CN114269746A - 一种螺芳环化合物、其制备及应用 - Google Patents

一种螺芳环化合物、其制备及应用 Download PDF

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Publication number
CN114269746A
CN114269746A CN202080053803.7A CN202080053803A CN114269746A CN 114269746 A CN114269746 A CN 114269746A CN 202080053803 A CN202080053803 A CN 202080053803A CN 114269746 A CN114269746 A CN 114269746A
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郑乾刚
曾庆龙
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Shanghai Yituo Pharmaceutical Technology Co ltd
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Shanghai Yituo Pharmaceutical Technology Co ltd
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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
    • A61K31/495—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
    • 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
    • A61K31/4985—Pyrazines or piperazines 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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D471/10—Spiro-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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明提供了具有SHP2抑制活性的化合物、其制备方法及用途，具体地，本发明提供了一种式(I)所示的化合物，其药学上可接受的盐，或其溶剂化物、同位素取代物、多晶型物、前药或代谢产物，其中，各基团的定义如说明书中所述。所述的化合物对SHP2具有较高的抑制活性，因此可以用于预防或治疗与SHP2相关的疾病。

Description

PCT国内申请，说明书已公开。

Claims (12)

  1. PCT国内申请，权利要求书已公开。
CN202080053803.7A 2019-08-01 2020-07-31 一种螺芳环化合物、其制备及应用 Pending CN114269746A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910705467.9A CN112300160A (zh) 2019-08-01 2019-08-01 一种螺芳环化合物、其制备及应用
CN2019107054679 2019-08-01
PCT/CN2020/106214 WO2021018287A1 (zh) 2019-08-01 2020-07-31 一种螺芳环化合物、其制备及应用

Publications (1)

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CN114269746A true CN114269746A (zh) 2022-04-01

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CN202080053803.7A Pending CN114269746A (zh) 2019-08-01 2020-07-31 一种螺芳环化合物、其制备及应用

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WO (1) WO2021018287A1 (zh)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11179397B2 (en) 2018-10-03 2021-11-23 Gilead Sciences, Inc. Imidazopyrimidine derivatives
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
EP4208261A1 (en) 2020-09-03 2023-07-12 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
KR20240004960A (ko) 2021-05-05 2024-01-11 레볼루션 메디슨즈, 인크. Ras 억제제
IL308195A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors for cancer treatment
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ｒａｓ阻害剤及びその使用
CN114716448B (zh) * 2021-05-13 2024-01-30 中国科学院上海药物研究所 抑制shp2活性的杂环化合物、其制备方法及用途
TW202313041A (zh) 2021-06-09 2023-04-01 瑞士商諾華公司 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
US20230102398A1 (en) * 2021-09-27 2023-03-30 New York University Therapeutic targeting of kmt2d mutant lung squamous cell carcinoma through rtk-ras signaling inhibition
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN115521305A (zh) * 2022-09-20 2022-12-27 中国药科大学 Shp2&nampt双靶向化合物及其药物组合物和用途

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105899491A (zh) * 2014-01-17 2016-08-24 诺华股份有限公司 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物
CN105916845A (zh) * 2014-01-17 2016-08-31 诺华股份有限公司 用于抑制shp2活性的n-氮杂螺环烷取代的n-杂芳基化合物和组合物
WO2018136265A1 (en) * 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
WO2019075265A1 (en) * 2017-10-12 2019-04-18 Revolution Medicines, Inc. PYRIDINE, PYRAZINE AND TRIAZINE COMPOUNDS AS ALLOSTERIC INHIBITORS OF SHP2
WO2019118909A1 (en) * 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
CN110156786A (zh) * 2018-02-13 2019-08-23 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CN111153901A (zh) * 2018-11-07 2020-05-15 如东凌达生物医药科技有限公司 一类含氮稠杂环类shp2抑制剂化合物、制备方法和用途
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116478132A (zh) * 2016-07-12 2023-07-25 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪
MX2019008696A (es) * 2017-01-23 2019-09-13 Revolution Medicines Inc Compuestos de piridina como inhibidores de shp2 alostericos.

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105899491A (zh) * 2014-01-17 2016-08-24 诺华股份有限公司 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物
CN105916845A (zh) * 2014-01-17 2016-08-31 诺华股份有限公司 用于抑制shp2活性的n-氮杂螺环烷取代的n-杂芳基化合物和组合物
WO2018136265A1 (en) * 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
WO2019075265A1 (en) * 2017-10-12 2019-04-18 Revolution Medicines, Inc. PYRIDINE, PYRAZINE AND TRIAZINE COMPOUNDS AS ALLOSTERIC INHIBITORS OF SHP2
WO2019118909A1 (en) * 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
CN110156786A (zh) * 2018-02-13 2019-08-23 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CN111153901A (zh) * 2018-11-07 2020-05-15 如东凌达生物医药科技有限公司 一类含氮稠杂环类shp2抑制剂化合物、制备方法和用途
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用

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