TWI858848B - ＥｒｂＢ受體抑制劑 - Google Patents

ＥｒｂＢ受體抑制劑 Download PDF

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Publication number
TWI858848B
TWI858848B TW112129260A TW112129260A TWI858848B TW I858848 B TWI858848 B TW I858848B TW 112129260 A TW112129260 A TW 112129260A TW 112129260 A TW112129260 A TW 112129260A TW I858848 B TWI858848 B TW I858848B
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TW
Taiwan
Prior art keywords
compound
compounds
mixture
mmol
stirred
Prior art date
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TW112129260A
Other languages
English (en)
Chinese (zh)
Other versions
TW202344253A (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
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Publication of TW202344253A publication Critical patent/TW202344253A/zh
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Publication of TWI858848B publication Critical patent/TWI858848B/zh

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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
    • 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
    • A61P35/04—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
    • 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (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)
TW112129260A 2018-05-08 2019-05-07 ＥｒｂＢ受體抑制劑 TWI858848B (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
TW202344253A TW202344253A (zh) 2023-11-16
TWI858848B true TWI858848B (zh) 2024-10-11

Family

ID=68467752

Family Applications (2)

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

Family Applications After (1)

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

Country Status (15)

Country Link
US (2) US10822334B2 (https=)
EP (2) EP4410291A3 (https=)
JP (2) JP7540953B2 (https=)
KR (1) KR102806778B1 (https=)
CN (4) CN112266384B (https=)
AR (1) AR117424A1 (https=)
AU (1) AU2019267959B2 (https=)
BR (1) BR112020022829A2 (https=)
CA (1) CA3099315A1 (https=)
DK (1) DK3814341T3 (https=)
ES (1) ES2977196T3 (https=)
MX (2) MX2020011868A (https=)
PT (1) PT3814341T (https=)
TW (2) TWI858848B (https=)
WO (1) WO2019214634A1 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
EP4523755A3 (en) * 2018-09-18 2025-06-11 F. Hoffmann-La Roche AG Quinazoline derivatives as antitumor agents
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
CA3194724A1 (en) * 2020-10-05 2022-04-14 Dana-Farber Cancer Institute, Inc. Potent and selective inhibitors of her2
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
IL312004A (en) * 2021-10-20 2024-06-01 Hoffmann La Roche Crystalline forms of quinazoline derivatives, their preparation, assembly and use
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
CN118715216A (zh) * 2022-03-28 2024-09-27 江苏恒瑞医药股份有限公司 含氮杂环类化合物、其制备方法及其在医药上的应用
AU2023329558A1 (en) 2022-08-24 2025-02-27 Toray Industries, Inc. Medicament for treatment and/or prevention of cancer
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
WO2025051148A1 (zh) * 2023-09-05 2025-03-13 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 (3)

* 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
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

Family Cites Families (6)

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US5994071A (en) 1997-04-04 1999-11-30 Albany Medical College Assessment of prostate cancer
US20050043336A1 (en) * 2001-11-03 2005-02-24 Hennequin Laurent Francois Andre Quinazoline derivatives as antitumor agents
GB0321648D0 (en) * 2003-09-16 2003-10-15 Astrazeneca Ab Quinazoline derivatives
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
ATE488513T1 (de) * 2005-09-20 2010-12-15 Astrazeneca Ab 4-(1h-indazol-5-ylamino)chinazolinverbindungen als inhibitoren der erbb-rezeptortyrosinkinase zur behandlung von krebs
ATE446294T1 (de) * 2005-11-15 2009-11-15 Array Biopharma Inc N4-phenyl-chinazolin-4-aminderivate und verwandte verbindungen als inhibitoren der erbb-typ-i- rezeptortyrosinkinase zur behandlung hyperproliferativer krankheiten

Patent Citations (3)

* 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
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

Also Published As

Publication number Publication date
US20210009587A1 (en) 2021-01-14
MX2023008954A (es) 2023-08-18
CN111587248A (zh) 2020-08-25
DK3814341T3 (da) 2024-04-22
US11447492B2 (en) 2022-09-20
CN111662289A (zh) 2020-09-15
MX2020011868A (es) 2021-02-26
CN111747953B (zh) 2021-05-07
KR20210013071A (ko) 2021-02-03
ES2977196T3 (es) 2024-08-20
US20200317669A1 (en) 2020-10-08
KR102806778B1 (ko) 2025-05-12
PT3814341T (pt) 2024-04-11
TW202015690A (zh) 2020-05-01
JP2021523159A (ja) 2021-09-02
EP3814341A4 (en) 2022-01-05
AU2019267959A1 (en) 2020-11-26
US10822334B2 (en) 2020-11-03
EP3814341B1 (en) 2024-03-20
AU2019267959B2 (en) 2024-06-06
JP7810734B2 (ja) 2026-02-03
CN112266384A (zh) 2021-01-26
JP2024050653A (ja) 2024-04-10
WO2019214634A1 (en) 2019-11-14
CA3099315A1 (en) 2019-11-14
TW202344253A (zh) 2023-11-16
AR117424A1 (es) 2021-08-04
JP7540953B2 (ja) 2024-08-27
EP3814341A1 (en) 2021-05-05
EP4410291A3 (en) 2024-08-14
EP4410291A2 (en) 2024-08-07
TWI811358B (zh) 2023-08-11
BR112020022829A2 (pt) 2021-02-02
CN111747953A (zh) 2020-10-09
CN112266384B (zh) 2022-09-23

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