CN116056697A - 作为nav1.8抑制剂的2-氧代-噁唑烷-5-甲酰胺 - Google Patents
作为nav1.8抑制剂的2-氧代-噁唑烷-5-甲酰胺 Download PDFInfo
- Publication number
- CN116056697A CN116056697A CN202180043518.1A CN202180043518A CN116056697A CN 116056697 A CN116056697 A CN 116056697A CN 202180043518 A CN202180043518 A CN 202180043518A CN 116056697 A CN116056697 A CN 116056697A
- Authority
- CN
- China
- Prior art keywords
- methyl
- alkyl
- carboxamide
- oxooxazolidine
- chloro
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings 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
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings 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
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
-
- 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
-
- 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
- C07D417/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063040463P | 2020-06-17 | 2020-06-17 | |
| US63/040,463 | 2020-06-17 | ||
| PCT/US2021/037157 WO2021257418A1 (en) | 2020-06-17 | 2021-06-14 | 2-oxo-oxazolidine-5-carboxamides as nav1.8 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN116056697A true CN116056697A (zh) | 2023-05-02 |
Family
ID=79268310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180043518.1A Pending CN116056697A (zh) | 2020-06-17 | 2021-06-14 | 作为nav1.8抑制剂的2-氧代-噁唑烷-5-甲酰胺 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US12516046B2 (cg-RX-API-DMAC10.html) |
| EP (1) | EP4167994A4 (cg-RX-API-DMAC10.html) |
| JP (1) | JP2023530319A (cg-RX-API-DMAC10.html) |
| KR (1) | KR20230026404A (cg-RX-API-DMAC10.html) |
| CN (1) | CN116056697A (cg-RX-API-DMAC10.html) |
| AU (1) | AU2021292061A1 (cg-RX-API-DMAC10.html) |
| BR (1) | BR112022024450A2 (cg-RX-API-DMAC10.html) |
| MX (1) | MX2022015579A (cg-RX-API-DMAC10.html) |
| WO (1) | WO2021257418A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2023013147A (es) * | 2021-05-07 | 2023-11-28 | Merck Sharp & Dohme Llc | Aril 3-oxopiperazin carboxamidas y heteroaril 3-oxopiperazin carboxamidas como inhibidores de nav1.8. |
| SI4347031T1 (sl) | 2021-06-04 | 2026-01-30 | Vertex Pharmaceuticals Incorporated | N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov |
| US20240368135A1 (en) | 2021-06-04 | 2024-11-07 | Vertex Pharmaceuticals Incorporated | Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels |
| 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 |
| SMT202600064T1 (it) | 2021-06-04 | 2026-03-09 | Vertex Pharma | Forme farmaceutiche solide e regimi di dosaggio comprendenti (2r,3s,4s,5r)-4-[[3-(3,4-difluoro-2-metossi-fenil)-4,5-dimetil-5-(trifluorometil) tetraidrofuran-2-carbonil]ammino]piridin-2-carbossammide |
| WO2022256842A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels |
| CA3221939A1 (en) | 2021-06-04 | 2022-12-08 | Vertex Pharmaceuticals Incorporated | N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs as modulators of sodium channels |
| AU2023255558A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| AU2023257313A1 (en) | 2022-04-22 | 2024-10-31 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds for the treatment of pain |
| IL316422A (en) | 2022-04-22 | 2024-12-01 | Vertex Pharma | Heteroaryl compounds for pain treatment |
| JP2025513455A (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 |
| CA3256486A1 (en) | 2022-04-25 | 2023-11-02 | Siteone Therapeutics, Inc. | Bicyclic Na V1.8 Heterocyclic Amide Inhibitors for Pain Management |
| US20250313524A1 (en) * | 2022-05-10 | 2025-10-09 | Relay Therapeutics, Inc. | Pi3k-alpha inhibitors and methods of use thereof |
| KR20250120351A (ko) | 2022-12-06 | 2025-08-08 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법 |
| KR20260116140A (ko) | 2023-10-23 | 2026-07-28 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료를 위한 헤테로아릴 화합물 |
| 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 |
| KR20260116141A (ko) | 2023-10-23 | 2026-07-28 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료용 화합물 및 이의 고체 형태의 제조방법 |
| KR20260118418A (ko) | 2023-10-23 | 2026-07-30 | 버텍스 파마슈티칼스 인코포레이티드 | 통증 치료를 위한 헤테로아릴 화합물 |
| AU2024393245A1 (en) | 2023-12-07 | 2026-06-18 | Vertex Pharmaceuticals Incorporated | Dosing regimens and formulations of suzetrigine for use in the treatment of acute and chronic pain |
| AU2025211735A1 (en) | 2024-01-24 | 2026-07-16 | Siteone Therapeutics, Inc. | 2-aryl cycloalkyl and heterocycloalkyl inhibitors of nav1.8 for the treatment of pain |
| TW202606663A (zh) | 2024-06-28 | 2026-02-16 | 美商維泰克斯製藥公司 | 用於治療疼痛之雜芳基化合物 |
| LU605402B1 (en) | 2024-07-11 | 2026-07-14 | 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 |
|---|---|---|---|---|
| US20120220605A1 (en) * | 2009-09-04 | 2012-08-30 | Zalicus Pharmaceuticals Ltd. | Oxopiperazine derivatives for the treatment of pain and epilepsy |
| CN103906733A (zh) * | 2011-06-24 | 2014-07-02 | 安姆根有限公司 | Trpm8拮抗剂及其在治疗中的用途 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20001420A1 (es) | 1998-12-23 | 2000-12-18 | Pfizer | Moduladores de ccr5 |
| US6849639B2 (en) * | 1999-12-14 | 2005-02-01 | Amgen Inc. | Integrin inhibitors and their methods of use |
| GB0514017D0 (en) | 2005-07-07 | 2005-08-17 | Ionix Pharmaceuticals Ltd | Chemical compounds |
| EP2212290B1 (en) | 2007-10-11 | 2014-12-03 | Vertex Pharmaceuticals Incorporated | Aryl amides useful as inhibitors of voltage-gated sodium channels |
| MX2010003864A (es) | 2007-10-11 | 2010-06-01 | Vertex Pharma | Amidas utiles como inhibidores de canales de sodio dependientes de voltaje. |
| CA2701946A1 (en) | 2007-10-11 | 2009-04-16 | Vertex Pharmaceuticals Incorporated | Heteroaryl amides useful as inhibitors of voltage-gated sodium channels |
| KR102226587B1 (ko) | 2013-01-31 | 2021-03-11 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 조절제로서의 퀴놀린 및 퀴나졸린 아미드 |
| BR112015018284B1 (pt) | 2013-01-31 | 2023-03-07 | Vertex Pharmaceuticals Incorporated | Amidas como moduladores de canais de sódio, seus usos, e composição farmacêutica |
| CN105026373B (zh) | 2013-01-31 | 2018-03-30 | 沃泰克斯药物股份有限公司 | 作为钠通道调节剂的吡啶酮酰胺 |
| WO2014146111A2 (en) | 2013-03-15 | 2014-09-18 | The Regents Of The University Of California | Analgesic compounds and methods of use |
| JP6337109B2 (ja) | 2013-07-19 | 2018-06-06 | 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スルホンアミド |
| SG11201604477SA (en) | 2013-12-13 | 2016-07-28 | Vertex Pharma | Prodrugs of pyridone amides useful as modulators of sodium channels |
| KR101844984B1 (ko) | 2016-05-31 | 2018-04-03 | 한림대학교 산학협력단 | 5원 헤테로사이클릭 유도체, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
| KR102714561B1 (ko) | 2017-05-16 | 2024-10-10 | 버텍스 파마슈티칼스 인코포레이티드 | 나트륨 채널의 조절제로서의 중수소화 피리돈 아미드 및 이의 프로드럭 |
| AU2018300150A1 (en) | 2017-07-11 | 2020-01-30 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| GEAP202315648A (en) * | 2018-11-02 | 2023-07-25 | Merck Sharp & Dohme Llc | 2-amino-n-heteroaryl-nicotinamides as nav1.8 inhibitors |
| FR3096186B1 (fr) | 2019-05-13 | 2021-06-04 | Soc Dexploitation Des Procedes Marechal | Système de socle de connexion électrique |
| US11802122B2 (en) | 2020-06-17 | 2023-10-31 | Merck Sharp & Dohme Llc | 2-oxoimidazolidine-4-carboxamides as NAv1.8 inhibitors |
| CN115697327A (zh) | 2020-06-17 | 2023-02-03 | 默沙东有限责任公司 | 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺 |
-
2021
- 2021-06-14 KR KR1020237001356A patent/KR20230026404A/ko active Pending
- 2021-06-14 AU AU2021292061A patent/AU2021292061A1/en active Pending
- 2021-06-14 US US18/009,306 patent/US12516046B2/en active Active
- 2021-06-14 WO PCT/US2021/037157 patent/WO2021257418A1/en not_active Ceased
- 2021-06-14 BR BR112022024450A patent/BR112022024450A2/pt unknown
- 2021-06-14 EP EP21827155.9A patent/EP4167994A4/en active Pending
- 2021-06-14 CN CN202180043518.1A patent/CN116056697A/zh active Pending
- 2021-06-14 MX MX2022015579A patent/MX2022015579A/es unknown
- 2021-06-14 JP JP2022577339A patent/JP2023530319A/ja not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120220605A1 (en) * | 2009-09-04 | 2012-08-30 | Zalicus Pharmaceuticals Ltd. | Oxopiperazine derivatives for the treatment of pain and epilepsy |
| CN103906733A (zh) * | 2011-06-24 | 2014-07-02 | 安姆根有限公司 | Trpm8拮抗剂及其在治疗中的用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20230227441A1 (en) | 2023-07-20 |
| EP4167994A4 (en) | 2024-07-24 |
| MX2022015579A (es) | 2023-01-24 |
| EP4167994A1 (en) | 2023-04-26 |
| BR112022024450A2 (pt) | 2022-12-27 |
| AU2021292061A1 (en) | 2023-01-19 |
| JP2023530319A (ja) | 2023-07-14 |
| US12516046B2 (en) | 2026-01-06 |
| WO2021257418A1 (en) | 2021-12-23 |
| CA3182610A1 (en) | 2021-12-23 |
| KR20230026404A (ko) | 2023-02-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20230502 |