JP2015510941A5 - - Google Patents

Info

Publication number

JP2015510941A5

JP2015510941A5 JP2015501819A JP2015501819A JP2015510941A5 JP 2015510941 A5 JP2015510941 A5 JP 2015510941A5 JP 2015501819 A JP2015501819 A JP 2015501819A JP 2015501819 A JP2015501819 A JP 2015501819A JP 2015510941 A5 JP2015510941 A5 JP 2015510941A5

Authority

JP

Japan

Prior art keywords

alkyl

use according

app

alzheimer

disease

Prior art date

2013-03-15

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

• Espacenet
• Global Dossier
• Discuss

• 229940126077 BACE inhibitor Drugs 0.000 claims 24
• 239000003814 drug Substances 0.000 claims 24
• 208000024827 Alzheimer disease Diseases 0.000 claims 21
• VCCRNZQBSJXYJD-UHFFFAOYSA-N galangin Chemical group C=1C(O)=CC(O)=C(C(C=2O)=O)C=1OC=2C1=CC=CC=C1 VCCRNZQBSJXYJD-UHFFFAOYSA-N 0.000 claims 12
• 125000000217 alkyl group Chemical group 0.000 claims 10
• 229910052736 halogen Inorganic materials 0.000 claims 10
• 150000002367 halogens Chemical class 0.000 claims 10
• 125000001072 heteroaryl group Chemical group 0.000 claims 8
• 208000010877 cognitive disease Diseases 0.000 claims 7
• 230000007423 decrease Effects 0.000 claims 6
• 229930003935 flavonoid Natural products 0.000 claims 6
• 150000002215 flavonoids Chemical class 0.000 claims 6
• 235000017173 flavonoids Nutrition 0.000 claims 6
• CIPSYTVGZURWPT-UHFFFAOYSA-N galangin Natural products OC1=C(Oc2cc(O)c(O)cc2C1=O)c3ccccc3 CIPSYTVGZURWPT-UHFFFAOYSA-N 0.000 claims 6
• SUYJZKRQHBQNCA-UHFFFAOYSA-N pinobanksin Natural products O1C2=CC(O)=CC(O)=C2C(=O)C(O)C1C1=CC=CC=C1 SUYJZKRQHBQNCA-UHFFFAOYSA-N 0.000 claims 6
• KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 5
• 208000024891 symptom Diseases 0.000 claims 5
• JMGZEFIQIZZSBH-UHFFFAOYSA-N Bioquercetin Natural products CC1OC(OCC(O)C2OC(OC3=C(Oc4cc(O)cc(O)c4C3=O)c5ccc(O)c(O)c5)C(O)C2O)C(O)C(O)C1O JMGZEFIQIZZSBH-UHFFFAOYSA-N 0.000 claims 4
• 150000007942 carboxylates Chemical class 0.000 claims 4
• IVTMALDHFAHOGL-UHFFFAOYSA-N eriodictyol 7-O-rutinoside Natural products OC1C(O)C(O)C(C)OC1OCC1C(O)C(O)C(O)C(OC=2C=C3C(C(C(O)=C(O3)C=3C=C(O)C(O)=CC=3)=O)=C(O)C=2)O1 IVTMALDHFAHOGL-UHFFFAOYSA-N 0.000 claims 4
• FDRQPMVGJOQVTL-UHFFFAOYSA-N quercetin rutinoside Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC=2C(C3=C(O)C=C(O)C=C3OC=2C=2C=C(O)C(O)=CC=2)=O)O1 FDRQPMVGJOQVTL-UHFFFAOYSA-N 0.000 claims 4
• IKGXIBQEEMLURG-NVPNHPEKSA-N rutin Chemical group O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@H](OC=2C(C3=C(O)C=C(O)C=C3OC=2C=2C=C(O)C(O)=CC=2)=O)O1 IKGXIBQEEMLURG-NVPNHPEKSA-N 0.000 claims 4
• ALABRVAAKCSLSC-UHFFFAOYSA-N rutin Natural products CC1OC(OCC2OC(O)C(O)C(O)C2O)C(O)C(O)C1OC3=C(Oc4cc(O)cc(O)c4C3=O)c5ccc(O)c(O)c5 ALABRVAAKCSLSC-UHFFFAOYSA-N 0.000 claims 4
• 235000005493 rutin Nutrition 0.000 claims 4
• 229960004555 rutoside Drugs 0.000 claims 4
• 102100021257 Beta-secretase 1 Human genes 0.000 claims 3
• 208000031124 Dementia Alzheimer type Diseases 0.000 claims 3
• 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 claims 3
• 241000124008 Mammalia Species 0.000 claims 3
• 239000000651 prodrug Substances 0.000 claims 3
• 229940002612 prodrug Drugs 0.000 claims 3
• 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims 2
• 239000004480 active ingredient Substances 0.000 claims 2
• 206010064930 age-related macular degeneration Diseases 0.000 claims 2
• 206010002022 amyloidosis Diseases 0.000 claims 2
• 210000004556 brain Anatomy 0.000 claims 2
• 229910052794 bromium Inorganic materials 0.000 claims 2
• 230000002490 cerebral effect Effects 0.000 claims 2
• 229910052801 chlorine Inorganic materials 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
• 229910001851 flerovium Inorganic materials 0.000 claims 2
• 229910052740 iodine Inorganic materials 0.000 claims 2
• 208000002780 macular degeneration Diseases 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 2
• 230000004770 neurodegeneration Effects 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 108700028369 Alleles Proteins 0.000 claims 1
• 101710137189 Amyloid-beta A4 protein Proteins 0.000 claims 1
• 101710151993 Amyloid-beta precursor protein Proteins 0.000 claims 1
• 102100022704 Amyloid-beta precursor protein Human genes 0.000 claims 1
• 208000028698 Cognitive impairment Diseases 0.000 claims 1
• 206010012289 Dementia Diseases 0.000 claims 1
• 239000000443 aerosol Substances 0.000 claims 1
• 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 1
• 230000003542 behavioural effect Effects 0.000 claims 1
• 239000000090 biomarker Substances 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 230000003930 cognitive ability Effects 0.000 claims 1
• 230000001149 cognitive effect Effects 0.000 claims 1
• 230000003920 cognitive function Effects 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 230000001747 exhibiting effect Effects 0.000 claims 1
• 239000003112 inhibitor Substances 0.000 claims 1
• 230000005764 inhibitory process Effects 0.000 claims 1
• 238000001990 intravenous administration Methods 0.000 claims 1
• 208000027061 mild cognitive impairment Diseases 0.000 claims 1
• 230000035772 mutation Effects 0.000 claims 1
• 230000007505 plaque formation Effects 0.000 claims 1
• 125000006239 protecting group Chemical group 0.000 claims 1
• 238000011084 recovery Methods 0.000 claims 1
• 230000006641 stabilisation Effects 0.000 claims 1
• 238000011105 stabilization Methods 0.000 claims 1
• 230000037317 transdermal delivery Effects 0.000 claims 1
• 230000007704 transition Effects 0.000 claims 1