Patents Examined by Cecilia M. Jaisle
  • Substituted 8?-pyri(MI)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-]pyrimidin-6-one derivatives
    Patent number: 7547705
    Abstract: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: June 16, 2009
    Assignees: Sanofi-Aventis, Mitsubishi Pharma Corporation
    Inventors: Nathalie Chereze, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
  • Dihydropteridione intermediate compounds
    Patent number: 7547780
    Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: June 16, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Matthias Hoffman, Christian Eickmeier
  • Met kinase inhibitors
    Patent number: 7547782
    Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: June 16, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Xiao-Tao Chen, David K. Williams, John S. Tokarski, Robert F. Kaltenbach
  • Inhibitors of Akt activity
    Patent number: 7544677
    Abstract: The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 9, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Nicholas D. P. Cosford, John C. Hartnett, Yiwei Li, Jun Liang, Peter J. Manley, Lou Anne Neilson, Tony Siu, Zhicai Wu
  • Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof
    Patent number: 7544682
    Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I) and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.
    Type: Grant
    Filed: January 8, 2007
    Date of Patent: June 9, 2009
    Assignee: Sanofi-Aventis
    Inventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Pierre Perreaut
  • 4-amino-7,8-dihydropteridines, pharmaceutical compositions containing them and their use for the treatment of diseases which are caused by an increased nitric oxide level
    Patent number: 7541360
    Abstract: The present invention relates to the area of NO synthase inhibition and, more particularly, relates to novel 4-amino-7,8-dihydropteridines, pharmaceutical compositions containing said compounds, and the use of said compounds in the treatment of a disorder characterized by a disturbed nitric oxide level.
    Type: Grant
    Filed: December 30, 2003
    Date of Patent: June 2, 2009
    Assignee: Vasopharm GmbH
    Inventors: Robert Doblhofer, Frank Tegtmeier
  • 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of ?-secretase (BACE)
    Patent number: 7531545
    Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: May 12, 2009
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Ellen E. Baxter, Christopher John Creighton, Yifang Huang, Chi Luo, Michael H. Parker, Allen B. Reitz, Charles H. Reynolds, Tina Morgan Ross, Eric D. Strobel, Brett A. Tounge
  • Sulfonamides
    Patent number: 7528139
    Abstract: Compounds of the formula (I), in which R6, R7, R8, R9 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: March 17, 2005
    Date of Patent: May 5, 2009
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Guenter Hoelzemann, Helene Crassier, Alfred Jonczyk, Wolfgang Staehle, Wilfried Rautenberg
  • Bicyclic pyrimidine derivatives
    Patent number: 7524852
    Abstract: [wherein m and n may be the same or different and each represents an integer of 1 to 3 wherein m+n is 4 or less; R1 represents —NR4R5 (wherein R4 and R5 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl or the like); R2 represents the above Formula (II), Formula (IV) or the like; A represents a single bond, —C(?O)—, —SO2—, —OC(?O)— or the like; and R3 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aralkyl or the like] Bicyclic pyrimidine derivatives represented by the above Formula (I), or quaternary ammonium salts thereof, or pharmaceutically acceptable salts thereof, or the like, are provided.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: April 28, 2009
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hitoshi Arai, Tsutomu Matsumura, Hiroshi Ishida, Yosuke Yamaura, Seiji Aratake, Etsuo Ohshima, Koji Yanagawa, Motoki Miyama, Koji Suzuki, Ari Kawabe, Satoshi Nakanishi, Katsuya Kobayashi, Takashi Sato, Ichiro Miki, Kimihisa Ueno, Shinya Fujii, Miho Iwase
  • Hydrazines and derivatives production process from hydrazines and dicarboxylic acid
    Patent number: 7517983
    Abstract: The present invention describes a process to form hydrazides from the reaction of a hydrazine and a dicarboxylic, using a Lewis acid as a main reagent of the reaction. The reaction occurs in a safe reactional environment, utilizing smooth conditions, neither involving high temperatures nor high pressures, producing the desired products with high yields, between 90-95%. The invention also describes a kit for utilization of chemiluminescent substances, comprised of two solutions.
    Type: Grant
    Filed: November 25, 2004
    Date of Patent: April 14, 2009
    Assignee: Universidade Federal Do Rio De Janeiro-UFRG
    Inventors: Cláudio Cerqueira Lopes, Rosângela Sabattini Capella Lopes, Jarí Nobrega Cardoso, Jacqueline Alves da Silva, Letícia Gomes Ferreira
  • Heterocyclic inhibitors of MEK and methods of use thereof
    Patent number: 7517994
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: May 18, 2005
    Date of Patent: April 14, 2009
    Assignee: Array Biopharma Inc.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Pyridazine derivatives and their use as therapeutic agents
    Patent number: 7514436
    Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: April 7, 2009
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Heinz W. Gschwend, Vishnumurthy Kodumuru, Shifeng Liu, Rajender Kamboj
  • Process for the oxidation of certain substituted sulfilimines to insecticidal sulfoximines
    Patent number: 7511149
    Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: March 31, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
  • Pyridazin-3(2H)-one derivatives and their use as PDE4 inhibitors
    Patent number: 7511038
    Abstract: New pyridazin-e-(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4.
    Type: Grant
    Filed: November 8, 2004
    Date of Patent: March 31, 2009
    Assignee: Laboratorios Almirall S.A.
    Inventors: Vittorio Dal Piaz, Nuria Aguilar Izquierdo, Maria Antonia Buil Albero, Yolanda Garrido Rubio, Maria Paola Giovannoni, Jordi Gracia Ferrer, Wenceslao Lumeras Amador, Claudia Vergelli
  • Substituted 8?-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one and 8?-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one derivatives
    Patent number: 7507743
    Abstract: The invention relates to therapeutic uses of a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. Specifically, the invention relates to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer disease.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: March 24, 2009
    Assignees: Sanofi-Aventis, Mitsubishi Pharma Corporation
    Inventors: Pascal George, Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
  • Pyridazinone derivatives
    Patent number: 7507734
    Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: March 24, 2009
    Assignee: Aventis Pharma S.A.
    Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
  • Derivatives of pyrido[2,3-d]pyrimidine, the preparation thereof, and the therapeutic application of the same
    Patent number: 7504406
    Abstract: The invention relates to derivatives of pyrido[2,3-d]pyrimidine, to the preparation thereof, and to the therapeutic application of the same.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: March 17, 2009
    Assignee: Sanofi-Aventis
    Inventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Claude Muneaux, Pierre Perreaut
  • 2-(piperidin-4-yl)-4,5-dihydro-2H-pyridazin-3-one derivatives as PDE4 inhibitors
    Patent number: 7494990
    Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: February 1, 2005
    Date of Patent: February 24, 2009
    Assignee: NYCOMED GmbH
    Inventors: Wiro M. P. B. Menge, Geert Jan Sterk
  • Amide derivatives of 7-amino-3-phenyl-dihydropyrimido[4,5-d]pyrimidinones, their manufacture and use as pharmaceutical agents
    Patent number: 7494993
    Abstract: The present invention relates to novel amide derivatives of 7-amino-3-phenyl dihydropyrimido[4,5-d]pyrimidinones, to a process for their manufacture, medicaments containing them and their manufacture as well as the use of these compounds as pharmaceutically active agents. The present derivatives are new compounds of the general formula (I).
    Type: Grant
    Filed: August 30, 2005
    Date of Patent: February 24, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Engh, Hubert Hertenberger, Konrad Honold, Birgit Masjost, Petra Rueger, Wolfgang Schaefer, Stefan Scheiblich, Manfred Schwaiger
  • Pyridazin-3(2H)-one derivatives
    Patent number: 7491722
    Abstract: Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4. R1, R2 and R4 are organic radicals, R3 is a cyclic group, and R5 is an ester or an aryl or heteroaryl group.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: February 17, 2009
    Assignee: Laboratorios Almirall S.A.
    Inventors: Vittorio Dal Piaz, Nuria Aguilar Izquierdo, Maria Antonia Buil Albero, Marta Carrascal Riera, Jordi Gracia Ferrer, Maria Paola Giovannoni, Claudia Vergelli