BR112019020111A2 - saxitoxinas 11,13-modificadas para o tratamento de dor - Google Patents
saxitoxinas 11,13-modificadas para o tratamento de dor Download PDFInfo
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- BR112019020111A2 BR112019020111A2 BR112019020111A BR112019020111A BR112019020111A2 BR 112019020111 A2 BR112019020111 A2 BR 112019020111A2 BR 112019020111 A BR112019020111 A BR 112019020111A BR 112019020111 A BR112019020111 A BR 112019020111A BR 112019020111 A2 BR112019020111 A2 BR 112019020111A2
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- Prior art keywords
- alkyl
- halo
- compound
- petition
- formula
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- 150000005621 tetraalkylammonium salts Chemical class 0.000 description 1
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- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
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- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
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- ZEWQUBUPAILYHI-UHFFFAOYSA-N trifluoperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 ZEWQUBUPAILYHI-UHFFFAOYSA-N 0.000 description 1
- 229960002324 trifluoperazine Drugs 0.000 description 1
- PBIMIGNDTBRRPI-UHFFFAOYSA-N trifluoro borate Chemical compound FOB(OF)OF PBIMIGNDTBRRPI-UHFFFAOYSA-N 0.000 description 1
- PNQBEPDZQUOCNY-UHFFFAOYSA-N trifluoroacetyl chloride Chemical compound FC(F)(F)C(Cl)=O PNQBEPDZQUOCNY-UHFFFAOYSA-N 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 125000000025 triisopropylsilyl group Chemical group C(C)(C)[Si](C(C)C)(C(C)C)* 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- LZTRCELOJRDYMQ-UHFFFAOYSA-N triphenylmethanol Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(O)C1=CC=CC=C1 LZTRCELOJRDYMQ-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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| US201762478523P | 2017-03-29 | 2017-03-29 | |
| PCT/US2018/025301 WO2018183781A1 (en) | 2017-03-29 | 2018-03-29 | 11,13-modified saxitoxins for the treatment of pain |
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| BR112019020111A BR112019020111A2 (pt) | 2017-03-29 | 2018-03-29 | saxitoxinas 11,13-modificadas para o tratamento de dor |
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| BR112019020111A2 (pt) | 2017-03-29 | 2020-05-05 | Siteone Therapeutics Inc | saxitoxinas 11,13-modificadas para o tratamento de dor |
| 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 |
| US12162886B2 (en) | 2018-10-03 | 2024-12-10 | 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 |
| HUE069128T2 (hu) | 2019-12-06 | 2025-02-28 | Vertex Pharma | Szubsztituált tetrahidrofurán vegyületek mint nátriumcsatornák modulátorai |
| 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 |
| US20240285596A1 (en) | 2021-06-04 | 2024-08-29 | Vertex Pharmaceuticals Incorporated | Solid dosage forms and dosing regimens comprising (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-methoxy-phenyl)-4,5-dimethyl-5-(trifluoromethyl) tetrahydrofuran-2-carbonyl]amino]pyridine-2-carboxamide |
| AU2022284886A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamides as modulators of sodium channels |
| US20240294512A1 (en) | 2021-06-04 | 2024-09-05 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| US20240368135A1 (en) | 2021-06-04 | 2024-11-07 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| JP2025513454A (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 |
| AU2023255558A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| CN119522214A (zh) | 2022-04-22 | 2025-02-25 | 沃泰克斯药物股份有限公司 | 用于治疗疼痛的杂芳基化合物 |
| TW202404969A (zh) | 2022-04-22 | 2024-02-01 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| KR20250120351A (ko) | 2022-12-06 | 2025-08-08 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법 |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| TW202523313A (zh) | 2023-10-23 | 2025-06-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090511A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing modulators of sodium channels and solid forms of the same for treating pain |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating pain |
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| 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 |
| BR112019020111A2 (pt) | 2017-03-29 | 2020-05-05 | Siteone Therapeutics Inc | saxitoxinas 11,13-modificadas para o tratamento de dor |
| US12162886B2 (en) | 2018-10-03 | 2024-12-10 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
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-
2018
- 2018-03-29 BR BR112019020111A patent/BR112019020111A2/pt not_active Application Discontinuation
- 2018-03-29 CA CA3058214A patent/CA3058214A1/en active Pending
- 2018-03-29 EP EP18720448.2A patent/EP3601291A1/en active Pending
- 2018-03-29 CN CN201880035534.4A patent/CN110831945B/zh active Active
- 2018-03-29 KR KR1020197031530A patent/KR20200012833A/ko not_active Ceased
- 2018-03-29 AU AU2018243463A patent/AU2018243463C1/en active Active
- 2018-03-29 MX MX2019011530A patent/MX2019011530A/es unknown
- 2018-03-29 US US16/499,205 patent/US11236097B2/en active Active
- 2018-03-29 WO PCT/US2018/025301 patent/WO2018183781A1/en not_active Ceased
- 2018-03-29 JP JP2019553572A patent/JP7090100B2/ja active Active
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2019
- 2019-09-24 IL IL269599A patent/IL269599B2/en unknown
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2022
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| CN110831945A (zh) | 2020-02-21 |
| JP2020515610A (ja) | 2020-05-28 |
| IL269599A (en) | 2019-11-28 |
| KR20200012833A (ko) | 2020-02-05 |
| IL269599B1 (en) | 2023-03-01 |
| CA3058214A1 (en) | 2018-10-04 |
| AU2018243463A8 (en) | 2019-11-07 |
| MX2019011530A (es) | 2020-01-27 |
| US11834456B2 (en) | 2023-12-05 |
| RU2019134300A (ru) | 2021-04-29 |
| CN110831945B (zh) | 2023-08-08 |
| WO2018183781A1 (en) | 2018-10-04 |
| US11236097B2 (en) | 2022-02-01 |
| RU2019134300A3 (enExample) | 2021-05-25 |
| AU2018243463B2 (en) | 2022-05-19 |
| US20220259218A1 (en) | 2022-08-18 |
| IL269599B2 (en) | 2023-07-01 |
| AU2018243463A1 (en) | 2019-10-31 |
| JP7090100B2 (ja) | 2022-06-23 |
| EP3601291A1 (en) | 2020-02-05 |
| AU2018243463C1 (en) | 2022-12-01 |
| US20200102318A1 (en) | 2020-04-02 |
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