Patents by Inventor Julian M. C. Golec

Julian M. C. Golec 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).

  • Compositions useful as inhibitors of protein kinases
    Patent number: 6846928
    Abstract: The present invention relates to compounds useful as 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: March 14, 2003
    Date of Patent: January 25, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard, Albert C. Pierce
  • Carbamate caspase inhibitors and uses thereof
    Publication number: 20040053920
    Abstract: This invention provides caspase inhibitors of formula I: 1
    Type: Application
    Filed: August 21, 2003
    Publication date: March 18, 2004
    Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M.C. Golec
  • Inhibitors of interleukin 1-beta converting enzyme
    Publication number: 20040048855
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.
    Type: Application
    Filed: April 25, 2003
    Publication date: March 11, 2004
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Julian M .C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L.C. Robidoux, Marion W. Wannamaker
  • Carbamate caspase inhibitors and uses thereof
    Patent number: 6689784
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; secretion.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: February 10, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Ronald Knegtel, Michael Mortimore, David Kay, Julian M. C. Golec
  • Caspase inhibitor prodrugs
    Publication number: 20040019017
    Abstract: The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of caspase inhibitors from these compounds through selective bond cleavage. This invention further relates to pharmaceutical compositions comprising these compounds, which are particularly well-suited for treatment of caspase-mediated diseases, including inflammatory and degenerative diseases. This invention further relates to methods for preparing compounds of this invention.
    Type: Application
    Filed: February 11, 2003
    Publication date: January 29, 2004
    Inventors: Michael Mortimore, Julian M.C. Golec
  • Compositions useful as inhibitors of protein kinases
    Publication number: 20040009981
    Abstract: The present invention relates to compounds useful as 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 14, 2003
    Publication date: January 15, 2004
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • Indazole compounds useful as protein kinase inhibitors
    Publication number: 20040009968
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: January 23, 2003
    Publication date: January 15, 2004
    Inventors: Hayley Binch, Guy Brenchley, Julian M. C. Golec, Ronald Knegtel, Michael Mortimore, Sanjay Patel, Alistair Rutherford
  • Compositions useful as inhibitors of protein kinases
    Publication number: 20040009974
    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 14, 2003
    Publication date: January 15, 2004
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • Compositions useful as inhibitors of protein kinases
    Publication number: 20040002496
    Abstract: The present invention relates to compounds useful as 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 14, 2003
    Publication date: January 1, 2004
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M. C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • Caspase inhibitors and uses thereof
    Publication number: 20030232846
    Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors.
    Type: Application
    Filed: June 10, 2002
    Publication date: December 18, 2003
    Inventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
  • Compositions useful as inhibitors of protein kinases
    Publication number: 20030225073
    Abstract: The present invention relates to compounds useful as 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 14, 2003
    Publication date: December 4, 2003
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard, Albert C. Pierce
  • Inhibitors of interleukin-1beta converting enzyme
    Publication number: 20030225269
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are 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 ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.
    Type: Application
    Filed: January 28, 2002
    Publication date: December 4, 2003
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M.C. Golec, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Robert E. Zelle
  • Pyrazole compounds useful as protein kinase inhibitors
    Patent number: 6653301
    Abstract: This invention describes novel pyrazole compounds of formula IIa: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-7 membered ring having 0-3 heteroatoms; and R2 and R2 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: November 25, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M. C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
  • Caspase inhibitors and uses thereof
    Patent number: 6632962
    Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals. The compounds have the general formula I: wherein X is F or Cl; R1 is COOH, COO(alkyl), or an isostere thereof; and R2 is an aryl group.
    Type: Grant
    Filed: April 3, 2001
    Date of Patent: October 14, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Julian M. C. Golec, Paul Charifson, Guy Brenchley
  • Pyrazole compounds useful as protein kinase inhibitors
    Patent number: 6610677
    Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: wherein Z1 is N or C—R9, Z2 is N or CH, and Z3 is N or C—Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2′, R3, and R9 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2001
    Date of Patent: August 26, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Davies, Pan Li, Julian M. C. Golec, Jean-Damien Charrier, Ronald Knegtel, David Bebbington
  • Inhibitors of interleukin-1&bgr; converting enzyme
    Patent number: 6573259
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: June 3, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Julian M. C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L. C. Robidoux, Marion W. Wannamaker
  • Pyrazole compounds useful as protein kinase inhibitors
    Publication number: 20030078275
    Abstract: This invention describes novel pyrazole compounds of formula IIa: 1
    Type: Application
    Filed: December 19, 2001
    Publication date: April 24, 2003
    Inventors: David Bebbington, Jean-Damien Charrier, Robert Davies, Julian M.C. Golec, David Kay, Ronald Knegtel, Sanjay Patel
  • Inhibitors of interleukin-1beta converting enzyme
    Publication number: 20030069228
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;- (“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.
    Type: Application
    Filed: October 23, 2001
    Publication date: April 10, 2003
    Inventors: Julian M.C. Golec, David J. Lauffer, David J. Livingston, Michael D. Mullican, Mark A. Murcko, Philip L. Nyce, Andrea L.C. Robidoux, Marion W. Wannamaker
  • Imidazole and benzimidazole caspase inhibitors and uses thereof
    Publication number: 20020169177
    Abstract: This invention provides caspase inhibitors having the formula: 1
    Type: Application
    Filed: November 19, 2001
    Publication date: November 14, 2002
    Inventors: David Kay, Julian M.C. Golec
  • Caspase inhibitors and uses thereof
    Publication number: 20020132833
    Abstract: This invention provides novel compounds that are effective as inhibitors of caspase and cellular apoptosis. The invention also provides methods for using the compounds to treat caspase-mediated diseases in mammals.
    Type: Application
    Filed: April 3, 2001
    Publication date: September 19, 2002
    Inventors: Julian M.C. Golec, Paul Charifson, Guy Brenchley