CN111093645A - Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂 - Google Patents

Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂 Download PDF

Info

Publication number
CN111093645A
CN111093645A CN201880044480.8A CN201880044480A CN111093645A CN 111093645 A CN111093645 A CN 111093645A CN 201880044480 A CN201880044480 A CN 201880044480A CN 111093645 A CN111093645 A CN 111093645A
Authority
CN
China
Prior art keywords
alkyl
alkoxy
independently
cyano
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.)
Pending
Application number
CN201880044480.8A
Other languages
English (en)
Chinese (zh)
Inventor
宋运涛
A.J.布里奇斯
陈晓颀
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.)
CS Pharmatech Ltd
Original Assignee
CS Pharmatech Ltd
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 CS Pharmatech Ltd filed Critical CS Pharmatech Ltd
Publication of CN111093645A publication Critical patent/CN111093645A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201880044480.8A 2017-07-05 2018-07-05 Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂 Pending CN111093645A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762528697P 2017-07-05 2017-07-05
US62/528697 2017-07-05
PCT/US2018/040904 WO2019010295A1 (en) 2017-07-05 2018-07-05 SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF EGFR TYROSINE KINASE

Publications (1)

Publication Number Publication Date
CN111093645A true CN111093645A (zh) 2020-05-01

Family

ID=64950363

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880044480.8A Pending CN111093645A (zh) 2017-07-05 2018-07-05 Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂

Country Status (7)

Country Link
US (1) US20200131176A1 (enExample)
EP (1) EP3648753A4 (enExample)
JP (1) JP2020526499A (enExample)
KR (1) KR20200028966A (enExample)
CN (1) CN111093645A (enExample)
CA (1) CA3068854A1 (enExample)
WO (1) WO2019010295A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111566100A (zh) * 2018-02-12 2020-08-21 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
CN113651800A (zh) * 2021-09-07 2021-11-16 山东铂源药业有限公司 一种甲磺酸奥希替尼的制备方法
CN115650974A (zh) * 2022-08-04 2023-01-31 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-顺式戊二烯酰胺衍生物及应用

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019501222A (ja) 2016-01-07 2019-01-17 シーエス ファーマテック リミテッド Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬
MY199042A (en) * 2017-06-13 2023-10-11 Beijing Adamadle Biotechnology Llc Aminopyrimidine compound, preparation method therefor and use thereof
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
MA55380A (fr) * 2019-03-19 2022-01-26 B2Sbio Inc Dérivé hétéroaryle, son procédé de production et composition pharmaceutique le comprenant en tant que constituant efficace
JP2022526713A (ja) 2019-03-21 2022-05-26 オンクセオ がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子
CN111747931A (zh) * 2019-03-29 2020-10-09 深圳福沃药业有限公司 用于治疗癌症的氮杂芳环酰胺衍生物
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
KR20220079593A (ko) 2019-10-03 2022-06-13 브리스톨-마이어스 스큅 컴퍼니 키나제 억제제로서의 인다졸 카르복스아미드
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
TW202128670A (zh) * 2019-11-26 2021-08-01 大陸商上海翰森生物醫藥科技有限公司 含氮多環類衍生物抑制劑、其製備方法和應用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021243596A1 (en) * 2020-06-03 2021-12-09 InventisBio Co., Ltd. Aminopyrimidine compounds, preparation methods and uses thereof
WO2022131741A1 (ko) * 2020-12-14 2022-06-23 보로노이바이오 주식회사 아이소옥사졸리딘 유도체 화합물 및 이의 용도
KR20240027583A (ko) * 2021-04-30 2024-03-04 수조우 푸허 바이오파마 컴퍼니 리미티드 폐암 치료를 위한 피리미디닐아미노벤젠
CA3180295A1 (en) * 2021-05-17 2022-11-24 Youn Ho Lee Heteroaryl derivative compounds, and uses thereof
WO2024094064A1 (en) * 2022-11-02 2024-05-10 Suzhou Puhe Biopharma Co., Ltd Pyrimidinylaminobenzenes for treating lung cancer with distant metastasis
KR20250097933A (ko) * 2022-11-03 2025-06-30 보로노이 주식회사 Egfr 억제제의 퓨마르산염, 타타르산염, 말산염, 및 시트르산염

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8450335B2 (en) * 2008-06-27 2013-05-28 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
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
US10266517B2 (en) * 2014-12-23 2019-04-23 Dana-Farber Cancer Institute, Inc. Pyrimidines as EGFR inhibitors and methods of treating disorders
JP2019501222A (ja) * 2016-01-07 2019-01-17 シーエス ファーマテック リミテッド Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬
CN108602802B (zh) * 2016-07-26 2020-01-21 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

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111566100A (zh) * 2018-02-12 2020-08-21 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
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
CN113651800A (zh) * 2021-09-07 2021-11-16 山东铂源药业有限公司 一种甲磺酸奥希替尼的制备方法
CN113651800B (zh) * 2021-09-07 2022-08-19 山东铂源药业股份有限公司 一种甲磺酸奥希替尼的制备方法
CN115650974A (zh) * 2022-08-04 2023-01-31 天津大学 N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-顺式戊二烯酰胺衍生物及应用

Also Published As

Publication number Publication date
WO2019010295A1 (en) 2019-01-10
KR20200028966A (ko) 2020-03-17
JP2020526499A (ja) 2020-08-31
EP3648753A4 (en) 2021-03-17
US20200131176A1 (en) 2020-04-30
EP3648753A1 (en) 2020-05-13
CA3068854A1 (en) 2019-01-10

Similar Documents

Publication Publication Date Title
CN111093645A (zh) Egfr酪氨酸激酶的临床上重要的突变体的选择性抑制剂
CN109328059B (zh) Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
CN117736207A (zh) 二酰基甘油激酶调节化合物
CN118286225A (zh) 作为细胞周期蛋白依赖性激酶抑制剂的2-氨基-吡啶或2-氨基-嘧啶衍生物
ES2911040T3 (es) Nuevos derivados de heteroaril amida como inhibidores selectivos de histona deacetilasa 1 y 2 (HDAC1/2)
CN111801320A (zh) 苯甲酰胺化合物
CN104761544A (zh) Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
CN113316576A (zh) 用于治疗癌症的作为HPK1抑制剂的2,3-二氢-1H-吡咯并[3,4-c]吡啶-1-酮衍生物
TW201105326A (en) Diamino heterocyclic carboxamide compound
JP2016501251A (ja) がんの治療のための新規二環フェニル−ピリジン／ピラジン
WO2015158310A1 (zh) 一种酪氨酸激酶抑制剂及其用途
CN104321322A (zh) 作为c-met蛋白激酶调节剂的新型3,5-二取代-3h-咪唑并[4,5-b]吡啶和3,5-二取代-3h-[1,2,3]三唑并[4,5-b]吡啶化合物
WO2018153293A1 (zh) 二噁烷并喹唑啉与二噁烷并喹啉类化合物及其制备方法与应用
CN103539780A (zh) 取代的吡唑酮化合物及其使用方法和用途
CN115698004A (zh) 作为hpk1抑制剂的氮杂内酰胺化合物
CN107531683A (zh) Usp7抑制剂化合物及使用方法
WO2017097216A1 (zh) 五元杂环酰胺类wnt通路抑制剂
CN120712259A (zh) 作为sos1抑制剂的唑基吡啶哒嗪酮酰胺
HK40017966A (en) Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
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
CN107056754B (zh) 内嵌脲类结构的wnt通路抑制剂
RU2819642C1 (ru) Соединения азалактама в качестве ингибиторов hpk1
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
HK40084694A (en) Azalactam compounds as hpk1 inhibitors

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
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40017966

Country of ref document: HK

WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20200501