CN108024993B - 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂 - Google Patents

取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂 Download PDF

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CN108024993B
CN108024993B CN201580067776.8A CN201580067776A CN108024993B CN 108024993 B CN108024993 B CN 108024993B CN 201580067776 A CN201580067776 A CN 201580067776A CN 108024993 B CN108024993 B CN 108024993B
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pharmaceutically acceptable
mmol
acceptable salt
methyl
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CN108024993A (zh
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J·彭
M·J·科斯坦佐
M·N·格雷科
M·A·格林
V·L·怀尔德
D·张
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Beta Pharma Shanghai Co ltd
Beta Pharma Inc
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Beta Pharma Inc
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    • 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
    • C07D403/02—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
    • 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
    • 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
    • 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
    • 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
    • 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

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  • 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)
CN201580067776.8A 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂 Active CN108024993B (zh)

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CN202011112986.3A CN112457298B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂
CN202011112988.2A CN112375067B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂

Applications Claiming Priority (5)

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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

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CN202011112988.2A Division CN112375067B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂
CN202011112986.3A Division CN112457298B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂

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CN108024993B true CN108024993B (zh) 2020-11-06

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CN202011112986.3A Active CN112457298B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂
CN202011112988.2A Active CN112375067B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂

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CN202011112988.2A Active CN112375067B (zh) 2014-12-11 2015-12-11 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂

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EP (1) EP3229798A4 (enExample)
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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)
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IL (1) IL252554A0 (enExample)
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PH (1) PH12017501057A1 (enExample)
SG (2) SG10201909060SA (enExample)
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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.
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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
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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
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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
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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
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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
KR20170098865A (ko) 2017-08-30
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
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

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