JP7169729B1 - Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物 - Google Patents

Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物 Download PDF

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Publication number
JP7169729B1
JP7169729B1 JP2022542202A JP2022542202A JP7169729B1 JP 7169729 B1 JP7169729 B1 JP 7169729B1 JP 2022542202 A JP2022542202 A JP 2022542202A JP 2022542202 A JP2022542202 A JP 2022542202A JP 7169729 B1 JP7169729 B1 JP 7169729B1
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methyl
compound
phenyl
hydroxy
oxy
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JPWO2022173032A5 (https=
JPWO2022173032A1 (https=
Inventor
友博 吉成
裕貴 石岡
英次 河南
英之 渡邊
賢一 川口
和幸 倉本
智禎 今泉
貴裕 森川
壽雄 濱口
直 ▲今▼田
光晶 奥村
建之 長島
耕平 稲村
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Astellas Pharma Inc
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Astellas Pharma Inc
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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
    • C07D487/08—Bridged 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2022542202A 2021-02-15 2022-02-14 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物 Active JP7169729B1 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2022172197A JP7851842B2 (ja) 2021-02-15 2022-10-27 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
JP2025279854A JP2026048973A (ja) 2021-02-15 2025-12-24 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2021021656 2021-02-15
JP2021021656 2021-02-15
PCT/JP2022/005582 WO2022173032A1 (ja) 2021-02-15 2022-02-14 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物

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JP2022172197A Division JP7851842B2 (ja) 2021-02-15 2022-10-27 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物

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JPWO2022173032A1 JPWO2022173032A1 (https=) 2022-08-18
JP7169729B1 true JP7169729B1 (ja) 2022-11-11
JPWO2022173032A5 JPWO2022173032A5 (https=) 2023-01-24

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JP2022542202A Active JP7169729B1 (ja) 2021-02-15 2022-02-14 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
JP2022172197A Active JP7851842B2 (ja) 2021-02-15 2022-10-27 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
JP2025279854A Pending JP2026048973A (ja) 2021-02-15 2025-12-24 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物

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JP2022172197A Active JP7851842B2 (ja) 2021-02-15 2022-10-27 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
JP2025279854A Pending JP2026048973A (ja) 2021-02-15 2025-12-24 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物

Country Status (19)

Country Link
US (2) US12384794B2 (https=)
EP (2) EP4293024B1 (https=)
JP (3) JP7169729B1 (https=)
KR (1) KR20230145361A (https=)
CN (1) CN116848120B (https=)
AR (1) AR124870A1 (https=)
AU (1) AU2022221145A1 (https=)
CA (1) CA3211051A1 (https=)
CL (1) CL2023002383A1 (https=)
CO (1) CO2023010710A2 (https=)
CR (1) CR20230404A (https=)
DO (1) DOP2023000161A (https=)
EC (1) ECSP23067156A (https=)
IL (1) IL305077A (https=)
JO (1) JOP20230190A1 (https=)
MX (1) MX2023009521A (https=)
PE (1) PE20240235A1 (https=)
WO (1) WO2022173032A1 (https=)
ZA (1) ZA202307791B (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022191505A (ja) * 2021-02-15 2022-12-27 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
JP2025528008A (ja) * 2022-08-12 2025-08-26 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓ阻害活性を有する二官能性化合物を含む抗がん剤の組合せ
JP2025530624A (ja) * 2022-08-12 2025-09-17 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓ阻害活性を有する二官能性化合物を含む抗がん剤の組合せ

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WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
WO2023119677A1 (en) 2021-12-24 2023-06-29 Astellas Pharma Inc. Pharmaceutical composition comprising a quinazoline compound
TW202346270A (zh) 2022-03-11 2023-12-01 日商安斯泰來製藥股份有限公司 用於誘發g12d突變kras蛋白分解之雜環化合物
US20250145631A1 (en) 2022-07-21 2025-05-08 Astellas Pharma Inc. Heterocyclic compound acting on g12d mutant kras protein
TW202412789A (zh) 2022-08-05 2024-04-01 日商安斯泰來製藥股份有限公司 用於誘導突變kras蛋白分解之雜環化合物
EP4570795A1 (en) 2022-08-09 2025-06-18 Astellas Pharma, Inc. Heterocyclic compound for inducing degradation of g12v mutant kras protein
EP4570794A1 (en) 2022-08-09 2025-06-18 Astellas Pharma, Inc. Heterocyclic compound for inhibiting and/or inducing degradation of kras protein
WO2024032747A1 (zh) 2022-08-12 2024-02-15 正大天晴药业集团股份有限公司 三环类化合物及其医药用途
WO2024034123A1 (ja) * 2022-08-12 2024-02-15 アステラス製薬株式会社 複素環化合物を含む医薬組成物
CN115873018B (zh) * 2022-11-18 2024-03-15 中国药科大学 苯并嘧啶和苯并三嗪类造血祖细胞激酶1降解剂及其应用
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto
WO2024188281A1 (zh) * 2023-03-13 2024-09-19 南京明德新药研发有限公司 含喹唑啉结构的化合物及其应用
KR20260016466A (ko) * 2023-03-27 2026-02-03 셴젠 이오노바 라이프 사이언스 시오., 엘티디. Kras(g12d) 단백질의 분해 및 억제를 위한 화합물
AR133027A1 (es) * 2023-06-22 2025-08-20 Astellas Pharma Inc Composición farmacéutica que comprende un compuesto de quinazolina
AR133028A1 (es) 2023-06-22 2025-08-20 Astellas Pharma Inc Composición farmacéutica que comprende un degradador de todas las kras
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2025052649A1 (ja) * 2023-09-08 2025-03-13 アステラス製薬株式会社 単一の軸不斉化合物の選択的製造法
TW202528311A (zh) 2023-09-13 2025-07-16 日商安斯泰來製藥股份有限公司 包含具有ｇ１２ｄ突變ｋｒａｓ蛋白分解誘導作用之雜環化合物的抗體藥物複合體
US20250114346A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
US20250114339A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor
AU2024360867A1 (en) * 2023-10-10 2026-04-02 Aurigene Oncology Limited Substituted tricyclic compounds as kras degraders
WO2025108479A1 (en) * 2023-11-24 2025-05-30 Shenzhen Ionova Life Science Co., Ltd. Compounds for degradation or inhibition of kras mutant proteins and uses thereof
WO2025151765A1 (en) * 2024-01-10 2025-07-17 1200 Pharma Llc Kras g12d degraders and uses thereof
TW202545930A (zh) * 2024-01-24 2025-12-01 日商安斯泰來製藥股份有限公司 用於誘導kras蛋白質之分解之雜環化合物
TW202545934A (zh) * 2024-02-05 2025-12-01 日商安斯泰來製藥股份有限公司 包含具有突變ｋｒａｓ蛋白分解誘導作用之雜環化合物的抗體藥物複合體
WO2025168124A1 (zh) * 2024-02-08 2025-08-14 杭州多域生物技术有限公司 喹唑啉类化合物、其药物组合物及其应用

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JP2015508414A (ja) * 2012-01-12 2015-03-19 イエール ユニバーシティ Ｅ３ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法
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Publication number Priority date Publication date Assignee Title
JP2022191505A (ja) * 2021-02-15 2022-12-27 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
JP2025528008A (ja) * 2022-08-12 2025-08-26 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓ阻害活性を有する二官能性化合物を含む抗がん剤の組合せ
JP2025530624A (ja) * 2022-08-12 2025-09-17 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓ阻害活性を有する二官能性化合物を含む抗がん剤の組合せ

Also Published As

Publication number Publication date
US20240182483A1 (en) 2024-06-06
JP2026048973A (ja) 2026-03-17
PE20240235A1 (es) 2024-02-16
EP4293024B1 (en) 2026-04-08
US20250340561A1 (en) 2025-11-06
KR20230145361A (ko) 2023-10-17
IL305077A (en) 2023-10-01
CA3211051A1 (en) 2022-08-18
JOP20230190A1 (ar) 2023-08-14
CN116848120B (zh) 2026-02-13
TW202245751A (zh) 2022-12-01
BR112023015067A2 (pt) 2023-10-03
CN116848120A (zh) 2023-10-03
EP4706774A3 (en) 2026-04-15
EP4706774A2 (en) 2026-03-11
US12384794B2 (en) 2025-08-12
AU2022221145A1 (en) 2023-09-21
DOP2023000161A (es) 2023-09-29
MX2023009521A (es) 2023-08-24
EP4293024A4 (en) 2025-03-05
CO2023010710A2 (es) 2023-09-18
ECSP23067156A (es) 2023-10-31
AR124870A1 (es) 2023-05-17
JP2022191505A (ja) 2022-12-27
WO2022173032A1 (ja) 2022-08-18
JPWO2022173032A1 (https=) 2022-08-18
EP4293024A1 (en) 2023-12-20
ZA202307791B (en) 2024-12-18
CR20230404A (es) 2023-09-21
CL2023002383A1 (es) 2024-01-19
JP7851842B2 (ja) 2026-04-27

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