KR20170098865A - Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체 - Google Patents

Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체 Download PDF

Info

Publication number
KR20170098865A
KR20170098865A KR1020177019147A KR20177019147A KR20170098865A KR 20170098865 A KR20170098865 A KR 20170098865A KR 1020177019147 A KR1020177019147 A KR 1020177019147A KR 20177019147 A KR20177019147 A KR 20177019147A KR 20170098865 A KR20170098865 A KR 20170098865A
Authority
KR
South Korea
Prior art keywords
pharmaceutically acceptable
prodrug
solvate
acceptable salt
cancer
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.)
Ceased
Application number
KR1020177019147A
Other languages
English (en)
Korean (ko)
Inventor
지롱 펭
마이클 존 코스탄조
마이클 니콜라스 그레코
마이클 앨런 그린
빅토리아 린 와일드
돈 장
Original Assignee
베타 파마, 인크.
베타 파마 (상하이) 코., 엘티디.
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 베타 파마, 인크., 베타 파마 (상하이) 코., 엘티디. filed Critical 베타 파마, 인크.
Publication of KR20170098865A publication Critical patent/KR20170098865A/ko
Ceased legal-status Critical Current

Links

Images

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
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020177019147A 2014-12-11 2015-12-11 Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체 Ceased KR20170098865A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462090869P 2014-12-11 2014-12-11
US62/090,869 2014-12-11
US201562166883P 2015-05-27 2015-05-27
US62/166,883 2015-05-27
PCT/US2015/065286 WO2016094821A2 (en) 2014-12-11 2015-12-11 Substituted 2-anilinopyrimidine derivatives as egfr modulators

Publications (1)

Publication Number Publication Date
KR20170098865A true KR20170098865A (ko) 2017-08-30

Family

ID=56108380

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177019147A Ceased KR20170098865A (ko) 2014-12-11 2015-12-11 Egfr 조정제로서의 치환된 2-아닐리노피리미딘 유도체

Country Status (17)

Country Link
US (2) US10590111B2 (enExample)
EP (1) EP3229798A4 (enExample)
JP (2) JP6709786B2 (enExample)
KR (1) KR20170098865A (enExample)
CN (3) CN108024993B (enExample)
AU (1) AU2015360360B2 (enExample)
BR (1) BR112017012272A2 (enExample)
CA (1) CA2970185C (enExample)
CO (1) CO2017006962A2 (enExample)
EA (1) EA036453B1 (enExample)
HK (1) HK1245634A1 (enExample)
IL (1) IL252554A0 (enExample)
MX (1) MX382869B (enExample)
PH (1) PH12017501057A1 (enExample)
SG (2) SG10201909060SA (enExample)
TW (1) TWI618704B (enExample)
WO (1) WO2016094821A2 (enExample)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP6709786B2 (ja) * 2014-12-11 2020-06-17 ベータ ファーマ,インコーポレイテッド Egfrモジュレーターとしての置換2−アミノピリミジン誘導体
CN119970741A (zh) 2016-05-11 2025-05-13 贝达医药公司 作为用于治疗脑癌之治疗剂的2-苯胺基嘧啶衍生物
MX383920B (es) 2016-05-26 2025-03-14 Recurium Ip Holdings Llc Compuestos inhibidores de egfr.
EP3471730B1 (en) * 2016-06-17 2021-10-20 Beta Pharma, Inc. Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof
CN106243044A (zh) * 2016-06-30 2016-12-21 浙江大学 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用
EP3492462B1 (en) 2016-07-26 2023-08-30 Shenzhen TargetRx, Inc. Amino pyrimidine compound for inhibiting protein tyrosine kinase activity
TW201904577A (zh) * 2017-06-16 2019-02-01 美商貝達醫藥公司 N-(2-(2-二甲胺基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)胺基)苯基)丙烯醯胺及其鹽之醫藥調配物
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
CN107935995A (zh) * 2017-11-28 2018-04-20 中山大学 一种新型2‑苯胺基嘧啶衍生物及其在制备抗肿瘤药物中的应用
CN108017633A (zh) * 2018-01-30 2018-05-11 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用
MX2020013808A (es) * 2018-06-18 2021-05-27 UCB Biopharma SRL Antagonista de gremlina-1 para la prevencion y el tratamiento del cancer.
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
CN114430681A (zh) * 2019-09-23 2022-05-03 贝达医药公司 使用egfr和cdk4/6抑制剂的组合治疗egfr突变相关的癌症
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
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
AU2022312430A1 (en) * 2021-07-13 2024-02-29 ACEA Therapeutics, Inc. Heterocyclic compounds and uses thereof
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
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
WO2023209084A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
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
WO2025238661A1 (en) * 2024-05-17 2025-11-20 Bdr Lifesciences Private Limited An improved process for the preparation of osimertinib

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001047922A2 (en) * 1999-12-24 2001-07-05 Aventis Pharma Limited Azaindoles
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
EP2102194A1 (en) * 2006-12-08 2009-09-23 F. Hoffmann-Roche AG Substituted pyrimidines and their use as jnk modulators
US8349898B2 (en) * 2008-11-18 2013-01-08 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
US9908884B2 (en) * 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
EP2704572B1 (en) * 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
EP4119551A1 (en) * 2011-07-27 2023-01-18 Astrazeneca AB 2-(2,4,5-substituted-anilino)pyrimidine compounds
WO2013169401A1 (en) * 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
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
EP3778584A1 (en) * 2014-06-19 2021-02-17 ARIAD Pharmaceuticals, Inc. Production process of 2-chloro-4-heteroaryl-pyrimidine derivatives
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
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
JP6709786B2 (ja) * 2014-12-11 2020-06-17 ベータ ファーマ,インコーポレイテッド Egfrモジュレーターとしての置換2−アミノピリミジン誘導体

Also Published As

Publication number Publication date
BR112017012272A2 (pt) 2018-01-30
CN112375067B (zh) 2024-03-15
PH12017501057A1 (en) 2018-03-05
MX2017007664A (es) 2018-01-23
EA036453B1 (ru) 2020-11-12
WO2016094821A3 (en) 2016-08-25
CN112457298B (zh) 2024-05-07
US20170362203A1 (en) 2017-12-21
WO2016094821A2 (en) 2016-06-16
US10590111B2 (en) 2020-03-17
MX382869B (es) 2025-03-13
EP3229798A2 (en) 2017-10-18
AU2015360360B2 (en) 2020-06-25
CO2017006962A2 (es) 2017-10-20
AU2015360360A1 (en) 2017-06-08
CN108024993A (zh) 2018-05-11
CN112457298A (zh) 2021-03-09
HK1245634A1 (zh) 2018-08-31
CN108024993B (zh) 2020-11-06
US20200216421A1 (en) 2020-07-09
JP2020143131A (ja) 2020-09-10
US11414401B2 (en) 2022-08-16
CA2970185A1 (en) 2016-06-16
EP3229798A4 (en) 2018-05-30
IL252554A0 (en) 2017-07-31
CA2970185C (en) 2023-10-17
JP6709786B2 (ja) 2020-06-17
CN112375067A (zh) 2021-02-19
JP7181558B2 (ja) 2022-12-01
JP2017537114A (ja) 2017-12-14
TWI618704B (zh) 2018-03-21
SG10201909060SA (en) 2019-11-28
EA201790921A1 (ru) 2017-12-29
SG11201704685TA (en) 2017-07-28
TW201632512A (zh) 2016-09-16

Similar Documents

Publication Publication Date Title
JP7181558B2 (ja) Egfrモジュレーターとしての置換2-アミノピリミジン誘導体
JP6431593B6 (ja) ピリジニルアミノピリミジン誘導体、その製造方法、および用途
CN105315285B (zh) 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
CN107835811B (zh) 苯胺嘧啶衍生物及其用途
TW201940166A (zh) 作為cdk4及cdk6抑制劑之2h-吲唑衍生物及其治療用途
CN105377835A (zh) 酪氨酸蛋白激酶调节剂及其应用方法
JP2020189852A (ja) キナーゼ阻害活性を有するベンズヒドロール−ピラゾール誘導体及びその使用
TW201934546A (zh) 嘧啶類化合物、其製備方法及其醫藥用途
CN108503627A (zh) 用作egfr抑制剂的2,4-二取代苯-1,5-二胺衍生物及其应用
JP2025081599A (ja) Egfrキナーゼを阻害する化合物、調製方法、及びその使用
CN111542322A (zh) 突变型egfr家族酪氨酸激酶的抑制剂
WO2017211216A1 (zh) 稠合嘧啶哌啶环衍生物及其制备方法和应用
OA18657A (en) Substituted 2-anilinopyrimidine derivatives as EGFR modulators.
HK40081466A (en) Efgr inhibitor, preparation method therefor, and application thereof
WO2023134582A1 (zh) 一种嘧啶-2,4-二胺衍生物及其制备方法和用途
HK1221953A1 (zh) 酪氨酸蛋白激酶调节剂及其应用方法
KR20160030296A (ko) 단백질 티로신 키나제 조절자 및 사용 방법

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20170711

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: 20201208

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20221228

Patent event code: PE09021S01D

E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20230306

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20221228

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I