KR20180105161A - Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제 - Google Patents

Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제 Download PDF

Info

Publication number
KR20180105161A
KR20180105161A KR1020187022731A KR20187022731A KR20180105161A KR 20180105161 A KR20180105161 A KR 20180105161A KR 1020187022731 A KR1020187022731 A KR 1020187022731A KR 20187022731 A KR20187022731 A KR 20187022731A KR 20180105161 A KR20180105161 A KR 20180105161A
Authority
KR
South Korea
Prior art keywords
alkyl
independently
alkoxy
methyl
compound
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.)
Withdrawn
Application number
KR1020187022731A
Other languages
English (en)
Korean (ko)
Inventor
윤타오 송
알렉산더 제임스 브리지스
Original Assignee
씨에스 파마테크 리미티드
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 씨에스 파마테크 리미티드 filed Critical 씨에스 파마테크 리미티드
Publication of KR20180105161A publication Critical patent/KR20180105161A/ko
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/135Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F20/00Homopolymers and copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide or nitrile thereof
    • C08F20/02Monocarboxylic acids having less than ten carbon atoms, Derivatives thereof
    • C08F20/52Amides or imides
    • C08F20/54Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F20/00Homopolymers and copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide or nitrile thereof
    • C08F20/02Monocarboxylic acids having less than ten carbon atoms, Derivatives thereof
    • C08F20/52Amides or imides
    • C08F20/54Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide
    • C08F20/58Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide containing oxygen in addition to the carbonamido oxygen, e.g. N-methylolacrylamide, N-acryloylmorpholine
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F20/00Homopolymers and copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide or nitrile thereof
    • C08F20/02Monocarboxylic acids having less than ten carbon atoms, Derivatives thereof
    • C08F20/52Amides or imides
    • C08F20/54Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide
    • C08F20/60Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide containing nitrogen in addition to the carbonamido nitrogen

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Polymers & Plastics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020187022731A 2016-01-07 2017-01-06 Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제 Withdrawn KR20180105161A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662276221P 2016-01-07 2016-01-07
US62/276,221 2016-01-07
US201662399730P 2016-09-26 2016-09-26
US62/399,730 2016-09-26
PCT/US2017/012466 WO2017120429A1 (en) 2016-01-07 2017-01-06 Selective inhibitors of clinically important mutants of the egfr tyrosine kinase

Publications (1)

Publication Number Publication Date
KR20180105161A true KR20180105161A (ko) 2018-09-27

Family

ID=59274526

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187022731A Withdrawn KR20180105161A (ko) 2016-01-07 2017-01-06 Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제

Country Status (7)

Country Link
US (1) US10435388B2 (enExample)
EP (1) EP3399968B8 (enExample)
JP (2) JP2019501222A (enExample)
KR (1) KR20180105161A (enExample)
CN (1) CN109328059B (enExample)
TW (1) TWI726968B (enExample)
WO (1) WO2017120429A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220088407A (ko) * 2019-07-26 2022-06-27 메드샤인 디스커버리 아이엔씨. Egfr 및 erbb2에 작용하는 피리미딘계 화합물

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106117185B (zh) * 2015-08-31 2017-11-07 广州必贝特医药技术有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用
WO2017120429A1 (en) 2016-01-07 2017-07-13 CS Pharmasciences, Inc. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
KR20220130249A (ko) 2016-05-26 2022-09-26 리커리엄 아이피 홀딩스, 엘엘씨 Egfr 억제제 화합물
WO2018019204A1 (zh) * 2016-07-26 2018-02-01 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
CN109923114B (zh) 2016-09-09 2022-11-01 因赛特公司 作为hpk1调节剂的吡唑并吡啶衍生物和其用于治疗癌症的用途
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
AU2018286221B2 (en) * 2017-06-13 2021-02-25 Beijing Adamadle Biotechnology Limited Liability Company Aminopyrimidine compound, preparation method therefor and use thereof
CA3068854A1 (en) * 2017-07-05 2019-01-10 Cs Pharmatech Limited Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
SG11201913556SA (en) * 2017-07-28 2020-02-27 Yuhan Corp Intermediates useful for the synthesis of a selective inhibitor against protein kinase and processes for preparing the same
WO2019023621A1 (en) 2017-07-28 2019-01-31 Yale University ANTICANCER DRUGS AND METHODS OF MAKING AND USING THEM
US11267810B2 (en) * 2017-08-30 2022-03-08 Shenzhen Targetrx, Inc. Aminopyrimidine compound and composition comprising same and use thereof
CN109503573A (zh) * 2017-09-14 2019-03-22 昆明圣加南生物科技有限公司 2-取代苯胺基嘧啶衍生物及其用途
CN107827875B (zh) * 2017-09-25 2021-07-09 文韬创新药物研究(北京)有限责任公司 一种苯并咪唑类衍生物作为周期蛋白依赖性激酶4/6抑制剂的应用
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
CA3087800A1 (en) * 2018-02-20 2019-08-29 Dana-Farber Cancer Institute, Inc. Pharmaceutical combinations of egfr inhibitors and methods of use thereof
AU2019223955B2 (en) 2018-02-20 2024-06-13 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as HPK1 inhibitors for treating cancer
US20210085688A1 (en) * 2018-02-20 2021-03-25 Dana-Farber Cancer Institute, Inc. Pharmaceutical combinations of egfr inhibitors and methods of use thereof
JP7478142B2 (ja) 2018-06-07 2024-05-02 ディスアーム セラピューティクス, インコーポレイテッド Sarm1阻害剤
US20210292333A1 (en) 2018-06-15 2021-09-23 Cadila Healthcare Limited Condensed azaheteroaryl compounds having antibacterial activity against tuberculosis bacteria
CN110790749B (zh) * 2018-08-03 2023-07-14 北京普祺医药科技股份有限公司 一种含氮杂环化合物、药物组合物以及其用途
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
CN110857292A (zh) * 2018-08-22 2020-03-03 上海艾力斯医药科技有限公司 一种egfr激酶抑制剂及其制备方法和应用
US12083114B2 (en) 2018-12-19 2024-09-10 Disarm Therapeutics, Inc. Inhibitors of SARM1 in combination with neuro-protective agents
CN111410651B (zh) * 2019-01-05 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂的盐及其晶型
CN113227073B (zh) * 2019-01-05 2022-09-16 山东轩竹医药科技有限公司 Egfr酪氨酸激酶的选择性抑制剂的盐及其晶型
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
EP3943491B1 (en) * 2019-03-19 2025-06-18 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
CN111825658B (zh) * 2019-04-18 2024-11-08 华东理工大学 Egfr三突变抑制剂及其应用
CN112174961A (zh) * 2019-07-04 2021-01-05 微境生物医药科技(上海)有限公司 一类抑制egfr激酶的化合物及其制备方法和用途
WO2021026180A1 (en) 2019-08-06 2021-02-11 Incyte Corporation Solid forms of an hpk1 inhibitor
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
CN113045475A (zh) * 2019-12-27 2021-06-29 上海泓博智源医药股份有限公司 一种5-溴-7-甲基吲哚的制备方法
CN113493419A (zh) * 2020-03-18 2021-10-12 南京药石科技股份有限公司 Egfr酪氨酸激酶抑制剂及其用途
WO2021243596A1 (en) * 2020-06-03 2021-12-09 InventisBio Co., Ltd. Aminopyrimidine compounds, preparation methods and uses thereof
TW202214600A (zh) * 2020-09-24 2022-04-16 大陸商廣州費米子科技有限責任公司 嘧啶基衍生物、其製備方法及其用途
CA3195035A1 (en) * 2020-10-12 2022-04-21 Dana Farber Cancer Institute, Inc. Covalent egfr inhibitors and methods of use thereof
CN116507627A (zh) * 2020-11-02 2023-07-28 勃林格殷格翰国际有限公司 作为egfr抑制剂的经取代1h-吡唑并[4,3-c]吡啶及衍生物
CN114539269B (zh) * 2020-11-19 2023-04-28 上海医药工业研究院有限公司 一种含氮大环化合物、其制备方法及其应用
US20240002378A1 (en) * 2020-11-30 2024-01-04 H. Lee Moffitt Cancer Center And Research Institute, Inc. Merged scaffold taf1 inhibitors
JP7628729B2 (ja) * 2020-12-02 2025-02-12 上海和誉生物医薬科技有限公司 2,3-ジヒドロ-1H-ピロロ[3,2-b]ピリジン誘導体、その製造方法および使用
CA3223412A1 (en) * 2021-06-23 2022-12-29 Erika BUTLER Process for preparing egfr inhibitors
IL309469A (en) * 2021-06-23 2024-02-01 Blueprint Medicines Corp Salt and crystal forms of epidermal growth factor receptor inhibitor
CN115701429B (zh) * 2021-08-02 2024-03-12 上海和誉生物医药科技有限公司 4-(1h-吲哚-1-基)嘧啶-2-氨基衍生物及其制备方法和应用
MX2024000261A (es) * 2021-08-06 2024-03-14 Abbisko Therapeutics Co Ltd Derivado de pirimidina o piridina, metodo de preparacion del mismo y aplicacion del mismo en la industria farmaceutica.
CN115703760B (zh) * 2021-08-11 2024-05-31 山东大学 2,4-二取代嘧啶类细胞周期蛋白依赖性激酶酶抑制剂及其制备方法和应用
CN116283914A (zh) * 2021-12-01 2023-06-23 上海艾力斯医药科技股份有限公司 一类嘧啶类化合物、其制备方法及应用

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035296A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Improved release of medicament active agents from a chewing gum coating
AU725548B2 (en) 1997-03-11 2000-10-12 E.I. Du Pont De Nemours And Company Heteroaryl azole herbicides
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
US7582631B2 (en) * 2004-01-14 2009-09-01 Amgen Inc. Substituted heterocyclic compounds and methods of use
EP2327693B9 (en) 2007-12-14 2012-10-24 Pulmagen Therapeutics (Asthma) Limited Indoles and their therapeutic use
NZ589843A (en) 2008-06-27 2012-12-21 Avila Therapeutics Inc Pyrimidine heteroaryl compounds and uses thereof as protein kinase inhibitors
WO2010142934A1 (en) 2009-06-12 2010-12-16 Pulmagen Therapeutics (Asthma) Limited Indole derivatives as ligands of crth2 receptors
CN105175396B (zh) 2011-07-27 2018-01-16 阿斯利康(瑞典)有限公司 取代的4‑甲氧基‑n3‑(嘧啶‑2‑基)苯‑1,3‑二胺化合物及其盐
EP2763976B1 (en) * 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
EP2870150B1 (en) 2012-07-03 2019-06-19 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
CN104513253A (zh) * 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
CN104761544B (zh) 2014-01-03 2019-03-15 北京轩义医药科技有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
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
JP6468611B2 (ja) 2014-05-13 2019-02-13 アリアド ファーマシューティカルズ, インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物
CN106660993B (zh) * 2014-06-12 2020-09-11 上海复尚慧创医药研究有限公司 一类激酶抑制剂
GEP20207111B (en) * 2014-06-19 2020-05-25 Ariad Pharma Inc Heteroaryl compounds for kinase inhibition
CN105315259B (zh) 2014-07-29 2018-03-09 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物、其制备方法及应用
CN106458969A (zh) 2014-08-25 2017-02-22 四川海思科制药有限公司 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途
CN105461695B (zh) 2014-09-29 2018-03-27 齐鲁制药有限公司 嘧啶或三嗪衍生物及其制备方法和用途
CN111171000B (zh) * 2014-10-11 2023-09-01 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
KR102073854B1 (ko) 2014-10-13 2020-02-05 주식회사유한양행 Egfr 돌연변이 키나아제 활성을 조절하기 위한 화합물 및 조성물
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
WO2016105525A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
RU2677706C1 (ru) 2014-12-23 2019-01-21 Мицубиси Хайтек Пэйпер Юроп Гмбх Теплочувствительный записывающий материал для офсетной печати
CN104788427B (zh) 2015-02-05 2017-05-31 上海泓博智源医药股份有限公司 3‑(2‑嘧啶氨基)苯基丙烯酰胺类化合物及其应用
CN104844580B (zh) 2015-04-17 2017-10-20 中国药科大学 嘧啶类化合物、其制备方法及医药用途
CN107973791B (zh) 2015-04-29 2020-04-07 南京圣和药业股份有限公司 稠环或三环芳基嘧啶化合物用作激酶抑制剂
HK1251567A1 (zh) 2015-05-13 2019-02-01 Ariad Pharmaceuticals, Inc. 用於激酶抑制的杂芳基化合物
CA2992317A1 (en) 2015-07-16 2017-01-19 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Aniline pyrimidine derivatives and uses thereof
CN105001208A (zh) 2015-08-06 2015-10-28 南京雷科星生物技术有限公司 一种表皮生长因子受体egfr抑制剂及其制备方法与用途
CN106117185B (zh) 2015-08-31 2017-11-07 广州必贝特医药技术有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用
CN106749193B (zh) * 2015-11-23 2020-11-20 南京圣和药业股份有限公司 吲唑取代的表皮生长因子受体抑制剂及其应用
CN106928150B (zh) 2015-12-31 2020-07-31 恩瑞生物医药科技(上海)有限公司 丙烯酰胺苯胺衍生物及其药学上的应用
WO2017120429A1 (en) 2016-01-07 2017-07-13 CS Pharmasciences, Inc. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
CN106279160B (zh) 2016-03-18 2017-09-26 海南越康生物医药有限公司 N‑苯基‑2‑氨基嘧啶类化合物制备方法和用途
WO2017190637A1 (zh) 2016-05-06 2017-11-09 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的稠合嘧啶类化合物
EP3454860B1 (en) 2016-05-11 2025-09-17 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
WO2018019204A1 (zh) 2016-07-26 2018-02-01 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
CA3068854A1 (en) 2017-07-05 2019-01-10 Cs Pharmatech Limited Selective inhibitors of clinically important mutants of the egfr tyrosine kinase

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220088407A (ko) * 2019-07-26 2022-06-27 메드샤인 디스커버리 아이엔씨. Egfr 및 erbb2에 작용하는 피리미딘계 화합물

Also Published As

Publication number Publication date
TWI726968B (zh) 2021-05-11
US10435388B2 (en) 2019-10-08
TW201734013A (zh) 2017-10-01
CN109328059A (zh) 2019-02-12
EP3399968B8 (en) 2021-12-01
CN109328059B (zh) 2021-08-17
JP2019501222A (ja) 2019-01-17
JP2021091703A (ja) 2021-06-17
US20190023689A1 (en) 2019-01-24
EP3399968A4 (en) 2019-07-24
EP3399968A1 (en) 2018-11-14
WO2017120429A1 (en) 2017-07-13
EP3399968B1 (en) 2021-10-20

Similar Documents

Publication Publication Date Title
TWI726968B (zh) Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑
KR20200028966A (ko) Efgr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제
JP5832524B2 (ja) ピリドン及びアザピリドン化合物、並びにそれらの使用方法
TWI733679B (zh) Hpk1抑制劑及其使用方法
CN101360499B (zh) 吡唑并[1,5-a]嘧啶衍生物在制备抑制蛋白激酶的药物中的用途
CN108699057B (zh) 5-取代的2-(吗啉-4-基)-1,7-萘啶
JP2022084663A (ja) Tam阻害剤としてのピロロトリアジン化合物
CN109923114A (zh) 作为hpk1调节剂的吡唑并吡啶衍生物和其用于治疗癌症的用途
CN104761544A (zh) Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
CN115667255A (zh) 卤代杂芳基和其他杂环激酶抑制剂及其用途
TW200938202A (en) Heterocyclic compounds
TW201213324A (en) Fused heterocyclic compounds
TW202400601A (zh) 作為parp抑製劑的取代的三環類化合物及其用途
CN112574255A (zh) 一类基于有机胂的cdk抑制剂及其制备方法和用途
TWI818424B (zh) 含氮多環稠環類化合物,其藥物組合物、製備方法和用途
KR20190100337A (ko) 피라졸로피리미딘 화합물 및 이의 사용 방법
CN115698004A (zh) 作为hpk1抑制剂的氮杂内酰胺化合物
WO2020182188A1 (zh) 取代的杂芳基化合物及其组合物和用途
HK40004229A (en) Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
HK40004229B (zh) Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
TW202005967A (zh) Egfr酪胺酸激酶之臨床上重要的突變體之選擇性抑制劑
HK40017966A (en) Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
CN103748095B (zh) 二环杂芳族化合物
HK40057478B (zh) Hpk1抑制剂及其使用方法
CN121001994A (zh) Atm激酶抑制剂

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20180807

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20220105

Comment text: Request for Examination of Application

PC1202 Submission of document of withdrawal before decision of registration

Comment text: [Withdrawal of Procedure relating to Patent, etc.] Withdrawal (Abandonment)

Patent event code: PC12021R01D

Patent event date: 20220316

WITB Written withdrawal of application