JPWO2019246454A5 - - Google Patents
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- JPWO2019246454A5 JPWO2019246454A5 JP2020570933A JP2020570933A JPWO2019246454A5 JP WO2019246454 A5 JPWO2019246454 A5 JP WO2019246454A5 JP 2020570933 A JP2020570933 A JP 2020570933A JP 2020570933 A JP2020570933 A JP 2020570933A JP WO2019246454 A5 JPWO2019246454 A5 JP WO2019246454A5
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- 150000001875 compounds Chemical class 0.000 claims description 64
- 150000003839 salts Chemical class 0.000 claims description 49
- 238000000034 method Methods 0.000 claims description 39
- 239000008194 pharmaceutical composition Substances 0.000 claims description 38
- 125000000217 alkyl group Chemical group 0.000 claims description 37
- 125000000623 heterocyclic group Chemical group 0.000 claims description 31
- 125000003545 alkoxy group Chemical group 0.000 claims description 22
- 229910052799 carbon Inorganic materials 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 22
- 239000001257 hydrogen Substances 0.000 claims description 22
- 229940122755 Ion transporter inhibitor Drugs 0.000 claims description 20
- 230000000975 bioactive effect Effects 0.000 claims description 20
- 239000002207 metabolite Substances 0.000 claims description 20
- 108090000623 proteins and genes Proteins 0.000 claims description 17
- 102000004169 proteins and genes Human genes 0.000 claims description 17
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 13
- 102100035227 Solute carrier family 22 member 8 Human genes 0.000 claims description 13
- 101710102389 Solute carrier family 22 member 8 Proteins 0.000 claims description 13
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 12
- 150000002367 halogens Chemical class 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 238000009825 accumulation Methods 0.000 claims description 10
- 230000008499 blood brain barrier function Effects 0.000 claims description 10
- 210000001218 blood-brain barrier Anatomy 0.000 claims description 10
- 210000004556 brain Anatomy 0.000 claims description 10
- 108091005804 Peptidases Proteins 0.000 claims description 9
- 239000004365 Protease Substances 0.000 claims description 9
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims description 9
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- 238000004519 manufacturing process Methods 0.000 claims description 6
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- 239000008177 pharmaceutical agent Substances 0.000 claims description 6
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- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 229910052717 sulfur Inorganic materials 0.000 claims description 5
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
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- CZWCKYRVOZZJNM-UHFFFAOYSA-N Prasterone sodium sulfate Natural products C1C(OS(O)(=O)=O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 CZWCKYRVOZZJNM-UHFFFAOYSA-N 0.000 claims description 4
- 101710150875 TAR DNA-binding protein 43 Proteins 0.000 claims description 4
- 102100040347 TAR DNA-binding protein 43 Human genes 0.000 claims description 4
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 4
- 230000002776 aggregation Effects 0.000 claims description 4
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- CZWCKYRVOZZJNM-USOAJAOKSA-N dehydroepiandrosterone sulfate Chemical compound C1[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 CZWCKYRVOZZJNM-USOAJAOKSA-N 0.000 claims description 4
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 4
- 230000002708 enhancing effect Effects 0.000 claims description 4
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 4
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 4
- 230000009529 traumatic brain injury Effects 0.000 claims description 4
- 238000000338 in vitro Methods 0.000 claims description 3
- 238000001727 in vivo Methods 0.000 claims description 3
- 230000001105 regulatory effect Effects 0.000 claims description 3
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 claims description 2
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical class CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims description 2
- 206010003694 Atrophy Diseases 0.000 claims description 2
- 201000011240 Frontotemporal dementia Diseases 0.000 claims description 2
- 108010024636 Glutathione Proteins 0.000 claims description 2
- 102000016252 Huntingtin Human genes 0.000 claims description 2
- 108050004784 Huntingtin Proteins 0.000 claims description 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims description 2
- 201000002832 Lewy body dementia Diseases 0.000 claims description 2
- 208000001089 Multiple system atrophy Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010033799 Paralysis Diseases 0.000 claims description 2
- 101000685685 Rattus norvegicus Solute carrier family 22 member 23 Proteins 0.000 claims description 2
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 claims description 2
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 claims description 2
- -1 a-β Proteins 0.000 claims description 2
- 230000032683 aging Effects 0.000 claims description 2
- 102000003802 alpha-Synuclein Human genes 0.000 claims description 2
- 108090000185 alpha-Synuclein Proteins 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 125000000129 anionic group Chemical group 0.000 claims description 2
- 230000037444 atrophy Effects 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 claims description 2
- 229960003638 dopamine Drugs 0.000 claims description 2
- 229960003180 glutathione Drugs 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 201000010901 lateral sclerosis Diseases 0.000 claims description 2
- 125000006578 monocyclic heterocycloalkyl group Chemical group 0.000 claims description 2
- 208000005264 motor neuron disease Diseases 0.000 claims description 2
- 230000003387 muscular Effects 0.000 claims description 2
- 230000000626 neurodegenerative effect Effects 0.000 claims description 2
- 230000004112 neuroprotection Effects 0.000 claims description 2
- 230000000324 neuroprotective effect Effects 0.000 claims description 2
- 239000002858 neurotransmitter agent Substances 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 229960002748 norepinephrine Drugs 0.000 claims description 2
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000036470 plasma concentration Effects 0.000 claims description 2
- 230000007112 pro inflammatory response Effects 0.000 claims description 2
- 230000000750 progressive effect Effects 0.000 claims description 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims description 2
- 229940076279 serotonin Drugs 0.000 claims description 2
- 102000013498 tau Proteins Human genes 0.000 claims description 2
- 108010026424 tau Proteins Proteins 0.000 claims description 2
- 230000002123 temporal effect Effects 0.000 claims description 2
- 229940116269 uric acid Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010029240 Neuritis Diseases 0.000 description 3
- 125000002950 monocyclic group Chemical group 0.000 description 3
- 102100036930 Solute carrier family 22 member 6 Human genes 0.000 description 2
- 101710102683 Solute carrier family 22 member 6 Proteins 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000002314 neuroinflammatory effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862687733P | 2018-06-20 | 2018-06-20 | |
| US62/687,733 | 2018-06-20 | ||
| US201862752265P | 2018-10-29 | 2018-10-29 | |
| US62/752,265 | 2018-10-29 | ||
| PCT/US2019/038328 WO2019246454A1 (en) | 2018-06-20 | 2019-06-20 | Method of treating a condition associated with neurodegeneration using inhibitors of oat3 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021527692A JP2021527692A (ja) | 2021-10-14 |
| JPWO2019246454A5 true JPWO2019246454A5 (https=) | 2022-06-27 |
| JP2021527692A5 JP2021527692A5 (https=) | 2022-06-27 |
Family
ID=67211909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020570933A Pending JP2021527692A (ja) | 2018-06-20 | 2019-06-20 | Ｏａｔ３の阻害剤を用いた神経変性に関連する状態の処置方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20210290597A1 (https=) |
| EP (1) | EP3810133A1 (https=) |
| JP (1) | JP2021527692A (https=) |
| CN (1) | CN112512523A (https=) |
| WO (1) | WO2019246454A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021195431A1 (en) * | 2020-03-25 | 2021-09-30 | The Brigham And Women's Hospital, Inc. | Inhaled xenon therapy in neurodegenerative disease |
| CN113777197B (zh) * | 2021-09-16 | 2022-05-27 | 福州大学 | 一种同时测定桔霉素和1-羟基-2-萘甲酸的方法 |
| WO2024112921A1 (en) * | 2022-11-22 | 2024-05-30 | Mcphs University | Treatment of tartaric acid toxicity in dogs with probenecid |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4279637A (en) * | 1979-06-02 | 1981-07-21 | Velsicol Chemical Corporation | Herbicidal N-substituted 4-imidazolin-2-ones |
| RU2223952C2 (ru) * | 2001-06-04 | 2004-02-20 | Институт физиологически активных веществ РАН | Производные n,s-замещенных n'-1-[(гетеро)арил]-n'-[(гетеро)арил]метилизотиомочевин или их солей с фармакологически приемлемыми кислотами нх, способы получения их солей и оснований, фармацевтическая композиция, способ лечения и способ изучения глутаматэргической системы |
| US9422252B2 (en) * | 2012-05-22 | 2016-08-23 | Autifony Therapeutics Limited | Triazoles as Kv3 inhibitors |
| CN110114881B (zh) * | 2017-03-08 | 2020-03-27 | 长江存储科技有限责任公司 | 三维存储器件的贯穿阵列触点结构 |
| EP3703675A4 (en) * | 2017-10-30 | 2021-06-16 | Neuropore Therapies, Inc. | SUBSTITUTED PHENYLSULFONYLPHÉNYLTRIAZOLETHIONES AND ASSOCIATED USES |
-
2019
- 2019-06-20 US US17/253,581 patent/US20210290597A1/en not_active Abandoned
- 2019-06-20 JP JP2020570933A patent/JP2021527692A/ja active Pending
- 2019-06-20 CN CN201980047291.0A patent/CN112512523A/zh active Pending
- 2019-06-20 EP EP19737383.0A patent/EP3810133A1/en not_active Withdrawn
- 2019-06-20 WO PCT/US2019/038328 patent/WO2019246454A1/en not_active Ceased
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