Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/245)
  • Patent number: 8975235
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 10, 2015
    Assignee: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Publication number: 20140356322
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Patent number: 8846936
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140256744
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140213538
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 31, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
  • Patent number: 8785442
    Abstract: The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors.
    Type: Grant
    Filed: January 30, 2011
    Date of Patent: July 22, 2014
    Assignee: Curegenix, Inc.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Patent number: 8778983
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: July 15, 2014
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda, David Nathan Zalatan
  • Patent number: 8735430
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: May 27, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki
  • Patent number: 8735362
    Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: May 27, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20140080828
    Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 20, 2014
    Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITY
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
  • Patent number: 8664220
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: March 4, 2014
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas J. Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
  • Publication number: 20140031353
    Abstract: The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors.
    Type: Application
    Filed: January 30, 2011
    Publication date: January 30, 2014
    Applicant: CUREGENIX, INC.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Publication number: 20140031364
    Abstract: Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 30, 2014
    Applicant: IL-YANG PHARM. CO., LTD.
    Inventors: Dong Yeon Kim, Dae Jin Cho, Gong Yeal Lee, Hong Youb Kim, Seok Hun Woo, Hae Un Lee, Sung Moo Kim, Choong Am Ahn, Seung Bin Yoon
  • Publication number: 20140024690
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: March 23, 2012
    Publication date: January 23, 2014
    Applicant: PFIZER Inc.
    Inventors: Joseph Alan Abramite, Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Patent number: 8629157
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain (I).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khor, Doris Riether, Lifen Wu, Renee M. Zindell
  • Patent number: 8592402
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: November 26, 2013
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas J. Seiders, Wang Bowei
  • Patent number: 8546588
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: October 1, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 8546563
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
  • Publication number: 20130231342
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Application
    Filed: July 27, 2011
    Publication date: September 5, 2013
    Applicant: Oryzon Fenomics S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
  • Publication number: 20130165490
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, G2, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 21, 2013
    Publication date: June 27, 2013
    Applicants: Syngenta Crop Protection LLC
    Inventors: Myriem El Qacemi, Thomas Pitterna, Jerome Yves Cassayre, Peter Renold
  • Patent number: 8455499
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: June 4, 2013
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
  • Publication number: 20130072449
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: August 14, 2012
    Publication date: March 21, 2013
    Applicant: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20130072490
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 21, 2013
    Applicant: Amira Pharmaceuticals INC.
    Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
  • Patent number: 8383616
    Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: February 26, 2013
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite SpA
    Inventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Claudio Pisano, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati
  • Publication number: 20130041000
    Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.
    Type: Application
    Filed: August 14, 2012
    Publication date: February 14, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
  • Patent number: 8372874
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: February 12, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Monika Ermann
  • Publication number: 20130030022
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Patent number: 8349871
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: January 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • Publication number: 20120289522
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: October 1, 2010
    Publication date: November 15, 2012
    Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20120238517
    Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: December 1, 2010
    Publication date: September 20, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Publication number: 20120196839
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: August 3, 2010
    Publication date: August 2, 2012
    Applicant: AMIRA PHARMACEUTICALS INC.
    Inventors: John Howard Hutchinson, Thomas J. Seiders, Bowei Wang
  • Patent number: 8217066
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: July 10, 2012
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Lucy Zhao, Jeannie M. Arruda, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
  • Publication number: 20120142666
    Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: June 8, 2010
    Publication date: June 7, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
  • Patent number: 8178568
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: May 15, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John Regan, Doris Riether
  • Patent number: 8158825
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: April 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • Publication number: 20120071483
    Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate cell stress response for treating said disease.
    Type: Application
    Filed: October 29, 2010
    Publication date: March 22, 2012
    Applicant: PHARNEXT
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko
  • Patent number: 8129407
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: March 6, 2012
    Assignee: Eisai Inc.
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Publication number: 20120046290
    Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: October 31, 2007
    Publication date: February 23, 2012
    Inventors: Jacques Dumas, Uday Khire, Timothy B. Lowinger, Holger Paulsen, Bernd Riedl, William J. Scott, Roger A. Smith, Jill Wood, Holia Hatoum-Mokdad, Wendy Lee, Aniko Redman, Jeffrey Johnson, Robert Sibley
  • Publication number: 20120015991
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: September 27, 2011
    Publication date: January 19, 2012
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard HUTCHINSON, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
  • Publication number: 20120010172
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 31, 2009
    Publication date: January 12, 2012
    Applicant: McDERMOTT WILL & EMERY LLP
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20120010184
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: September 21, 2011
    Publication date: January 12, 2012
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
  • Publication number: 20110301134
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: December 10, 2009
    Publication date: December 8, 2011
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
  • Publication number: 20110301211
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: December 15, 2009
    Publication date: December 8, 2011
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
  • Publication number: 20110301142
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: December 15, 2009
    Publication date: December 8, 2011
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr, Lucy Zhao
  • Publication number: 20110288131
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3 and R4 are as defined in claim 1; or a salt or oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: January 13, 2010
    Publication date: November 24, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Myriem El Qacemi, Thomas Pitterna, Jerome Yves Cassayre, Peter Renold