JP2020515610A5 - - Google Patents
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- JP2020515610A5 JP2020515610A5 JP2019553572A JP2019553572A JP2020515610A5 JP 2020515610 A5 JP2020515610 A5 JP 2020515610A5 JP 2019553572 A JP2019553572 A JP 2019553572A JP 2019553572 A JP2019553572 A JP 2019553572A JP 2020515610 A5 JP2020515610 A5 JP 2020515610A5
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- JP
- Japan
- Prior art keywords
- alkyl
- halo
- compound according
- compound
- hydrogen
- 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 claims description 111
- 150000001875 compounds Chemical class 0.000 claims description 106
- 125000003545 alkoxy group Chemical group 0.000 claims description 44
- 239000001257 hydrogen Substances 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 44
- 125000001475 halogen functional group Chemical group 0.000 claims description 38
- 150000003839 salts Chemical class 0.000 claims description 30
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- 208000002193 Pain Diseases 0.000 claims description 25
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 22
- 125000003118 aryl group Chemical group 0.000 claims description 21
- 239000000203 mixture Substances 0.000 claims description 20
- 150000002431 hydrogen Chemical class 0.000 claims description 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 17
- 125000004104 aryloxy group Chemical group 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 239000012453 solvate Substances 0.000 claims description 15
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- -1 halo-C 1-6 alkylthio Chemical group 0.000 claims description 9
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims description 8
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 8
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims description 8
- 125000005138 alkoxysulfonyl group Chemical group 0.000 claims description 8
- 235000010290 biphenyl Nutrition 0.000 claims description 8
- 150000004074 biphenyls Chemical group 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 241000124008 Mammalia Species 0.000 claims description 7
- 150000004677 hydrates Chemical class 0.000 claims description 6
- 125000004802 cyanophenyl group Chemical group 0.000 claims description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 206010015958 Eye pain Diseases 0.000 claims description 4
- 230000001154 acute effect Effects 0.000 claims description 4
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 4
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims description 4
- 206010011224 Cough Diseases 0.000 claims description 3
- 208000003251 Pruritus Diseases 0.000 claims description 3
- 125000001544 thienyl group Chemical group 0.000 claims description 3
- 206010058019 Cancer Pain Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 208000000094 Chronic Pain Diseases 0.000 claims description 2
- 208000006561 Cluster Headache Diseases 0.000 claims description 2
- 206010061788 Corneal infection Diseases 0.000 claims description 2
- 208000028006 Corneal injury Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 2
- 206010013774 Dry eye Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 206010015150 Erythema Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 208000010412 Glaucoma Diseases 0.000 claims description 2
- 208000007514 Herpes zoster Diseases 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000004550 Postoperative Pain Diseases 0.000 claims description 2
- 208000027520 Somatoform disease Diseases 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 125000002047 benzodioxolyl group Chemical group O1OC(C2=C1C=CC=C2)* 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000003016 chromanyl group Chemical group O1C(CCC2=CC=CC=C12)* 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 208000018912 cluster headache syndrome Diseases 0.000 claims description 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 231100000321 erythema Toxicity 0.000 claims description 2
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 208000004296 neuralgia Diseases 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 208000027753 pain disease Diseases 0.000 claims description 2
- 230000001314 paroxysmal effect Effects 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 210000003497 sciatic nerve Anatomy 0.000 claims description 2
- 238000001356 surgical procedure Methods 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 208000020049 trigeminal nerve disease Diseases 0.000 claims description 2
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims 1
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims 1
- 238000000034 method Methods 0.000 description 15
- 0 CC(*1)(CN(C2)C(NC[C@@](C=*3)NC3=[N+])=NC)[C@@]2N1C(C)=O Chemical compound CC(*1)(CN(C2)C(NC[C@@](C=*3)NC3=[N+])=NC)[C@@]2N1C(C)=O 0.000 description 12
- DIAAYZGONSGOTP-UHFFFAOYSA-N Cc1cccc2c1OCCC21CC1 Chemical compound Cc1cccc2c1OCCC21CC1 DIAAYZGONSGOTP-UHFFFAOYSA-N 0.000 description 2
- 108010052164 Sodium Channels Proteins 0.000 description 2
- 102000018674 Sodium Channels Human genes 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 125000005842 heteroatom Chemical group 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- RPQXVSUAYFXFJA-HGRQIUPRSA-N saxitoxin Chemical class NC(=O)OC[C@@H]1N=C(N)N2CCC(O)(O)[C@@]22N=C(N)N[C@@H]12 RPQXVSUAYFXFJA-HGRQIUPRSA-N 0.000 description 2
- XJWNRCKYCHREJD-UHFFFAOYSA-N CC(C)c1c2OCCC3(CCC3)c2ccc1 Chemical compound CC(C)c1c2OCCC3(CCC3)c2ccc1 XJWNRCKYCHREJD-UHFFFAOYSA-N 0.000 description 1
- ZAVDOSIMBQUKCN-UHFFFAOYSA-N CCc1cccc2c1OCC21CC1 Chemical compound CCc1cccc2c1OCC21CC1 ZAVDOSIMBQUKCN-UHFFFAOYSA-N 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762478523P | 2017-03-29 | 2017-03-29 | |
| US62/478,523 | 2017-03-29 | ||
| PCT/US2018/025301 WO2018183781A1 (en) | 2017-03-29 | 2018-03-29 | 11,13-modified saxitoxins for the treatment of pain |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020515610A JP2020515610A (ja) | 2020-05-28 |
| JP2020515610A5 true JP2020515610A5 (enExample) | 2021-05-20 |
| JP7090100B2 JP7090100B2 (ja) | 2022-06-23 |
Family
ID=62063184
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019553572A Active JP7090100B2 (ja) | 2017-03-29 | 2018-03-29 | 疼痛の処置のための１１，１３－修飾サキシトキシン： |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11236097B2 (enExample) |
| EP (1) | EP3601291B1 (enExample) |
| JP (1) | JP7090100B2 (enExample) |
| KR (1) | KR20200012833A (enExample) |
| CN (1) | CN110831945B (enExample) |
| AU (1) | AU2018243463C1 (enExample) |
| BR (1) | BR112019020111A2 (enExample) |
| CA (1) | CA3058214A1 (enExample) |
| IL (1) | IL269599B2 (enExample) |
| MX (1) | MX2019011530A (enExample) |
| WO (1) | WO2018183781A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020515611A (ja) * | 2017-03-29 | 2020-05-28 | サイトワン セラピューティクス， インコーポレイテッド | 疼痛の処置のための１１，１３−修飾サキシトキシン |
| CA3058214A1 (en) | 2017-03-29 | 2018-10-04 | The Board Of Trustees Of The Leland Stanford Junior University | 11,13-modified saxitoxins for the treatment of pain |
| EP3860714B1 (en) | 2018-10-03 | 2023-09-06 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| CN110128292A (zh) * | 2019-06-12 | 2019-08-16 | 成都美域高制药有限公司 | 一种Ozanimod中间体4-氰基茚酮的合成方法 |
| PH12022551379A1 (en) | 2019-12-06 | 2023-05-03 | Vertex Pharma | Substituted tetrahydrofurans as modulators of sodium channels |
| SMT202600064T1 (it) | 2021-06-04 | 2026-03-09 | Vertex Pharma | Forme farmaceutiche solide e regimi di dosaggio comprendenti (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-metossi-fenil)-4,5-dimetil-5-(trifluorometil) tetraidrofuran-2-carbonil]ammino]piridin-2-carbossammide |
| WO2022256842A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| SI4347031T1 (sl) | 2021-06-04 | 2026-01-30 | Vertex Pharmaceuticals Incorporated | N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov |
| US20240368135A1 (en) | 2021-06-04 | 2024-11-07 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| CA3221939A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| CN117794918A (zh) | 2021-06-04 | 2024-03-29 | 沃泰克斯药物股份有限公司 | 经取代的四氢呋喃类似物作为钠通道调节剂 |
| IL316422A (en) | 2022-04-22 | 2024-12-01 | Vertex Pharma | Heteroaryl compounds for pain treatment |
| AU2023257313A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| AU2023255558A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| JP2025513455A (ja) | 2022-04-22 | 2025-04-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | 疼痛の治療のためのヘテロアリール化合物 |
| KR20250120351A (ko) | 2022-12-06 | 2025-08-08 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법 |
| TW202535867A (zh) | 2023-10-23 | 2025-09-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之鈉通道調節劑及其固體形式的製備方法 |
| KR20260116140A (ko) | 2023-10-23 | 2026-07-28 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료를 위한 헤테로아릴 화합물 |
| KR20260116141A (ko) | 2023-10-23 | 2026-07-28 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료용 화합물 및 이의 고체 형태의 제조방법 |
| KR20260118418A (ko) | 2023-10-23 | 2026-07-30 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료를 위한 헤테로아릴 화합물 |
| AU2024393245A1 (en) | 2023-12-07 | 2026-06-18 | Vertex Pharmaceuticals Incorporated | Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic pain |
| TW202606663A (zh) | 2024-06-28 | 2026-02-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| LU605402B1 (en) | 2024-07-11 | 2026-07-14 | Sea4Us Biotecnologia E Recursos Marinhos Sa | Oxazolidone-derived compounds and their use in the treatment of chronic and acute pain |
| WO2026030525A1 (en) | 2024-07-31 | 2026-02-05 | Vertex Pharmaceuticals Incorporated | Zilvetrigine dosage forms and dosing regimens for treating pain |
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| CA2944549A1 (en) * | 2014-04-09 | 2015-10-15 | Siteone Therapeutics, Inc. | 10',11'-modified saxitoxin useful for the treatment of pain |
| AU2016329201A1 (en) | 2015-09-30 | 2018-04-26 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| JP2020515611A (ja) | 2017-03-29 | 2020-05-28 | サイトワン セラピューティクス， インコーポレイテッド | 疼痛の処置のための１１，１３−修飾サキシトキシン |
| CA3058214A1 (en) | 2017-03-29 | 2018-10-04 | The Board Of Trustees Of The Leland Stanford Junior University | 11,13-modified saxitoxins for the treatment of pain |
| EP3860714B1 (en) | 2018-10-03 | 2023-09-06 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| EP4196482B1 (en) | 2020-08-14 | 2025-10-01 | SiteOne Therapeutics, Inc. | Non-hydrated ketone inhibitors of nav1.7 for the treatment of pain |
-
2018
- 2018-03-29 CA CA3058214A patent/CA3058214A1/en active Pending
- 2018-03-29 EP EP18720448.2A patent/EP3601291B1/en active Active
- 2018-03-29 BR BR112019020111-4A patent/BR112019020111A2/pt not_active Application Discontinuation
- 2018-03-29 MX MX2019011530A patent/MX2019011530A/es unknown
- 2018-03-29 WO PCT/US2018/025301 patent/WO2018183781A1/en not_active Ceased
- 2018-03-29 JP JP2019553572A patent/JP7090100B2/ja active Active
- 2018-03-29 CN CN201880035534.4A patent/CN110831945B/zh active Active
- 2018-03-29 AU AU2018243463A patent/AU2018243463C1/en active Active
- 2018-03-29 KR KR1020197031530A patent/KR20200012833A/ko not_active Ceased
- 2018-03-29 US US16/499,205 patent/US11236097B2/en active Active
-
2019
- 2019-09-24 IL IL269599A patent/IL269599B2/en unknown
-
2022
- 2022-01-26 US US17/585,530 patent/US11834456B2/en active Active
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