The Five-membered Hetero Ring Consists Of One Nitrogen And Four Carbons Patents (Class 514/408)
Spiro ring system (Class 514/409)
Polycyclo ring system having the five-membered hetero ring as one of the cyclos (Class 514/410)
Additional hetero ring (Class 514/422)
C=x bonded directly to the five-membered hetero ring by nonionic bonding (x is chalcogen) (Class 514/423)
Chalcogen bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/424)
Nitrogen bonded directly to the five-membered hetero ring by nonionic bonding (Class 514/426)
Two double bonds between ring members of the five-membered hetero ring (e.g., pyrrole, etc.) (Class 514/427)
Chalcogen bonded indirectly to the five-membered hetero ring by acyclic nonionic bonding (Class 514/428)
Carbocyclic ring bonded directly to the five-membered hetero ring (Class 514/429)
  • Bone grafting material, method and implant
    Patent number: 7189409
    Abstract: A bone grafting material, a method of producing the same, and an implant. The bone grafting material comprises a porous carrier of ceramic or glass ceramic or glass material and at least one pyrrolidone arranged in the carrier.
    Type: Grant
    Filed: March 9, 2004
    Date of Patent: March 13, 2007
    Assignee: Inion Ltd.
    Inventors: Eija Pirhonen, Loredana Moimas, Franz Weber
  • Pyrrolo-naphthyl acids and methods for using them
    Patent number: 7186749
    Abstract: The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: March 6, 2007
    Assignee: Wyeth
    Inventors: Thomas J. Commons, Douglas John Jenkins
  • Biphenyl-derivatives as p38-kinase inhibitors
    Patent number: 7183297
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: October 16, 2002
    Date of Patent: February 27, 2007
    Assignee: Glaxo Group Limited
    Inventors: Richard Martyn Angell, Nicola Mary Aston, Paul Bamborough, Mark James Bamford, George Stuart Cockerill, Stephen Sean Flack, Dramane Ibrahim Lainé, Ann Louise Walker
  • Dyeing compositions for keratinous fibers containing paraphenylenediamine derivatives with pyrrolidinyl group
    Patent number: 7179301
    Abstract: The invention concerns novel dyeing compositions for keratinous fibers comprising at least a paraphenylenediamine derivative with pyrrolidinyl group as oxidation base, a dyeing method and a dyeing kit using said composition.
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: February 20, 2007
    Assignee: L'Oreal S.A.
    Inventors: Laurent Vidal, Eric Terranova, Stéphane Sabelle
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 7176229
    Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: November 7, 2005
    Date of Patent: February 13, 2007
    Assignee: ICOS Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence Edward Burgess, John Joseph Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
  • Methods to mobilize progenitor/stem cells
    Patent number: 7169750
    Abstract: Methods to elevate progenitor and stem cell counts in animal subjects using compounds which bind to the chemokine receptor CXCR4 are disclosed. Preferred embodiments of such compounds are of the formula Z-linker-Z? ??(1) or pharmaceutically acceptable salt thereof wherein Z is of the formula wherein A comprises a monocyclic or bicyclic fused ring system containing at least one N and B is H or an organic moiety of 1–20 atoms, Z? is of the formula —Ar(Y)j; wherein Ar is an aromatic or heteroaromatic moiety, and each Y is independently a non-interfering substituent and j is 0–3; and “linker” represents a bond, alkylene (1–6C) or may comprise aryl, fused aryl, oxygen atoms contained in an alkylene chain, or may contain keto groups or nitrogen or sulfur atoms.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: January 30, 2007
    Assignee: Anormed, Inc.
    Inventors: Gary Bridger, Michael J. Abrams, Geoffrey W. Henson, Ronald T. MacFarland, Gary B. Calandra
  • Glucocorticoid receptor modulators
    Patent number: 7166593
    Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonist and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below.
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: January 23, 2007
    Assignee: Pfizer, Inc.
    Inventors: Robert L. Dow, Kevin K. Liu, Bradley P. Morgan, Andrew G. Swick
  • Methods for increasing schwann cell survival
    Patent number: 7160857
    Abstract: Methods for increasing Schwann cell survival are disclosed. The methods of the invention are useful for the treatment of conditions such as peripheral neuropathies, including diabetic neuropathies.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: January 9, 2007
    Inventors: Nadine A. Tatton, William G. Tatton
  • Diphenylmethyl compounds useful as muscarinic receptor antagonists
    Patent number: 7151115
    Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, R6, R7 and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: January 23, 2006
    Date of Patent: December 19, 2006
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, Sarah Dunham, Li Li
  • Pharmaceutical compositions for headache, migraine, nausea and emesis
    Patent number: 7148208
    Abstract: S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of nausea and vomiting. The compositions of the invention are also effective in preventing or alleviating emesis associated with migraines or other medical conditions such as chemotherapy or radiotherapy, as well as other symptoms of migraines including phonophobia and photophobia.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: December 12, 2006
    Assignee: Meditor Pharmaceuticals Ltd.
    Inventors: Raphael Barkan, Alexander Mirimsky
  • Amino ceramide-like compounds and therapeutic methods of use
    Patent number: 7148251
    Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: December 12, 2006
    Assignee: The Regents of the University of Michigan
    Inventor: James A. Shayman
  • Arylpyrrolidine derivatives as NK-1 /SSRI antagonists
    Patent number: 7138423
    Abstract: The present disclosure relates to chemical compounds and their use in treatment of human diseases. A particular embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salts or solvates thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
    Type: Grant
    Filed: July 18, 2005
    Date of Patent: November 21, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Huan He, Joanne J. Bronson
  • Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals
    Patent number: 7138414
    Abstract: The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the formula I where the radicals are defined as specified, and also their pharmaceutically acceptable salts and processes for their preparation. The compounds are suitable, for example, for treating type 2 diabetes.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: November 21, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Elisabeth Defossa, Dieter Kadereit, Erich Von Roedern, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt
  • Compounds and therapeutic uses thereof
    Patent number: 7138416
    Abstract: The invention discloses a novel series of compound represented by general formula (I), its derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, pharmaceutically acceptable salts, and solvates wherein X, n, k, z, R1, R2, R3, R4, R5 and R6 are as defined in the specification that are useful in (i) normalizing elevated blood glucose levels in diabetics, (ii) treating disorders related to glucose intolerance and (iii) for scavenging free radicals in mammals.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: November 21, 2006
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventor: Alangudi Sankaranarayanan
  • Sodium channel modulators
    Patent number: 7132422
    Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
    Type: Grant
    Filed: February 4, 2005
    Date of Patent: November 7, 2006
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, David C. Green, Daniel Marquess
  • Isoindolinone kinase inhibitors
    Patent number: 7129260
    Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: June 2, 2004
    Date of Patent: October 31, 2006
    Assignee: Abbott Laboratories
    Inventors: Michael L. Curtin, Steven K. Davidsen, Robin R. Frey, Howard R. Heyman, James H. Holms, Michael Michaelides, Douglas H. Steinman
  • ?- and ?-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
    Patent number: 7115618
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 30, 2004
    Date of Patent: October 3, 2006
    Assignee: G.D. Searle & Co.
    Inventors: Michael J. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
  • Colorectal neoplasia prophylaxis
    Patent number: 7115577
    Abstract: Development of colorectal neoplasia in a patient subject or predisposed to colorectal neoplasia is reduced by the steps of (a) determining a patient is subject or predisposed to colorectal neoplasia; and (b) enterically delivering into the gut of the person an effective amount of an aminoglycoside antibiotic having poor gut absorption, whereby the development of the colorectal neoplasia is reduced as compared with otherwise similar non-treated patients.
    Type: Grant
    Filed: December 27, 2004
    Date of Patent: October 3, 2006
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jonathan Graff, Matthew Wieduwilt
  • Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7109217
    Abstract: Disclosed are compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: September 19, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
  • Derivatives of succinic and glutaric acids and analogs thereof useful as inhibitors of phex
    Patent number: 7105539
    Abstract: The present invention relates to derivatives of succinic and glutaric acids and analogues thereof, having the following general formula: useful as inhibitors of PHEX. These derivatives are useful for promoting generation of bone mass and treating or preventing diseases or conditions associated with a phosphate metabolism defect. Methods for preparation and intermediates are also disclosed.
    Type: Grant
    Filed: December 3, 2003
    Date of Patent: September 12, 2006
    Assignee: Enobia Pharma
    Inventors: Denis Gravel, Elaref S. Ratemi, Mostafa Hatam, Guy Boileau, Philippe Crine, Isabelle Lemire
  • Cholinesterase inhibitors to treat disorders of attention
    Patent number: 7105540
    Abstract: The present invention provides novel methods of treating disorders of attention or improving attention in humans by administering an effective amount of a cholinesterase inhibitor.
    Type: Grant
    Filed: September 24, 2002
    Date of Patent: September 12, 2006
    Assignee: Eisai Co. Ltd.
    Inventors: Lawrence T. Friedhoff, Paul J. Tiseo, Sharon L. Rogers
  • Method of healing skin wounds in mammals and a composition therefor
    Patent number: 7094431
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Monoamine reuptake inhibitors for treatment of CNS disorders
    Patent number: 7084165
    Abstract: The present invention relates to compounds that are useful exhibit activity as serotonin, norepinephrine and dopamine reuptake inhibitors, and their pharmaceutically acceptable salts, and their use in the treatment of central nervous system and other disorders.
    Type: Grant
    Filed: September 4, 2003
    Date of Patent: August 1, 2006
    Assignee: Pfizer Inc
    Inventors: Harry Ralph Howard, Jr., Christopher Joseph Schmidt, Thomas Francis Seeger, Mark Leonard Elliot
  • Diphenylmethyl compounds useful as muscarinic receptor antagonists
    Patent number: 7071224
    Abstract: This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, R6, R7 and R8are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: July 4, 2006
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Yu-Hua Ji, Sarah Dunham, Li Li
  • Aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
    Patent number: 7064218
    Abstract: The present invention provides novel compounds possessing one or more of the following activities: antibacterial, antifungal and antitumor activity. The compounds are of Formula (I): Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
    Type: Grant
    Filed: December 24, 2002
    Date of Patent: June 20, 2006
    Assignee: Genelabs Technologies, Inc.
    Inventors: Natalia B. Dyatkina, Dong-Fang Shi, Christopher Don Roberts, Mark Douglas Velligan, Sebastian Johannes Reinhard Liehr, Janos Botyanszki, Wentao Zhang, Alexander Khorlin, Peter Harold Nelson, Joseph Martin Muchowski
  • Methods of reducing angiogenesis
    Patent number: 7045534
    Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.
    Type: Grant
    Filed: February 3, 2003
    Date of Patent: May 16, 2006
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: John Cooke, Christopher Heeschen, Michael Weis
  • Method for producing 1,3-disubstituted 2-nitroguanidines
    Patent number: 7026307
    Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which R1, R2, R4 and Het are as defined in the description, with anhydrous hydrogen halide in the presence of a nitrile.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: April 11, 2006
    Assignee: Bayer CropScience AG
    Inventors: Jörn Stölting, Kai van Laak, Wolfram Sirges, Armin Heyn, Torsten Taschner
  • Use of AP-1 activators to treat glaucoma and ocular hypertension
    Patent number: 7005446
    Abstract: Compositions comprising AP-1 activators and methods of use for treating glaucoma and ocular hypertension are disclosed.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: February 28, 2006
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Debra L. Shade, Iok-Hou Pang, Abbot F. Clark
  • Cyclic AMP-specific phosphodiesterase inhibitors
    Patent number: 6998416
    Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
    Type: Grant
    Filed: January 15, 2004
    Date of Patent: February 14, 2006
    Assignee: Icos Corporation
    Inventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlachter
  • Combinations of active ingredients, which exhibit insecticidal and acaricidal properties
    Patent number: 6994866
    Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula ?in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (23) listed in the disclosure. maintaining device useful in producing polyurethane foams.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: February 7, 2006
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Benzophenones as inhibitors of reverse transcriptase
    Patent number: 6995283
    Abstract: The present invention is directed to beazophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: February 7, 2006
    Assignee: SmithKline Beecham Corporation
    Inventor: Joseph Howing Chan
  • Use of serotonergic compound for a method of treatment of hot flushes in post-menopausal women
    Patent number: 6987124
    Abstract: The present invention relates to a method of treatment of hot flushes with a 5-HT2C receptor agonist and in particular to the use of the selective 5-HT2C receptor agonists 1-[6-chloro-5-(trifluoromethyl)-2-pyridinyl]-piperazine and (S)-(+)-3-[(2,3-dihydro-5-methoxy-1H-inden-4-yl)oxy-pyrrolidine or pharmaceutically acceptable acid addition salts thereof for the manufacture of a pharmaceutical formulation adapted for the treatment of hot flushes.
    Type: Grant
    Filed: September 27, 2002
    Date of Patent: January 17, 2006
    Assignee: Akzo Nobel N.V.
    Inventor: Hermanus Henricus Gerardus Berendsen
  • 2-pyrrolidinone derivatives substituted at position 4 for reducing the extracellular glutamate level
    Patent number: 6984659
    Abstract: 2-pyrrolidinone derivatives which have in position 4 at least one substituent are described herein. Methods of treating polygltamine disorders such as Huntington's disease, dentorubropallidoluysian atrophy (DRPLA), spinal and bulbar muscular atrophy (SBMA), and spinocerebellar ataxias with 2-pyrrolidinone derivatives are also descibed.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: January 10, 2006
    Assignee: Klinikum der Albert-Ludwigs Universitaet
    Inventors: Thomas J. Feuerstein, Rainer Knoerle
  • Sulfonamide compounds and uses thereof
    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
  • Kappa agonist compounds, pharmaceutical formulations and method of prevention and treatment of pruritus therewith
    Patent number: 6960612
    Abstract: Methods for prevention or treatment of pruritus are provided. The methods comprise administering to a patient an effective amount of a kappa opioid receptor agonist compound. The involved kappa opioid receptor agonist compounds are of the type represented by the following formula III wherein R1, R2, Ar, X7, and n are as defied in the specification.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: November 1, 2005
    Assignee: Adolor Corporation
    Inventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
  • Use of glycogen phosphorylase inhibitors for treatment of cardiovascular diseases
    Patent number: 6960610
    Abstract: The present invention provides methods which may effectively be used in the treatment and prevention of early cardiac and early cardiovascular diseases, for example of ischemic origin, such as left ventricular hypertrophy, coronary artery disease, essential hypertension, acute hypertensive emergency, cardiomyopathy, heart insufficiency, exercise tolerance, chronic heart failure, arrhythmia, cardiac dysrhythmia, syncopy, arteriosclerosis, mild chronic heart failure, angina pectoris, cardiac bypass reocclusion, intermittent claudication (arteriosclerosis oblitterens), diastolic dysfunction and systolic dysfunction, as well as improving the success of heart transplantations, through administration of glycogen phosphorylase inhibitor compounds.
    Type: Grant
    Filed: May 5, 2003
    Date of Patent: November 1, 2005
    Assignee: Novo Nordick, A/S
    Inventors: Klaus Asger Rytved, Nils Dragsted, Niels Chresten Berg Nyborg, Lars Iversen, Marit Kristiansen
  • Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
    Patent number: 6951848
    Abstract: Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disclosed is a method for treating a patient having an inflammatory disease and/or viral infection comprising administering an effective amount of a compound of Formula I. In particular embodiments, the invention is a method for treating a patient infected with HIV.
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: October 4, 2005
    Assignee: Millennium Pharmaceuticals, Inc.,
    Inventors: Geraldine C. B. Harriman, Kenneth G. Carson, Daniel L. Flynn, Michael E. Solomon, Yuntao Song, Bharat K. Trivedi, Bruce D. Roth, Christine N. Kolz, Ly Pham, Kuai-lin Sun
  • Compounds which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 6949570
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, 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: May 7, 2002
    Date of Patent: September 27, 2005
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Susan Ashwell, Reinhardt Bernhard Baudy, Michael A. Pleiss, Dimitrios Sarantakis, Eugene D. Thorsett
  • Compounds for the treatment of protozoal diseases
    Patent number: 6949567
    Abstract: The invention relates to new diphenylurea having the formula (I) or a salt thereof, where Y is C?O, C?S, C?NH, (C?O)2 or SO2; and to processes for the preparation of these compounds and to their use in the treatment of protozoal diseases and to diseases where the inhibition of intracellular protein-degradation pathways is of benefit.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: September 27, 2005
    Assignee: 4SC AG
    Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Jürgen Kraus, Rolf Krauss, Johan Leban, Stefano Pegoraro, Wael Saeb, Kristina Wolf
  • Antibacterial agents
    Patent number: 6908911
    Abstract: Selected compounds of formula (I) are antibacterial agents: formula (I) wherein R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl (C1-C6 alkyl)- or aryl (C1-C6 alkyl)-group, and A represents a group of formula (IA), or (IB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 are each independently hydrogen or C1-C6 alkyl, heterocyclic or aryl (C1-C6 alkyl)-, R5 and R6 when taken together with the nitrogen atom to which they are attached from an optionally substituted saturated heterocyclic ring of 3 to 8 atoms which ring is optionally fused to a carbocyclic or second heterocyclic ring
    Type: Grant
    Filed: August 10, 1999
    Date of Patent: June 21, 2005
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
  • Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1
    Patent number: 6903123
    Abstract: Disclosed are nociceptin ORL-1 receptor agonists of the formula wherein: (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; R2 is H; and R3 is —C(H)(R)—NR7R8; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; R7 is —(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8 is H; or R7 and R8 together form a substituted piperidinyl or piperazinyl ring; x is 0-10; and R9 is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) R2 is —NHR7 or and R3 is H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: June 7, 2005
    Assignee: Schering Corporation
    Inventors: Duane A. Burnett, Mary Ann Caplen, Michael F. Czarniecki, Martin S. Domalksi, Ginny D. Ho, Deen Tulshian, Wen-Lian Wu
  • Phenylheteroalkylamine derivatives
    Patent number: 6900243
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 31, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
  • Synergistic therapeutic compositions and methods
    Patent number: 6900234
    Abstract: Compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, synergistic compositions comprising amounts of at least two therapeutic agents selected from the group consisting of a renin inhibitor, an angiotensin I converting enzyme inhibitor and an angiotensin II antagonist, which inhibitors and antagonists are present in amounts sufficient to cause synergistic therapeutic effects such as lowering blood pressure and treating congestive heart failure in a mammal.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: May 31, 2005
    Assignee: Pfizer, Inc.
    Inventor: Anthony Andrea Fossa
  • Use of substituted 4-biarylbutyric and 5-biarylpentanoic acid derivatives as matrix metalloprotease inhibitors for the treatment of respiratory diseases
    Patent number: 6900194
    Abstract: Novel 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives, use of substituted 4-Biarylbutyric and 5-Biarylpentanoic Acid Derivatives as Matrix Metalloprotease Inhibitors for the Treatment of Respiratory Diseases, pharmaceutical compositions containing them, and a process for using them. The compounds of the invention have the generalized formula (I) (T)xA—B—D—E—CO2H wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group, x is 0, 1, or 2; the group D represents (a), (b), (c), or (d); the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 20, 1999
    Date of Patent: May 31, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mary F. Fitzgerald, Philip J. Gardiner, Kevin Nash, Graham Sturton, Günter Benz, Rolf Henning, Karl-Heinz Schlemmer, Bernd Riedl, Helmut Haning, Lorenz Mayr
  • Acyl sulfonamides as inhibitors of HIV integrase
    Patent number: 6890942
    Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: May 10, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
  • Histamine H3 receptor ligands
    Patent number: 6878736
    Abstract: Compounds of formula (I) (and pharmaceutically acceptable salts thereof) are histamine H3 receptor ligands.
    Type: Grant
    Filed: February 15, 1999
    Date of Patent: April 12, 2005
    Assignee: James Black Foundation Limited
    Inventors: Sarkis Barret Kalindjian, Ildiko Maria Buck, Ian Duncan Linney, Gillian Fairfull Watt, Elaine Anne Harper, Nigel Paul Shankley
  • Substituted cyclic amine metalloprotease inhibitors
    Patent number: 6872742
    Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: March 29, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Michael George Natchus, Biswanath De, Stanislaw Pikul, Neil Gregory Almstead, Roger Gunnard Bookland, Yetunde Olabisi Taiwo, Menyan Cheng
  • Active substance combinations having insecticidal and acaricidal properties
    Patent number: 6864276
    Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.
    Type: Grant
    Filed: May 7, 2001
    Date of Patent: March 8, 2005
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Use of EP4 receptor ligands in the treatment of neuropathic pain and colon cancer
    Patent number: 6861441
    Abstract: The present invention relates to the use of an EP4 receptor ligand in the manufacture of a medicament for use in the treatment of neuropathic pain, colon cancer, migraine, and for increasing the latency of HIV infection.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: March 1, 2005
    Assignee: SmithKline Beecham Corporation
    Inventors: Nicholas Maughan Clayton, Susanne Denise Collins, Steven Michael Foord, Gerard Martin Paul Giblin, Richard John Coles, Mark Bamford, Jennifer M Doughty, Richard Green
  • Potentiation of the microbicide 2-(thiocyanomethylthio)benzothiazole using an N-alkyl heterocyclic compound
    Patent number: RE39033
    Abstract: Microbicidal compositions are described. The compositions comprise (a) 2-(Thiocyanomethylthio)benzothiazole (TCMTB) and (b) an N-alkyl heterocyclic compound of the formula: The variable “n” ranges from 5 to 17, and the heterocyclic ring defined by is a substituted or unsubstituted ring having four to eight members. Components (a) and (b) are present in a combined amount effective to control the growth of at least one microorganism. Methods for controlling the growth of microorganisms on various substrates or in aqueous systems are also described. Also described is the industrial application of the microbicidal composition in the leather industry, the lumber industry, the papermaking industry, the textile industry, the agricultural industry, and the coating industry, as well as in aqueous systems.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: March 21, 2006
    Assignee: Buckman Laboratories International, Inc.
    Inventors: Marilyn S. Whittemore, Daniel E. Glover, S. Rao Rayudu, Dean T. Didato