20080119533
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Application
    Filed: November 30, 2007
    Publication date: May 22, 2008
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Edward Turos, Rajesh Kumar Mishra
  • Patent number: 7342039
    Abstract: The present invention relates to substituted indole oximes and methods of using them.
    Type: Grant
    Filed: September 23, 2004
    Date of Patent: March 11, 2008
    Assignee: Wyeth
    Inventors: Lisa Marie Havran, John Anthony Butera, Hassan Mahmoud Elokdah, Douglas John Jenkins, Eric Gould Gundersen
  • Patent number: 7342035
    Abstract: In particular, zolmitriptan or a pharmaceutically acceptable salt thereof, which includes a) Preparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with ?-keto-?-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Transesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Saponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Decarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: March 11, 2008
    Assignee: Inke, S.A.
    Inventors: Montserrat Armengol Asparo, Pere Dalmases Barjoan
  • Patent number: 7332611
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Grant
    Filed: May 8, 2006
    Date of Patent: February 19, 2008
    Assignee: University of South Florida
    Inventors: Edward Turos, Rajesh Kumar Mishra
  • Publication number: 20080027053
    Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.
    Type: Application
    Filed: July 9, 2007
    Publication date: January 31, 2008
    Inventors: Mark J. Macielag, Manomi A. Tennakoon
  • Publication number: 20080021079
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by inhibiting the activity of KSP are disclosed.
    Type: Application
    Filed: May 5, 2004
    Publication date: January 24, 2008
    Inventors: Han-Jie Zhou, Gustave Bergnes
  • Patent number: 7309791
    Abstract: The invention relates to new compounds, being 3-phenylpropionic acid derivatives of formula I wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; Z represents NH, N—C1–C10-alkyl, N-aryl, N-heteroaryl, S, or O; X represents O, S, NH, N—C1–C10-alkyl, N-aryl, NSO2—C1–C10-alkyl, N—SO2-aryl, or N—SO2-heteroaryl; R1, to R6 each independently represent hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof. The compounds are the ligands of PPAR-gamma receptor and are useful as medicaments.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: December 18, 2007
    Assignee: Adamed Sp. z.o.o
    Inventors: Zbigniew Majka, Katarzyna Ewa Rusin, Dominik Daniel Kludkiewicz, Krzysztof Kurowski, Katarzyna Joanna Matusiewicz, Tomasz Stawinski, Daniel Sulikowski, Piotr Kowalczyk
  • 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: 7294719
    Abstract: A process for producing N-carboxyanhydrides is disclosed. The process produces N-carboxyanhydrides as a product and HCl as a by-product. The HCl by-product is purged from the reaction mixture by passing a purge gas through the reaction mixture as a carbonylation reagent is reacting with an amino acid or a salt thereof. The N-carboxyanhydrides produced by this process have a relatively lower chloride impurity content, relatively higher yields can be achieved, and the N-carboxyanhydrides can be produced on a larger scale.
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: November 13, 2007
    Assignee: Sigma-Aldrich Co.
    Inventors: John Michael Carubia, Thomas Mark Weaver, Ettigounder Ponnusamy
  • Patent number: 7285565
    Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Grant
    Filed: January 14, 2005
    Date of Patent: October 23, 2007
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Patent number: 7279494
    Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of formula I or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Grant
    Filed: April 1, 2004
    Date of Patent: October 9, 2007
    Assignee: Pfizer Inc.
    Inventors: Adam Renslo, Mikhail Fedor Gordeev, Dinesh Vinoobhai Patel, Hongwu Gao, Vara Prasad Venkata Nagendra Josyula
  • Patent number: 7279582
    Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: October 25, 2002
    Date of Patent: October 9, 2007
    Assignee: Abbott Laboratories
    Inventors: Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
  • Patent number: 7273867
    Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: September 25, 2007
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Bertram Cezanne, Johannes Gleitz, Christopher Barnes
  • Patent number: 7265140
    Abstract: The present invention relates to acyloxymethylcarbamate oxazolidinones. The compounds of the present invention have potent activity with excellent oral bioavailability against Gram-positive and Gram-negative bacteria.
    Type: Grant
    Filed: September 9, 2004
    Date of Patent: September 4, 2007
    Assignee: Pfizer Inc
    Inventors: Vara Prasad Venkata Nagendra Josyula, Robert C. Gadwood, Lisa Marie Thomasco, Ji-Young Kim, Allison Laura Choy, Frederick Earl Boyer
  • Patent number: 7262299
    Abstract: A process for performing a catalytic Diels-Alder reaction by reacting a diene with a dienophile in the presence of a heterogeneous catalyst comprising a zeolitic material exchanged or impregnated with ions of a Lewis acidic metal is described. The catalyst, for example, copper-exchanged zeolite Y, may be treated with chiral bis(imine) compounds to direct the chirality of the reaction products. The catalyst can be separated from the reaction mixture and re-used in further Diels Alder reactions.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: August 28, 2007
    Assignee: Johnson Matthey PLC
    Inventors: Neil Aubrey Caplan, Frederick Ernest Hancock
  • Patent number: 7259263
    Abstract: The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.
    Type: Grant
    Filed: June 29, 2005
    Date of Patent: August 21, 2007
    Assignee: Jansen Pharmaceutica N.V.
    Inventors: Dennis J. Hlasta, Craig A. Zificsak
  • Patent number: 7238814
    Abstract: The invention describes compositions and kits comprising 4-aza-4-(2-methyl-2-sulfanylpropyl) tricyclo(5.2.1.0<2,6>)dec-8-ene-3,5-dione; 4-aza-4-(2-methyl-2-(nitrosothio)propyl) tricyclo(5.2.1.0<2,6>)dec-8-ene-3,5-dione; 4-{1-methyl-1-((2,4,6-trimethoxyphenyl)methylthio)ethyl}-1,3-oxazolidin-2-one; 2-aAmino-3-methyl-3-((2,4,6-trimethoxyphenyl)methylthio)butan-1-ol; 4-(1-methyl-1-(nitrosothio)ethyl)-1,3-oxazolidin-2-one; or pharmaceutically acceptable salts thereof. The compositions of the invention can further comprise at least one penetration enhancer, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: July 3, 2007
    Assignee: NitroMed, Inc.
    Inventors: Przemyslaw A. Marek, Andzrej M. Trocha, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson
  • Patent number: 7223870
    Abstract: Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: May 29, 2007
    Assignee: Pfizer Inc.
    Inventors: Arun Ghosh, Stephane Caron, Janice E. Sieser
  • Patent number: 7211668
    Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R?; R1, R? is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nuc
    Type: Grant
    Filed: April 6, 2004
    Date of Patent: May 1, 2007
    Assignee: Panagene, Inc.
    Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Sung Hee Lee
  • Patent number: 7199143
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein —N-HET is, for example, (Ic) or (If) wherein R1 is, for example, halogen or a (1–4C)alkyl group which is substituted by one substituent selected from, for example, hydroxy, (1–4C)alkoxy, amino, cyano or azido; Q is selected from, for example, Q1 wherein R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, wherein m is 0, 1 or 2; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: February 25, 2003
    Date of Patent: April 3, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hales, Folkert Reck, Fei Zhou, Paul Robert Fleming, Daniel Robert Carcanague
  • Patent number: 7192954
    Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: March 20, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Ian M. Bell, Cory R. Theberge, Theresa M. Williams, C. Blair Zartman, Xu-Fang Zhang, Steven N. Gallicchio
  • Patent number: 7186844
    Abstract: A method for producing a cyclic carbamate ester produces the cyclic carbamate ester by reacting an organic compound having at least two halogen atoms per molecule, an amine having at least two hydrogen atoms on a nitrogen atom, and carbon dioxide.
    Type: Grant
    Filed: January 3, 2005
    Date of Patent: March 6, 2007
    Assignee: Mitsubishi Gas Chemical Co., Inc.
    Inventor: Kazuto Ikemoto
  • Patent number: 7186738
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such as (TAa1) and (TAa5): R4h, R5h, R6h are for example selected from hydrogen, (1–4C)alkyl, (1–4C)alkoxy-carbonyl, (1–4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: March 6, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
  • Patent number: 7166607
    Abstract: The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: January 23, 2007
    Assignee: AstraZeneca AB
    Inventors: Roger Bonnert, Stephen Brough, Tony Cook, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
  • Patent number: 7160912
    Abstract: The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.
    Type: Grant
    Filed: July 3, 2003
    Date of Patent: January 9, 2007
    Assignees: Dr.Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.
    Inventors: Natesan Selvakumar, Jagattaran Das, Sanjay Trehan, Javed Iqbal, Magadi Sitaram Kumar, Ramanujam Rajagopalan, Mamidi Naga Venkata Srinivasa Rao
  • Patent number: 7157482
    Abstract: Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example phenyl or pyridyl, substituted with T; T is for example selected from (TAa1 to TAa12) such as (TAa1 and TAa5); formula (II): R4h, R5h, R6h are for example selected from hydrogen, (1-4C)alkyl, (1-4C)alkoxycarbonyl, (1-4C)alkanoyl and carbamoyl; processes for making them, compositions containing them and their use as antibacterial agents are described.
    Type: Grant
    Filed: March 16, 2004
    Date of Patent: January 2, 2007
    Assignee: AstraZeneca AB
    Inventors: Michael Barry Gravestock, Neil James Hale, Sheila Irene Hauck
  • Patent number: 7125863
    Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.
    Type: Grant
    Filed: April 26, 2001
    Date of Patent: October 24, 2006
    Assignee: Ferring BV
    Inventors: David Michael Evans, Gary Robert William Pitt
  • Patent number: 7115777
    Abstract: The present inventions relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, the use and manufacture of a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).
    Type: Grant
    Filed: May 28, 2003
    Date of Patent: October 3, 2006
    Assignee: Novartis AG
    Inventors: Thomas Allmendinger, Peter Furter
  • Patent number: 7091196
    Abstract: The invention provides a family of compounds useful as anti-infective agents and/or anti-proliferative agents, for example, chemotherapeutic agents, anti-fungal agents, anti-bacterial agents, anti-parasitic agents, anti-viral agents, and/or anti-inflammatory agents, and/or prokinetic (gastrointestinal modulatory) agents, having the formula: or pharmaceutically acceptable salts, esters, or prodrugs thereof.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: August 15, 2006
    Assignee: Rib-X Pharmaceuticals, Inc.
    Inventors: Deping Wang, Joyce A. Sutcliffe, Adegboyega K. Oyelere, Timothy S. McConnell, Joseph A. Ippolito, John N. Abelson, Dane M. Springer, Joseph M. Salvino, Rongliang Lou, Joel A. Goldberg, Jay J. Farmer, Erin M. Duffy, Ashoke Bhattacharjee
  • Patent number: 7087629
    Abstract: Compounds of formula (I) or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q3 and Q5; R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
    Type: Grant
    Filed: March 6, 2003
    Date of Patent: August 8, 2006
    Assignee: AstraZeneca AB
    Inventor: Michael Barry Gravestock
  • Patent number: 7074785
    Abstract: Novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, A, R4 and m have the meanings given in the description, a number of processes for preparing these substances, and their use for controlling pests, and also novel intermediates and their preparation.
    Type: Grant
    Filed: September 4, 2002
    Date of Patent: July 11, 2006
    Assignee: Bayer Cropscience AG
    Inventors: Thomas Seitz, Martin Füsslein, Johannes Rudolf Jansen, Udo Kraatz, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Christoph Erdelen, deceased
  • Patent number: 7049443
    Abstract: The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compounds and the bioavailability of these oxazolidinone compounds is improved by improving the solubility thereof.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: May 23, 2006
    Assignee: Pharmacia & Upjohn Company
    Inventor: Jackson B. Hester, Jr.
  • Patent number: 7034017
    Abstract: This invention relates to compounds of formula (I) wherein R1 represents optionally substituted phenyl, R2 represents optionally substituted and the remaining “R” groups are as defined in the specification and claims, as well as a method for making such materials, pharmaceutical compositions containing such materials, and methods of using such materials in medical treatment.
    Type: Grant
    Filed: January 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
  • Patent number: 7030148
    Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I) where R1, R2, R3, Y1, Y2, Y3, and Z are as defined in the description; their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutical acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: April 18, 2006
    Assignee: Dr. Reddy's Research Foundation
    Inventors: Selvakumar Natesan, Jagattaran Das, Javed Iqbal, Sitaram Kumar Magadi, Srinivasa Rao Naga Venkata Mamidi, Rajagopalan Ramanujam, Baskaran Sundarababu, Braj Bhushan Lohray
  • Patent number: 7002020
    Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: February 21, 2006
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
  • Patent number: 6992103
    Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
    Type: Grant
    Filed: November 29, 2002
    Date of Patent: January 31, 2006
    Assignee: SmithKline Beecham P.L.C.
    Inventors: Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Steven James Stanway, Leontine Saskia Trouw
  • Patent number: 6979741
    Abstract: Acetyl Coenzyme A Carboxylase inhibitors, pharmaceutical compositions containing such compounds and the use of such compounds to treat for example, Metabolic Syndrome including atherosclerosis, diabetes and obesity.
    Type: Grant
    Filed: February 20, 2003
    Date of Patent: December 27, 2005
    Assignee: Pfizer Inc.
    Inventors: David A. Perry, H. James Harwood
  • Patent number: 6967196
    Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: November 22, 2005
    Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.
    Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
  • Patent number: 6949537
    Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: September 27, 2005
    Assignee: Semafore Pharmaceuticals, Inc.
    Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
  • Patent number: 6943179
    Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: September 13, 2005
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
  • Patent number: 6939867
    Abstract: Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with ?-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: September 6, 2005
    Assignee: Pfizer Inc.
    Inventors: Robert L. Dow, Ernest S. Paight
  • Patent number: 6909005
    Abstract: The present invention provides an improved (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone product which is prepared by a method which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VII) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: June 21, 2005
    Assignee: AstraZeneca UK Limited
    Inventor: Rajnikant Patel
  • Patent number: 6897230
    Abstract: Oxazolidinones having a bicyclic[3.1.0]hexane containing moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof, and wherein the variables R1, R2, R3, R4, R4a, A, Ar, HAr, n, r, and s are as defined herein.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: May 24, 2005
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasumichi Fukuda, Milton L. Hammond
  • Patent number: 6887995
    Abstract: The present invention relates to a one-step process to prepare pharmacologically active 2-oxo-5-oxazolidinylmethylacetamides.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: May 3, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: William R. Perrault, Bruce Allen Pearlman, Delara B. Godrej
  • Patent number: 6884813
    Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein A is a structure i, ii, iii, or iv X is CR7; Y is —S(?O)n—, —S(?NR8)—, or —S(?NR8)(?O)—; Z is —NHC(?O)R1, —NHC(?S)R1, —NR-het1, —O-het1, —S-het1, or -het2; and n is independently 0, 1, or 2. The compounds of formula I are useful as antimicrobials against a number of human and veterinary pathogens.
    Type: Grant
    Filed: January 21, 2003
    Date of Patent: April 26, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Adam Renslo, Gary W. Luehr, Stuart Lam, Neil E. Westlund, Dinesh V. Patel
  • Patent number: 6875784
    Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: April 5, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail Fedor Gordeev, Adam Renslo, Dinesh Vinoobhai Patel
  • Patent number: 6869965
    Abstract: Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo-quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.
    Type: Grant
    Filed: December 5, 2003
    Date of Patent: March 22, 2005
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Dinesh V. Patel, Michael R. Barbachyn, James R. Gage
  • Patent number: 6852716
    Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: February 8, 2005
    Assignee: Pfizer Inc
    Inventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
  • Patent number: 6833453
    Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.
    Type: Grant
    Filed: October 17, 2001
    Date of Patent: December 21, 2004
    Assignee: Pharmacia & Upjohn Company
    Inventors: William R. Perrault, Robert C. Gadwood