Patents by Inventor Ralph P. Robinson

Ralph P. Robinson has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20240174637
    Abstract: Provided herein are compounds (e.g., compounds of Formulae (A-I), (B-I), (C-I)), and pharmaceutically acceptable salts, stereoisomers, tautomers, isotopically labeled derivatives, solvates, hydrates, polymorphs, co-crystals, and prodrugs thereof, pharmaceutical compositions thereof, and kits comprising the same. The compounds provided herein are degraders of GRK2 proteins and are therefore useful for, e.g., treating and/or preventing diseases (e.g., cancer) in a subject, for inhibiting tumor growth in a subject, for inhibiting the activity of GRK2 and/or degrading a GRK2 protein in vitro or in vivo, etc. In certain embodiments, the compounds provided herein are selective for GRK2. Also provided herein are methods and synthetic intermediates useful in the preparation of compounds described herein.
    Type: Application
    Filed: January 21, 2022
    Publication date: May 30, 2024
    Inventors: Grazia Piizzi, Eugene L. Piatnitski Chekler, Jonathan Barry Hurov, Alexandra Lantermann, Kiley Marie Couto, Hua Xu, Sourav Sarkar, Bruce Allen Lefker, Ralph P. Robinson, Volodymyr Kysil
  • Patent number: 8635860
    Abstract: A system for reversing heat transfer from an exhaust system assembly on a vehicle comprising an engine block assembly and transaxle assembly operatively connected and located in an engine compartment of an automobile. The system comprises a number one exhaust manifold stay mount, a number two exhaust manifold stay mount, and a front exhaust collector pipe bracket and stay mount. The system comprises an exhaust system with a front exhaust collector pipe located beneath the engine block assembly. The system comprises an engine block assembly heat shield with a cross-section generally comprising the shape of a “U” that is located next to the surface of the engine block assembly. The engine block assembly heat shield is located over and overlays the front exhaust collector pipe bracket and stay mount, the number one exhaust manifold stay mount, and the number two exhaust manifold stay mount.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: January 28, 2014
    Inventor: Ralph P. Robinson
  • Publication number: 20130072427
    Abstract: Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: July 22, 2010
    Publication date: March 21, 2013
    Inventors: Cristiano Guimaraes, Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Publication number: 20120295845
    Abstract: Compounds of formula (I) wherein: X is (A) or (B); Y is O or a bond; R1 is —C(O)—O—R3 or R2 is hydrogen, cyano, C1-C6 alkyl, or C3-C6 cycloalkyl; R5 is hydrogen, cyano, nitro, C1-C6 fluoroalkyl, C1-C6 alkyl, C1-C6 alkoxy, fluoroalkoxy, or C3-C6 cycloalkyl; R6 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, —C(O)—NH2, or C1-C6 alkyl substituted with hydroxy or C1-C6 alkoxy; m is 1 or 2, wherein when m is 1 then R8 is hydrogen, C1-C6 alkyl, —CH2—(C1-C5)haloalkyl, C3-C6 cycloalkyl, or C1-C6 alkyl substituted with hydroxy; and when m is 2 then each R8 is independently C1-C3 alkyl or —CH2—(C1—C2)haloalkyl; modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: November 16, 2010
    Publication date: November 22, 2012
    Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Publication number: 20110020460
    Abstract: Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: June 4, 2010
    Publication date: January 27, 2011
    Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Publication number: 20100285145
    Abstract: Compounds of Formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: May 6, 2010
    Publication date: November 11, 2010
    Inventors: Etzer Darout, Michael P. DeNinno, Kentaro Futatsugi, Cristiano Guimaraes, Bruce A. Lefker, Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Patent number: 7553877
    Abstract: The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1—R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: June 30, 2009
    Assignee: Pfizer, Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Patent number: 7468378
    Abstract: This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1—R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.
    Type: Grant
    Filed: February 3, 2005
    Date of Patent: December 23, 2008
    Assignee: Pfizer Inc.
    Inventors: Peter Bertinato, Michel A. Couturier, Ernest S. Hamanaka, Marcus D. Ewing, Ralph P. Robinson, Derek L. Tickner
  • Patent number: 7393958
    Abstract: This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: July 1, 2008
    Assignee: Pfizer, Inc.
    Inventors: Peter Bertinato, Michel A. Couturier, Ernest S. Hamanaka, Marcus D. Ewing, Ralph P. Robinson, Derek L. Tickner
  • Patent number: 7368573
    Abstract: This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R1-R7, X1, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: May 6, 2008
    Assignee: Pfizer Inc.
    Inventors: Peter Bertinato, Michel A. Couturier, Ernest S. Hamanaka, Marcus D. Ewing, Ralph P. Robinson, Derek L. Tickner
  • Patent number: 7138406
    Abstract: The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1–R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: November 21, 2006
    Assignees: Pfizer, Inc., Pfizer Products, Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Patent number: 6852719
    Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below.
    Type: Grant
    Filed: October 26, 2001
    Date of Patent: February 8, 2005
    Assignees: Pfizer Inc., Pfizer Products, Inc.
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Publication number: 20040138262
    Abstract: The present invention provides compounds of the formula 1
    Type: Application
    Filed: July 8, 2003
    Publication date: July 15, 2004
    Applicant: Pfizer Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Publication number: 20040014741
    Abstract: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
    Type: Application
    Filed: October 26, 2001
    Publication date: January 22, 2004
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Publication number: 20020147224
    Abstract: The present invention relates to a compound of the formula 1
    Type: Application
    Filed: April 5, 2002
    Publication date: October 10, 2002
    Inventors: Ralph P. Robinson, Ellen R. Laird
  • Patent number: 6458822
    Abstract: The present invention relates to a compound of the formula wherein R1, R2, R3 and R4 are as defined above, and pharmaceutically acceptable salts and solvates thereof, that are useful, for example, as matrix metalloproteinase inhibitors. The present invention is also directed to pharmaceutical compositions comprising such compounds and methods of treatment for diseases such as osteoarthritis, rheumatoid arthritis, cancer, osteoporosis, tissue ulceration, restinosis, periodontal disease, inflammation, epidermolysis bullosa, scleritis, stroke, Alzheimer's disease, and the like, characterized by inappropriate matrix metalloproteinase activity. Processes for the synthesis of compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: December 5, 2000
    Date of Patent: October 1, 2002
    Assignee: Pfizer Inc.
    Inventors: Ralph P. Robinson, Ellen R. Laird
  • Publication number: 20020107235
    Abstract: The present invention provides non-steroidal compounds of Formula I, and prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds.
    Type: Application
    Filed: October 26, 2001
    Publication date: August 8, 2002
    Inventors: Kevin K. Liu, Bradley P. Morgan, Ralph P. Robinson
  • Patent number: 6380219
    Abstract: A compound of the formula wherein n, X, R3, R4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: April 30, 2002
    Assignee: Pfizer Inc
    Inventors: Ralph P. Robinson, James P. Rizzi
  • Publication number: 20010041710
    Abstract: The present invention relates to a compound of the formula 1
    Type: Application
    Filed: December 5, 2000
    Publication date: November 15, 2001
    Inventors: Ralph P. Robinson, Ellen R. Laird
  • Patent number: 6214870
    Abstract: The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.
    Type: Grant
    Filed: March 28, 2000
    Date of Patent: April 10, 2001
    Assignee: Pfizer Inc
    Inventors: Kim F. McClure, Ralph P. Robinson