JP7104070B2 - ナトリウムチャネルの調節因子としての重水素化ピリドンアミドおよびそのプロドラッグ - Google Patents
ナトリウムチャネルの調節因子としての重水素化ピリドンアミドおよびそのプロドラッグ Download PDFInfo
- Publication number
- JP7104070B2 JP7104070B2 JP2019563132A JP2019563132A JP7104070B2 JP 7104070 B2 JP7104070 B2 JP 7104070B2 JP 2019563132 A JP2019563132 A JP 2019563132A JP 2019563132 A JP2019563132 A JP 2019563132A JP 7104070 B2 JP7104070 B2 JP 7104070B2
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- Prior art keywords
- pain
- compound
- pharmaceutically acceptable
- composition
- pharmaceutical composition
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- Expired - Fee Related
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762507172P | 2017-05-16 | 2017-05-16 | |
| US62/507,172 | 2017-05-16 | ||
| US201762547718P | 2017-08-18 | 2017-08-18 | |
| US62/547,718 | 2017-08-18 | ||
| PCT/US2018/032939 WO2018213426A1 (en) | 2017-05-16 | 2018-05-16 | Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020519661A JP2020519661A (ja) | 2020-07-02 |
| JP2020519661A5 JP2020519661A5 (https=) | 2021-07-26 |
| JP7104070B2 true JP7104070B2 (ja) | 2022-07-20 |
Family
ID=62567801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019563132A Expired - Fee Related JP7104070B2 (ja) | 2017-05-16 | 2018-05-16 | ナトリウムチャネルの調節因子としての重水素化ピリドンアミドおよびそのプロドラッグ |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US11358977B2 (https=) |
| EP (1) | EP3625214B1 (https=) |
| JP (1) | JP7104070B2 (https=) |
| KR (1) | KR102714561B1 (https=) |
| CN (1) | CN110740993B (https=) |
| AU (1) | AU2018271110A1 (https=) |
| BR (1) | BR112019024016A2 (https=) |
| CA (1) | CA3063901A1 (https=) |
| CL (1) | CL2019003239A1 (https=) |
| CO (1) | CO2019013021A2 (https=) |
| ES (1) | ES2927712T3 (https=) |
| IL (1) | IL270680B (https=) |
| MA (1) | MA49137A (https=) |
| MX (1) | MX390793B (https=) |
| UA (1) | UA124857C2 (https=) |
| WO (1) | WO2018213426A1 (https=) |
| ZA (1) | ZA201907619B (https=) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019157505A1 (en) * | 2018-02-12 | 2019-08-15 | Vertex Pharmaceuticals Incorporated | A method of treating pain |
| EP3873893A1 (en) | 2018-11-02 | 2021-09-08 | Merck Sharp & Dohme Corp. | 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors |
| CA3125244A1 (en) * | 2019-01-04 | 2020-07-09 | Jiangsu Hengrui Medicine Co., Ltd. | 6-oxo-1,6-dihydropyridazine derivative, preparation method therefor and medical use thereof |
| US12441703B2 (en) | 2019-01-10 | 2025-10-14 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| CN112996774B (zh) * | 2019-01-25 | 2022-11-22 | 江苏恒瑞医药股份有限公司 | 2-氧代-1,2-二氢吡啶类衍生物、其制备方法及其在医药上的应用 |
| CN112996776B (zh) * | 2019-02-20 | 2024-03-15 | 福建盛迪医药有限公司 | 6-氧代-1,6-二氢哒嗪类前药衍生物、其制备方法及其在医药上的应用 |
| WO2020206119A1 (en) * | 2019-04-02 | 2020-10-08 | Vertex Pharmaceuticals Incorporated | Process for making pyridone amides and prodrugs thereof useful as modulators of sodium channels |
| WO2020219867A1 (en) * | 2019-04-25 | 2020-10-29 | Vertex Pharmaceuticals Incorporated | Pyridone amide co-crystal compositions for the treatment of pain |
| US12528782B2 (en) | 2019-07-16 | 2026-01-20 | Bristol-Myers Squibb Company | Prodrugs in the modulation of interleukin |
| WO2021018165A1 (zh) * | 2019-07-30 | 2021-02-04 | 江苏恒瑞医药股份有限公司 | 吡啶苯甲酰胺类衍生物、其制备方法及其在医药上的应用 |
| WO2021032074A1 (zh) * | 2019-08-19 | 2021-02-25 | 江苏恒瑞医药股份有限公司 | 苯甲酰胺稠芳环类衍生物、其制备方法及其在医药上的应用 |
| CA3164134A1 (en) | 2019-12-06 | 2021-06-10 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofurans as modulators of sodium channels |
| CN114437062B (zh) * | 2020-04-30 | 2024-05-17 | 成都海博为药业有限公司 | 一种可作为钠通道调节剂的化合物及其用途 |
| JP2023530319A (ja) | 2020-06-17 | 2023-07-14 | メルク・シャープ・アンド・ドーム・エルエルシー | Nav1.8阻害剤としての2-オキソ-オキサゾリジン-5-カルボキサミド |
| GEP20257750B (en) | 2020-06-17 | 2025-03-25 | Merck Sharp & Dohme Llc | 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors |
| CN113880771B (zh) * | 2020-07-03 | 2023-09-19 | 福建盛迪医药有限公司 | 一种选择性Nav抑制剂的结晶形式及其制备方法 |
| WO2022037647A1 (zh) * | 2020-08-19 | 2022-02-24 | 江苏恒瑞医药股份有限公司 | 一种选择性Nav抑制剂的结晶形式及其制备方法 |
| TW202214259A (zh) * | 2020-08-19 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種選擇性NaV抑制劑的前藥及其晶型 |
| CN111808019B (zh) * | 2020-09-08 | 2020-11-27 | 上海济煜医药科技有限公司 | 一种并环化合物及其应用 |
| JP2023554430A (ja) * | 2020-12-18 | 2023-12-27 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド | Nav1.8阻害剤としての含窒素2,3-ジヒドロキナゾリノン化合物 |
| JP2024502231A (ja) * | 2020-12-18 | 2024-01-18 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド | Nav1.8電位依存性ナトリウムチャネルを阻害するためおよびNav1.8介在疾患を治療するために有用な化学化合物 |
| CN116964065A (zh) * | 2021-02-26 | 2023-10-27 | 江苏恒瑞医药股份有限公司 | 一种选择性NaV抑制剂的可药用盐、结晶形式及其制备方法 |
| EP4334293A1 (en) | 2021-05-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors |
| SI4347031T1 (sl) | 2021-06-04 | 2026-01-30 | Vertex Pharmaceuticals Incorporated | N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov |
| JP2024520646A (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モジュレーターとしてのn-(ヒドロキシアルキル(ヘテロ)アリール)テトラヒドロフランカルボキサミド類似体 |
| MA64856B1 (fr) | 2021-06-04 | 2026-02-27 | Vertex Pharmaceuticals Incorporated | Formes de dosage solides et regimens de dosage comprenant le [[3-(3,4-difluoro-2-méthoxy-phényl)-4,5-diméthyl-5-(trifluorométhyl) tétrahydrofuranne-2-carbonyl]amino]pyridine-2-carboxamide |
| WO2022256676A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| JP2024520643A (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ヒドロキシ及び(ハロ)アルコキシ置換テトラヒドロフラン |
| CA3221788A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| AR126669A1 (es) | 2021-08-02 | 2023-11-01 | Eurofarma Laboratorios S A | COMPUESTOS N-ACILIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS |
| UY39882A (es) | 2021-08-02 | 2023-06-15 | Eurofarma Laboratorios S A | COMPUESTOS NACILHIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS |
| EP4426290A4 (en) * | 2021-11-02 | 2025-10-08 | Schedule 1 Therapeutics Inc | USE OF CANNABINOID COMPOSITIONS TO TREAT PAIN ASSOCIATED WITH SMALL FIBER NEUROPATHY |
| JP2025513452A (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 |
| AU2023257313A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| UY40234A (es) | 2022-04-22 | 2023-11-15 | Vertex Pharma | Compuestos heteroarilo para el tratamiento del dolor |
| GEAP202516634A (en) | 2022-04-22 | 2025-02-25 | Vertex Pharma | Heteroaryl compounds for the treatment of pain |
| IL316433A (en) | 2022-04-25 | 2024-12-01 | Siteone Therapeutics Inc | Bicyclic heterocyclic amide inhibitors of NA v1.8 for the treatment of pain |
| AU2023391870A1 (en) | 2022-12-06 | 2025-06-05 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
| PY2404641A (es) | 2023-01-30 | 2024-10-03 | Eurofarma Laboratorios S A | COMPUESTOS FENÓLICOS BLOQUEADORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, SUS COMPOSICIONES, SUS USOS, LOS MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y SUS KITS |
| WO2024159285A1 (pt) | 2023-01-30 | 2024-08-08 | Eurofarma Laboratórios S.A. | Compostos aril piridinas bloqueadores de nav 1.7 e/ou nav 1.8, seus processos de obtenção, composições, usos, métodos de tratamento destes e kits |
| AR131715A1 (es) | 2023-01-30 | 2025-04-23 | Eurofarma Laboratorios S A | AMIDAS BLOQUEADORAS DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE LOS MISMOS Y KITS |
| PY2404093A (es) | 2023-01-30 | 2024-10-03 | Eurofarma Laboratorios S A | Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y kits |
| EP4660184A1 (en) | 2023-01-30 | 2025-12-10 | Eurofarma Laboratórios S.A. | Nav1.7- and/or nav1.8-inhibiting hydroxamates, processes for the preparation thereof, compositions, uses, methods for treatment using same, and kits |
| 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 |
| WO2025090480A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2025090465A1 (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 |
| WO2025122953A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic pain |
| WO2025160286A1 (en) | 2024-01-24 | 2025-07-31 | Siteone Therapeutics, Inc. | 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain |
| US20260001877A1 (en) | 2024-06-28 | 2026-01-01 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2026013449A2 (en) | 2024-07-11 | 2026-01-15 | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016506963A (ja) | 2013-01-31 | 2016-03-07 | 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Vertex Pharmaceuticals Incorporated | ナトリウムチャネルの調節剤としてのピリドンアミド |
| JP2017504591A (ja) | 2013-12-13 | 2017-02-09 | 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Vertex Pharmaceuticals Incorporated | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
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| JP2016506963A (ja) | 2013-01-31 | 2016-03-07 | 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Vertex Pharmaceuticals Incorporated | ナトリウムチャネルの調節剤としてのピリドンアミド |
| JP2017504591A (ja) | 2013-12-13 | 2017-02-09 | 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Vertex Pharmaceuticals Incorporated | ナトリウムチャネルの調節剤として有用なピリドンアミドのプロドラッグ |
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| WO2018213426A1 (en) | 2018-11-22 |
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| UA124857C2 (uk) | 2021-12-01 |
| US11358977B2 (en) | 2022-06-14 |
| KR20200006128A (ko) | 2020-01-17 |
| MA49137A (fr) | 2021-04-21 |
| AU2018271110A1 (en) | 2019-12-05 |
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| EP3625214A1 (en) | 2020-03-25 |
| IL270680B (en) | 2022-06-01 |
| CA3063901A1 (en) | 2018-11-22 |
| CN110740993B (zh) | 2023-09-01 |
| BR112019024016A2 (pt) | 2020-06-09 |
| JP2020519661A (ja) | 2020-07-02 |
| CL2019003239A1 (es) | 2020-04-17 |
| MX2019013574A (es) | 2019-12-18 |
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