Bicyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/253)
  • Patent number: 7488435
    Abstract: The present invention relates to novel 1,3-diimine copper complexes and the use of 1,3-diimine copper complexes for the deposition of copper on substrates or in or on porous solids in an Atomic Layer Deposition process.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: February 10, 2009
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Kyung-Ho Park
  • Patent number: 7482343
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: January 27, 2009
    Assignees: Cytokinetics, Inc., SmithKline Beecham Corporation
    Inventors: Han-Jie Zhou, David J. Morgans, Jr., Gustave Bergnes, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Nicholas D. Adams
  • Publication number: 20090023733
    Abstract: The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
    Type: Application
    Filed: March 6, 2007
    Publication date: January 22, 2009
    Inventors: Peter Cage, Mark Furber, Christopher Luckhurst, Matthew Perry, Brian Springthorpe
  • Patent number: 7470694
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: December 30, 2008
    Assignee: SmithKline Beecham, PLC
    Inventors: Colin Andrew Leach, Stephen Allan Smith, Steven James Stanway
  • Patent number: 7470693
    Abstract: The invention is directed to compounds having the following Formula I: and methods of using them for the treatment of proliferative diseases.
    Type: Grant
    Filed: April 19, 2006
    Date of Patent: December 30, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Gretchen M. Schroeder, Lyndon A. M. Cornelius
  • Patent number: 7465736
    Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: December 16, 2008
    Assignee: Laboratoires Serono S.A.
    Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
  • Patent number: 7462620
    Abstract: Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
    Type: Grant
    Filed: July 7, 2006
    Date of Patent: December 9, 2008
    Assignee: SmithKline Beecham, PLC
    Inventors: Deirdre Mary Bernadette Hickey, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith
  • Patent number: 7456185
    Abstract: Compounds having the formula (I), are useful as p38 kinase inhibitors, wherein R4 and R5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R6 and R7 are optional substituents, and Q is a non-aromatic moiety as defined in the specification.
    Type: Grant
    Filed: March 27, 2007
    Date of Patent: November 25, 2008
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl, Teresa Alejandra Trejo-Martin
  • Patent number: 7442794
    Abstract: The invention relates to the compounds of formula I, a process for their production and their use as anti-inflammatory agents.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: October 28, 2008
    Assignee: Schering AG
    Inventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
  • Publication number: 20080261968
    Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.
    Type: Application
    Filed: November 20, 2007
    Publication date: October 23, 2008
    Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgurtel, Bert Nolte, Arthur Taveras
  • Patent number: 7439246
    Abstract: In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: October 21, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhong Chen, Tram N. Huynh, Wayne Vaccaro, Xiao-Tao Chen, Kyoung S. Kim, Zhen-wei Cai
  • Publication number: 20080255164
    Abstract: This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
    Type: Application
    Filed: November 13, 2006
    Publication date: October 16, 2008
    Applicant: ASTRAZENECA AB
    Inventors: Jeffrey Albert, Donald Andisik, Phil Edwards, Mark Sylvester
  • Patent number: 7420056
    Abstract: Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related methods of treatment are also provided.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: September 2, 2008
    Assignee: Gruenenthal GmbH
    Inventors: Sven Kuehnert, Stefan Oberboersch, Corinna Sundermann, Michael Haurand, Ruth Jostock, Klaus Schiene, Thomas Tzschentke, Thomas Christoph, Dagmar Kaulartz, Saskia Zemolka
  • Publication number: 20080194558
    Abstract: This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R3 groups. The invention also includes methods of using these compounds as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
    Type: Application
    Filed: April 21, 2008
    Publication date: August 14, 2008
    Applicant: ARRAY BIOPHARM, INC.
    Inventors: Eli Wallace, George Topalov, Joseph Lyssikatos, Alexandre Buckmelter, Qian Zhao
  • Publication number: 20080188454
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: December 28, 2007
    Publication date: August 7, 2008
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Thilo J. Heckrodt, Joane Litvak
  • Patent number: 7375102
    Abstract: Compounds are provided having the formula: wherein variables A1, A2, A3, A4, R1, R2, R3, R4, Q and L are as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: May 20, 2008
    Assignee: AMGEN SF, LLC
    Inventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic, Jiwen Liu
  • Patent number: 7365199
    Abstract: A dye-forming coupler of formula (I), a silver halide photographic light-sensitive material containing the coupler, and an azomethine dye compound derived from the coupler: wherein Q is a residue that forms, together with the —N—C?N— moiety, a nitrogen-containing 6-membered ring; RA is a certain alkyl group having at least 7 carbon atoms, or -L-R1; X is an aryl group; Y is a hydrogen atom, or a group capable of being split-off upon a coupling reaction; wherein, when RA is -L-R1, L is a divalent linking group, and R1 is a substituent; and -L-R1 does not represent an alkyl, alkenyl, alkynyl, or aryl group, and -L-R1 does not represent a heterocyclic group that bonds, with a carbon atom therein, to the nitrogen atom of the nitrogen-containing 6-membered ring formed by Q and the —N—C?N— moiety.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: April 29, 2008
    Assignee: FUJIFILM Corporation
    Inventors: Shigeki Uehira, Kiyoshi Takeuchi
  • Patent number: 7365066
    Abstract: Novel pyrazolopyridine derivative compounds are disclosed and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors useful in the treatment of cancer and other disease states influenced by TGF beta.
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: April 29, 2008
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Rosanne Bonjouklian, Junkai Liao, William Thomas McMillen, Brandon Lee Parkhurst, Jason Scott Sawyer, Jonathan Michael Yingling, Jeremy Schulenburg York
  • Publication number: 20080076784
    Abstract: The application relates to novel heterocyclic compounds of the general formula (I) (I*) in which R, R1, R2, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aromatase inhibitors.
    Type: Application
    Filed: May 27, 2005
    Publication date: March 27, 2008
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Christoph Schumacher, Michael Quirmbach
  • Publication number: 20080045546
    Abstract: This invention relates to tetrahydro-naphthalene and urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene and urea derivatives of the present invention have vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).
    Type: Application
    Filed: October 2, 2004
    Publication date: February 21, 2008
    Inventors: Axel Bouchon, Nicole Diedrichs, Achim Hermann, Klemens Lustig, Heinrich Meier, Josef Pemerstorfer, Elke Reissmuller, Muneto Mogi, Takeshi Yura, Hiroshi Fujishima, Masanori Seki, Yuji Koriyama, Kayo Yasoshima, Keiko Misawa, Masaomi Tajimi, Noriyuki Yammoto, Klaus Urbahns, Fumihiko Hayashi, Yasuhiro Tsukimi, Jang Gupta
  • Publication number: 20080045550
    Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Application
    Filed: June 21, 2007
    Publication date: February 21, 2008
    Inventors: Andreas D. Christ, Rainer E. Martin
  • Patent number: 7321033
    Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: January 22, 2008
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden, David Louis Clark, Alan Xin Xiang
  • Patent number: 7312180
    Abstract: A description is given of 4-(4-trifluoromethylpyrazolyl)pyrimidines of the formula (I) and of their use as herbicides. In this general formula (I), R1, R2, R3 and R4 are various radicals and Y is an aromatic or heteroaromatic radical.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: December 25, 2007
    Assignee: Bayer CropScience GmbH
    Inventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Heinz Kehne, Martin Hills, Dieter Feucht
  • Patent number: 7307168
    Abstract: The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: December 11, 2007
    Assignee: EGIS Gyógyszergyár Rt.
    Inventors: László Pongó, József Reiter, Gyula Simig, Gábor Berecz, György Clementis, Péter Slégel, János Szulágyi, László Koncz, Györgyi Vereczkeyné Donáth, Kálmán Nagy, Gyuláné Körtvélyessy
  • Patent number: 7297700
    Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: November 20, 2007
    Assignee: Renovis, Inc.
    Inventors: Michael G. Kelly, John Kincaid
  • Patent number: 7256287
    Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-aza-benzimidazole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents. This invention further relates to small molecules which suppress cytokines and leukocytes.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: August 14, 2007
    Assignee: Avanir Pharmaceuticals
    Inventors: Jagadish C. Sircar, Richard J. Thomas, Mark L. Richards, Anjana Sinha
  • Patent number: 7253168
    Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
    Type: Grant
    Filed: April 6, 2005
    Date of Patent: August 7, 2007
    Assignee: Neurogen Corporation
    Inventors: Alan J. Hutchison, Bertrand L. Chenard, James G. Tarrant, Guiying Li, Manuka Ghosh, George P. Luke, John M. Peterson, Wallace C. Pringle, Mary-Margaret E. O'Donnell, Kyungae Lee, Linda M. Gustavson, Dario Doller
  • Patent number: 7238698
    Abstract: Compounds having the formula (I), are useful as p38 kinase inhibitors, wherein R4 and R5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R6 and R7 are optional substituents, and Q is a non-aromatic moiety as defined in the specification.
    Type: Grant
    Filed: April 15, 2004
    Date of Patent: July 3, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl, Teresa Alejandra Trejo-Martin
  • Patent number: 7232902
    Abstract: The invention relates to a process for the preparation of certain pyrimidinone compounds.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: June 19, 2007
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Keith Raymond Mulholland, Andrew R Ross, Graham Ralph Slater, Gillian Elizabeth Smith
  • Patent number: 7223767
    Abstract: Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein m, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula (I).
    Type: Grant
    Filed: August 11, 2004
    Date of Patent: May 29, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: Robin Douglas Clark, Richard Leo Cournoyer, Counde O′Yang
  • Patent number: 7223766
    Abstract: Compounds in which a pyrimidine nucleus is bridged at the 5 and 6 position and are further substituted at positions 2 and 4 with substituents comprising aromatic moieties are useful in treating subjects with rheumatoid arthritis ameliorated by inhibition of TGF? activity.
    Type: Grant
    Filed: March 26, 2004
    Date of Patent: May 29, 2007
    Assignee: Scios, Inc.
    Inventors: Sundeep Dugar, Sarvajit Chakravarty, Aurelia Conte, Jonathan Axon, Glenn McEnroe, Alison Murphy
  • Patent number: 7220750
    Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: May 22, 2007
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Thomas Metz, Flavio Solca, Birgit Jung, Anke Baum
  • Patent number: 7214800
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: May 8, 2003
    Date of Patent: May 8, 2007
    Assignees: Cytokinetics, Inc., Smithkline Beecham Corporation
    Inventors: Bainian Feng, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight, Michael Gerard Darcy
  • Patent number: 7196091
    Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra, Rb, Rc, Rd, X and n are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibiting effect on the signal transduction mediated by tyrosine kinases, their use in treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract and the preparation thereof.
    Type: Grant
    Filed: June 3, 2004
    Date of Patent: March 27, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Rainer Soyka, Birgit Jung
  • Patent number: 7192949
    Abstract: The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: March 20, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, Robert M. Garbaccio
  • Patent number: 7193080
    Abstract: A dye-forming coupler and compound of formula (I): wherein Q represents a residue that forms, together with —N—C?N—, a nitrogen-containing 6-membered ring; RA represents an aryl, heterocyclic, or —(R1)r—(R4)m group; X represents an aryl group; Y represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent: wherein, when RA represents an —(R1)r—(R4)m group, R1 represents a methylene group, a methine group, or a carbon atom; r is 1 to 30; R4 represents a substituent except for a hydrogen atom; m is 1 to 30; and the —(R1)r—(R4)m group does not represent a straight-chain alkyl group.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: March 20, 2007
    Assignee: Fuji Photo Film, Co., Ltd.
    Inventors: Kiyoshi Takeuchi, Shigeki Uehira, Mario Aoki
  • Patent number: 7176310
    Abstract: This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions containing the compounds are useful in treating inflammatory disorders in mammals.
    Type: Grant
    Filed: April 4, 2003
    Date of Patent: February 13, 2007
    Assignee: UCB SA
    Inventors: Theodore A. Baughman, Jim P. Boyce, Ihab S. Darwish, J. Jeffry Howbert, Nathan C. Ihle, Randy W. Jackson, Scott C. Jeffrey, Dean Maeda, Kraig M. Yager
  • Patent number: 7169924
    Abstract: Compound of formula (I): are disclosed in which: R1 is an aryl group, optionally substituted by 1, 2, 3 or 4 substituents which may be the same or different selected from C(1-6)alkyl, C(1-6)alkoxy, C(1-6)alkylthio, hydroxy, halogen, CN, and mono to perfluoro-C(1-4)alkyl; R2 is halogen, C(1-3)alkyl, C(1-3)alkoxy, hydroxyC(1-3)alkyl, C(1-3)alkylthio, C(1-3)alkylsulphinyl, aminoC(1-3)alkyl, mono- or di-C(1-3)alkylaminoC(1-3)alkyl, C(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkoxyC(1-3)alkylcarbonylaminoC(1-3)alkyl, C(1-3)alkylsulphonylaminoC(1-3)alkyl, C(1-3)alkylcarboxy, C(1-3)alkylcarboxyC(1-3)alkyl, and R3 is hydrogen, halogen, C(1-3)alkyl, or hydroxyC(1-3)alkcyl; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused 5-or 6-membered carbocyclic ring; or R2 and R3 together with the pyrimidone ring carbon atoms to which they are attached form a fused benzo or heteroaryl ring ring optionally substituted by 1, 2, 3 or 4 substituents which may be the same or dif
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: January 30, 2007
    Assignee: SmithKline Beecham plc
    Inventors: Richard Leonard Elliott, Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith
  • Patent number: 7166595
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: May 2, 2003
    Date of Patent: January 23, 2007
    Assignees: Cytokinetics, Inc., SmithKline Beecham Corporation
    Inventors: Han-Jie Zhou, David J. Morgans, Jr., Gustave Bergnes, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Nicholas D. Adams
  • Patent number: 7160890
    Abstract: This invention pertains to compounds which specifically inhibit the adenosine A3 receptor and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compounds.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: January 9, 2007
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Bryan McKibben, David J. Witter
  • Patent number: 7161002
    Abstract: The present invention provides novel quinazolinone compositions of matter comprising enantiomerically pure compound represented by Formula I: or a pharmaceutically acceptable salt thereof, having a detectable amount of one or more starting material and/or reagent used in the synthesis thereof.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: January 9, 2007
    Assignees: Cytokinetics, Inc., SmithKline Beecham Corporation
    Inventors: Gustave Bergnes, Edward Ha, George Yiannikourous, Panos Kalaritis, Brandon E. Yonce, Kurt Alan Welday, Jr.
  • Patent number: 7160889
    Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein ring A is phenyl or a 5-or 6-membered heterocyclic ring which may be saturated, partially saturated or unsaturated and may be aromatic or non-aromatic and which contains 1, 2 or 3 ring heteroatoms selected from O, N and S; Z is —O—, —NH— or —S—; and X1, R1, R2, R3, m and R4 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in producing an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, and in the treatment of disease states such as cancer, rheumatoid arthritis and psorlasis.
    Type: Grant
    Filed: April 3, 2001
    Date of Patent: January 9, 2007
    Assignee: AstraZeneca AB
    Inventors: Laurent Francois Andre Hennequin, Elaine Sophie Elizabeth Stokes
  • Patent number: 7153861
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use is treating atheroscelerosis.
    Type: Grant
    Filed: October 27, 2003
    Date of Patent: December 26, 2006
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Colin Andrew Leach, Stephen Allan Smith, Steven James Stanway
  • Patent number: 7138398
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2 and R3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the treatment and prophylaxis of diseases, for example cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis and atherosclerosis. The compounds of formula (I) are able to modulate the body's own production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis ofisorders associated with an impaired cGMP balance. The invention also relates to methods for producing compounds of formula (I), to their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and to pharmaceutical preparations containing the compounds of formula (I).
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: November 21, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel
  • Patent number: 7119111
    Abstract: Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: May 27, 2003
    Date of Patent: October 10, 2006
    Assignee: Amgen, Inc.
    Inventors: Qi Huang, Matthew Kaller, Thomas Nguyen, Mark H. Norman, Robert Rzasa, Hui-Ling Wang, Wenge Zhong
  • Patent number: 7105682
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: September 12, 2006
    Assignee: Amgen Inc.
    Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
  • Patent number: 7102009
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: July 17, 2002
    Date of Patent: September 5, 2006
    Assignee: Amgen Inc.
    Inventors: Vinod F. Patel, Benny Askew, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Julie Germain, Gregory J. Habgood, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Babak Riahi, Chester Chenguang Yuan, Daniel Elbaum
  • Patent number: 7098330
    Abstract: This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: August 29, 2006
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian M. C. Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert J. Davies
  • Patent number: 7087627
    Abstract: Compositions for the inhibition of the formation of new vasculature by angiogenesis are provided comprising the combination of a vasculature damaging agent and an inhibitor of the formation or action of nitric oxide in mammalian systems. There are also provided the use of said combinations in medicaments and kits of said compounds and treatment employing said materials.
    Type: Grant
    Filed: February 15, 2000
    Date of Patent: August 8, 2006
    Assignee: Angiogene Pharmaceuticals Ltd.
    Inventor: Peter David Davis
  • Patent number: RE39266
    Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinedione derivatives of the general formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: September 5, 2006
    Assignee: Dr. Reddy's Laboratories, Limited
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Ranga Madhavan Gurram, Rajagopalan Ramanujam, Ranjan Chakrabarti, Sarma K. S. Pakala