JP2005516967A5 - - Google Patents

Info

Publication number

JP2005516967A5

JP2005516967A5 JP2003559508A JP2003559508A JP2005516967A5 JP 2005516967 A5 JP2005516967 A5 JP 2005516967A5 JP 2003559508 A JP2003559508 A JP 2003559508A JP 2003559508 A JP2003559508 A JP 2003559508A JP 2005516967 A5 JP2005516967 A5 JP 2005516967A5

Authority

JP

Japan

Prior art keywords

secretase inhibitor

inhibitor according

manufacture

amyloid

secretase

Prior art date

2003-01-20

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.)

Withdrawn

Links

• Espacenet
• Global Dossier
• Discuss

• 239000002439 beta secretase inhibitor Substances 0.000 claims 8
• DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• 238000004519 manufacturing process Methods 0.000 claims 4
• 229910052736 halogen Inorganic materials 0.000 claims 3
• 125000005843 halogen group Chemical group 0.000 claims 3
• 208000024827 Alzheimer disease Diseases 0.000 claims 2
• 101710137189 Amyloid-beta A4 protein Proteins 0.000 claims 2
• 101710151993 Amyloid-beta precursor protein Proteins 0.000 claims 2
• 102100022704 Amyloid-beta precursor protein Human genes 0.000 claims 2
• 125000005354 acylalkyl group Chemical group 0.000 claims 2
• 125000005243 carbonyl alkyl group Chemical group 0.000 claims 2
• 125000001188 haloalkyl group Chemical group 0.000 claims 2
• 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
• 125000005429 oxyalkyl group Chemical group 0.000 claims 2
• 125000004963 sulfonylalkyl group Chemical group 0.000 claims 2
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
• 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 1
• 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 1
• 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 1
• 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 1
• 230000007082 Aβ accumulation Effects 0.000 claims 1
• 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
• 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
• 206010012289 Dementia Diseases 0.000 claims 1
• 201000010374 Down Syndrome Diseases 0.000 claims 1
• 206010044688 Trisomy 21 Diseases 0.000 claims 1
• 235000018936 Vitellaria paradoxa Nutrition 0.000 claims 1
• 125000003342 alkenyl group Chemical group 0.000 claims 1
• 125000000217 alkyl group Chemical group 0.000 claims 1
• 125000000304 alkynyl group Chemical group 0.000 claims 1
• 206010002022 amyloidosis Diseases 0.000 claims 1
• 125000003118 aryl group Chemical group 0.000 claims 1
• 230000015572 biosynthetic process Effects 0.000 claims 1
• 229910052794 bromium Inorganic materials 0.000 claims 1
• 125000004432 carbon atom Chemical group C* 0.000 claims 1
• 125000004181 carboxyalkyl group Chemical group 0.000 claims 1
• 229910052801 chlorine Inorganic materials 0.000 claims 1
• 125000004093 cyano group Chemical group *C#N 0.000 claims 1
• 125000004966 cyanoalkyl group Chemical group 0.000 claims 1
• 230000003412 degenerative effect Effects 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 229940079593 drug Drugs 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 229910052731 fluorine Inorganic materials 0.000 claims 1
• 125000000623 heterocyclic group Chemical group 0.000 claims 1
• 125000001183 hydrocarbyl group Chemical group 0.000 claims 1
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
• 239000003112 inhibitor Substances 0.000 claims 1
• 230000002401 inhibitory effect Effects 0.000 claims 1
• 229910052740 iodine Inorganic materials 0.000 claims 1
• 230000001404 mediated effect Effects 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
• 230000007331 pathological accumulation Effects 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 230000002265 prevention Effects 0.000 claims 1