Patents by Inventor Kevin M. Belyk
Kevin M. Belyk 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: 20230174567Abstract: The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3?-fluoro-thio-guanosine monophosphate or 3?-F-thio-GMP. 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: May 20, 2021Publication date: June 8, 2023Applicant: Merck Sharp & Dohme LLCInventors: Travis Armiger, Kevin M. Belyk, Tamas Benkovics, Cheol K. Chung, Yining Ji Chen, Heather Claire Johnson, Artis Klapars, Zhijian Liu, Zhuqing Liu, Jeffrey C. Moore, Andrew J. Neel, Feng Peng, Stephan M. Rummelt, Nastaran Salehi Marzuarani, Benjamin D. Sherry, Zhiguo Jake Song, Ben William Hulme Turnbull, Lu Wang, Feng Xu
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Publication number: 20210154221Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula I and derivatives thereof.Type: ApplicationFiled: February 3, 2021Publication date: May 27, 2021Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme LimitedInventors: Mark McLaughlin, Edward Cleator, Jongrock Kong, Andrew William Gibson, David R. Lieberman, Alejandro Diequez Vazquez, Stephen Philip Keen, Michael J. Williams, Jeffrey C. Moore, Erika M. Milczek, Feng Peng, Kevin M. Belyk, Zhiguo Jake Song
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Patent number: 10815214Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.Type: GrantFiled: September 19, 2019Date of Patent: October 27, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Mark E. Scott, Paul G. Bulger, Kevin M. Belyk, John Limanto, Guy R. Humphrey
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Publication number: 20200010449Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.Type: ApplicationFiled: September 19, 2019Publication date: January 9, 2020Applicant: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Mark E. Scott, Paul G. Bulger, Kevin M. Belyk, John Limanto, Guy R. Humphrey
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Patent number: 10457690Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.Type: GrantFiled: June 3, 2016Date of Patent: October 29, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill
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Patent number: 10202401Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.Type: GrantFiled: November 9, 2017Date of Patent: February 12, 2019Assignees: MSD R&D CN CO., LTD, MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME LIMITEDInventors: Hongming Li, Jingjun Yin, Kevin M. Belyk, Kevin R. Campos, Qinghao Chen, Alan M. Hyde, Tetsuji Itoh, Artis Klapars, Matthew Thomas Tudge, Edward Cleator, Aaron M. Dumas, Louis-Charles Campeau, Yonggang Chen, Ji Qi, Wensong Xiao
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Publication number: 20190022115Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula (I) and derivatives thereof.Type: ApplicationFiled: September 16, 2016Publication date: January 24, 2019Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme LimitedInventors: Vinay M. Girijavallabhan, Mark McLaughlin, Edward Cleator, Jongrock Kong, Andrew William Gibson, David R. Lieberman, Alejandro Dieguez Vazquez, Stephen Philip Keen, Michael J. Williams, Jeffrey C. Moore, Erika M. Milczek, Feng Peng, Kevin M. Belyk, Zhiguo Jake Song
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Publication number: 20180179223Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.Type: ApplicationFiled: June 3, 2016Publication date: June 28, 2018Applicant: MERCK SHARP & DOHME CORP.Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill
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Publication number: 20180065985Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.Type: ApplicationFiled: November 9, 2017Publication date: March 8, 2018Applicants: Merck Sharpe & Dohme Corp., MSD R&D (China) Co., Ltd., Merck Sharp & Dohme LimitedInventors: Hongming Li, Jingjun Yin, Kevin M. Belyk, Kevin R. Campos, Qinghao Chen, Alan M. Hyde, Tetsuji Itoh, Artis Klapars, Matthew Thomas Tudge, Edward Cleator, Aaron M. Dumas, Louis-Charles Campeau, Yonggang Chen, Ji Qi, Wensong Xiao
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Patent number: 9890128Abstract: The present invention is directed to a process for making Substituted Quinazoline Compounds of formula (I): which are useful for the treatment and prophylaxis of HCMV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).Type: GrantFiled: December 8, 2014Date of Patent: February 13, 2018Assignees: MERCK SHARP & DOHME CORP., AICURIS ANTI-INFECTIVE CURES GMBHInventors: Michael Luzung, Guy Humphrey, Bangping Xiang, Kevin M. Belyk, Stephen Mark Dalby, Wilfried Schwab, Burkhard Klenke, Tom Moody, Gareth Brown
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Publication number: 20170166586Abstract: The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that are useful as synthetic intermediates in the process of the invention.Type: ApplicationFiled: July 10, 2015Publication date: June 15, 2017Inventors: Hongming Li, Jingjun Yin, Kevin M. Belyk, Kevin R. Campos, Qinghao Chen, Alan M. Hyde, Tetsuji Itoh, Artis Klapars, Matthew Thomas Tudge, Edward Cleator, Aaron M. Dumas, Louis-Charles Campeau, Yonggang Chen, Ji Qi, Wensong Xiao
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Patent number: 9487523Abstract: The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine, utilizing a highly effective spiroacid synthesis.Type: GrantFiled: March 13, 2013Date of Patent: November 8, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin M. Belyk, Edward Cleator, Shen-Chun Kuo, Peter Emmanuel Maligres, Bangping Xiang, Nobuyoshi Yasuda, Jianguo Yin
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Publication number: 20160311781Abstract: The present invention is directed to a process for making Substituted Quinazoline Compounds of formula (I): which are useful for the treatment and prophylaxis of HCMV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).Type: ApplicationFiled: December 8, 2014Publication date: October 27, 2016Inventors: Michael Luzung, Guy Humphrey, Bangping Xiang, Kevin M. Belyk, Stephen Mark Dalby, Wilfried Schwab, Burkhard Klenke, Tom Moody, Gareth Brown
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Patent number: 9139585Abstract: This invention relates to compounds of Formula I-VI having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: October 25, 2012Date of Patent: September 22, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Publication number: 20150038707Abstract: Methods for preventing pest infestations are disclosed. In some embodiments, the methods for preventing infestations involve use of pyrethroid insecticides or the stereoisomers or salts thereof.Type: ApplicationFiled: September 19, 2013Publication date: February 5, 2015Inventors: Kevin M. Belyk, Edward Cleator, Shen-Chun Kuo, Peter Emmanuel Maligres, Bangping Xiang, Nobuyoshi Yasuda, Jianguo Yin
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Publication number: 20140309213Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: October 16, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Patent number: 8357798Abstract: Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.Type: GrantFiled: June 4, 2010Date of Patent: January 22, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin M. Belyk, Henry G. Morrison, Philip Jones, Vincenzo Summa, V. Brett Cooper, Amar J. Mahajan, Daniel J. Kumke, Hsien-Hsin Tung, Lawrence Wai, Vanessa Pruzinsky, Philip Pye, Remy Angelaud, Danny Mancheno
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Patent number: 7754731Abstract: Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.Type: GrantFiled: December 2, 2005Date of Patent: July 13, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin M. Belyk, Henry G. Morrison, Amar J. Mahajan, Daniel J. Kumke, Hsien-Hsin Tung, Lawrence Wai, Vanessa Pruzinsky
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Patent number: 7214768Abstract: This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.Type: GrantFiled: April 8, 2002Date of Patent: May 8, 2007Assignee: Merck & Co., Inc.Inventors: Kevin M. Belyk, William R. Leonard
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Publication number: 20040158034Abstract: This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.Type: ApplicationFiled: October 10, 2003Publication date: August 12, 2004Inventors: Kevin M. Belyk, William R. Leonard