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.
Inventors:
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
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.
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.
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.
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.
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
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.
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
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.
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.
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
Abstract: The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
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.
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
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.
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
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
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
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
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.
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