Patent number: 8557826
Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.
Type:
Grant
Filed:
October 6, 2010
Date of Patent:
October 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Andrew W. Stamford, Jared N Cumming
Patent number: 8557798
Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
Type:
Grant
Filed:
November 17, 2009
Date of Patent:
October 15, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
Patent number: 8551984
Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
Type:
Grant
Filed:
December 15, 2010
Date of Patent:
October 8, 2013
Assignees:
Merck Sharp & Dohme Corp., Merck Canada Inc.
Inventors:
Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
Patent number: 8541434
Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.
Type:
Grant
Filed:
August 19, 2009
Date of Patent:
September 24, 2013
Assignees:
Merck Sharp & Dohme Corp., Southern Research Institute
Inventors:
Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Ashok Arasappan, Frank Bennett, Jeremy Clark, Anita T. Fowler, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, John A. Secrist, III, Neng-Yang Shih
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