Patents by Inventor Ronald Knegtel

Ronald Knegtel 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).

  • Triazole compounds useful as protein kinase inhibitors
    Patent number: 7951820
    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: Grant
    Filed: July 25, 2006
    Date of Patent: May 31, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Ronald Knegtel, Hayley Binch, Julian M. C. Golec, Pan Li, Jean-Damien Charrier
  • CRYSTAL STRUCTURE OF AURORA-2 PROTEIN AND BINDING POCKETS THEREOF
    Publication number: 20110104782
    Abstract: The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data storage medium encoded with the structural coordinates of Aurora-2 binding pockets and methods of using a computer to evaluate the ability of a compound to bind to the molecule or molecular complex. This invention also provides methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention provides methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Aurora-2 or homologues thereof.
    Type: Application
    Filed: September 27, 2010
    Publication date: May 5, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Graham Cheetham, Ronald Knegtel, Lovorka Swenson, Joyce T. Coll, Suzanne Renwick, Peter Weber
  • COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20110086856
    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: December 14, 2010
    Publication date: April 14, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Juliam M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
  • KINASE INHIBITORS
    Publication number: 20110077237
    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: April 1, 2010
    Publication date: March 31, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Guy W. Bemis, Francois Maltais, Tiansheng Wang, Ronald Knegtel, Chris Davis, Damien Fraysse, Dean Boyall, Luca Settimo, Stephen Young, Michael Mortimore
  • Thiophene-carboxamides useful as inhibitors of protein kinases
    Patent number: 7915305
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase represented by formula (I): or a pharmaceutically acceptable salt thereof. 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: Grant
    Filed: January 23, 2007
    Date of Patent: March 29, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
  • TETRAHYDROPTERIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20110021519
    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: June 8, 2010
    Publication date: January 27, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
  • Compositions useful as inhibitors of protein kinases
    Patent number: 7863282
    Abstract: A compound of formula Ia: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 15, 2006
    Date of Patent: January 4, 2011
    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
  • Fused cyclic systems useful as inhibitors of TEC family protein kinases
    Patent number: 7855214
    Abstract: The present invention relates to compounds useful as inhibitors of Tec family protein kinases. These compounds have the general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, G, Cy1, and X are as defined herein. 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: January 26, 2005
    Date of Patent: December 21, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Sanjay Patel, David Kay, Ronald Knegtel, Oliver Philps
  • Thiophene-carboxamides useful as inhibitors of protein kinases
    Patent number: 7851495
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.
    Type: Grant
    Filed: May 22, 2007
    Date of Patent: December 14, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
  • Compounds useful as protein kinase inhibitors
    Patent number: 7838517
    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: Grant
    Filed: May 15, 2009
    Date of Patent: November 23, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
  • Thiophene-carboxamides useful as inhibitors of protein kinases
    Patent number: 7829590
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by structural formula I: or pharmaceutically acceptable salts thereof, wherein values of the variables of structural formula are as described in the specification and claims. The invention also provides pharmaceutically acceptable compositions comprising the compounds or salts, 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: Grant
    Filed: April 12, 2007
    Date of Patent: November 9, 2010
    Inventors: Guy Brenchley, Steven Durrant, Jean-Damien Charrier, Ronald Knegtel, Sharn Ramaya, Shazia Sadiq
  • COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20100280026
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: February 26, 2010
    Publication date: November 4, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Jeremy Green, Huai Gao, Young-Choon Moon, Guy Brenchley, Ronald Knegtel, Francoise Pierard
  • PYRAZOLE COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
    Publication number: 20100256170
    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: January 4, 2010
    Publication date: October 7, 2010
    Applicant: 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
  • Crystal structure of aurora-2 protein and binding pockets thereof
    Patent number: 7809541
    Abstract: The present invention provides crystalline molecules or molecular complexes which comprise binding pockets of Aurora-2 or its homologues. The invention also provides crystals comprising Aurora-2. The present invention also relates to a computer comprising a data storage medium encoded with the structural coordinates of Aurora-2 binding pockets and methods of using a computer to evaluate the ability of a compound to bind to the molecule or molecular complex. This invention also provides methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. In addition, this invention provides methods of using the structure coordinates to screen for and design compounds, including inhibitory compounds, that bind to Aurora-2 or homologues thereof.
    Type: Grant
    Filed: February 13, 2008
    Date of Patent: October 5, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Graham Cheetham, Ronald Knegtel, Lovorka Swenson, Joyce T. Coll, Suzanne Renwick, Peter Weber
  • Caspase inhibitors and uses thereof
    Patent number: 7807659
    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-? 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: Grant
    Filed: September 14, 2006
    Date of Patent: October 5, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anita Diu-Hercend, Julian Golec, Thierry Hercend, Ronald Knegtel, Paul Lang, Andrew Miller, Karen Miller, Michael Mortimore, Peter Weber
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    Publication number: 20100222318
    Abstract: The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: December 18, 2009
    Publication date: September 2, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean Damien Charrier, Steven Durrant, David Kay, Ronald Knegtel, Somhairle MacCormick, Michael Mortimore, Michael O'Donnell, Joanne Pinder, Alistair Rutherford, Anisa Nizarali Virani, Stephen Young, Philip Michael Reaper
  • Pyridones useful as inhibitors of kinases
    Patent number: 7786130
    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: Grant
    Filed: August 28, 2006
    Date of Patent: August 31, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Sharn Ramaya, Steven Durrant, Juan-Miguel Jimenez, Guy Brenchley, Ronald Knegtel, Michael Mortimore
  • 5-CYANO-4- (PYRROLO [2,3] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
    Publication number: 20100189773
    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: December 21, 2007
    Publication date: July 29, 2010
    Inventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
  • DIHYDRODIAZEPINES USEFUL AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20100190765
    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: September 29, 2009
    Publication date: July 29, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
  • Tetrahydropteridines useful as inhibitors of protein kinases
    Patent number: 7763629
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. 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: Grant
    Filed: April 12, 2007
    Date of Patent: July 27, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel