JPWO2019139869A5 - - Google Patents
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- JPWO2019139869A5 JPWO2019139869A5 JP2020538987A JP2020538987A JPWO2019139869A5 JP WO2019139869 A5 JPWO2019139869 A5 JP WO2019139869A5 JP 2020538987 A JP2020538987 A JP 2020538987A JP 2020538987 A JP2020538987 A JP 2020538987A JP WO2019139869 A5 JPWO2019139869 A5 JP WO2019139869A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- heterocyclyl
- pharmaceutical composition
- aralkyl
- Prior art date
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 description 68
- 229910052739 hydrogen Inorganic materials 0.000 description 48
- 239000001257 hydrogen Substances 0.000 description 48
- 238000000034 method Methods 0.000 description 48
- 125000000623 heterocyclic group Chemical group 0.000 description 44
- 239000008194 pharmaceutical composition Substances 0.000 description 41
- 125000003710 aryl alkyl group Chemical group 0.000 description 36
- 125000003118 aryl group Chemical group 0.000 description 36
- 125000001072 heteroaryl group Chemical group 0.000 description 36
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 34
- 150000002431 hydrogen Chemical class 0.000 description 31
- 125000001424 substituent group Chemical group 0.000 description 30
- 125000003545 alkoxy group Chemical group 0.000 description 29
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 description 28
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 28
- 150000001345 alkine derivatives Chemical class 0.000 description 28
- 239000000203 mixture Substances 0.000 description 28
- 125000005843 halogen group Chemical group 0.000 description 26
- 125000004093 cyano group Chemical group *C#N 0.000 description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 17
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 16
- 150000001875 compounds Chemical class 0.000 description 16
- 229910052805 deuterium Inorganic materials 0.000 description 16
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 15
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 12
- 230000004770 neurodegeneration Effects 0.000 description 10
- 208000015122 neurodegenerative disease Diseases 0.000 description 10
- 239000000651 prodrug Substances 0.000 description 10
- 229940002612 prodrug Drugs 0.000 description 10
- 150000003839 salts Chemical class 0.000 description 10
- 239000012453 solvate Substances 0.000 description 10
- 208000024827 Alzheimer disease Diseases 0.000 description 8
- 125000003342 alkenyl group Chemical group 0.000 description 8
- 125000000304 alkynyl group Chemical group 0.000 description 8
- 125000000753 cycloalkyl group Chemical group 0.000 description 8
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 description 8
- 239000000126 substance Substances 0.000 description 8
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 7
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 7
- 239000005711 Benzoic acid Substances 0.000 description 6
- 125000004422 alkyl sulphonamide group Chemical group 0.000 description 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 6
- 235000010233 benzoic acid Nutrition 0.000 description 6
- 125000001153 fluoro group Chemical group F* 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 4
- -1 4- (4-cyanophenyl) piperidine-1-carbonyl Chemical group 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000006186 oral dosage form Substances 0.000 description 3
- YPMKPCAILYDVBN-UHFFFAOYSA-N (2-methylphenyl) benzoate Chemical group CC1=CC=CC=C1OC(=O)C1=CC=CC=C1 YPMKPCAILYDVBN-UHFFFAOYSA-N 0.000 description 2
- NWFKBPLDXGCDKS-UHFFFAOYSA-N 3-[(3,5-dimethoxyphenyl)sulfamoyl]benzoic acid Chemical compound COC1=CC(OC)=CC(NS(=O)(=O)C=2C=C(C=CC=2)C(O)=O)=C1 NWFKBPLDXGCDKS-UHFFFAOYSA-N 0.000 description 2
- PQQOVHKHXHTFRM-UHFFFAOYSA-N 4-(2,4-dichlorophenyl)-1-ethyl-2-[(4-phenylphenyl)methyl]imidazole Chemical compound CCN1C=C(N=C1CC2=CC=C(C=C2)C3=CC=CC=C3)C4=C(C=C(C=C4)Cl)Cl PQQOVHKHXHTFRM-UHFFFAOYSA-N 0.000 description 2
- ZRVJBWOTSBBSEB-UHFFFAOYSA-N CC1=C(NS(=O)(=O)C2=CC=CC(=C2)C(O)=O)C=C(C=C1)C(F)(F)F Chemical compound CC1=C(NS(=O)(=O)C2=CC=CC(=C2)C(O)=O)C=C(C=C1)C(F)(F)F ZRVJBWOTSBBSEB-UHFFFAOYSA-N 0.000 description 2
- 108010064397 amyloid beta-protein (1-40) Proteins 0.000 description 2
- 108010064539 amyloid beta-protein (1-42) Proteins 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 2
- 206010012289 Dementia Diseases 0.000 description 1
- 201000010374 Down Syndrome Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 208000030886 Traumatic Brain injury Diseases 0.000 description 1
- 206010044688 Trisomy 21 Diseases 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000006207 intravenous dosage form Substances 0.000 description 1
- 230000000155 isotopic effect Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 239000006201 parenteral dosage form Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000009529 traumatic brain injury Effects 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023144990A JP2023182589A (ja) | 2018-01-10 | 2023-09-07 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| JP2025165134A JP2026021312A (ja) | 2018-01-10 | 2025-10-01 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862615869P | 2018-01-10 | 2018-01-10 | |
| US62/615,869 | 2018-01-10 | ||
| PCT/US2019/012608 WO2019139869A1 (en) | 2018-01-10 | 2019-01-08 | Pharmaceutical compositions comprising phenylsulfonamides, and their therapeutic applications |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023144990A Division JP2023182589A (ja) | 2018-01-10 | 2023-09-07 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021510168A JP2021510168A (ja) | 2021-04-15 |
| JPWO2019139869A5 true JPWO2019139869A5 (https=) | 2022-01-18 |
| JP2021510168A5 JP2021510168A5 (https=) | 2022-01-18 |
| JP7395480B2 JP7395480B2 (ja) | 2023-12-11 |
Family
ID=65411932
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020538987A Active JP7395480B2 (ja) | 2018-01-10 | 2019-01-08 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| JP2023144990A Pending JP2023182589A (ja) | 2018-01-10 | 2023-09-07 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| JP2025165134A Pending JP2026021312A (ja) | 2018-01-10 | 2025-10-01 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023144990A Pending JP2023182589A (ja) | 2018-01-10 | 2023-09-07 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| JP2025165134A Pending JP2026021312A (ja) | 2018-01-10 | 2025-10-01 | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US11701334B2 (https=) |
| EP (1) | EP3737382A1 (https=) |
| JP (3) | JP7395480B2 (https=) |
| AU (2) | AU2019207491A1 (https=) |
| CA (1) | CA3087856A1 (https=) |
| TW (2) | TWI823890B (https=) |
| WO (1) | WO2019139869A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7395480B2 (ja) | 2018-01-10 | 2023-12-11 | クラ セラピューティクス, エルエルシー | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| EP3997068A1 (en) * | 2019-07-11 | 2022-05-18 | Cura Therapeutics, LLC | Sulfone compounds and pharmaceutical compositions thereof, and their therapeutic applications for the treatment of neurodegenerative diseases |
| CA3146159A1 (en) * | 2019-07-11 | 2021-01-14 | Cura Therapeutics, Llc | Phenyl compounds and pharmaceutical compositions thereof, and their therapeutic applications |
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| WO2017160069A1 (ko) | 2016-03-15 | 2017-09-21 | 재단법인 의약바이오컨버젼스연구단 | 신규한 벤젠설폰아미드 유도체 및 이의 용도 |
| CN109081818B (zh) | 2017-06-14 | 2022-04-22 | 南京华威医药科技集团有限公司 | 新型吲哚胺2,3-双加氧化酶抑制剂 |
| CN109651208B (zh) | 2017-10-10 | 2022-01-04 | 中国科学院上海药物研究所 | N-芳基磺酰胺类化合物,其药物组合物及其用途 |
| JP7395480B2 (ja) * | 2018-01-10 | 2023-12-11 | クラ セラピューティクス, エルエルシー | フェニルスルホンアミドを含む薬学的組成物、及びそれらの治療的適用 |
| CN109293537A (zh) | 2018-11-12 | 2019-02-01 | 中国药科大学 | 磺酰胺类化合物及其医药用途 |
| CA3146159A1 (en) * | 2019-07-11 | 2021-01-14 | Cura Therapeutics, Llc | Phenyl compounds and pharmaceutical compositions thereof, and their therapeutic applications |
| EP3997068A1 (en) | 2019-07-11 | 2022-05-18 | Cura Therapeutics, LLC | Sulfone compounds and pharmaceutical compositions thereof, and their therapeutic applications for the treatment of neurodegenerative diseases |
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2019
- 2019-01-08 JP JP2020538987A patent/JP7395480B2/ja active Active
- 2019-01-08 CA CA3087856A patent/CA3087856A1/en active Pending
- 2019-01-08 TW TW108100722A patent/TWI823890B/zh active
- 2019-01-08 WO PCT/US2019/012608 patent/WO2019139869A1/en not_active Ceased
- 2019-01-08 TW TW112141994A patent/TW202406538A/zh unknown
- 2019-01-08 EP EP19705255.8A patent/EP3737382A1/en active Pending
- 2019-01-08 US US16/961,191 patent/US11701334B2/en active Active
- 2019-01-08 AU AU2019207491A patent/AU2019207491A1/en not_active Abandoned
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2023
- 2023-06-02 US US18/205,283 patent/US20240016768A1/en not_active Abandoned
- 2023-09-07 JP JP2023144990A patent/JP2023182589A/ja active Pending
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2024
- 2024-08-28 US US18/817,959 patent/US20250177334A1/en active Pending
- 2024-11-07 AU AU2024259810A patent/AU2024259810A1/en active Pending
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2025
- 2025-10-01 JP JP2025165134A patent/JP2026021312A/ja active Pending
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