AR124870A1 - 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
- AR124870A1 AR124870A1 ARP220100290A ARP220100290A AR124870A1 AR 124870 A1 AR124870 A1 AR 124870A1 AR P220100290 A ARP220100290 A AR P220100290A AR P220100290 A ARP220100290 A AR P220100290A AR 124870 A1 AR124870 A1 AR 124870A1
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- nitrogen
- sulfur
- alkyl
- oxygen
- Prior art date
Links
- -1 QUINAZOLINE COMPOUND Chemical class 0.000 title abstract 8
- 102100030708 GTPase KRas Human genes 0.000 title abstract 3
- 102200006539 rs121913529 Human genes 0.000 title abstract 3
- 230000015556 catabolic process Effects 0.000 title abstract 2
- 238000006731 degradation reaction Methods 0.000 title abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 14
- 229910052760 oxygen Inorganic materials 0.000 abstract 8
- 229910052717 sulfur Inorganic materials 0.000 abstract 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 7
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 7
- 125000005842 heteroatom Chemical group 0.000 abstract 7
- 229910052757 nitrogen Chemical group 0.000 abstract 7
- 239000001301 oxygen Substances 0.000 abstract 7
- 239000011593 sulfur Chemical group 0.000 abstract 7
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 201000002528 pancreatic cancer Diseases 0.000 abstract 4
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 2
- 229940124597 therapeutic agent Drugs 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
- 229920002554 vinyl polymer Polymers 0.000 abstract 1
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
- 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
Landscapes
- 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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021021656 | 2021-02-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR124870A1 true AR124870A1 (es) | 2023-05-17 |
Family
ID=82838828
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220100290A AR124870A1 (es) | 2021-02-15 | 2022-02-14 | Compuesto de quinazolina para inducir la degradación de la proteína kras mutante g12d |
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
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 |
| JP7169729B1 (ja) | 2022-11-11 |
| 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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