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).
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Publication number: 20240092818Abstract: The present invention relates to efficient synthetic processes useful in the preparation of antiviral nucleosides, particularly uridine 4-oxime 5?-(2-methylpropanoate) {(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]oxolan-2-yl}methyl 2-methylpropanoate and pharmaceutically acceptable salts, derivatives, tautomers, isomers, and prodrugs of, which may be active as antiviral agents, as well as compositions and methods thereof. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.Type: ApplicationFiled: December 17, 2021Publication date: March 21, 2024Applicant: Merck Sharp & Dohme LLCInventors: Tamas Benkovics, Patrick S. Fier, Anna Fryszkowska, Mark A. Huffman, Tetsuji Itoh, Jongrock Kong, Peter E. Maligres, Kevin M. Maloney, John McIntosh, Grant S. Murphy, Steven M. Silverman, Hao Yang
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Publication number: 20230287032Abstract: The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (O—{[(2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl}O,O-dihydrogen phosphorothioate, also known as 2?-(S)-fluoro-thio-adenosine monophosphate or 2?-F-thio-AMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.Type: ApplicationFiled: August 11, 2021Publication date: September 14, 2023Applicant: Merck Sharp & Dohme LLCInventors: Cheol Keun Chung, Zhijian Liu, Peter E. Maligres, Edna Mao, Jennifer V. Obligacion, Eric M. Phillips, Michael Pirnot, Marc Poirier, Zhiguo Jake Song, Tao Wang
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Patent number: 10308633Abstract: 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: GrantFiled: September 26, 2016Date of Patent: June 4, 2019Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme LimitedInventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
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Patent number: 10251903Abstract: 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: GrantFiled: October 20, 2015Date of Patent: April 9, 2019Assignees: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLCInventors: 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
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Patent number: 10214554Abstract: 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: GrantFiled: February 8, 2017Date of Patent: February 26, 2019Assignee: 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
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Publication number: 20180265493Abstract: 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: ApplicationFiled: September 26, 2016Publication date: September 20, 2018Applicants: 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
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Publication number: 20170246198Abstract: 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: ApplicationFiled: October 20, 2015Publication date: August 31, 2017Applicants: 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
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Publication number: 20170226146Abstract: 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: ApplicationFiled: February 8, 2017Publication date: August 10, 2017Inventors: 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
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Patent number: 9725464Abstract: 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: GrantFiled: October 24, 2014Date of Patent: August 8, 2017Assignee: 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
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Publication number: 20160257698Abstract: 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: ApplicationFiled: October 24, 2014Publication date: September 8, 2016Applicant: 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
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Patent number: 9145348Abstract: 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: GrantFiled: October 26, 2012Date of Patent: September 29, 2015Assignee: Merck Sharpe & Dohme Corp.Inventors: Cheol K. Chung, Guy R. Humphrey, Peter E. Maligres, Timothy J. Wright
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Publication number: 20140303380Abstract: 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: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Cheol K. Chung, Guy R. Humphey, Peter E. Maligres, Timothy J. Wright
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Patent number: 8686141Abstract: 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: GrantFiled: December 22, 2008Date of Patent: April 1, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Guy R. Humphrey, Ross A. Miller, Peter E. Maligres, Steven Weissman
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Publication number: 20130338141Abstract: 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: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Inventors: 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
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Patent number: 8513234Abstract: 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: GrantFiled: October 2, 2009Date of Patent: August 20, 2013Assignee: 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
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Publication number: 20100280244Abstract: 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: ApplicationFiled: December 22, 2008Publication date: November 4, 2010Inventors: Guy R. Humphrey, Ross A. Miller, Peter E. Maligres, Steven Weissman
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Publication number: 20100087419Abstract: 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: ApplicationFiled: October 2, 2009Publication date: April 8, 2010Inventors: 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
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Publication number: 20040030134Abstract: 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: ApplicationFiled: September 11, 2003Publication date: February 12, 2004Inventors: James Christopher McWilliams, Elizabeth Buck, Kan K. Eng, Guy R. Humphrey, Peter E. Maligres, Jess W. Sager, Marjorie See Waters
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Patent number: 6469172Abstract: 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: GrantFiled: March 5, 2001Date of Patent: October 22, 2002Assignee: Merck & Co., Inc.Inventors: Peter E. Maligres, Jaemoon Lee
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Publication number: 20010051727Abstract: 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: ApplicationFiled: March 5, 2001Publication date: December 13, 2001Inventors: Peter E. Maligres, Jaemoon Lee