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

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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
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JP2020526499A5 (enExample
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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，
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    • 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
    • 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
    • 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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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

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

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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

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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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024516430A (ja) * 2021-04-30 2024-04-15 スゾウ プヘ バイオファーマ シーオー．， エルティーディー 肺がん治療のためのピリミジニルアミノベンゼン
JP2024519626A (ja) * 2021-05-17 2024-05-21 ボロノイ インコーポレイテッド ヘテロアリール誘導体化合物およびその用途｛Ｈｅｔｅｒｏａｒｙｌ ｄｅｒｉｖａｔｉｖｅ ｃｏｍｐｏｕｎｄｓ，ａｎｄ ｕｓｅｓ ｔｈｅｒｅｏｆ｝

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017120429A1 (en) 2016-01-07 2017-07-13 CS Pharmasciences, Inc. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
ES2963921T3 (es) * 2017-06-13 2024-04-03 Beijing Avlstone Biotechnology Co Ltd Compuestos de aminopirimidina, su método de preparación y uso de los mismos
US20210101881A1 (en) * 2018-02-12 2021-04-08 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Pyrimidine compound, preparation method thereof and medical 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
JP7109013B2 (ja) 2019-03-19 2022-07-29 ボロノイ インコーポレイテッド ヘテロアリール誘導体、ヘテロアリール誘導体の生成方法、およびヘテロアリール誘導体を有効成分として含む医薬組成物
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN111747950B (zh) 2019-03-29 2024-01-23 深圳福沃药业有限公司 用于治疗癌症的嘧啶衍生物
US12523663B2 (en) 2019-06-04 2026-01-13 Inserm (Institut National De La Santé Et De La Rescherche Médicale) Use of CD9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
US12275721B2 (en) 2019-10-03 2025-04-15 Bristol-Myers Squibb Company Indazole carboxamides as kinase inhibitors
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
WO2021104305A1 (zh) * 2019-11-26 2021-06-03 上海翰森生物医药科技有限公司 含氮多环类衍生物抑制剂、其制备方法和应用
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
KR20220085735A (ko) * 2020-12-14 2022-06-22 보로노이바이오 주식회사 아이소옥사졸리딘 유도체 화합물 및 이의 용도
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
CN120035590A (zh) * 2022-11-03 2025-05-23 株式会社沃若诺伊 Egfr抑制剂的延胡索酸盐、酒石酸盐、苹果酸盐和柠檬酸盐

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
AU2009262068C1 (en) * 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
WO2016105525A2 (en) * 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
WO2017120429A1 (en) * 2016-01-07 2017-07-13 CS Pharmasciences, Inc. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase

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

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024516430A (ja) * 2021-04-30 2024-04-15 スゾウ プヘ バイオファーマ シーオー．， エルティーディー 肺がん治療のためのピリミジニルアミノベンゼン
JP2024519626A (ja) * 2021-05-17 2024-05-21 ボロノイ インコーポレイテッド ヘテロアリール誘導体化合物およびその用途｛Ｈｅｔｅｒｏａｒｙｌ ｄｅｒｉｖａｔｉｖｅ ｃｏｍｐｏｕｎｄｓ，ａｎｄ ｕｓｅｓ ｔｈｅｒｅｏｆ｝
JP7896880B2 (ja) 2021-05-17 2026-07-29 ボロノイ インコーポレイテッド ヘテロアリール誘導体化合物およびその用途｛Ｈｅｔｅｒｏａｒｙｌ ｄｅｒｉｖａｔｉｖｅ ｃｏｍｐｏｕｎｄｓ，ａｎｄ ｕｓｅｓ ｔｈｅｒｅｏｆ｝

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

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