CN117597339A - 作为nav1.8抑制剂的芳基3-氧代哌嗪甲酰胺和杂芳基3-氧代哌嗪甲酰胺 - Google Patents

作为nav1.8抑制剂的芳基3-氧代哌嗪甲酰胺和杂芳基3-氧代哌嗪甲酰胺 Download PDF

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Publication number
CN117597339A
CN117597339A CN202280047884.9A CN202280047884A CN117597339A CN 117597339 A CN117597339 A CN 117597339A CN 202280047884 A CN202280047884 A CN 202280047884A CN 117597339 A CN117597339 A CN 117597339A
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China
Prior art keywords
group
methyl
carboxamide
alkyl
oxopiperazine
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Pending
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CN202280047884.9A
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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·莱顿
刘洪�
刘建
A·A·沙
M·D·范海斯特
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Merck Sharp & Dohme BV
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Merck Sharp & Dohme BV
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Publication of CN117597339A publication Critical patent/CN117597339A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202280047884.9A 2021-05-07 2022-05-02 作为nav1.8抑制剂的芳基3-氧代哌嗪甲酰胺和杂芳基3-氧代哌嗪甲酰胺 Pending CN117597339A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163185608P 2021-05-07 2021-05-07
US63/185,608 2021-05-07
PCT/US2022/027262 WO2022235558A1 (en) 2021-05-07 2022-05-02 Aryl 3-oxopiperazine carboxamides and heteroaryl 3-oxopiperazine carboxamides as nav1.8 inhibitors

Publications (1)

Publication Number Publication Date
CN117597339A true CN117597339A (zh) 2024-02-23

Family

ID=83932809

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202280047884.9A Pending CN117597339A (zh) 2021-05-07 2022-05-02 作为nav1.8抑制剂的芳基3-氧代哌嗪甲酰胺和杂芳基3-氧代哌嗪甲酰胺

Country Status (10)

Country Link
US (1) US20240246932A1 (enExample)
EP (1) EP4334306A4 (enExample)
JP (1) JP7846132B2 (enExample)
KR (1) KR20240006606A (enExample)
CN (1) CN117597339A (enExample)
AU (1) AU2022270061B2 (enExample)
BR (1) BR112023023186A2 (enExample)
CA (1) CA3217605A1 (enExample)
MX (1) MX2023013147A (enExample)
WO (1) WO2022235558A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2023257313A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
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
IL316422A (en) 2022-04-22 2024-12-01 Vertex Pharma Heteroaryl compounds for pain treatment
AU2023255558A1 (en) 2022-04-22 2024-10-31 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
KR20250120351A (ko) 2022-12-06 2025-08-08 버텍스 파마슈티칼스 인코포레이티드 나트륨 채널의 치환된 테트라하이드로푸란 조절제의 합성을 위한 방법
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
KR20260116140A (ko) 2023-10-23 2026-07-28 버텍스 파마슈티칼스 인코포레이티드 통증 치료를 위한 헤테로아릴 화합물
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
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

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2007002410A (es) * 2004-08-30 2007-05-07 Neuromed Pharmaceuticals Ltd Derivados de urea como bloqueadores de canal de calcio.
EP1809290A2 (en) * 2004-11-03 2007-07-25 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as ion channel modulators and methods of use
CL2008000835A1 (es) * 2007-03-23 2008-10-03 Icagen Inc Pfizer Ltd Compuestos derivados de sulfonamidas, inhibidores de los canales de calcio; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del dolor, sindrome de intestino irritable, enfermedad de crohn, taquiarritm
CA2771472A1 (en) * 2009-09-04 2011-03-10 Zalicus Pharmaceuticals Ltd. Oxopiperazine derivatives for the treatment of pain and epilepsy
GEAP202315648A (en) * 2018-11-02 2023-07-25 Merck Sharp & Dohme Llc 2-amino-n-heteroaryl-nicotinamides 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
KR20230026404A (ko) 2020-06-17 2023-02-24 머크 샤프 앤드 돔 엘엘씨 Nav1.8 억제제로서의 2-옥소-옥사졸리딘-5-카르복스아미드
US11802122B2 (en) 2020-06-17 2023-10-31 Merck Sharp & Dohme Llc 2-oxoimidazolidine-4-carboxamides as NAv1.8 inhibitors
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

Also Published As

Publication number Publication date
AU2022270061A1 (en) 2023-11-16
EP4334306A4 (en) 2025-04-02
CA3217605A1 (en) 2022-11-10
BR112023023186A2 (pt) 2024-01-30
WO2022235558A1 (en) 2022-11-10
MX2023013147A (es) 2023-11-28
KR20240006606A (ko) 2024-01-15
EP4334306A1 (en) 2024-03-13
AU2022270061B2 (en) 2026-02-19
US20240246932A1 (en) 2024-07-25
JP7846132B2 (ja) 2026-04-14
JP2024519487A (ja) 2024-05-14

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