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CO2022003782A2 - Inhibidores de kras g12d - Google Patents

Inhibidores de kras g12d

Info

Publication number
CO2022003782A2
CO2022003782A2 CONC2022/0003782A CO2022003782A CO2022003782A2 CO 2022003782 A2 CO2022003782 A2 CO 2022003782A2 CO 2022003782 A CO2022003782 A CO 2022003782A CO 2022003782 A2 CO2022003782 A2 CO 2022003782A2
Authority
CO
Colombia
Prior art keywords
kras
inhibitors
compounds
relates
present
Prior art date
Application number
CONC2022/0003782A
Other languages
English (en)
Inventor
Xiaolun Wang
Aaron Craig Burns
James Gail Christensen
John Michael Ketcham
John David Lawson
Matthew Arnold Marx
Christopher Ronald Smith
Shelley Allen
James Francis Blake
Mark Joseph Chicarelli
Joshua Ryan Dahlke
Donghua Dai
Jay Bradford Fell
John Peter Fischer
Macedonio J Mejia
Brad Newhouse
Phong Nguyen
Jacob Matthew O'leary
Spencer Pajk
Martha E Rodriguez
Pavel Savechenkov
Tony P Tang
Guy P A Vigers
Qian Zhao
Dean Russell Kahn
John Gaudino
Michael Christopher Hilton
Original Assignee
Array Biopharma Inc
Mirati Therapeutics Inc
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 Array Biopharma Inc, Mirati Therapeutics Inc filed Critical Array Biopharma Inc
Publication of CO2022003782A2 publication Critical patent/CO2022003782A2/es

Links

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)

Abstract

La presente invención se refiere a compuestos que inhiben KRas G12D. En particular, la presente invención se refiere a compuestos que inhiben la actividad de KRas G12D, composiciones farmacéuticas que comprenden los compuestos y métodos de uso de las mismas.
CONC2022/0003782A 2019-08-29 2022-03-29 Inhibidores de kras g12d CO2022003782A2 (es)

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
CO2022003782A2 true CO2022003782A2 (es) 2022-07-08

Family

ID=74683570

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0003782A CO2022003782A2 (es) 2019-08-29 2022-03-29 Inhibidores de kras g12d

Country Status (15)

Country Link
US (3) US11453683B1 (es)
EP (1) EP4021444A4 (es)
JP (1) JP7622043B2 (es)
KR (1) KR20220071193A (es)
CN (1) CN114615981B (es)
AU (1) AU2020337938A1 (es)
BR (1) BR112022003543A2 (es)
CA (1) CA3148745A1 (es)
CL (1) CL2022000447A1 (es)
CO (1) CO2022003782A2 (es)
IL (1) IL290845A (es)
MX (1) MX2022002465A (es)
TW (1) TW202122396A (es)
WO (1) WO2021041671A1 (es)
ZA (1) ZA202202362B (es)

Families Citing this family (176)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3849536A4 (en) 2018-09-10 2022-06-29 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
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
AU2020337938A1 (en) 2019-08-29 2022-03-17 Array Biopharma Inc. KRas G12D inhibitors
EP4034123A4 (en) 2019-09-24 2023-11-01 Mirati Therapeutics, Inc. COMBINATION THERAPIES
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
IL294048A (en) 2019-12-20 2022-08-01 Mirati Therapeutics Inc Sos1 inhibitors
US20230279025A1 (en) * 2020-07-16 2023-09-07 Mirati Therapeutics, Inc. Kras g12d inhibitors
EP4192585A4 (en) * 2020-08-04 2024-08-21 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2022042630A1 (en) * 2020-08-26 2022-03-03 InventisBio Co., Ltd. Heteroaryl compounds, preparation methods and uses thereof
KR20230081726A (ko) 2020-09-03 2023-06-07 레볼루션 메디슨즈, 인크. Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도
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
US20240034733A1 (en) * 2020-11-03 2024-02-01 Mirati Therapeutics, Inc. Kras g12d inhibitors
AU2021401232A1 (en) * 2020-12-15 2023-06-22 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
TW202241869A (zh) * 2020-12-22 2022-11-01 大陸商上海科州藥物研發有限公司 作為ｋｒａｓ抑制劑的雜環化合物的製備及其應用方法
EP4269404A4 (en) * 2020-12-25 2024-12-04 Xizang Haisco Pharmaceutical Co., Ltd. KETOHEXOKINASE INHIBITORS AND USE THEREOF
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
TW202245751A (zh) 2021-02-15 2022-12-01 日商安斯泰來製藥股份有限公司 用於誘發g12d突變kras蛋白之分解之喹唑啉化合物
JPWO2022173033A1 (es) 2021-02-15 2022-08-18
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
CN116964057A (zh) * 2021-03-10 2023-10-27 贝达医药公司 作为kras抑制剂的吡啶并嘧啶衍生物
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
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
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
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
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
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
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
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
WO2022194191A1 (en) * 2021-03-16 2022-09-22 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of kras g12d
BR112023018785A2 (pt) * 2021-03-17 2023-12-12 Genfleet Therapeutics Shanghai Inc Composto cíclico fundido com pirimidina, método de preparação do mesmo e uso do mesmo
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
CN115141215B (zh) * 2021-03-30 2023-09-15 上海德琪医药科技有限公司 Kras g12d蛋白抑制剂和其用途
CN117715915A (zh) * 2021-04-09 2024-03-15 杭州英创医药科技有限公司 作为kras g12d抑制剂的杂环化合物
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
CN116157401A (zh) * 2021-04-28 2023-05-23 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
AU2022265682A1 (en) * 2021-04-29 2023-11-09 Amgen Inc. 2-aminobenzothiazole compounds and methods of use thereof
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
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
TW202337890A (zh) * 2021-04-30 2023-10-01 大陸商江蘇恆瑞醫藥股份有限公司 橋環類化合物、其製備方法及其在醫藥上的應用
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
UY39779A (es) * 2021-05-21 2023-01-31 Blossomhill Therapeutics Inc Compuestos macrocíclicos para tratar enfermedades
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
CA3217694A1 (en) 2021-05-24 2022-12-01 Zusheng XU Nitrogen-containing heterocyclic compound, method for preparing same and use of same
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
CA3216294A1 (en) 2021-05-28 2022-12-01 Redx Pharma Plc. Compounds
JP2024522187A (ja) 2021-06-09 2024-06-11 イーライ リリー アンド カンパニー Ｋｒａｓ ｇ１２ｄ阻害剤としての置換縮合アジン
BR112023025869A2 (pt) 2021-06-10 2024-02-27 Redx Pharma Plc Derivados de quinazolina úteis como inibidores de ras
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
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
TW202317587A (zh) * 2021-06-21 2023-05-01 大陸商江蘇恆瑞醫藥股份有限公司 稠合四環類化合物、其製備方法及其在醫藥上的應用
WO2022271823A1 (en) * 2021-06-23 2022-12-29 Newave Pharmaceutical Inc. Mutant kras modulators and uses thereof
US20240368192A1 (en) 2021-06-30 2024-11-07 Shanghai Allist Pharmaceuticals Co., Ltd. Nitrogen-Containing Heterocyclic Compound, and Preparation Method Therefor, Intermediate Thereof, and Application 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
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
EP4370522A1 (en) * 2021-07-14 2024-05-22 Nikang Therapeutics, Inc. Alkylidene derivatives as kras inhibitors
WO2023283933A1 (en) * 2021-07-16 2023-01-19 Silexon Biotech Co., Ltd. Compounds useful as kras g12d inhibitors
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
CA3226720A1 (en) * 2021-07-23 2023-01-26 Suzhou Zanrong Pharma Limited Kras g12d inhibitors and uses thereof
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
CA3228310A1 (en) * 2021-08-10 2023-02-16 Michael M. YAMANO Heterocyclic compounds and methods of use
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
EP4387967A1 (en) * 2021-08-18 2024-06-26 Jacobio Pharmaceuticals Co., Ltd. 1, 4-oxazepane derivatives and uses thereof
WO2023020521A1 (en) * 2021-08-18 2023-02-23 Jacobio Pharmaceuticals Co., Ltd. Pyridine fused pyrimidine derivatives and use 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
CN116284055A (zh) * 2021-09-10 2023-06-23 润佳（苏州）医药科技有限公司 一种kras抑制剂及其用途
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
US20240409558A1 (en) 2021-09-13 2024-12-12 Biomea Fusion, Inc. Irreversible inhibitors of kras
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
WO2023059594A1 (en) * 2021-10-05 2023-04-13 Mirati Therapeutics, Inc. Combinations of kras g12d inhibitors with pi3ka inhibitors and related methods of treatment
WO2023059598A1 (en) * 2021-10-05 2023-04-13 Mirati Therapeutics, Inc. Combination therapies of kras g12d inhibitors with shp-2 inhibitors
CN118369119A (zh) * 2021-10-05 2024-07-19 米拉蒂治疗股份有限公司 KRAS G12D抑制剂与泛ErbB家族抑制剂的组合疗法
MX2024004214A (es) * 2021-10-05 2024-07-29 Mirati Therapeutics Inc Combinaciones de inhibidores de kras g12d con irinotecán y métodos de tratamiento relacionados.
CN118382459A (zh) * 2021-10-05 2024-07-23 米拉蒂治疗股份有限公司 Kras g12d抑制剂与sos1抑制剂的组合疗法
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
CN115974896A (zh) * 2021-10-15 2023-04-18 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
WO2023097227A1 (en) * 2021-11-24 2023-06-01 Merck Sharp & Dohme Llc Small molecule inhibitors of kras mutated proteins
JP2024545416A (ja) * 2021-11-30 2024-12-06 ベータ・ファーマ・インコーポレイテッド Ｋｒａｓオンコプロテイン阻害剤としての縮合ピリミジン誘導体
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
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
EP4442686A1 (en) 2021-12-02 2024-10-09 Abbisko Therapeutics Co., Ltd Kras inhibitors, preparation method therefor, and pharmaceutical use thereof
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
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
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
WO2023134465A1 (zh) * 2022-01-11 2023-07-20 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
TWI841200B (zh) * 2022-01-21 2024-05-01 大陸商上海湃隆生物科技有限公司 雜環類化合物、藥物組成物及其應用
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
CN116514847A (zh) 2022-01-30 2023-08-01 上海医药集团股份有限公司 一种喹啉类化合物及其应用
WO2023154766A1 (en) 2022-02-09 2023-08-17 Quanta Therapeutics, Inc. Kras modulators and uses thereof
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
KR20240163107A (ko) 2022-03-11 2024-11-18 컴쿼트 바이오사이언시즈 인크. 헤테로환 화합물 및 이의 용도
KR20240162042A (ko) 2022-03-11 2024-11-14 아스텔라스세이야쿠 가부시키가이샤 G12d 변이 kras 단백의 분해를 유도하기 위한 복소환 화합물
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
CN119095853A (zh) 2022-03-25 2024-12-06 伊莱利利公司 Kras抑制剂
JPWO2023190748A1 (es) 2022-03-31 2023-10-05
CN116891488A (zh) 2022-04-11 2023-10-17 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
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
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2023205719A1 (en) 2022-04-21 2023-10-26 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2023212549A1 (en) * 2022-04-26 2023-11-02 Erasca, Inc. Tricyclic pyridones and pyrimidones
TW202400609A (zh) * 2022-04-26 2024-01-01 美商伊瑞斯卡公司 三環吡啶酮及嘧啶酮
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)
KR20250013185A (ko) * 2022-05-19 2025-01-31 제넨테크, 인크. 아자-테트라시클릭 옥사제핀 화합물 및 이의 용도
AU2023276596A1 (en) 2022-05-25 2025-01-02 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
US20240067662A1 (en) 2022-06-10 2024-02-29 Bristol-Myers Squibb Company Kras inhibitors
WO2023244600A1 (en) * 2022-06-15 2023-12-21 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
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
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
TW202409051A (zh) * 2022-07-27 2024-03-01 大陸商江蘇恆瑞醫藥股份有限公司 稠環類化合物、其製備方法及其在醫藥上的應用
WO2024029613A1 (ja) * 2022-08-05 2024-02-08 アステラス製薬株式会社 変異ｋｒａｓタンパクの分解を誘導するための複素環化合物
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
AU2023320565A1 (en) 2022-08-05 2025-01-23 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2024036270A1 (en) 2022-08-11 2024-02-15 Bristol-Myers Squibb Company Kras inhibitors
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
WO2024044334A2 (en) * 2022-08-24 2024-02-29 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
WO2024054926A1 (en) * 2022-09-07 2024-03-14 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
WO2024056063A1 (zh) * 2022-09-16 2024-03-21 南京明德新药研发有限公司 含六氢螺环[环丙烷-1,2'-吡咯嗪]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
CN117917416A (zh) * 2022-10-21 2024-04-23 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
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
JP2024071370A (ja) * 2022-11-14 2024-05-24 アムジエン・インコーポレーテツド 大環状ｋｒａｓ阻害剤及び使用方法
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
WO2024115890A1 (en) 2022-11-28 2024-06-06 Redx Pharma Plc 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
WO2024123102A1 (ko) * 2022-12-07 2024-06-13 에스케이바이오팜 주식회사 Kras g12d 저해제로서 신규한 3환 화합물 및 이의 용도
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
WO2024131827A1 (zh) * 2022-12-23 2024-06-27 上海和誉生物医药科技有限公司 一种kras g12d抑制剂及其应用
CN115894503A (zh) * 2022-12-30 2023-04-04 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
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
US20240343736A1 (en) 2023-03-30 2024-10-17 Eli Lilly And Company Kras inhibitors
JP2024146897A (ja) 2023-03-31 2024-10-15 イーライ リリー アンド カンパニー Ｋｒａｓ阻害剤
WO2024238343A1 (en) * 2023-05-12 2024-11-21 Blossomhill Therapeutics, Inc. Fused ring kras inhibitors for treating disease
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
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2024261257A1 (en) 2023-06-22 2024-12-26 Astellas Pharma Inc. Pharmaceutical composition comprising a quinazoline compound
WO2024261256A1 (en) 2023-06-22 2024-12-26 Astellas Pharma Inc. PHARMACEUTICAL COMPOSITION COMPRISING A pan-KRAS DEGRADER
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

Family Cites Families (207)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2241891T3 (es) 2001-01-02 2005-11-01 F. Hoffmann-La Roche Ag Derivados de quinazolona como antagonistas de receptores adrenergicos alfa-1a/b.
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
BRPI0911688A2 (pt) 2008-07-31 2015-07-28 Genentech Inc "compostos de pirimidina, composições e métodos de uso"
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
CA2759614C (en) 2009-04-22 2017-09-19 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
US20110269244A1 (en) 2009-12-30 2011-11-03 Petter Russell C Ligand-directed covalent modification of 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
CN104582703A (zh) * 2012-06-08 2015-04-29 森索睿翁公司 用于治疗耳鸣的h4受体抑制剂
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.
EP3401314B1 (en) 2013-03-15 2023-11-08 Araxes Pharma LLC Covalent inhibitors of kras g12c
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
CN106488910B (zh) 2013-10-10 2020-07-31 亚瑞克西斯制药公司 Kras g12c的抑制剂
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
WO2015184349A2 (en) 2014-05-30 2015-12-03 The Trustees Of Columbia University In The City Of New York Multivalent ras binding compounds
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
AR102094A1 (es) 2014-09-25 2017-02-01 Araxes Pharma Llc Inhibidores de proteínas kras con una mutación g12c
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
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
WO2016172692A1 (en) 2015-04-24 2016-10-27 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
WO2017053722A1 (en) 2015-09-24 2017-03-30 Ionis Pharmaceuticals, Inc. Modulators of kras expression
EP3356339A1 (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
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356353A1 (en) 2015-09-28 2018-08-08 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
WO2017058768A1 (en) 2015-09-28 2017-04-06 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
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
JP6953400B2 (ja) 2015-10-22 2021-10-27 ザ スクリプス リサーチ インスティテュート システイン反応性プローブとその使用
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
WO2017100546A1 (en) 2015-12-09 2017-06-15 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
MX2018013983A (es) * 2016-05-18 2019-08-16 Mirati Therapeutics Inc Inhibidores g12c de kras.
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
US10280172B2 (en) * 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
JP2019534260A (ja) 2016-10-07 2019-11-28 アラクセス ファーマ エルエルシー Ｒａｓの阻害剤としての複素環式化合物およびその使用方法
BR112019011035A2 (pt) 2016-11-30 2019-10-15 Bantam Pharmaceutical Llc métodos de uso de compostos pirazol e pirazol substituído e para o tratamento de doenças hiperproliferativas
AU2017366901B2 (en) 2016-11-30 2022-09-29 Bantam Pharmaceutical, Llc Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases
BR112019012263A2 (pt) 2016-12-15 2020-01-28 Univ California composições e métodos para tratar câncer
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
CN110167928A (zh) 2016-12-22 2019-08-23 勃林格殷格翰国际有限公司 作为sos1抑制剂的新型经苄基氨基取代的喹唑啉和衍生物
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic 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
EP3573964A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573966A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused n-heterocyclic compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
MX2019012532A (es) 2017-04-20 2019-12-02 Univ California Moduladores de k-ras.
IL293443A (en) 2017-09-08 2022-07-01 Amgen Inc Inhibitors of kras g12c and methods of using the same
US11545829B2 (en) 2018-07-31 2023-01-03 Honda Motor Co., Ltd. Power prediction system, power prediction device, power prediction method, program, and storage medium
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
CN111193490A (zh) 2018-11-14 2020-05-22 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
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
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
WO2020172332A1 (en) 2019-02-20 2020-08-27 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
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
CA3132675A1 (en) 2019-03-05 2020-09-10 Questor Technology Inc. Gas incinerator system
JP7453989B2 (ja) 2019-03-05 2024-03-21 アストラゼネカ・アクチエボラーグ 抗癌剤として有用な縮合三環式化合物
AU2020231218A1 (en) 2019-03-06 2021-09-16 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
JP2022527495A (ja) 2019-03-29 2022-06-02 クラ オンコロジー， インコーポレイテッド ファルネシルトランスフェラーゼ阻害剤による扁平上皮癌の治療方法
SG11202110174PA (en) 2019-03-29 2021-10-28 Dicerna Pharmaceuticals Inc Compositions and methods for the treatment of kras associated diseases or disorders
KR102222693B1 (ko) 2019-04-04 2021-03-04 금정제약 주식회사 H-rev107 유래 펩타이드의 신규한 용도
US20220227740A1 (en) 2019-04-15 2022-07-21 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
US11530206B2 (en) 2019-05-10 2022-12-20 Deciphera Pharmaceuticals, Llc Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
TW202108574A (zh) 2019-05-10 2021-03-01 美商迪賽孚爾製藥有限公司 雜芳基胺基嘧啶醯胺自噬抑制劑及其使用方法
AU2020276695A1 (en) 2019-05-13 2021-12-23 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
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
AU2020277398A1 (en) 2019-05-21 2021-12-09 Amgen Inc. Solid state forms
PE20220504A1 (es) 2019-05-21 2022-04-07 Amgen Inc Formas en estado solido
KR20220010542A (ko) 2019-05-21 2022-01-25 인벤티스바이오 컴퍼니 리미티드 헤테로 고리 화합물, 이의 제조 방법 및 용도
WO2020247914A1 (en) 2019-06-07 2020-12-10 Emory University Kras g12v mutant binds to jak1, inhibitors, pharmaceutical compositions, and methods related thereto
JP2022536728A (ja) 2019-06-12 2022-08-18 ヴァンダービルト ユニバーシティー アミノ酸輸送阻害剤としてのジベンジルアミン類
AU2020291464A1 (en) 2019-06-12 2022-02-03 Vanderbilt University Amino acid transport inhibitors and the uses thereof
CN114040914B (zh) 2019-07-01 2024-10-22 江苏恒瑞医药股份有限公司 喹唑啉酮类衍生物、其制备方法及其在医药上的应用
CN112300195B (zh) 2019-08-02 2021-12-24 上海济煜医药科技有限公司 四并环类化合物及其制备方法和应用
US20210040089A1 (en) 2019-08-07 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
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
KR20220050143A (ko) 2019-08-22 2022-04-22 더 리젠츠 오브 더 유니버시티 오브 미시간 Kras-관련 암 치료 방법
WO2021037018A1 (zh) 2019-08-26 2021-03-04 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
AU2020337938A1 (en) 2019-08-29 2022-03-17 Array Biopharma Inc. KRas G12D inhibitors
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
JP2022554042A (ja) 2019-09-06 2022-12-28 ウェルマーカー・バイオ・カンパニー・リミテッド バイオマーカー型治療用組成物
CN114375197A (zh) 2019-09-10 2022-04-19 小利兰·斯坦福大学理事会 治疗kras突变癌症的方法
WO2021051034A1 (en) 2019-09-13 2021-03-18 Biotheryx, Inc. Ras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
EP4031542A4 (en) 2019-09-18 2023-10-25 Merck Sharp & Dohme LLC KRAS G12C MUTANT SMALL MOLECULE INHIBITORS
CN114728968B (zh) 2019-09-20 2024-11-15 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
US20230010886A1 (en) 2019-09-23 2023-01-12 Suzhou Puhe BioPharma Co., Ltd. Shp2 inhibitors and uses thereof
EP4034123A4 (en) 2019-09-24 2023-11-01 Mirati Therapeutics, Inc. COMBINATION THERAPIES
US20210094919A1 (en) 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CN114929706A (zh) 2019-09-29 2022-08-19 百济神州有限公司 Kras g12c的抑制剂
WO2021063346A1 (zh) 2019-09-30 2021-04-08 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
WO2021068898A1 (zh) 2019-10-10 2021-04-15 信达生物制药(苏州)有限公司 新颖的kras g12c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
WO2021076655A1 (en) 2019-10-15 2021-04-22 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
CN112694475A (zh) 2019-10-23 2021-04-23 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
EP4050006B1 (en) 2019-10-23 2025-01-01 SK Biopharmaceuticals Co., Ltd. Bicyclic compound and use thereof
WO2021081212A1 (en) 2019-10-24 2021-04-29 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
JOP20220101A1 (ar) 2019-10-28 2023-01-30 Merck Sharp & Dohme مثبطات صغيرة الجزئ لطافر G12C لبروتين ساركوما جرذان Kirsten (KRAS)
EP4053118B1 (en) 2019-10-30 2024-10-09 Genfleet Therapeutics (Shanghai) Inc. Substituted heterocyclic fused cyclic compound, preparation method therefor and pharmaceutical use thereof
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
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
CN114901366A (zh) 2019-11-04 2022-08-12 锐新医药公司 Ras抑制剂
KR20220109407A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
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
PE20221323A1 (es) 2019-11-07 2022-09-09 Chugai Pharmaceutical Co Ltd Compuesto de peptidos ciclicos que tiene accion inhibidora de kras
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
JP2023505100A (ja) 2019-11-27 2023-02-08 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ｒａｓ阻害剤及びその使用
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
WO2021106230A1 (ja) 2019-11-29 2021-06-03 大鵬薬品工業株式会社 新規なフェノール化合物又はその塩
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
WO2021126799A1 (en) 2019-12-18 2021-06-24 Merck Sharp & Dohme Corp. Macrocyclic peptides as potent inhibitors of k-ras g12d mutant
WO2021120045A1 (en) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
BR112022011421A2 (pt) 2019-12-19 2022-08-30 Jacobio Pharmaceuticals Co Ltd Inibidores da proteína mutante kras
WO2021121371A1 (zh) 2019-12-19 2021-06-24 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
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
WO2021129820A1 (zh) 2019-12-27 2021-07-01 微境生物医药科技(上海)有限公司 含螺环的喹唑啉化合物
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
IL294526A (en) 2020-01-10 2022-09-01 Incyte Corp Tricyclic compounds as inhibitors of kras
CN115175908B (zh) 2020-01-13 2024-07-23 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
WO2021147967A1 (zh) 2020-01-21 2021-07-29 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
US20230099858A1 (en) 2020-02-20 2023-03-30 Beta Pharma, Inc. Pyridopyrimidine derivatives as kras inhibitors
US20230143751A1 (en) 2020-02-24 2023-05-11 Shanghai Zheye Biotechnology Co. Ltd. Aromatic Compound And Use Thereof In Preparing Antineoplastic 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
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
JP2023516381A (ja) 2020-03-03 2023-04-19 ウェルマーカー・バイオ・カンパニー・リミテッド Ｋｒａｓ変異および活性化ｒｏｎが存在する癌の予防または治療のための医薬組成物
CA3174538A1 (en) 2020-03-05 2021-09-10 The Regents Of The Universtiy Of Michigan Inhibitors of egfr, kras, braf, and other targets and use of the same
US20230097789A1 (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
AU2021233058B2 (en) 2020-03-12 2024-05-16 D3 Bio(Wuxi) Co., Ltd Pyrimidoheterocyclic compounds and application thereof
WO2021185233A1 (en) 2020-03-17 2021-09-23 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
EP4130000A4 (en) 2020-03-25 2024-07-10 Wigen Biomedicine Technology (Shanghai) Co., Ltd. SPIRO-RING-CONTAINING QUINAZOLINE COMPOUND
AU2021248363B2 (en) 2020-04-03 2024-02-15 Medshine Discovery Inc. Octahydropyrazinodiazanaphthyridine dione compounds
US20220370416A1 (en) 2020-04-06 2022-11-24 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
WO2021203768A1 (zh) 2020-04-08 2021-10-14 江苏恒瑞医药股份有限公司 嘧啶并二环类衍生物、其制备方法及其在医药上的应用
CA3179692A1 (en) 2020-04-16 2021-10-21 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
US20230174526A1 (en) 2020-04-29 2023-06-08 Shanghai Ringene Biopharma Co., Ltd. Benzothiazolyl biaryl compound, and preparation method and use
WO2021219090A1 (zh) 2020-04-29 2021-11-04 北京泰德制药股份有限公司 喹喔啉二酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
TW202144349A (zh) 2020-04-30 2021-12-01 大陸商上海科州藥物研發有限公司 作為ｋｒａｓ抑制劑的雜環化合物的製備及其應用方法
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
WO2021243280A2 (en) 2020-05-29 2021-12-02 Syros Pharmaceuticals, Inc. Methods of treating cancer in patients with an anomalous kras gene or deletions within chromosome 9
AU2021285032A1 (en) 2020-06-02 2022-12-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2021244603A1 (en) 2020-06-04 2021-12-09 Shanghai Antengene Corporation Limited Inhibitors of kras g12c protein and uses thereof
WO2021245499A1 (en) 2020-06-04 2021-12-09 Pillai Universal Llc Novel small molecules for targeted degradation of untargetable kras in cancer therapy
WO2021248079A1 (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
WO2021248090A1 (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
WO2021248082A1 (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
EP4168414A1 (en) 2020-06-18 2023-04-26 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
CN115836055A (zh) 2020-06-30 2023-03-21 益方生物科技(上海)股份有限公司 喹唑啉化合物、其制备方法和用途
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
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
EP4196228A1 (en) 2020-08-13 2023-06-21 Albert Einstein College of Medicine N-cyclyl-sulfonamides useful for inhibiting raf

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