JP2019516727A5 - - Google Patents

Info

Publication number

JP2019516727A5

JP2019516727A5 JP2018560665A JP2018560665A JP2019516727A5 JP 2019516727 A5 JP2019516727 A5 JP 2019516727A5 JP 2018560665 A JP2018560665 A JP 2018560665A JP 2018560665 A JP2018560665 A JP 2018560665A JP 2019516727 A5 JP2019516727 A5 JP 2019516727A5

Authority

JP

Japan

Prior art keywords

composition

subject

pharmaceutically acceptable

ebselen

acceptable salt

Prior art date

2017-05-18

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
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• 239000000203 mixture Substances 0.000 claims description 48
• 238000000034 method Methods 0.000 claims description 38
• 150000001875 compounds Chemical class 0.000 claims description 25
• DYEFUKCXAQOFHX-UHFFFAOYSA-N Ebselen Chemical compound [se]1C2=CC=CC=C2C(=O)N1C1=CC=CC=C1 DYEFUKCXAQOFHX-UHFFFAOYSA-N 0.000 claims description 18
• 102000006587 Glutathione peroxidase Human genes 0.000 claims description 18
• 108700016172 Glutathione peroxidases Proteins 0.000 claims description 18
• 229950010033 ebselen Drugs 0.000 claims description 18
• 150000003839 salts Chemical class 0.000 claims description 15
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
• 208000009205 Tinnitus Diseases 0.000 claims description 11
• 239000012453 solvate Substances 0.000 claims description 11
• 231100000886 tinnitus Toxicity 0.000 claims description 11
• 229920000858 Cyclodextrin Polymers 0.000 claims description 10
• 239000001116 FEMA 4028 Substances 0.000 claims description 10
• 229960004853 betadex Drugs 0.000 claims description 10
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
• 238000012360 testing method Methods 0.000 claims description 7
• 208000012886 Vertigo Diseases 0.000 claims description 6
• -1 phenylacetyl Chemical group 0.000 claims description 6
• 231100000889 vertigo Toxicity 0.000 claims description 6
• 206010011878 Deafness Diseases 0.000 claims description 5
• 208000002173 dizziness Diseases 0.000 claims description 5
• 210000003027 ear inner Anatomy 0.000 claims description 5
• 208000016354 hearing loss disease Diseases 0.000 claims description 5
• 208000027530 Meniere disease Diseases 0.000 claims description 4
• MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 4
• 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims description 4
• WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 claims description 4
• 235000011175 beta-cyclodextrine Nutrition 0.000 claims description 4
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
• 239000002934 diuretic Substances 0.000 claims description 4
• 230000001882 diuretic effect Effects 0.000 claims description 4
• 208000005457 endolymphatic hydrops Diseases 0.000 claims description 4
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
• 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
• 125000004043 oxo group Chemical group O=* 0.000 claims description 4
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
• 150000003254 radicals Chemical class 0.000 claims description 4
• 229910052711 selenium Inorganic materials 0.000 claims description 4
• 239000011669 selenium Substances 0.000 claims description 4
• 238000012076 audiometry Methods 0.000 claims description 3
• 231100000888 hearing loss Toxicity 0.000 claims description 3
• 230000010370 hearing loss Effects 0.000 claims description 3
• 238000005259 measurement Methods 0.000 claims description 3
• 239000008194 pharmaceutical composition Substances 0.000 claims description 3
• 208000024891 symptom Diseases 0.000 claims description 3
• GIANIJCPTPUNBA-QMMMGPOBSA-N (2s)-3-(4-hydroxyphenyl)-2-nitramidopropanoic acid Chemical compound [O-][N+](=O)N[C@H](C(=O)O)CC1=CC=C(O)C=C1 GIANIJCPTPUNBA-QMMMGPOBSA-N 0.000 claims description 2
• 206010061218 Inflammation Diseases 0.000 claims description 2
• OUUQCZGPVNCOIJ-UHFFFAOYSA-M Superoxide Chemical compound [O-][O] OUUQCZGPVNCOIJ-UHFFFAOYSA-M 0.000 claims description 2
• 231100000895 deafness Toxicity 0.000 claims description 2
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
• 230000004054 inflammatory process Effects 0.000 claims description 2
• 230000001720 vestibular Effects 0.000 claims description 2
• 230000009429 distress Effects 0.000 claims 3
• 238000011156 evaluation Methods 0.000 claims 3
• 239000007909 solid dosage form Substances 0.000 claims 2
• 239000002775 capsule Substances 0.000 claims 1
• 239000002552 dosage form Substances 0.000 claims 1
• 230000006870 function Effects 0.000 claims 1
• 238000002595 magnetic resonance imaging Methods 0.000 description 3
• SHVXEKYNBOITNG-KYJUHHDHSA-N (5s)-5-benzyl-1-[4-[(2s)-1-[2-(4-hydroxyphenyl)ethyl]-5,6-dioxopiperazin-2-yl]butyl]-4-(2-phenylethyl)piperazine-2,3-dione Chemical compound C1=CC(O)=CC=C1CCN1C(=O)C(=O)NC[C@@H]1CCCCN1C(=O)C(=O)N(CCC=2C=CC=CC=2)[C@@H](CC=2C=CC=CC=2)C1 SHVXEKYNBOITNG-KYJUHHDHSA-N 0.000 description 1
• 0 *C1NC(*)SC1 Chemical compound *C1NC(*)SC1 0.000 description 1
• PWKSKIMOESPYIA-UHFFFAOYSA-N CC(NC(CS)C(O)=O)=O Chemical compound CC(NC(CS)C(O)=O)=O PWKSKIMOESPYIA-UHFFFAOYSA-N 0.000 description 1
• 238000004820 blood count Methods 0.000 description 1
• 230000000694 effects Effects 0.000 description 1
• CMFNMSMUKZHDEY-UHFFFAOYSA-M peroxynitrite Chemical compound [O-]ON=O CMFNMSMUKZHDEY-UHFFFAOYSA-M 0.000 description 1