TWI874443B - KRas G12D抑制劑 - Google Patents

KRas G12D抑制劑 Download PDF

Info

Publication number
TWI874443B
TWI874443B TW109129561A TW109129561A TWI874443B TW I874443 B TWI874443 B TW I874443B TW 109129561 A TW109129561 A TW 109129561A TW 109129561 A TW109129561 A TW 109129561A TW I874443 B TWI874443 B TW I874443B
Authority
TW
Taiwan
Prior art keywords
group
compound
pharmaceutically acceptable
acceptable salt
alkyl
Prior art date
Application number
TW109129561A
Other languages
English (en)
Chinese (zh)
Other versions
TW202122396A (zh
Inventor
小稜 王
馬修 阿諾德 馬克思
詹姆士 蓋兒 克里斯騰森
亞倫 克雷格 伯恩斯
克里斯托弗 羅納德 史密斯
約翰 麥可 凱瑟姆
托尼 Ｐ 湯
杰伊 布拉德福德 費爾
詹姆士 F 布萊克
瑪莎 Ｅ 羅德里格斯
瑪瑟多尼奧 Ｊ 梅加
帕維爾 薩維琴科夫
馬克 約瑟夫 奇卡雷利
峰 阮
蓋伊 Ｐ Ａ 威格士
東樺 戴
雪莉 艾倫
約書亞 達爾克
斯賓瑟 帕杰克
布拉德 紐豪斯
雅各布 Ｍ 奧萊里
千 趙
約翰 大衛 勞森
約翰 彼得 費希爾
Original Assignee
美商米拉蒂醫療公司
美商陣列生化製藥公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 美商米拉蒂醫療公司, 美商陣列生化製藥公司 filed Critical 美商米拉蒂醫療公司
Publication of TW202122396A publication Critical patent/TW202122396A/zh
Application granted granted Critical
Publication of TWI874443B publication Critical patent/TWI874443B/zh

Links

Classifications

    • 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
    • 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
    • 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)
TW109129561A 2019-08-29 2020-08-28 KRas G12D抑制劑 TWI874443B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201962893604P 2019-08-29 2019-08-29
US62/893,604 2019-08-29
US202063052840P 2020-07-16 2020-07-16
US63/052,840 2020-07-16
US202063058188P 2020-07-29 2020-07-29
US63/058,188 2020-07-29

Publications (2)

Publication Number Publication Date
TW202122396A TW202122396A (zh) 2021-06-16
TWI874443B true TWI874443B (zh) 2025-03-01

Family

ID=74683570

Family Applications (2)

Application Number Title Priority Date Filing Date
TW109129561A TWI874443B (zh) 2019-08-29 2020-08-28 KRas G12D抑制劑
TW114103629A TWI912127B (zh) 2019-08-29 2020-08-28 KRas G12D抑制劑

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW114103629A TWI912127B (zh) 2019-08-29 2020-08-28 KRas G12D抑制劑

Country Status (16)

Country Link
US (3) US11453683B1 (https=)
EP (1) EP4021444A4 (https=)
JP (2) JP7622043B2 (https=)
KR (1) KR20220071193A (https=)
CN (1) CN114615981B (https=)
AU (1) AU2020337938B2 (https=)
BR (1) BR112022003543A2 (https=)
CA (1) CA3148745A1 (https=)
CL (1) CL2022000447A1 (https=)
CO (1) CO2022003782A2 (https=)
IL (1) IL290845B1 (https=)
MX (1) MX2022002465A (https=)
PH (1) PH12022550469A1 (https=)
TW (2) TWI874443B (https=)
WO (1) WO2021041671A1 (https=)
ZA (1) ZA202202362B (https=)

Families Citing this family (244)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
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
EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
WO2020085504A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法
MX2021002804A (es) 2018-12-05 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2022015375A1 (en) * 2020-07-16 2022-01-20 Mirati Therapeutics, Inc. Kras g12d inhibitors
EP4192585A4 (en) * 2020-08-04 2024-08-21 Mirati Therapeutics, Inc. Kras g12d inhibitors
EP4204412A4 (en) * 2020-08-26 2024-10-09 InventisBio Co., Ltd. HETEROARYL COMPOUNDS, PRODUCTION PROCESSES AND USES THEREOF
CA3191279A1 (en) 2020-08-28 2022-03-03 Yi Liu Heterocyclic compounds and uses thereof
US20250195521A1 (en) 2020-09-03 2025-06-19 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
WO2022061251A1 (en) * 2020-09-18 2022-03-24 Plexxikon Inc. Compounds and methods for kras modulation and indications therefor
WO2022068921A1 (zh) * 2020-09-30 2022-04-07 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
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス， インコーポレイテッド アザキナゾリン汎ＫＲａｓ阻害剤
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
CA3203080A1 (en) * 2020-12-22 2022-06-30 Hongqi Tian Preparation and application method of heterocyclic compound as kras inhibitor
JP2024501507A (ja) * 2020-12-25 2024-01-12 スーチュアン ハイスーク ファーマシューティカル カンパニー リミテッド ケトヘキソキナーゼ阻害剤及びその用途
WO2022170999A1 (zh) * 2021-02-09 2022-08-18 南京明德新药研发有限公司 吡啶[4，3-d]嘧啶类化合物
WO2022173032A1 (ja) 2021-02-15 2022-08-18 アステラス製薬株式会社 Ｇ１２ｄ変異ｋｒａｓタンパクの分解を誘導するためのキナゾリン化合物
EP4293025B1 (en) 2021-02-15 2025-10-29 Astellas Pharma Inc. 4-aminoquinazoline compound
WO2022184178A1 (en) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
US20240199644A1 (en) * 2021-03-07 2024-06-20 Jacobio Pharmaceuticals Co., Ltd. Fused Ring Derivatives Useful as KRAS G12D Inhibitors
JP2024509280A (ja) * 2021-03-10 2024-02-29 ベータ・ファーマ・インコーポレイテッド Ｋｒａｓ阻害物質としてのピリドピリミジン誘導体
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
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
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
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
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
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
WO2022194191A1 (en) * 2021-03-16 2022-09-22 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of kras g12d
CA3211725A1 (en) * 2021-03-17 2022-09-22 Tao Jiang Pyrimidine-fused cyclic compound, preparation method therefor and use thereof
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
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
CN116157400B (zh) * 2021-03-30 2024-10-22 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
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
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
WO2022221386A1 (en) * 2021-04-14 2022-10-20 Erasca, Inc. Selective kras inhibitors
EP4322954A4 (en) * 2021-04-16 2025-01-29 Merck Sharp & Dohme LLC SMALL MOLECULAR INHIBITORS OF THE KRAS G12D MUTANT
WO2022227987A1 (zh) * 2021-04-28 2022-11-03 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
US20250059205A1 (en) * 2021-04-29 2025-02-20 Amgen Inc. Heterocyclic Compounds and Methods of Use
MX2023012725A (es) * 2021-04-29 2024-09-23 Amgen Inc Compuestos de 2-aminobenzotiazol y metodos de uso de los mismos.
CN115260158A (zh) * 2021-04-30 2022-11-01 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
CN117203207A (zh) * 2021-04-30 2023-12-08 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
CN117222650A (zh) * 2021-04-30 2023-12-12 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
JP2024516450A (ja) * 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ｒａｓ阻害剤及びその使用
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
US20240300980A1 (en) * 2021-05-22 2024-09-12 Shanghai Kechow Pharma, Inc. Heterocyclic compounds as kras inhibitor, and preparation therefor and use thereof in treatment
US20230391785A1 (en) 2021-05-24 2023-12-07 280 Bio, Inc. Nitrogen-containing heterocyclic compound, method for preparing same and use of same
CN115385937A (zh) * 2021-05-25 2022-11-25 江苏恒瑞医药股份有限公司 嘧啶并环烷基类化合物、其制备方法及其在医药上的应用
CN115385938A (zh) * 2021-05-25 2022-11-25 江苏恒瑞医药股份有限公司 苯并嘧啶类化合物、其制备方法及其在医药上的应用
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
BR112023024906A2 (pt) 2021-05-28 2024-02-15 Redx Pharma Plc Compostos
WO2022261154A1 (en) 2021-06-09 2022-12-15 Eli Lilly And Company Substituted fused azines as kras g12d inhibitors
BR112023025869A2 (pt) 2021-06-10 2024-02-27 Redx Pharma Plc Derivados de quinazolina úteis como inibidores de ras
CN115466272A (zh) * 2021-06-11 2022-12-13 博瑞生物医药（苏州）股份有限公司 一种嘧啶并杂环化合物，包含其的药物组合物及其用途
WO2022262686A1 (en) * 2021-06-13 2022-12-22 Jingrui Biopharma Co., Ltd. Kras g12d inhibitors
US20240383921A1 (en) * 2021-06-16 2024-11-21 Erasca, Inc. Amide and urea-containing tricyclic kras inhibitors
WO2022266069A1 (en) * 2021-06-16 2022-12-22 Erasca, Inc. Tricyclic kras g12d inhibitors
TW202317580A (zh) * 2021-06-18 2023-05-01 大陸商南京燧坤智能科技有限公司 用作ｋｒａｓ ｇ１２ｄ抑制劑的氘代化合物
EP4361157A4 (en) * 2021-06-21 2024-10-16 Jiangsu Hengrui Pharmaceuticals Co., Ltd. FUSED TETRACYCLIC COMPOUND, ITS PREPARATION METHOD AND ITS USE IN MEDICINE
WO2022271823A1 (en) * 2021-06-23 2022-12-29 Newave Pharmaceutical Inc. Mutant kras modulators and uses thereof
JP2024524524A (ja) * 2021-06-30 2024-07-05 上海艾力斯医薬科技股▲ふん▼有限公司 窒素含有複素環化合物、その製造方法、中間体及び使用
AU2022303440A1 (en) * 2021-07-02 2024-02-22 Shanghai De Novo Pharmatech Co., Ltd. Kras g12d inhibitor and use thereof
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
CN117751116A (zh) * 2021-07-07 2024-03-22 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
TW202317589A (zh) * 2021-07-14 2023-05-01 美商尼坎醫療公司 作為ｋｒａｓ抑制劑的伸烷基衍生物
WO2023284537A1 (en) * 2021-07-16 2023-01-19 Shanghai Zion Pharma Co. Limited Kras g12d inhibitors and uses thereof
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
WO2023001141A1 (en) * 2021-07-23 2023-01-26 Shanghai Zion Pharma Co. Limited Kras g12d inhibitors and uses thereof
WO2023018812A1 (en) * 2021-08-10 2023-02-16 Amgen Inc. Heterocyclic compounds and methods of use
TW202321261A (zh) * 2021-08-10 2023-06-01 美商伊瑞斯卡公司 選擇性ｋｒａｓ抑制劑
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
CN116669740A (zh) * 2021-08-16 2023-08-29 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
WO2023020523A1 (en) * 2021-08-18 2023-02-23 Jacobio Pharmaceuticals Co., Ltd. Bicyclic derivatives and use thereof
WO2023020521A1 (en) * 2021-08-18 2023-02-23 Jacobio Pharmaceuticals Co., Ltd. Pyridine fused pyrimidine derivatives and use thereof
UY39906A (es) * 2021-08-18 2023-03-31 Jacobio Pharmaceuticals Co Ltd Derivados de 1,4-oxazepano y usos de los mismos
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
US20240409558A1 (en) 2021-09-13 2024-12-12 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
WO2023051586A1 (zh) * 2021-09-29 2023-04-06 先声再明医药有限公司 Kras g12d抑制剂化合物及其制备方法和应用
AU2022361380A1 (en) 2021-10-05 2024-04-11 Mirati Therapeutics, Inc. Combination therapies of kras g12d inhibitors with sos1 inhibitors
MX2024004216A (es) 2021-10-05 2024-06-20 Mirati Therapeutics Inc Terapias combinadas de inhibidores de kras g12d con inhibidores de la familia pan erbb.
IL311834A (en) 2021-10-05 2024-05-01 Mirati Therapeutics Inc Combinations of KRAS G12D inhibitors with PI3KA inhibitors and therapeutic methods
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
AU2022361219A1 (en) 2021-10-05 2024-04-11 Mirati Therapeutics, Inc. Combinations of kras g12d inhibitors with irinotecan and related methods of treatment
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
WO2023061463A1 (zh) * 2021-10-15 2023-04-20 广东东阳光药业有限公司 新的嘧啶并吡啶化合物、其药物组合物及其用途
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
EP4436571A4 (en) * 2021-11-24 2025-10-15 Merck Sharp & Dohme Llc SMALL MOLECULE INHIBITORS OF KRAS MUTATIONAL PROTEINS
US20250250286A1 (en) * 2021-11-30 2025-08-07 Beta Pharma, Inc. Fused pyrimidine derivatives as kras oncoprotein inhibitors
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
CN117940436A (zh) * 2021-12-02 2024-04-26 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
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
EP4452974A4 (en) * 2021-12-21 2025-11-19 Bridgene Biosciences Inc RAS ONCOPROTEIN INHIBITORS
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
EP4371991A4 (en) 2022-01-21 2025-02-26 Usynova Pharmaceuticals Ltd. Benzopyrimidine compounds and use thereof
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
EP4471037A1 (en) 2022-01-30 2024-12-04 Shanghai Pharmaceuticals Holding Co., Ltd. Quinoline compound and use thereof
AU2023216698A1 (en) * 2022-02-03 2024-06-13 Mirati Therapeutics, Inc. Quinazoline pan-kras inhibitors
CA3243798A1 (en) 2022-02-09 2023-08-17 Quanta Therapeutics, Inc. Kras Modulators and Their Uses
WO2023152255A1 (en) 2022-02-10 2023-08-17 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
US20240059712A1 (en) * 2022-03-09 2024-02-22 Risen (Suzhou) Pharma Tech Co., Ltd. Bifunctional compounds and pharmaceutical uses thereof
TW202346270A (zh) 2022-03-11 2023-12-01 日商安斯泰來製藥股份有限公司 用於誘發g12d突變kras蛋白分解之雜環化合物
AU2023231139A1 (en) 2022-03-11 2024-09-05 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
CN117659049A (zh) * 2022-08-23 2024-03-08 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
WO2023179629A1 (zh) * 2022-03-22 2023-09-28 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.
EP4473970A4 (en) 2022-03-31 2026-01-21 Eisai R&D Man Co Ltd PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF TUMORS
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
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
CN118434748A (zh) * 2022-04-15 2024-08-02 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
CR20240451A (es) 2022-04-21 2024-12-04 Gilead Sciences Inc Compuestos de modulación de kras g12d
WO2023212548A1 (en) * 2022-04-26 2023-11-02 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2023212549A1 (en) * 2022-04-26 2023-11-02 Erasca, Inc. Tricyclic pyridones and pyrimidones
CA3247639A1 (en) 2022-05-06 2023-11-09 PAQ Therapeutics Inc. CHIMERAS TARGET KRAS-G12D PROTEOLYSIS
WO2023213269A1 (en) * 2022-05-06 2023-11-09 Zai Lab (Shanghai) Co., Ltd. Amide-substituted heterocyclic compounds as kras g12d modulators and uses thereof
WO2023220421A1 (en) * 2022-05-13 2023-11-16 Ranok Therapeutics (Hangzhou) Co. Ltd. Inhibitors of kras(g12d)
CR20240508A (es) * 2022-05-19 2024-12-20 Genentech Inc Compuestos aza-tetracíclicos de oxazepina y usos de los mismos
WO2023230190A1 (en) 2022-05-25 2023-11-30 Quanta Therapeutics, Inc. Pyrimidine based modulators and uses thereof
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
CN119630676A (zh) 2022-06-10 2025-03-14 百时美施贵宝公司 作为kras抑制剂的吡啶并[4,3-d]嘧啶衍生物
EP4540244A1 (en) * 2022-06-15 2025-04-23 Mirati Therapeutics, Inc. Prodrugs of pan-kras inhibitors
WO2023246903A1 (zh) * 2022-06-24 2023-12-28 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
CN117327102B (zh) * 2022-06-30 2026-04-28 重庆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
AU2023302139A1 (en) 2022-07-05 2024-12-19 Pfizer Inc. Pyrido[4,3-d]pyrimidine compounds
WO2024008179A1 (en) * 2022-07-07 2024-01-11 Beigene, Ltd. Heterocyclic compounds, compositions thereof, and methods of treatment therewith
TW202408520A (zh) * 2022-07-08 2024-03-01 大陸商貝達藥業股份有限公司 Kras g12d抑制劑及其在醫藥上的應用
CN117466796A (zh) * 2022-07-20 2024-01-30 上海皓鸿生物医药科技有限公司 一种((2R,7aS)-2-氟六氢-1H-吡咯嗪-7a-基)甲醇的制备方法
US20250145631A1 (en) 2022-07-21 2025-05-08 Astellas Pharma Inc. Heterocyclic compound acting on g12d mutant kras protein
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
AU2023314335A1 (en) 2022-07-29 2025-02-27 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Pharmaceutical composition comprising kras g12d inhibitor
CN119585278A (zh) * 2022-08-05 2025-03-07 杭州中美华东制药有限公司 具有KRas G12D抑制作用的化合物
IL318647A (en) 2022-08-05 2025-03-01 Kumquat Biosciences Inc Heterocyclic compounds and their uses
TW202412789A (zh) 2022-08-05 2024-04-01 日商安斯泰來製藥股份有限公司 用於誘導突變kras蛋白分解之雜環化合物
JP2025526744A (ja) 2022-08-11 2025-08-15 ブリストル－マイヤーズ スクイブ カンパニー Ｋｒａｓ阻害剤
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
JP2025527530A (ja) * 2022-08-16 2025-08-22 ブリストル－マイヤーズ スクイブ カンパニー Ｋｒａｓ阻害剤
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
US20260070929A1 (en) * 2022-08-24 2026-03-12 Ranok Therapeutics (Hangzhou) Co. Ltd. Methods and compositions for modulating kras(g12d)
WO2024045066A1 (en) * 2022-08-31 2024-03-07 Nikang Therapeutics, Inc. Alkylidene carbamate as kras inhibitors
EP4584276A1 (en) * 2022-09-07 2025-07-16 Bristol-Myers Squibb Company Kras g12d inhibitors
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
WO2024061333A1 (zh) * 2022-09-21 2024-03-28 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
EP4631942A1 (en) 2022-10-21 2025-10-15 Leadingtac Pharmaceutical (Shaoxing) Co., Ltd. Pan-kras degrading agent, and preparation method therefor and use thereof
JP2025536369A (ja) * 2022-10-21 2025-11-05 リーディングタック ファーマシューティカル（シャオシン）カンパニー，リミテッド Ｋｒａｓ ｇ１２ｄ分解剤及びその製造方法並びに応用
WO2024092420A1 (zh) * 2022-10-31 2024-05-10 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
AU2023382606A1 (en) 2022-11-14 2025-05-08 Amgen Inc. Macrocyclic kras inhibitors and methods of use
TW202430179A (zh) 2022-11-21 2024-08-01 美商樹線生物科學公司 螺環二氫哌喃并嘧啶ＫＲａｓ抑制劑
KR20250113487A (ko) 2022-11-28 2025-07-25 레드엑스 파마 리미티드 화합물
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
WO2024123102A1 (ko) * 2022-12-07 2024-06-13 에스케이바이오팜 주식회사 Kras g12d 저해제로서 신규한 3환 화합물 및 이의 용도
EP4640689A1 (en) 2022-12-20 2025-10-29 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Crystal form of kras g12d inhibitor and preparation method therefor
EP4640684A1 (en) 2022-12-23 2025-10-29 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
KR20260041941A (ko) * 2023-03-15 2026-03-27 콴타 테라퓨틱스, 인크. Kras 조절 인자 및 이의 용도
KR20250164300A (ko) 2023-03-30 2025-11-24 일라이 릴리 앤드 캄파니 KRas 억제제
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
EP4678643A1 (en) 2023-04-14 2026-01-14 Sunshine Lake Pharma Co., Ltd. Kras inhibitor compound, pharmaceutical composition thereof, and use thereof
EP4709729A1 (en) 2023-05-12 2026-03-18 Jazz Pharmaceuticals Ireland Ltd. Pyrazolo[4,3-f]quinazoline derivatives as modulators of g12d mutant kras useful for the treatment of cancer
CN121487732A (zh) * 2023-05-12 2026-02-06 荣山医药股份有限公司 用于治疗疾病的稠环kras抑制剂
CN121532183A (zh) * 2023-05-15 2026-02-13 米拉蒂治疗公司 Kras g12s和g12c抑制剂
WO2024243186A2 (en) * 2023-05-22 2024-11-28 Board Of Regents, The University Of Texas System Heterocyclic compounds as nras inhibitors
PE20252789A1 (es) 2023-05-24 2025-12-22 Kumquat Biosciences Inc Compuestos heterociclicos y usos de estos
CN121605110A (zh) 2023-06-06 2026-03-03 金橘生物科技公司 取代杂环化合物及其用途
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
CN121399088A (zh) * 2023-07-13 2026-01-23 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
CN121843946A (zh) * 2023-07-24 2026-04-10 米拉蒂治疗公司 Mrtx1133合成的方法和中间体
WO2025026903A1 (en) 2023-07-31 2025-02-06 Bayer Aktiengesellschaft Imidazo pyrimidine compounds for the treatment of cancer
CN121909197A (zh) 2023-08-22 2026-04-21 赛诺菲 2-(3,8-二氮杂双环[3.2.1]辛-3-基)-1,3,5-三嗪衍生物作为用于治疗癌症的kras g12d抑制剂
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
US20250101043A1 (en) 2023-09-27 2025-03-27 Eli Lilly And Company Kras inhibitors
CN121941690A (zh) 2023-10-03 2026-04-28 Paq医疗公司 Kras蛋白水解靶向嵌合体
CN121969634A (zh) * 2023-10-08 2026-05-01 成都海博为药业有限公司 一种稠环化合物及应用
US20250114346A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
US20250114339A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor
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
WO2025080956A1 (en) 2023-10-12 2025-04-17 Mirati Therapeutics, Inc. Mrtx1133 pharmaceutical compositions
AU2024361909A1 (en) 2023-10-20 2026-03-26 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025107579A1 (zh) * 2023-11-20 2025-05-30 贝达药业股份有限公司 一种靶向泛kras蛋白降解剂的化合物及其应用
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
WO2025145207A1 (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
WO2025194054A1 (en) * 2024-03-14 2025-09-18 Amgen Inc. Spirocyclic compounds as modulators of kras and uses thereof
TW202602882A (zh) * 2024-03-14 2026-01-16 美商安進公司 作為ｋｒａｓ調節劑的大環化合物及其用途
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
WO2025253326A1 (ko) * 2024-06-05 2025-12-11 에스케이바이오팜 주식회사 Kras 저해제로서 신규한 3환 화합물 및 이의 용도
WO2026059955A1 (en) 2024-09-11 2026-03-19 Eli Lilly And Company (3-((6-(2-amino-benzo[d]thiazol-4-yl)-3-(pyrrolidin-1-yl)-7,9-dihydrofuro[3,4-f]quinazolin-1-yl)amino)- piperidin-2-one derivatives as kras inhibitors for the treatment of cancer
WO2026075942A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors
WO2026075945A1 (en) 2024-10-01 2026-04-09 Eli Lilly And Company Kras inhibitors
WO2026080796A1 (en) 2024-10-11 2026-04-16 Mirati Therapeutics, Inc. Mrtx1133 capsule pharmaceutical compositions

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017201161A1 (en) * 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
US20180155348A1 (en) * 2016-09-29 2018-06-07 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
TW201922739A (zh) * 2017-09-08 2019-06-16 美商安進公司 Kras g12c抑制劑以及其使用方法
WO2020146613A1 (en) * 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors

Family Cites Families (203)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002053558A1 (en) 2001-01-02 2002-07-11 F.Hoffman-La Roche Ag Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists
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
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
EP2518063B1 (en) 2006-12-21 2017-02-01 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
WO2008103470A2 (en) 2007-02-21 2008-08-28 Trustees Of Columbia University In The City Of New York Oncogenic-ras-signal dependent lethal compounds
US20100298289A1 (en) 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
CA2729045A1 (en) 2008-07-31 2010-02-04 Philippe Bergeron Pyrimidine compounds, compositions and methods of use
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
JP2012524800A (ja) 2009-04-22 2012-10-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ モノアシルグリセロールリパーゼ阻害剤としてのアゼチジニルジアミド
EP2518064A1 (en) 2009-12-25 2012-10-31 Mochida Pharmaceutical Co., Ltd. Novel aryl urea derivative
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
HUE039713T2 (hu) 2012-06-08 2019-02-28 Sensorion H4 receptor inhibitorok tinnitus kezelésére
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
CA2904393A1 (en) 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EP3055290B1 (en) 2013-10-10 2019-10-02 Araxes Pharma LLC Inhibitors of kras g12c
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
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 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インヒビター
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
US10017540B2 (en) 2015-03-11 2018-07-10 California Institute Of Technology Cyclic peptide binder against oncogenic K-Ras
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
US10421764B2 (en) 2015-04-24 2019-09-24 H. Lee Moffitt Cancer Center And Research Institute, Inc. Mutant KRas inhibitors
AU2016258192B2 (en) 2015-05-06 2021-07-29 Leidos Biomedical Research, Inc. 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
EP3356351A1 (en) 2015-09-28 2018-08-08 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
WO2017058805A1 (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
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
EP3365686A4 (en) 2015-10-22 2019-03-27 The Scripps Research Institute REACTIVE CYSTEINSONS 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
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
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
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
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
CA3081983A1 (en) 2016-11-30 2018-06-07 Bantam Pharmaceutical, Llc Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases
US12150934B2 (en) 2016-11-30 2024-11-26 Bantam Pharmaceutical, Llc Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
KR20190095355A (ko) 2016-12-15 2019-08-14 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 암의 치료를 위한 조성물 및 방법
EP3558979B1 (en) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors
CN110366550A (zh) 2016-12-22 2019-10-22 美国安进公司 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
WO2018140513A1 (en) 2017-01-26 2018-08-02 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
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone 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
EP3573966A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused n-heterocyclic compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
EP3612526A2 (en) 2017-04-20 2020-02-26 The Regents of the University of California K-ras modulators
EP3832583A4 (en) 2018-07-31 2021-12-08 Honda Motor Co., Ltd. PERFORMANCE FORECAST SYSTEM, PERFORMANCE FORECAST DEVICE, PERFORMANCE FORECAST METHOD, PROGRAM AND STORAGE MEDIUM
CN109413550B (zh) 2018-09-30 2021-03-09 华为技术有限公司 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
US20220193242A1 (en) 2019-02-07 2022-06-23 The Regents Of The University Of California Immunophilin-dependent inhibitors and uses thereof
US20220221355A1 (en) 2019-02-11 2022-07-14 Mesomat Inc. Sensing fibers for structural health monitoring
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
CN114026116A (zh) 2019-02-20 2022-02-08 弗雷德哈钦森癌症研究中心 Ras新抗原特异性结合蛋白及其用途
GB201902392D0 (en) 2019-02-21 2019-04-10 Cambridge Entpr Ltd Modular binding proteins
WO2020176693A2 (en) 2019-02-26 2020-09-03 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
KR102934231B1 (ko) 2019-03-05 2026-03-06 아스트라제네카 아베 항암제로 유용한 융합 삼환식 화합물
US12117170B2 (en) 2019-03-05 2024-10-15 Questor Technology Inc. Gas incinerator system
EP3941938A1 (en) 2019-03-06 2022-01-26 Dana-Farber Cancer Institute, Inc. T cell receptors specific to b-cell maturation antigen for treatment of cancer
US20220160714A1 (en) 2019-03-22 2022-05-26 Icahn School Of Medicine At Mount Sinai Methods for treating colorectal cancer
BR112021018739A2 (pt) 2019-03-29 2022-05-03 Dicerna Pharmaceuticals Inc Composições e métodos para o tratamento de doenças ou distúrbios associados a kras
CA3134825A1 (en) 2019-03-29 2020-10-08 Kura Oncology, Inc. Methods of treating squamous cell carcinomas with farnesyltransferase inhibitors
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
KR20220012255A (ko) 2019-04-28 2022-02-03 젠플리트 테라퓨틱스 (상하이) 아이엔씨. 옥사아자퀴나졸린-7(8h)-케톤 화합물, 이의 제조 방법 및 이의 약학적 응용
US11518758B2 (en) 2019-05-10 2022-12-06 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
PE20220597A1 (es) 2019-05-10 2022-04-22 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos
EP3969449B1 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
US11879013B2 (en) 2019-05-14 2024-01-23 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
JP7502337B2 (ja) 2019-05-20 2024-06-18 カリフォルニア インスティチュート オブ テクノロジー Ｋｒａｓ ｇ１２ｃインヒビター及びその使用
AU2020277398B2 (en) 2019-05-21 2026-01-29 Amgen Inc. Solid state forms
CN114437065A (zh) 2019-05-21 2022-05-06 益方生物科技(上海)股份有限公司 杂环化合物，其制备方法和用途
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
WO2020236947A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
US12577278B2 (en) 2019-06-07 2026-03-17 Emory University KRAS G12V mutant binds to JAK1, inhibitors, pharmaceutical compositions, and methods related thereto
CA3141405A1 (en) 2019-06-12 2020-12-17 H. Charles Manning Amino acid transport inhibitors and the uses thereof
CN114269715A (zh) 2019-06-12 2022-04-01 范德比尔特大学 作为氨基酸转运抑制剂的二苄基胺
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
JP7756069B6 (ja) 2019-08-02 2025-11-27 上海済▲ユウ▼医薬科技股▲フン▼有限公司 四環式化合物、その調製と使用の方法
CN112341457A (zh) 2019-08-07 2021-02-09 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CN114174298B (zh) 2019-08-14 2023-08-01 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
WO2021031952A1 (zh) 2019-08-16 2021-02-25 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
MX2022002108A (es) 2019-08-22 2022-03-17 Univ Michigan Regents Metodo para tratar canceres asociados con kras.
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
MX2022002465A (es) * 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021043322A1 (zh) 2019-09-06 2021-03-11 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
EP3819300A4 (en) 2019-09-06 2021-11-24 Wellmarker Bio Co., Ltd. THERAPEUTIC COMPOSITION BASED ON BIOMARKERS
WO2021050732A1 (en) 2019-09-10 2021-03-18 The Board Of Trustees Of The Leland Stanford Junior University Methods of treating kras mutant cancers
US20230002371A1 (en) 2019-09-13 2023-01-05 Biotheryx, Inc. Ras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
US20220402916A1 (en) 2019-09-18 2022-12-22 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
WO2021052499A1 (zh) 2019-09-20 2021-03-25 上海济煜医药科技有限公司 稠合吡啶酮类化合物及其制备方法和应用
CN114502165A (zh) 2019-09-23 2022-05-13 苏州浦合医药科技有限公司 Shp2抑制剂及其用途
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
TW202115062A (zh) 2019-09-25 2021-04-16 大陸商北京加科思新藥研發有限公司 Kras突變蛋白抑制劑
WO2021058018A1 (en) 2019-09-29 2021-04-01 Beigene, Ltd. Inhibitors of kras g12c
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
CN114555586B (zh) 2019-10-10 2023-06-23 信达生物制药(苏州)有限公司 Krasg12c蛋白抑制剂及其制备方法和用途
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
US12331035B2 (en) 2019-10-23 2025-06-17 Sk Biopharmaceuticals Co., Ltd. Bicyclic compound and use thereof
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
EP4048671B1 (en) 2019-10-24 2026-03-18 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
JP7601869B2 (ja) 2019-10-30 2024-12-17 ▲勁▼方医▲薬▼科技（上海）有限公司 置換された複素環－環系化合物、その調製方法及び医薬への応用
WO2021084765A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
US20230023023A1 (en) 2019-10-31 2023-01-26 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
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
AU2020377925A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
IL322454A (en) 2019-11-04 2025-09-01 Revolution Medicines Inc ras inhibitors
BR112022007535A2 (pt) 2019-11-07 2022-07-12 Chugai Pharmaceutical Co Ltd Composto peptídico cíclico tendo ação inibitória de kras
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
CN114630832A (zh) 2019-11-15 2022-06-14 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
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC 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
WO2021109737A1 (zh) 2019-12-02 2021-06-10 上海璎黎药业有限公司 一种含氧杂环化合物、其制备方法及应用
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
WO2021126799A1 (en) 2019-12-18 2021-06-24 Merck Sharp & Dohme Corp. Macrocyclic peptides as potent inhibitors of k-ras g12d mutant
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
IL293962B2 (en) 2019-12-19 2025-10-01 Jacobio Pharmaceuticals Co Ltd Mutant KRAS protein inhibitors
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
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
CA3164995A1 (en) 2019-12-20 2021-06-24 Erasca, Inc. Tricyclic pyridones and pyrimidones
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
JP7850663B2 (ja) 2019-12-27 2026-04-23 ウィゲン・バイオメディシン・テクノロジー・（シャンハイ）・カンパニー・リミテッド スピロ環含有キナゾリン化合物
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
WO2021139748A1 (en) 2020-01-08 2021-07-15 Ascentage Pharma (Suzhou) Co., Ltd. Spirocyclic tetrahydroquinazolines
US20210269434A1 (en) 2020-01-10 2021-09-02 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
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
KR102396930B1 (ko) 2020-01-15 2022-05-12 한국과학기술연구원 피리도[3,4-d]피리미딘 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
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
CN114845997B (zh) 2020-02-24 2024-03-29 上海喆邺生物科技有限公司 芳香类化合物及其在制备抗肿瘤药物中的应用
US20210292330A1 (en) 2020-02-28 2021-09-23 Erasca, Inc. Pyrrolidine-fused heterocycles
CN114901663B (zh) 2020-03-02 2024-07-02 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
KR20210111711A (ko) 2020-03-03 2021-09-13 웰마커바이오 주식회사 Kras 돌연변이 및 활성화된 ron이 존재하는 암의 예방 또는 치료용 약학 조성물
WO2021178741A1 (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
CN115397413A (zh) 2020-03-05 2022-11-25 密歇根大学董事会 Egfr、kras、braf和其他靶标的抑制剂及其用途
AU2021233058B2 (en) 2020-03-12 2024-05-16 D3 Bio(Wuxi) Co., Ltd Pyrimidoheterocyclic compounds and application thereof
TW202144345A (zh) 2020-03-17 2021-12-01 大陸商北京加科思新藥研發有限公司 Ｋｒａｓ突變蛋白抑制劑
CA3170068A1 (en) 2020-03-25 2021-09-30 Yuli Xie Spiro ring-containing quinazoline compound
WO2021197499A1 (zh) 2020-04-03 2021-10-07 南京明德新药研发有限公司 八氢吡嗪并二氮杂萘啶二酮类化生物
CN115803030A (zh) 2020-04-06 2023-03-14 阿维纳斯企业公司 用于kras靶向降解的化合物和方法
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
AU2021254794A1 (en) 2020-04-16 2022-12-15 Incyte Corporation Fused tricyclic KRAS inhibitors
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
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
CA3177261A1 (en) 2020-04-29 2021-11-04 Shanghai Ringene Biopharma Co., Ltd. Benzothiazolyl biaryl compound, and preparation method and use
WO2021219072A1 (zh) 2020-04-30 2021-11-04 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
US11739102B2 (en) 2020-05-13 2023-08-29 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
CA3180314A1 (en) 2020-05-29 2021-12-02 John Graeme HODGSON Methods of treating cancer in patients with an anomalous kras gene or deletions within chromosome 9
JP7808058B2 (ja) 2020-06-02 2026-01-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング がんを治療するための縮合環化２－アミノ－３－シアノチオフェン及び誘導体
WO2021244603A1 (en) 2020-06-04 2021-12-09 Shanghai Antengene Corporation Limited Inhibitors of kras g12c protein and uses thereof
US20230202981A1 (en) 2020-06-04 2023-06-29 Baskaran Pillai Novel small molecules for targeted degradation of untargetable kras in cancer therapy
WO2021248082A1 (en) 2020-06-05 2021-12-09 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
US20230026856A1 (en) 2020-06-05 2023-01-26 Sparcbio Llc Heterocyclic compounds and methods of use 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
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
US20230227466A1 (en) 2020-06-18 2023-07-20 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
WO2022002102A1 (en) 2020-06-30 2022-01-06 InventisBio Co., Ltd. Quinazoline compounds, preparation methods and uses thereof
WO2022015375A1 (en) 2020-07-16 2022-01-20 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
JP7584815B2 (ja) 2020-08-02 2024-11-18 上▲海▼▲哲▼▲イェ▼生物科技有限公司 抗腫瘍薬物における芳香族化合物及びその用途
EP4192585A4 (en) 2020-08-04 2024-08-21 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017201161A1 (en) * 2016-05-18 2017-11-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
US20180155348A1 (en) * 2016-09-29 2018-06-07 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
TW201922739A (zh) * 2017-09-08 2019-06-16 美商安進公司 Kras g12c抑制劑以及其使用方法
WO2020146613A1 (en) * 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors

Also Published As

Publication number Publication date
AU2020337938B2 (en) 2025-09-25
JP2025063176A (ja) 2025-04-15
TW202523663A (zh) 2025-06-16
CO2022003782A2 (es) 2022-07-08
JP7622043B2 (ja) 2025-01-27
CA3148745A1 (en) 2021-03-04
US11453683B1 (en) 2022-09-27
EP4021444A1 (en) 2022-07-06
JP2022546043A (ja) 2022-11-02
CN114615981B (zh) 2024-04-12
WO2021041671A1 (en) 2021-03-04
US20240309020A1 (en) 2024-09-19
EP4021444A4 (en) 2023-01-04
IL290845B1 (en) 2026-01-01
MX2022002465A (es) 2022-05-19
BR112022003543A2 (pt) 2022-05-24
CN114615981A (zh) 2022-06-10
PH12022550469A1 (en) 2023-02-27
IL290845A (en) 2022-04-01
TWI912127B (zh) 2026-01-11
US11964989B2 (en) 2024-04-23
KR20220071193A (ko) 2022-05-31
US20230077225A1 (en) 2023-03-09
ZA202202362B (en) 2022-09-28
CL2022000447A1 (es) 2022-10-21
TW202122396A (zh) 2021-06-16
AU2020337938A1 (en) 2022-03-17

Similar Documents

Publication Publication Date Title
TWI874443B (zh) KRas G12D抑制劑
TWI809005B (zh) Kras g12c抑制劑
TWI680970B (zh) 可做為ｓｕｍｏ活化酵素抑制劑之雜芳基化合物
TWI781342B (zh) KEAP1-Nrf2蛋白-蛋白交互作用抑制劑
WO2022076625A1 (en) Modulators of cystic fibrosis transmembrane conductance regulator
TWI845638B (zh) Ｅｅｄ及ｐｒｃ２調節劑之巨環唑并吡啶衍生物
TWI739779B (zh) 布魯頓氏酪胺酸激酶抑制劑及其使用方法
TW201718536A (zh) 可作為ＴＮＦα調節劑之雜環化合物
CN104470925A (zh) 作为激酶抑制剂的咪唑并三嗪甲腈
CN117813307A (zh) 白介素-1受体相关激酶的双官能降解物及其治疗用途
TW201718537A (zh) 做為人類免疫缺陷病毒複製抑制劑之吡啶－３－基乙酸衍生物
KR20230123471A (ko) 화합물, 조성물 및 방법
TW202417449A (zh) Cdk2抑制劑及使用彼等之方法
JP2020503348A (ja) ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−３−イル酢酸誘導体
CN113149996A (zh) 一种作为cdk9抑制剂的多环酰胺类衍生物、其制备方法及用途
HK40076948B (zh) Kras g12d抑制剂
HK40076948A (en) Kras g12d inhibitors
KR20260062970A (ko) 거대고리 화합물 및 이의 제조 방법과 용도
TW202613115A (zh) Btk降解劑及其用途
HK40101612A (zh) Shp2磷酸酶抑制剂及其使用方法
HK40120619A (zh) 含吲唑的巨环化合物及其用途
HK40044783A (en) Kras g12c inhibitors
HK40044087B (zh) Shp2磷酸酶抑制剂及其使用方法
HK40044783B (zh) Kras g12c抑制剂
HK1248678B (zh) 核受体调节剂