CN110831945B - 用于治疗疼痛的11,13-修饰的石房蛤毒素类化合物 - Google Patents
用于治疗疼痛的11,13-修饰的石房蛤毒素类化合物 Download PDFInfo
- Publication number
- CN110831945B CN110831945B CN201880035534.4A CN201880035534A CN110831945B CN 110831945 B CN110831945 B CN 110831945B CN 201880035534 A CN201880035534 A CN 201880035534A CN 110831945 B CN110831945 B CN 110831945B
- Authority
- CN
- China
- Prior art keywords
- compound
- alkyl
- formula
- pharmaceutically acceptable
- pain
- 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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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]
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762478523P | 2017-03-29 | 2017-03-29 | |
| US62/478523 | 2017-03-29 | ||
| PCT/US2018/025301 WO2018183781A1 (en) | 2017-03-29 | 2018-03-29 | 11,13-modified saxitoxins for the treatment of pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN110831945A CN110831945A (zh) | 2020-02-21 |
| CN110831945B true CN110831945B (zh) | 2023-08-08 |
Family
ID=62063184
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880035534.4A Active CN110831945B (zh) | 2017-03-29 | 2018-03-29 | 用于治疗疼痛的11,13-修饰的石房蛤毒素类化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11236097B2 (enExample) |
| EP (1) | EP3601291A1 (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 (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018243463C1 (en) | 2017-03-29 | 2022-12-01 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| WO2018183782A1 (en) * | 2017-03-29 | 2018-10-04 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| WO2020072835A1 (en) | 2018-10-03 | 2020-04-09 | 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 |
| MX2022006865A (es) | 2019-12-06 | 2022-07-11 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio. |
| JP2024520648A (ja) | 2021-06-04 | 2024-05-24 | 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 | ナトリウムチャネルの調節因子としての置換テトラヒドロフラン-2-カルボキサミド |
| WO2022256842A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| WO2022256676A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| DK4347031T3 (da) | 2021-06-04 | 2025-12-01 | Vertex Pharma | N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| BR112023025264A2 (pt) | 2021-06-04 | 2024-02-20 | Vertex Pharma | Formas farmacêuticas sólidas e regimes posológicos compreendendo (2r,3s,4s,5r)-4-[[3- (3,4-difluoro-2-metóxi-fenil)-4,5-dimetil-5-(trifluorometil) tetra-hidrofuran-2-carbonil]amino ]piridina-2-carboxamida |
| EP4511117A1 (en) | 2022-04-22 | 2025-02-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| CA3256604A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | HETEROARYL COMPOUNDS FOR PAIN RELIEF |
| 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 |
| GEAP202516632A (en) | 2022-04-22 | 2025-02-25 | Vertex Pharma | Heteroaryl compounds for the treatment of pain |
| CN120603815A (zh) | 2022-12-06 | 2025-09-05 | 沃泰克斯药物股份有限公司 | 钠通道的取代四氢呋喃调节剂的合成方法 |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| WO2025090465A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| 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 |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating pain |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN102459273A (zh) * | 2009-05-07 | 2012-05-16 | 里兰斯坦福初级大学理事会 | 用于研究、成像以及治疗疼痛的方法和组合物 |
| CN102811722A (zh) * | 2010-02-10 | 2012-12-05 | 菲特托克斯有限公司 | 用石房蛤毒素衍生物对触觉丧失进行的治疗 |
| US20170029431A1 (en) * | 2014-04-09 | 2017-02-02 | Siteone Therapeutics, Inc. | 10',11'-modified saxitoxins useful for the treatment of pain |
| WO2017059385A1 (en) * | 2015-09-30 | 2017-04-06 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
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| AU2018243463C1 (en) | 2017-03-29 | 2022-12-01 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| WO2018183782A1 (en) | 2017-03-29 | 2018-10-04 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| WO2020072835A1 (en) | 2018-10-03 | 2020-04-09 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
| US20230339958A1 (en) | 2020-08-14 | 2023-10-26 | Siteone Therapeutics, Inc. | Non-hydrated ketone inhibitors of nav1.7 for the treatment of pain |
-
2018
- 2018-03-29 AU AU2018243463A patent/AU2018243463C1/en active Active
- 2018-03-29 JP JP2019553572A patent/JP7090100B2/ja active Active
- 2018-03-29 KR KR1020197031530A patent/KR20200012833A/ko not_active Ceased
- 2018-03-29 WO PCT/US2018/025301 patent/WO2018183781A1/en not_active Ceased
- 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 US US16/499,205 patent/US11236097B2/en active Active
- 2018-03-29 MX MX2019011530A patent/MX2019011530A/es unknown
- 2018-03-29 BR BR112019020111A patent/BR112019020111A2/pt not_active Application Discontinuation
- 2018-03-29 CA CA3058214A patent/CA3058214A1/en active Pending
-
2019
- 2019-09-24 IL IL269599A patent/IL269599B2/en unknown
-
2022
- 2022-01-26 US US17/585,530 patent/US11834456B2/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102459273A (zh) * | 2009-05-07 | 2012-05-16 | 里兰斯坦福初级大学理事会 | 用于研究、成像以及治疗疼痛的方法和组合物 |
| CN102811722A (zh) * | 2010-02-10 | 2012-12-05 | 菲特托克斯有限公司 | 用石房蛤毒素衍生物对触觉丧失进行的治疗 |
| US20170029431A1 (en) * | 2014-04-09 | 2017-02-02 | Siteone Therapeutics, Inc. | 10',11'-modified saxitoxins useful for the treatment of pain |
| WO2017059385A1 (en) * | 2015-09-30 | 2017-04-06 | Siteone Therapeutics, Inc. | 11,13-modified saxitoxins for the treatment of pain |
Non-Patent Citations (1)
| Title |
|---|
| Synthesis of saxitoxin derivatives bearing guanidine and urea groups at C13 and evaluation of their inhibitory activity on voltage-gated sodium channels;Takafumi Akimoto,等;《Organic & Biomolecular Chemistry》;20130808;第11卷(第38期);6642-6649 * |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2019134300A (ru) | 2021-04-29 |
| MX2019011530A (es) | 2020-01-27 |
| US20200102318A1 (en) | 2020-04-02 |
| IL269599B1 (en) | 2023-03-01 |
| AU2018243463C1 (en) | 2022-12-01 |
| AU2018243463A1 (en) | 2019-10-31 |
| CA3058214A1 (en) | 2018-10-04 |
| IL269599B2 (en) | 2023-07-01 |
| AU2018243463B2 (en) | 2022-05-19 |
| JP2020515610A (ja) | 2020-05-28 |
| US20220259218A1 (en) | 2022-08-18 |
| WO2018183781A1 (en) | 2018-10-04 |
| EP3601291A1 (en) | 2020-02-05 |
| US11834456B2 (en) | 2023-12-05 |
| AU2018243463A8 (en) | 2019-11-07 |
| JP7090100B2 (ja) | 2022-06-23 |
| BR112019020111A2 (pt) | 2020-05-05 |
| KR20200012833A (ko) | 2020-02-05 |
| IL269599A (en) | 2019-11-28 |
| CN110831945A (zh) | 2020-02-21 |
| US11236097B2 (en) | 2022-02-01 |
| RU2019134300A3 (enExample) | 2021-05-25 |
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| EP3860714B1 (en) | 11,13-modified saxitoxins for the treatment of pain | |
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