CL2023002383A1 - Compuesto de quinazolina para inducir la degradación de la proteína kras mutante g12d - Google Patents
Compuesto de quinazolina para inducir la degradación de la proteína kras mutante g12dInfo
- Publication number
- CL2023002383A1 CL2023002383A1 CL2023002383A CL2023002383A CL2023002383A1 CL 2023002383 A1 CL2023002383 A1 CL 2023002383A1 CL 2023002383 A CL2023002383 A CL 2023002383A CL 2023002383 A CL2023002383 A CL 2023002383A CL 2023002383 A1 CL2023002383 A1 CL 2023002383A1
- Authority
- CL
- Chile
- Prior art keywords
- pancreatic cancer
- quinazoline compound
- compound
- kras protein
- mutant kras
- Prior art date
Links
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (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)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Proporcionar un compuesto útil como ingrediente activo de una composición farmacéutica para tratar el cáncer de páncreas. Los presentes inventores han estudiado un compuesto que es útil como ingrediente activo de una composición farmacéutica para tratar el cáncer de páncreas y han descubierto que un compuesto de quinazolina tiene una excelente acción inductora de degradación sobre una proteína KRAS mutante G12D y una actividad inhibidora de KRAS mutante G12D, y puede usarse como agente terapéutico para el cáncer de páncreas, con lo cual se completa la presente invención. El compuesto de quinazolina o una sal de este de la presente invención se puede usar como agente terapéutico para el cáncer de páncreas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021021656 | 2021-02-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2023002383A1 true CL2023002383A1 (es) | 2024-01-19 |
Family
ID=82838828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2023002383A CL2023002383A1 (es) | 2021-02-15 | 2023-08-11 | Compuesto de quinazolina para inducir la degradación de la proteína kras mutante g12d |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US12384794B2 (es) |
| EP (1) | EP4293024A4 (es) |
| JP (2) | JP7169729B1 (es) |
| KR (1) | KR20230145361A (es) |
| CN (1) | CN116848120A (es) |
| AR (1) | AR124870A1 (es) |
| AU (1) | AU2022221145A1 (es) |
| BR (1) | BR112023015067A2 (es) |
| CA (1) | CA3211051A1 (es) |
| CL (1) | CL2023002383A1 (es) |
| CO (1) | CO2023010710A2 (es) |
| CR (1) | CR20230404A (es) |
| DO (1) | DOP2023000161A (es) |
| EC (1) | ECSP23067156A (es) |
| IL (1) | IL305077A (es) |
| MX (1) | MX2023009521A (es) |
| PE (1) | PE20240235A1 (es) |
| TW (1) | TW202245751A (es) |
| WO (1) | WO2022173032A1 (es) |
| ZA (1) | ZA202307791B (es) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12384794B2 (en) * | 2021-02-15 | 2025-08-12 | Astellas Pharma Inc. | Quinazoline compound for inducing degradation of G12D mutant KRAS protein |
| WO2023119677A1 (en) | 2021-12-24 | 2023-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising a quinazoline compound |
| JPWO2023171781A1 (es) | 2022-03-11 | 2023-09-14 | ||
| WO2024019103A1 (ja) | 2022-07-21 | 2024-01-25 | アステラス製薬株式会社 | G12d変異krasタンパクに作用する複素環化合物 |
| KR20250044266A (ko) | 2022-08-05 | 2025-03-31 | 아스텔라스세이야쿠 가부시키가이샤 | 변이 kras 단백의 분해를 유도하기 위한 복소환 화합물 |
| TW202413346A (zh) | 2022-08-09 | 2024-04-01 | 日商安斯泰來製藥股份有限公司 | 用於誘導g12v突變kras蛋白之分解之雜環化合物 |
| EP4570794A1 (en) | 2022-08-09 | 2025-06-18 | Astellas Pharma, Inc. | Heterocyclic compound for inhibiting and/or inducing degradation of kras protein |
| CA3264252A1 (en) * | 2022-08-12 | 2024-02-15 | Astellas Pharma Inc. | Combination of anticancer agents comprising a bifunctional compound with inhibitory activity against mutant Kirsten rat sarcoma virus G12D |
| 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 |
| JP7733274B1 (ja) * | 2022-08-12 | 2025-09-02 | 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 |
| 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 |
| KR20250151412A (ko) | 2023-01-26 | 2025-10-21 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레블론계 kras 분해 단백질 및 이와 관련된 용도 |
| 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 |
| WO2024199266A1 (en) * | 2023-03-27 | 2024-10-03 | Shenzhen Ionova Life Science Co., Ltd. | Compounds for degradation and inhibition of kras (g12d) protein |
| AR133028A1 (es) | 2023-06-22 | 2025-08-20 | Astellas Pharma Inc | Composición farmacéutica que comprende un degradador de todas las kras |
| AR133027A1 (es) * | 2023-06-22 | 2025-08-20 | Astellas Pharma Inc | Composición farmacéutica que comprende un compuesto de quinazolina |
| WO2025054530A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as 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 |
| WO2025080592A1 (en) | 2023-10-09 | 2025-04-17 | Incyte Corporation | Combination comprising a kras g12d inhibitor and an egfr inhibitor for use in the treatment of cancer |
| WO2025080593A1 (en) | 2023-10-09 | 2025-04-17 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| WO2025078984A1 (en) * | 2023-10-10 | 2025-04-17 | 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 |
| JP7724392B1 (ja) * | 2024-01-24 | 2025-08-15 | アステラス製薬株式会社 | Krasタンパクの分解を誘導するための複素環化合物 |
| WO2025169901A1 (ja) * | 2024-02-05 | 2025-08-14 | アステラス製薬株式会社 | 変異krasタンパク分解誘導作用を有する複素環化合物を含む抗体薬物複合体 |
| 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 |
|---|---|---|---|---|
| HK1208875A1 (en) | 2012-01-12 | 2016-03-18 | 耶鲁大学 | Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase |
| MX387318B (es) | 2014-04-14 | 2025-03-18 | Arvinas Operations Inc | Moduladores de la proteólisis basados en imida y métodos de uso asociados. |
| 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 |
| US10822312B2 (en) * | 2016-03-30 | 2020-11-03 | 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 |
| JP7720698B2 (ja) * | 2018-04-04 | 2025-08-08 | アルビナス・オペレーションズ・インコーポレイテッド | タンパク質分解の調節因子および関連する使用方法 |
| US12365677B2 (en) | 2018-07-20 | 2025-07-22 | Dana-Farber Cancer Institute, Inc. | Degraders that target proteins via KEAP1 |
| JP7622043B2 (ja) | 2019-08-29 | 2025-01-27 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12d阻害剤 |
| 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 |
| US20220370416A1 (en) | 2020-04-06 | 2022-11-24 | Arvinas Operations, Inc. | Compounds and methods for targeted degradation of kras |
| WO2022061348A1 (en) | 2020-09-16 | 2022-03-24 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2022148421A1 (en) | 2021-01-08 | 2022-07-14 | Beigene, Ltd. | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| WO2022148422A1 (en) | 2021-01-08 | 2022-07-14 | Beigene, Ltd. | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| US12384794B2 (en) * | 2021-02-15 | 2025-08-12 | Astellas Pharma Inc. | Quinazoline compound for inducing degradation of G12D mutant KRAS protein |
| WO2023119677A1 (en) * | 2021-12-24 | 2023-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising a quinazoline compound |
-
2022
- 2022-02-14 US US18/268,001 patent/US12384794B2/en active Active
- 2022-02-14 AU AU2022221145A patent/AU2022221145A1/en active Pending
- 2022-02-14 CR CR20230404A patent/CR20230404A/es unknown
- 2022-02-14 PE PE2023002366A patent/PE20240235A1/es unknown
- 2022-02-14 IL IL305077A patent/IL305077A/en unknown
- 2022-02-14 WO PCT/JP2022/005582 patent/WO2022173032A1/ja not_active Ceased
- 2022-02-14 MX MX2023009521A patent/MX2023009521A/es unknown
- 2022-02-14 KR KR1020237027669A patent/KR20230145361A/ko active Pending
- 2022-02-14 CA CA3211051A patent/CA3211051A1/en active Pending
- 2022-02-14 BR BR112023015067A patent/BR112023015067A2/pt active Search and Examination
- 2022-02-14 JP JP2022542202A patent/JP7169729B1/ja active Active
- 2022-02-14 CN CN202280014815.8A patent/CN116848120A/zh active Pending
- 2022-02-14 EP EP22752854.4A patent/EP4293024A4/en active Pending
- 2022-02-14 TW TW111105240A patent/TW202245751A/zh unknown
- 2022-02-14 AR ARP220100290A patent/AR124870A1/es unknown
- 2022-10-27 JP JP2022172197A patent/JP2022191505A/ja active Pending
-
2023
- 2023-08-08 ZA ZA2023/07791A patent/ZA202307791B/en unknown
- 2023-08-11 CL CL2023002383A patent/CL2023002383A1/es 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
Also Published As
| Publication number | Publication date |
|---|---|
| TW202245751A (zh) | 2022-12-01 |
| ZA202307791B (en) | 2024-12-18 |
| JPWO2022173032A1 (es) | 2022-08-18 |
| KR20230145361A (ko) | 2023-10-17 |
| CO2023010710A2 (es) | 2023-09-18 |
| WO2022173032A1 (ja) | 2022-08-18 |
| US12384794B2 (en) | 2025-08-12 |
| JP2022191505A (ja) | 2022-12-27 |
| US20240182483A1 (en) | 2024-06-06 |
| US20250340561A1 (en) | 2025-11-06 |
| IL305077A (en) | 2023-10-01 |
| DOP2023000161A (es) | 2023-09-29 |
| CN116848120A (zh) | 2023-10-03 |
| JP7169729B1 (ja) | 2022-11-11 |
| CR20230404A (es) | 2023-09-21 |
| AU2022221145A1 (en) | 2023-09-21 |
| EP4293024A4 (en) | 2025-03-05 |
| PE20240235A1 (es) | 2024-02-16 |
| AR124870A1 (es) | 2023-05-17 |
| MX2023009521A (es) | 2023-08-24 |
| ECSP23067156A (es) | 2023-10-31 |
| CA3211051A1 (en) | 2022-08-18 |
| BR112023015067A2 (pt) | 2023-10-03 |
| EP4293024A1 (en) | 2023-12-20 |
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