CN112955436A - 6-氧代-1,6-二氢哒嗪类衍生物、其制备方法及其在医药上的应用 - Google Patents

6-氧代-1,6-二氢哒嗪类衍生物、其制备方法及其在医药上的应用 Download PDF

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CN112955436A
CN112955436A CN202080005993.5A CN202080005993A CN112955436A CN 112955436 A CN112955436 A CN 112955436A CN 202080005993 A CN202080005993 A CN 202080005993A CN 112955436 A CN112955436 A CN 112955436A
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compound
group
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pharmaceutically acceptable
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CN112955436B (zh
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杨方龙
郁楠
池江涛
贺峰
陶维康
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Fujian Shengdi Pharmaceutical Co ltd
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/22—Nitrogen and oxygen atoms
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/20—Nitrogen atoms

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

6‑氧代‑1,6‑二氢哒嗪类衍生物、其制备方法及其在医药上的应用。特别地，通式(I)所示的6‑氧代‑1,6‑二氢哒嗪类衍生物、其制备方法及含有该衍生物的药物组合物，以及其作为NaV抑制剂的用途和其在制备治疗和/或预防疼痛和疼痛相关疾病的药物中的用途。其中通式(I)的各取代基与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (20)

  1. PCT国内申请，权利要求书已公开。
CN202080005993.5A 2019-01-04 2020-01-03 6-氧代-1,6-二氢哒嗪类衍生物、其制备方法及其在医药上的应用 Active CN112955436B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN201910006240 2019-01-04
CN2019100062405 2019-01-04
CN201910380318X 2019-05-08
CN201910380318 2019-05-08
CN2019103841181 2019-05-09
CN201910384118 2019-05-09
CN2019105679153 2019-06-27
CN201910567915 2019-06-27
PCT/CN2020/070186 WO2020140959A1 (zh) 2019-01-04 2020-01-03 6-氧代-1,6-二氢哒嗪类衍生物、其制备方法及其在医药上的应用

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CN112955436A true CN112955436A (zh) 2021-06-11
CN112955436B CN112955436B (zh) 2023-08-11

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US (1) US20220073471A1 (zh)
EP (1) EP3907218A4 (zh)
JP (1) JP2022515909A (zh)
KR (1) KR20210112336A (zh)
CN (1) CN112955436B (zh)
AU (1) AU2020205139A1 (zh)
BR (1) BR112021012909A2 (zh)
CA (1) CA3125244A1 (zh)
MX (1) MX2021007970A (zh)
TW (1) TW202039443A (zh)
WO (1) WO2020140959A1 (zh)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021032074A1 (zh) * 2019-08-19 2021-02-25 江苏恒瑞医药股份有限公司 苯甲酰胺稠芳环类衍生物、其制备方法及其在医药上的应用
TW202214259A (zh) * 2020-08-19 2022-04-16 大陸商江蘇恆瑞醫藥股份有限公司 一種選擇性ＮａＶ抑制劑的前藥及其晶型
WO2022037647A1 (zh) * 2020-08-19 2022-02-24 江苏恒瑞医药股份有限公司 一种选择性Nav抑制剂的结晶形式及其制备方法
TW202302118A (zh) * 2021-02-26 2023-01-16 大陸商江蘇恒瑞醫藥股份有限公司 一種選擇性ｎａｖ抑制劑的可藥用鹽、結晶形式及其製備方法
CN113277942B (zh) * 2021-05-25 2024-05-03 都创(上海)医药开发有限公司 一种基于微通道反应技术快速制备5-氯-2-氟-4-(三氟甲基)苯甲酸的方法
EP4347584A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated N-(hydroxyalkyl (hetero)aryl) tetrahydrofuran carboxamide analogs 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
EP4347033A1 (en) 2021-06-04 2024-04-10 Vertex Pharmaceuticals Incorporated Hydroxy and (halo)alkoxy substituted tetrahydrofurans as modulators of sodium channels
WO2022256702A1 (en) 2021-06-04 2022-12-08 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofuran-2-carboxamides as modulators of sodium channels
JP2024520649A (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 （２ｒ，３ｓ，４ｓ，５ｒ）－４－［［３－（３，４－ジフルオロ－２－メトキシ－フェニル）－４，５－ジメチル－５－（トリフルオロメチル）テトラヒドロフラン－２－カルボニル］アミノ］ピリジン－２－カルボキサミドを含む固体剤形及び投与レジメン
AR126073A1 (es) 2021-06-04 2023-09-06 Vertex Pharma N-(hidroxialquil(hetero)aril)tetrahidrofuran carboxamidas como moduladores de canales de sodio
IL309666A (en) 2021-07-09 2024-02-01 Plexium Inc Aryl compounds and pharmaceutical preparations that modulate IKZF2
US20230382910A1 (en) 2022-04-22 2023-11-30 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
US20230373925A1 (en) 2022-04-22 2023-11-23 Vertex Pharma Heteroaryl compounds for the treatment of pain
WO2023205465A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205468A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
CN116947713A (zh) * 2022-04-25 2023-10-27 中国科学院上海药物研究所 并环类化合物及其应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101883758A (zh) * 2007-10-11 2010-11-10 沃泰克斯药物股份有限公司 用作电压门控的钠通道抑制剂的芳基酰胺类化合物
CN104968647A (zh) * 2013-01-31 2015-10-07 沃泰克斯药物股份有限公司 作为钠通道调节剂的酰胺
CN105026373A (zh) * 2013-01-31 2015-11-04 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
WO2018213426A1 (en) * 2017-05-16 2018-11-22 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101883758A (zh) * 2007-10-11 2010-11-10 沃泰克斯药物股份有限公司 用作电压门控的钠通道抑制剂的芳基酰胺类化合物
CN104968647A (zh) * 2013-01-31 2015-10-07 沃泰克斯药物股份有限公司 作为钠通道调节剂的酰胺
CN105026373A (zh) * 2013-01-31 2015-11-04 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
WO2018213426A1 (en) * 2017-05-16 2018-11-22 Vertex Pharmaceuticals Incorporated Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels

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MX2021007970A (es) 2021-08-16
TW202039443A (zh) 2020-11-01
AU2020205139A1 (en) 2021-08-19
JP2022515909A (ja) 2022-02-22
EP3907218A1 (en) 2021-11-10
US20220073471A1 (en) 2022-03-10
BR112021012909A2 (pt) 2021-09-14
WO2020140959A1 (zh) 2020-07-09
CA3125244A1 (en) 2020-07-09
CN112955436B (zh) 2023-08-11
EP3907218A4 (en) 2022-09-21
KR20210112336A (ko) 2021-09-14

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