CN111093645A - Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂 - Google Patents

Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂 Download PDF

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Publication number
CN111093645A
CN111093645A CN201880044480.8A CN201880044480A CN111093645A CN 111093645 A CN111093645 A CN 111093645A CN 201880044480 A CN201880044480 A CN 201880044480A CN 111093645 A CN111093645 A CN 111093645A
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alkyl
alkoxy
independently
cyano
compound
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CN201880044480.8A
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English (en)
Chinese (zh)
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宋运涛
A.J.布里奇斯
陈晓颀
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CS Pharmatech Ltd
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CS Pharmatech Ltd
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    • 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
    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN201880044480.8A 2017-07-05 2018-07-05 Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂 Pending CN111093645A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762528697P 2017-07-05 2017-07-05
US62/528697 2017-07-05
PCT/US2018/040904 WO2019010295A1 (en) 2017-07-05 2018-07-05 SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF EGFR TYROSINE KINASE

Publications (1)

Publication Number Publication Date
CN111093645A true CN111093645A (zh) 2020-05-01

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880044480.8A Pending CN111093645A (zh) 2017-07-05 2018-07-05 Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂

Country Status (7)

Country Link
US (1) US20200131176A1 (https=)
EP (1) EP3648753A4 (https=)
JP (1) JP2020526499A (https=)
KR (1) KR20200028966A (https=)
CN (1) CN111093645A (https=)
CA (1) CA3068854A1 (https=)
WO (1) WO2019010295A1 (https=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111566100A (zh) * 2018-02-12 2020-08-21 恩瑞生物医药科技（上海）有限公司 嘧啶类化合物、其制备方法及其医药用途
CN113651800A (zh) * 2021-09-07 2021-11-16 山东铂源药业有限公司 一种甲磺酸奥希替尼的制备方法
CN115667251A (zh) * 2021-05-17 2023-01-31 株式会社沃若诺伊生物 杂芳基衍生物化合物、及其用途
CN115650974A (zh) * 2022-08-04 2023-01-31 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-顺式戊二烯酰胺衍生物及应用

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3399968B8 (en) 2016-01-07 2021-12-01 Xuanzhu Biopharmaceutical Co., Ltd. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
US11352352B2 (en) * 2017-06-13 2022-06-07 Beijing Adamadle Biotechnology Limited Liability Company Aminopyrimidine compound, preparation method therefor and use thereof
AU2020240382B2 (en) 2019-03-19 2022-08-25 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN111747950B (zh) * 2019-03-29 2024-01-23 深圳福沃药业有限公司 用于治疗癌症的嘧啶衍生物
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
ES2969756T3 (es) 2019-10-03 2024-05-22 Bristol Myers Squibb Co Indazol carboxamidas como inhibidores de cinasas
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021104305A1 (zh) * 2019-11-26 2021-06-03 上海翰森生物医药科技有限公司 含氮多环类衍生物抑制剂、其制备方法和应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021243596A1 (en) * 2020-06-03 2021-12-09 InventisBio Co., Ltd. Aminopyrimidine compounds, preparation methods and uses thereof
KR20220085735A (ko) * 2020-12-14 2022-06-22 보로노이바이오 주식회사 아이소옥사졸리딘 유도체 화합물 및 이의 용도
CN117561254A (zh) * 2021-04-30 2024-02-13 苏州浦合医药科技有限公司 用于肺癌治疗的嘧啶基氨基苯
WO2024094064A1 (en) * 2022-11-02 2024-05-10 Suzhou Puhe Biopharma Co., Ltd Pyrimidinylaminobenzenes for treating lung cancer with distant metastasis
CN120035590A (zh) * 2022-11-03 2025-05-23 株式会社沃若诺伊 Egfr抑制剂的延胡索酸盐、酒石酸盐、苹果酸盐和柠檬酸盐

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI546290B (zh) * 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
CN104860941B (zh) * 2014-02-25 2017-03-22 上海海雁医药科技有限公司 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物
CN113563332B (zh) * 2014-12-23 2024-12-17 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
EP3399968B8 (en) * 2016-01-07 2021-12-01 Xuanzhu Biopharmaceutical Co., Ltd. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
JP6740452B2 (ja) * 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111566100A (zh) * 2018-02-12 2020-08-21 恩瑞生物医药科技（上海）有限公司 嘧啶类化合物、其制备方法及其医药用途
CN111566100B (zh) * 2018-02-12 2023-10-27 恩瑞生物医药科技（上海）有限公司 嘧啶类化合物、其制备方法及其医药用途
CN115667251A (zh) * 2021-05-17 2023-01-31 株式会社沃若诺伊生物 杂芳基衍生物化合物、及其用途
CN113651800A (zh) * 2021-09-07 2021-11-16 山东铂源药业有限公司 一种甲磺酸奥希替尼的制备方法
CN113651800B (zh) * 2021-09-07 2022-08-19 山东铂源药业股份有限公司 一种甲磺酸奥希替尼的制备方法
CN115650974A (zh) * 2022-08-04 2023-01-31 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-顺式戊二烯酰胺衍生物及应用

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Publication number Publication date
JP2020526499A (ja) 2020-08-31
KR20200028966A (ko) 2020-03-17
CA3068854A1 (en) 2019-01-10
WO2019010295A1 (en) 2019-01-10
US20200131176A1 (en) 2020-04-30
EP3648753A4 (en) 2021-03-17
EP3648753A1 (en) 2020-05-13

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