JP2020526499A - Egfrチロシンキナーゼの臨床上重要な突然変異体の選択的阻害剤 - Google Patents

Egfrチロシンキナーゼの臨床上重要な突然変異体の選択的阻害剤 Download PDF

Info

Publication number
JP2020526499A
JP2020526499A JP2019572412A JP2019572412A JP2020526499A JP 2020526499 A JP2020526499 A JP 2020526499A JP 2019572412 A JP2019572412 A JP 2019572412A JP 2019572412 A JP2019572412 A JP 2019572412A JP 2020526499 A JP2020526499 A JP 2020526499A
Authority
JP
Japan
Prior art keywords
alkyl
alkoxy
independently
cyano
halo
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
JP2019572412A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020526499A5 (enExample
Inventor
ユンタオ ソン,
ユンタオ ソン,
アレクサンダー ジェイムズ ブリッジス,
アレクサンダー ジェイムズ ブリッジス,
シャオチー チェン,
シャオチー チェン,
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of JP2020526499A publication Critical patent/JP2020526499A/ja
Publication of JP2020526499A5 publication Critical patent/JP2020526499A5/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • C07D403/10Heterocyclic 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
    • 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)
  • 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)
JP2019572412A 2017-07-05 2018-07-05 Egfrチロシンキナーゼの臨床上重要な突然変異体の選択的阻害剤 Pending JP2020526499A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762528697P 2017-07-05 2017-07-05
US62/528,697 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 (2)

Publication Number Publication Date
JP2020526499A true JP2020526499A (ja) 2020-08-31
JP2020526499A5 JP2020526499A5 (enExample) 2021-07-26

Family

ID=64950363

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019572412A Pending JP2020526499A (ja) 2017-07-05 2018-07-05 Egfrチロシンキナーゼの臨床上重要な突然変異体の選択的阻害剤

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)

Families Citing this family (20)

* 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
WO2019154177A1 (zh) * 2018-02-12 2019-08-15 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
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
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
CN115650974B (zh) * 2022-08-04 2024-06-18 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
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017506667A (ja) * 2014-02-25 2017-03-09 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. 2,4−二置換ベンゼン−1,5−ジアミン誘導体およびその使用ならびにそれから製造される医薬組成物および薬用組成物
JP2019522011A (ja) * 2016-07-26 2019-08-08 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

Family Cites Families (3)

* 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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017506667A (ja) * 2014-02-25 2017-03-09 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. 2,4−二置換ベンゼン−1,5−ジアミン誘導体およびその使用ならびにそれから製造される医薬組成物および薬用組成物
JP2019522011A (ja) * 2016-07-26 2019-08-08 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

Also Published As

Publication number Publication date
WO2019010295A1 (en) 2019-01-10
KR20200028966A (ko) 2020-03-17
EP3648753A4 (en) 2021-03-17
US20200131176A1 (en) 2020-04-30
EP3648753A1 (en) 2020-05-13
CN111093645A (zh) 2020-05-01
CA3068854A1 (en) 2019-01-10

Similar Documents

Publication Publication Date Title
JP2020526499A (ja) Egfrチロシンキナーゼの臨床上重要な突然変異体の選択的阻害剤
US10435388B2 (en) Selective inhibitors of clinically important mutants of the EGFR tyrosine kinase
JP6869947B2 (ja) 置換キナゾリン化合物ならびにそのg12c変異kras、hrasおよび/またはnrasタンパク質の阻害剤としての使用
JP7034084B2 (ja) Tam阻害剤としてのピロロトリアジン化合物
CA2809553C (en) Imidazo[4,5-c]quinolines as dna-pk inhibitors
CN105793260B (zh) 作为用于治疗癌症的raf抑制剂的1‑(5‑叔丁基‑2‑芳基‑吡唑‑3‑基)‑3‑[2‑氟‑4‑[(3‑氧代‑4h‑吡啶并[2,3‑b]吡嗪‑8‑基)氧基]苯基]脲衍生物
JP2022043073A (ja) 二価ブロモドメインインヒビターおよびそれらの使用
CN102574842B (zh) 用于抑制pi3激酶的吡啶基咪唑酮衍生物
IL282737B1 (en) Cyclin-dependent kinase 7 (CDK7) inhibitors
CN101952287B (zh) 蛋白激酶抑制剂及其应用
CN107922431A (zh) Hpk1抑制剂及其使用方法
TWI707855B (zh) 咪唑并嗒類化合物及其用途
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
TW200925160A (en) Fused heterocyclic compound
CN107074778A (zh) 苯并咪唑类似物和相关方法
AU2022226671B2 (en) Aminopyrimidine compounds and methods of their use
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
HK40017966A (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
WO2024228035A1 (en) Ikk-alpha inhibitors
HK40057478B (zh) Hpk1抑制剂及其使用方法
HK40004229A (en) Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
HK40084694A (en) Azalactam compounds as hpk1 inhibitors
CN103748095B (zh) 二环杂芳族化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200114

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210517

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20210517

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20220414

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20220506

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20221128