JP2024505558A - ブルトン型チロシンキナーゼ（ｂｔｋ）分解剤としての置換ピロロピリミジンおよびピラゾロピリミジン - Google Patents

ブルトン型チロシンキナーゼ（ｂｔｋ）分解剤としての置換ピロロピリミジンおよびピラゾロピリミジン Download PDF

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JP2024505558A
JP2024505558A JP2023546433A JP2023546433A JP2024505558A JP 2024505558 A JP2024505558 A JP 2024505558A JP 2023546433 A JP2023546433 A JP 2023546433A JP 2023546433 A JP2023546433 A JP 2023546433A JP 2024505558 A JP2024505558 A JP 2024505558A
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amino
pyrimidin
piperazin
dioxopiperidin
chloro
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JP2024505558A5 (https=
Inventor
イミン チアン，
ウェイ ヘ，
ロバート ルオ，
ジエ スー，
フイ ジャン，
ケ リウ，
ジエ ファン，
Original Assignee
アキュター バイオテクノロジー インコーポレイテッド
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    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2023546433A 2021-02-03 2022-02-02 ブルトン型チロシンキナーゼ（ｂｔｋ）分解剤としての置換ピロロピリミジンおよびピラゾロピリミジン Pending JP2024505558A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163145126P 2021-02-03 2021-02-03
US63/145,126 2021-02-03
PCT/US2022/014830 WO2022169798A2 (en) 2021-02-03 2022-02-02 Substituted pyrrolopyrimidine and pyrazolopyrimidine as bruton's tyrosine kinase (btk) degraders

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JP2024505558A true JP2024505558A (ja) 2024-02-06
JP2024505558A5 JP2024505558A5 (https=) 2025-02-10

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US (2) US20240132502A1 (https=)
EP (2) EP4501327A3 (https=)
JP (1) JP2024505558A (https=)
KR (1) KR20230142539A (https=)
CN (1) CN117042769A (https=)
CA (1) CA3209082A1 (https=)
DK (1) DK4039688T3 (https=)
ES (1) ES3010513T3 (https=)
FI (1) FI4039688T3 (https=)
MX (1) MX2023008865A (https=)
WO (1) WO2022169798A2 (https=)

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TW202317099A (zh) * 2020-09-10 2023-05-01 美商絡速藥業公司 用於製備(s)-5-胺基-3-(4-((5-氟-2-甲氧基苯甲醯胺基)甲基)苯基)-1-(1,1,1-三氟丙烷-2-基)-1h-吡唑-4-甲醯胺之方法及中間體
CN118434717A (zh) * 2021-12-20 2024-08-02 西格马-奥尔德里奇有限责任公司 化学接头
WO2024169871A1 (zh) * 2023-02-17 2024-08-22 江苏威凯尔医药科技有限公司 Btk抑制剂及其用途
WO2024244888A1 (zh) * 2023-05-26 2024-12-05 广东弘烨医药科技有限公司 9元杂芳基化合物、含其的药物组合物及其制备方法和应用
AU2024298923A1 (en) 2023-07-25 2026-01-22 Monte Rosa Therapeutics Ag Substituted piperidinediones for targeted protein degradation
CN120535526A (zh) * 2024-02-26 2025-08-26 中国药科大学 直接结合蛋白酶体的非泛素依赖型蛋白水解靶向嵌合体NuTAC及其应用
WO2026040951A1 (zh) * 2024-08-19 2026-02-26 深圳市塔吉瑞生物医药股份有限公司 靶向btk蛋白降解靶向嵌合体类化合物及其组合物及用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017518276A (ja) * 2014-04-29 2017-07-06 チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物
JP2018527384A (ja) * 2015-09-16 2018-09-20 ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． がんの治療のためのｂｔｋ阻害剤としてのピラゾロピリミジン誘導体
US20190276459A1 (en) * 2018-03-10 2019-09-12 Yale University Modulators of btk proteolysis and methods of use
JP2019530650A (ja) * 2016-08-24 2019-10-24 アークル インコーポレイテッド アミノ−ピロロピリミジノン化合物およびその使用方法
WO2020239103A1 (zh) * 2019-05-31 2020-12-03 四川海思科制药有限公司 一种btk抑制剂环衍生物及其制备方法和药学上的应用
WO2020252397A1 (en) * 2019-06-12 2020-12-17 Baylor College Of Medicine Small molecule proteolysis-targeting chimeras and methods of use thereof

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US5114946A (en) 1987-06-12 1992-05-19 American Cyanamid Company Transdermal delivery of pharmaceuticals
US4818541A (en) 1987-08-19 1989-04-04 Schering Corporation Transdermal delivery of enantiomers of phenylpropanolamine
CN106146511A (zh) * 2015-04-03 2016-11-23 安润医药科技（苏州）有限公司 吡唑并嘧啶衍生物、制备方法、药物组合物及用途
ES2965081T3 (es) * 2016-07-07 2024-04-11 Daewoong Pharmaceutical Co Ltd Derivados 4-aminopirazolo[3,4-d]pirimidinil-azabiciclo y composición farmacéutica que comprende dichos derivados
WO2020023851A1 (en) * 2018-07-26 2020-01-30 Yale University Bifunctional substitued pyrimidines as modulators of fak proteolyse
CN112812100B (zh) * 2019-11-18 2022-04-05 四川海思科制药有限公司 一种具有降解btk激酶的化合物及其制备方法和药学上的应用
CN112979656A (zh) * 2019-12-12 2021-06-18 上海美志医药科技有限公司 一类靶向降解btk蛋白的化合物

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017518276A (ja) * 2014-04-29 2017-07-06 チョーチアン ディーティーアールエム バイオファーマ コーポレーション リミテッド ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物
JP2018527384A (ja) * 2015-09-16 2018-09-20 ロクソ オンコロジー， インコーポレイテッドＬｏｘｏ Ｏｎｃｏｌｏｇｙ， Ｉｎｃ． がんの治療のためのｂｔｋ阻害剤としてのピラゾロピリミジン誘導体
JP2019530650A (ja) * 2016-08-24 2019-10-24 アークル インコーポレイテッド アミノ−ピロロピリミジノン化合物およびその使用方法
US20190276459A1 (en) * 2018-03-10 2019-09-12 Yale University Modulators of btk proteolysis and methods of use
WO2020239103A1 (zh) * 2019-05-31 2020-12-03 四川海思科制药有限公司 一种btk抑制剂环衍生物及其制备方法和药学上的应用
WO2020252397A1 (en) * 2019-06-12 2020-12-17 Baylor College Of Medicine Small molecule proteolysis-targeting chimeras and methods of use thereof

Non-Patent Citations (1)

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Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 30(3), JPN6025051013, 2020, pages 126877, ISSN: 0005751667 *

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CN117042769A (zh) 2023-11-10
US20220259207A1 (en) 2022-08-18
ES3010513T3 (en) 2025-04-03
EP4039688B1 (en) 2024-10-09
DK4039688T3 (da) 2025-01-02
EP4039688A3 (en) 2022-11-23
WO2022169798A2 (en) 2022-08-11
EP4039688A2 (en) 2022-08-10
CA3209082A1 (en) 2022-08-11
MX2023008865A (es) 2023-08-31
FI4039688T3 (fi) 2024-12-19
EP4501327A3 (en) 2025-10-15
KR20230142539A (ko) 2023-10-11
US20240132502A1 (en) 2024-04-25
US11530222B2 (en) 2022-12-20
WO2022169798A3 (en) 2022-09-22
EP4501327A2 (en) 2025-02-05

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