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

Info

Publication number
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
Authority
CN
China
Prior art keywords
compound
pharmaceutically acceptable
mmol
acceptable salt
methyl
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.)
Active
Application number
CN201580067776.8A
Other languages
English (en)
Chinese (zh)
Other versions
CN108024993A (zh
Inventor
J·彭
M·J·科斯坦佐
M·N·格雷科
M·A·格林
V·L·怀尔德
D·张
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.)
Beta Pharma Shanghai Co ltd
Beta Pharma Inc
Original Assignee
Beta Pharma Shanghai Co ltd
Beta Pharma 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 Beta Pharma Shanghai Co ltd, Beta Pharma Inc filed Critical Beta Pharma Shanghai Co ltd
Priority to CN202011112988.2A priority Critical patent/CN112375067B/zh
Priority to CN202011112986.3A priority patent/CN112457298B/zh
Publication of CN108024993A publication Critical patent/CN108024993A/zh
Application granted granted Critical
Publication of CN108024993B publication Critical patent/CN108024993B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth 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)

Priority Applications (2)

Application Number Priority Date Filing Date Title
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
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

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

Related Child Applications (2)

Application Number Title Priority Date Filing Date
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

Publications (2)

Publication Number Publication Date
CN108024993A CN108024993A (zh) 2018-05-11
CN108024993B true CN108024993B (zh) 2020-11-06

Family

ID=56108380

Family Applications (3)

Application Number Title Priority Date Filing Date
CN201580067776.8A Active CN108024993B (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 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

Family Applications After (2)

Application Number Title Priority Date Filing Date
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

Country Status (17)

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

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN108024993B (zh) * 2014-12-11 2020-11-06 贝达医药公司 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
EP3454860B1 (en) * 2016-05-11 2025-09-17 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
AU2017269335B2 (en) 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
BR112018075823A2 (pt) * 2016-06-17 2019-03-26 Beta Pharma, Inc. sais farmacêuticos de n-(2-(2-(dimetilamino)etoxi)-4-metoxi-5-((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilamida e suas formas cristalinas
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
JP6740452B2 (ja) * 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物
CN110799191B (zh) 2017-06-16 2023-05-26 贝塔制药有限公司 N-(2-(2-(二甲氨基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)氨基)苯基)丙烯酰胺及其盐的药物制剂
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
PL3806898T3 (pl) * 2018-06-18 2026-02-23 UCB Biopharma SRL Antagonista gremlin-1 do zastosowania w leczeniu nowotworu
CA3112043A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
JP2022549272A (ja) * 2019-09-23 2022-11-24 ベータ・ファーマ・インコーポレイテッド Ｅｇｆｒ阻害剤とｃｄｋ４／６阻害剤の組み合わせを用いたｅｇｆｒ変異に関連する癌の治療
US20210161897A1 (en) 2019-11-12 2021-06-03 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
JP2023510426A (ja) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
WO2023287783A1 (en) * 2021-07-13 2023-01-19 ACEA Therapeutics, Inc. Heterocyclic compounds and uses thereof
IL315848A (en) 2022-03-31 2024-11-01 Astrazeneca Ab Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in combination with an AKT inhibitor for cancer treatment
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
PE20250268A1 (es) 2022-04-28 2025-01-29 Astrazeneca Ab Compuestos heteroaromaticos biciclicos condensados y uso en el tratamiento del cancer
EP4543920A1 (en) 2022-06-27 2025-04-30 Astrazeneca AB Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
CN119654152A (zh) 2022-07-08 2025-03-18 阿斯利康(瑞典)有限公司 与hgf-受体抑制剂组合用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂
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
OA12514A (en) * 1999-12-24 2006-05-29 Aventis Pharma Ltd Azaindoles.
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
CN101547917A (zh) * 2006-12-08 2009-09-30 霍夫曼-拉罗奇有限公司 用作jnk调节剂的取代的嘧啶类化合物及它们的应用
US8349898B2 (en) * 2008-11-18 2013-01-08 Wisconsin Alumni Research Foundation Sigma-1 receptor ligands and methods of use
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
US9834518B2 (en) * 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN103702990B (zh) * 2011-07-27 2015-09-09 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症
US20150166591A1 (en) * 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
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
CN110526912B (zh) 2014-06-19 2023-02-14 武田药品工业株式会社 用于激酶抑制的杂芳基化合物
WO2016029839A1 (zh) 2014-08-25 2016-03-03 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
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
CN108024993B (zh) 2014-12-11 2020-11-06 贝达医药公司 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

Also Published As

Publication number Publication date
CA2970185C (en) 2023-10-17
SG11201704685TA (en) 2017-07-28
JP7181558B2 (ja) 2022-12-01
JP2017537114A (ja) 2017-12-14
CO2017006962A2 (es) 2017-10-20
EP3229798A4 (en) 2018-05-30
CN112457298B (zh) 2024-05-07
SG10201909060SA (en) 2019-11-28
AU2015360360B2 (en) 2020-06-25
CN112375067B (zh) 2024-03-15
HK1245634A1 (zh) 2018-08-31
AU2015360360A1 (en) 2017-06-08
CN108024993A (zh) 2018-05-11
MX2017007664A (es) 2018-01-23
EA036453B1 (ru) 2020-11-12
KR20170098865A (ko) 2017-08-30
MX382869B (es) 2025-03-13
EP3229798A2 (en) 2017-10-18
TWI618704B (zh) 2018-03-21
EA201790921A1 (ru) 2017-12-29
CA2970185A1 (en) 2016-06-16
WO2016094821A2 (en) 2016-06-16
BR112017012272A2 (pt) 2018-01-30
CN112457298A (zh) 2021-03-09
TW201632512A (zh) 2016-09-16
WO2016094821A3 (en) 2016-08-25
US20170362203A1 (en) 2017-12-21
PH12017501057A1 (en) 2018-03-05
IL252554A0 (en) 2017-07-31
JP2020143131A (ja) 2020-09-10
US20200216421A1 (en) 2020-07-09
US10590111B2 (en) 2020-03-17
JP6709786B2 (ja) 2020-06-17
CN112375067A (zh) 2021-02-19
US11414401B2 (en) 2022-08-16

Similar Documents

Publication Publication Date Title
CN108024993B (zh) 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
TWI675028B (zh) 做為週期素依賴型激酶（ｃｄｋ）抑制劑之2-ｈ-吲唑衍生物及其醫療用途
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
JP7337395B2 (ja) Ｃｄｋ４およびｃｄｋ６阻害剤としての２ｈ－インダゾール誘導体およびその治療上の使用
WO2016015453A1 (zh) 吡啶胺基嘧啶衍生物、其制备方法及应用
TW201934546A (zh) 嘧啶類化合物、其製備方法及其醫藥用途
CN103936762B (zh) 吗啉并喹啉类化合物，其制备方法和用途
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
CN102088979B (zh) 4-(3-氯-2-氟苯胺基)-7-甲氧基-6-{[1-(n-甲基氨基甲酰基甲基)哌啶-4-基]氧基}喹唑啉的富马酸盐
EP1954281B1 (en) Cancer treatment method
EP3471730B1 (en) 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
CN112203659A (zh) 作为tyro3、axl和mertk(tam)家族受体酪氨酸激酶抑制剂的杂环化合物
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
HK40116343A (zh) 外核苷酸焦磷酸酶-磷酸二酯酶(enpp1)抑制剂及其用途
CN118772111A (zh) 一种取代的氨基嘧啶类化合物、药物组合物及其用途

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
GR01 Patent grant
GR01 Patent grant