CN115697327A - 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺 - Google Patents

作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺 Download PDF

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Publication number
CN115697327A
CN115697327A CN202180043604.2A CN202180043604A CN115697327A CN 115697327 A CN115697327 A CN 115697327A CN 202180043604 A CN202180043604 A CN 202180043604A CN 115697327 A CN115697327 A CN 115697327A
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CN
China
Prior art keywords
group
alkyl
substituted
cycloalkyl
aryl
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
Application number
CN202180043604.2A
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English (en)
Chinese (zh)
Inventor
A·阿拉萨潘
I·M·贝尔
J·M·科克斯
M·J·凯利三世
M·E·雷顿
刘洪�
刘建
A·A·沙
M·D·范海斯特
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Merck Sharp & Dohme BV
Original Assignee
Merck Sharp & Dohme BV
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme BV filed Critical Merck Sharp & Dohme BV
Publication of CN115697327A publication Critical patent/CN115697327A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • 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
    • 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

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  • 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)
CN202180043604.2A 2020-06-17 2021-06-14 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺 Pending CN115697327A (zh)

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
CN115697327A true CN115697327A (zh) 2023-02-03

Family

ID=79268285

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180043604.2A Pending CN115697327A (zh) 2020-06-17 2021-06-14 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺

Country Status (10)

Country Link
US (1) US20230227405A1 (enExample)
EP (1) EP4167993A4 (enExample)
JP (1) JP2023530320A (enExample)
KR (1) KR20230026405A (enExample)
CN (1) CN115697327A (enExample)
AU (1) AU2021292062A1 (enExample)
BR (1) BR112022024476A2 (enExample)
CA (1) CA3180372A1 (enExample)
MX (1) MX2022015580A (enExample)
WO (1) WO2021257420A1 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230026404A (ko) 2020-06-17 2023-02-24 머크 샤프 앤드 돔 엘엘씨 Nav1.8 억제제로서의 2-옥소-옥사졸리딘-5-카르복스아미드
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.
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
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
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
WO2022256842A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
US20240368135A1 (en) 2021-06-04 2024-11-07 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides 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
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
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
CA3256486A1 (en) 2022-04-25 2023-11-02 Siteone Therapeutics, Inc. Bicyclic Na V1.8 Heterocyclic Amide Inhibitors for Pain Management
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN107567453A (zh) * 2015-03-13 2018-01-09 艾伯维公司 (吲唑‑4‑基)六氢吡咯并吡咯酮类及使用方法

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PE20001420A1 (es) * 1998-12-23 2000-12-18 Pfizer Moduladores de ccr5
KR20060073930A (ko) * 2003-08-08 2006-06-29 버텍스 파마슈티칼스 인코포레이티드 통증 치료시 나트륨 또는 칼슘 채널 차단제로서 유용한헤테로아릴아미노설포닐페닐 유도체
GB0514017D0 (en) * 2005-07-07 2005-08-17 Ionix Pharmaceuticals Ltd Chemical compounds
WO2014146111A2 (en) * 2013-03-15 2014-09-18 The Regents Of The University Of California Analgesic compounds and methods of use

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN107567453A (zh) * 2015-03-13 2018-01-09 艾伯维公司 (吲唑‑4‑基)六氢吡咯并吡咯酮类及使用方法

Also Published As

Publication number Publication date
BR112022024476A2 (pt) 2022-12-27
WO2021257420A1 (en) 2021-12-23
EP4167993A4 (en) 2024-07-24
AU2021292062A1 (en) 2023-01-19
JP2023530320A (ja) 2023-07-14
CA3180372A1 (en) 2021-12-23
MX2022015580A (es) 2023-01-24
US20230227405A1 (en) 2023-07-20
KR20230026405A (ko) 2023-02-24
EP4167993A1 (en) 2023-04-26

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