Patents by Inventor Julian Golec

Julian 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).

  • Patent number: 7427681
    Abstract: This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; 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; and Ry, 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: February 10, 2004
    Date of Patent: September 23, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Françoise Pierard
  • Publication number: 20080070953
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? 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 interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Application
    Filed: September 18, 2007
    Publication date: March 20, 2008
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Bemis, Julian Golec, David Lauffer, Michael Mullican, Mark Murcko, David Livingston
  • Publication number: 20080039449
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? 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-?-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-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.
    Type: Application
    Filed: January 18, 2007
    Publication date: February 14, 2008
    Inventors: Mark Batchelor, David Bebbington, Guy Bemis, Wolf Fridman, Roger Gillespie, Julian Golec, David Lauffer, David Livingston, Saroop Matharu, Michael Mullican, Mark Murcko, Robert Murdoch, Robert Zelle
  • Publication number: 20070270444
    Abstract: This invention describes novel pyrazole compounds of formula IV: 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 independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 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: Application
    Filed: March 6, 2006
    Publication date: November 22, 2007
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
  • Publication number: 20070190634
    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: April 11, 2007
    Publication date: August 16, 2007
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • Publication number: 20070185125
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: August 25, 2006
    Publication date: August 9, 2007
    Inventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Julian Golec, Michael Mortimore
  • Publication number: 20070179133
    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: August 15, 2006
    Publication date: August 2, 2007
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Julian Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • Publication number: 20070173516
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: August 17, 2006
    Publication date: July 26, 2007
    Inventors: Michael Mortimore, Julian Golec
  • Publication number: 20070010457
    Abstract: The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-y inducing factor-(IGIF), interferon-?-(“IFN-?”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention.
    Type: Application
    Filed: September 14, 2006
    Publication date: January 11, 2007
    Inventors: Anita Diu-Hercend, Julian Golec, Thierry Hercend, Ronald Knegtel, Paul Lang, Andrew Miller, Karen Miller, Michael Mortimore, Peter Weber
  • Publication number: 20060258658
    Abstract: This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 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; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.
    Type: Application
    Filed: July 25, 2006
    Publication date: November 16, 2006
    Inventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian Golec, Pan Li, Jean-Damien Charrier
  • Patent number: 7008948
    Abstract: This invention describes novel pyrazole compounds of formula IV: 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 independently selected from T-R3, or taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5-8 membered ring having 1-3 ring heteroatoms selected from oxygen, sulfur, or nitrogen; and R2, R2?, T, and R3 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: July 22, 2003
    Date of Patent: March 7, 2006
    Assignee: Vertex Pharmaceuticals, Incorporated
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
  • Publication number: 20050143436
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? 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-?-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-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.
    Type: Application
    Filed: November 29, 2004
    Publication date: June 30, 2005
    Inventors: Mark Batchelor, David Bebbington, Guy Bemis, Wolf Fridman, Roger Gillespie, Julian Golec, David Lauffer, David Livingston, Saroop Matharu, Michael Mullican, Mark Murcko, Robert Murdoch, Robert Zelle
  • Publication number: 20050038023
    Abstract: This invention describes novel pyrazole compounds of formula IIIa: 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, Ry, 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: Application
    Filed: August 1, 2003
    Publication date: February 17, 2005
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
  • Publication number: 20050004110
    Abstract: This invention describes novel pyrazole compounds of formula III: 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, 5-8 membered carbocyclo ring; 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: Application
    Filed: September 14, 2001
    Publication date: January 6, 2005
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian Golec, Sanjay Patel, Jean- Damien Charrier, David Kay, Robert Davies
  • Publication number: 20040224944
    Abstract: This invention describes novel pyrazole compounds of formula IV: 1
    Type: Application
    Filed: July 22, 2003
    Publication date: November 11, 2004
    Inventors: David Bebbington, Hayley Binch, Ronald Knegtel, Julian Golec, Sanjay Patel, Jean-Damien Charrier, David Kay, Robert Davies, Pan Li, Marion Wannamaker, Cornelia Forster, Albert Pierce
  • Publication number: 20040214814
    Abstract: This invention describes novel pyrazole compounds of formula IIIc: 1
    Type: Application
    Filed: December 19, 2001
    Publication date: October 28, 2004
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Andrew Miller, Ronald Knegtel
  • Publication number: 20040167141
    Abstract: This invention describes novel pyrazole compounds of formula II: 1
    Type: Application
    Filed: February 10, 2004
    Publication date: August 26, 2004
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
  • Publication number: 20040097501
    Abstract: This invention describes novel triazole compounds of formula IX: 1
    Type: Application
    Filed: September 14, 2001
    Publication date: May 20, 2004
    Inventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian Golec, Pan Li, Jean-Damien Charier
  • Patent number: 6727251
    Abstract: This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; 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; and Ry, 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 20, 2001
    Date of Patent: April 27, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
  • Publication number: 20040048797
    Abstract: The present invention relates to methods for identifying compounds useful for regulating TNF-alpha levels and/or activity. The invention also relates to methods for decreasing TNF-alpha levels and/or activity. Compounds and compositions according to this invention are useful for treating TNF-mediated diseases. The invention also relates to kits comprising the compounds and compositions herein and a tool for measuring TNF-alpha activity and/or levels.
    Type: Application
    Filed: April 17, 2003
    Publication date: March 11, 2004
    Inventors: Karen Miller, Anita Diu-Hercend, Thierry Hercend, Paul Lang, Peter Weber, Julian Golec, Michael Mortimore