CR20220614A - 2-amino-3-cianotiofenos anulados y derivados para el tratamiento del cáncer - Google Patents
2-amino-3-cianotiofenos anulados y derivados para el tratamiento del cáncerInfo
- Publication number
- CR20220614A CR20220614A CR20220614A CR20220614A CR20220614A CR 20220614 A CR20220614 A CR 20220614A CR 20220614 A CR20220614 A CR 20220614A CR 20220614 A CR20220614 A CR 20220614A CR 20220614 A CR20220614 A CR 20220614A
- Authority
- CR
- Costa Rica
- Prior art keywords
- treatment
- annulated
- cancer
- derivatives
- amino
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
-
- 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
-
- 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
- C07D487/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención comprende compuestos de la fórmula (I) , en donde R<sup>1a</sup>, R<sup>1b</sup>, R<sup>2a</sup>, R<sup>2b</sup>, Z, R<sup>3</sup> a R<sup>5</sup>, A, p, U, V, W, L y E tienen los significados dados en las reivindicaciones y la memoria descriptiva, su uso como inhibidores de proteínas mutantes de la familia Ras, composiciones farmacéuticas y preparaciones que contienen dichos compuestos y su uso como medicamentos/usos médicos, especialmente como agentes para el tratamiento y/o prevención de enfermedades oncológicas.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063033505P | 2020-06-02 | 2020-06-02 | |
| EP20212067 | 2020-12-05 | ||
| PCT/EP2021/064612 WO2021245051A1 (en) | 2020-06-02 | 2021-06-01 | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20220614A true CR20220614A (es) | 2023-05-08 |
Family
ID=76269742
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20220614A CR20220614A (es) | 2020-06-02 | 2021-06-01 | 2-amino-3-cianotiofenos anulados y derivados para el tratamiento del cáncer |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US11945812B2 (es) |
| EP (2) | EP4157837B1 (es) |
| JP (2) | JP7808056B2 (es) |
| KR (1) | KR20230019462A (es) |
| CN (3) | CN121758439A (es) |
| AU (1) | AU2021285032A1 (es) |
| BR (1) | BR112022023462A2 (es) |
| CA (1) | CA3183656A1 (es) |
| CL (1) | CL2022003289A1 (es) |
| CO (1) | CO2022017049A2 (es) |
| CR (1) | CR20220614A (es) |
| DO (1) | DOP2022000266A (es) |
| EC (1) | ECSP22089077A (es) |
| IL (1) | IL298633A (es) |
| JO (1) | JOP20220325A1 (es) |
| MX (1) | MX2022015260A (es) |
| PE (1) | PE20240493A1 (es) |
| TW (1) | TW202210474A (es) |
| WO (2) | WO2021245055A1 (es) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| ES3004338T3 (en) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Combination therapies |
| KR102871791B1 (ko) | 2018-09-10 | 2025-10-15 | 미라티 테라퓨틱스, 인크. | 병용 요법 |
| WO2020055761A1 (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 |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| JP7592601B2 (ja) | 2019-01-10 | 2024-12-02 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| CA3148745A1 (en) | 2019-08-29 | 2021-03-04 | Xiaolun Wang | Kras g12d inhibitors |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| KR20220130126A (ko) | 2019-12-20 | 2022-09-26 | 미라티 테라퓨틱스, 인크. | Sos1 억제제 |
| AU2021285032A1 (en) | 2020-06-02 | 2022-12-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| US12286431B2 (en) | 2020-09-11 | 2025-04-29 | Mirati Therapeutics, Inc. | Crystalline forms of a KRas G12C inhibitor |
| MX2023003338A (es) | 2020-09-23 | 2023-06-14 | Erasca Inc | Piridonas y pirimidonas tricíclicas. |
| US12398154B2 (en) | 2020-12-15 | 2025-08-26 | Mirati Therapeutics, Inc. | Azaquinazoline pan-KRas inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| AR125782A1 (es) | 2021-05-05 | 2023-08-16 | Revolution Medicines Inc | Inhibidores de ras |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| EP4441056A1 (en) * | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| CN119013272A (zh) * | 2021-12-01 | 2024-11-22 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及其衍生物 |
| TW202340209A (zh) | 2021-12-01 | 2023-10-16 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| EP4441051A1 (en) * | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| CR20240233A (es) | 2021-12-01 | 2024-07-17 | Univ Vanderbilt | Tiofenos 2-amino-3-ciano anulados y derivados para el tratamiento del cáncer |
| EP4452964A1 (en) * | 2021-12-22 | 2024-10-30 | Boehringer Ingelheim International GmbH | Heteroaromatic compounds for the treatment of cancer |
| JP2025503511A (ja) | 2021-12-28 | 2025-02-04 | アストラゼネカ ユーケー リミテッド | 抗体－薬物コンジュゲート及びｒａｓｇ１２ｃ阻害剤の組み合わせ |
| EP4475956A1 (en) | 2022-02-09 | 2024-12-18 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| WO2023230190A1 (en) | 2022-05-25 | 2023-11-30 | Quanta Therapeutics, Inc. | Pyrimidine based modulators and uses thereof |
| AU2023285116A1 (en) | 2022-06-10 | 2024-12-19 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN120035583A (zh) * | 2022-06-15 | 2025-05-23 | 米拉蒂治疗股份有限公司 | Pan-kras抑制剂 |
| AU2024234154A1 (en) | 2023-03-15 | 2025-09-25 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
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| WO2024216016A1 (en) | 2023-04-14 | 2024-10-17 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| AU2024252105A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| CN121712509A (zh) | 2023-05-04 | 2026-03-20 | 锐新医药公司 | 用于ras相关疾病或病症的组合疗法 |
| US20250019385A1 (en) * | 2023-05-30 | 2025-01-16 | Boehringer Ingelheim International Gmbh | Spirocyclic annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
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| IL327306A (en) | 2023-10-12 | 2026-05-01 | Revolution Medicines Inc | Macrocyclic RAS inhibitors |
| US20250205238A1 (en) | 2023-12-20 | 2025-06-26 | Boehringer Ingelheim International Gmbh | Anti-cancer combination therapy |
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| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
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| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
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| EP3972978A4 (en) | 2019-05-20 | 2023-04-26 | California Institute Of Technology | KRAS G12C INHIBITORS AND THEIR USES |
| RS63719B1 (sr) | 2019-12-11 | 2022-11-30 | Lilly Co Eli | Kras g12c inhibitori |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| TWI770760B (zh) | 2020-01-08 | 2022-07-11 | 大陸商蘇州亞盛藥業有限公司 | 螺環四氫喹唑啉 |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| CN113683616B (zh) | 2020-05-18 | 2025-12-30 | 广州百霆医药科技有限公司 | Kras g12c突变蛋白抑制剂 |
| AU2021285032A1 (en) | 2020-06-02 | 2022-12-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| EP4441056A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| TW202340209A (zh) | 2021-12-01 | 2023-10-16 | 德商百靈佳殷格翰國際股份有限公司 | 用於治療癌症之環狀2-胺基-3-氰基噻吩及衍生物 |
| US20230227470A1 (en) | 2021-12-01 | 2023-07-20 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2023099623A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| EP4441051A1 (en) | 2021-12-01 | 2024-10-09 | Boehringer Ingelheim International GmbH | Kras degrading compounds comprising annulated 2-amino-3-cyano thiophenes |
| CN119013272A (zh) | 2021-12-01 | 2024-11-22 | 勃林格殷格翰国际有限公司 | 用于治疗癌症的环状2-氨基-3-氰基噻吩及其衍生物 |
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2021
- 2021-06-01 AU AU2021285032A patent/AU2021285032A1/en not_active Abandoned
- 2021-06-01 BR BR112022023462A patent/BR112022023462A2/pt unknown
- 2021-06-01 PE PE2022002820A patent/PE20240493A1/es unknown
- 2021-06-01 WO PCT/EP2021/064616 patent/WO2021245055A1/en not_active Ceased
- 2021-06-01 WO PCT/EP2021/064612 patent/WO2021245051A1/en not_active Ceased
- 2021-06-01 KR KR1020227046273A patent/KR20230019462A/ko active Pending
- 2021-06-01 EP EP21729877.7A patent/EP4157837B1/en active Active
- 2021-06-01 CN CN202511504774.2A patent/CN121758439A/zh active Pending
- 2021-06-01 CA CA3183656A patent/CA3183656A1/en active Pending
- 2021-06-01 JP JP2022574134A patent/JP7808056B2/ja active Active
- 2021-06-01 TW TW110119842A patent/TW202210474A/zh unknown
- 2021-06-01 US US17/335,620 patent/US11945812B2/en active Active
- 2021-06-01 JP JP2022574317A patent/JP7808058B2/ja active Active
- 2021-06-01 IL IL298633A patent/IL298633A/en unknown
- 2021-06-01 US US18/000,442 patent/US20230212164A1/en active Pending
- 2021-06-01 CN CN202180039453.3A patent/CN116034106B/zh active Active
- 2021-06-01 EP EP21729875.1A patent/EP4157836B1/en active Active
- 2021-06-01 CN CN202180059643.1A patent/CN116234806B/zh active Active
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2022
- 2022-11-21 EC ECSENADI202289077A patent/ECSP22089077A/es unknown
- 2022-11-23 CL CL2022003289A patent/CL2022003289A1/es unknown
- 2022-11-25 DO DO2022000266A patent/DOP2022000266A/es unknown
- 2022-11-29 CO CONC2022/0017049A patent/CO2022017049A2/es unknown
- 2022-12-01 JO JOJO/P/2022/0325A patent/JOP20220325A1/ar unknown
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2024
- 2024-02-14 US US18/441,380 patent/US12545670B2/en active Active
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