Abstract: Provided is a compound represented by general formula (6) and pharmaceutically acceptable salts thereof. (In the formula, R1 is a hydrogen atom or a C1-6 alkyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 haloalkyl group.
Abstract: The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.
Abstract: The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
Type:
Grant
Filed:
June 20, 2011
Date of Patent:
November 11, 2014
Assignee:
Pfizer Inc.
Inventors:
Michelle Marie Claffey, Jennifer Elizabeth Davoren, John Adams Lowe, III, Robert Joseph Mather
Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Type:
Grant
Filed:
January 20, 2011
Date of Patent:
November 11, 2014
Assignee:
CHDI Foundation, Inc.
Inventors:
Celia Dominguez, Leticia M. Toledo-Sherman, Dirk Winkler, Frederick Brookfield, Paula C. De Aguiar Pena
Abstract: Arylalkyl esters of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are herbicides for control of weeds especially those species common to rice and wheat cropping systems and in pasture management programs.
Type:
Grant
Filed:
January 24, 2012
Date of Patent:
November 11, 2014
Assignee:
Dow AgroSciences, LLC.
Inventors:
Carla N. Yerkes, Christian T. Lowe, Joseph D. Eckelbarger, Jeffrey B. Epp, Katherine A. Guenthenspberger, Thomas L. Siddall, Paul R. Schmitzer
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:
Grant
Filed:
August 17, 2011
Date of Patent:
November 4, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
Type:
Grant
Filed:
May 10, 2011
Date of Patent:
November 4, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
Abstract: The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M?, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
Type:
Grant
Filed:
November 11, 2011
Date of Patent:
October 14, 2014
Assignee:
Codexis, Inc.
Inventors:
Jack Liang, James Lalonde, Jun Zhu, John M. Gruber, John D. Munger, Jr.
Abstract: Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine, Formula (II). The intermediate is useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof in high yield and purity.
Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Type:
Grant
Filed:
February 5, 2013
Date of Patent:
October 7, 2014
Assignee:
Rigel Pharmacuticals, Inc.
Inventors:
Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
Type:
Grant
Filed:
December 8, 2010
Date of Patent:
September 30, 2014
Assignee:
Roche Palo Alto LLC
Inventors:
Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
Type:
Grant
Filed:
February 8, 2012
Date of Patent:
September 23, 2014
Assignee:
Bayer Healthcare LLC
Inventors:
Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood
Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
Type:
Grant
Filed:
November 21, 2012
Date of Patent:
September 23, 2014
Assignee:
Gilead Sciences, Inc.
Inventors:
Christiane Yoakim, Murray D. Bailey, Francois Bilodeau, Rebekah Carson, Lee Fader, Stephen Kawai, Sebastien Morin, Carl Thibeault, Bruno Simoneau, Simon Surprenant, Youla S. Tsantrizos, Steven R. Laplante
Abstract: The invention relates to pyrimidine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
Type:
Grant
Filed:
April 15, 2010
Date of Patent:
September 16, 2014
Assignee:
Wyeth LLC
Inventors:
Kevin Joseph Curran, Joshua Aaron Kaplan, David James Richard, Jeroen Cunera Verheijen, Arie Zask
Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
Type:
Grant
Filed:
November 7, 2012
Date of Patent:
September 16, 2014
Assignee:
Pfizer Inc.
Inventors:
Edward L. Conn, David Hepworth, Roger B. Ruggeri
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.
Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Type:
Grant
Filed:
August 7, 2013
Date of Patent:
September 2, 2014
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
Abstract: 4-amido-pyrimidine compounds, derivatives and compositions thereof, and synthetic methods described herein are useful for modulating ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Type:
Grant
Filed:
May 22, 2006
Date of Patent:
September 2, 2014
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor