JP2005500370A5 - - Google Patents

Info

Publication number

JP2005500370A5

JP2005500370A5 JP2003519045A JP2003519045A JP2005500370A5 JP 2005500370 A5 JP2005500370 A5 JP 2005500370A5 JP 2003519045 A JP2003519045 A JP 2003519045A JP 2003519045 A JP2003519045 A JP 2003519045A JP 2005500370 A5 JP2005500370 A5 JP 2005500370A5

Authority

JP

Japan

Prior art keywords

formula

group

compound

cycloalkyl

alkyl

Prior art date

2002-08-05

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.)

Pending

Links

• Espacenet
• Global Dossier
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• 150000001875 compounds Chemical class 0.000 claims 11
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
• 125000003545 alkoxy group Chemical group 0.000 claims 8
• 125000005843 halogen group Chemical group 0.000 claims 8
• 125000000217 alkyl group Chemical group 0.000 claims 6
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
• 125000003386 piperidinyl group Chemical group 0.000 claims 6
• 150000003839 salts Chemical class 0.000 claims 6
• 239000012453 solvate Substances 0.000 claims 6
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 5
• 125000000753 cycloalkyl group Chemical group 0.000 claims 5
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
• 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 4
• 239000002253 acid Substances 0.000 claims 4
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
• -1 methylenedioxy Chemical group 0.000 claims 3
• 125000004043 oxo group Chemical group O=* 0.000 claims 3
• 239000008194 pharmaceutical composition Substances 0.000 claims 3
• 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
• 208000024827 Alzheimer disease Diseases 0.000 claims 2
• MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 2
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
• 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 2
• 229910052739 hydrogen Inorganic materials 0.000 claims 2
• 239000001257 hydrogen Substances 0.000 claims 2
• 239000003112 inhibitor Substances 0.000 claims 2
• 229910052760 oxygen Inorganic materials 0.000 claims 2
• 239000001301 oxygen Substances 0.000 claims 2
• 238000005897 peptide coupling reaction Methods 0.000 claims 2
• 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
• 229910052717 sulfur Inorganic materials 0.000 claims 2
• 125000004434 sulfur atom Chemical group 0.000 claims 2
• 230000001225 therapeutic effect Effects 0.000 claims 2
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
• 206010059245 Angiopathy Diseases 0.000 claims 1
• 201000010374 Down Syndrome Diseases 0.000 claims 1
• 208000018737 Parkinson disease Diseases 0.000 claims 1
• 206010039966 Senile dementia Diseases 0.000 claims 1
• 206010044688 Trisomy 21 Diseases 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• 150000001412 amines Chemical class 0.000 claims 1
• 150000001413 amino acids Chemical class 0.000 claims 1
• 230000015572 biosynthetic process Effects 0.000 claims 1
• 208000026106 cerebrovascular disease Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
• 229910052731 fluorine Inorganic materials 0.000 claims 1
• 125000001153 fluoro group Chemical group F* 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
• 125000004430 oxygen atom Chemical group O* 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 208000024891 symptom Diseases 0.000 claims 1
• 0 C[C@@](C1)[C@]2C1[C@@](C)*CC2 Chemical compound C[C@@](C1)[C@]2C1[C@@](C)*CC2 0.000 description 3