Patents by Inventor Peter E. Maligres

Peter E. Maligres 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: 10308633
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: June 4, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • Patent number: 10251903
    Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: October 20, 2015
    Date of Patent: April 9, 2019
    Assignees: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Bryon L. Simmons, Kevin R. Campos, Artis Klapars, Alistair J. Stewart, Benjamin A. Mayes, Peter E. Maligres, Alan Hyde, Steven Mark Silverman, Yong-Li Zhong, Adel M. Moussa, Kenneth Baker, Kara Van Valkenburg
  • Patent number: 10214554
    Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: February 26, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Amude Kassim, John Limanto, Michael Shevlin, Peter E. Maligres, Daniel A. DiRocco, James F. Dropinski, Rose Mathew, Yi Ning Ji Chen, Edward C. Sherer, Mikhail Reibarkh, Artis Klapars, Alan Hyde, Susan L. Zultanski, Aaron Moment, Bryon Simmons, Tyler A. Davis, Timothy James Wright, Ralph Calabria, Louis charles Campeau
  • Publication number: 20180265493
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Application
    Filed: September 26, 2016
    Publication date: September 20, 2018
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited.
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • Publication number: 20170246198
    Abstract: The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: October 20, 2015
    Publication date: August 31, 2017
    Applicants: IDENIX Pharmaceuticals LLC, Merck Sharp & Dohme Corp.
    Inventors: Bryon L. SIMMONS, Kevin R. CAMPOS, Artis KLAPARS, Alistair J. STEWART, Benjamin A. MAYES, Peter E. MALIGRES, Alan HYDE, Steven Mark SILVERMAN, Yong-Li ZHONG, Adel M. MOUSSA, Kenneth BAKER, Kara van VALKENBURG
  • Publication number: 20170226146
    Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: February 8, 2017
    Publication date: August 10, 2017
    Inventors: John Y.L. Chung, Amude Kassim, John Limanto, Michael Shevlin, Peter E. Maligres, Daniel A. DiRocco, James F. Dropinski, Rose Mathew, Yi Ning Ji Chen, Edward C. Sherer, Mikhail Reibarkh, Artis Klapars, Alan Hyde, Susan L. Zultanski, Aaron Moment, Bryon Simmons, Tyler A. Davis, Timothy James Wright, Ralph Calabria, Louis Charles Campeau
  • Patent number: 9725464
    Abstract: The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: August 8, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian Mangion, Cheng-yi Chen, Ingyu Jeon, Yonggang Chen, Hongmei Li, Hoa N. Nguyen, Peter E. Maligres, Artis Klapars, Ilia Zavialov, Nobuyoshi Yasuda
  • Publication number: 20160257698
    Abstract: The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
    Type: Application
    Filed: October 24, 2014
    Publication date: September 8, 2016
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Ian Mangion, Cheng-yi Chen, Ingyu Jeon, Yonggang Chen, Hongmei Li, Hoa N. Nguyen, Peter E. Maligres, Artis Klapars, Ilia Zavialov, Nobuyoshi Yasuda
  • Patent number: 9145348
    Abstract: An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: September 29, 2015
    Assignee: Merck Sharpe & Dohme Corp.
    Inventors: Cheol K. Chung, Guy R. Humphrey, Peter E. Maligres, Timothy J. Wright
  • Publication number: 20140303380
    Abstract: An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Cheol K. Chung, Guy R. Humphey, Peter E. Maligres, Timothy J. Wright
  • Patent number: 8686141
    Abstract: Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Guy R. Humphrey, Ross A. Miller, Peter E. Maligres, Steven Weissman
  • Publication number: 20130338141
    Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.
    Type: Application
    Filed: August 19, 2013
    Publication date: December 19, 2013
    Inventors: Richard C. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddes, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
  • Patent number: 8513234
    Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard C. A. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddess, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
  • Publication number: 20100280244
    Abstract: Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
    Type: Application
    Filed: December 22, 2008
    Publication date: November 4, 2010
    Inventors: Guy R. Humphrey, Ross A. Miller, Peter E. Maligres, Steven Weissman
  • Publication number: 20100087419
    Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.
    Type: Application
    Filed: October 2, 2009
    Publication date: April 8, 2010
    Inventors: Richard C. A. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddess, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
  • Publication number: 20040030134
    Abstract: A novel process is provided for the preparation of chiral intermediates useful in the asymmetric syntheses of &agr;v&bgr;3 integrin receptor antagonists. Also provided are the enantiomerically enriched intermediates that are obtained from the process.
    Type: Application
    Filed: September 11, 2003
    Publication date: February 12, 2004
    Inventors: James Christopher McWilliams, Elizabeth Buck, Kan K. Eng, Guy R. Humphrey, Peter E. Maligres, Jess W. Sager, Marjorie See Waters
  • Patent number: 6469172
    Abstract: An improved and efficient synthesis for the preparation of 2-amino-6-[(4-aminopiperidin-1-yl]methyl]pyridine, an intermediate compound in the preparation of muscarinic M3 receptor antagonists, includes as a final step the removal of trimethylacetyl and an amino protecting group from 2-trimethylacetyl-amino-6-[(4-protected aminopiperidin-1-yl)methyl]pyridine.
    Type: Grant
    Filed: March 5, 2001
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Peter E. Maligres, Jaemoon Lee
  • Publication number: 20010051727
    Abstract: An improved and efficient synthesis for the preparation of 2-amino-6-[(4-aminopiperidin-1-yl]methyl]pyridine, an intermediate compound in the preparation of muscarinic M3 receptor antagonists, includes as a final step the removal of trimethylacetyl and an amino protecting group from 2-trimethylacetyl-amino-6-[(4-protected aminopiperidin-1-yl)methyl]pyridine.
    Type: Application
    Filed: March 5, 2001
    Publication date: December 13, 2001
    Inventors: Peter E. Maligres, Jaemoon Lee
  • Patent number: 6239280
    Abstract: The present invention is directed to a process for synthesizing 1,5 disubstituted imidazoles with biaryl components of the formula (I): which are usefull as Farnesyl-Protein Transferase inhibitors.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: May 29, 2001
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Jennifer A. Cowen, Peter E. Maligres, J. Christopher McWilliams, Marjorie S. Waters
  • Patent number: 6140508
    Abstract: The present invention is directed to a process for synthesizing 1,5-disubstituted imidazoles, which are useful in the preparation of farnesyl-protein transferase inhibitors.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: October 31, 2000
    Assignee: Merck & Co., inc.
    Inventors: David Askin, Jennifer A. Cowen, Peter E. Maligres, J. Christopher McWilliams, Marjorie S. Waters