TWI811358B - ＥｒｂＢ受體抑制劑 - Google Patents

ＥｒｂＢ受體抑制劑 Download PDF

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Publication number
TWI811358B
TWI811358B TW108115721A TW108115721A TWI811358B TW I811358 B TWI811358 B TW I811358B TW 108115721 A TW108115721 A TW 108115721A TW 108115721 A TW108115721 A TW 108115721A TW I811358 B TWI811358 B TW I811358B
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TW
Taiwan
Prior art keywords
compound
alkyl
pharmaceutically acceptable
acceptable salt
halogen
Prior art date
Application number
TW108115721A
Other languages
English (en)
Chinese (zh)
Other versions
TW202015690A (zh
Inventor
李正濤
鍾衛
家秉 王
慶北 曾
漢忠 徐
楊振帆
小林 張
Original Assignee
大陸商迪哲（江蘇）醫藥股份有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication of TW202015690A publication Critical patent/TW202015690A/zh
Application granted granted Critical
Publication of TWI811358B publication Critical patent/TWI811358B/zh

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Classifications

    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW108115721A 2018-05-08 2019-05-07 ＥｒｂＢ受體抑制劑 TWI811358B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
WOPCT/CN2018/085998 2018-05-08
CN2018085998 2018-05-08

Publications (2)

Publication Number Publication Date
TW202015690A TW202015690A (zh) 2020-05-01
TWI811358B true TWI811358B (zh) 2023-08-11

Family

ID=68467752

Family Applications (2)

Application Number Title Priority Date Filing Date
TW108115721A TWI811358B (zh) 2018-05-08 2019-05-07 ＥｒｂＢ受體抑制劑
TW112129260A TWI858848B (zh) 2018-05-08 2019-05-07 ＥｒｂＢ受體抑制劑

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW112129260A TWI858848B (zh) 2018-05-08 2019-05-07 ＥｒｂＢ受體抑制劑

Country Status (14)

Country Link
US (2) US10822334B2 (enExample)
EP (2) EP3814341B1 (enExample)
JP (2) JP7540953B2 (enExample)
KR (1) KR102806778B1 (enExample)
CN (4) CN111587248A (enExample)
AR (1) AR117424A1 (enExample)
AU (1) AU2019267959B2 (enExample)
CA (1) CA3099315A1 (enExample)
DK (1) DK3814341T3 (enExample)
ES (1) ES2977196T3 (enExample)
MX (2) MX2020011868A (enExample)
PT (1) PT3814341T (enExample)
TW (2) TWI811358B (enExample)
WO (1) WO2019214634A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI858848B (zh) * 2018-05-08 2024-10-11 大陸商迪哲（江蘇）醫藥股份有限公司 ＥｒｂＢ受體抑制劑

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WO2019196622A1 (zh) * 2018-04-09 2019-10-17 威尚（上海）生物医药有限公司 具有穿过血脑屏障能力的5取代二氟哌啶化合物
CN110357858B (zh) 2018-04-09 2022-02-18 威尚（上海）生物医药有限公司 具有穿过血脑屏障能力的5取代二氟哌啶化合物
HRP20240293T1 (hr) 2018-09-18 2024-05-24 F. Hoffmann - La Roche Ag Derivati kinazolina kao protutumorska sredstva
AR117788A1 (es) * 2019-01-14 2021-08-25 Pi Industries Ltd Compuestos de fenilamidina 3-sustituida, preparación y uso
TWI879751B (zh) * 2020-03-23 2025-04-11 印度商皮埃企業有限公司 3-被取代的苯基脒化合物及其製備和用途
KR20230167009A (ko) * 2020-10-05 2023-12-07 다나-파버 캔서 인스티튜트 인크. Her2에 대한 강력하고 선택적인 억제제
TW202309022A (zh) 2021-04-13 2023-03-01 美商努法倫特公司 用於治療具egfr突變之癌症之胺基取代雜環
CR20240163A (es) * 2021-10-20 2024-06-12 Hoffmann La Roche Formas cristalinas de derivados de quinazolina, preparación, composición y uso de estas
CN114262327B (zh) * 2021-12-30 2023-01-03 武汉九州钰民医药科技有限公司 一种her2小分子抑制剂图卡替尼的制备工艺
CN114671867B (zh) * 2022-03-15 2023-09-19 上海法默生物科技有限公司 妥卡替尼中间体7-羟基-[1,2,4]三唑并[1,5-a]吡啶的制备方法
US20250206760A1 (en) * 2022-03-28 2025-06-26 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Nitrogen-containing heterocyclic compound, preparation method therefor, and pharmaceutical application thereof
JPWO2024043252A1 (enExample) 2022-08-24 2024-02-29
AU2023410324A1 (en) 2022-12-22 2025-05-15 Boehringer Ingelheim International Gmbh Crystalline forms of a her2 inhibitor
CN116102491A (zh) * 2023-02-17 2023-05-12 浙江晖石药业有限公司 一种利用连续流技术进行金属催化偶联的应用
TW202446386A (zh) * 2023-04-14 2024-12-01 大陸商迪哲（江蘇）醫藥股份有限公司 喹唑啉ＥｒｂＢ抑制劑的藥物形式
CN116903615A (zh) * 2023-06-21 2023-10-20 江苏丽源医药有限公司 一种妥卡替尼及其中间体的制备方法
CN121568696A (zh) 2023-07-28 2026-02-24 勃林格殷格翰国际有限公司 制备her2抑制剂的方法
CN119320383A (zh) * 2023-09-05 2025-01-17 北京鞍石生物科技股份有限公司 含氮杂芳基化合物及其制备方法和应用
CN117534669A (zh) * 2023-11-01 2024-02-09 上海凌凯医药科技有限公司 五元氮杂环并吡啶醇的制备方法
CN117658818B (zh) * 2023-11-03 2025-02-07 江西巍华化学有限公司 一种4-氟-3-硝基三氟甲苯的制备方法

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2003040109A2 (en) * 2001-11-03 2003-05-15 Astrazeneca Ab Quinazoline derivatives as antitumor agents
WO2006092573A1 (en) * 2005-03-04 2006-09-08 Astrazeneca Ab Indazolylamino qionazoline derivatives as antitumor agents

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US5994071A (en) 1997-04-04 1999-11-30 Albany Medical College Assessment of prostate cancer
RU2004116911A (ru) * 2001-11-03 2005-11-10 Астразенека Аб (Se) Производные хиназолина в качестве противоопухолевых средств
GB0321648D0 (en) * 2003-09-16 2003-10-15 Astrazeneca Ab Quinazoline derivatives
ES2354457T3 (es) * 2005-09-20 2011-03-15 Astrazeneca Ab Compuestos de 4-(1h-indazol-5-il-amino)-quinazolina como inhibidores del receptor erbb de la tirosina quinasa para el tratamiento del cáncer.
CN101273033A (zh) * 2005-09-20 2008-09-24 阿斯利康(瑞典)有限公司 作为治疗癌症的erbb受体酪氨酸激酶抑制剂的4-（1h-吲哚-5-基-氨基）-喹唑啉化合物
DE602006021645D1 (de) * 2005-11-15 2011-06-09 Array Biopharma Inc Verfahren und Zwischenverbindungen zur Herstellung von N4-Phenyl-Quinazolin-4-Amin Derivaten
TWI811358B (zh) * 2018-05-08 2023-08-11 大陸商迪哲（江蘇）醫藥股份有限公司 ＥｒｂＢ受體抑制劑

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003040109A2 (en) * 2001-11-03 2003-05-15 Astrazeneca Ab Quinazoline derivatives as antitumor agents
WO2006092573A1 (en) * 2005-03-04 2006-09-08 Astrazeneca Ab Indazolylamino qionazoline derivatives as antitumor agents

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI858848B (zh) * 2018-05-08 2024-10-11 大陸商迪哲（江蘇）醫藥股份有限公司 ＥｒｂＢ受體抑制劑

Also Published As

Publication number Publication date
CN111747953B (zh) 2021-05-07
CA3099315A1 (en) 2019-11-14
TW202015690A (zh) 2020-05-01
KR20210013071A (ko) 2021-02-03
AU2019267959A1 (en) 2020-11-26
AU2019267959B2 (en) 2024-06-06
US20200317669A1 (en) 2020-10-08
EP3814341A4 (en) 2022-01-05
BR112020022829A2 (pt) 2021-02-02
CN112266384A (zh) 2021-01-26
CN111662289A (zh) 2020-09-15
AR117424A1 (es) 2021-08-04
EP3814341A1 (en) 2021-05-05
PT3814341T (pt) 2024-04-11
TW202344253A (zh) 2023-11-16
ES2977196T3 (es) 2024-08-20
EP4410291A3 (en) 2024-08-14
EP3814341B1 (en) 2024-03-20
CN111747953A (zh) 2020-10-09
CN112266384B (zh) 2022-09-23
JP2024050653A (ja) 2024-04-10
US11447492B2 (en) 2022-09-20
JP2021523159A (ja) 2021-09-02
US20210009587A1 (en) 2021-01-14
WO2019214634A1 (en) 2019-11-14
KR102806778B1 (ko) 2025-05-12
US10822334B2 (en) 2020-11-03
EP4410291A2 (en) 2024-08-07
TWI858848B (zh) 2024-10-11
JP7810734B2 (ja) 2026-02-03
CN111587248A (zh) 2020-08-25
MX2020011868A (es) 2021-02-26
JP7540953B2 (ja) 2024-08-27
DK3814341T3 (da) 2024-04-22
MX2023008954A (es) 2023-08-18

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