Patents by Inventor John Stellwagen

John Stellwagen 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: 11807634
    Abstract: The present invention provides a compound of Formula (I): an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular NaV1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.
    Type: Grant
    Filed: June 10, 2021
    Date of Patent: November 7, 2023
    Assignee: AMGEN INC.
    Inventors: Benjamin C Milgram, Isaac E Marx, John Stellwagen, Wei Zhao, Alan H. Cherney
  • Publication number: 20230234948
    Abstract: The present invention provides a compound of Formula (I): (I); an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular NaV1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.
    Type: Application
    Filed: June 10, 2021
    Publication date: July 27, 2023
    Applicant: AMGEN INC.
    Inventors: BENJAMIN C. MILGRAM, ISSAC E. MARX, JOHN STELLWAGEN, WEI ZHAO, ALAN H. CHERNEY
  • Patent number: 11332459
    Abstract: The present invention relates to inhibitors of Transient Receptor Potential Channel 6 (TRPC6) protein activity. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: May 17, 2022
    Assignee: TEIJIN PHARMA LIMITED
    Inventors: Michael D. Bartberger, Nagasree Chakka, Hua Gao, Angel Guzman-Perez, Daniel B. Horne, Zihao Hua, Madeleine Kieffer, Daniel C. H. Lin, Benjamin Charles Milgram, Jane Panteleev, Laurie Schenkel, John Stellwagen, Matthew Weiss, Ryan D. White, Wei Zhao
  • Publication number: 20210387977
    Abstract: The present invention provides a compound of Formula (I): an enantiomer, diastereoisomer, atropisomer thereof, a mixture thereof, or a pharmaceutically acceptable salt thereof, that inhibits voltage-gated sodium channels, in particular NaV1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders, cough, and itch. Also provided are pharmaceutical compositions containing the compounds of the present invention. Also further provided is an atropi-selective preparation of said compounds of Formula (I), and intermediate thereof.
    Type: Application
    Filed: June 10, 2021
    Publication date: December 16, 2021
    Applicant: AMGEN INC.
    Inventors: BENJAMIN C. MILGRAM, Isaac E. MARX, John STELLWAGEN, Wei ZHAO, Alan H. CHERNEY
  • Publication number: 20200308145
    Abstract: The present invention relates to inhibitors of Transient Receptor Potential Channel 6 (TRPC6) protein activity. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
    Type: Application
    Filed: October 18, 2018
    Publication date: October 1, 2020
    Applicant: Amgen Inc.
    Inventors: Michael D. BARTBERGER, Nagasree CHAKKA, Hua GAO, Angel GUZMAN-PEREZ, Daniel B. HORNE, Zihao HUA, Madeleine KIEFFER, Daniel C. H. Lin, Benjamin Charles MILGRAM, Jane PANTELEEV, Laurie SCHENKEL, John STELLWAGEN, Matthew WEISS, Ryan D. WHITE, Wei ZHAO
  • Patent number: 10472356
    Abstract: The present invention provides compounds of Formula (I), wherein: as defined in the specification, an enantiomer, diastereomer, atropisomer thereof, or a mixture thereof, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: November 12, 2019
    Assignee: AMGEN INC.
    Inventors: Matthew Weiss, Benjamin Charles Milgram, Thomas Dineen, John Stellwagen, Angel Guzman-Perez, Alessandro Boezio, Issac E. Marx
  • Publication number: 20180051021
    Abstract: The present invention provides compounds of Formula (I), wherein: as defined in the specification, an enantiomer, diastereomer, atropisomer thereof, or a mixture thereof, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 2, 2016
    Publication date: February 22, 2018
    Applicant: AMGEN INC.
    Inventors: Matthew WEISS, Benjamin Charles MILGRAM, Thomas DINEEN, John STELLWAGEN, Angel GUZMAN-PEREZ, Alessandro BOEZIO, Issac E. MARX
  • Patent number: 9556135
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
    Type: Grant
    Filed: October 10, 2013
    Date of Patent: January 31, 2017
    Assignee: Amgen, Inc.
    Inventors: Richard T. Lewis, Jennifer R. Allen, Yuan Cheng, Deborah Choquette, Oleg Epstein, Angel Guzman-Perez, Paul E. Harrington, Zihao Hua, Randall W. Hungate, Jason Brooks Human, Ted Judd, Qingyian Liu, Patricia Lopez, Ana Elena Minatti, Philip Olivieri, Karina Romero, Shannon Rumfelt, Robert M. Rzasa, Laurie Schenkel, John Stellwagen, Ryan White, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
  • Patent number: 9309263
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: April 12, 2016
    Assignee: Amgen Inc.
    Inventors: Ryan White, Jennifer R. Allen, Oleg Epstein, Fang-Tsao Hong, Zihao Hua, Jason Brooks Human, Patricia Lopez, Philip R. Olivieri, Karina Romero, Laurie Schenkel, John Stellwagen, Nuria A. Tamayo, Xiao Mei Zheng
  • Publication number: 20150259308
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
    Type: Application
    Filed: October 10, 2013
    Publication date: September 17, 2015
    Applicant: AMGEN INC.
    Inventors: Richard T. Lewis, Jennifer R. Allen, Yuan Cheng, Deborah Choquette, Oleg Epstein, Angel Guzman-Perez, Paul E. Harrington, Zihao Hua, Randall W. Hungate, Jason Brooks Human, Ted Judd, Qingyian Liu, Patricia Lopez, Ana Elena Minatti, Philip Olivieri, Karina Romero, Shannon Rumfelt, Robert M. Rzasa, Laurie Schenkel, John Stellwagen, Ryan White, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
  • Publication number: 20150252059
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Application
    Filed: May 20, 2015
    Publication date: September 10, 2015
    Inventors: Richard T. LEWIS, Jennifer R. ALLEN, James BROWN, Angel GUZMAN-PEREZ, Zihao HUA, Ted JUDD, Qingyian LIU, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE
  • Patent number: 9096615
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: August 4, 2015
    Assignee: AMGEN INC.
    Inventors: Richard T. Lewis, Jennifer R. Allen, James Brown, Angel Guzman-Perez, Zihao Hua, Ted Judd, Qingyian Liu, Philip R. Olivieri, Karina Romero, Laurie Schenkel, John Stellwagen, Ryan White
  • Publication number: 20150038497
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Application
    Filed: July 29, 2014
    Publication date: February 5, 2015
    Inventors: Richard T. LEWIS, Jennifer R. ALLEN, James BROWN, Angel GUZMAN-PEREZ, Zihao HUA, Ted JUDD, Qingyian LIU, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE
  • Publication number: 20140213581
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A5, A6, A8, R1, R2, R3, R7, X, Y, n and o of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, compounds of Formula III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III, and sub-Formulas thereof.
    Type: Application
    Filed: January 28, 2014
    Publication date: July 31, 2014
    Inventors: Ryan WHITE, Jennifer R. ALLEN, Oleg EPSTEIN, Fang-Tsao HONG, Zihao HUA, Jason Brooks HUMAN, Patricia LOPEZ, Philip R. OLIVIERI, Karina ROMERO, Laurie SCHENKEL, John STELLWAGEN, Nuria A. TAMAYO, Xiao Mei ZHENG
  • Publication number: 20140107109
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Inventors: Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG
  • Publication number: 20140080851
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: November 25, 2013
    Publication date: March 20, 2014
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: GEORGE ADJABENG, JERRY LEROY ADAMS, SCOTT HOWARD DICKERSON, KEITH HORNBERGER, NEIL W. JOHNSON, KEVIN KUNTZ, KIMBERLY PETROV, JEFFREY M. RALPH, TARA RENAE RHEAULT, GREGORY SCHAAF, JOHN STELLWAGEN, XINRONG TIAN, DAVID E. UEHLING, ALEX G. WATERSON, BRIAN WILSON
  • Publication number: 20130144055
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: January 31, 2013
    Publication date: June 6, 2013
    Applicant: GlaxoSmithKline LLC
    Inventors: George Adjabeng, Jerry Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
  • Patent number: 8415345
    Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: April 9, 2013
    Assignee: Glaxo SmithKline LLC
    Inventors: George Adjabeng, Jerry Leroy Adams, Scott Howard Dickerson, Keith Hornberger, Neil W. Johnson, Kevin Kuntz, Kimberly Petrov, Jeffrey M. Ralph, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, Xinrong Tian, David E. Uehling, Alex G. Waterson, Brian Wilson
  • Publication number: 20120190666
    Abstract: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3K? kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3K?, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: May 12, 2010
    Publication date: July 26, 2012
    Applicant: Amgen Inc.
    Inventors: Christiane Bode, Alessandro Boezio, Alan C. Cheng, Deborah Choquette, James Robert Coats, Katrina Woodin Copeland, Hongbing Huang, Daniel La, Richard Thomas Lewis, Hongyu Liao, Michele Potashman, John Stellwagen, Shuyan Yi, Mark H. Norman, Markian M. Stec, Emily Anne Peterson, Russell Graceffa
  • Publication number: 20110190280
    Abstract: The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
    Type: Application
    Filed: August 27, 2008
    Publication date: August 4, 2011
    Inventors: George Adjabeng, Neil Bifulco, Ronda G. Davis-Ward, Scott Howard Dickerson, Kelly Horne Donaldson, Philip Anthony Harris, Keith Hornberger, Kimberly Petrov, Tara Renae Rheault, Gregory Schaaf, John Stellwagen, David Edward Uehling, Alex Gregory Waterson