JPWO2022173032A5 - - Google Patents
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- Publication number
- JPWO2022173032A5 JPWO2022173032A5 JP2022542202A JP2022542202A JPWO2022173032A5 JP WO2022173032 A5 JPWO2022173032 A5 JP WO2022173032A5 JP 2022542202 A JP2022542202 A JP 2022542202A JP 2022542202 A JP2022542202 A JP 2022542202A JP WO2022173032 A5 JPWO2022173032 A5 JP WO2022173032A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- phenyl
- hydroxy
- oxy
- compound
- 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.)
- Granted
Links
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 108
- 150000001875 compounds Chemical class 0.000 claims 74
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 48
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 42
- 150000003839 salts Chemical class 0.000 claims 37
- -1 {6-cyclopropyl-4-[(1S,4S)-2,5-diazabicyclo[2.2.1]heptane-2- yl]-2-{[1-(2,2-difluoroethyl)piperidin-4-yl]oxy}-7-(6-fluoro-5-methyl-1H-indazol-4-yl)quinazolin-8-yl }oxy Chemical group 0.000 claims 29
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 4
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JPWO2022173032A1 JPWO2022173032A1 (https=) | 2022-08-18 |
| JP7169729B1 JP7169729B1 (ja) | 2022-11-11 |
| JPWO2022173032A5 true JPWO2022173032A5 (https=) | 2023-01-24 |
Family
ID=82838828
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| WO2022173032A1 (ja) * | 2021-02-15 | 2022-08-18 | 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 |
| 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 |
| AR130192A1 (es) * | 2022-08-12 | 2024-11-13 | Astellas Pharma Inc | Combinaciones antineoplásicas que comprenden quimioterapia |
| AR130191A1 (es) * | 2022-08-12 | 2024-11-13 | Astellas Pharma Inc | Combinaciones antineoplásicas que comprenden tratamiento dirigido |
| 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 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102668696B1 (ko) | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| RU2738833C9 (ru) | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| WO2017172979A1 (en) * | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| WO2019195609A2 (en) * | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| CA3102996A1 (en) | 2018-07-20 | 2020-01-23 | Dana-Farber Cancer Institute, Inc. | Degraders that target proteins via keap1 |
| MX2022002465A (es) * | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| US20230002371A1 (en) | 2019-09-13 | 2023-01-05 | Biotheryx, Inc. | Ras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2021106231A1 (en) | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| CN115803030A (zh) | 2020-04-06 | 2023-03-14 | 阿维纳斯企业公司 | 用于kras靶向降解的化合物和方法 |
| US20240025863A1 (en) | 2020-09-16 | 2024-01-25 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2022148422A1 (en) | 2021-01-08 | 2022-07-14 | Beigene, Ltd. | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| US20240092803A1 (en) | 2021-01-08 | 2024-03-21 | Beigene Switzerland Gmbh | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| WO2022173032A1 (ja) * | 2021-02-15 | 2022-08-18 | 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 |
| WO2023119677A1 (en) * | 2021-12-24 | 2023-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising a quinazoline compound |
-
2022
- 2022-02-14 WO PCT/JP2022/005582 patent/WO2022173032A1/ja not_active Ceased
- 2022-02-14 AU AU2022221145A patent/AU2022221145A1/en active Pending
- 2022-02-14 CR CR20230404A patent/CR20230404A/es unknown
- 2022-02-14 US US18/268,001 patent/US12384794B2/en active Active
- 2022-02-14 EP EP22752854.4A patent/EP4293024B1/en active Active
- 2022-02-14 CN CN202280014815.8A patent/CN116848120B/zh active Active
- 2022-02-14 IL IL305077A patent/IL305077A/en unknown
- 2022-02-14 CA CA3211051A patent/CA3211051A1/en active Pending
- 2022-02-14 EP EP26152405.2A patent/EP4706774A3/en active Pending
- 2022-02-14 AR ARP220100290A patent/AR124870A1/es unknown
- 2022-02-14 PE PE2023002366A patent/PE20240235A1/es unknown
- 2022-02-14 KR KR1020237027669A patent/KR20230145361A/ko active Pending
- 2022-02-14 MX MX2023009521A patent/MX2023009521A/es unknown
- 2022-02-14 JP JP2022542202A patent/JP7169729B1/ja active Active
- 2022-10-27 JP JP2022172197A patent/JP7851842B2/ja active Active
-
2023
- 2023-08-08 ZA ZA2023/07791A patent/ZA202307791B/en unknown
- 2023-08-11 CL CL2023002383A patent/CL2023002383A1/es unknown
- 2023-08-14 JO JOJO/P/2023/0190A patent/JOP20230190A1/ar unknown
- 2023-08-15 DO DO2023000161A patent/DOP2023000161A/es unknown
- 2023-08-16 CO CONC2023/0010710A patent/CO2023010710A2/es unknown
- 2023-09-05 EC ECSENADI202367156A patent/ECSP23067156A/es unknown
-
2025
- 2025-07-14 US US19/268,038 patent/US20250340561A1/en active Pending
- 2025-12-24 JP JP2025279854A patent/JP2026048973A/ja active Pending
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