CN111315750A - 作为mTORC1/2双激酶抑制剂的吡啶并嘧啶类化合物 - Google Patents

作为mTORC1/2双激酶抑制剂的吡啶并嘧啶类化合物 Download PDF

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Publication number
CN111315750A
CN111315750A CN201880071134.9A CN201880071134A CN111315750A CN 111315750 A CN111315750 A CN 111315750A CN 201880071134 A CN201880071134 A CN 201880071134A CN 111315750 A CN111315750 A CN 111315750A
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compound
mol
reaction
pharmaceutically acceptable
optionally substituted
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CN201880071134.9A
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CN111315750B (zh
Inventor
陈新海
陈兆国
张丽
于衍新
周凯
胡伯羽
王校飞
胡国平
黎健
陈曙辉
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Medshine Discovery Inc
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Medshine Discovery Inc
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    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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

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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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本发明公开了一系列吡啶并嘧啶类化合物，及其制备mTORC1/2双激酶活性抑制剂相关药物中的应用，具体公开了式(IV)所示化合物、其互变异构体或其药学上可接受的盐在制备mTORC1/2双激酶活性抑制剂相关药物中的应用。

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN201880071134.9A 2017-11-06 2018-11-02 作为mTORC1/2双激酶抑制剂的吡啶并嘧啶类化合物 Active CN111315750B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201711080753 2017-11-06
CN2017110807538 2017-11-06
CN201810136962 2018-02-09
CN2018101369628 2018-02-09
CN201810661825 2018-06-25
CN2018106618256 2018-06-25
PCT/CN2018/113683 WO2019085996A1 (zh) 2017-11-06 2018-11-02 作为mTORC1/2双激酶抑制剂的吡啶并嘧啶类化合物

Publications (2)

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CN111315750A true CN111315750A (zh) 2020-06-19
CN111315750B CN111315750B (zh) 2022-12-23

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Country Status (7)

Country Link
US (1) US11377444B2 (zh)
EP (1) EP3712157A4 (zh)
JP (1) JP7340519B2 (zh)
CN (1) CN111315750B (zh)
BR (1) BR112020008991A2 (zh)
RU (1) RU2771201C2 (zh)
WO (1) WO2019085996A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020147842A1 (zh) * 2019-01-18 2020-07-23 南京明德新药研发有限公司 吡啶并嘧啶类化合物在制备治疗鼻咽癌药物中的应用
WO2020224585A1 (zh) * 2019-05-06 2020-11-12 南京明德新药研发有限公司 一种mTORC1/2双激酶活性抑制剂的盐型、晶型及其制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103030653A (zh) * 2011-09-30 2013-04-10 上海恒瑞医药有限公司 杂芳基并嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5161102B2 (ja) * 2005-11-22 2013-03-13 クドス ファーマシューティカルズ リミテッド ｍＴＯＲ阻害剤としてのピリドピリミジン、ピラゾピリミジンおよびピリミドピリミジン誘導体
CN101360746B (zh) 2005-11-22 2013-12-11 库多斯药物有限公司 作为mTOR抑制剂的吡啶并-、吡唑并-和嘧啶并-嘧啶衍生物
UA96304C2 (en) 2006-08-23 2011-10-25 Кудос Фармасьютикалз Лимитед 2-METHYLMORPHOLINE PYRIDO-, PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
SI2057156T1 (sl) 2006-08-23 2017-06-30 Kudos Pharmaceuticals Limited Derivati 2-metilmorfolin pirido-, pirazo- in pirimido-pirimidina kot inhibitorji mTOR
AU2009276339B2 (en) * 2008-07-31 2012-06-07 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
GB201004200D0 (en) * 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103030653A (zh) * 2011-09-30 2013-04-10 上海恒瑞医药有限公司 杂芳基并嘧啶类衍生物及其可药用盐、其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
EP3712157A1 (en) 2020-09-23
RU2771201C2 (ru) 2022-04-28
EP3712157A4 (en) 2021-04-28
JP2021501778A (ja) 2021-01-21
JP7340519B2 (ja) 2023-09-07
BR112020008991A2 (pt) 2020-11-17
US20200339568A1 (en) 2020-10-29
WO2019085996A1 (zh) 2019-05-09
US11377444B2 (en) 2022-07-05
RU2020118222A3 (zh) 2021-12-08
RU2020118222A (ru) 2021-12-08
CN111315750B (zh) 2022-12-23

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