Patents by Inventor Michael Robin Hale

Michael Robin 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).

  • SULPHONAMIDE DERIVATIVES AS PRODRUGS OF ASPARTYL PROTEASE INHIBITORS
    Publication number: 20100124543
    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: July 16, 2009
    Publication date: May 20, 2010
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
    Patent number: 7592368
    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: October 4, 2004
    Date of Patent: September 22, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Prodrugs of an ERK protein kinase inhibitor
    Patent number: 7358258
    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: Grant
    Filed: May 13, 2005
    Date of Patent: April 15, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Robin Hale, Francois Maltais, Gabriel Martinez-Botella, Judith Straub, Qing Tang
  • Heterocyclic inhibitors of ERK2 and uses thereof
    Patent number: 7345054
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: March 18, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Robin Hale, Francois Maltais, Qing Tang, Judith Straub, Alexander Aronov
  • Heterocyclic inhibitors of ERK2 and uses thereof
    Patent number: 7304061
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: December 4, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Robin Hale, Francois Maltais, Qing Tang, Judith Straub, Alexander Aronov
  • Pyrazole-derived kinase inhibitors and uses thereof
    Patent number: 7279476
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: January 5, 2005
    Date of Patent: October 9, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Oing Tang, Francois Maltais, James Walter Janetka, Michael Robin Hale
  • Pyrazole-derived kinase inhibitors and uses thereof
    Patent number: 7183307
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: May 3, 2004
    Date of Patent: February 27, 2007
    Assignee: Vertex Pharmaceuticals Incroporated
    Inventors: Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
  • Heterocyclic inhibitors of ERK2 and uses thereof
    Publication number: 20050234059
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A1, A2, TmR1, X, R2, R3, R9, R12, and R13 are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.
    Type: Application
    Filed: March 10, 2005
    Publication date: October 20, 2005
    Inventors: Michael Robin Hale, Francois Maltais, Qing Tang, Judith Straub, Alexander Aronov
  • Pyrazole-derived kinase inhibitors and uses thereof
    Patent number: 6875789
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: April 5, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Qing Tang, Francois Maltais, James Walter Janetka, Michael Robin Hale
  • Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
    Patent number: 6838474
    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: February 19, 2003
    Date of Patent: January 4, 2005
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Pyrazole-derived kinase inhibitors and uses thereof
    Publication number: 20040209935
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: May 3, 2004
    Publication date: October 21, 2004
    Inventors: Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
  • Pyrazole-derived kinase inhibitors and uses thereof
    Patent number: 6750239
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: June 15, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
  • Sulfonamide inhibitors of aspartyl protease
    Publication number: 20040097594
    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: June 20, 2003
    Publication date: May 20, 2004
    Inventors: Michael Robin Hale, Clarence Webster Andrews, Eric Steven Furfine, Ronald George Sherrill, Andrew Spaltenstein, Gregory Thomas Lowen
  • Heterocyclic inhibitors of ERK2 and uses thereof
    Publication number: 20040029857
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: April 25, 2003
    Publication date: February 12, 2004
    Inventors: Michael Robin Hale, Francois Maltais, Qing Tang, Judith Straub, Alexander Aronov
  • Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
    Publication number: 20030207871
    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: February 19, 2003
    Publication date: November 6, 2003
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Sulfonamide inhibitors of aspartyl protease
    Patent number: 6613743
    Abstract: The present invention relates to a novel class of sulfonamides of formula I 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. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: September 2, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Robin Hale, Clarence Webster Andrews, III, Eric Steven Furfine, Ronald George Sherrill, Andrew Spaltenstein, Gregory Thomas Lowen
  • Pyrazole-derived kinase inhibitors and uses thereof
    Publication number: 20030144337
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: August 2, 2002
    Publication date: July 31, 2003
    Inventors: Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
  • Pyrazole-derived kinase inhibitors and uses thereof
    Publication number: 20030139452
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: August 2, 2002
    Publication date: July 24, 2003
    Inventors: Qing Tang, Francois Maltais, James Walter Janetka, Michael Robin Hale
  • Sulphonamide derivatives as prodrugs of aspartyl protease inhibitors
    Patent number: 6559137
    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: June 23, 2000
    Date of Patent: May 6, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Prodrugs of aspartyle protease inhibitors
    Publication number: 20020082249
    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: November 30, 2001
    Publication date: June 27, 2002
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Andrew Spaltenstein, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski