Patents Examined by Cecilia M. Jaisle
  • Phthalazine derivatives as inhibitors of protein kinase
    Patent number: 8044041
    Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives of formula (III) that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: October 25, 2011
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
  • Fused heterocyclic derivative and use thereof
    Patent number: 8044049
    Abstract: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.
    Type: Grant
    Filed: August 3, 2007
    Date of Patent: October 25, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nozomu Sakai, Shinichi Imamura, Naoki Miyamoto, Takaharu Hirayama
  • N-formyl hydroxylamines compounds
    Patent number: 8044199
    Abstract: Novel N-formyl hydroxylamine compounds of formula I: wherein R1 is hydrogen, alkyl, heteroaryl, heterocycloalkyl, aryl, heteroaryl or cycloalkyl; R3 is hydrogen, halogen or alkoxy; R4 is pyridazinyl; n is 0 to 3; and wherein one or more of the ring nitrogen heteroatoms of said pyridazinyl is optionally oxidized and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: October 25, 2011
    Assignee: Vicuron Holdings LLC
    Inventors: Kathryn Rene Bracken, Simon Bushell, Karl Dean, Charles Francavilla, Rakesh K. Jain, Kwangho Lee, Mohindra Seepersaud, Lei Shu, Arathi Sundaram, Zhengyu Yuan
  • Method for producing bicyclic guanidines by use of a cyclic urea
    Patent number: 8039618
    Abstract: The present invention is directed to a method for producing bicyclic guanidines comprising heating a cyclic urea to a temperature >200° C. to form the bicyclic guanidines.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: October 18, 2011
    Assignee: PPG Industries Ohio, Inc.
    Inventors: Britt A. Minch, Charles R. Hickenboth, Richard F. Karabin, Steven R. Zawacky, Gregory J. McCollum
  • Method for producing alpha form crystals of sapropterin hydrochloride
    Patent number: 8039617
    Abstract: A method for selectively producing stable alpha form crystals of sapropterin hydrochloride is provided. In this method, the alpha form crystal of sapropterin hydrochloride is produced by dissolving sapropterin hydrochloride with hydrochloric acid at a concentration of not less than 4 mol/L at not less than 70 degrees C.; adding heated ethanol to the solution; and cooling the solution at a cooling rate of not faster than 3 degrees C./min to a temperature of 40 to 55 degrees C. to precipitate the crystals.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: October 18, 2011
    Assignees: Shiratori Pharmaceutical Co., Ltd., Daiichi Sankyo Company, Limited
    Inventors: Katsumi Hotoda, Hiroomi Kiyono, Shinnosuke Tazawa
  • Hydrates and polymorphs of 4-[[(7)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy--(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
    Patent number: 8034816
    Abstract: Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: October 11, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Peter Sieger, Gerd F. Kraemer, Rolf Herter, Matthias Hoffmann, Werner Rall, Rolf Schmid
  • Imidazopyridazine derivative having kinase inhibitory activity and pharmaceutical agent thereof
    Patent number: 8034812
    Abstract: The present invention provides an imidazopyridazine derivative compound having a potent kinase inhibitory activity and a pharmaceutical agent thereof useful for treatment or prevention of cancer and the like. One such compound is represented by the formula: or a salt thereof or a prodrug thereof. The pharmaceutical agent contains the imidazopyridazine derivative compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor, or a cancer metastasis suppressor.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: October 11, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nozomu Sakai, Shinichi Imamura, Naoki Miyamoto, Takaharu Hirayama
  • Triazolopyridazines as kinase modulators
    Patent number: 8030305
    Abstract: The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: October 4, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Tianbao Lu, Richard Alexander, Richard W. Connors, Maxwell D. Cummings, Robert A. Galemmo, Heather Rae Hufnagel, Dana L. Johnson, Ehab Khalil, Kristi A. Leonard, Thomas P. Markotan, Anna C. Maroney, Jan L. Sechler, Jeremy M. Travins, Robert W. Tuman
  • MAPK/ERK kinase inhibitors
    Patent number: 8030317
    Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: October 4, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Qing Dong, Stephen W. Kaldor
  • Azabicyclic heterocycles as cannabinoid receptor modulators
    Patent number: 8030306
    Abstract: The present application describes CB-1 inverse agonists according to Formula (I) and (Ia), pharmaceutical compositions comprising at least one compound according to Formula (I) or (Ia), and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) or (Ia), both alone and in combination with one or more additional therapeutic agents. The preferred compounds have the general Formula (Ia), including all prodrugs, pharmaceutically acceptable salts and stereoisomer, thereof, wherein R1, R2, Ar1, Ar2 are defined herein.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: October 4, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: William R. Ewing, Yeheng Zhu, Richard B. Sulsky
  • Octahydro-pyrrolo[3,4-b]pyrrole N-oxides
    Patent number: 8026240
    Abstract: The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compounds and compositions. Octahydro-pyrrolo[3,4-b]pyrrole N-oxides of formula (I) are prodrugs of histamine-3 antagonists, and are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole N-oxide compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: September 27, 2011
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Kennan C. Marsh, Huaqing Liu, Jae Y. Lee, Maria G. Beconi, Jill M. Wetter, Lawrence A. Black, Thomas C. Custer
  • Substituted pyridazine compounds and fungicidal uses thereof
    Patent number: 8022073
    Abstract: A pyridazine compound of the formula: has an excellent plant disease controlling effect.
    Type: Grant
    Filed: November 28, 2006
    Date of Patent: September 20, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Shin-ichiro Souma, Akio Manabe
  • Pyrido[2,3-d]pyrimidines useful as HCV inhibitors, and methods for the preparation thereof
    Patent number: 8022077
    Abstract: The present invention relates to the use of pyrido[2,3-d]pyrimidines of formula (I) wherein L, R1, R2 and R3 have specific meaning. The present invention also relates to the use of the compounds of formula (I) as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds of formula (I) per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: September 20, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson
  • Derivatives of pyrido[2,3-d]pyrimidine, the preparation thereof, and the therapeutic application of the same
    Patent number: 8008310
    Abstract: Derivatives of pyrido[2,3-d]pyrimidine are provided having formula (I) with Ar1, Ar2 and R1 as defined herein, which are useful for treating cell proliferative conditions, and to the preparation thereof, and to the therapeutic application of the same.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: August 30, 2011
    Assignee: Sanofi-Aventis
    Inventors: Bernard Bourrie, Pierre Casellas, Samir Jegham, Claude Muneaux, Pierre Perreaut
  • Process for producing 2,3-dihydropyridazine compound
    Patent number: 8008485
    Abstract: A process for producing a 2,3-dihydropyridazine compound represented by the formula (2): wherein R1, R2 and R3 are the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group which may be substituted with a halogen atom or atoms, an alkenyl group which may be substituted with a halogen atom or atoms, an alkoxy group which may be substituted with a halogen atom or atoms, an alkylthio group, an alkylsulfenyl group, an alkylsulfonyl group or a dialkylamino group; which comprises reacting a salt consisting of bromoacetic acid and an amine compound with a pyridazine compound represented by the formula (1): wherein R1, R2 and R3 are the same meanings as defined above.
    Type: Grant
    Filed: August 22, 2006
    Date of Patent: August 30, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Kazuaki Sasaki
  • Inhibitors of Akt activity
    Patent number: 8003643
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines 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: November 18, 2009
    Date of Patent: August 23, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Hexahydro-pyrazino[1,2-A]pyrimidine-4,7-dione derivatives substituted with amino acids
    Patent number: 7994168
    Abstract: The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments.
    Type: Grant
    Filed: February 21, 2007
    Date of Patent: August 9, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Petra Lennig, Siegfried Stengelin, Thomas Klabunde, Matthias Gossel, Pavel Safar, James Spoonamore, Gregory Merriman, Joseph T Klein, Brian Whiteley, Carolina Lanter, Kenneth Bordeau, Zhaoxia Yang, Martin Smrcina
  • Compositions useful as inhibitors of voltage-gated ion channels
    Patent number: 7968545
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 5, 2004
    Date of Patent: June 28, 2011
    Assignee: Vertex Pharmaceuticals Inc.
    Inventors: Dean M. Wilson, Andreas P. Termin, Timothy D. Neubert, Jian Wang, Yulian Zhang, Jesus E. Gonzalez, III, Esther Martinborough, Nicole Zimmerman
  • Pyridazinone kinase inhibitors
    Patent number: 7968546
    Abstract: Disclosed are compounds of Formula I wherein X is and R2, R1, A, B, D, E, R9 are as defined herein useful for treating cancers.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: June 28, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
  • Pyridazin-3(2)-one derivatives and their use as PDE4 inhibitors
    Patent number: 7960383
    Abstract: The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis or irritable bowel disease.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: June 14, 2011
    Assignee: Laboratorios Almirall SA
    Inventors: Antonia Maria Buil Albero, Vittorio Dal Piaz, Yolanda Garrido Rubio, Jordi Gracia Ferrer, Lluis Miquel Pages Santacana, Joan Taltavull Moll