TWI820266B - 巨環化合物及其用途 - Google Patents

巨環化合物及其用途 Download PDF

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Publication number
TWI820266B
TWI820266B TW108144324A TW108144324A TWI820266B TW I820266 B TWI820266 B TW I820266B TW 108144324 A TW108144324 A TW 108144324A TW 108144324 A TW108144324 A TW 108144324A TW I820266 B TWI820266 B TW I820266B
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TW
Taiwan
Prior art keywords
methyl
group
ring
cr4r5
ethyl acetate
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TW108144324A
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English (en)
Chinese (zh)
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TW202039494A (zh
Inventor
松本重充
原亮磨
野口直義
福士英人
新居田歩
佐佐木聡
生駒実
小林俊威
前川毅志
Original Assignee
日商思可海雅藥品股份有限公司
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=70975488&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI820266(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4748—Quinolines; Isoquinolines forming part of bridged ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW108144324A 2018-12-05 2019-12-04 巨環化合物及其用途 TWI820266B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2018-228234 2018-12-05
JP2018228234 2018-12-05

Publications (2)

Publication Number Publication Date
TW202039494A TW202039494A (zh) 2020-11-01
TWI820266B true TWI820266B (zh) 2023-11-01

Family

ID=70975488

Family Applications (1)

Application Number Title Priority Date Filing Date
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Country Status (18)

Country Link
US (1) US11518763B2 (https=)
EP (1) EP3890738A4 (https=)
JP (2) JP2022510736A (https=)
KR (1) KR102919982B1 (https=)
CN (1) CN113164468A (https=)
AR (1) AR117251A1 (https=)
AU (1) AU2019391942B2 (https=)
BR (1) BR112021010704A2 (https=)
CA (1) CA3121952C (https=)
CL (1) CL2021001451A1 (https=)
CO (1) CO2021007304A2 (https=)
MX (1) MX2021006527A (https=)
NZ (1) NZ776102A (https=)
PH (1) PH12021551262A1 (https=)
SG (1) SG11202105125XA (https=)
TW (1) TWI820266B (https=)
UA (1) UA127872C2 (https=)
WO (1) WO2020116660A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3833662B1 (en) 2018-08-20 2024-01-17 Janssen Pharmaceutica NV Inhibitors of keap1-nrf2 protein-protein interaction
AU2020283361B2 (en) 2019-05-31 2025-11-27 Ube Corporation Benzotriazole derivative
CN116406364A (zh) * 2020-09-14 2023-07-07 赛诺菲公司 用于治疗红细胞障碍和炎性疾病的四氢异喹啉衍生物
KR20260005897A (ko) * 2023-04-03 2026-01-12 에이스링크 테라퓨틱스, 인코포레이티드 신규 화합물 및 이의 용도
CN119707895B (zh) * 2023-12-18 2026-03-31 江苏苏中药业研究院有限公司 一种7-甲酰基-2,3-二氢苯并呋喃-4-碳腈的制备方法

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2015092713A1 (en) * 2013-12-18 2015-06-25 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2018181345A1 (ja) * 2017-03-28 2018-10-04 武田薬品工業株式会社 複素環化合物

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WO2012028959A1 (en) 2010-08-31 2012-03-08 Pablo Villoslada Agonists of neurotrophin receptors and their use as medicaments
DK3492455T3 (da) 2013-06-21 2023-08-14 Karyopharm Therapeutics Inc 1,2,4-triazoler som nukleare transportmodulatorer og anvendelse til behandling af specifikke former for cancer
LT3307739T (lt) 2015-06-15 2021-03-10 Glaxosmithkline Intellectual Property Development Limited Nrf2 reguliatoriai
WO2016203401A1 (en) 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
CA2988373A1 (en) 2015-06-15 2016-12-22 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
US10201531B2 (en) 2015-08-12 2019-02-12 Mochida Pharmaceutical Co., Ltd. Indazolyl-oxo-isothiazole compounds
US10364256B2 (en) 2015-10-06 2019-07-30 Glaxosmithkline Intellectual Property Development Limited Biaryl pyrazoles as NRF2 regulators
US10351530B2 (en) 2015-10-06 2019-07-16 Glaxosmithkline Intellectual Property Development Limited Arylcyclohexyl pyrazoles as NRF2 regulators
JP2020500919A (ja) 2016-12-12 2020-01-16 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎｒｆ２レギュレーターとしての３−カルボン酸ピロール
JP2020500918A (ja) 2016-12-12 2020-01-16 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎｒｆ２レギュレーターとしてのｎ−アリールピラゾール
EP3555068B1 (en) 2016-12-14 2020-12-02 GlaxoSmithKline Intellectual Property Development Limited 3-oxo-1,4-diazepinyle compounds as nrf2 activators
ES2901617T3 (es) 2016-12-14 2022-03-23 Glaxosmithkline Ip Dev Ltd Bisarilamidas como reguladores de NRF2
US11117905B2 (en) 2016-12-14 2021-09-14 Glaxosmithkline Intellectual Property Development Limited Bisaryl heterocycles as NRF2 activators
CA3044773A1 (en) 2016-12-15 2018-06-21 Glaxosmithkline Intellectual Property Development Limited Nrf2 activators
JP2020502152A (ja) 2016-12-15 2020-01-23 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｎｒｆ２アクチベーターとしてのエーテル結合トリアゾール
UY37551A (es) 2016-12-27 2018-07-31 Biogen Ma Inc Activador de nrf2
WO2018140876A1 (en) * 2017-01-30 2018-08-02 Biogen Ma Inc. Nrf2 activator
US20190389830A1 (en) 2017-01-30 2019-12-26 Biogen Ma Inc. Nrf2 activator

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Publication number Priority date Publication date Assignee Title
WO2015092713A1 (en) * 2013-12-18 2015-06-25 Glaxosmithkline Intellectual Property Development Limited Nrf2 regulators
WO2018181345A1 (ja) * 2017-03-28 2018-10-04 武田薬品工業株式会社 複素環化合物

Also Published As

Publication number Publication date
EP3890738A4 (en) 2022-08-17
SG11202105125XA (en) 2021-06-29
US20220119391A1 (en) 2022-04-21
PH12021551262A1 (en) 2021-10-25
CA3121952C (en) 2025-05-13
WO2020116660A1 (en) 2020-06-11
AU2019391942A1 (en) 2021-06-03
CO2021007304A2 (es) 2021-06-21
TW202039494A (zh) 2020-11-01
JP2024123202A (ja) 2024-09-10
NZ776102A (en) 2024-12-20
CN113164468A (zh) 2021-07-23
JP2022510736A (ja) 2022-01-27
MX2021006527A (es) 2021-07-21
AR117251A1 (es) 2021-07-21
AU2019391942B2 (en) 2024-03-21
CL2021001451A1 (es) 2021-12-24
UA127872C2 (uk) 2024-01-31
BR112021010704A2 (pt) 2021-08-24
KR20210099622A (ko) 2021-08-12
KR102919982B1 (ko) 2026-02-02
CA3121952A1 (en) 2020-06-11
US11518763B2 (en) 2022-12-06
EP3890738A1 (en) 2021-10-13

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