Patents Examined by Venkataraman Balasubram
  • Patent number: 7585870
    Abstract: This invention concerns HIV replication inhibitors of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: September 8, 2009
    Assignee: Tibotec BVBA
    Inventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig Arts
  • Patent number: 7563922
    Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) ?in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) ?with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: July 21, 2009
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jérôme Emile Georges Guillemont
  • Patent number: 7544690
    Abstract: The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.
    Type: Grant
    Filed: September 30, 2002
    Date of Patent: June 9, 2009
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Yoshinori Sekiguchi, Kosuke Kanuma, Katsunori Omodera, Thuy-Anh Tran, Bryan Aubrey Kramer, Nigel Robert Arnold Beeley
  • Patent number: 7511140
    Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.
    Type: Grant
    Filed: August 7, 2003
    Date of Patent: March 31, 2009
    Assignee: AstraZeneca AB
    Inventors: John Horbury, Nigel Philip Taylor
  • Patent number: 7491730
    Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: February 17, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Cornelia J. Forster, Larry C. Park, Marion W. Wannamaker, Yung-Mae M. Yao
  • Patent number: 7470700
    Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV inhibitors comprising Formula I: wherein the substituents are as described herein.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: December 30, 2008
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun Feng, Stephen L. Gwaltney, II, Stephen W. Kaldor, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang
  • Patent number: 7470681
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: December 30, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostik, Yumiko Wada
  • 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: 7465735
    Abstract: 5-Phenylpyrimidines, their preparation, compositions comprising them and their use 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C(?O)NRaRb or —C(?O)Rc; in whic
    Type: Grant
    Filed: November 15, 2002
    Date of Patent: December 16, 2008
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
  • Patent number: 7465725
    Abstract: This invention features pyrimidine compounds of formula (I): R1 is aryl, or heteroaryl; each of R2 and R4, independently, is Rc, halogen, nitro, cyano, isothionitro, SRc, or ORc; or R2 and R4, taken together, is carbonyl; R3 is Rc, alkenyl, alkynyl, ORc, OC(O)Rc, SO2Rc, S(O)Rc, S(O2)NRcRd, SRc, NRcRd, NRcCORd, NRcC(O)ORd, NRcC(O)NRcRd, NRcSO2Rd, CORc, C(O)ORc, or C(O)NRcRd; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is O, S, S(O), S(O2), or NRc; Y is a covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which each of Ra and Rb, independently, is H, alkyl, aryl, heteroaryl; and each of Rc and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: December 16, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Mitsunori Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostik, Weiwen Ying, Yumiko Wada, Keizo Koya
  • Patent number: 7462616
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
    Type: Grant
    Filed: October 24, 2006
    Date of Patent: December 9, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, John T. Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
  • Patent number: 7462614
    Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
    Type: Grant
    Filed: March 29, 2004
    Date of Patent: December 9, 2008
    Assignee: Smithkline Beecham Corporation
    Inventors: Mui Cheung, Nigel Paul King, Kevin Wayne Kuntz, Robert Anthony Mook, Jr., Mark Andrew Pobanz, James Michael Salovich, Brian John Wilson
  • Patent number: 7462625
    Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Grant
    Filed: September 11, 2006
    Date of Patent: December 9, 2008
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
  • Patent number: 7456176
    Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
    Type: Grant
    Filed: April 7, 2005
    Date of Patent: November 25, 2008
    Assignee: TargeGen, Inc.
    Inventors: Glenn Noronha, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Xianchang Gong, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Binqi Zeng, Ningning Zhao, Elena Dneprovskaia
  • Patent number: 7452879
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: October 5, 2006
    Date of Patent: November 18, 2008
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Patent number: 7452897
    Abstract: The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: November 18, 2008
    Assignees: Sanofi-Aventis, Mitsubishi Pharma Corporation
    Inventors: Alistair Lochead, Mourad Saady, Franck Slowinski, Philippe Yaiche
  • Patent number: 7449471
    Abstract: 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C (?O)NRaRb or —C(?O)Rc; in which Ra, Rb and Rc are as defined in the description; X is halogen, alkyl, alkoxy o
    Type: Grant
    Filed: February 22, 2007
    Date of Patent: November 11, 2008
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
  • Patent number: 7449470
    Abstract: The invention provides a compound of formula (I) wherein R and R? are selected from hydrogen, alkyl, alkenyl, alkynyl, or aryl; R? and R?? are selected from hydrogen, acyl, thio-acyl, seleno-acyl, alkyl, alkenyl, alkynyl, or aryl; or a pharmaceutically acceptable salt thereof, to interact with the adenosine receptors in the beneficial treatment and/or prevention of a (dis)order arising from the said receptors. The invention further provides pharmaceutical compositions comprising said compounds. The invention also relates to the use of said compositions for treating an/or preventing a variety of diseases.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: November 11, 2008
    Assignee: Universiteit Leiden
    Inventors: Lisa Chung Wai Chang, Adriaan P. Ijzerman, Johannes Brussee
  • Patent number: 7449574
    Abstract: The present invention relates to a triazine based photoactive compound containing an oxime ester group. The compound according to the present invention is a photoactive compound containing both an oxime ester group and a triazine group in one molecule, has excellent radical-generating efficiency due to effective absorption of UV radiation, particularly i-line (365 nm) radiation and can function as an effective initiator for photopolymerization of various compounds containing unsaturated groups, particularly an acryl compound.
    Type: Grant
    Filed: November 6, 2006
    Date of Patent: November 11, 2008
    Assignee: LG Chem, Ltd.
    Inventors: Sung Hyun Kim, Jeong Ae Yoon, Raisa Kharbash, Han Soo Kim, Xiang Li Li, Min Young Lim, Chang Ho Cho
  • Patent number: 7446209
    Abstract: This invention relates to a novel process for the synthesis of Temozolomide, an antitumor compound, and analogs, and to intermediates useful in this novel process.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: November 4, 2008
    Assignee: Schering Corporation
    Inventors: Shen-Chun Kuo, Janet L. Mas, Donald Hou