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CN111295384A - 双环类衍生物抑制剂、其制备方法和应用 - Google Patents

双环类衍生物抑制剂、其制备方法和应用 Download PDF

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Publication number
CN111295384A
CN111295384A CN201980005251.XA CN201980005251A CN111295384A CN 111295384 A CN111295384 A CN 111295384A CN 201980005251 A CN201980005251 A CN 201980005251A CN 111295384 A CN111295384 A CN 111295384A
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substituted
unsubstituted
cycloalkyl
aryl
heterocyclyl
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CN201980005251.XA
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CN111295384B (zh
Inventor
刘世强
鲍孟
袁逸达
王永升
周远锋
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)

Abstract

公开了含双环类衍生物抑制剂、其制备方法和应用。特别地，公开了涉及通式(I)所示的化合物、其制备方法及含有该化合物的药物组合物，及其作为蛋白质酪氨酸磷酸酶SHP‑2抑制剂，在治疗白血病、神经母细胞瘤、黑色素瘤、乳腺癌、肺癌及其结肠癌等疾病或病症的用途，其中通式(I)中的各取代基与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (23)

  1. PCT国内申请，权利要求书已公开。
CN201980005251.XA 2018-10-10 2019-10-10 双环类衍生物抑制剂、其制备方法和应用 Active CN111295384B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201811178108 2018-10-10
CN2018111781084 2018-10-10
PCT/CN2019/110306 WO2020073945A1 (zh) 2018-10-10 2019-10-10 双环类衍生物抑制剂、其制备方法和应用

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CN111295384A true CN111295384A (zh) 2020-06-16
CN111295384B CN111295384B (zh) 2022-08-12

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024513011A (ja) * 2021-03-29 2024-03-21 ニンバス サターン， インコーポレイテッド Ｈｐｋ１アンタゴニスト及びその使用
CN118994000A (zh) * 2024-07-30 2024-11-22 中国科学院合肥物质科学研究院 一种用于检测有机膦酸酯类神经毒剂及其水解产物的化合物及其应用

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018057884A1 (en) 2016-09-22 2018-03-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TWI848901B (zh) 2016-10-24 2024-07-21 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
KR20200139153A (ko) 2018-02-27 2020-12-11 인사이트 코포레이션 A2a / a2b 억제제로서의 이미다조피리미딘 및 트리아졸로피리미딘
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
EP4506035A3 (en) 2018-03-21 2025-04-16 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
JP7391046B2 (ja) 2018-05-18 2023-12-04 インサイト・コーポレイション Ａ２ａ／ａ２ｂ阻害剤としての縮合ピリミジン誘導体
CN117304191A (zh) 2018-07-05 2023-12-29 因赛特公司 作为a2a/a2b抑制剂的稠合吡嗪衍生物
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
EP4034539A1 (en) 2019-09-24 2022-08-03 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of making and using the same
JP7812056B2 (ja) 2019-11-08 2026-02-09 レヴォリューション・メディスンズ，インコーポレイテッド 二環式ヘテロアリール化合物及びその使用
CR20220354A (es) 2019-12-23 2022-12-19 Blueprint Medicines Corp Inhibidores de egfr
TW202214253A (zh) 2020-06-18 2022-04-16 美商銳新醫藥公司 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
CN117377673A (zh) * 2021-03-29 2024-01-09 林伯士萨顿公司 Hpk1拮抗剂和其用途
KR20240016974A (ko) * 2021-05-04 2024-02-06 상하이 즈헤예 바이오테크놀로지 씨오. 엘티디. 질소-함유 헤테로시클릭 피리딘 화합물
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
TW202309053A (zh) 2021-05-05 2023-03-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
JP2025521232A (ja) 2022-06-10 2025-07-08 レボリューション メディシンズ インコーポレイテッド 大環状ｒａｓ阻害剤
CN118344358A (zh) * 2023-01-16 2024-07-16 中国科学院上海有机化学研究所 Hpk1抑制剂及其制法和用途
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
EP4688790A1 (en) 2023-04-07 2026-02-11 Revolution Medicines, Inc. Macrocyclic ras inhibitors
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
KR20250169290A (ko) 2023-04-14 2025-12-02 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형, 이를 함유하는 조성물 및 이의 사용 방법
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025259899A1 (en) * 2024-06-13 2025-12-18 Oric Pharmaceuticals, Inc. Cip2a rna splice modifiers for use in treatment of cancer
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
CN118730998B (zh) * 2024-07-30 2025-03-28 中国科学院合肥物质科学研究院 一种用于神经毒剂检测的双分子共修饰金属sers衬底及其制备方法
CN118794937B (zh) * 2024-07-30 2025-03-07 中国科学院合肥物质科学研究院 一种用于有机膦神经毒剂痕量检测的双金属功能化sers衬底及其制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011246389A (ja) * 2010-05-26 2011-12-08 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有する縮環ピラゾール誘導体
CN102753548A (zh) * 2009-12-23 2012-10-24 武田药品工业株式会社 作为syk抑制剂的稠合的杂芳族吡咯烷酮
KR20130108876A (ko) * 2012-03-26 2013-10-07 중앙대학교 산학협력단 Ｓｈｐ－2의 활성을 특이적으로 저해하는 조성물 및 이의 제조방법
US20140171405A1 (en) * 2012-12-19 2014-06-19 Incyte Corporation Fused Pyrazoles as FGFR Inhibitors
WO2017210134A1 (en) * 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
US20180186815A1 (en) * 2016-12-29 2018-07-05 Urifer Ltd. Pharmaceutical compositions, methods for their preparation and their use in the treatment of cancer

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019165073A1 (en) * 2018-02-21 2019-08-29 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102753548A (zh) * 2009-12-23 2012-10-24 武田药品工业株式会社 作为syk抑制剂的稠合的杂芳族吡咯烷酮
JP2011246389A (ja) * 2010-05-26 2011-12-08 Oncotherapy Science Ltd Ｔｔｋ阻害作用を有する縮環ピラゾール誘導体
KR20130108876A (ko) * 2012-03-26 2013-10-07 중앙대학교 산학협력단 Ｓｈｐ－2의 활성을 특이적으로 저해하는 조성물 및 이의 제조방법
US20140171405A1 (en) * 2012-12-19 2014-06-19 Incyte Corporation Fused Pyrazoles as FGFR Inhibitors
WO2017210134A1 (en) * 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
US20180186815A1 (en) * 2016-12-29 2018-07-05 Urifer Ltd. Pharmaceutical compositions, methods for their preparation and their use in the treatment of cancer

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024513011A (ja) * 2021-03-29 2024-03-21 ニンバス サターン， インコーポレイテッド Ｈｐｋ１アンタゴニスト及びその使用
CN118994000A (zh) * 2024-07-30 2024-11-22 中国科学院合肥物质科学研究院 一种用于检测有机膦酸酯类神经毒剂及其水解产物的化合物及其应用
CN118994000B (zh) * 2024-07-30 2025-05-13 中国科学院合肥物质科学研究院 一种用于检测有机膦酸酯类神经毒剂及其水解产物的化合物及其应用

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