JP2023530320A - Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド - Google Patents
Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド Download PDFInfo
- Publication number
- JP2023530320A JP2023530320A JP2022577341A JP2022577341A JP2023530320A JP 2023530320 A JP2023530320 A JP 2023530320A JP 2022577341 A JP2022577341 A JP 2022577341A JP 2022577341 A JP2022577341 A JP 2022577341A JP 2023530320 A JP2023530320 A JP 2023530320A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- aryl
- substituted
- methyl
- 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.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
- C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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]
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063040465P | 2020-06-17 | 2020-06-17 | |
| US63/040,465 | 2020-06-17 | ||
| PCT/US2021/037160 WO2021257420A1 (en) | 2020-06-17 | 2021-06-14 | 5-oxopyrrolidine-3-carboxamides as nav1.8 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023530320A true JP2023530320A (ja) | 2023-07-14 |
| JP2023530320A5 JP2023530320A5 (https=) | 2024-06-20 |
| JPWO2021257420A5 JPWO2021257420A5 (https=) | 2024-06-20 |
Family
ID=79268285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022577341A Pending JP2023530320A (ja) | 2020-06-17 | 2021-06-14 | Ｎａｖ１．８阻害剤としての５－オキソピロリジン－３－カルボキサミド |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230227405A1 (https=) |
| EP (1) | EP4167993A4 (https=) |
| JP (1) | JP2023530320A (https=) |
| KR (1) | KR20230026405A (https=) |
| CN (1) | CN115697327A (https=) |
| AU (1) | AU2021292062A1 (https=) |
| BR (1) | BR112022024476A2 (https=) |
| CA (1) | CA3180372A1 (https=) |
| MX (1) | MX2022015580A (https=) |
| WO (1) | WO2021257420A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2024519487A (ja) * | 2021-05-07 | 2024-05-14 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｎａｖ１．８阻害薬としてのアリール ３－オキソピペラジンカルボキサミド類及びヘテロアリール ３－オキソピペラジンカルボキサミド類 |
| US12516046B2 (en) | 2020-06-17 | 2026-01-06 | Merck Sharp & Dohme Llc | 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2022256676A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| 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 |
| SI4347031T1 (sl) | 2021-06-04 | 2026-01-30 | Vertex Pharmaceuticals Incorporated | N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov |
| CA3221788A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2025090516A1 (en) | 2023-10-23 | 2025-05-01 | Vertex Pharmaceuticals Incorporated | Methods of preparing compounds for treating pain and solid forms thereof |
| 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 |
| 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 |
| 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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007007057A1 (en) * | 2005-07-07 | 2007-01-18 | Vernalis (R & D) Limited | Antagonists of sns sodium channels |
| JP2011032294A (ja) * | 2003-08-08 | 2011-02-17 | Vertex Pharmaceuticals Inc | 電位開口型のナトリウムチャネルのインヒビターとして有用な組成物 |
| JP2014527511A (ja) * | 2011-06-24 | 2014-10-16 | アムジエン・インコーポレーテツド | Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20001420A1 (es) * | 1998-12-23 | 2000-12-18 | Pfizer | Moduladores de ccr5 |
| WO2014146111A2 (en) * | 2013-03-15 | 2014-09-18 | The Regents Of The University Of California | Analgesic compounds and methods of use |
| CA2979534A1 (en) * | 2015-03-13 | 2016-09-22 | Abbvie Inc. | (indazol-4-yl)hexahydropyrrolopyrrolones and method of use |
-
2021
- 2021-06-14 BR BR112022024476A patent/BR112022024476A2/pt unknown
- 2021-06-14 MX MX2022015580A patent/MX2022015580A/es unknown
- 2021-06-14 US US18/009,310 patent/US20230227405A1/en active Pending
- 2021-06-14 CA CA3180372A patent/CA3180372A1/en active Pending
- 2021-06-14 WO PCT/US2021/037160 patent/WO2021257420A1/en not_active Ceased
- 2021-06-14 EP EP21826932.2A patent/EP4167993A4/en active Pending
- 2021-06-14 JP JP2022577341A patent/JP2023530320A/ja active Pending
- 2021-06-14 KR KR1020237001357A patent/KR20230026405A/ko active Pending
- 2021-06-14 CN CN202180043604.2A patent/CN115697327A/zh active Pending
- 2021-06-14 AU AU2021292062A patent/AU2021292062A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011032294A (ja) * | 2003-08-08 | 2011-02-17 | Vertex Pharmaceuticals Inc | 電位開口型のナトリウムチャネルのインヒビターとして有用な組成物 |
| WO2007007057A1 (en) * | 2005-07-07 | 2007-01-18 | Vernalis (R & D) Limited | Antagonists of sns sodium channels |
| JP2014527511A (ja) * | 2011-06-24 | 2014-10-16 | アムジエン・インコーポレーテツド | Ｔｒｐｍ８拮抗剤及び治療におけるそれらの使用 |
Non-Patent Citations (4)
| Title |
|---|
| REGISTRY (STN) [ONLINE], JPN7025002043, ISSN: 0005592125 * |
| REGISTRY (STN) [ONLINE], JPN7025002044, ISSN: 0005592126 * |
| REGISTRY (STN) [ONLINE], JPN7025002045, ISSN: 0005592127 * |
| REGISTRY (STN) [ONLINE], JPN7025002046, ISSN: 0005592128 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12516046B2 (en) | 2020-06-17 | 2026-01-06 | Merck Sharp & Dohme Llc | 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors |
| JP2024519487A (ja) * | 2021-05-07 | 2024-05-14 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｎａｖ１．８阻害薬としてのアリール ３－オキソピペラジンカルボキサミド類及びヘテロアリール ３－オキソピペラジンカルボキサミド類 |
| JP7846132B2 (ja) | 2021-05-07 | 2026-04-14 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｎａｖ１．８阻害薬としてのアリール ３－オキソピペラジンカルボキサミド類及びヘテロアリール ３－オキソピペラジンカルボキサミド類 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP4167993A1 (en) | 2023-04-26 |
| US20230227405A1 (en) | 2023-07-20 |
| AU2021292062A1 (en) | 2023-01-19 |
| MX2022015580A (es) | 2023-01-24 |
| CA3180372A1 (en) | 2021-12-23 |
| WO2021257420A1 (en) | 2021-12-23 |
| EP4167993A4 (en) | 2024-07-24 |
| CN115697327A (zh) | 2023-02-03 |
| KR20230026405A (ko) | 2023-02-24 |
| BR112022024476A2 (pt) | 2022-12-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
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| A621 | Written request for application examination |
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| A977 | Report on retrieval |
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| A02 | Decision of refusal |
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