AR111776A1 - Heteroarilos inhibidores de las proteínas ras mutantes de g12c - Google Patents
Heteroarilos inhibidores de las proteínas ras mutantes de g12cInfo
- Publication number
- AR111776A1 AR111776A1 ARP180101198A ARP180101198A AR111776A1 AR 111776 A1 AR111776 A1 AR 111776A1 AR P180101198 A ARP180101198 A AR P180101198A AR P180101198 A ARP180101198 A AR P180101198A AR 111776 A1 AR111776 A1 AR 111776A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- hydroxy
- heteroaryl
- alkoxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Procesos e intermedios usados para su preparación, a composiciones farmacéuticas que los contienen y a su uso en el tratamiento de trastornos proliferativos celulares. Reivindicación 1: Un compuesto de fórmula (1), en donde: el Anillo A se selecciona de arilo, heteroarilo monocíclico y heteroarilo bicíclico; R¹ se selecciona independientemente de alquilo C₁₋₄, halo hidroxi, alcoxi C₁₋₄, fluoroalquilo C₁₋₃, fluoroalcoxi C₁₋₃, ciano, acetilenilo, NR⁷R⁸, C(O)NR⁹R¹⁰, CH₂R¹¹, N=S(O)Me₂, S(O)Me y SO₂R¹²; b es 0, 1, 2 ó 3; W es N o CR¹³; X es O ó NR¹⁴; Y es CR¹⁵R¹⁶, CR¹⁷R¹⁸CR¹⁹R²⁰, C=O, o C(O)CR²¹R²²; R² es H, ciano, halo, alquilo C₁₋₄, alcoxi C₁₋₄, fluoroalquilo C₁₋₃, NR²³R²⁴, acetilenilo o CH₂OR²⁵; R³ es H, fluoroalquilo C₁₋₃, OR²⁶, NR²⁷R²⁸, CH₂R²⁹, SR³⁰ o C(O)R³¹; R⁴ es H o Me; R⁵ es H o Me; R⁶ es H o CH₂NMe₂; R⁷ es H, alquilo C₁₋₄, C₍O₎ₐₗqᵘⁱₗₒ C₁₋₃ o CO₂-alquilo C₁₋₃; R¹¹ es hidroxi, ciano, heterociclilo, NR³²R³³, C(O)NR³⁴R³⁵ o SO₂-alquilo C₁₋₃; R¹² es alquilo C₁₋₃, fluoroalquilo C₁₋₃ o NR³⁶R³⁷; R¹³ es H, alquilo C₁₋₄, halo, fluoroalquilo C₁₋₃ o alcoxi C₁₋₄; R¹⁵, R¹⁶, R¹⁷ y R¹⁸ se seleccionan independientemente de H y alquilo C₁₋₃; R¹⁹, R²⁰, R²¹ y R²² se seleccionan independientemente de H, alquilo C₁₋₃, y flúor; R²⁶ se selecciona del grupo que consiste en: H; alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃, halo, NR³⁸R³⁹, C(O)NR⁴⁰R⁴¹, SO₂Me, heteroarilo, cicloalquilo C₃₋₇ o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está opcionalmente sustituido además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄, y dicho heterociclilo está opcionalmente sustituido además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R²⁷ se selecciona del grupo que consiste en: H; C(O)R⁴²; alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃ halo, NR⁴³R⁴⁴, C(O)NR⁴⁵R⁴⁶, SO₂Me, heteroarilo, cicloalquilo C₃₋₇, o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄ y dicho heterociclilo está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, CH₂-ciclopropilo, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R²⁸ es H o Me; o R²⁷ y R²⁸ tomados junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico de 4, 5, 6 ó 7 miembros, en el que dicho anillo está opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, NR⁴⁷R⁴⁸, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, CH₂-ciclopropilo, heterociclilo o heteroarilo; R²⁹ se selecciona del grupo que consiste en: H; NR⁴⁹R⁵⁰; alquilo C₁₋₃ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃, halo, NR⁵¹R⁵², C(O)NR⁵³R⁵⁴, SO₂Me, heteroarilo, cicloalquilo C₃₋₇ o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄ y dicho heterociclilo está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, CH₂-ciclopropilo, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R³⁰ se selecciona del grupo que consiste en: alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, alcoxi C₁₋₃, halo, NR⁵⁵R⁵⁶, C(O)NR⁵⁷R⁵⁸, SO₂Me, heteroarilo, cicloalquilo C₃₋₇ o heterociclilo, en el que dicho heteroarilo o cicloalquilo C₃₋₇ está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, ciano, o alcoxi C₁₋₄, y dicho heterociclilo está sustituido opcionalmente además con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; cicloalquilo C₃₋₇ opcionalmente sustituido con alquilo C₁₋₄, hidroxi o halo; heterociclilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, C(O)Me, alcoxi C₁₋₃, fluoroalquilo C₁₋₃, cicloalquilo C₃₋₇, heterociclilo o heteroarilo; y heteroarilo opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo, ciano o alcoxi C₁₋₄; R³¹ es NR⁵⁹R⁶⁰; R⁴² es heteroarilo opcionalmente sustituido o alquilo C₁₋₄ opcionalmente sustituido; R⁴⁹ y R⁵¹ se seleccionan independientemente de H, alquilo C₁₋₄, heterociclilo y heteroarilo; R⁵⁹ y R⁶⁰ se seleccionan independientemente de H y alquilo C₁₋₄; o R⁵⁹ y R⁶⁰ tomados junto con el átomo de nitrógeno al que están unidos forman un anillo heterocíclico de 4, 5 ó 6 miembros, en el que dicho anillo está opcionalmente sustituido con alquilo C₁₋₄, hidroxi, halo o C(O)Me; R⁸, R⁹, R¹⁰, R¹⁴, R²³, R²⁴, R²⁵, R³², R³³, R³⁴, R³⁵, R³⁶, R³⁷, R³⁸, R³⁹, R⁴⁰, R⁴¹, R⁴³, R⁴⁴, R⁴⁵, R⁴⁶, R⁴⁷, R⁴⁸, R⁵⁰, R⁵², R⁵³, R⁵⁴, R⁵⁵, R⁵⁶, R⁵⁷ y R⁵⁸ se seleccionan independientemente de H y alquilo C₁₋₄; o una de sus sales farmacéuticamente aceptables.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762504638P | 2017-05-11 | 2017-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111776A1 true AR111776A1 (es) | 2019-08-21 |
Family
ID=62492577
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180101198A AR111776A1 (es) | 2017-05-11 | 2018-05-08 | Heteroarilos inhibidores de las proteínas ras mutantes de g12c |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20200109153A1 (es) |
| EP (1) | EP3621968A1 (es) |
| JP (1) | JP2020519589A (es) |
| CN (1) | CN110603258A (es) |
| AR (1) | AR111776A1 (es) |
| CA (1) | CA3061650A1 (es) |
| TW (1) | TW201906848A (es) |
| WO (1) | WO2018206539A1 (es) |
Families Citing this family (122)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11202012697QA (en) | 2018-01-19 | 2021-02-25 | Medshine Discovery Inc | Pyridone-pyrimidine derivative acting as krasg12c mutein inhibitor |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| TWI831855B (zh) | 2018-10-26 | 2024-02-11 | 日商大鵬藥品工業股份有限公司 | 新穎吲唑化合物或其鹽 |
| CN113382774A (zh) | 2019-02-12 | 2021-09-10 | 诺华股份有限公司 | 包含tno155和krasg12c抑制剂的药物组合 |
| CA3131156A1 (en) * | 2019-03-05 | 2020-09-10 | Astrazeneca Ab | Fused tricyclic compounds useful as anticancer agents |
| US20220251109A1 (en) * | 2019-04-28 | 2022-08-11 | Genfleet Therapeutics (Shanghai) Inc. | Oxaazaquinazoline-7(8h)-ketone compound, preparation method therefor and pharmaceutical application thereof |
| CN113993860B (zh) * | 2019-06-25 | 2023-08-01 | 正大天晴药业集团股份有限公司 | 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物 |
| CN114040914B (zh) * | 2019-07-01 | 2024-10-22 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| CN112300195B (zh) * | 2019-08-02 | 2021-12-24 | 上海济煜医药科技有限公司 | 四并环类化合物及其制备方法和应用 |
| CN112390818B (zh) * | 2019-08-12 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 取代的杂芳环并二氢嘧啶酮衍生物，其制法与医药上的用途 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN116947885B (zh) * | 2019-09-20 | 2026-01-23 | 上海济煜医药科技股份有限公司 | 稠合吡啶酮类化合物及其制备方法和应用 |
| CN114929706A (zh) * | 2019-09-29 | 2022-08-19 | 百济神州有限公司 | Kras g12c的抑制剂 |
| WO2021063346A1 (zh) * | 2019-09-30 | 2021-04-08 | 上海迪诺医药科技有限公司 | Kras g12c抑制剂及其应用 |
| CA3158793A1 (en) | 2019-10-28 | 2021-05-06 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| CN112745335B (zh) * | 2019-10-30 | 2024-08-30 | 武汉誉祥医药科技有限公司 | 一种三并杂环化合物及其用途 |
| EP4643644A3 (en) | 2019-11-01 | 2025-12-24 | Syngenta Crop Protection AG | Pesticidally active fused bicyclic heteroaromatic compounds |
| CR20220240A (es) | 2019-11-04 | 2022-08-03 | Revolution Medicines Inc | Inhibidores de ras |
| IL320513A (en) | 2019-11-04 | 2025-06-01 | Revolution Medicines Inc | RAS inhibitors |
| US11608346B2 (en) | 2019-11-04 | 2023-03-21 | Revolution Medicines, Inc. | Ras inhibitors |
| CN114980976A (zh) * | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| HUE060684T2 (hu) * | 2019-12-11 | 2023-04-28 | Lilly Co Eli | KRas G12C inhibitorok |
| CN111039845A (zh) * | 2019-12-18 | 2020-04-21 | 大连奇凯医药科技有限公司 | 一种4-氟-7-溴靛红的制备方法 |
| CN114761408B (zh) * | 2019-12-19 | 2023-09-15 | 贝达药业股份有限公司 | Kras g12c抑制剂及其在医药上的应用 |
| GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| KR20220164015A (ko) * | 2020-04-03 | 2022-12-12 | 메드샤인 디스커버리 아이엔씨. | 옥타하이드로피라지노디아자나프티리딘 디온 화합물 |
| TWI799871B (zh) * | 2020-05-27 | 2023-04-21 | 大陸商勁方醫藥科技(上海)有限公司 | 三環并環類化合物，其製法與醫藥上的用途 |
| TW202210633A (zh) | 2020-06-05 | 2022-03-16 | 法商昂席歐公司 | 用於治療癌症之dbait分子與kras抑制劑的組合 |
| EP4168002A1 (en) | 2020-06-18 | 2023-04-26 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to ras inhibitors |
| CN113980032B (zh) * | 2020-07-27 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 稠合四环类衍生物、其制备方法及其在医药上的应用 |
| CN114075219B (zh) * | 2020-08-14 | 2023-11-14 | 江苏恒瑞医药股份有限公司 | 喹啉稠环类衍生物、其制备方法及其在医药上的应用 |
| CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| US11690915B2 (en) | 2020-09-15 | 2023-07-04 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2022066805A1 (en) | 2020-09-23 | 2022-03-31 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| TWI880049B (zh) | 2020-12-04 | 2025-04-11 | 美商美國禮來大藥廠 | Kras g12c抑制劑 |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| CN114685531B (zh) * | 2020-12-25 | 2024-10-22 | 武汉誉祥医药科技有限公司 | 四并环化合物及其药物组合物和应用 |
| CA3210167A1 (en) * | 2021-02-09 | 2022-08-18 | Genentech, Inc. | Tetracyclic oxazepine compounds and uses thereof |
| CN117083280A (zh) * | 2021-03-07 | 2023-11-17 | 北京加科思新药研发有限公司 | Kras g12d抑制剂的稠环衍生物 |
| EP4310091A4 (en) * | 2021-03-17 | 2025-04-16 | Genfleet Therapeutics (Shanghai) Inc. | Pyrimidine-fused cyclic compound, preparation method therefor and use thereof |
| WO2022199587A1 (zh) * | 2021-03-24 | 2022-09-29 | 南京明德新药研发有限公司 | 嘧啶并杂环类化合物及其应用 |
| CN116113632B (zh) * | 2021-03-30 | 2025-08-29 | 浙江海正药业股份有限公司 | 杂环类衍生物、其制备方法及其医药上的用途 |
| WO2022216762A1 (en) * | 2021-04-08 | 2022-10-13 | Genentech, Inc. | Oxazepine compounds and uses thereof in the treatment of cancer |
| CR20230558A (es) | 2021-05-05 | 2024-01-24 | Revolution Medicines Inc | Inhibidores de ras para el tratamiento del cáncer |
| CN118561952A (zh) | 2021-05-05 | 2024-08-30 | 锐新医药公司 | Ras抑制剂 |
| US20240293558A1 (en) | 2021-06-16 | 2024-09-05 | Erasca, Inc. | Kras inhibitor conjugates |
| KR20240024903A (ko) | 2021-06-21 | 2024-02-26 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 융합된 사환식 화합물, 이에 대한 제조 방법 및 의학에서 이의 적용 |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途 |
| CR20240002A (es) | 2021-06-24 | 2024-02-13 | Syngenta Crop Protection Ag | Derivados de 2-[3-[1 [(quinazolin-4-il)amino]etil]pirazin-2-il]tiazol-5-carbonitrilo y compuestos similares como plaguicidas |
| CN115557974A (zh) * | 2021-07-02 | 2023-01-03 | 上海迪诺医药科技有限公司 | Kras g12d抑制剂及其应用 |
| WO2023001123A1 (zh) * | 2021-07-19 | 2023-01-26 | 上海艾力斯医药科技股份有限公司 | 新型吡啶并嘧啶衍生物 |
| JP2024525993A (ja) * | 2021-07-23 | 2024-07-12 | スゾウ、ザンロン、ファーマ、リミテッド | Ｋｒａｓ ｇ１２ｄ阻害剤およびその使用 |
| TW202315626A (zh) * | 2021-08-31 | 2023-04-16 | 大陸商勁方醫藥科技(上海)有限公司 | 嘧啶并環類化合物及其製法和用途 |
| IL309086A (en) | 2021-09-01 | 2024-02-01 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| EP4389751A1 (en) | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| AU2022349569A1 (en) | 2021-09-22 | 2024-04-04 | Sichuan Huiyu Pharmaceutical Co., Ltd. | Pyridine derivative and use thereof |
| WO2023046135A1 (en) * | 2021-09-27 | 2023-03-30 | Jacobio Pharmaceuticals Co., Ltd. | Polycyclic fused ring derivatives and use thereof |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| TW202322819A (zh) * | 2021-10-22 | 2023-06-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 含氮的四環化合物、其製備方法及其在醫藥上的應用 |
| CN118176198A (zh) * | 2021-11-01 | 2024-06-11 | 江苏恒瑞医药股份有限公司 | 含氮的四环化合物、其制备方法及其在医药上的应用 |
| WO2023103906A1 (zh) * | 2021-12-07 | 2023-06-15 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| US20250282782A1 (en) | 2021-12-17 | 2025-09-11 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| CA3245251A1 (en) | 2022-03-04 | 2023-09-07 | Eli Lilly And Company | TREATMENT METHOD COMPRISING KRAS G12C INHIBITORS AND 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 |
| KR20240163107A (ko) | 2022-03-11 | 2024-11-18 | 컴쿼트 바이오사이언시즈 인크. | 헤테로환 화합물 및 이의 용도 |
| US20250249019A1 (en) | 2022-04-08 | 2025-08-07 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and aurora a inhibitors |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| JP7735594B2 (ja) * | 2022-05-19 | 2025-09-08 | ジェネンテック， インコーポレイテッド | アザ四環式オキサゼピン化合物及びその使用 |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| EP4543873A1 (en) | 2022-06-21 | 2025-04-30 | Syngenta Crop Protection AG | Pesticidally active fused bicyclic heteroaromatic compounds |
| CR20240556A (es) * | 2022-07-05 | 2025-01-29 | Pfizer | Compuestos de pirido[4,3-d]pirimidina |
| AU2023314335A1 (en) * | 2022-07-29 | 2025-02-27 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Pharmaceutical composition comprising kras g12d inhibitor |
| JP2025525946A (ja) | 2022-08-05 | 2025-08-07 | カムクワット バイオサイエンシーズ インコーポレイテッド | 複素環式化合物およびその使用 |
| TW202416982A (zh) * | 2022-08-11 | 2024-05-01 | 英屬開曼群島商百濟神州有限公司 | 雜環化合物、其組成物及用其進行治療之方法 |
| CN119677754A (zh) * | 2022-08-11 | 2025-03-21 | 百济神州(苏州)生物科技有限公司 | 杂环化合物、其组合物及用其进行治疗的方法 |
| CN119654327A (zh) * | 2022-08-11 | 2025-03-18 | 百济神州(苏州)生物科技有限公司 | 杂环化合物、其组合物及其治疗方法 |
| WO2024041621A1 (en) * | 2022-08-25 | 2024-02-29 | Jacobio Pharmaceuticals Co., Ltd. | K-ras mutant protein inhibitors |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| WO2024051721A1 (en) * | 2022-09-07 | 2024-03-14 | Nikang Therapeutics, Inc. | Tetracyclic derivatives as kras inhibitors |
| WO2024138486A1 (en) * | 2022-12-29 | 2024-07-04 | Nikang Therapeutics, Inc. | Tetracyclic derivatives as kras inhibitors |
| CN120077050A (zh) * | 2022-10-18 | 2025-05-30 | 伊迪恩斯股份有限公司 | 新颖三杂环化合物 |
| AU2023377064A1 (en) | 2022-11-09 | 2025-05-22 | Revolution Medicines, Inc. | Compounds, complexes, and methods for their preparation and of their use |
| CN115583937B (zh) * | 2022-11-21 | 2023-05-02 | 北京志道生物科技有限公司 | 以吲哚或氮杂吲哚为母核的kras抑制剂及其制备方法 |
| WO2024110554A1 (en) | 2022-11-23 | 2024-05-30 | Syngenta Crop Protection Ag | N-[(1 -[2-[6-(pyridazin-3-yl]-1,2,4-triazol-3-yl]ethyl]-quinazolin-4-amine and n-[1-[3-(6-(pyridazin-3-yl)pyrazin-2-yl]ethyl]-8-quinazolin-4-amine derivatives as pesticides |
| WO2024120419A1 (en) * | 2022-12-06 | 2024-06-13 | Zai Lab (Shanghai) Co., Ltd. | Fused tetracyclic compounds as kras g12d modulators and uses thereof |
| WO2024120433A1 (en) * | 2022-12-07 | 2024-06-13 | Jacobio Pharmaceuticals Co., Ltd. | Fused cyclic compounds and use thereof |
| WO2024149214A1 (en) * | 2023-01-10 | 2024-07-18 | Nikang Therapeutics, Inc. | Bifunctional compounds for degrading kras-12d via ubiquitin proteasome pathway |
| CN120548318A (zh) * | 2023-01-18 | 2025-08-26 | 苏州赞荣医药科技有限公司 | Kras g12d抑制剂和其用途 |
| WO2024197503A1 (en) * | 2023-03-27 | 2024-10-03 | Nikang Therapeutics , Inc. | Tricyclic derivatives as kras inhibitors |
| CR20250458A (es) | 2023-03-30 | 2025-11-21 | Revolution Medicines Inc | Composiciones para inducir la hidrólisis de ras gtp y sus usos |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| KR20260005904A (ko) | 2023-04-07 | 2026-01-12 | 레볼루션 메디슨즈, 인크. | 매크로사이클릭 ras 억제제 |
| 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 |
| AU2024251341A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| WO2024217545A1 (zh) * | 2023-04-21 | 2024-10-24 | 江苏恒瑞医药股份有限公司 | 一种含氮四环化合物的结晶形式及其制备方法 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024230734A1 (en) * | 2023-05-08 | 2024-11-14 | Jacobio Pharmaceuticals Co., Ltd. | K-ras inhibitors and use thereof |
| WO2024243186A2 (en) * | 2023-05-22 | 2024-11-28 | Board Of Regents, The University Of Texas System | Heterocyclic compounds as nras inhibitors |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CN121219016A (zh) | 2023-06-02 | 2025-12-26 | 第一三共株式会社 | 抗-her3抗体-药物缀合物和rasg12c抑制剂的组合 |
| TW202502779A (zh) | 2023-06-30 | 2025-01-16 | 美商金橘生物科技公司 | 取代的雜芳族胺及其用途 |
| WO2025022007A1 (en) | 2023-07-27 | 2025-01-30 | Syngenta Crop Protection Ag | Pesticidally active quinazoline compounds |
| WO2025022008A1 (en) | 2023-07-27 | 2025-01-30 | Syngenta Crop Protection Ag | Pesticidally active quinazoline compounds |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| US12466840B2 (en) | 2023-10-20 | 2025-11-11 | Merck Sharp & Dohme Llc | Small molecule inhibitors of KRAS proteins |
| WO2025132349A1 (en) | 2023-12-19 | 2025-06-26 | Syngenta Crop Protection Ag | Pesticidally active quinazoline compounds |
| WO2025132754A1 (en) | 2023-12-21 | 2025-06-26 | Syngenta Crop Protection Ag | Pesticidally active quinazoline compounds |
| WO2025171055A1 (en) | 2024-02-06 | 2025-08-14 | Kumquat Biosciences Inc. | Heterocyclic conjugates and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025230971A1 (en) | 2024-04-30 | 2025-11-06 | Kumquat Biosciences Inc. | Macrocyclic heterocycles as anticancer agents |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005051392A1 (en) * | 2003-11-20 | 2005-06-09 | Children's Hospital Medical Center | Gtpase inhibitors and methods of use |
| WO2011121350A1 (en) * | 2010-04-01 | 2011-10-06 | Astrazeneca Ab | 4 -amino -7,8- dihydropyrimido [5, 4 - f] [1, 4] oxazepin- 5 ( 6h) - one based dgat1 inhibitors |
| CA2903176A1 (en) * | 2013-03-14 | 2014-09-18 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| US9862701B2 (en) * | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10730867B2 (en) * | 2015-09-28 | 2020-08-04 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
-
2018
- 2018-05-08 CN CN201880030263.3A patent/CN110603258A/zh active Pending
- 2018-05-08 TW TW107115513A patent/TW201906848A/zh unknown
- 2018-05-08 US US16/611,538 patent/US20200109153A1/en not_active Abandoned
- 2018-05-08 JP JP2019561278A patent/JP2020519589A/ja not_active Withdrawn
- 2018-05-08 EP EP18728518.4A patent/EP3621968A1/en not_active Withdrawn
- 2018-05-08 CA CA3061650A patent/CA3061650A1/en not_active Abandoned
- 2018-05-08 AR ARP180101198A patent/AR111776A1/es unknown
- 2018-05-08 WO PCT/EP2018/061787 patent/WO2018206539A1/en not_active Ceased
-
2021
- 2021-10-05 US US17/449,974 patent/US20220127281A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP3621968A1 (en) | 2020-03-18 |
| US20220127281A1 (en) | 2022-04-28 |
| CA3061650A1 (en) | 2018-11-15 |
| WO2018206539A1 (en) | 2018-11-15 |
| JP2020519589A (ja) | 2020-07-02 |
| US20200109153A1 (en) | 2020-04-09 |
| TW201906848A (zh) | 2019-02-16 |
| CN110603258A (zh) | 2019-12-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR111776A1 (es) | Heteroarilos inhibidores de las proteínas ras mutantes de g12c | |
| AR113905A1 (es) | Feniléteres herbicidas | |
| AR114083A2 (es) | AGENTES INDUCTORES DE APOPTOSIS CON SELECTIVIDAD POR Bcl-2 PARA EL TRATAMIENTO DE CÁNCER Y ENFERMEDADES INMUNES | |
| AR088989A1 (es) | Derivados biciclicos de dihidroisoquinolin-1-ona | |
| AR087747A1 (es) | Derivados de quinolona utiles como agentes antibacterianos y composiciones farmaceuticas que los contienen | |
| AR109905A1 (es) | Pirrolidinas sustituidas como moduladores de cftr | |
| AR110227A2 (es) | Derivados de pirazol con acción sobre fgf | |
| AR098492A1 (es) | Derivados de purina | |
| AR091464A1 (es) | Compuestos biciclicos de tiofenilamida | |
| AR097633A1 (es) | Pesticidas de azol bicíclico sustituido con heterociclos | |
| AR091261A1 (es) | Derivados de alcoholes 1-fenil-2-piridinilalquilicos como inhibidores de la fosfodiesterasa | |
| AR124443A1 (es) | Compuestos y composición para el tratamiento de condiciones asociadas con cgas | |
| AR088014A1 (es) | Derivados de alcoholes 1-fenil-2-piridinil alquilicos como inhibidores de la fosfodiesterasa | |
| AR094684A1 (es) | Triterpenoides de c-19 modificados, con actividad inhibidora de la maduración del vih | |
| AR111241A1 (es) | Compuestos de imidazo-piperidina fusionada como inhibidores de jak | |
| AR087984A1 (es) | Derivados biciclicos de dihidroquinolina-2-ona | |
| AR100886A1 (es) | 3-amino-1,5,6,7-tetrahidro-4h-indol-4-onas | |
| AR099936A1 (es) | Heterociclos condensados sustituidos como moduladores de gpr119 para el tratamiento de la diabetes, obesidad, dislipidemia y trastornos relacionados | |
| AR109304A1 (es) | Compuesto de oxadiazol y su uso | |
| AR113886A1 (es) | Derivados de indol macrocíclicos | |
| AR093796A1 (es) | Derivados del alcohol 1-fenil-2-piridinil alquilico como inhibidores de la fosfodiesterasa | |
| AR105360A1 (es) | Hidrazidas de ácido carboxílico heteroarilo sustituidas o sus sales y su uso para aumentar la tolerancia al estrés en plantas | |
| AR097950A1 (es) | N-hetaril(tio)carbonil-2-(benzocicloalquen-1-il)ciclaminas | |
| AR113969A1 (es) | Tiofeniluracilos sustituidos así como sus sales y su uso como principios activos herbicidas | |
| AR095047A1 (es) | Acoplamiento electroquímico de un fenol a un naftol |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |