PE20230161A1 - Inhibidores de proteinas kras mutantes - Google Patents
Inhibidores de proteinas kras mutantesInfo
- Publication number
- PE20230161A1 PE20230161A1 PE2022001137A PE2022001137A PE20230161A1 PE 20230161 A1 PE20230161 A1 PE 20230161A1 PE 2022001137 A PE2022001137 A PE 2022001137A PE 2022001137 A PE2022001137 A PE 2022001137A PE 20230161 A1 PE20230161 A1 PE 20230161A1
- Authority
- PE
- Peru
- Prior art keywords
- alkynyl
- alkenyl
- alkyl
- compound
- mutant kras
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- QRRJEUIQLZNPIO-UHFFFAOYSA-N C(C=C)(=O)N1CCN(CC1)C1=C(C(N(C2=NC(=C(C=C12)Cl)C1=C(C(=C(C(=C1F)F)F)F)N)C=1C(=NC=CC=1C)C(C)C)=O)C#N Chemical compound C(C=C)(=O)N1CCN(CC1)C1=C(C(N(C2=NC(=C(C=C12)Cl)C1=C(C(=C(C(=C1F)F)F)F)N)C=1C(=NC=CC=1C)C(C)C)=O)C#N QRRJEUIQLZNPIO-UHFFFAOYSA-N 0.000 abstract 1
- 102100030708 GTPase KRas Human genes 0.000 abstract 1
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07D487/04—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Peptides Or Proteins (AREA)
Abstract
La presente invencion se refiere a un compuesto de la formula (I), sus estereoisomeros, atropisomeros y sales farmaceuticamente aceptables; en donde cada R11, R12, R13, R14 o R15 esta seleccionado, independientemente, de halogeno, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, heteroalquilo C2-6, -CN, entre otros, opcionalmente sustituidos; R21 o R22 esta seleccionado, independientemente, de hidrogeno, halogeno, alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6; entre otros; R3 esta seleccionado de -alquilo C1-14, -alquenilo C2-14, -alquinilo C2-14, entre otros. Un compuesto seleccionado es 4-(4-acriloilpiperazin-1-il)-7-(2-amino-3,4,5,6-tetrafluorofenil)-6-cloro-1-(2-isopropil-4- metil piridin-3-il)-2-oxo-1,2-dihidro-1,8-naftiridin-3-carbonitrilo. Tambien refiere a una composicion farmaceutica que lo comprende. Dicho compuesto es inhibidor de la proteina KRAS mutante, siendo util para el tratamiento del cancer.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019126687 | 2019-12-19 | ||
| CN2020070885 | 2020-01-08 | ||
| CN2020073723 | 2020-01-22 | ||
| CN2020078565 | 2020-03-10 | ||
| PCT/CN2020/137497 WO2021121367A1 (en) | 2019-12-19 | 2020-12-18 | Kras mutant protein inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230161A1 true PE20230161A1 (es) | 2023-02-01 |
Family
ID=76478185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022001137A PE20230161A1 (es) | 2019-12-19 | 2020-12-18 | Inhibidores de proteinas kras mutantes |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US11180506B2 (es) |
| EP (1) | EP4077326A4 (es) |
| JP (1) | JP7644517B2 (es) |
| KR (1) | KR20220119088A (es) |
| CN (4) | CN114349750A (es) |
| AU (1) | AU2020404319A1 (es) |
| BR (1) | BR112022011421A2 (es) |
| CA (1) | CA3165238A1 (es) |
| CL (1) | CL2022001670A1 (es) |
| CO (1) | CO2022010098A2 (es) |
| CR (1) | CR20220351A (es) |
| IL (1) | IL293962B2 (es) |
| MX (1) | MX2022007527A (es) |
| PE (1) | PE20230161A1 (es) |
| PH (1) | PH12022551503A1 (es) |
| TW (1) | TWI871397B (es) |
| WO (1) | WO2021121367A1 (es) |
| ZA (2) | ZA202207450B (es) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3577109A4 (en) | 2017-01-31 | 2020-11-18 | Arvinas Operations, Inc. | CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM |
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| WO2020018975A1 (en) | 2018-07-20 | 2020-01-23 | Genentech, Inc. | Sulfonimidamide compounds as inhibitors of interleukin-1 activity |
| PT3849537T (pt) | 2018-09-10 | 2025-01-22 | Mirati Therapeutics Inc | Terapêuticas de combinação |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| WO2020085493A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 新規なインダゾール化合物又はその塩 |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| KR20210121168A (ko) * | 2019-01-29 | 2021-10-07 | 브라이트제네 바이오-메디컬 테크놀로지 코., 엘티디. | 복소환식 화합물인 벤조피리돈 및 그 사용 |
| KR20220071193A (ko) | 2019-08-29 | 2022-05-31 | 미라티 테라퓨틱스, 인크. | Kras g12d 억제제 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| US11890285B2 (en) | 2019-09-24 | 2024-02-06 | Mirati Therapeutics, Inc. | Combination therapies |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| AU2020405129A1 (en) | 2019-12-19 | 2022-06-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| CN114349750A (zh) * | 2019-12-19 | 2022-04-15 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| CN115135315B (zh) | 2019-12-20 | 2024-11-26 | 米拉蒂治疗股份有限公司 | Sos1抑制剂 |
| CN114671866A (zh) * | 2020-12-25 | 2022-06-28 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| WO2021249563A1 (zh) * | 2020-06-12 | 2021-12-16 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| MX2023002942A (es) | 2020-09-11 | 2023-05-22 | Mirati Therapeutics Inc | Formas cristalinas de un inhibidor de kras g12c. |
| CN115916778A (zh) * | 2020-09-12 | 2023-04-04 | 赛诺哈勃药业（成都）有限公司 | 甲硫氨酸腺苷转移酶抑制剂、其制备方法及应用 |
| PE20231207A1 (es) | 2020-09-15 | 2023-08-17 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer |
| KR20230094198A (ko) | 2020-09-23 | 2023-06-27 | 에라스카, 아이엔씨. | 3환식 피리돈 및 피리미돈 |
| CA3198885A1 (en) | 2020-12-15 | 2022-06-23 | Xiaolun Wang | Azaquinazoline pan-kras inhibitors |
| US11999753B2 (en) | 2020-12-16 | 2024-06-04 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-KRas inhibitors |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| PE20240089A1 (es) | 2021-05-05 | 2024-01-16 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cancer |
| MX2023013085A (es) | 2021-05-05 | 2023-11-16 | Revolution Medicines Inc | Inhibidores de ras. |
| WO2022237815A1 (en) * | 2021-05-12 | 2022-11-17 | Jacobio Pharmaceuticals Co., Ltd. | Novel forms of Compound I and use thereof |
| KR20240041917A (ko) | 2021-07-27 | 2024-04-01 | 도레이 카부시키가이샤 | 암의 치료 및/또는 예방을 위한 의약품 |
| CN115894520A (zh) * | 2021-09-23 | 2023-04-04 | 上海和誉生物医药科技有限公司 | 一种大环k-ras g12c抑制剂及其制备方法和在药学上的应用 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| CN119136806A (zh) | 2022-03-08 | 2024-12-13 | 锐新医药公司 | 用于治疗免疫难治性肺癌的方法 |
| CN116327956B (zh) * | 2022-04-01 | 2025-11-28 | 劲方医药科技(上海)股份有限公司 | 药物组合物、其用途及癌症的治疗方法 |
| CN120504682A (zh) | 2022-06-10 | 2025-08-19 | 锐新医药公司 | 大环ras抑制剂 |
| KR102724980B1 (ko) | 2022-09-21 | 2024-10-31 | 한화솔루션 주식회사 | 탠덤 태양전지 및 이의 제조방법 |
| WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| IL320639A (en) | 2022-11-09 | 2025-07-01 | Revolution Medicines Inc | Compounds, complexes and methods for their preparation and use |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| AU2024253668A1 (en) | 2023-04-07 | 2025-11-13 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| US20240352038A1 (en) | 2023-04-14 | 2024-10-24 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025036475A1 (en) * | 2023-08-17 | 2025-02-20 | Jacobio Pharmaceuticals Co., Ltd. | A pharmaceutical combination and use thereof |
| WO2025036470A1 (en) * | 2023-08-17 | 2025-02-20 | Jacobio Pharmaceuticals Co., Ltd. | Use of compound a for treating a cancer |
| WO2025067459A2 (en) | 2023-09-29 | 2025-04-03 | D3 Bio (Wuxi) Co., Ltd. | Therapies for the treatment of cancer |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202535891A (zh) | 2023-10-20 | 2025-09-16 | 美商默沙東有限責任公司 | Ｋｒａｓ蛋白之小分子抑制劑 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012080187A1 (de) | 2010-12-16 | 2012-06-21 | Bayer Cropscience Ag | 6-(2-aminophenyl)-picolinate und deren verwendung als herbizide |
| WO2015058084A1 (en) | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
| US10892525B2 (en) | 2016-06-29 | 2021-01-12 | University Of Kentucky Research Foundation | Rechargeable batteries including high-voltage cathode and redox shuttle conferring overcharge protection |
| JP2019529484A (ja) * | 2016-09-29 | 2019-10-17 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤 |
| CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| JOP20190272A1 (ar) * | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| EA202091186A1 (ru) * | 2017-11-15 | 2020-10-01 | Мирати Терапьютикс, Инк. | ИНГИБИТОРЫ KRas G12C |
| CN113121530B (zh) * | 2018-01-19 | 2022-08-05 | 勤浩医药（苏州）有限公司 | 作为krasg12c突变蛋白抑制剂的吡啶酮并嘧啶类衍生物 |
| MX2020012204A (es) * | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| CA3100390A1 (en) * | 2018-06-12 | 2020-03-12 | Amgen Inc. | Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer |
| CN114349750A (zh) * | 2019-12-19 | 2022-04-15 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
-
2020
- 2020-12-18 CN CN202111617953.9A patent/CN114349750A/zh active Pending
- 2020-12-18 KR KR1020227024638A patent/KR20220119088A/ko active Pending
- 2020-12-18 CR CR20220351A patent/CR20220351A/es unknown
- 2020-12-18 BR BR112022011421A patent/BR112022011421A2/pt unknown
- 2020-12-18 AU AU2020404319A patent/AU2020404319A1/en active Pending
- 2020-12-18 CN CN202210597916.4A patent/CN115192577B/zh active Active
- 2020-12-18 PH PH1/2022/551503A patent/PH12022551503A1/en unknown
- 2020-12-18 PE PE2022001137A patent/PE20230161A1/es unknown
- 2020-12-18 IL IL293962A patent/IL293962B2/en unknown
- 2020-12-18 TW TW109145045A patent/TWI871397B/zh active
- 2020-12-18 EP EP20903388.5A patent/EP4077326A4/en active Pending
- 2020-12-18 WO PCT/CN2020/137497 patent/WO2021121367A1/en not_active Ceased
- 2020-12-18 CN CN202111058976.0A patent/CN113651814B/zh active Active
- 2020-12-18 JP JP2022537297A patent/JP7644517B2/ja active Active
- 2020-12-18 CN CN202080014581.8A patent/CN113454083A/zh active Pending
- 2020-12-18 MX MX2022007527A patent/MX2022007527A/es unknown
- 2020-12-18 CA CA3165238A patent/CA3165238A1/en active Pending
-
2021
- 2021-03-10 US US17/197,095 patent/US11180506B2/en active Active
- 2021-08-20 US US17/407,418 patent/US11787811B2/en active Active
- 2021-12-27 US US17/562,492 patent/US12195473B2/en active Active
-
2022
- 2022-06-17 CL CL2022001670A patent/CL2022001670A1/es unknown
- 2022-07-05 ZA ZA2022/07450A patent/ZA202207450B/en unknown
- 2022-07-18 CO CONC2022/0010098A patent/CO2022010098A2/es unknown
- 2022-08-05 ZA ZA2022/08783A patent/ZA202208783B/en unknown
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