TW202317106A - 作為egfr抑制劑之取代胺基吡啶化合物 - Google Patents

作為egfr抑制劑之取代胺基吡啶化合物 Download PDF

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Publication number
TW202317106A
TW202317106A TW111131849A TW111131849A TW202317106A TW 202317106 A TW202317106 A TW 202317106A TW 111131849 A TW111131849 A TW 111131849A TW 111131849 A TW111131849 A TW 111131849A TW 202317106 A TW202317106 A TW 202317106A
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Taiwan
Prior art keywords
pyrazol
amino
pyrimidin
pyridin
ethynyl
Prior art date
Application number
TW111131849A
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English (en)
Chinese (zh)
Inventor
李秉文
李炫周
李圭珍
崔秀份
朴率
金熙俊
金渼松
尹永愛
玄官勳
金泰均
沈載永
瑪麗安 布萊恩
斯科特 庫杜克
詹姆斯 坎貝爾 羅伯遜
Original Assignee
南韓商柳韓洋行
美商健生生物科技公司
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Application filed by 南韓商柳韓洋行, 美商健生生物科技公司 filed Critical 南韓商柳韓洋行
Publication of TW202317106A publication Critical patent/TW202317106A/zh

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    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
TW111131849A 2021-08-27 2022-08-24 作為egfr抑制劑之取代胺基吡啶化合物 TW202317106A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202163237647P 2021-08-27 2021-08-27
US63/237,647 2021-08-27

Publications (1)

Publication Number Publication Date
TW202317106A true TW202317106A (zh) 2023-05-01

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TW111131849A TW202317106A (zh) 2021-08-27 2022-08-24 作為egfr抑制劑之取代胺基吡啶化合物

Country Status (8)

Country Link
US (1) US11981658B2 (enExample)
EP (1) EP4392415A4 (enExample)
JP (1) JP7894442B2 (enExample)
KR (1) KR20240052797A (enExample)
CN (1) CN117980297A (enExample)
AR (1) AR126892A1 (enExample)
TW (1) TW202317106A (enExample)
WO (1) WO2023027518A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024188338A1 (zh) * 2023-03-16 2024-09-19 微境生物医药科技(上海)有限公司 Kif18a抑制剂
TW202513556A (zh) * 2023-06-09 2025-04-01 南韓商柳韓洋行 嘧啶/吡啶衍生物或其鹽及以此為成分之藥物組成物
CN118955498A (zh) * 2024-07-25 2024-11-15 浙江大学 一种靶向Tau蛋白的新型PET显像剂及其制备方法

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JP4316893B2 (ja) 2001-05-16 2009-08-19 バーテックス ファーマシューティカルズ インコーポレイテッド Ｓｒｃおよび他のプロテインキナーゼのインヒビター
EP1590341B1 (en) * 2003-01-17 2009-06-17 Warner-Lambert Company LLC 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
US7642354B2 (en) 2004-04-13 2010-01-05 Icagen, Inc. Polycyclic pyrazines as potassium ion channel modulators
EP1737852A2 (en) 2004-04-13 2007-01-03 Icagen, Inc. Polycyclic pyridines as potassium ion channel modulators
JP2007532669A (ja) 2004-04-13 2007-11-15 イカジェン インコーポレイテッド カリウムイオンチャネル調節剤としての多環式ピリミジン
WO2006106721A1 (ja) 2005-03-30 2006-10-12 Shionogi & Co., Ltd. チロシンキナーゼ阻害作用を有するピリミジン誘導体
GB0719644D0 (en) 2007-10-05 2007-11-14 Cancer Rec Tech Ltd Therapeutic compounds and their use
US7989465B2 (en) * 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
JP5600063B2 (ja) * 2007-10-19 2014-10-01 セルジーン アビロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
WO2013192125A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
EP3181564B1 (en) 2012-11-20 2019-09-18 H. Hoffnabb-La Roche Ag Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
RU2015147601A (ru) 2013-05-01 2017-06-05 Ф. Хоффманн-Ля Рош Аг С-связанные гетероциклоалкилзамещенные пиримидины и их применения
CN104761544B (zh) * 2014-01-03 2019-03-15 北京轩义医药科技有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
US20170166598A1 (en) 2014-05-13 2017-06-15 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CA2949793C (en) * 2014-06-19 2024-02-27 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN106588885B (zh) 2016-11-10 2019-03-19 浙江大学 2-取代芳环-嘧啶类衍生物及制备和应用
WO2019126731A1 (en) * 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
WO2019222538A1 (en) 2018-05-16 2019-11-21 The University Of North Carolina At Chapel Hill Aminopyrimidines and aminopyridines as mertk inhibitors and their application in cancer treatment
KR102297587B1 (ko) * 2018-08-07 2021-09-06 재단법인 대구경북첨단의료산업진흥재단 치환된 n-헤테로아릴 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물
US20220177459A1 (en) 2019-04-02 2022-06-09 Hinova Pharmaceuticals Inc. Aromatic amine compound and use thereof in preparation of ar and brd4 dual inhibitors and regulators
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
HRP20241633T1 (hr) * 2019-06-28 2025-02-14 Chengdu Zenitar Biomedical Technology Co., Ltd. 2,4-disupstituirani derivat pirimidina, postupak njegove pripreme i njegova uporaba
JP2023502969A (ja) 2019-11-15 2023-01-26 ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル ＭｅｒＴＫおよびＴＹＲＯ３の二重阻害剤としてのアリールアミノピリミジンおよびその方法

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KR20240052797A (ko) 2024-04-23
EP4392415A1 (en) 2024-07-03
JP7894442B2 (ja) 2026-07-23
JP2024534169A (ja) 2024-09-18
US11981658B2 (en) 2024-05-14
WO2023027518A1 (en) 2023-03-02
CN117980297A (zh) 2024-05-03
EP4392415A4 (en) 2025-10-01
AR126892A1 (es) 2023-11-29
US20230086884A1 (en) 2023-03-23

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