JP2021527692A - 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 - Google Patents
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 Download PDFInfo
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- JP2021527692A JP2021527692A JP2020570933A JP2020570933A JP2021527692A JP 2021527692 A JP2021527692 A JP 2021527692A JP 2020570933 A JP2020570933 A JP 2020570933A JP 2020570933 A JP2020570933 A JP 2020570933A JP 2021527692 A JP2021527692 A JP 2021527692A
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- Prior art keywords
- alkyl
- compound
- substituted
- pharmaceutically acceptable
- formula
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- 0 CC(C)CN(C=**1N)C1=* Chemical compound CC(C)CN(C=**1N)C1=* 0.000 description 9
- LADGTIIIXLYISM-UHFFFAOYSA-N Nc(cc1)ccc1S(c(cc1)cc(C(F)(F)F)c1Cl)(=O)=O Chemical compound Nc(cc1)ccc1S(c(cc1)cc(C(F)(F)F)c1Cl)(=O)=O LADGTIIIXLYISM-UHFFFAOYSA-N 0.000 description 2
- PZTNXINTRBOLNC-XQRVVYSFSA-N C/C(/SC)=N/NC Chemical compound C/C(/SC)=N/NC PZTNXINTRBOLNC-XQRVVYSFSA-N 0.000 description 1
- VLGPDTPSKUUHKR-UHFFFAOYSA-N CC(C)(C)OC(Nc(cc1)ccc1Br)=O Chemical compound CC(C)(C)OC(Nc(cc1)ccc1Br)=O VLGPDTPSKUUHKR-UHFFFAOYSA-N 0.000 description 1
- HCJYSFKDQZWNEM-UHFFFAOYSA-N CC(C=CC(C1)S)=C1C(F)(F)F Chemical compound CC(C=CC(C1)S)=C1C(F)(F)F HCJYSFKDQZWNEM-UHFFFAOYSA-N 0.000 description 1
- LMSLRBRLMMNGRO-UHFFFAOYSA-N CN(C(c(cc1)cc(C(F)(F)F)c1Cl)=O)OC Chemical compound CN(C(c(cc1)cc(C(F)(F)F)c1Cl)=O)OC LMSLRBRLMMNGRO-UHFFFAOYSA-N 0.000 description 1
- GYTKPAJDGDSJFQ-UHFFFAOYSA-N FC(c(cc1)ccc1N(C=NN1)C1=S)(c(cc1C(F)(F)F)ccc1Cl)F Chemical compound FC(c(cc1)ccc1N(C=NN1)C1=S)(c(cc1C(F)(F)F)ccc1Cl)F GYTKPAJDGDSJFQ-UHFFFAOYSA-N 0.000 description 1
- WZVHLUMAQLUNTJ-UHFFFAOYSA-N FC(c1cc(Br)ncc1)(F)F Chemical compound FC(c1cc(Br)ncc1)(F)F WZVHLUMAQLUNTJ-UHFFFAOYSA-N 0.000 description 1
- ASPDJZINBYYZRU-UHFFFAOYSA-N Nc(cc1)cc(C(F)(F)F)c1Cl Chemical compound Nc(cc1)cc(C(F)(F)F)c1Cl ASPDJZINBYYZRU-UHFFFAOYSA-N 0.000 description 1
- TZQVSGOOKNNDFU-UHFFFAOYSA-N Nc(cc1)ccc1Sc1ccccc1 Chemical compound Nc(cc1)ccc1Sc1ccccc1 TZQVSGOOKNNDFU-UHFFFAOYSA-N 0.000 description 1
- RLCFHQSJTSVRHI-UHFFFAOYSA-N O=S(c(cc1)ccc1N(C=CN1)C1=S)(c(cc1C(F)(F)F)ccc1Cl)=O Chemical compound O=S(c(cc1)ccc1N(C=CN1)C1=S)(c(cc1C(F)(F)F)ccc1Cl)=O RLCFHQSJTSVRHI-UHFFFAOYSA-N 0.000 description 1
- FOTLYDRVDFFNIJ-UHFFFAOYSA-N O=S(c(cc1)ccc1N=C=S)(c(cc1)cc(C(F)(F)F)c1Cl)=O Chemical compound O=S(c(cc1)ccc1N=C=S)(c(cc1)cc(C(F)(F)F)c1Cl)=O FOTLYDRVDFFNIJ-UHFFFAOYSA-N 0.000 description 1
- KFGJUXQSOMLBHN-UHFFFAOYSA-N O=S(c(cc1)ccc1N=C=S)(c1cc(C(F)(F)F)ccn1)=O Chemical compound O=S(c(cc1)ccc1N=C=S)(c1cc(C(F)(F)F)ccn1)=O KFGJUXQSOMLBHN-UHFFFAOYSA-N 0.000 description 1
- FOMSGBYEGHXIGM-UHFFFAOYSA-N O=S(c1ccc(CN(C=NN2)C2=S)cc1)(c1cc(C(F)(F)F)ccn1)=O Chemical compound O=S(c1ccc(CN(C=NN2)C2=S)cc1)(c1cc(C(F)(F)F)ccn1)=O FOMSGBYEGHXIGM-UHFFFAOYSA-N 0.000 description 1
- RREQHIRSFDYSRZ-UHFFFAOYSA-N O=S(c1ccccc1)(c(cc1)ccc1N=C=S)=O Chemical compound O=S(c1ccccc1)(c(cc1)ccc1N=C=S)=O RREQHIRSFDYSRZ-UHFFFAOYSA-N 0.000 description 1
- DXRVYZGVVFZCFP-UHFFFAOYSA-N [O-][N+](c(c(Br)c1)ccc1Br)=O Chemical compound [O-][N+](c(c(Br)c1)ccc1Br)=O DXRVYZGVVFZCFP-UHFFFAOYSA-N 0.000 description 1
- OOCXIQYEGGBCQA-UHFFFAOYSA-N [O-][N+](c(c(N1CCCCC1)c1)ccc1Br)=O Chemical compound [O-][N+](c(c(N1CCCCC1)c1)ccc1Br)=O OOCXIQYEGGBCQA-UHFFFAOYSA-N 0.000 description 1
- LLCDEFQWBSNEML-UHFFFAOYSA-N [O-][N+](c(c(N1CCCCC1)c1)ccc1S(c(cc1)cc(C(F)(F)F)c1Cl)(=O)=O)=O Chemical compound [O-][N+](c(c(N1CCCCC1)c1)ccc1S(c(cc1)cc(C(F)(F)F)c1Cl)(=O)=O)=O LLCDEFQWBSNEML-UHFFFAOYSA-N 0.000 description 1
- WPOSXCOIYOPEMJ-UHFFFAOYSA-N [O-][N+](c(cc1)ccc1Sc1cc(C(F)(F)F)ccn1)=O Chemical compound [O-][N+](c(cc1)ccc1Sc1cc(C(F)(F)F)ccn1)=O WPOSXCOIYOPEMJ-UHFFFAOYSA-N 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/70—One oxygen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/84—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 true JP2021527692A (ja) | 2021-10-14 |
| JPWO2019246454A5 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 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002098851A1 (en) * | 2001-06-04 | 2002-12-12 | Institut Fiziologicheski Aktivnykh Veschestv Rossiyskov Akademii Nauk | Derivatives 0f n,s-substitutions n'-1 [(hetero)aryl] alkyl-n'-[hetero) aryl] methyl isothioureas, method for producing salts and bases thereof, physiologically active n,s-substitutions n'-1 [(hetero)aryl] alkyl-n'-[hetero) aryl] methyl isothioureas, a pharmaceutical composition and curing method |
| WO2013175215A1 (en) * | 2012-05-22 | 2013-11-28 | Autifony Therapeutics Limited | Triazoles as kv3 inhibitors |
| JP7277473B2 (ja) * | 2017-10-30 | 2023-05-19 | ニューロポア セラピーズ インコーポレイテッド | 置換フェニルスルホニルフェニルトリアゾールチオンおよびその使用法 |
| JP2023076473A (ja) * | 2017-03-08 | 2023-06-01 | 長江存儲科技有限責任公司 | 3次元メモリデバイスのスルーアレイコンタクト構造 |
Family Cites Families (1)
| 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 |
-
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
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002098851A1 (en) * | 2001-06-04 | 2002-12-12 | Institut Fiziologicheski Aktivnykh Veschestv Rossiyskov Akademii Nauk | Derivatives 0f n,s-substitutions n'-1 [(hetero)aryl] alkyl-n'-[hetero) aryl] methyl isothioureas, method for producing salts and bases thereof, physiologically active n,s-substitutions n'-1 [(hetero)aryl] alkyl-n'-[hetero) aryl] methyl isothioureas, a pharmaceutical composition and curing method |
| WO2013175215A1 (en) * | 2012-05-22 | 2013-11-28 | Autifony Therapeutics Limited | Triazoles as kv3 inhibitors |
| JP2023076473A (ja) * | 2017-03-08 | 2023-06-01 | 長江存儲科技有限責任公司 | 3次元メモリデバイスのスルーアレイコンタクト構造 |
| JP7277473B2 (ja) * | 2017-10-30 | 2023-05-19 | ニューロポア セラピーズ インコーポレイテッド | 置換フェニルスルホニルフェニルトリアゾールチオンおよびその使用法 |
Non-Patent Citations (2)
| Title |
|---|
| J. NEURAL. TRANSM. (VIENNA), vol. 116, no. 9, JPN6023026724, 2009, pages 1079 - 1086, ISSN: 0005269742 * |
| 日薬理誌, vol. 122, no. 1, JPN6023026723, 2003, pages 55 - 64, ISSN: 0005095406 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3810133A1 (en) | 2021-04-28 |
| WO2019246454A1 (en) | 2019-12-26 |
| US20210290597A1 (en) | 2021-09-23 |
| CN112512523A (zh) | 2021-03-16 |
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