Search Patents
  • Beta-secretase modulators and methods of use
    Publication number: 20070185103
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: November 14, 2006
    Publication date: August 9, 2007
    Inventors: Brian Albrecht, Denise Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod Patel, Lewis Pennington, Matthew Weiss, Quifen Xue, Bryant Yang, Wenge Zhong
  • Beta-secretase modulators and methods of use
    Publication number: 20070173521
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, W, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: November 14, 2006
    Publication date: July 26, 2007
    Inventors: Qiufen Xue, Brian Albrecht, Denise Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod Patel, Lewis Pennington, Matthew Weiss, Bryant Yang, Wenge Zhong
  • Beta-secretase modulators and methods of use
    Patent number: 7745484
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: November 10, 2006
    Date of Patent: June 29, 2010
    Assignee: Amgen Inc.
    Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Dan Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang
  • Beta-secretase modulators and methods of use
    Publication number: 20070185144
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: November 10, 2006
    Publication date: August 9, 2007
    Applicant: Amgen Inc.
    Inventors: Wenge Zhong, Stephen Hitchcock, Brian Albrecht, Michael Bartberger, James Brown, Ryan Brown, Stuart Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang
  • Beta-Secretase modulators and methods of use
    Patent number: 7973047
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: July 5, 2011
    Assignee: Amgen Inc.
    Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
  • Beta-secretase modulators and methods of use
    Patent number: 8163766
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: April 24, 2012
    Assignee: Amgen Inc.
    Inventors: Wenge Zhong, Stephen A. Hitchcock, Vinod F. Patel, Yuan Cheng, Michael Croghan, Randall W. Hungate, Daniel La, Patricia Lopez, Matthew K. Kaller, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Lewis Pennington, Matthew Weiss, Ted Judd, Russell Graceffa, Qiufen Xue, Charles Kreiman, Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Scott Harried, Craig Masse, Bryant Yang
  • Beta-Secretase modulators and methods of use
    Patent number: 7872009
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: January 18, 2011
    Assignee: Amgen Inc.
    Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong
  • Beta-secretase modulators and methods of use
    Patent number: 7838676
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, W, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: November 23, 2010
    Assignee: Amgen Inc.
    Inventors: Qiufen Xue, Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Bryant Yang, Wenge Zhong
  • BETA-SECRETASE MODULATORS AND METHODS OF USE
    Publication number: 20100222338
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: May 13, 2010
    Publication date: September 2, 2010
    Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
  • PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL, PYRROLO[2,3-B]PYRIDINYL ACRYLAMIDES AND EPOXIDES THEREOF
    Publication number: 20190002466
    Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
    Type: Application
    Filed: April 19, 2016
    Publication date: January 3, 2019
    Applicant: Pfizer Inc.
    Inventors: Atli THORARENSEN, Matthew Frank BROWN, Agustin CASIMIRO-GARCIA, Ye CHE, Mark Edward FLANAGAN, Adam Matthew GILBERT, Matthew Merrill HAYWARD, Jean-Baptiste TELLIEZ, Rayomand Jal UNWALLA, John I. TRUJILLO, Sidney Xi LIANG
  • PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL AND PYRROLO[2,3-D]PYRIDINYL ACRYLAMIDES
    Publication number: 20170247372
    Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
    Type: Application
    Filed: March 1, 2017
    Publication date: August 31, 2017
    Applicant: Pfizer Inc.
    Inventors: Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo
  • PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL AND PYRROLO[2,3-D]PYRIDINYL ACRYLAMIDES
    Publication number: 20230009153
    Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
    Type: Application
    Filed: August 4, 2021
    Publication date: January 12, 2023
    Applicant: Pfizer Inc.
    Inventors: Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo
  • BETA-SECRETASE MODULATORS AND METHODS OF USE
    Publication number: 20110118250
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: October 21, 2010
    Publication date: May 19, 2011
    Applicant: Amgen Inc.
    Inventors: Brian K. Albrecht, Denise Lyn Andersen, Michael Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Stephen Hitchcock, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig Masse, Holger Monenschein, Thomas Nguyen, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Wenge Zhong
  • Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof
    Patent number: 10703756
    Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
    Type: Grant
    Filed: April 19, 2016
    Date of Patent: July 7, 2020
    Assignee: Pfizer Inc.
    Inventors: Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo, Sidney Xi Liang
  • Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
    Patent number: 9617258
    Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof, having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: April 11, 2017
    Assignee: Pfizer Inc.
    Inventors: Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo
  • Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
    Patent number: 11111242
    Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.
    Type: Grant
    Filed: March 1, 2017
    Date of Patent: September 7, 2021
    Assignee: Pfizer Inc.
    Inventors: Atli Thorarensen, Matthew Frank Brown, Agustin Casimiro-Garcia, Ye Che, Jotham Wadsworth Coe, Mark Edward Flanagan, Adam Matthew Gilbert, Matthew Merrill Hayward, Jonathan David Langille, Justin Ian Montgomery, Jean-Baptiste Telliez, Rayomand Jal Unwalla, John I. Trujillo
  • Novel phosphorus-containing derivatives
    Publication number: 20040127465
    Abstract: A compound of the Formula I 1
    Type: Application
    Filed: December 12, 2003
    Publication date: July 1, 2004
    Applicant: Pfizer Inc
    Inventors: Matthew F. Brown, Matthew M. Hayward
  • Novel piperazine derivatives
    Publication number: 20040034034
    Abstract: The present invention relates to compounds of the formula I 1
    Type: Application
    Filed: October 18, 2002
    Publication date: February 19, 2004
    Inventors: Laura C. Blumberg, Matthew F. Brown, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
  • Triazole furan compounds as agonists of the APJ receptor
    Patent number: 10736883
    Abstract: Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula (I) and Formula (II) have the following structures: (I); (II). Intermediates (V) are also claimed.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: August 11, 2020
    Assignee: AMGEN INC.
    Inventors: Matthew Brown, Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, James S. Harvey, Julie Anne Heath, Lars V. Heumann, Jonathan Houze, Frank Kayser, Aarif Yusuf Khakoo, David j. Kopecky, Su-Jen Lai, Zhihua Ma, Julio C. Medina, Jeffrey T. Mihalic, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Malgorzata Wanska, Wen-Chen Yeh
  • Methods of using piperazine derivatives
    Publication number: 20040092529
    Abstract: The present invention relates to compounds of the formula I 1
    Type: Application
    Filed: October 16, 2003
    Publication date: May 13, 2004
    Applicant: Pfizer Inc
    Inventors: Laura C. Blumberg, Matthew F. Brown, Anderson S. Gaweco, Ronald P. Gladue, Matthew M. Hayward, Gregory D. Lundquist, Christopher S. Poss, Andrei Shavnya
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