Patents by Inventor Michael R. Hale

Michael R. Hale 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).

  • Patent number: 7419967
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: August 25, 2005
    Date of Patent: September 2, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R Hale, Clarence W Andrews, III, Eric S Furfine, Ronald G Sherrill, Andrew Spaltenstein, Gregory T Lowen
  • Patent number: 7407962
    Abstract: The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.
    Type: Grant
    Filed: February 3, 2004
    Date of Patent: August 5, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, Michael R. Hale, Francois Maltais, Qing Tang
  • Patent number: 7354919
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein, kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: July 24, 2003
    Date of Patent: April 8, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, James W. Janetka, Francois Maltais, Jingrong Cao
  • Patent number: 7304071
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: or a pharmaceutically acceptable salt thereof, wherein Ring B, Z1, Z2, U, T, m, n, p, Q, Q?, R1, R2, Rx, R3, and R6 are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.
    Type: Grant
    Filed: August 12, 2003
    Date of Patent: December 4, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John Cochran, Jeremy Green, Michael R. Hale, Brian Ledford, Francois Maltais, Suganthini Nanthakumar
  • Patent number: 6962936
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where Ht, R2, T, and m are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: November 8, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Francois Maltais
  • Patent number: 6878728
    Abstract: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: April 12, 2005
    Assignee: Vertex Pharmaceutical Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger
  • Publication number: 20040220200
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 11, 2004
    Publication date: November 4, 2004
    Inventors: Francois Maltais, Alex Aronov, Michael R. Hale, Young-Choon Moon
  • Publication number: 20040214928
    Abstract: The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.
    Type: Application
    Filed: February 3, 2004
    Publication date: October 28, 2004
    Inventors: Alex Aronov, Michael R. Hale, Francois Maltais, Qing Tang
  • Publication number: 20040127488
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Application
    Filed: July 2, 2003
    Publication date: July 1, 2004
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, Francois Maltais, Clarence Webster Andrews, John Franklin Miller, Vicente Samano
  • Publication number: 20040122000
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Application
    Filed: October 21, 2003
    Publication date: June 24, 2004
    Applicant: Vertex Pharmaceuticals Incorporated.
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Publication number: 20040106615
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: 1
    Type: Application
    Filed: August 12, 2003
    Publication date: June 3, 2004
    Inventors: John Cochran, Jeremy Green, Michael R. Hale, Brian Ledford, Francois Maltais, Suganthini Nanthakumar
  • Patent number: 6706711
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases, such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: March 16, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Michael R. Hale
  • Patent number: 6617350
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: September 9, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald George Sherrill, Andrew Spaltenstein, Eric Steven Furfine, François Maltais, Clarence Webster Andrews, III, John Franklin Miller, Vicente Samano
  • Publication number: 20030158238
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: April 26, 2002
    Publication date: August 21, 2003
    Inventors: Michael R. Hale, Francois Maltais
  • Publication number: 20030144217
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Application
    Filed: August 21, 2002
    Publication date: July 31, 2003
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger D. Tung, Michael R. Hale, Christopher T. Baker, Andrew Spaltenstein, Eric S. Furfine, Istvan Kaldor, Wieslaw M. Kazmierski
  • Publication number: 20030134888
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: April 26, 2002
    Publication date: July 17, 2003
    Inventor: Michael R. Hale
  • Publication number: 20020198388
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Application
    Filed: August 9, 2001
    Publication date: December 26, 2002
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Christopher T. Baker, Timothy A. Stammers, Ronald G. Sherrill, Andrew Spaltenstein, Eric S. Furfine, Francois Maltais, Clarence W. Andrews, John F. Miller, Vicente Samano
  • Patent number: 6436989
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Grant
    Filed: December 24, 1997
    Date of Patent: August 20, 2002
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Michael R. Hale, Roger D. Tung, Christopher T. Baker, Andrew Spaltenstein
  • Patent number: D503222
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: March 22, 2005
    Inventor: Michael R. Hale
  • Patent number: D505193
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: May 17, 2005
    Inventor: Michael R. Hale