CN106687457B - 用于激酶抑制的杂芳基化合物 - Google Patents

用于激酶抑制的杂芳基化合物 Download PDF

Info

Publication number
CN106687457B
CN106687457B CN201580037958.0A CN201580037958A CN106687457B CN 106687457 B CN106687457 B CN 106687457B CN 201580037958 A CN201580037958 A CN 201580037958A CN 106687457 B CN106687457 B CN 106687457B
Authority
CN
China
Prior art keywords
amino
group
methyl
alkyl
dihydro
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201580037958.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN106687457A (zh
Inventor
黄卫生
李峰
戴维·C·达尔加诺
巩永进
阿乐克谢·V·爱什陈科
安娜·科尔曼
威廉·C·莎士比亚
安吉拉·V·维斯特
徐永进
杨颖文
张蕴
周天军
朱笑天
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Takeda Pharmaceutical Co Ltd
Original Assignee
Ariad Pharmaceuticals Inc
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.)
Filing date
Publication date
Application filed by Ariad Pharmaceuticals Inc filed Critical Ariad Pharmaceuticals Inc
Publication of CN106687457A publication Critical patent/CN106687457A/zh
Application granted granted Critical
Publication of CN106687457B publication Critical patent/CN106687457B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D471/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201580037958.0A 2014-05-13 2015-05-13 用于激酶抑制的杂芳基化合物 Expired - Fee Related CN106687457B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461992742P 2014-05-13 2014-05-13
US61/992,742 2014-05-13
PCT/US2015/030522 WO2015175632A1 (en) 2014-05-13 2015-05-13 Heteroaryl compounds for kinase inhibition

Publications (2)

Publication Number Publication Date
CN106687457A CN106687457A (zh) 2017-05-17
CN106687457B true CN106687457B (zh) 2020-01-10

Family

ID=54480594

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580037958.0A Expired - Fee Related CN106687457B (zh) 2014-05-13 2015-05-13 用于激酶抑制的杂芳基化合物

Country Status (5)

Country Link
US (1) US20170166598A1 (https=)
EP (1) EP3143015B1 (https=)
JP (1) JP6468611B2 (https=)
CN (1) CN106687457B (https=)
WO (1) WO2015175632A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12466825B2 (en) 2019-11-14 2025-11-11 Amgen Inc. Synthesis of KRAS G12C inhibitor compound

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3778584A1 (en) * 2014-06-19 2021-02-17 ARIAD Pharmaceuticals, Inc. Production process of 2-chloro-4-heteroaryl-pyrimidine derivatives
WO2016054987A1 (zh) * 2014-10-11 2016-04-14 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
CN105085489B (zh) 2014-11-05 2019-03-01 益方生物科技（上海）有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
CA2984586C (en) 2015-04-29 2021-02-16 Guangdong Zhongsheng Pharmaceutical Co., Ltd. Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor
EP3294712A4 (en) * 2015-05-13 2018-11-07 ARIAD Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN106810553B (zh) * 2015-11-30 2020-03-17 江苏正大丰海制药有限公司 3-(4,5-取代氨基嘧啶)苯基衍生物及其应用
TWI726968B (zh) 2016-01-07 2021-05-11 開曼群島商Ｃｓ醫藥技術公司 Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑
CN107344934B (zh) * 2016-05-04 2019-08-23 江苏正大丰海制药有限公司 药物活性物质的固体形式
WO2018050108A1 (zh) * 2016-09-19 2018-03-22 江苏正大丰海制药有限公司 氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用
WO2018079310A1 (ja) 2016-10-31 2018-05-03 大鵬薬品工業株式会社 エクソン２０挿入変異型ｅｇｆｒ選択的阻害剤
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． Ｅｇｆｒタンパク質分解標的化キメラ分子およびその関連する使用方法
AR111469A1 (es) 2017-04-21 2019-07-17 Yuhan Corp Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma
SG11201913517UA (en) 2017-07-28 2020-02-27 Yuhan Corp Improved process for preparing aminopyrimidine derivatives
PL3677266T3 (pl) 2017-09-01 2024-07-01 Taiho Pharmaceutical Co., Ltd. Selektywny inhibitor egfr z mutacją w eksonie 18 i/lub eksonie 21
EP3613738A1 (en) * 2018-08-23 2020-02-26 Lead Discovery Center GmbH 4-substituted pyrrolo[2,3-b]pyridine as erbb modulators useful for treating cancer
ES3033635T3 (en) * 2018-12-28 2025-08-06 Taiho Pharmaceutical Co Ltd L718 and/or l792 mutant treatment-resistant egfr inhibitor for use in the treatment of cancer
PT3943491T (pt) 2019-03-19 2025-07-28 Voronoi Inc Derivado de heteroarilo, método para a produção do mesmo e composição farmacêutica que compreende o mesmo como componente eficaz
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
DK3959211T3 (da) * 2019-04-24 2026-04-27 Bayer Ag 4h-pyrrol[3,2-c]pyridin-4-on-forbindelser
US12433597B2 (en) * 2019-06-04 2025-10-07 Trisalus Life Sciences, Inc. Atraumatic occlusive system with compartment for measurement of vascular pressure change
MX2022003004A (es) 2019-09-13 2022-04-07 Holistick Medical Implante medico, dispositivo de colocacion, metodo de produccion de un implante medico y metodo de colocacion de un implante medico.
CN110746307B (zh) * 2019-11-01 2021-07-06 韶远科技（上海)有限公司 一种1-硝基-2-乙基-4-氟苯的制备方法
WO2021094379A1 (en) 2019-11-12 2021-05-20 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
WO2021148396A1 (en) 2020-01-20 2021-07-29 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
JP7626774B2 (ja) * 2020-02-03 2025-02-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン
EP4100409B1 (en) 2020-02-03 2024-08-28 Boehringer Ingelheim International GmbH [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors
US11608343B2 (en) 2020-04-24 2023-03-21 Boehringer Ingelheim International Gmbh Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
KR20230094197A (ko) 2020-09-23 2023-06-27 스코르피온 테라퓨틱스, 인코퍼레이티드 암 치료에 유용한 피롤로[3,2-c]피리딘-4-온 유도체들
WO2022072632A1 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
TW202229282A (zh) 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
KR20230107419A (ko) 2020-10-09 2023-07-14 스코르피온 테라퓨틱스, 인코퍼레이티드 암 치료 방법
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
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
TW202317106A (zh) * 2021-08-27 2023-05-01 南韓商柳韓洋行 作為egfr抑制劑之取代胺基吡啶化合物
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer
JP2025510910A (ja) 2022-03-31 2025-04-15 アストラゼネカ・アクチエボラーグ 癌の処置のための、ａｋｔ阻害剤との組み合わせにおける上皮成長因子受容体（ｅｇｆｒ）チロシンキナーゼ阻害剤
CN114957224B (zh) * 2022-05-17 2024-03-19 浙大城市学院 一种肿瘤低氧靶向的egfr抑制剂及其应用
CA3259492A1 (en) 2022-06-27 2024-01-04 Astrazeneca Ab COMBINATIONS INVOLVING EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER
KR20250044679A (ko) 2022-07-08 2025-04-01 아스트라제네카 아베 암 치료를 위한 hgf-수용체 억제제와 병용의 상피 성장 인자 수용체 티로신 키나아제 억제제
WO2024122617A1 (ja) * 2022-12-08 2024-06-13 塩野義製薬株式会社 セロトニン受容体結合活性を有する含窒素複素環および炭素環誘導体
WO2024254298A1 (en) 2023-06-08 2024-12-12 Scorpion Therapeutics, Inc. A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer
CN121712773A (zh) 2023-06-08 2026-03-20 安塔列斯疗法股份有限公司 1,5-二氢-4h-吡咯并[3,2-c]吡啶-4-酮用于癌症治疗

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158571A1 (en) * 2008-06-27 2009-12-30 Avila Therapeutics And Uses Thereof Heteroaryl compounds and uses thereof
WO2013014448A1 (en) * 2011-07-27 2013-01-31 Astrazeneca Ab 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0311274D0 (en) * 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
PT1948180E (pt) * 2005-11-11 2013-05-10 Boehringer Ingelheim Int Tratamento de combinação de cancro compreendendo inibidores de egfr/her2
PL2171090T3 (pl) * 2007-06-08 2013-09-30 Genentech Inc Markery ekspresji genów odporności guza na leczenie hamujące HER2
CN101723936B (zh) * 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
US9908884B2 (en) * 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
WO2011082266A2 (en) * 2009-12-30 2011-07-07 Arqule, Inc. Substituted heterocyclic compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158571A1 (en) * 2008-06-27 2009-12-30 Avila Therapeutics And Uses Thereof Heteroaryl compounds and uses thereof
WO2013014448A1 (en) * 2011-07-27 2013-01-31 Astrazeneca Ab 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR);Richard A. Ward,et al.;《Journal of Medicinal Chemistry》;20130809;第56卷;第7025-7048页 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12466825B2 (en) 2019-11-14 2025-11-11 Amgen Inc. Synthesis of KRAS G12C inhibitor compound

Also Published As

Publication number Publication date
CN106687457A (zh) 2017-05-17
WO2015175632A1 (en) 2015-11-19
EP3143015B1 (en) 2019-02-20
EP3143015A1 (en) 2017-03-22
JP2017518282A (ja) 2017-07-06
JP6468611B2 (ja) 2019-02-13
EP3143015A4 (en) 2017-11-01
US20170166598A1 (en) 2017-06-15

Similar Documents

Publication Publication Date Title
JP7212733B2 (ja) キナーゼ阻害のためのヘテロアリール化合物
CN106687457B (zh) 用于激酶抑制的杂芳基化合物
US20210323976A1 (en) Heteroaryl compounds for kinase inhibition
HK40018134B (en) Heteroaryl compounds for kinase inhibition
HK40018134A (en) Heteroaryl compounds for kinase inhibition
HK1237764B (zh) 用於激酶抑制的杂芳基化合物
HK40001021A (en) Heteroaryl compounds for kinase inhibition
HK40001021B (en) Heteroaryl compounds for kinase inhibition
HK1237764A1 (en) Heteroaryl compounds for kinase inhibition
HK1236525B (en) Heteroaryl compounds for kinase inhibition
HK1236525A1 (en) Heteroaryl compounds for kinase inhibition

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1237764

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
TR01 Transfer of patent right
TR01 Transfer of patent right

Effective date of registration: 20220408

Address after: Osaka, Japan

Patentee after: TAKEDA PHARMACEUTICAL Co.,Ltd.

Address before: Massachusetts

Patentee before: ARIAD PHARMACEUTICALS, Inc.

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20200110