CN114728969A - 作为dna-pk抑制剂的嘧啶并咪唑类化合物 - Google Patents

作为dna-pk抑制剂的嘧啶并咪唑类化合物 Download PDF

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CN114728969A
CN114728969A CN202080081020.XA CN202080081020A CN114728969A CN 114728969 A CN114728969 A CN 114728969A CN 202080081020 A CN202080081020 A CN 202080081020A CN 114728969 A CN114728969 A CN 114728969A
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reaction
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reduced pressure
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CN114728969B (zh
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陈新海
夏尚华
陈兆国
郭祖浩
于衍新
周凯
胡伯羽
张丽
姜奋
王晶晶
胡国平
黎健
陈曙辉
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Zai Lab Shanghai Co ltd
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Medshine Discovery Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

一类DNA‑PK抑制剂，具体为式(IV)所示化合物或其药学上可接受的盐，及其在制备DNA‑PK抑制剂相关药物中的应用。

Description

PCT国内申请，说明书已公开。

Claims (14)

  1. PCT国内申请，权利要求书已公开。
CN202080081020.XA 2019-11-25 2020-11-25 作为dna-pk抑制剂的嘧啶并咪唑类化合物 Active CN114728969B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN2019111649615 2019-11-25
CN201911164961 2019-11-25
CN2020102093523 2020-03-23
CN202010209352 2020-03-23
CN2020109118790 2020-09-02
CN202010911879 2020-09-02
CN2020112697680 2020-11-13
CN202011269768 2020-11-13
PCT/CN2020/131275 WO2021104277A1 (zh) 2019-11-25 2020-11-25 作为dna-pk抑制剂的嘧啶并咪唑类化合物

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CN114728969A true CN114728969A (zh) 2022-07-08
CN114728969B CN114728969B (zh) 2024-03-08

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US (1) US20230026616A1 (zh)
EP (1) EP4067359A4 (zh)
JP (1) JP7383818B2 (zh)
KR (1) KR20220106799A (zh)
CN (1) CN114728969B (zh)
AU (1) AU2020390962B2 (zh)
CA (1) CA3159290A1 (zh)
IL (1) IL293318A (zh)
TW (1) TWI807228B (zh)
WO (1) WO2021104277A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113121573A (zh) * 2019-12-31 2021-07-16 成都百裕制药股份有限公司 嘌呤衍生物及其在医药上的应用

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI765640B (zh) * 2020-04-10 2022-05-21 大陸商南京明德新藥研發有限公司 作為dna-pk抑制劑的氨基嘧啶化合物及其衍生物
CN116406272A (zh) * 2020-07-20 2023-07-07 首药控股(北京)股份有限公司 Dna-pk选择性抑制剂及其制备方法和用途
CN114249753A (zh) * 2020-09-22 2022-03-29 山东轩竹医药科技有限公司 ***并吡啶类激酶抑制剂
WO2022135555A1 (zh) * 2020-12-24 2022-06-30 江苏恒瑞医药股份有限公司 嘌呤酮类化合物、其制备方法及其在医药上的应用
EP4342899A1 (en) * 2021-05-19 2024-03-27 Zai Lab (Shanghai) Co., Ltd. Salt form and crystal form of heterocyclic substituted purinone derivative
WO2023274310A1 (zh) * 2021-06-29 2023-01-05 成都百裕制药股份有限公司 嘌呤衍生物的晶型及其药物组合物
WO2023165603A1 (en) * 2022-03-03 2023-09-07 Zai Lab (Shanghai) Co., Ltd. Dna-pk inhibitor and combination use thereof

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WO2009062059A2 (en) * 2007-11-08 2009-05-14 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
CN101679412A (zh) * 2007-05-23 2010-03-24 药典有限责任公司 作为PKC-θ抑制剂的嘌呤酮类和1H-咪唑并吡啶酮类
US20120315291A1 (en) * 2010-02-10 2012-12-13 Glaxosmithkline Llc Purine derivatives and their pharmaceutical uses
CN103998036A (zh) * 2011-10-19 2014-08-20 西格诺药品有限公司 利用tor激酶抑制剂治疗癌症
CN110177791A (zh) * 2016-12-20 2019-08-27 阿斯利康(瑞典)有限公司 氨基-***并吡啶化合物及其在治疗癌症中的用途
TW202138372A (zh) * 2020-04-10 2021-10-16 大陸商南京明德新藥研發有限公司 作為ｄｎａ－ｐｋ抑制劑的氨基嘧啶化合物及其衍生物
CN113956272A (zh) * 2020-07-20 2022-01-21 首药控股(北京)有限公司 Dna-pk选择性抑制剂及其制备方法和用途
WO2022242658A1 (zh) * 2021-05-19 2022-11-24 南京明德新药研发有限公司 杂环取代的嘌呤酮衍生物的盐型及晶型

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US11052091B2 (en) * 2016-12-21 2021-07-06 Ono Pharmaceutical Co., Ltd. BRK inhibitory compound
TWI820146B (zh) 2018-06-15 2023-11-01 瑞典商阿斯特捷利康公司 嘌呤酮化合物及其在治療癌症中之用途
JP2023503931A (ja) * 2019-11-22 2023-02-01 メッドシャイン ディスカバリー インコーポレイテッド Ｄｎａ－ｐｋ阻害剤としてのピリミドピロール系スピロ化合物及びその誘導体
CN116406272A (zh) * 2020-07-20 2023-07-07 首药控股(北京)股份有限公司 Dna-pk选择性抑制剂及其制备方法和用途

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CN101679412A (zh) * 2007-05-23 2010-03-24 药典有限责任公司 作为PKC-θ抑制剂的嘌呤酮类和1H-咪唑并吡啶酮类
WO2009062059A2 (en) * 2007-11-08 2009-05-14 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
US20120315291A1 (en) * 2010-02-10 2012-12-13 Glaxosmithkline Llc Purine derivatives and their pharmaceutical uses
CN103998036A (zh) * 2011-10-19 2014-08-20 西格诺药品有限公司 利用tor激酶抑制剂治疗癌症
CN107157990A (zh) * 2011-10-19 2017-09-15 西格诺药品有限公司 利用tor激酶抑制剂治疗癌症
CN110177791A (zh) * 2016-12-20 2019-08-27 阿斯利康(瑞典)有限公司 氨基-***并吡啶化合物及其在治疗癌症中的用途
TW202138372A (zh) * 2020-04-10 2021-10-16 大陸商南京明德新藥研發有限公司 作為ｄｎａ－ｐｋ抑制劑的氨基嘧啶化合物及其衍生物
CN113956272A (zh) * 2020-07-20 2022-01-21 首药控股(北京)有限公司 Dna-pk选择性抑制剂及其制备方法和用途
WO2022242658A1 (zh) * 2021-05-19 2022-11-24 南京明德新药研发有限公司 杂环取代的嘌呤酮衍生物的盐型及晶型

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113121573A (zh) * 2019-12-31 2021-07-16 成都百裕制药股份有限公司 嘌呤衍生物及其在医药上的应用

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EP4067359A1 (en) 2022-10-05
JP7383818B2 (ja) 2023-11-20
IL293318A (en) 2022-07-01
WO2021104277A1 (zh) 2021-06-03
CN114728969B (zh) 2024-03-08
US20230026616A1 (en) 2023-01-26
JP2023504021A (ja) 2023-02-01
TW202120506A (zh) 2021-06-01
CA3159290A1 (en) 2021-06-03
AU2020390962A1 (en) 2022-07-14
KR20220106799A (ko) 2022-07-29
AU2020390962B2 (en) 2023-09-28
EP4067359A4 (en) 2024-01-10
TWI807228B (zh) 2023-07-01

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