CN115397815A - 稠合二环类衍生物、其制备方法及其在医药上的应用 - Google Patents

稠合二环类衍生物、其制备方法及其在医药上的应用 Download PDF

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Publication number
CN115397815A
CN115397815A CN202180013602.9A CN202180013602A CN115397815A CN 115397815 A CN115397815 A CN 115397815A CN 202180013602 A CN202180013602 A CN 202180013602A CN 115397815 A CN115397815 A CN 115397815A
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formula
compound
group
pharmaceutically acceptable
tautomer
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CN202180013602.9A
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CN115397815B (zh
Inventor
李心
张志高
陈阳
李之浩
贺峰
陶维康
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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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    • 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
    • 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
    • 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
    • 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
    • C07D487/08—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
    • C07D498/02—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 two hetero rings
    • C07D498/08—Bridged 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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

一种通式(I)所示的稠合二环类衍生物、其制备方法及含有该衍生物的药物组合物以及其作为治疗剂的用途，特别是作为AKT1/2/3(AKT pan)抑制剂的用途和用于制备治疗和/或预防肿瘤的药物中的用途。通式(I)中各基团的定义如说明书中所定义。

Description

PCT国内申请，说明书已公开。

Claims (27)

  1. PCT国内申请，权利要求书已公开。
CN202180013602.9A 2020-03-17 2021-03-16 稠合二环类衍生物、其制备方法及其在医药上的应用 Active CN115397815B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN202010185224 2020-03-17
CN202010185224X 2020-03-17
CN2020104184531 2020-05-18
CN202010418453 2020-05-18
CN2021102411592 2021-03-04
CN202110241159 2021-03-04
PCT/CN2021/081033 WO2021185238A1 (zh) 2020-03-17 2021-03-16 稠合二环类衍生物、其制备方法及其在医药上的应用

Publications (2)

Publication Number Publication Date
CN115397815A true CN115397815A (zh) 2022-11-25
CN115397815B CN115397815B (zh) 2024-06-14

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Country Link
US (1) US20230148417A1 (zh)
EP (1) EP4122922A4 (zh)
JP (1) JP2023520140A (zh)
KR (1) KR20220154722A (zh)
CN (1) CN115397815B (zh)
AU (1) AU2021238799A1 (zh)
BR (1) BR112022017856A2 (zh)
CA (1) CA3167999A1 (zh)
MX (1) MX2022011188A (zh)
TW (1) TW202136269A (zh)
WO (1) WO2021185238A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117940410A (zh) * 2021-09-17 2024-04-26 江苏恒瑞医药股份有限公司 一种稠合二环类衍生物的可药用盐、晶型及其制备方法

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006071819A1 (en) * 2004-12-28 2006-07-06 Exelixis, Inc. [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
WO2008075109A1 (en) * 2006-12-21 2008-06-26 Astex Therapeutics Limited Substituted piperidines having protein kinase inhibiting activity
CN101918373A (zh) * 2007-07-05 2010-12-15 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
CN102216302A (zh) * 2008-11-11 2011-10-12 伊莱利利公司 Akt和p70 s6激酶抑制剂
CN102574857A (zh) * 2009-07-08 2012-07-11 利奥制药有限公司 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物
CN107074867A (zh) * 2014-08-21 2017-08-18 辉瑞公司 作为jak抑制剂的氨基嘧啶基化合物
CN108368112A (zh) * 2015-12-18 2018-08-03 豪夫迈·罗氏有限公司 治疗性化合物、组合物和它们的使用方法
WO2019078619A1 (en) * 2017-10-18 2019-04-25 Cj Healthcare Corporation HETEROCYCLIC COMPOUND FOR USE AS A PROTEIN KINASE INHIBITOR

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2450522B (en) 2007-06-29 2011-12-07 Motorola Inc Method and apparatus for determining beamforming weights for an antenna array
JP5635910B2 (ja) 2008-01-09 2014-12-03 アレイ バイオファーマ、インコーポレイテッド ＡＫＴタンパク質キナーゼ阻害剤としての５Ｈ−シクロペンタ［ｄ］ピリミジン

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006071819A1 (en) * 2004-12-28 2006-07-06 Exelixis, Inc. [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
WO2008075109A1 (en) * 2006-12-21 2008-06-26 Astex Therapeutics Limited Substituted piperidines having protein kinase inhibiting activity
US20100093748A1 (en) * 2006-12-21 2010-04-15 Astex Therapeutics Limited Substituted piperidines having protein kinase inhibiting activity
CN101918373A (zh) * 2007-07-05 2010-12-15 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
CN102216302A (zh) * 2008-11-11 2011-10-12 伊莱利利公司 Akt和p70 s6激酶抑制剂
CN102574857A (zh) * 2009-07-08 2012-07-11 利奥制药有限公司 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物
CN107074867A (zh) * 2014-08-21 2017-08-18 辉瑞公司 作为jak抑制剂的氨基嘧啶基化合物
CN108368112A (zh) * 2015-12-18 2018-08-03 豪夫迈·罗氏有限公司 治疗性化合物、组合物和它们的使用方法
WO2019078619A1 (en) * 2017-10-18 2019-04-25 Cj Healthcare Corporation HETEROCYCLIC COMPOUND FOR USE AS A PROTEIN KINASE INHIBITOR

Also Published As

Publication number Publication date
KR20220154722A (ko) 2022-11-22
CN115397815B (zh) 2024-06-14
EP4122922A4 (en) 2023-08-23
CA3167999A1 (en) 2021-09-23
BR112022017856A2 (pt) 2022-11-01
TW202136269A (zh) 2021-10-01
AU2021238799A1 (en) 2022-09-22
EP4122922A1 (en) 2023-01-25
WO2021185238A1 (zh) 2021-09-23
JP2023520140A (ja) 2023-05-16
MX2022011188A (es) 2022-11-08
US20230148417A1 (en) 2023-05-11

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