- A practical synthesis of a γ-secretase inhibitor
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(Chemical Equation Presented) A practical and scaleable synthesis of the γ-secretase inhibitor 1 is reported. The inhibitor consists of a central trisubstituted cyclohexane core with appended propionic acid, 2,5-difluorophenyl, and 4-chlorophenylsulfonyl
- Scott, Jeremy P.,Lieberman, David R.,Beureux, Olivier M.,Brands, Karel M. J.,Davies, Antony J.,Gibson, Andrew W.,Hammond, Deborah C.,McWilliams, Chris J.,Stewart, Gavin W.,Wilson, Robert D.,Dolling, Ulf-H.
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p. 4149 - 4155
(2008/02/05)
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- HETEROCYCLIC METHYL SULFONE DERIVATIVE
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Provided is a compound capable of inhibiting production or secretion of β amyloid protein. A compound represented by the following formula (1): (wherein, R1 represents a heterocyclic group which may have a substituent, R2 represents a cyclic hydrocarbon group which may have a substituent or a heterocyclic group which may have a substituent, R3 represents a cyclic hydrocarbon group which may have a substituent or a heterocyclic group which may have a substituent, R4 represents a hydrogen atom or a C1-6 alkyl group, and X represents -S-,-SO- or -SO2-) an N-oxide or S-oxide thereof; a salt thereof; or a solvate thereof; and a medicament containing any of them.
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Page/Page column 15
(2010/11/08)
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- CYCLOHEXYL SULPHONES FOR TREATMENT OF CANCER
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Sulphones of formula (I) are disclosed for use in treatment of cancer.
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Page/Page column 25
(2010/11/25)
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- Aryl sulfones: A new class of γ-secretase inhibitors
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The development of a novel series of 4-aryl, 4-phenylsulfonyl cyclohexananone-derived γ-secretase inhibitors for the potential treatment of Alzheimer's disease is described.
- Teall, Martin,Oakley, Paul,Harrison, Timothy,Shaw, Duncan,Kay, Euan,Elliott, Jason,Gerhard, Ute,Castro, Jose L.,Shearman, Mark,Ball, Richard G.,Tsou, Nancy N.
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p. 2685 - 2688
(2007/10/03)
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- The new cyclohexylpropionic sulfone
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Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
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Page/Page column 12
(2008/06/13)
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- BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
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Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.
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- SYNTHESIS OF CYCLOHEXANONE DERIVATIVES
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A novel process for preparing cyclohexanones (1) is described. The products are useful as gamma-secretase inhibitors, or as intermediates in the synthesis of other gamma-secretase inhibitors.
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