KR20230026405A - Nav1.8 억제제로서의 5-옥소피롤리딘-3-카르복스아미드 - Google Patents
Nav1.8 억제제로서의 5-옥소피롤리딘-3-카르복스아미드 Download PDFInfo
- Publication number
- KR20230026405A KR20230026405A KR1020237001357A KR20237001357A KR20230026405A KR 20230026405 A KR20230026405 A KR 20230026405A KR 1020237001357 A KR1020237001357 A KR 1020237001357A KR 20237001357 A KR20237001357 A KR 20237001357A KR 20230026405 A KR20230026405 A KR 20230026405A
- Authority
- KR
- South Korea
- 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
-
- 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
- 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
-
- 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)
- 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)
- Rheumatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pain & Pain Management (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 (1)
| Publication Number | Publication Date |
|---|---|
| KR20230026405A true KR20230026405A (ko) | 2023-02-24 |
Family
ID=79268285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020237001357A Pending KR20230026405A (ko) | 2020-06-17 | 2021-06-14 | Nav1.8 억제제로서의 5-옥소피롤리딘-3-카르복스아미드 |
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=) |
Families Citing this family (24)
| 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 |
| GEP20257795B (en) * | 2021-05-07 | 2025-09-25 | Merck Sharp & Dohme Llc | Cycloalkyl 3-oxopiperazine carboxamides and cycloheteroalkyl 3-oxopiperazine carboxamides as nav1.8 inhibitors |
| AU2022270061B2 (en) * | 2021-05-07 | 2026-02-19 | Merck Sharp & Dohme Llc | Aryl 3-oxopiperazine carboxamides and heteroaryl 3-oxopiperazine carboxamides as nav1.8 inhibitors |
| CA3221938A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran analogs as modulators of sodium channels |
| SMT202500481T1 (it) | 2021-06-04 | 2026-01-12 | Vertex Pharma | N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio |
| US20240400544A1 (en) | 2021-06-04 | 2024-12-05 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| AU2022283934A1 (en) | 2021-06-04 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| WO2022256842A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| HRP20260068T1 (hr) | 2021-06-04 | 2026-02-27 | Vertex Pharmaceuticals Incorporated | Čvrsti farmaceutski oblici i režimi doziranja koji obuhvaćaju (2r,3s,4s,5r)-4-[[3-(3,4-difluor-2-metoksifenil)-4,5-dimetil-5-(trifluormetil)tetrahidrofuran-2-karbonil]amino]piridin-2-karboksamid |
| CA3256248A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | HETEROARYL COMPOUNDS FOR PAIN RELIEF |
| US20230382910A1 (en) | 2022-04-22 | 2023-11-30 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| WO2023205463A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| CA3257285A1 (en) | 2022-04-22 | 2023-10-26 | Vertex Pharmaceuticals Incorporated | HETEROARYL COMPOUNDS FOR PAIN RELIEF |
| JP2025516005A (ja) | 2022-04-25 | 2025-05-23 | 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ｎａｖ１．８の二環式複素環アミド阻害剤 |
| WO2024123815A1 (en) | 2022-12-06 | 2024-06-13 | Vertex Pharmaceuticals Incorporated | Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels |
| 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 |
| US20250186419A1 (en) | 2023-12-07 | 2025-06-12 | Vertex Pharmaceuticals Incorporated | Dosing regimens for treating 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 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20001420A1 (es) * | 1998-12-23 | 2000-12-18 | Pfizer | Moduladores de ccr5 |
| EP1673357A2 (en) * | 2003-08-08 | 2006-06-28 | Vertex Pharmaceuticals Incorporated | Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain |
| GB0514017D0 (en) * | 2005-07-07 | 2005-08-17 | Ionix Pharmaceuticals Ltd | Chemical compounds |
| 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 |
| WO2014146111A2 (en) * | 2013-03-15 | 2014-09-18 | The Regents Of The University Of California | Analgesic compounds and methods of use |
| JP2018507900A (ja) * | 2015-03-13 | 2018-03-22 | アッヴィ・インコーポレイテッド | （インダゾール−４−イル）ヘキサヒドロピロロピロロン及び使用方法 |
-
2021
- 2021-06-14 CN CN202180043604.2A patent/CN115697327A/zh active Pending
- 2021-06-14 US US18/009,310 patent/US20230227405A1/en active Pending
- 2021-06-14 EP EP21826932.2A patent/EP4167993A4/en active Pending
- 2021-06-14 WO PCT/US2021/037160 patent/WO2021257420A1/en not_active Ceased
- 2021-06-14 JP JP2022577341A patent/JP2023530320A/ja active Pending
- 2021-06-14 AU AU2021292062A patent/AU2021292062A1/en active Pending
- 2021-06-14 KR KR1020237001357A patent/KR20230026405A/ko active Pending
- 2021-06-14 CA CA3180372A patent/CA3180372A1/en active Pending
- 2021-06-14 MX MX2022015580A patent/MX2022015580A/es unknown
- 2021-06-14 BR BR112022024476A patent/BR112022024476A2/pt unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112022024476A2 (pt) | 2022-12-27 |
| JP2023530320A (ja) | 2023-07-14 |
| US20230227405A1 (en) | 2023-07-20 |
| WO2021257420A1 (en) | 2021-12-23 |
| AU2021292062A1 (en) | 2023-01-19 |
| CN115697327A (zh) | 2023-02-03 |
| EP4167993A4 (en) | 2024-07-24 |
| CA3180372A1 (en) | 2021-12-23 |
| EP4167993A1 (en) | 2023-04-26 |
| MX2022015580A (es) | 2023-01-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| PA0201 | Request for examination |
St.27 status event code: A-1-2-D10-D11-exm-PA0201 |
|
| E13 | Pre-grant limitation requested |
Free format text: ST27 STATUS EVENT CODE: A-2-3-E10-E13-LIM-X000 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| D21 | Rejection of application intended |
Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |