Patents by Inventor Guy R. Humphrey
Guy R. Humphrey 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: 11584724Abstract: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.Type: GrantFiled: April 18, 2019Date of Patent: February 21, 2023Assignees: Merck Sharp & Dohme LLC, Werthenstein BioPharma GmbHInventors: Kevin M. Maloney, Kallol Basu, Michael James Di Maso, Guy R. Humphrey, Alfred Y. Lee, Feng Peng, Hong Ren, Siwei Zhang
-
Publication number: 20220242866Abstract: The present invention provides processes for the preparation of 2-fluoroadenine, as well as certain intermediates useful in the preparation of 2?-deoxy-4?-C-ethynyl-2-fluoroadenosine (EFdA): EFdA.Type: ApplicationFiled: June 18, 2020Publication date: August 4, 2022Applicant: Merck Sharp & Dohme Corp.Inventors: John Y.L. Chung, Cynthia Marilyn Hong, Guy R. Humphrey, Kevin M. Maloney, Yingju Xu, Richard J. Varsolona
-
Publication number: 20210122717Abstract: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.Type: ApplicationFiled: April 18, 2019Publication date: April 29, 2021Applicants: Merck Sharp & Dohme Corp., Werthenstein BioPharma GmbHInventors: Kevin M. Maloney, Kallol Basu, John Y.L. Chung, Richard Desmond, Michael James Di Maso, Guy R. Humphrey, Alfred Y. Lee, Dan Lehnherr, Feng Peng, Hong Ren, Mark Weisel, Siwei Zhang, Patrick Larpent
-
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
-
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
-
Patent number: 10435386Abstract: 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: January 30, 2017Date of Patent: October 8, 2019Assignee: MERCK SHARP & DOHME CORP.Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
-
Patent number: 10392353Abstract: Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.Type: GrantFiled: November 18, 2016Date of Patent: August 27, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Guy R. Humphrey, Zhijian Liu, Mark McLaughlin, Yingju Xu, Younong Yu
-
Publication number: 20180346429Abstract: Disclosed herein is a novel process for preparing substituted quinazoline compounds of formula (I) using a hydrogen bonding catalyst.Type: ApplicationFiled: November 18, 2016Publication date: December 6, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Guy R. Humphrey, Zhijian Liu, Mark McLaughlin, Yingju Xu, Younong Yu
-
Patent number: 9873707Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.Type: GrantFiled: October 14, 2014Date of Patent: January 23, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Feng Xu, Richard Desmond, Guy R. Humphrey, Hongming Li, Ji Qi, Rebecca T. Ruck, Zhiguo Jake Song, Tao Wang, Yong-Li Zhong, Jeonghan Park, Laura Marie Artino, Richard John Varsolona
-
Publication number: 20170137403Abstract: 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: January 30, 2017Publication date: May 18, 2017Applicant: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
-
Patent number: 9598397Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.Type: GrantFiled: December 2, 2014Date of Patent: March 21, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Yang Cao, Donald R. Gauthier, Jr., Guy R. Humphrey, Tetsuji Itoh, Michel Journet, Gang Qian, Benjamin D. Sherry, David M. Tschaen
-
Patent number: 9580407Abstract: 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: December 3, 2013Date of Patent: February 28, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
-
Publication number: 20160297794Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase and HIV replication, and the treatment of human immunodeficiency virus infection in humans.Type: ApplicationFiled: December 2, 2014Publication date: October 13, 2016Applicant: MERCK SHARP & DOHME CORP.Inventors: Yang Cao, Donald R. Gauthier, Jr., Guy R. Humphrey, Tetsuji Itoh, Michel Journet, Gang Qian, Benjamin D. Sherry, David M. Tschaen
-
Publication number: 20160251375Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.Type: ApplicationFiled: October 14, 2014Publication date: September 1, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Feng XU, Richard DESMOND, Guy R. HUMPHREY, Hongming LI, Ji QI, Rebecca T. RUCK, Zhiguo Jake SONG, Tao WANG, Yong-Li ZHONG, Jeonghan PARK, Laura Marie ARTINO, Richard John VARSOLONA
-
Publication number: 20150299167Abstract: 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: December 3, 2013Publication date: October 22, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
-
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
-
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
-
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
-
Patent number: 7576118Abstract: The present invention provides an asymmetric hydrogenation process for the preparation of chiral cycloalkanoindole DP receptor antagonists in high enantiomeric excess.Type: GrantFiled: April 1, 2005Date of Patent: August 18, 2009Assignee: Merck & Co., Inc.Inventors: David M. Tellers, Guy R. Humphrey
-
Patent number: 6750220Abstract: The tris(hydroxymethyl)aminomethane (“TRIS”) salt of 3-(pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid is a potent antagonist of the integrin &agr;v&bgr;3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions containing the salt and methods of using the salt.Type: GrantFiled: June 18, 2002Date of Patent: June 15, 2004Assignee: Merck & Co., Inc.Inventors: Guy R. Humphrey, Wei Xu