Patents Assigned to Merck Sharp & Dohme Limited
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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: 10472345Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.Type: GrantFiled: January 30, 2017Date of Patent: November 12, 2019Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme LimitedInventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Xu, Dongfang Meng
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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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Publication number: 20190055216Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.Type: ApplicationFiled: January 30, 2017Publication date: February 21, 2019Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME LIMITEDInventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Yu, Dongfang Meng
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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: 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: 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: 9242917Abstract: The present invention relates to different forms of a HCV inhibitory compound.Type: GrantFiled: August 16, 2012Date of Patent: January 26, 2016Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.Inventors: Gregory L Beutner, Robert M Wenslow, Jr., Eric J Choi, Clinton Scott Shultz, Jeremy Scott, Juan D Arredondo, Laura Artino
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Patent number: 9238571Abstract: The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.Type: GrantFiled: September 21, 2010Date of Patent: January 19, 2016Assignee: Merck Sharp & Dohme LimitedInventor: Robert Ward
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Patent number: 9108959Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.Type: GrantFiled: February 27, 2012Date of Patent: August 18, 2015Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme LimitedInventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
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Patent number: 9073825Abstract: A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)RA, or C(O)NHCH(X)COOH; provided that X is a C2-C6 alkyl, or a C3-C8 cycloalkyl and RA is a C1-6 alkyl or aryl; These compounds are used to make Compound AType: GrantFiled: August 16, 2012Date of Patent: July 7, 2015Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.Inventors: Nobuyoshi Yasuda, Jeffrey T. Kuethe, Guy Humphrey, Gregory L. Beutner, Yong-Li Zhong, Edward Cleator, Carl Baxter
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Patent number: 8674105Abstract: The instant invention relates to crystalline forms of Compound A, an inhibitor of c-MET kinase. Specifically, the instant invention relates to hydrochloride salts of Compound A.Type: GrantFiled: September 21, 2010Date of Patent: March 18, 2014Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.Inventors: Paolo Avalle, Minhua Chen
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IGF-1R specific antibodies useful in the detection and diagnosis of cellular proliferative disorders
Patent number: 8344112Abstract: The present invention relates to mammalian antibodies, designated 12B1 and antigen-binding portions thereof that specifically bind to insulin-like growth factor I receptor (IGF-IR), preferably human IGF-IR. Also included are chimeric, bispecific, derivatized, single chain antibodies derived from the antibodies disclosed herein. Nucleic acid molecules encoding the mammalian antibodies as well as methods of use thereof are also disclosed. Also included are pharmaceutical compositions comprising these antibodies and methods of using the antibodies and compositions thereof for treatment and diagnosis of pathological hyperproliferative oncogenic disorders associated with expression of IGF-1R.Type: GrantFiled: July 25, 2008Date of Patent: January 1, 2013Assignee: Merck Sharp & Dohme LimitedInventors: Liliane Goetsch, David Brooks, Michael Chastain, Zhi-Qiang Zhang, Nathalie Corvaia -
Patent number: 8242103Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.Type: GrantFiled: May 16, 2006Date of Patent: August 14, 2012Assignee: Merck Sharp & Dohme LimitedInventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
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Patent number: 8203004Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.Type: GrantFiled: November 3, 2006Date of Patent: June 19, 2012Assignee: Merck, Sharp & Dohme LimitedInventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Mciver, Paul Joseph Oakley, Martin Richard Teall
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Patent number: 7985758Abstract: Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.Type: GrantFiled: April 2, 2007Date of Patent: July 26, 2011Assignee: Merck, Sharp & Dohme LimitedInventors: Andrew Madin, Mark Peter Ridgill, Janusz Josef Kulagowski
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Publication number: 20110003862Abstract: Compounds of the formula (I), inhibit D-amino acid oxidase and hence find use in treating degenerative and psychiatric diseases.Type: ApplicationFiled: February 15, 2007Publication date: January 6, 2011Applicants: MERCK SHARP & DOHME LIMITED, MERCK & CO., INC.Inventors: Philip E. Brandish, Nicholas Brandon, Alister Campbell, Timothy Sparey
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Patent number: 7851638Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.Type: GrantFiled: October 1, 2009Date of Patent: December 14, 2010Assignee: Merck Sharp & Dohme LimitedInventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
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Patent number: 7825135Abstract: The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.Type: GrantFiled: March 23, 2005Date of Patent: November 2, 2010Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.Inventors: Wesley Blackaby, Mark E. Duggan, David Hallett, George D. Hartman, Andrew S. Jennings, William H. Leister, Richard T. Lewis, Craig W. Lindsley, Elizabeth Naylor, Leslie J. Street, Yi Wang, David D. Wisnoski, Scott E. Wolkenberg, Zhijian Zhao