PH12022550469A1 - Kras g12d inhibitors - Google Patents
Kras g12d inhibitorsInfo
- Publication number
- PH12022550469A1 PH12022550469A1 PH1/2022/550469A PH12022550469A PH12022550469A1 PH 12022550469 A1 PH12022550469 A1 PH 12022550469A1 PH 12022550469 A PH12022550469 A PH 12022550469A PH 12022550469 A1 PH12022550469 A1 PH 12022550469A1
- Authority
- PH
- Philippines
- Prior art keywords
- kras
- inhibitors
- compounds
- inhibit
- relates
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 101150105104 Kras gene Proteins 0.000 abstract 2
- 102200006539 rs121913529 Human genes 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 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
-
- 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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962893604P | 2019-08-29 | 2019-08-29 | |
| US202063052840P | 2020-07-16 | 2020-07-16 | |
| US202063058188P | 2020-07-29 | 2020-07-29 | |
| PCT/US2020/048194 WO2021041671A1 (en) | 2019-08-29 | 2020-08-27 | Kras g12d inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PH12022550469A1 true PH12022550469A1 (en) | 2023-02-27 |
Family
ID=74683570
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH1/2022/550469A PH12022550469A1 (en) | 2019-08-29 | 2020-08-27 | Kras g12d inhibitors |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US11453683B1 (enExample) |
| EP (1) | EP4021444A4 (enExample) |
| JP (2) | JP7622043B2 (enExample) |
| KR (1) | KR20220071193A (enExample) |
| CN (1) | CN114615981B (enExample) |
| AU (1) | AU2020337938B2 (enExample) |
| BR (1) | BR112022003543A2 (enExample) |
| CA (1) | CA3148745A1 (enExample) |
| CL (1) | CL2022000447A1 (enExample) |
| CO (1) | CO2022003782A2 (enExample) |
| IL (1) | IL290845A (enExample) |
| MX (1) | MX2022002465A (enExample) |
| PH (1) | PH12022550469A1 (enExample) |
| TW (2) | TWI874443B (enExample) |
| WO (1) | WO2021041671A1 (enExample) |
| ZA (1) | ZA202202362B (enExample) |
Families Citing this family (228)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| US12336995B2 (en) | 2018-09-10 | 2025-06-24 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020055760A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| HRP20250059T1 (hr) | 2018-09-10 | 2025-03-28 | Mirati Therapeutics, Inc. | Kombinirane terapije |
| 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 |
| JP2022509724A (ja) | 2018-12-05 | 2022-01-24 | 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 |
| 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 |
| 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 |
| AU2020356455A1 (en) | 2019-09-24 | 2022-04-14 | Mirati Therapeutics, Inc. | Combination therapies |
| PE20221253A1 (es) | 2019-10-28 | 2022-08-16 | Merck Sharp & Dohme | Inhibidores de pequenas moleculas de mutante g12c de kras |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| CN115135315B (zh) | 2019-12-20 | 2024-11-26 | 米拉蒂治疗股份有限公司 | Sos1抑制剂 |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| US20230279025A1 (en) * | 2020-07-16 | 2023-09-07 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| US20230339976A1 (en) | 2020-08-04 | 2023-10-26 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| CN115968286A (zh) * | 2020-08-26 | 2023-04-14 | 益方生物科技(上海)股份有限公司 | 杂芳基化合物,其制备方法和用途 |
| CN116368130A (zh) | 2020-08-28 | 2023-06-30 | 金橘生物科技公司 | 杂环化合物及其用途 |
| IL301062A (en) | 2020-09-03 | 2023-05-01 | Revolution Medicines Inc | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| JP2023540809A (ja) | 2020-09-11 | 2023-09-26 | 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阻害剤の結晶形態 |
| US20230081426A1 (en) * | 2020-09-18 | 2023-03-16 | Plexxikon Inc. | Compounds and methods for kras modulation and indications therefor |
| CN116323624A (zh) * | 2020-09-30 | 2023-06-23 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| WO2022098625A1 (en) * | 2020-11-03 | 2022-05-12 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| KR20230142465A (ko) | 2020-12-15 | 2023-10-11 | 미라티 테라퓨틱스, 인크. | 아자퀴나졸린 범-KRas 저해제 |
| WO2022133038A1 (en) | 2020-12-16 | 2022-06-23 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| EP4269405A4 (en) * | 2020-12-22 | 2024-07-24 | Shanghai Kechow Pharma, Inc. | Preparation and application method of heterocyclic compound as kras inhibitor |
| WO2022135390A1 (zh) * | 2020-12-25 | 2022-06-30 | 四川海思科制药有限公司 | 己酮糖激酶抑制剂及其用途 |
| CN116848112A (zh) * | 2021-02-09 | 2023-10-03 | 南京明德新药研发有限公司 | 吡啶[4,3-d]嘧啶类化合物 |
| PE20240235A1 (es) | 2021-02-15 | 2024-02-16 | Astellas Pharma Inc | Compuesto de quinazolina para inducir la degradacion de la proteina kras mutante g12d |
| WO2022173033A1 (ja) | 2021-02-15 | 2022-08-18 | アステラス製薬株式会社 | 4-アミノキナゾリン化合物 |
| WO2022184178A1 (en) * | 2021-03-05 | 2022-09-09 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| WO2022188729A1 (en) * | 2021-03-07 | 2022-09-15 | Jacobio Pharmaceuticals Co., Ltd. | Fused ring derivatives useful as kras g12d inhibitors |
| WO2022192332A1 (en) * | 2021-03-10 | 2022-09-15 | Beta Pharma, Inc. | Pyridopyrimidine derivatives as kras inhibitors |
| CN115073451A (zh) * | 2021-03-15 | 2022-09-20 | 药雅科技(上海)有限公司 | Krasg12d突变蛋白抑制剂的制备及其应用 |
| TWI810803B (zh) * | 2021-03-15 | 2023-08-01 | 大陸商藥雅科技(上海)有限公司 | 突變蛋白抑制劑的製備及其應用 |
| CN116964058A (zh) * | 2021-03-15 | 2023-10-27 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| CN115160309B (zh) * | 2021-04-07 | 2024-04-09 | 药雅科技(上海)有限公司 | Krasg12c突变蛋白杂环类抑制剂的制备及其应用 |
| CN115490689B (zh) * | 2021-06-17 | 2024-04-09 | 药雅科技(上海)有限公司 | 不可逆krasg12c抑制剂的制备及其应用 |
| CN115073450A (zh) * | 2021-03-15 | 2022-09-20 | 药雅科技(上海)有限公司 | Krasg12c突变蛋白抑制剂的制备及其应用 |
| CN115260214A (zh) * | 2021-04-29 | 2022-11-01 | 药雅科技(上海)有限公司 | 稠环类krasg12d突变蛋白抑制剂的制备及其应用 |
| CN115304603B (zh) * | 2021-05-07 | 2024-04-09 | 药雅科技(上海)有限公司 | 喹唑啉类抑制剂的制备及其应用 |
| WO2022194191A1 (en) * | 2021-03-16 | 2022-09-22 | Guangdong Newopp Biopharmaceuticals Co., Ltd. | Heterocyclic compounds as inhibitors of kras g12d |
| KR20230157463A (ko) * | 2021-03-17 | 2023-11-16 | 젠플리트 테라퓨틱스 (상하이) 아이엔씨. | 피리미딘-융합된 환형 화합물, 이의 제조 방법 및 이의 용도 |
| CN115109078A (zh) * | 2021-03-22 | 2022-09-27 | 苏州泽璟生物制药股份有限公司 | 嘧啶并吡啶类抑制剂及其制备方法和应用 |
| CN115124524A (zh) * | 2021-03-26 | 2022-09-30 | 浙江海正药业股份有限公司 | 三环类衍生物及其制备方法和用途 |
| WO2022206724A1 (zh) * | 2021-03-30 | 2022-10-06 | 浙江海正药业股份有限公司 | 杂环类衍生物及其制备方法和用途 |
| CN117659051A (zh) * | 2021-03-30 | 2024-03-08 | 上海德琪医药科技有限公司 | Kras g12d蛋白抑制剂和其用途 |
| US20250255868A1 (en) * | 2021-04-09 | 2025-08-14 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic compound acting as kras g12d inhibitor |
| WO2022217042A1 (en) * | 2021-04-09 | 2022-10-13 | Ikena Oncology, Inc. | Naphthyl-substituted quinoline-4(1h)-ones and related compounds and their use in treating medical conditions |
| CN115197245A (zh) * | 2021-04-09 | 2022-10-18 | 上海拓界生物医药科技有限公司 | 一种Kras抑制剂及其制备方法 |
| WO2022221386A1 (en) * | 2021-04-14 | 2022-10-20 | Erasca, Inc. | Selective kras inhibitors |
| US20240239788A1 (en) * | 2021-04-16 | 2024-07-18 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras g12d mutant |
| CN116157401B (zh) * | 2021-04-28 | 2025-06-20 | 浙江海正药业股份有限公司 | 杂环类衍生物及其制备方法和用途 |
| MX2023012725A (es) * | 2021-04-29 | 2024-09-23 | Amgen Inc | Compuestos de 2-aminobenzotiazol y metodos de uso de los mismos. |
| WO2022228568A1 (zh) * | 2021-04-30 | 2022-11-03 | 劲方医药科技(上海)有限公司 | 吡啶或嘧啶并环类化合物,其制法与医药上的用途 |
| WO2022228543A1 (zh) * | 2021-04-30 | 2022-11-03 | 江苏恒瑞医药股份有限公司 | 桥环类化合物、其制备方法及其在医药上的应用 |
| WO2022228576A1 (zh) * | 2021-04-30 | 2022-11-03 | 上海医药集团股份有限公司 | 一种靶向蛋白调节剂的化合物及其应用 |
| EP4334324A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2022236578A1 (en) * | 2021-05-10 | 2022-11-17 | Nikang Therapeutics, Inc. | Exocyclic amino quinazoline derivatives as kras inhibitors |
| WO2022246092A1 (en) * | 2021-05-21 | 2022-11-24 | Blossomhill Therapeutics, Inc. | Macrocyclic compounds for treating disease |
| CN117813306A (zh) * | 2021-05-22 | 2024-04-02 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物,及其制备和治疗用途 |
| KR20240024848A (ko) | 2021-05-24 | 2024-02-26 | 상하이 잉리 파마슈티컬 컴퍼니 리미티드 | 질소 함유 헤테로고리 화합물, 이의 제조 방법 및 이의 응용 |
| WO2022247757A1 (zh) * | 2021-05-26 | 2022-12-01 | 南京明德新药研发有限公司 | 氟取代的嘧啶并吡啶类化合物及其应用 |
| AU2022279653A1 (en) | 2021-05-28 | 2023-11-09 | Redx Pharma Plc. | Pyrido[4,3-d]pyrimidine compounds capable of inhibiting kras mutant proteins |
| CN117500799A (zh) | 2021-06-09 | 2024-02-02 | 伊莱利利公司 | 作为kras g12d抑制剂的取代的稠合吖嗪 |
| KR20240021197A (ko) | 2021-06-10 | 2024-02-16 | 레드엑스 파마 피엘씨 | Ras 억제제로서 유용한 퀴나졸린 유도체 |
| WO2022262686A1 (en) * | 2021-06-13 | 2022-12-22 | Jingrui Biopharma Co., Ltd. | Kras g12d inhibitors |
| WO2022266167A1 (en) * | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Amide and urea-containing tricyclic kras inhibitors |
| WO2022266069A1 (en) * | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Tricyclic kras g12d inhibitors |
| CN116057059B (zh) * | 2021-06-18 | 2024-03-08 | 南京燧坤智能科技有限公司 | 用作kras g12d抑制剂的氘代化合物 |
| US20240327434A1 (en) * | 2021-06-21 | 2024-10-03 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Fused tetracyclic compound, preparation method therefor and application thereof in medicine |
| WO2022271823A1 (en) * | 2021-06-23 | 2022-12-29 | Newave Pharmaceutical Inc. | Mutant kras modulators and uses thereof |
| WO2023274324A1 (zh) | 2021-06-30 | 2023-01-05 | 上海艾力斯医药科技股份有限公司 | 一种含氮杂环化合物、其制备方法、中间体及应用 |
| EP4365176A4 (en) * | 2021-07-02 | 2025-06-25 | Shanghai de Novo Pharmatech Co., Ltd. | KRAS G12D INHIBITOR AND ITS USE |
| CN117460737A (zh) * | 2021-07-05 | 2024-01-26 | 四川科伦博泰生物医药股份有限公司 | 杂芳环化合物、其制备方法及用途 |
| WO2023280280A1 (zh) * | 2021-07-07 | 2023-01-12 | 微境生物医药科技(上海)有限公司 | 作为KRas G12D抑制剂的稠环化合物 |
| CN117980310A (zh) * | 2021-07-14 | 2024-05-03 | 尼坎治疗公司 | 作为kras抑制剂的亚烷基衍生物 |
| WO2023284881A1 (en) * | 2021-07-16 | 2023-01-19 | Silexon Ai Technology Co., Ltd. | Heterocyclic compounds useful as kras g12d inhibitors |
| WO2023283933A1 (en) * | 2021-07-16 | 2023-01-19 | Silexon Biotech Co., Ltd. | Compounds useful as kras g12d inhibitors |
| CN117157292A (zh) * | 2021-07-16 | 2023-12-01 | 苏州赞荣医药科技有限公司 | Kras g12d抑制剂和其用途 |
| CN117242079A (zh) * | 2021-07-23 | 2023-12-15 | 苏州赞荣医药科技有限公司 | Kras g12d抑制剂和其用途 |
| EP4384522A1 (en) * | 2021-08-10 | 2024-06-19 | Erasca, Inc. | Selective kras inhibitors |
| EP4384160A4 (en) * | 2021-08-10 | 2025-10-29 | Amgen Inc | HETEROCYCLIC COMPOUNDS AND METHODS OF USE |
| JP2024532735A (ja) * | 2021-08-10 | 2024-09-10 | アムジエン・インコーポレーテツド | 複素環式化合物及び使用方法 |
| WO2023020347A1 (zh) * | 2021-08-16 | 2023-02-23 | 华润医药研究院(深圳)有限公司 | 嘧啶并吡啶类化合物及其制备方法和医药用途 |
| WO2023020521A1 (en) * | 2021-08-18 | 2023-02-23 | Jacobio Pharmaceuticals Co., Ltd. | Pyridine fused pyrimidine derivatives and use thereof |
| US20250019377A1 (en) * | 2021-08-18 | 2025-01-16 | Jacobio Pharmaceuticals Co., Ltd | 1, 4-oxazepane derivatives and uses thereof |
| WO2023020523A1 (en) * | 2021-08-18 | 2023-02-23 | Jacobio Pharmaceuticals Co., Ltd. | Bicyclic derivatives and use thereof |
| CN116323625A (zh) * | 2021-08-25 | 2023-06-23 | 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 |
| WO2023030495A1 (en) * | 2021-09-03 | 2023-03-09 | Ascentage Pharma (Suzhou) Co., Ltd. | Kras inhibitors |
| CN115785124B (zh) * | 2021-09-10 | 2024-11-08 | 润佳(苏州)医药科技有限公司 | Kras g12d抑制剂及其用途 |
| CN116284055B (zh) * | 2021-09-10 | 2025-09-23 | 润佳(苏州)医药科技有限公司 | 一种kras抑制剂及其用途 |
| WO2023039240A1 (en) | 2021-09-13 | 2023-03-16 | Biomea Fusion, Inc. | IRREVERSIBLE INHIBITORS OF KRas |
| CN116143805B (zh) * | 2021-09-17 | 2025-10-17 | 上海凌达生物医药有限公司 | 一类含氮杂环联芳基类化合物、制备方法和用途 |
| CN118043330A (zh) * | 2021-09-29 | 2024-05-14 | 海南先声再明医药股份有限公司 | Kras g12d抑制剂化合物及其制备方法和应用 |
| AU2022359880A1 (en) * | 2021-10-05 | 2024-04-11 | Mirati Therapeutics, Inc. | COMBINATION THERAPIES OF KRAS G12D INHIBITORS WITH Pan ErbB FAMILY INHIBITORS |
| KR20240073112A (ko) * | 2021-10-05 | 2024-05-24 | 미라티 테라퓨틱스, 인크. | PI3Ka 억제제와 KRAS G12D 억제제의 조합 및 관련된 치료 방법 |
| CN118354794A (zh) * | 2021-10-05 | 2024-07-16 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂与伊立替康的组合及相关治疗方法 |
| CN118401254A (zh) * | 2021-10-05 | 2024-07-26 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂与shp-2抑制剂的组合疗法 |
| CA3233570A1 (en) * | 2021-10-05 | 2023-04-13 | Jill HALLIN | Combination therapies of kras g12d inhibitors with sos1 inhibitors |
| WO2023056951A1 (zh) * | 2021-10-08 | 2023-04-13 | 杭州德睿智药科技有限公司 | 芳基取代并杂环化合物 |
| WO2023061294A1 (zh) * | 2021-10-13 | 2023-04-20 | 再鼎医药(上海)有限公司 | 含氮杂环类衍生物调节剂、其制备方法及应用 |
| EP4417606A4 (en) * | 2021-10-15 | 2025-10-22 | Sunshine Lake Pharma Co Ltd | NOVEL PYRIMIDOPYRIDINE COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF |
| WO2023072188A1 (zh) * | 2021-10-29 | 2023-05-04 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| WO2023077441A1 (en) * | 2021-11-05 | 2023-05-11 | Ranok Therapeutics (Hangzhou) Co. Ltd. | Methods and compositions for targeted protein degradation |
| CN118302162A (zh) * | 2021-11-24 | 2024-07-05 | 默沙东有限责任公司 | Kras突变蛋白的小分子抑制剂 |
| AU2022399372A1 (en) * | 2021-11-30 | 2024-05-16 | Beta Pharma, Inc. | Fused pyrimidine derivatives as kras oncoprotein inhibitors |
| WO2023098426A1 (zh) * | 2021-12-02 | 2023-06-08 | 上海和誉生物医药科技有限公司 | 一种7-(萘-1-基)吡啶并[4,3-d]嘧啶衍生物及其制备和应用 |
| WO2023098425A1 (zh) | 2021-12-02 | 2023-06-08 | 上海和誉生物医药科技有限公司 | 一种kras抑制剂及其制备和在药学上的应用 |
| CN116217591A (zh) * | 2021-12-02 | 2023-06-06 | 思路迪生物医药(上海)有限公司 | 一类作为kras g12d突变抑制剂的吡啶并嘧啶类衍生物 |
| 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 |
| CN116253748A (zh) * | 2021-12-09 | 2023-06-13 | 苏州浦合医药科技有限公司 | 取代的双环杂芳基化合物作为kras g12d抑制剂 |
| WO2023122154A1 (en) * | 2021-12-21 | 2023-06-29 | Bridgene Biosciences, Inc. | Inhibitors of ras oncoproteins |
| CN116332959A (zh) * | 2021-12-24 | 2023-06-27 | 苏州泽璟生物制药股份有限公司 | Krasg12d蛋白水解调节剂及其制备方法和应用 |
| WO2023119677A1 (en) * | 2021-12-24 | 2023-06-29 | Astellas Pharma Inc. | Pharmaceutical composition comprising a quinazoline compound |
| WO2023125989A1 (zh) * | 2021-12-31 | 2023-07-06 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| CN118434747A (zh) * | 2022-01-11 | 2024-08-02 | 上海艾力斯医药科技股份有限公司 | 一种含氮杂环化合物、其制备方法、中间体及应用 |
| WO2023137223A1 (en) * | 2022-01-17 | 2023-07-20 | Newave Pharmaceutical Inc. | Pan-kras inhibitors and uses thereof |
| KR20240136407A (ko) | 2022-01-21 | 2024-09-13 | 유시노바 파마슈티컬스 리미티드 | 벤조피리미딘 화합물 및 이의 용도 |
| CN118556063A (zh) * | 2022-01-21 | 2024-08-27 | 上海湃隆生物科技有限公司 | 杂环类化合物、药物组合物及其应用 |
| WO2023138524A1 (zh) * | 2022-01-24 | 2023-07-27 | 贝达药业股份有限公司 | Kras g12d降解剂及其在医药上的应用 |
| WO2023143312A1 (zh) * | 2022-01-28 | 2023-08-03 | 上海艾力斯医药科技股份有限公司 | 一种含氮杂环化合物、其制备方法及应用 |
| JP2025504041A (ja) | 2022-01-30 | 2025-02-06 | シャンハイ ファーマシューティカルズ ホールディング カンパニー,リミティド | キノリン系化合物及びその使用 |
| CA3243798A1 (en) | 2022-02-09 | 2023-08-17 | Quanta Therapeutics, Inc. | Kras Modulators and Their Uses |
| EP4476221A1 (en) | 2022-02-10 | 2024-12-18 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
| WO2023151621A1 (zh) * | 2022-02-11 | 2023-08-17 | 泰励生物科技(上海)有限公司 | 具有抗kras突变肿瘤活性的化合物 |
| WO2023173014A1 (en) * | 2022-03-09 | 2023-09-14 | Blossomhill Therapeutics, Inc. | Kras inhibitors and their use |
| CN116891514A (zh) * | 2022-04-06 | 2023-10-17 | 润佳(苏州)医药科技有限公司 | 一种双官能化合物及其用途 |
| AR128761A1 (es) | 2022-03-11 | 2024-06-12 | Astellas Pharma Inc | Compuesto heterocíclico para inducir la degradación de la proteína kras mutante en g12d |
| CA3244383A1 (en) | 2022-03-11 | 2023-09-14 | Kumquat Biosciences Inc. | HETEROCYCLIC COMPOUNDS AND RELATED USES |
| CN119317628A (zh) * | 2022-03-22 | 2025-01-14 | 苏州泽璟生物制药股份有限公司 | 取代桥环类抑制剂及其制备方法和应用 |
| MX2024011631A (es) | 2022-03-25 | 2024-09-30 | Lilly Co Eli | Inhibidores de kras. |
| US20250177406A1 (en) | 2022-03-31 | 2025-06-05 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumors |
| CN116891488B (zh) * | 2022-04-11 | 2025-12-12 | 成都海博为药业有限公司 | 稠环化合物、包含其的药物组合物及应用 |
| WO2023198078A1 (zh) * | 2022-04-11 | 2023-10-19 | 杭州英创医药科技有限公司 | 作为kras g12d抑制剂的多环化合物 |
| WO2023198191A1 (zh) * | 2022-04-15 | 2023-10-19 | 杭州多域生物技术有限公司 | 一种六元并六元化合物、制备方法、药物组合物和应用 |
| US20230374036A1 (en) | 2022-04-21 | 2023-11-23 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2023212549A1 (en) * | 2022-04-26 | 2023-11-02 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| EP4514809A1 (en) * | 2022-04-26 | 2025-03-05 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| KR20250019626A (ko) | 2022-05-06 | 2025-02-10 | 피에이큐 테라퓨틱스 인코포레이티드 | Kras g12d 단백질분해 표적화 키메라 |
| WO2023213269A1 (en) * | 2022-05-06 | 2023-11-09 | Zai Lab (Shanghai) Co., Ltd. | Amide-substituted heterocyclic compounds as kras g12d modulators and uses thereof |
| US20230365595A1 (en) * | 2022-05-13 | 2023-11-16 | Ranok Therapeutics (Hangzhou) Co. Ltd. | Inhibitors of kras(g12d) |
| 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 |
| CA3257281A1 (en) | 2022-05-25 | 2023-11-30 | Quanta Therapeutics, Inc. | PYRIMIDINE-BASED MODULATORS AND THEIR USES |
| CN114907387B (zh) * | 2022-05-26 | 2023-11-10 | 中山大学 | 嘧啶并吡咯类kras抑制剂及其制备方法与应用 |
| JP2025519584A (ja) | 2022-06-10 | 2025-06-26 | ブリストル-マイヤーズ スクイブ カンパニー | Kras阻害剤としてのピリド[4,3-d]ピリミジン誘導体 |
| US20250376483A1 (en) * | 2022-06-15 | 2025-12-11 | Mirati Therapeutics, Inc. | Prodrugs of pan-kras inhibitors |
| CN117642408A (zh) * | 2022-06-24 | 2024-03-01 | 暨南大学 | 含硒杂环类化合物及其药用组合物和应用 |
| WO2024001839A1 (zh) * | 2022-06-29 | 2024-01-04 | 四川科伦博泰生物医药股份有限公司 | 杂芳环化合物、其制备方法及用途 |
| CN117327102A (zh) * | 2022-06-30 | 2024-01-02 | 北京华森英诺生物科技有限公司 | Kras抑制剂、其制备方法及应用 |
| WO2024008068A1 (en) * | 2022-07-04 | 2024-01-11 | Jacobio Pharmaceuticals Co., Ltd. | K-ras mutant protein inhibitors |
| WO2024009191A1 (en) | 2022-07-05 | 2024-01-11 | Pfizer Inc. | Pyrido[4,3-d]pyrimidine compounds |
| EP4551574A1 (en) * | 2022-07-07 | 2025-05-14 | BeiGene, Ltd. | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
| WO2024008178A1 (zh) * | 2022-07-08 | 2024-01-11 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| CA3262030A1 (en) | 2022-07-21 | 2025-06-12 | Astellas Pharma Inc. | HETEROCYCLIC COMPOUND ACTING ON THE MUTANT KRAS PROTEIN G12D |
| WO2024022444A1 (zh) | 2022-07-27 | 2024-02-01 | 江苏恒瑞医药股份有限公司 | 稠环类化合物、其制备方法及其在医药上的应用 |
| TW202408536A (zh) | 2022-07-29 | 2024-03-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種包含kras g12d抑制劑的醫藥組成物 |
| KR20250044266A (ko) | 2022-08-05 | 2025-03-31 | 아스텔라스세이야쿠 가부시키가이샤 | 변이 kras 단백의 분해를 유도하기 위한 복소환 화합물 |
| WO2024027814A1 (zh) * | 2022-08-05 | 2024-02-08 | 杭州中美华东制药有限公司 | 具有KRas G12D抑制作用的化合物 |
| 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 |
| CN119677726A (zh) | 2022-08-11 | 2025-03-21 | 百时美施贵宝公司 | Kras抑制剂 |
| 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 |
| WO2024040109A2 (en) * | 2022-08-16 | 2024-02-22 | Bristol-Myers Squibb Company | Kras inhibitors |
| WO2024040131A1 (en) | 2022-08-17 | 2024-02-22 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| CN120018863A (zh) * | 2022-08-24 | 2025-05-16 | 珃诺生物医药科技(杭州)有限公司 | 用于调节kras(g12d)的方法和组合物 |
| WO2024045066A1 (en) * | 2022-08-31 | 2024-03-07 | Nikang Therapeutics, Inc. | Alkylidene carbamate as kras inhibitors |
| JP2025530170A (ja) * | 2022-09-07 | 2025-09-11 | ブリストル-マイヤーズ スクイブ カンパニー | Kras g12d阻害剤 |
| WO2024054625A2 (en) * | 2022-09-08 | 2024-03-14 | Nikang Therapeutics, Inc. | Bifunctional compounds for degrading kras g12d via ubiquitin proteasome pathway |
| TW202426463A (zh) * | 2022-09-09 | 2024-07-01 | 大陸商上海翰森生物醫藥科技有限公司 | 含嘧啶多環類生物抑制劑、其製備方法和應用 |
| TW202416976A (zh) * | 2022-09-16 | 2024-05-01 | 大陸商南京明德新藥研發有限公司 | 含六氫螺環[環丙烷—1,2'—吡咯𠯤]的化合物 |
| CN119855815A (zh) * | 2022-09-21 | 2025-04-18 | 甘李药业股份有限公司 | 一种kras突变蛋白抑制剂、及其制备方法和应用 |
| JP2025534419A (ja) | 2022-09-30 | 2025-10-15 | トラスヴェダ リミテッド | Kras変異腫瘍に対する抗腫瘍活性を有する化合物 |
| WO2024083258A1 (zh) * | 2022-10-21 | 2024-04-25 | 上海领泰生物医药科技有限公司 | Kras g12d降解剂及其制备方法和应用 |
| WO2024083256A1 (zh) | 2022-10-21 | 2024-04-25 | 上海领泰生物医药科技有限公司 | pan-KRAS降解剂及其制备方法和应用 |
| CN120166992A (zh) * | 2022-10-31 | 2025-06-17 | 上海皓元医药股份有限公司 | 一种((2R,7aS)-2-氟六氢-1H-吡咯嗪-7a-基)甲醇的制备方法 |
| IL320388A (en) * | 2022-11-14 | 2025-06-01 | Amgen Inc | Macrocyclic KRAS inhibitors and methods of use |
| IL320913A (en) | 2022-11-21 | 2025-07-01 | Treeline Biosciences Inc | Spirocyclic dihydropyranopyrimidine KRAS inhibitors |
| AU2023402587A1 (en) | 2022-11-28 | 2025-06-12 | Redx Pharma Limited | Compounds |
| CN116554208A (zh) * | 2022-12-02 | 2023-08-08 | 苏州浦合医药科技有限公司 | 取代的双环杂芳基化合物作为kras g12d抑制剂 |
| CN120712271A (zh) * | 2022-12-07 | 2025-09-26 | 爱思开生物制药株式会社 | 作为kras g12d抑制剂的新型三环化合物及其用途 |
| TW202430184A (zh) | 2022-12-20 | 2024-08-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | Kras g12d抑制劑的結晶形式及製備方法 |
| AU2023412117A1 (en) | 2022-12-23 | 2025-06-19 | Abbisko Therapeutics Co., Ltd. | Kras g12d inhibitors and uses thereof |
| CN115894503B (zh) * | 2022-12-30 | 2025-06-13 | 合肥诺全医药有限公司 | 一种氮杂环戊烷衍生物的制备方法 |
| WO2024158242A1 (ko) * | 2023-01-25 | 2024-08-02 | 주식회사 엔바이오스 | Kras g12d 돌연변이 억제용 화합물 및 이를 유효성분으로 포함하는 암질환 예방 또는 치료용 조성물 |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
| WO2024179546A1 (en) * | 2023-03-01 | 2024-09-06 | Ascentage Pharma (Suzhou) Co., Ltd. | Kras inhibitors |
| WO2024186680A1 (en) * | 2023-03-03 | 2024-09-12 | Frontier Medicines Corporation | Methods for preparing pyrrolizidine compounds |
| WO2024192424A1 (en) | 2023-03-15 | 2024-09-19 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| CN121079301A (zh) | 2023-03-30 | 2025-12-05 | 伊莱利利公司 | Kras抑制剂 |
| US20240368193A1 (en) | 2023-03-31 | 2024-11-07 | Eli Lilly And Company | Kras inhibitors |
| AU2023439518A1 (en) | 2023-04-06 | 2025-08-28 | Eisai R&D Management Co., Ltd. | Pharmaceutical composition for treating tumors |
| CN118791506A (zh) | 2023-04-14 | 2024-10-18 | 广东东阳光药业股份有限公司 | Kras抑制剂化合物、其药物组合物及其用途 |
| WO2024236452A1 (en) | 2023-05-12 | 2024-11-21 | Jazz Pharmaceuticals Ireland Ltd. | Pyrazolo[4,3-f]quinazoline derivatives as modulators of g12d mutant kras useful for the treatment of cancer |
| AU2024273014A1 (en) * | 2023-05-12 | 2025-11-13 | Blossomhill Therapeutics, Inc. | Fused ring kras inhibitors for treating disease |
| WO2024238633A2 (en) * | 2023-05-15 | 2024-11-21 | Mirati Therapeutics, Inc. | Kras g12s and g12c inhibitors |
| 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 |
| 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 |
| WO2025011634A1 (zh) * | 2023-07-13 | 2025-01-16 | 上海森辉医药有限公司 | Kras g12d中间体的制备方法 |
| WO2025016899A1 (en) | 2023-07-19 | 2025-01-23 | Bayer Aktiengesellschaft | Spirocyclic compounds for the treatment of cancer |
| WO2025024447A2 (en) * | 2023-07-24 | 2025-01-30 | Mirati Therapeutics, Inc. | Processes and intermediates for synthesis of mrtx1133 |
| WO2025026903A1 (en) | 2023-07-31 | 2025-02-06 | Bayer Aktiengesellschaft | Imidazo pyrimidine compounds for the treatment of cancer |
| TW202525817A (zh) | 2023-08-22 | 2025-07-01 | 法商賽諾菲公司 | 三𠯤化合物 |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶KRas抑制劑 |
| WO2025072457A1 (en) | 2023-09-27 | 2025-04-03 | Eli Lilly And Company | Kras inhibitors |
| US20250144225A1 (en) * | 2023-10-03 | 2025-05-08 | PAQ Therapeutics Inc. | KRAS Proteolysis Targeting Chimeras |
| TW202523324A (zh) * | 2023-10-08 | 2025-06-16 | 大陸商成都海博為藥業有限公司 | 一種稠環化合物及應用 |
| US20250114339A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor |
| 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 |
| WO2025077770A1 (zh) * | 2023-10-10 | 2025-04-17 | 成都海博为药业有限公司 | 一种稠环化合物及在kras抑制剂方面的应用 |
| US20250120981A1 (en) | 2023-10-12 | 2025-04-17 | Mirati Therapeutics, Inc. | Mrtx1133 pharmaceutical compositions |
| 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 |
| TW202521531A (zh) * | 2023-11-20 | 2025-06-01 | 大陸商貝達藥業股份有限公司 | 一種靶向泛kras蛋白降解劑的化合物及其應用 |
| CN117683052A (zh) * | 2023-12-07 | 2024-03-12 | 上海相辉医药科技有限公司 | 一种kras g12d抑制剂mrtx1133的制备方法 |
| CN117756640B (zh) * | 2023-12-14 | 2025-09-26 | 江苏宝众宝达药业股份有限公司 | 一种两步升温法制备高纯度3,3'-二氨基联苯胺的方法 |
| WO2025136346A1 (en) * | 2023-12-19 | 2025-06-26 | Amgen Inc. | Indazole containing compounds and methods of use |
| KR102738924B1 (ko) * | 2023-12-26 | 2024-12-06 | 주식회사 베노바이오 | Kras g12d 변이가 존재하는 암 치료를 위한 신규한 화합물 및 이를 이용한 암의 예방 또는 치료용 조성물 |
| US20250215087A1 (en) | 2023-12-29 | 2025-07-03 | Bristol-Myers Squibb Company | Combination therapy of kras inhibitor and treg depleting agent |
| CN119661556B (zh) * | 2024-01-26 | 2025-12-09 | 苏州盛迪亚生物医药有限公司 | 一种稠环类化合物的可药用盐、其结晶形式及用途 |
| WO2025163494A1 (en) | 2024-01-29 | 2025-08-07 | Jazz Pharmaceuticals Ireland Ltd. | Condensed azines for the treatment of cancer |
| WO2025170938A1 (en) * | 2024-02-06 | 2025-08-14 | Windermere Therapeutics, Inc. | Kras(g12d) inhibitors |
| WO2025194057A1 (en) * | 2024-03-14 | 2025-09-18 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025194054A1 (en) * | 2024-03-14 | 2025-09-18 | Amgen Inc. | Spirocyclic compounds as modulators of kras and uses thereof |
| WO2025217015A1 (en) | 2024-04-08 | 2025-10-16 | Mirati Therapeutics, Inc. | Combination therapies using prmt5 inhibitors and kras g12d inhibitors for the treatment of cancer |
| WO2025231310A1 (en) | 2024-05-03 | 2025-11-06 | Mirati Therapeutics, Inc. | Crystalline forms of mrtx1133 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
Family Cites Families (207)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0116662A (pt) | 2001-01-02 | 2003-09-23 | Hoffmann La Roche | Derivados de quinazolona como antagonistas receptores alfa 1a/b adrenérgicos |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| US7105667B2 (en) | 2001-05-01 | 2006-09-12 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
| US20080051387A1 (en) | 2006-06-09 | 2008-02-28 | Yuelian Xu | Tetrahydropyrido[3,4-d]pyrimidines and related analogues |
| US9259426B2 (en) | 2006-07-20 | 2016-02-16 | Gilead Sciences, Inc. | 4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| CA2673299C (en) | 2006-12-21 | 2016-04-12 | Sloan-Kettering Institute For Cancer Research | Pyridazinone compounds for the treatment of proliferative diseases |
| WO2008103470A2 (en) | 2007-02-21 | 2008-08-28 | Trustees Of Columbia University In The City Of New York | Oncogenic-ras-signal dependent lethal compounds |
| WO2009047255A1 (en) | 2007-10-09 | 2009-04-16 | Ucb Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| PE20110403A1 (es) | 2008-07-31 | 2011-07-04 | Genentech Inc | Compuestos biciclicos fusionados de pirimidina en el tratamiento del cancer |
| WO2010120996A1 (en) | 2009-04-17 | 2010-10-21 | Wyeth Llc | 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
| TW201105665A (en) | 2009-04-22 | 2011-02-16 | Janssen Pharmaceutica Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| WO2011078369A1 (ja) | 2009-12-25 | 2011-06-30 | 持田製薬株式会社 | 新規アリールウレア誘導体 |
| EP2519664A4 (en) | 2009-12-30 | 2014-03-12 | Avila Therapeutics Inc | LIGAND-RELATED COVALENTS MODIFYING A PROTEIN |
| CN104379563B (zh) | 2012-04-10 | 2018-12-21 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| SI2858647T1 (sl) * | 2012-06-08 | 2018-11-30 | Sensorion | Inhibitorji receptorja H4 za zdravljenje tinitusa |
| US9695133B2 (en) | 2012-07-13 | 2017-07-04 | The Trustees Of Columbia University In The City Of New York | Quinazolinone-based oncogenic-RAS-selective lethal compounds and their use |
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| WO2014143659A1 (en) | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras g12c |
| MX364438B (es) | 2013-03-15 | 2019-04-26 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
| UA119971C2 (uk) | 2013-10-10 | 2019-09-10 | Араксіс Фарма Ллк | Інгібітори g12c kras |
| MA40074A (fr) | 2014-05-30 | 2015-12-03 | Univ Columbia | Composés liant ras multivalents |
| WO2016025650A1 (en) | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a cdk4/6 inhibitor and related methods |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US9862701B2 (en) | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| US10017540B2 (en) | 2015-03-11 | 2018-07-10 | California Institute Of Technology | Cyclic peptide binder against oncogenic K-Ras |
| EA201792214A1 (ru) | 2015-04-10 | 2018-01-31 | Араксис Фарма Ллк | Соединения замещенного хиназолина |
| JP6789239B2 (ja) | 2015-04-15 | 2020-11-25 | アラクセス ファーマ エルエルシー | Krasの縮合三環系インヒビターおよびその使用の方法 |
| WO2016172692A1 (en) | 2015-04-24 | 2016-10-27 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Mutant kras inhibitors |
| CA2983927A1 (en) | 2015-05-06 | 2016-11-10 | The Regents Of The University Of California | K-ras modulators |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| CN108513588A (zh) | 2015-09-24 | 2018-09-07 | Ionis制药公司 | Kras表达的调节剂 |
| US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10689356B2 (en) | 2015-09-28 | 2020-06-23 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3364977A4 (en) | 2015-10-19 | 2019-09-04 | Araxes Pharma LLC | PROCESS FOR SCREENING INHIBITORS OF RAS |
| CA3001847A1 (en) | 2015-10-22 | 2017-04-27 | The Scripps Research Institute | Cysteine reactive probes and uses thereof |
| WO2017080980A1 (en) | 2015-11-09 | 2017-05-18 | Astrazeneca Ab | Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer |
| WO2017079864A1 (en) | 2015-11-12 | 2017-05-18 | Hangzhou Yier Biotech Co., Ltd. | Treatment of cancers related to chronically active ras |
| CA3005089A1 (en) | 2015-11-16 | 2017-05-26 | Araxes Pharma Llc | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| US20170283445A1 (en) | 2016-04-05 | 2017-10-05 | University Of South Carolina | Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins |
| AU2017266911B2 (en) * | 2016-05-18 | 2021-09-02 | Array Biopharma, Inc. | KRas G12C inhibitors |
| 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 |
| 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 |
| CN110312711A (zh) | 2016-10-07 | 2019-10-08 | 亚瑞克西斯制药公司 | 作为ras抑制剂的杂环化合物及其使用方法 |
| MX2019006296A (es) | 2016-11-30 | 2019-11-12 | Bantam Pharmaceutical Llc | Métodos de uso de compuestos de pirazol y pirazol sustituido y para el tratamiento de enfermedades hiperproliferativas. |
| CA3081983A1 (en) | 2016-11-30 | 2018-06-07 | Bantam Pharmaceutical, Llc | Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases |
| AU2017378487B2 (en) | 2016-12-15 | 2022-03-31 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| EP3878850A1 (en) | 2016-12-22 | 2021-09-15 | Boehringer Ingelheim International GmbH | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
| SI3558955T1 (sl) | 2016-12-22 | 2021-12-31 | Amgen Inc., | Derivati benzizotiazola, izotiazola(3,4-b)piridina, kinazolina, ftalazina, pirido(2,3-d)piridazina in pirido(2,3-D)pirimidina, kot zaviralci KRAS G12C za zdravljenje pljučnega raka, raka trebušne slinavke ali kolorektalnega raka |
| US10344026B2 (en) | 2017-01-18 | 2019-07-09 | Nantbio, Inc. | Compositions and methods of targeting mutant K-ras |
| WO2018140598A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused n-heterocyclic compounds and methods of use thereof |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| US11274093B2 (en) | 2017-01-26 | 2022-03-15 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ-ヘテロ二環式化合物およびその使用方法 |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| SG11201909570PA (en) | 2017-04-20 | 2019-11-28 | Univ California | K-ras modulators |
| EP3679040B1 (en) * | 2017-09-08 | 2022-08-03 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| EP3832583A4 (en) | 2018-07-31 | 2021-12-08 | Honda Motor Co., Ltd. | ENERGY PREDICTION SYSTEM, ENERGY PREDICTION DEVICE, ENERGY PREDICTION METHOD, STORAGE PROGRAM AND MEDIA |
| CN113038342B (zh) | 2018-09-30 | 2022-10-14 | 荣耀终端有限公司 | 音频播放电路和终端 |
| CN111193490B (zh) | 2018-11-14 | 2025-05-13 | 天津大学 | 散热结构、带散热结构的体声波谐振器、滤波器和电子设备 |
| 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 |
| WO2020163598A1 (en) | 2019-02-07 | 2020-08-13 | The Regents Of The University Of California | Immunophilin-dependent inhibitors and uses thereof |
| KR20210124404A (ko) | 2019-02-11 | 2021-10-14 | 메소맷 인크. | 구조적 스트레인을 모니터링 하기 위한 감지 섬유 |
| KR102747104B1 (ko) | 2019-02-18 | 2024-12-27 | 한국과학기술연구원 | 단백질 키나아제 저해 활성을 갖는 신규한 피리도[3,4-d]피리미딘-8-온 유도체 및 이를 포함하는 암의 예방, 개선 또는 치료용 약학 조성물 |
| EP3927727A1 (en) | 2019-02-20 | 2021-12-29 | Fred Hutchinson Cancer Research Center | Binding proteins specific for ras neoantigens and uses thereof |
| GB201902392D0 (en) | 2019-02-21 | 2019-04-10 | Cambridge Entpr Ltd | Modular binding proteins |
| EP3931564A4 (en) | 2019-02-26 | 2023-04-26 | Cell Response, Inc. | Methods for treating map3k8 positive cancers |
| WO2020177629A1 (zh) | 2019-03-01 | 2020-09-10 | 劲方医药科技(上海)有限公司 | 螺环取代的嘧啶并环类化合物,其制法与医药上的用途 |
| WO2020176963A1 (en) | 2019-03-05 | 2020-09-10 | Questor Technology Inc. | Gas incinerator system |
| SG11202109451TA (en) | 2019-03-05 | 2021-09-29 | Astrazeneca Ab | Fused tricyclic compounds useful as anticancer agents |
| CA3131138A1 (en) | 2019-03-06 | 2020-09-10 | Dana-Farber Cancer Institute, Inc. | T cell receptors specific to b-cell maturation antigen for treatment of cancer |
| WO2020198125A1 (en) | 2019-03-22 | 2020-10-01 | Icahn School Of Medicine At Mount Sinai | Methods for treating colorectal cancer |
| CA3134825A1 (en) | 2019-03-29 | 2020-10-08 | Kura Oncology, Inc. | Methods of treating squamous cell carcinomas with farnesyltransferase inhibitors |
| MX2021011928A (es) | 2019-03-29 | 2022-01-04 | Dicerna Pharmaceuticals Inc | Composiciones y metodos para el tratamiento de enfermedades o trastornos asociados con kras. |
| KR102222693B1 (ko) | 2019-04-04 | 2021-03-04 | 금정제약 주식회사 | H-rev107 유래 펩타이드의 신규한 용도 |
| WO2020214537A1 (en) | 2019-04-15 | 2020-10-22 | Tosk, Inc. | Modulators of ras gtpase |
| US20200335182A1 (en) | 2019-04-16 | 2020-10-22 | Uratim Ltd. | Method and apparatus for facilitating the binding of biological macromolecules with the use of gluing molecular agents with applications in RAS mutations and related conditions |
| WO2020221239A1 (zh) | 2019-04-28 | 2020-11-05 | 劲方医药科技(上海)有限公司 | 氧杂氮杂喹唑啉-7(8h)-酮类化合物,其制法与医药上的用途 |
| IL287795B2 (en) | 2019-05-10 | 2025-05-01 | Deciphera Pharmaceuticals Llc | Heteroarylaminopyrimidine amides as autophagy inhibitors and methods of using them |
| CN118878519A (zh) | 2019-05-10 | 2024-11-01 | 德西费拉制药有限责任公司 | 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法 |
| KR102881316B1 (ko) | 2019-05-13 | 2025-11-05 | 노파르티스 아게 | 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태 |
| WO2020230091A1 (en) | 2019-05-14 | 2020-11-19 | Janssen Biotech, Inc. | Combination therapies with bispecific anti-egfr/c-met antibodies and third generation egfr tyrosine kinase inhibitors |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| WO2020236940A1 (en) | 2019-05-20 | 2020-11-26 | California Institute Of Technology | Kras g12c inhibitors and uses thereof |
| CA3140394A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| WO2020233592A1 (en) | 2019-05-21 | 2020-11-26 | Inventisbio Shanghai Ltd. | Heterocyclic compounds, preparation methods and uses thereof |
| EP3972963A1 (en) | 2019-05-21 | 2022-03-30 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| JP7092935B2 (ja) | 2019-05-21 | 2022-06-28 | アムジエン・インコーポレーテツド | 固体形態 |
| WO2020247914A1 (en) | 2019-06-07 | 2020-12-10 | Emory University | Kras g12v mutant binds to jak1, inhibitors, pharmaceutical compositions, and methods related thereto |
| CN114222729A (zh) | 2019-06-12 | 2022-03-22 | 范德比尔特大学 | 氨基酸转运抑制剂及其用途 |
| AU2020291936A1 (en) | 2019-06-12 | 2022-02-03 | Vanderbilt University | Dibenzylamines as amino acid transport inhibitors |
| WO2021000885A1 (zh) | 2019-07-01 | 2021-01-07 | 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 |
| CA3149403A1 (en) | 2019-08-02 | 2021-02-11 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Tetracyclic compound, preparation method and use thereof |
| WO2021023247A1 (en) | 2019-08-07 | 2021-02-11 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitor |
| WO2021027943A1 (zh) | 2019-08-14 | 2021-02-18 | 正大天晴药业集团南京顺欣制药有限公司 | 哒嗪酮并嘧啶类衍生物及其医药用途 |
| CN112390797A (zh) | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | 新型螺环类K-Ras G12C抑制剂 |
| CN114222743A (zh) | 2019-08-16 | 2022-03-22 | 劲方医药科技(上海)有限公司 | 氧代六元环并嘧啶类化合物,其制法与医药上的用途 |
| CA3150759A1 (en) | 2019-08-22 | 2021-02-25 | The Regents Of The Universtiy Of Michigan | Method of treating kras-associated cancers |
| CN114269735B (zh) | 2019-08-26 | 2024-02-23 | 南京创济生物医药有限公司 | 二氢或四氢喹唑啉类化合物及其中间体、制备方法和应用 |
| 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 |
| CN114616232A (zh) | 2019-09-06 | 2022-06-10 | 正大天晴药业集团南京顺欣制药有限公司 | 氮杂环庚烷并嘧啶类衍生物及其医药用途 |
| CN112771053A (zh) | 2019-09-06 | 2021-05-07 | 伟迈可生物有限公司 | 基于生物标志物的治疗组合物 |
| KR20220061997A (ko) | 2019-09-10 | 2022-05-13 | 더 보드 오브 트러스티스 오브 더 리랜드 스탠포드 쥬니어 유니버시티 | Kras 돌연변이체 암의 치료 방법 |
| WO2021051034A1 (en) | 2019-09-13 | 2021-03-18 | Biotheryx, Inc. | Ras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2021055728A1 (en) | 2019-09-18 | 2021-03-25 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| TWI761961B (zh) | 2019-09-20 | 2022-04-21 | 大陸商上海濟煜醫藥科技有限公司 | 稠合吡啶酮類化合物及其製備方法和應用 |
| WO2021061515A1 (en) | 2019-09-23 | 2021-04-01 | Synblia Therapeutics, Inc. | Shp2 inhibitors and uses thereof |
| AU2020356455A1 (en) | 2019-09-24 | 2022-04-14 | Mirati Therapeutics, Inc. | Combination therapies |
| CN112552295A (zh) | 2019-09-25 | 2021-03-26 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| CN114929706A (zh) | 2019-09-29 | 2022-08-19 | 百济神州有限公司 | Kras g12c的抑制剂 |
| CN112574224A (zh) | 2019-09-30 | 2021-03-30 | 上海迪诺医药科技有限公司 | Kras g12c抑制剂及其应用 |
| US20230257374A1 (en) | 2019-10-10 | 2023-08-17 | Innovent Biologics (Suzhou) Co., Ltd. | Novel kras g12c protein inhibitor, preparation method therefor, and use thereof |
| JP6754125B1 (ja) | 2019-10-15 | 2020-09-09 | 学校法人東京理科大学 | Brap2作用増強剤 |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| CN112694475B (zh) | 2019-10-23 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 环烷基类和杂环烷基类抑制剂及其制备方法和应用 |
| KR20220088441A (ko) | 2019-10-23 | 2022-06-27 | 에스케이바이오팜 주식회사 | 바이사이클릭 화합물 및 이의 용도 |
| MX2022004656A (es) | 2019-10-24 | 2022-05-25 | Amgen Inc | Derivados de piridopirimidina utiles como inhibidores de kras g12c y kras g12d en el tratamiento del cancer. |
| PE20221253A1 (es) | 2019-10-28 | 2022-08-16 | Merck Sharp & Dohme | Inhibidores de pequenas moleculas de mutante g12c de kras |
| LT4053118T (lt) | 2019-10-30 | 2024-12-10 | Genfleet Therapeutics (Shanghai) Inc. | Pakeistas heterociklinis junginys su sujungtais žiedais, jo paruošimo būdas ir naudojimas farmacijoje |
| WO2021084765A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd | 4-aminobut-2-enamide derivatives and salts thereof |
| CN115551500A (zh) | 2019-10-31 | 2022-12-30 | 大鹏药品工业株式会社 | 4-氨基丁-2-烯酰胺衍生物及其盐 |
| BR112022008535A2 (pt) | 2019-11-04 | 2022-08-09 | Revolution Medicines Inc | Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras |
| US11739074B2 (en) | 2019-11-04 | 2023-08-29 | Revolution Medicines, Inc. | Ras inhibitors |
| CR20220241A (es) | 2019-11-04 | 2022-08-03 | Revolution Medicines Inc | Inhibidores de ras |
| CN113286794B (zh) | 2019-11-04 | 2024-03-12 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| JP6880352B1 (ja) | 2019-11-07 | 2021-06-02 | 中外製薬株式会社 | Kras阻害作用を有する環状ペプチド化合物 |
| CN112778301A (zh) | 2019-11-07 | 2021-05-11 | 苏州泽璟生物制药股份有限公司 | 四氢吡啶并嘧啶类抑制剂及其制备方法和应用 |
| WO2021093758A1 (zh) | 2019-11-15 | 2021-05-20 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| CN113614080B (zh) | 2019-11-29 | 2022-06-28 | 苏州信诺维医药科技股份有限公司 | Kras g12c抑制剂化合物及其用途 |
| WO2021106231A1 (en) | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| JP7480298B2 (ja) | 2019-12-02 | 2024-05-09 | シャンハイ インリー ファーマシューティカル カンパニー リミテッド | 酸素含有複素環化合物、その製造方法及び使用 |
| WO2021113595A1 (en) | 2019-12-06 | 2021-06-10 | Beta Pharma, Inc. | Phosphorus derivatives as kras inhibitors |
| WO2021120045A1 (en) | 2019-12-18 | 2021-06-24 | InventisBio Co., Ltd. | Heterocyclic compounds, preparation methods and uses thereof |
| US12365706B2 (en) | 2019-12-18 | 2025-07-22 | Merck Sharp & Dohme Llc | Macrocyclic peptides as potent inhibitors of K-RAS G12D mutant |
| 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 |
| WO2021121397A1 (zh) | 2019-12-19 | 2021-06-24 | 首药控股(北京)股份有限公司 | 取代的炔基杂环化合物 |
| CN113454083A (zh) | 2019-12-19 | 2021-09-28 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| WO2021127404A1 (en) | 2019-12-20 | 2021-06-24 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| TR201920922A2 (tr) | 2019-12-20 | 2020-06-22 | Ankara Ueniversitesi | 3/4-((2E,6E)-3,7,11-Trimetildodeka-2,6,10-trieniltiyo)benzamid Türevi Bileşikler |
| CN113045565A (zh) | 2019-12-27 | 2021-06-29 | 微境生物医药科技(上海)有限公司 | 新型K-Ras G12C抑制剂 |
| CA3162106A1 (en) | 2019-12-27 | 2021-07-01 | Yuli Xie | Spiro ring-containing quinazoline compound |
| WO2021139678A1 (zh) | 2020-01-07 | 2021-07-15 | 广州百霆医药科技有限公司 | 吡啶并嘧啶类kras g12c突变蛋白抑制剂 |
| CN113087700B (zh) | 2020-01-08 | 2023-03-14 | 苏州亚盛药业有限公司 | 螺环四氢喹唑啉 |
| AU2021206240A1 (en) | 2020-01-10 | 2022-08-25 | Incyte Corporation | Tricyclic compounds as inhibitors of KRAS |
| WO2021143693A1 (zh) | 2020-01-13 | 2021-07-22 | 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 |
| KR102396930B1 (ko) | 2020-01-15 | 2022-05-12 | 한국과학기술연구원 | 피리도[3,4-d]피리미딘 유도체 및 이를 포함하는 치료용 약학 조성물 |
| KR102382613B1 (ko) | 2020-01-15 | 2022-04-06 | 한국과학기술연구원 | 단백질 키나아제 저해 활성을 갖는 7-아미노-3,4-디히드로피리미도피리미딘-2-온 유도체 및 이를 포함하는 치료용 약학 조성물 |
| WO2021150613A1 (en) | 2020-01-20 | 2021-07-29 | Incyte Corporation | Spiro compounds as inhibitors of kras |
| CN115003668A (zh) | 2020-01-21 | 2022-09-02 | 南京明德新药研发有限公司 | 作为kras抑制剂的大环类化合物 |
| GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
| CN115135650A (zh) | 2020-02-20 | 2022-09-30 | 贝达医药公司 | 作为kras抑制剂的吡啶并嘧啶衍生物 |
| EP4112606A4 (en) | 2020-02-24 | 2024-04-10 | Shanghai Zheye Biotechnology Co., Ltd. | AROMATIC COMPOUND AND ITS USE IN THE PREPARATION OF ANTINEOPLASIC DRUGS |
| CN113637005B (zh) | 2020-02-24 | 2024-05-24 | 泰励生物科技(上海)有限公司 | 用于癌症治疗的kras抑制剂 |
| WO2021173923A1 (en) | 2020-02-28 | 2021-09-02 | Erasca, Inc. | Pyrrolidine-fused heterocycles |
| WO2021175199A1 (zh) | 2020-03-02 | 2021-09-10 | 上海喆邺生物科技有限公司 | 一类芳香杂环类化合物及其在药物中的应用 |
| EP4115887A4 (en) | 2020-03-03 | 2024-07-17 | Wellmarker Bio Co., Ltd. | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF CANCER HAVING KRAS MUTATION AND RON ACTIVATION |
| US20230098205A1 (en) | 2020-03-05 | 2023-03-30 | The Regents Of The University Of Michigan | Inhibitors of egfr, kras, braf, and other targets and use of the same |
| CA3172812A1 (en) | 2020-03-05 | 2021-09-10 | The Regents Of The University Of Michigan | Inhibitors of egfr, kras, braf, and other targets and use of the same |
| CN117050079A (zh) | 2020-03-12 | 2023-11-14 | 德昇济医药(无锡)有限公司 | 嘧啶并杂环类化合物及其应用 |
| WO2021185233A1 (en) | 2020-03-17 | 2021-09-23 | Jacobio Pharmaceuticals Co., Ltd. | Kras mutant protein inhibitors |
| US12391692B2 (en) | 2020-03-25 | 2025-08-19 | Wigen Boimedicine Technology (Shanghai) Co., Ltd. | Spiro ring-containing quinazoline compound |
| KR20220164015A (ko) | 2020-04-03 | 2022-12-12 | 메드샤인 디스커버리 아이엔씨. | 옥타하이드로피라지노디아자나프티리딘 디온 화합물 |
| US20220370416A1 (en) | 2020-04-06 | 2022-11-24 | Arvinas Operations, Inc. | Compounds and methods for targeted degradation of kras |
| TW202144338A (zh) | 2020-04-08 | 2021-12-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 嘧啶并二環類衍生物、其製備方法及其在醫藥上的應用 |
| BR112022020841A2 (pt) | 2020-04-16 | 2023-05-02 | Incyte Corp | Inibidores de kras tricíclicos fundidos |
| WO2021216770A1 (en) | 2020-04-22 | 2021-10-28 | Accutar Biotechnology Inc. | Substituted tetrahydroquinazoline compounds as kras inhibitors |
| US20230242586A1 (en) | 2020-04-23 | 2023-08-03 | The Regents Of The University Of California | Ras inhibitors and uses thereof |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| CN113563323B (zh) | 2020-04-29 | 2023-12-01 | 上海凌达生物医药有限公司 | 一类苯并噻唑基联芳基类化合物、制备方法和用途 |
| CN115135636B (zh) | 2020-04-29 | 2024-08-23 | 北京泰德制药股份有限公司 | 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂 |
| CN116194456B (zh) | 2020-04-30 | 2025-08-29 | 上海科州药物股份有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| WO2021231526A1 (en) | 2020-05-13 | 2021-11-18 | Incyte Corporation | Fused pyrimidine compounds as kras inhibitors |
| CN113666923A (zh) | 2020-05-15 | 2021-11-19 | 苏州泽璟生物制药股份有限公司 | 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用 |
| WO2021236475A1 (en) | 2020-05-18 | 2021-11-25 | Asinex Corporation | Compounds that inhibit asparagine synthetase and their methods of use |
| 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 |
| AU2021280351A1 (en) | 2020-05-29 | 2023-01-05 | Syros Pharmaceuticals, Inc. | Methods of treating cancer in patients with an anomalous KRAS gene or deletions within chromosome 9 |
| US20230212164A1 (en) | 2020-06-02 | 2023-07-06 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| BR112022024300A2 (pt) | 2020-06-04 | 2023-01-24 | Pillai Universal Llc | Moléculas pequenas para degradação direcionada de kras não direcionado na terapia de câncer |
| US20230212170A1 (en) | 2020-06-04 | 2023-07-06 | Shanghai Antengene Corporation Limited | Inhibitors of kras g12c protein and uses thereof |
| WO2021248079A1 (en) | 2020-06-05 | 2021-12-09 | Sparcbio Llc | Heterocyclic compounds and methods of use thereof |
| US20230023009A1 (en) | 2020-06-05 | 2023-01-26 | Sparcbio Llc | Heterocyclic compounds and methods of use thereof |
| WO2021248082A1 (en) | 2020-06-05 | 2021-12-09 | Sparcbio Llc | Heterocyclic compounds and methods of use thereof |
| US20230026856A1 (en) | 2020-06-05 | 2023-01-26 | Sparcbio Llc | Heterocyclic compounds and methods of use thereof |
| WO2021248083A1 (en) | 2020-06-05 | 2021-12-09 | Sparcbio Llc | Heterocyclic compounds and methods of use thereof |
| WO2021252339A1 (en) | 2020-06-08 | 2021-12-16 | Accutar Biotechnology, Inc. | Substituted purine-2,6-dione compounds as kras inhibitors |
| 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 |
| WO2021257828A1 (en) | 2020-06-18 | 2021-12-23 | Shy Therapeutics, Llc | Substituted thienopyrimidines that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| WO2021259331A1 (zh) | 2020-06-24 | 2021-12-30 | 南京明德新药研发有限公司 | 八元含n杂环类化合物 |
| JP2023531269A (ja) | 2020-06-30 | 2023-07-21 | インベンティスバイオ カンパニー リミテッド | キナゾリン化合物、その製造方法および用途 |
| US20230279025A1 (en) * | 2020-07-16 | 2023-09-07 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022017339A1 (zh) | 2020-07-20 | 2022-01-27 | 江苏恒瑞医药股份有限公司 | 稠合哒嗪类衍生物、其制备方法及其在医药上的应用 |
| EP4194452A4 (en) | 2020-08-02 | 2024-08-21 | Shanghai Zheye Biotechnology Co., Ltd. | AROMATIC COMPOUND AND ITS USE IN ANTITUMOUS MEDICINES |
| US20230339976A1 (en) | 2020-08-04 | 2023-10-26 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022028492A1 (en) | 2020-08-05 | 2022-02-10 | Beigene, Ltd. | Imidazotriazine and pyrrolopyrimidine derivatives as kras g12c inhibitors |
| US20230303551A1 (en) | 2020-08-13 | 2023-09-28 | Albert Einstein College Of Medicine | N-cyclyl-sulfonamides useful for inhibiting raf |
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