CN113316575A - 作为TGF-βR1激酶抑制剂的5-(4-吡啶氧基)吡唑类化合物 - Google Patents

作为TGF-βR1激酶抑制剂的5-(4-吡啶氧基)吡唑类化合物 Download PDF

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CN113316575A
CN113316575A CN202080009676.0A CN202080009676A CN113316575A CN 113316575 A CN113316575 A CN 113316575A CN 202080009676 A CN202080009676 A CN 202080009676A CN 113316575 A CN113316575 A CN 113316575A
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China
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compound
isomer
mmol
pharmaceutically acceptable
acceptable salt
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CN202080009676.0A
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CN113316575B (zh
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付翔宇
丁照中
胡利红
陈曙辉
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Shanghai Institute of Materia Medica of CAS
Jiangsu Aosaikang Pharmaceutical Co Ltd
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Shanghai Institute of Materia Medica of CAS
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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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

本发明公开了一类作为TGF‑βR1抑制剂的5‑(4‑吡啶氧基)吡唑类化合物，以及它们在制备TGF‑βR1抑制剂药物中的应用。具体公开了式(I)所示化合物、其药学上可接受的盐或其异构体。

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN202080009676.0A 2019-01-24 2020-01-22 作为TGF-βR1激酶抑制剂的5-(4-吡啶氧基)吡唑类化合物 Active CN113316575B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019100699362 2019-01-24
CN201910069936 2019-01-24
PCT/CN2020/073832 WO2020151749A1 (zh) 2019-01-24 2020-01-22 作为TGF-βR1激酶抑制剂的5-(4-吡啶氧基)吡唑类化合物

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CN113316575A true CN113316575A (zh) 2021-08-27
CN113316575B CN113316575B (zh) 2022-03-18

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US (1) US20220098171A1 (zh)
EP (1) EP3922631A4 (zh)
JP (1) JP7331116B2 (zh)
KR (1) KR20210118891A (zh)
CN (1) CN113316575B (zh)
WO (1) WO2020151749A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113993859A (zh) * 2019-06-25 2022-01-28 益方生物科技(上海)股份有限公司 杂环化合物、其制备方法及其使用方法

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022017208A1 (zh) * 2020-07-23 2022-01-27 江苏奥赛康药业有限公司 作为TGF-βR1抑制剂的吡啶氧基连吡唑类化合物的盐型、晶型以及其药物组合物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1951939A (zh) * 2001-05-24 2007-04-25 伊莱利利公司 作为药物的新的吡唑衍生物
TW201329067A (zh) * 2011-12-08 2013-07-16 Amgen Inc 作為ｇｋａ活化劑之脲化合物
CN106470992A (zh) * 2014-06-17 2017-03-01 正大天晴药业集团股份有限公司 作为pi3k抑制剂的吡啶并[1,2‑a]嘧啶酮类似物
CN106795139A (zh) * 2014-10-07 2017-05-31 伊莱利利公司 氨基吡啶基氧基吡唑化合物
CN109071538A (zh) * 2017-01-22 2018-12-21 福建广生堂药业股份有限公司 作为ask1抑制剂的吡啶衍生物及其制备方法和应用

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020258006A1 (en) * 2019-06-25 2020-12-30 Inventisbio Shanghai Ltd. Heterocyclic compounds, preparation methods therefor, and methods of uses thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1951939A (zh) * 2001-05-24 2007-04-25 伊莱利利公司 作为药物的新的吡唑衍生物
TW201329067A (zh) * 2011-12-08 2013-07-16 Amgen Inc 作為ｇｋａ活化劑之脲化合物
CN106470992A (zh) * 2014-06-17 2017-03-01 正大天晴药业集团股份有限公司 作为pi3k抑制剂的吡啶并[1,2‑a]嘧啶酮类似物
CN106795139A (zh) * 2014-10-07 2017-05-31 伊莱利利公司 氨基吡啶基氧基吡唑化合物
CN109071538A (zh) * 2017-01-22 2018-12-21 福建广生堂药业股份有限公司 作为ask1抑制剂的吡啶衍生物及其制备方法和应用

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113993859A (zh) * 2019-06-25 2022-01-28 益方生物科技(上海)股份有限公司 杂环化合物、其制备方法及其使用方法

Also Published As

Publication number Publication date
CN113316575B (zh) 2022-03-18
EP3922631A1 (en) 2021-12-15
KR20210118891A (ko) 2021-10-01
JP2022518544A (ja) 2022-03-15
EP3922631A4 (en) 2022-10-26
WO2020151749A1 (zh) 2020-07-30
JP7331116B2 (ja) 2023-08-22
US20220098171A1 (en) 2022-03-31

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