Publication number: 20140275058
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
Type:
Application
Filed:
March 6, 2014
Publication date:
September 18, 2014
Inventors:
Ana Elena MINATTI, Jonathan D. LOW, Jennifer R. ALLEN, Albert AMEGADZIE, James BROWN, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Patricia LOPEZ, Vu Van MA, Nobuko NISHIMURA, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Kelvin SHAM, Adrian L. SMITH, Ryan WHITE, Qiufen XUE
Publication number: 20140107109
Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
Type:
Application
Filed:
December 18, 2013
Publication date:
April 17, 2014
Inventors:
Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG