Fluorinated piperidine acetic acids as γ-secretase modulators
We report herein a novel series of difluoropiperidine acetic acids as modulators of γ-secretase. Synthesis of 2-aryl-3,3-difluoropiperidine analogs was facilitated by a unique and selective β-difluorination with Selectfluor. Compounds 1f and 2c were selec
Stanton, Matthew G.,Hubbs, Jed,Sloman, David,Hamblett, Christopher,Andrade, Paula,Angagaw, Minilik,Bi, Grace,Black, Regina M.,Crispino, Jamie,Cruz, Jonathan C.,Fan, Eric,Farris, Georgia,Hughes, Bethany L.,Kenific, Candia M.,Middleton, Richard E.,Nikov, George,Sajonz, Peter,Shah, Sanjiv,Shomer, Nirah,Szewczak, Alexander A.,Tanga, Flobert,Tudge, Matthew T.,Shearman, Mark,Munoz, Benito
scheme or table
p. 755 - 758
(2010/05/19)
SILYLATED PIPERIDINE DERIVATIVES
Compounds of formula I: I wherein at least one of R4 and R5 comprises Si(R6)3 as a substituent selectively attenuate production of A?(1-42) and hence find use in treatment of Alzheimer's disease and related conditions.
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Page/Page column 22
(2008/12/07)
DIFLUORINATED PIPERIDINES FOR TREATMENT OF ALZHEIMER'S DISEASE AND RELATED CONDITIONS
Compounds of formula (I). Selectively inhibit production of Aβ(1-42) and hence find use in treatment of diseases associated with deposition of β-amyloid in the brain.
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Page/Page column 21-22
(2008/06/13)
Synthesis of C2-symmetric trans-2,6-diarylpiperidinones via aryl cuprate addition: an unexpected stereochemical outcome
An efficient procedure for the preparation of trans-2,6-diaryl piperidinones has been developed. Addition of aryl Grignard reagents to 2-aryl dihydropyridones under catalytic copper promoted conditions generates the trans isomer exclusively, an unprecedented stereochemical event. The X-ray structures of both starting material and product have been solved and shed light on the steric constraints and substrate geometry leading to the observed product. The reaction conditions tolerate a variety of aromatic nucleophiles to generate C2-symmetric products in good overall yields.
Hamblett, Christopher L.,Sloman, David L.,Kliman, Laura T.,Adams, Bruce,Ball, Richard G.,Stanton, Matthew G.
p. 2079 - 2082
(2008/02/04)
PIPERIDINE DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE
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.
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Page/Page column 21-22
(2008/06/13)
PIPERIDINES AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER’S DISEASE
Compounds of formula (I) are modulators of gamma-secretase, and hence are useful in treatment of Alzheimer’s disease.
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Page/Page column 26-27
(2008/06/13)
PIPERIDINES AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER'S DISEASE
Compounds of formula (I), selectively inhibit production of Aβ (1-42) and hence are useful in treatment or prevention of disease assocaited with deposition of β -amyloid in the brain.
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Page/Page column 91
(2010/11/08)
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