JP2010520276A5 - - Google Patents

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Publication number

JP2010520276A5

JP2010520276A5 JP2009552641A JP2009552641A JP2010520276A5 JP 2010520276 A5 JP2010520276 A5 JP 2010520276A5 JP 2009552641 A JP2009552641 A JP 2009552641A JP 2009552641 A JP2009552641 A JP 2009552641A JP 2010520276 A5 JP2010520276 A5 JP 2010520276A5

Authority

JP

Japan

Prior art keywords

alkyl

fluoroalkyl

alkylene

nhc

compound according

Prior art date

2008-03-05

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

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• 125000003709 fluoroalkyl group Chemical group 0.000 claims 29
• 150000001875 compounds Chemical class 0.000 claims 24
• 125000000217 alkyl group Chemical group 0.000 claims 22
• 125000002947 alkylene group Chemical group 0.000 claims 15
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 14
• -1 hydroxy, methoxy Chemical group 0.000 claims 14
• 125000001153 fluoro group Chemical group F* 0.000 claims 9
• 125000003545 alkoxy group Chemical group 0.000 claims 8
• 125000004428 fluoroalkoxy group Chemical group 0.000 claims 8
• 150000003839 salts Chemical class 0.000 claims 8
• 239000012453 solvate Substances 0.000 claims 8
• 125000004429 atom Chemical group 0.000 claims 6
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
• 125000001246 bromo group Chemical group Br* 0.000 claims 5
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
• 239000012458 free base Substances 0.000 claims 4
• 125000004356 hydroxy functional group Chemical group O* 0.000 claims 4
• 125000002346 iodo group Chemical group I* 0.000 claims 4
• 238000000034 method Methods 0.000 claims 4
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
• JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 3
• 229910052757 nitrogen Inorganic materials 0.000 claims 3
• 125000001424 substituent group Chemical group 0.000 claims 3
• 108700028369 Alleles Proteins 0.000 claims 2
• 208000024827 Alzheimer disease Diseases 0.000 claims 2
• 108010060159 Apolipoprotein E4 Proteins 0.000 claims 2
• 201000010374 Down Syndrome Diseases 0.000 claims 2
• 125000004414 alkyl thio group Chemical group 0.000 claims 2
• 230000003941 amyloidogenesis Effects 0.000 claims 2
• 125000004093 cyano group Chemical group *C#N 0.000 claims 2
• 208000025688 early-onset autosomal dominant Alzheimer disease Diseases 0.000 claims 2
• 208000015756 familial Alzheimer disease Diseases 0.000 claims 2
• 125000005843 halogen group Chemical group 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 2
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 125000004455 (C1-C3) alkylthio group Chemical group 0.000 claims 1
• MNCMBBIFTVWHIP-UHFFFAOYSA-N 1-anthracen-9-yl-2,2,2-trifluoroethanone Chemical group C1=CC=C2C(C(=O)C(F)(F)F)=C(C=CC=C3)C3=CC2=C1 MNCMBBIFTVWHIP-UHFFFAOYSA-N 0.000 claims 1
• 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
• XCUAIINAJCDIPM-XVFCMESISA-N N(4)-hydroxycytidine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=NO)C=C1 XCUAIINAJCDIPM-XVFCMESISA-N 0.000 claims 1
• 206010044688 Trisomy 21 Diseases 0.000 claims 1
• XAKBSHICSHRJCL-UHFFFAOYSA-N [CH2]C(=O)C1=CC=CC=C1 Chemical group [CH2]C(=O)C1=CC=CC=C1 XAKBSHICSHRJCL-UHFFFAOYSA-N 0.000 claims 1
• 239000000470 constituent Substances 0.000 claims 1
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
• 238000001514 detection method Methods 0.000 claims 1
• 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
• 125000000524 functional group Chemical group 0.000 claims 1
• XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical class I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims 1
• 238000003384 imaging method Methods 0.000 claims 1
• 238000001727 in vivo Methods 0.000 claims 1
• 238000002595 magnetic resonance imaging Methods 0.000 claims 1
• 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
• 125000001209 o-nitrophenyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])[N+]([O-])=O 0.000 claims 1
• 239000002243 precursor Substances 0.000 claims 1
• 230000002265 prevention Effects 0.000 claims 1
• 238000004611 spectroscopical analysis Methods 0.000 claims 1
• 208000011580 syndromic disease Diseases 0.000 claims 1
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
• 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
• 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
• 229920002554 vinyl polymer Polymers 0.000 claims 1