Halogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/313)
  • Patent number: 9040550
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: May 26, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8853397
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: October 7, 2014
    Assignee: Rigel Pharmacuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Publication number: 20140288017
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 8822685
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 8816074
    Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: August 26, 2014
    Assignee: University of Georgia Foundation, Inc.
    Inventors: Chung K. Chu, Jianing Wang
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Patent number: 8691984
    Abstract: The present invention provides a method of storing TAIC in which TAIC is prevented from suffering from freezing and solidification during storage thereof in the winter season. In the method of the present invention, the triallyl isocyanurate is mixed with a silane coupling agent to prepare a composition comprising both thereof, and the resulting composition is stored. In the preferred embodiment of the present invention, the silane coupling agent is used in an amount of 5 to 30% by weight based on the weight of the triallyl isocyanurate, and ?-methacryloxypropyl trimethoxysilane is used as the silane coupling agent.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 8, 2014
    Assignee: Nippon Kasei Chemical Company Limited
    Inventor: Mabuko Yamaura
  • Patent number: 8604193
    Abstract: Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: December 10, 2013
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Stacey Heumann, Christopher M. Levins, Steven Pfeiffer, Donald Tang
  • Publication number: 20130109707
    Abstract: This invention relates to novel fluorouracil derivatives of Formula I or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a thymidylate synthase inhibitor.
    Type: Application
    Filed: February 28, 2011
    Publication date: May 2, 2013
    Applicant: Concert Pharmaceuticals ,Inc.
    Inventors: Rose A. Persichetti, Julie F. Liu
  • Patent number: 8410266
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: April 2, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
  • Patent number: 8362027
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Grant
    Filed: August 8, 2011
    Date of Patent: January 29, 2013
    Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Publication number: 20130018026
    Abstract: The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 17, 2013
    Inventor: Keith R. Latham
  • Publication number: 20130012490
    Abstract: A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
  • Patent number: 8318756
    Abstract: Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: November 27, 2012
    Assignee: Adherex Technologies, Inc.
    Inventors: Thomas Spector, William Paul Peters, Donald W. Kufe, Brian Huber
  • Publication number: 20120220613
    Abstract: To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. The marker for determining sensitivity to an anti-cancer agent is formed of a protein selected from the group consisting of a protein or a fragment thereof which is detected as a peak at m/z of 16,450 to 16,620, a protein or a fragment thereof which is detected as a peak at m/z of 22,080 to 22,310, and a protein or a fragment thereof which is detected as a peak at m/z of 17,100 to 17,270, the peaks being determined by means of a mass spectrometer.
    Type: Application
    Filed: October 29, 2010
    Publication date: August 30, 2012
    Applicants: Kabushiki Kaisha Yakult Honsha, Keio University
    Inventors: Yusuke Tanigawara, Sayo Suzuki, Hidehiro Irie, Akito Nishimuta, Tetsuya Suzuki, Shinji Sugimoto
  • Patent number: 8148525
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: April 3, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sasha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Publication number: 20120052040
    Abstract: Compositions comprising anti-fibrotic agent(s) and/or polymeric compositions can be used in various medical applications including the prevention of surgical adhesions, treatment of inflammatory arthritis, treatment of scars and keloids, the treatment of vascular disease, and the prevention of cartilage loss.
    Type: Application
    Filed: March 22, 2011
    Publication date: March 1, 2012
    Applicant: Angiotech International AG
    Inventors: William L. Hunter, Philip M. Toleikis, David M. Gravelt, Arpita Maiti, Richard T. Liggins, Aniko Takacs-Cox, Rui Avelar, Troy A.E. Loss, Dechi Guan, Kaiyue Wang
  • Publication number: 20120022257
    Abstract: Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.
    Type: Application
    Filed: January 26, 2010
    Publication date: January 26, 2012
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Stacey Heumann, Christopher M. Levins, Steven Pfeiffer, Donald Tang
  • Publication number: 20110294754
    Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.
    Type: Application
    Filed: June 1, 2010
    Publication date: December 1, 2011
    Inventors: Ilan ZIV, Hagit Grimberg
  • Patent number: 8034824
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: October 11, 2011
    Assignees: Kowa Co., Ltd., Tokyo University of Science Educational Foundation Administrative Organization
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Publication number: 20100292260
    Abstract: The invention relates to 6-vinyl pyrimidine pyrimidinone derivatives and the use thereof as medicaments in particular for the treatment of HTV infections, the use thereof for preparing pharmaceutical compositions and methods for the preparation thereof.
    Type: Application
    Filed: October 13, 2006
    Publication date: November 18, 2010
    Applicant: UNIVERSITA DEGLI STUDI DE SIENA
    Inventors: Maurizio Botta, Federico Corelli, Elena Petricci, Marco Radi, Giovanni Maga, Jose A. Este, Antonello Mai
  • Publication number: 20100278896
    Abstract: A solid, implantable dosage form comprising a therapeutically active agent in solid form, optionally with one or more pharmaceutically acceptable excipients, wherein the one or more excipients, when present, do not lead to a significant delay or prolongation of the release of active agent, as compared to an equivalent dosage form containing no excipients when tested in vitro.
    Type: Application
    Filed: November 17, 2008
    Publication date: November 4, 2010
    Applicant: UCL BUSINESS PLC
    Inventors: Peng T. Khaw, Stephen Brocchini
  • Publication number: 20100239521
    Abstract: The various embodiments herein provide a method for producing a carrier system for the encapsulation or entrapment of a bioactive agent. According to one embodiment herein, producing a carrier complex of a bioactive ingredient disposed within a carrier material, the method comprising the steps of: (a) providing a complexation zone supplied with an aqueous medium containing the carrier material; (b) simultaneously stirring and heating the aqueous medium; (c) adding the bioactive ingredient to the aqueous medium and maintaining the complexation zone under conditions of temperature effective to facilitate complexation of the bioactive ingredient by the carrier material; and (d) recovering from the complexation zone a carrier complex of the bioactive ingredient.
    Type: Application
    Filed: June 1, 2010
    Publication date: September 23, 2010
    Inventor: MOHAMMAD REZA MOZAFARI
  • Publication number: 20100179127
    Abstract: The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments and to medicaments comprising them.
    Type: Application
    Filed: June 23, 2006
    Publication date: July 15, 2010
    Inventors: Philipp Floersheim, Wolfgang Froestl, Sebastien Guery, Kiemens Kaupmann, Manuel Koller
  • Patent number: 7704971
    Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.
    Type: Grant
    Filed: September 1, 2006
    Date of Patent: April 27, 2010
    Assignee: SmithKlineBeecham Corporation
    Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
  • Publication number: 20090281063
    Abstract: The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing them efficiently to arrive into the mammary gland. The present invention provides an iontophoretic preparation for treating breast cancer and/or mastitis which contains a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent as an active ingredient and has a donor to be applied on a nipple part for topical administration of the active ingredient from the nipple part to the mammary gland by application of electric potential.
    Type: Application
    Filed: October 11, 2006
    Publication date: November 12, 2009
    Applicants: KOWA CO., LTD., TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION ADMINISTRATIVE ORGANIZATION
    Inventors: Toshio Inagi, Makoto Kanebako, Hiroshi Terada, Kimiko Makino, Masakazu Toi
  • Patent number: 7517889
    Abstract: The present invention is directed to a compound of Formula (I) wherein Cy1, Cy2, L1, L2, and R1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischem
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: April 14, 2009
    Assignee: Aventis Pharmaceuticals, Inc.
    Inventors: Keith John Harris, Bin Cao
  • Patent number: 7495006
    Abstract: Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
    Type: Grant
    Filed: December 8, 2005
    Date of Patent: February 24, 2009
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Shuli Mao, Michael Hager
  • Patent number: 7488823
    Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.
    Type: Grant
    Filed: November 10, 2003
    Date of Patent: February 10, 2009
    Assignee: Array Biopharma, Inc.
    Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
  • Publication number: 20080318907
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Application
    Filed: March 12, 2007
    Publication date: December 25, 2008
    Applicant: The Trustees of California State University
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20080262005
    Abstract: Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6, R7, n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: May 13, 2005
    Publication date: October 23, 2008
    Applicant: NEUROCRINE BIOSCIENCES, INC.
    Inventors: Yun-Fei Zhu, Zhiqiang Gou, Mi Chen, Liren Zhao
  • Publication number: 20080161310
    Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
    Type: Application
    Filed: March 5, 2008
    Publication date: July 3, 2008
    Applicant: Sanofi-Aventis
    Inventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
  • Patent number: 7285533
    Abstract: A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2 ligand chimeras, nucleic acid encoding Apo-2 ligand, and antibodies to Apo-2 ligand are also provided. Methods of using Apo-2 ligand to induce apoptosis and to treat pathological conditions such as cancer, are further provided.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: October 23, 2007
    Assignee: Genentech, Inc.
    Inventor: Avi J. Ashkenazi
  • Patent number: 7119096
    Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.
    Type: Grant
    Filed: October 1, 2001
    Date of Patent: October 10, 2006
    Assignee: SmithKlineBeecham Corporation
    Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
  • Patent number: 7115544
    Abstract: A plant growth regulator for cotton harvest, which contains as an active ingredient, a compound of formula (I): wherein X is CH or nitrogen; Z is halogen; A is oxygen, sulfur, or NH; R1 is hydroxyl, C1–C7 alkoxy, C3–C7 alkenyloxy, C3–C7 alkynyloxy, C5–C7 cycloalkoxy, {(C1–C7 alkoxy)carbonyl}C1–C3 alkoxy, (C1–C7 alkylamino)oxy, {di(C1–C7 alkyl)amino}oxy, (C3–C7 alkylideneamino)oxy, C1–C7 alkylamino, di(C1–C7 alkyl)amino, C3–C7 alkenylamino, C3–C7 alkynylamino, C5–C7 cycloalkylamino, {(C1–C7 alkoxy)carbonyl}C1–C3 alkylamino, or (C1–C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1–C3 alkyl, or C1–C3 alkoxy.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: October 3, 2006
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 7109334
    Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: September 19, 2006
    Assignee: Shire BioChem, Inc.
    Inventor: Qing Yu
  • Patent number: 7034156
    Abstract: The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the formula (II) in which R1 is hydrogen, cyano, nitro or halogen, R2 is cyano, nitro, halogen or optionally substituted alkyl or alkoxy, R3 is hydrogen, hydroxyl, mercapto, amino, hydroxyamino, hydrazino, halogen, or one of the radicals —R6, -Q-R6, —NH—R6, —NH—O—R6, —NH—SO2—R6, —N(SO2—R6)2, —CQ1-R6, —CQ1-Q2-R6, —CQ1-NH—R6, -Q2-CQ1-R6, —NH—CQ1-R6, —N(SO2—R6)(CQ1-R6), -Q2-CQ1-Q2-R6, —NH—CQ1-Q2-R6 or -Q2-CQ1-NH—R6, where Q is O, S, SO or SO2, Q1 and Q2 are each independently oxygen or sulphur and R6 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R4 is hydrogen, halogen or optionally substituted alkyl, and R5 is fluorine- and/or chlorine-substituted alkyl, as intermediates for the 1-amino-3-phenyluracil derivatives, and to a process f
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: April 25, 2006
    Assignee: Bayer CropScience AG
    Inventors: Jörn Stölting, Dorothee Hoischen, Roland Andree, Karl-Heinz Linker, Holger Weintritt, Heinz-Jürgen Wroblowsky
  • Patent number: 7009050
    Abstract: The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. The compounds are of the formula: wherein B is uracil-1-yl or cytosin-1-yl having a 5-substituent selected from halogen, alkyl, alkenyl, and alkynyl, with the proviso that where B is uracil-1-yl, the 5-substituent is not methyl. The compounds are useful in the treatment of Herpes simplex virus (HSV).
    Type: Grant
    Filed: January 15, 2003
    Date of Patent: March 7, 2006
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Victor E. Marquez, Pamela L. Russ
  • Patent number: 6794506
    Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Grant
    Filed: July 19, 2001
    Date of Patent: September 21, 2004
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu, Frank Stappenbeck
  • Patent number: 6794384
    Abstract: The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: September 21, 2004
    Assignee: De Montfort University
    Inventors: Gerard Andrew Potter, Lawrence Hylton Patterson, Michael Danny Burke
  • Patent number: 6780821
    Abstract: The invention relates to new substituted phenyluracils of the general formula (I) in which n, Q, R1, R2, R3, R4, R5 and X have the meanings given in the description, to process and new intermediates for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: August 24, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Dieter Feucht, Rolf Pontzen, Ingo Wetcholowsky, Hans-Georg Schwarz
  • Patent number: 6746668
    Abstract: A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2 ligand chimeras, nucleic acid encoding Apo-2 ligand, and antibodies to Apo-2 ligand are also provided. Methods of using Apo-2 ligand to induce apoptosis and to treat pathological conditions such as cancer, are further provided.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: June 8, 2004
    Assignee: Genentech, Inc.
    Inventor: Avi J. Ashkenazi
  • Patent number: 6734139
    Abstract: The present invention provides herbicidal active compound combinations which comprise, N-aryl-uracils and herbicidally active compounds and/or compounds which improve crop plant compatibility. The combinations find use in controlling monocotyledonous and dicotyledonous weeds in crops of useful plants.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: May 11, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Feucht, Peter Dahmen, Mark Wilhelm Drewes, Birgit Krauskopf, Mathias Kremer, Rolf Pontzen, Ingo Wetcholowsky, Roland Andree
  • Patent number: 6713486
    Abstract: 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C6-10 aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-4 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O—(C1-6 alkyl)-substituted oximino, C—1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethlyl, C1-6 alkoxymethyl, C1-6 acyloxynethyl, carbamoyloxymethyl, anminomethyl, N—(C1-3 alkyl)aminomethyl, N,N-di(C1-3 alkyl)aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl)amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl)carbamoyl, aminocarbamoyl, dimethylamin
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: March 30, 2004
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jong-Chan Son, Seun-Shil Shin, Shin-Keol Kim, Chong-Kyo Lee, Hae-Soo Kim
  • Publication number: 20040030134
    Abstract: A novel process is provided for the preparation of chiral intermediates useful in the asymmetric syntheses of &agr;v&bgr;3 integrin receptor antagonists. Also provided are the enantiomerically enriched intermediates that are obtained from the process.
    Type: Application
    Filed: September 11, 2003
    Publication date: February 12, 2004
    Inventors: James Christopher McWilliams, Elizabeth Buck, Kan K. Eng, Guy R. Humphrey, Peter E. Maligres, Jess W. Sager, Marjorie See Waters
  • Patent number: 6686155
    Abstract: The present invention relates to prognostic methods which are useful in medicine, particularly cancer chemotherapy. The object of the invention to provide a method for assessing GST-pi expression levels in fixed or fixed and paraffin embedded tissues and prognosticate the probable resistance or sensitivity of a patient's tumor to treatment with platinum-based therapies by examination of the amount of GST-pi mRNA in a patient's tumor cells and comparing it to a predetermined threshold expression level. More specifically, the invention provides to oligonucleotide primer pair GST-pi and methods comprising their use for detecting levels of GST-pi mRNA.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: February 3, 2004
    Assignee: Response Genetics, Inc.
    Inventor: Kathleen D. Danenberg
  • Patent number: 6677345
    Abstract: A range is disclosed of pyrimidine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDK's) and which thereby can provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to differ from that of known CDK inhibitors such as olomoucine and roscovitine.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: January 13, 2004
    Assignee: Cancer Research Campaign Technology Limited
    Inventors: Roger J Griffin, Alan H Calvert, Nicola J Curtin, David R Newell, Bernard T Golding, Jane A Endicott, Martin E M Noble, Francis T Boyle, Philip J Jewsbury
  • Patent number: 6649760
    Abstract: Phenyluracils of the general formula (I) in which Q, R1, R2, R3, R4, R5 and R6 each have one of the meanings given in the description, and processes for their preparation and their use as herbicides.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: November 18, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Hans-Georg Schwarz, Karl-Heinz Linker, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Publication number: 20030207865
    Abstract: This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
    Type: Application
    Filed: October 23, 2001
    Publication date: November 6, 2003
    Inventors: Brian R. Dixon, Cedo M. Bagi, Catherine R. Brennan, David R. Brittelli, William H. Bullock, Jinshan Chen, William L. Collibee, Robert Dally, Jeffrey S. Johnson, Harold C. E. Kluender, William F. Lathrop, Peiying Liu, Carol Ann Mase, Aniko M. Redman, William J. Scott, Klaus Urbahns, Donald J. Wolanin
  • Patent number: 6624120
    Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which m, n, Q, R1, R2, R3, R4, R5, X and Y are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.
    Type: Grant
    Filed: December 13, 2001
    Date of Patent: September 23, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Hans-Georg Schwarz, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen