JP2014529613A5 - - Google Patents

Info

Publication number

JP2014529613A5

JP2014529613A5 JP2014527357A JP2014527357A JP2014529613A5 JP 2014529613 A5 JP2014529613 A5 JP 2014529613A5 JP 2014527357 A JP2014527357 A JP 2014527357A JP 2014527357 A JP2014527357 A JP 2014527357A JP 2014529613 A5 JP2014529613 A5 JP 2014529613A5

Authority

JP

Japan

Prior art keywords

compound

alkyl

seq

haloalkyl

amyloid beta

Prior art date

2012-08-27

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.)

Pending

Links

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• 150000001875 compounds Chemical class 0.000 claims 34
• 125000000217 alkyl group Chemical group 0.000 claims 28
• 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 16
• 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 16
• 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 14
• 125000001475 halogen functional group Chemical group 0.000 claims 14
• 210000002569 neuron Anatomy 0.000 claims 11
• 210000004027 cell Anatomy 0.000 claims 10
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
• 239000003795 chemical substances by application Substances 0.000 claims 9
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 8
• 150000003839 salts Chemical class 0.000 claims 8
• 208000010877 cognitive disease Diseases 0.000 claims 7
• 239000003814 drug Substances 0.000 claims 7
• 230000002401 inhibitory effect Effects 0.000 claims 7
• 102100028662 Sigma intracellular receptor 2 Human genes 0.000 claims 6
• 101710109012 Sigma intracellular receptor 2 Proteins 0.000 claims 6
• 230000006999 cognitive decline Effects 0.000 claims 6
• 239000012634 fragment Substances 0.000 claims 5
• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
• 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 4
• 102000003939 Membrane transport proteins Human genes 0.000 claims 4
• 108090000301 Membrane transport proteins Proteins 0.000 claims 4
• 125000003545 alkoxy group Chemical group 0.000 claims 4
• 229940079593 drug Drugs 0.000 claims 4
• 230000000694 effects Effects 0.000 claims 4
• 230000009061 membrane transport Effects 0.000 claims 4
• 229940123586 Sigma 2 receptor antagonist Drugs 0.000 claims 3
• 230000005856 abnormality Effects 0.000 claims 3
• 230000007470 synaptic degeneration Effects 0.000 claims 3
• 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 2
• 102100037651 AP-2 complex subunit sigma Human genes 0.000 claims 2
• 208000024827 Alzheimer disease Diseases 0.000 claims 2
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
• 101000806914 Homo sapiens AP-2 complex subunit sigma Proteins 0.000 claims 2
• 230000002730 additional effect Effects 0.000 claims 2
• 238000010171 animal model Methods 0.000 claims 2
• 239000005557 antagonist Substances 0.000 claims 2
• 239000000427 antigen Substances 0.000 claims 2
• 102000036639 antigens Human genes 0.000 claims 2
• 108091007433 antigens Proteins 0.000 claims 2
• 230000001149 cognitive effect Effects 0.000 claims 2
• 230000008897 memory decline Effects 0.000 claims 2
• 210000000225 synapse Anatomy 0.000 claims 2
• 238000012360 testing method Methods 0.000 claims 2
• 230000032258 transport Effects 0.000 claims 2
• 230000031836 visual learning Effects 0.000 claims 2
• 238000012347 Morris Water Maze Methods 0.000 claims 1
• 238000003556 assay Methods 0.000 claims 1
• 230000003750 conditioning effect Effects 0.000 claims 1
• 230000007547 defect Effects 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 230000000971 hippocampal effect Effects 0.000 claims 1
• 230000013016 learning Effects 0.000 claims 1
• 230000027928 long-term synaptic potentiation Effects 0.000 claims 1
• 230000007774 longterm Effects 0.000 claims 1
• 230000001404 mediated effect Effects 0.000 claims 1
• 230000015654 memory Effects 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 208000027061 mild cognitive impairment Diseases 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• 230000001629 suppression Effects 0.000 claims 1
• 230000003976 synaptic dysfunction Effects 0.000 claims 1