Patents Assigned to Merck Sharp & Dohme Limited
  • Patent number: 10472345
    Abstract: 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: Grant
    Filed: January 30, 2017
    Date of Patent: November 12, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Xu, Dongfang Meng
  • 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
  • Publication number: 20190055216
    Abstract: 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: Application
    Filed: January 30, 2017
    Publication date: February 21, 2019
    Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME LIMITED
    Inventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Yu, Dongfang Meng
  • Patent number: 10202401
    Abstract: 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: Grant
    Filed: November 9, 2017
    Date of Patent: February 12, 2019
    Assignees: MSD R&D CN CO., LTD, MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME LIMITED
    Inventors: 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
  • Publication number: 20190022115
    Abstract: 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: Application
    Filed: September 16, 2016
    Publication date: January 24, 2019
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: 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
  • 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: 20180065985
    Abstract: 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: Application
    Filed: November 9, 2017
    Publication date: March 8, 2018
    Applicants: Merck Sharpe & Dohme Corp., MSD R&D (China) Co., Ltd., Merck Sharp & Dohme Limited
    Inventors: 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
  • Patent number: 9242917
    Abstract: The present invention relates to different forms of a HCV inhibitory compound.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: January 26, 2016
    Assignees: 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
  • Patent number: 9238571
    Abstract: The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Robert Ward
  • Patent number: 9108959
    Abstract: 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: Grant
    Filed: February 27, 2012
    Date of Patent: August 18, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
  • Patent number: 9073825
    Abstract: 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 A
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: July 7, 2015
    Assignees: 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
  • Patent number: 8674105
    Abstract: 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: Grant
    Filed: September 21, 2010
    Date of Patent: March 18, 2014
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Paolo Avalle, Minhua Chen
  • Patent number: 8344112
    Abstract: 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: Grant
    Filed: July 25, 2008
    Date of Patent: January 1, 2013
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Liliane Goetsch, David Brooks, Michael Chastain, Zhi-Qiang Zhang, Nathalie Corvaia
  • Patent number: 8242103
    Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Patent number: 8203004
    Abstract: 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: Grant
    Filed: November 3, 2006
    Date of Patent: June 19, 2012
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Mciver, Paul Joseph Oakley, Martin Richard Teall
  • Patent number: 7985758
    Abstract: 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: Grant
    Filed: April 2, 2007
    Date of Patent: July 26, 2011
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: Andrew Madin, Mark Peter Ridgill, Janusz Josef Kulagowski
  • Publication number: 20110003862
    Abstract: Compounds of the formula (I), inhibit D-amino acid oxidase and hence find use in treating degenerative and psychiatric diseases.
    Type: Application
    Filed: February 15, 2007
    Publication date: January 6, 2011
    Applicants: MERCK SHARP & DOHME LIMITED, MERCK & CO., INC.
    Inventors: Philip E. Brandish, Nicholas Brandon, Alister Campbell, Timothy Sparey
  • Patent number: 7851638
    Abstract: 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: Grant
    Filed: October 1, 2009
    Date of Patent: December 14, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
  • Patent number: 7825135
    Abstract: 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: Grant
    Filed: March 23, 2005
    Date of Patent: November 2, 2010
    Assignees: 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
  • Patent number: 7759492
    Abstract: An enantioselective route to compounds of formula I is disclosed: The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: July 20, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Stephen Philip Keen, Steven Fraser Oliver, Gavin William Stewart