BR112017006713A2 - inibidor de egfr, e preparação e aplicação do mesmo - Google Patents

inibidor de egfr, e preparação e aplicação do mesmo

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Publication number
BR112017006713A2
BR112017006713A2 BR112017006713A BR112017006713A BR112017006713A2 BR 112017006713 A2 BR112017006713 A2 BR 112017006713A2 BR 112017006713 A BR112017006713 A BR 112017006713A BR 112017006713 A BR112017006713 A BR 112017006713A BR 112017006713 A2 BR112017006713 A2 BR 112017006713A2
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BR
Brazil
Prior art keywords
egfr
mutant
application
preparation
substituted
Prior art date
Application number
BR112017006713A
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English (en)
Other versions
BR112017006713B1 (pt
Inventor
Zhang Fujun
Sun Guangjun
Wei Mingsong
Gao Peng
Bao Rudi
Wang Shaobao
TAN Songliang
Xiu Wenhua
Original Assignee
Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Publication date
Application filed by Jiangsu Hansoh Pharmaceutical Group Co Ltd, Shanghai Hansoh Biomedical Co Ltd filed Critical Jiangsu Hansoh Pharmaceutical Group Co Ltd
Publication of BR112017006713A2 publication Critical patent/BR112017006713A2/pt
Publication of BR112017006713B1 publication Critical patent/BR112017006713B1/pt

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    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
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    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

a presente invenção refere-se a um derivado de 4-substituído-2-(n-(5-substituído alil amida)fenil)amino)piridina, como representado pela fórmula (i), e uma preparação e aplicação do mesmo como um inibidor de egfr. o composto tem atividade de inibição do mutante de egfr l858r, o mutante de egfr t790m e o mutante de ativação de deleção de éxon 19, pode ser usado para tratar doenças mediadas apenas ou em parte por atividade de mutante de egfr, e tem uma ampla aplicação em fármacos para a prevenção e tratamento de cânceres, particularmente câncer de pulmão de célula não pequena.
BR112017006713-7A 2014-10-11 2015-09-30 Inibidores de egfr, seus usos e seu processo de preparação, e composição farmacêutica BR112017006713B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201410534203.9 2014-10-11
CN201410534203 2014-10-11
PCT/CN2015/091189 WO2016054987A1 (zh) 2014-10-11 2015-09-30 Egfr抑制剂及其制备和应用

Publications (2)

Publication Number Publication Date
BR112017006713A2 true BR112017006713A2 (pt) 2017-12-26
BR112017006713B1 BR112017006713B1 (pt) 2023-11-21

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US (2) US10259820B2 (pt)
EP (1) EP3205650B1 (pt)
JP (1) JP6691281B2 (pt)
KR (1) KR102589982B1 (pt)
CN (7) CN117069700A (pt)
AU (1) AU2015330506B2 (pt)
BR (1) BR112017006713B1 (pt)
CA (1) CA2959194A1 (pt)
CY (1) CY1124476T1 (pt)
DK (1) DK3205650T3 (pt)
ES (1) ES2886887T3 (pt)
HR (1) HRP20211392T1 (pt)
HU (1) HUE055233T2 (pt)
LT (1) LT3205650T (pt)
MX (1) MX2017004234A (pt)
PL (1) PL3205650T3 (pt)
PT (1) PT3205650T (pt)
RS (1) RS62350B1 (pt)
RU (1) RU2702631C2 (pt)
SI (1) SI3205650T1 (pt)
TW (1) TWI704138B (pt)
WO (1) WO2016054987A1 (pt)
ZA (1) ZA201701465B (pt)

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CN105384694B (zh) * 2014-08-22 2020-09-04 四川海思科制药有限公司 一种取代的氨基嘧啶衍生物及其制备方法和药物用途
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
CN113563332A (zh) 2014-12-23 2021-10-29 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
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
EP3399968B8 (en) * 2016-01-07 2021-12-01 Xuanzhu Biopharmaceutical Co., Ltd. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
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ES2857805T3 (es) * 2016-03-22 2021-09-29 Jiangsu Hansoh Pharmaceutical Group Co Ltd Forma policristalina de base libre o sal ácida del inhibidor de EGFR, método de preparación y aplicación
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
WO2017202311A1 (zh) * 2016-05-23 2017-11-30 中国科学院上海药物研究所 一种2-氨基嘧啶类化合物的多晶型形式
MX2018013413A (es) * 2016-05-26 2019-06-06 Zeno Royalties & Milestones Llc Compuestos inhibidores de egfr.
CN106083736A (zh) * 2016-06-21 2016-11-09 郑州泰基鸿诺医药股份有限公司 一种嘧啶类化合物、egfr抑制剂及其应用
CN110818690B (zh) * 2016-07-26 2021-08-10 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
CN107793413B (zh) * 2016-09-05 2021-09-28 上海科州药物研发有限公司 嘧啶杂环化合物及其制备方法和应用
KR102245280B1 (ko) * 2016-09-19 2021-04-27 난징 추앙트어 파마슈티컬 테크놀로지 컴퍼니 리미티드 중수소화 3-(4,5-치환 아미노피리미딘) 페닐 유도체 및 그의 응용
CN107973783A (zh) * 2016-10-21 2018-05-01 正大天晴药业集团股份有限公司 作为erk抑制剂的苯胺嘧啶衍生物
CN108057036B (zh) * 2016-11-07 2023-06-13 正大天晴药业集团股份有限公司 一种egfr抑制剂的固体药物组合物
CN108503627A (zh) * 2017-04-19 2018-09-07 郑州泰基鸿诺医药股份有限公司 用作egfr抑制剂的2,4-二取代苯-1,5-二胺衍生物及其应用
CR20190542A (es) * 2017-06-02 2020-01-14 Hoffmann La Roche Compuestos
CA3071345A1 (en) * 2017-07-28 2019-01-31 Yale University Anticancer drugs and methods of making and using same
WO2019042187A1 (zh) * 2017-08-30 2019-03-07 深圳市塔吉瑞生物医药有限公司 一种氨基嘧啶类化合物及包含该化合物的组合物及其用途
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
TWI702205B (zh) * 2017-10-06 2020-08-21 俄羅斯聯邦商拜奧卡德聯合股份公司 表皮生長因子受體抑制劑
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
WO2019177375A1 (ko) * 2018-03-13 2019-09-19 포로노이바이오 주식회사 2, 4, 5-치환된 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물
CN110272420A (zh) * 2018-03-16 2019-09-24 江苏正大丰海制药有限公司 氘代3-(4,5-取代氨基嘧啶)苯基化合物单甲磺酸盐晶型及其制备方法
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