The Six-membered Hetero Ring Consists Of Two Nitrogens And Four Carbons (e.g., 1,2-diazines, Etc.) Patents (Class 544/224)
  • Publication number: 20120245125
    Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.
    Type: Application
    Filed: June 8, 2012
    Publication date: September 27, 2012
    Applicants: Northwestern University
    Inventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
  • Patent number: 8273897
    Abstract: Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are reduced to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A radical is as defined in the description:
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: September 25, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Norbert Lui, Stefan Antons
  • Patent number: 8268754
    Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted dihydroazole compound of General Formula (1) or a salt thereof: where A1, A2, A3 and A4 are independently C—Y or N, A5 is —CH2—, etc., G1 is a benzene ring, etc., G2 is G2-1, G2-6, G2-9, etc., X is a halogen atom, C1-2haloalkyl, etc., Z is methyl, —NH2, etc., R1 is —C(O)R1a, etc., R1a is C1-4alkyl, etc., R2 is H, C1-4alkyl, etc., R3 is C1-2haloalkyl, etc., R4 is H, cyano, methyl, etc., m is an integer of 1, 2, 3, etc., n is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: September 18, 2012
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Eitatsu Ikeda, Hiroaki Takahashi, Mitsuaki Komoda
  • Patent number: 8258138
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives wherein R1, R2, R3, X1, and A are defined herein. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: September 4, 2012
    Assignee: Xention Limited
    Inventors: Derek Edward John, Mushtaq Mulla, Richard John Hamlyn, Simon Mark Jones, Derek Roland Pollard, Basil Hartzoulakis, Helen Payne, David Madge, John Ford
  • Patent number: 8258134
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Grant
    Filed: March 9, 2009
    Date of Patent: September 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
  • Patent number: 8252935
    Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of Het, R0, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: August 28, 2012
    Assignees: Janssen Pharmaceutica N.V., Cellzome Limited
    Inventors: Chih Yung Ho, Yan Zhang, Umar S. M. Maharoof, Jeremy Major, John Harrison
  • Publication number: 20120214785
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
  • Patent number: 8247414
    Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: August 21, 2012
    Assignee: Cephalon, Inc.
    Inventors: Edward R. Bacon, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Robert L. Hudkins, Kurt A. Josef, Ming Tao, Allison L. Zulli
  • Patent number: 8242055
    Abstract: The invention describes phenyl-substituted pyridazinones of the formula (I) as herbicides and insecticides. In this formula (I), A, B, G, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen, nitro and cyano.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: August 14, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Stefan Lehr, Thomas Schenke, Christopher Hugh Rosinger, Reiner Fischer, Isolde Häuser-Hahn, Dieter Feucht, Jan Dittgen, Pierre Cristau, Oliver Gaertzen, Stefan Herrmann, Olga Malsam, Eva-Maria Franken
  • Patent number: 8236950
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: August 7, 2012
    Assignee: Abbott Laboratories
    Inventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
  • Publication number: 20120184553
    Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
    Type: Application
    Filed: September 27, 2010
    Publication date: July 19, 2012
    Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
  • Patent number: 8222256
    Abstract: The invention provides methods of treating cancer with a compound which inhibits kinases, more specifically IGF1R and Abl, in combination with treatments(s) selected from surgery, radiation, monoclonal antibody, bone marrow or peripheral blood stem cell transplantation, and one or more chemotherapeutic agent(s).
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: July 17, 2012
    Assignee: Exelixis, Inc.
    Inventor: Wentao Zhang
  • Publication number: 20120178927
    Abstract: The invention relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.
    Type: Application
    Filed: July 12, 2011
    Publication date: July 12, 2012
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Stefan LEHR, Dieter FEUCHT, Eva-Maria FRANKEN, Olga MALSAM, Alfred ANGERMANN, Guido BOJACK, Christian ARNOLD, Martin Jeffery HILLS, Heinz KEHNE, Christopher Hugh ROSINGER
  • Patent number: 8212048
    Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: July 3, 2012
    Assignees: Sumitomo Chemical Company, Limited, Osaka University
    Inventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
  • Publication number: 20120165343
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
    Type: Application
    Filed: December 22, 2011
    Publication date: June 28, 2012
    Applicant: Pfizer Inc.
    Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
  • Patent number: 8207172
    Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 26, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Chengzhi Zhang, Jacques Dumas, Qingming Zhu, Roger Smith, Qingjie Liu, Sharad Verma, Jason Duquette, Qian Zhao, Dongping Fan, Georgiy Bondar, Philip Coish
  • Publication number: 20120135995
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R3, R4a, R4b, R5, W, m and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 2, 2010
    Publication date: May 31, 2012
    Applicant: E.I. Dupont de Nemours and Company
    Inventor: Paula Louise Sharpe
  • Patent number: 8188008
    Abstract: The invention describes phenyl-substituted pyridazinones of the formula (I) as herbicides and insecticides. In this formula (I), A, B, G, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen, nitro and cyano.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: May 29, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Stefan Lehr, Thomas Schenke, Christopher Hugh Rosinger, Reiner Fischer, Isolde Häuser-Hahn, Dieter Feucht, Jan Dittgen, Pierre Cristau, Oliver Gaertzen, Stefan Herrmann, Olga Malsam, Eva-Maria Franken
  • Patent number: 8188077
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: May 29, 2012
    Assignee: Abbott Laboratories
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Publication number: 20120129858
    Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formula I-III) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 19, 2010
    Publication date: May 24, 2012
    Inventors: Stephen David Penrose, Kevin James Doyle
  • Patent number: 8178538
    Abstract: The present invention is concerned with novel pyridazinones of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of CNS disorders.
    Type: Grant
    Filed: November 30, 2009
    Date of Patent: May 15, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Luca Gobbi, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento, Mark Rogers-Evans, Markus Rudolph
  • Patent number: 8173653
    Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: May 8, 2012
    Assignee: Merck Patent Gesellschaft MIT Beschraenkter Haftung
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat
  • Patent number: 8168734
    Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is independently halogen, cyano, —CF3, —CF2H, —CFH2, —OCF3, —OCF2H, —N?C?O, —N?C?S or alkyl having a carbon number of approximately 1 to approximately 20; in the alkyl, optional —CH2— may be substituted with —O—, —S—, —SO2—, —CO—, —COO—, —OCO—, —CH?CH—, —CF?CF— or —C?C—, and optional hydrogen may be substituted with halogen; Rb is fluorine or —CF3; A is independently 1,4-cyclohexylene, 1,4-cyclohexenylene, 1,4-phenylene, naphthalene-2,6-diyl, tetrahydronaphthalene-2,6-diyl, fluorene-2,7-diyl or bicyclo[2.2.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: May 1, 2012
    Assignees: JNC Corporation, Chisso Petrochemical Corporation
    Inventor: Takashi Kato
  • Patent number: 8158021
    Abstract: A polymerizable liquid crystal compound shown by the following formula (I), a polymerizable liquid crystal composition that includes the polymerizable liquid crystal compound and a chiral compound polymerizable with the polymerizable liquid crystal compound, a liquid crystalline polymer obtained by polymerizing the polymerizable liquid crystal compound or the polymerizable liquid crystal composition, and an optical anisotropic article that includes the liquid crystalline polymer. The polymerizable liquid crystal compound shows a liquid crystal phase over a wider temperature range, is chemically stable, can be inexpensively produced, and has a wide selective reflection wavelength band ?? (i.e., a large value ?n).
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: April 17, 2012
    Assignee: Zeon Corporation
    Inventors: Kei Sakamoto, Naoto Kogoshi, Yoshihide Yachi
  • Patent number: 8158631
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: April 17, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Ryan Craig Schoenfeld, Francisco Xavier Talamas
  • Patent number: 8153647
    Abstract: Disclosed are compounds according to formula (I): wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).
    Type: Grant
    Filed: December 15, 2008
    Date of Patent: April 10, 2012
    Assignee: Sanofi-Aventis
    Inventors: Jozsef Zsolt Bocskei, Gary McCort, Hans Matter, Henning Steinhagen, Bérangère Thiers
  • Publication number: 20120077806
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
    Type: Application
    Filed: September 23, 2011
    Publication date: March 29, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
  • Patent number: 8143408
    Abstract: The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: March 27, 2012
    Assignee: AstraZeneca AB
    Inventors: Yevgeni Besidski, Inger Kers, Martin Nylöf, Lars Sandberg, Karin Skogholm
  • Patent number: 8143252
    Abstract: Methods for inhibiting a neoplasm in a subject and methods of inhibiting undesired angiogenesis that include administering to a subject a therapeutically effective amount of at least one novel tetrahalogenated compound, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: March 27, 2012
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: William D. Figg, Erin Gardner, Michael Gutschow, Agnieszka Ambrozak
  • Publication number: 20120071651
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 22, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Publication number: 20120065066
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: May 16, 2009
    Publication date: March 15, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Christopher John Mathews, Louisa Robinson, Stephane Andre Marie Jeanmart
  • Patent number: 8133847
    Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyrido[2,3-b]pyrazines.
    Type: Grant
    Filed: July 16, 2007
    Date of Patent: March 13, 2012
    Assignee: Syngenta Limited
    Inventors: Neil Brian Carter, Matthew Robert Cordingley, Patrick Jelf Crowley, Michael Drysdale Turnbull
  • Patent number: 8114899
    Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: February 14, 2012
    Assignee: Sanofi-Aventis
    Inventors: Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
  • Publication number: 20120028803
    Abstract: A pyridazinone compound represented by formula (I) wherein R1 represents a C1-6 alkyl group or a (C1-6 alkyloxy) C1-6 alkyl group, R2 and R3 represent hydrogen or a C1-6 alkyl group, W represents halogen, etc., Z1 represents a C1-6 alkyl group, Z2 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, etc., and n represents 0, 1, 2, 3 or 4, has a weed-controlling effect and an arthropod-controlling effect.
    Type: Application
    Filed: March 12, 2010
    Publication date: February 2, 2012
    Inventor: Takafumi Fusaka
  • Publication number: 20120028971
    Abstract: The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: February 24, 2010
    Publication date: February 2, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Thomas Lampe, Michael Hahn, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Stefan Heitmeier, Nils Griebenow, Sherif El Sheikh, Volkhart Min-Jian Li, Eva-Maria Becker, Friederike Stoll, Andreas Knorr
  • Patent number: 8106045
    Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R? represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: September 9, 2005
    Date of Patent: January 31, 2012
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-Aventis
    Inventors: Kazutoshi Watanabe, Fumiaki Uehara, Shinsuke Hiki, Toshiyuki Kohara, Kenji Fukunaga, Satoshi Yokoshima
  • Patent number: 8106053
    Abstract: To find a compound having a tissue fibrinosis-inhibitory activity and a fibrinolytic activity, and to provide a novel compound that is useful for preventing and/or treating tissue fibrinosis diseases (pulmonary fibrosis, renal fibrosis etc.), diseases caused by pathological blood clots such as ischemic heart diseases (myocardial infarction, angina), intraatrial thrombus, pulmonary embolism, deep venous thrombosis, disseminated intravascular coagulation, ischemic cerebral diseases (cerebral infarction, cerebral bleeding) and arteriosclerosis and the like. To provide a pharmaceutical drug comprising a 5-phenyl-3-pyridazinone derivative represented by the following general formula (I): and an optical isomer thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, useful for preventing and/or treating disease conditions or symptoms mediated by plasminogen activator inhibitor-1.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: January 31, 2012
    Assignee: Kowa Company, Ltd.
    Inventors: Noriaki Gomi, Shinji Ina, Kenjirou Yamana, Yoshio Kaneko
  • Publication number: 20120010207
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 11, 2011
    Publication date: January 12, 2012
    Applicant: PFIZER LIMITED
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Marcel John De Groot
  • Patent number: 8080551
    Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: December 20, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
  • Publication number: 20110294818
    Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
    Type: Application
    Filed: July 28, 2011
    Publication date: December 1, 2011
    Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
  • Patent number: 8067589
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: November 29, 2011
    Assignee: Pfizer Inc
    Inventors: Tanisha D. Blake, Bruce C. Hamper, Wei Huang, James R. Kiefer, Jr., Joseph B. Moon, Bradley E. Neal, Kirk L. Olson, Matthew J. Pelc, Barbara A. Schweitzer, Atli Thorarensen, John I. Trujillo, Steven R. Turner
  • Publication number: 20110288296
    Abstract: The application relates to a reagent of the general formula R1R2N—ZnY LiY??(I) wherein R1, R2 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; Halon, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx; wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or
    Type: Application
    Filed: February 11, 2010
    Publication date: November 24, 2011
    Inventors: Paul Knochel, Marc Mosrin
  • Publication number: 20110281879
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 17, 2011
    Applicant: ViroBay, Inc.
    Inventor: Craig Mossman
  • Publication number: 20110281876
    Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.
    Type: Application
    Filed: June 10, 2011
    Publication date: November 17, 2011
    Applicant: Purdue Pharma L.P.
    Inventor: Qun SUN
  • Publication number: 20110263530
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Application
    Filed: June 28, 2011
    Publication date: October 27, 2011
    Applicant: Amgen Inc.
    Inventors: Victor J. CEE, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
  • Publication number: 20110263849
    Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.
    Type: Application
    Filed: December 25, 2009
    Publication date: October 27, 2011
    Applicants: GIFU UNIVERSITY, RIKEN
    Inventors: Masaaki Suzuki, Hisashi Doi, Hiroko Koyama
  • Publication number: 20110251068
    Abstract: Disclosed is a parasitic plant control agent which can control a parasitic plant effectively. Also disclosed is a parasitic plant control method. A parasitic plant can be controlled by inhibiting the metabolism of gentianose in the parasitic plant to inhibit the germination of the parasitic plant.
    Type: Application
    Filed: October 5, 2009
    Publication date: October 13, 2011
    Applicant: OSAKA UNIVERSITY
    Inventors: Atsushi Okazawa, Joseph Benesh
  • Publication number: 20110237595
    Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.
    Type: Application
    Filed: June 9, 2011
    Publication date: September 29, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Ahmed ABOUABDELLAH, Regine BARTSCH-LI, Christian HOORNAERT, Antoine RAVET
  • Publication number: 20110229941
    Abstract: Novel isolated DNA sequences which comprise all or part of a gene cluster encoding sanglifehrin synthase, processing and regulatory genes involved in the biosynthesis of a mixed non-ribosomal peptide/polyketide compound, or mutants having altered biosynthetic capability, polypeptides or mutants thereof encoded by DNA or the mutants, vectors containing the DNA or the mutants thereof, host cells transformed with the DNA, the mutants thereof, or the vector, and a method for producing sanglifehrin compounds. Compounds with cyclophilin inhibition activity used as immunosuppressants, antivirals or cardiac protection agents.
    Type: Application
    Filed: September 24, 2009
    Publication date: September 22, 2011
    Inventors: Wen Liu, Nan Jiang, Xudong Qu
  • Publication number: 20110223093
    Abstract: This invention relates to sulfur functionalized ionic liquid compounds that are useful in methods of carbon dioxide or sulfur dioxide removal to which they may be applied.
    Type: Application
    Filed: March 11, 2011
    Publication date: September 15, 2011
    Applicant: E.I. DU PONT DE NEMOURS AND COMAPNY
    Inventor: MARK A. SCIALDONE