Patents by Inventor George A. Moniz

George A. Moniz 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).

  • Crystalline FGFR4 inhibitor compound and uses thereof
    Patent number: 11498916
    Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-y1)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
    Type: Grant
    Filed: December 20, 2019
    Date of Patent: November 15, 2022
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: George Moniz, Kristen Sanders, Arani Chanda, Kenshi Yoshida, Ming-Hong Hao, Dominic Reynolds, Sudeep Prajapati, Anand Selvaraj, Takashi Satoh, John Wang
  • CRYSTALLINE FGFR4 INHIBITOR COMPOUND AND USES THEREOF
    Publication number: 20200317645
    Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-y1)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
    Type: Application
    Filed: December 20, 2019
    Publication date: October 8, 2020
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: George MONIZ, Kristen SANDERS, Arani CHANDA, Kenshi YOSHIDA
  • Crystalline FGFR4 inhibitor compound and uses thereof
    Patent number: 10562888
    Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
    Type: Grant
    Filed: April 13, 2016
    Date of Patent: February 18, 2020
    Assignee: Eisai R&D Management Co., LTD.
    Inventors: George Moniz, Kristen Sanders, Arani Chanda, Kenshi Yoshida
  • CRYSTALLINE FGFR4 INHIBITOR COMPOUND AND USES THEREOF
    Publication number: 20180093972
    Abstract: A number of crystalline forms of N-(2-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)-5-(4-ethylpiperazin-1-yl)phenyl)acrylamide are provided. These include a crystalline free base form, a crystalline monohydrochloride salt form, a crystalline dihydrochloride salt form, and a crystalline ethanesulfonate salt form. Methods of making and using crystalline compounds are also provided.
    Type: Application
    Filed: April 13, 2016
    Publication date: April 5, 2018
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: George MONIZ, Kristen SANDERS, Arani CHANDA, Kenshi YOSHIDA
  • Inhibitors of 11-?-hydroxy steroid dehydrogenase type 1
    Patent number: 8686011
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: April 1, 2014
    Assignees: Amgen Inc., Biovitrum AB
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
  • Process for making substituted 2-amino-thiazolones
    Patent number: 8541593
    Abstract: The present invention relates to methods of making compounds that inhibit 11-hydroxysteroid dehydrogenase type 1 enzyme (11-HSD1). One method comprises (a) contacting a compound of formula (II) sequentially with a chiral base in the presence of an amine, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I), wherein Z, R1, R2, and R3 are defined herein.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: September 24, 2013
    Assignee: Amgen Inc.
    Inventors: George A. Moniz, Matthew J. Frizzle, Charles Bernard, Michael Martinelli, Margaret M. Faul, Roger Nani, Jay Larrow
  • Inhibitors of 11-beta-hydroxysteroid dehydrogenase type 1
    Patent number: 8541592
    Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: September 24, 2013
    Assignees: Amgen Inc., Biovitrum AB
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle, Teresa L. Marshall
  • Process for making substituted 2-amino-thiazolones
    Patent number: 8536345
    Abstract: The present invention relates to methods of making compounds that inhibit 11-?-hydroxysteroid dehydrogenase type 1 enzyme (11-? HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I); wherein Z, R1, R2, and R3 are defined herein.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: September 17, 2013
    Assignee: Amgen Inc.
    Inventors: George A. Moniz, Matthew J. Frizzle, Charles Bernard, Michael Martinelli, Margaret Faul, Jay Larrow, Karl B. Hansen, Liane Klingensmith
  • INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1
    Publication number: 20120010256
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Application
    Filed: September 15, 2011
    Publication date: January 12, 2012
    Inventors: Martin HENRIKSSON, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, JR., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
  • PROCESS FOR PREPARING CERTAIN CINNAMIDE COMPOUNDS
    Publication number: 20110172427
    Abstract: This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12.
    Type: Application
    Filed: August 26, 2009
    Publication date: July 14, 2011
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Taiju Nakamura, Masaaki Matsuda, Yongbo Hu, Daiju Hasegawa, Yorihisa Hoshino, Kazato Inanaga, Minetaka Isomura, Nobuaki Sato, Kazuhiro Yoshizawa, George A. Moniz, Gordon D. Wilkie, Francis G. Fang, Yoshihiro Nishikawa
  • PROCESS FOR MAKING SUBSTITUTED 2-AMINO-THIAZOLONES
    Publication number: 20110160463
    Abstract: The present invention relates to methods of making compounds that inhibit 11-?-hydroxysteroid dehydrogenase type 1 enzyme (11-? HSD1). One method comprises (a) contacting a compound of formula (II) with a chiral base, deprotonating agent, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I); wherein Z, R1, R2, and R3 are defined herein.
    Type: Application
    Filed: June 16, 2009
    Publication date: June 30, 2011
    Inventors: George A. Moniz, Matthew J. Frizzle, Charles Bernard, Michael Martinelli, Margaret Faul, Jay Larrow, Karl B. Hansen, Liane Klingensmith
  • INHIBITORS OF 11-BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1
    Publication number: 20110082107
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Application
    Filed: October 5, 2010
    Publication date: April 7, 2011
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J.St. Jean, JR., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
  • PROCESS FOR MAKING SUBSTITUTED 2-AMINO-THIAZOLONES
    Publication number: 20100280255
    Abstract: The present invention relates to methods of making compounds that inhibit 11-hydroxysteroid dehydrogenase type 1 enzyme (11-HSD1). One method comprises (a) contacting a compound of formula (II) sequentially with a chiral base in the presence of an amine, and an alkylating agent R3-LG, (b) contacting the product of (a) with an acid to form a salt, and (c) reacting the salt with a base to form the compound of formula (I), wherein Z, R1, R2, and R3 are defined herein.
    Type: Application
    Filed: June 20, 2008
    Publication date: November 4, 2010
    Applicant: AMGEN INC.
    Inventors: George A. Moniz, Matthew J. Frizzle, Charles Bernard, Michael Martinelli, Margaret Faul, Roger Nani, Jay Larrow
  • Inhibitors of 11-?-hydroxy steroid dehydrogenase type 1
    Patent number: 7807700
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: October 5, 2010
    Assignee: Amgen Inc.
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
  • Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
    Publication number: 20080045503
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Application
    Filed: June 28, 2007
    Publication date: February 21, 2008
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric Bercot, Christopher Fotsch, Aiwen Li, Guolin Cai, Randall Hungate, Chester Yuan, Christopher Tegley, David St. Jean, Nianhe Han, Qi Huang, Qingyian Liu, Michael Bartberger, George Moniz, Matthew Frizzle
  • Inhibitors of 11-Beta-Hydroxy Steroid Dehydrogenase Type 1
    Publication number: 20070281938
    Abstract: The present invention relates to compounds with the formula (I) wherein R1, R2, R3, R4, and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Application
    Filed: May 24, 2005
    Publication date: December 6, 2007
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallagarda, Meredith Williams, Christopher Fostsch, Eric Bercot, Aiwen Li, Guolin Cai, Randall Hungate, Chester Yuan, Christopher Tegley, David St. Jean, Nianhe Han, Qi Huang, Qingyian Liu, Michael Bartberger, George Moniz, Matthew Frizzle
  • Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
    Publication number: 20070197598
    Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Application
    Filed: November 13, 2006
    Publication date: August 23, 2007
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric Bercot, Christopher Fotsch, Aiwen Li, Guolin Cai, Randall Hungate, Chester Yuan, Christopher Tegley, David Jean, Nianhe Han, Qi Huang, Qingyian Liu, Michael Bartberger, George Moniz, Matthew Frizzle, Teresa Marshall
  • Inhibitors of 11-?-hydroxy steroid dehydrogenase type 1
    Patent number: 7253196
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: August 7, 2007
    Assignees: Amgen, Inc., Biovitrum AB
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle
  • Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1
    Publication number: 20060142357
    Abstract: The present invention relates to compounds with the formula (I), (II), (III) or (IV): wherein R1, R2, R3, R4, R5, R6, R7, X and Z are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.
    Type: Application
    Filed: May 24, 2005
    Publication date: June 29, 2006
    Inventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric Bercot, Christopher Fotsch, Aiwen Li, Guolin Cai, Randall Hungate, Chester Yuan, Christopher Tegley, David Jean, Nianhe Han, Qi Huang, Qingyian Liu, Michael Bartberger, George Moniz, Matthew Frizzle