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

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 (2) US11453683B1 (es)
EP (1) EP4021444A4 (es)
JP (1) JP2022546043A (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 (137)

* 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
JP2022517222A (ja) 2019-01-10 2022-03-07 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
JP2022546043A (ja) 2019-08-29 2022-11-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
KR20220091480A (ko) 2019-09-24 2022-06-30 미라티 테라퓨틱스, 인크. 병용 요법
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
BR112022012106A2 (pt) 2019-12-20 2022-09-20 Mirati Therapeutics Inc Inibidores de sos1
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
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
MX2023007084A (es) * 2020-12-15 2023-08-30 Mirati Therapeutics Inc Inhibidores de pan-kras de azaquinazolina.
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
KR20230145360A (ko) 2021-02-15 2023-10-17 아스텔라스세이야쿠 가부시키가이샤 4-아미노퀴나졸린 화합물
BR112023015067A2 (pt) 2021-02-15 2023-10-03 Astellas Pharma Inc Composto de quinazolina para induzir a degradação de proteína kras g12d mutante
WO2022184178A1 (en) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
CN117083280A (zh) * 2021-03-07 2023-11-17 北京加科思新药研发有限公司 Kras g12d抑制剂的稠环衍生物
WO2022192332A1 (en) * 2021-03-10 2022-09-15 Beta Pharma, Inc. Pyridopyrimidine derivatives as kras inhibitors
CN115073451A (zh) * 2021-03-15 2022-09-20 药雅科技(上海)有限公司 Krasg12d突变蛋白抑制剂的制备及其应用
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
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
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
WO2022194066A1 (zh) * 2021-03-15 2022-09-22 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
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
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
WO2022194191A1 (en) * 2021-03-16 2022-09-22 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of kras g12d
WO2022194245A1 (zh) * 2021-03-17 2022-09-22 劲方医药科技(上海)有限公司 嘧啶并环类化合物及其制法和用途
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
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
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
WO2022221386A1 (en) * 2021-04-14 2022-10-20 Erasca, Inc. Selective kras inhibitors
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
WO2022232332A1 (en) * 2021-04-29 2022-11-03 Amgen Inc. 2-aminobenzothiazole compounds and methods of use thereof
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
WO2022228576A1 (zh) * 2021-04-30 2022-11-03 上海医药集团股份有限公司 一种靶向蛋白调节剂的化合物及其应用
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
EP4334324A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2022236578A1 (en) * 2021-05-10 2022-11-17 Nikang Therapeutics, Inc. Exocyclic amino quinazoline derivatives as kras inhibitors
UY39779A (es) * 2021-05-21 2023-01-31 Blossomhill Therapeutics Inc Compuestos macrocíclicos para tratar enfermedades
CN117813306A (zh) * 2021-05-22 2024-04-02 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物，及其制备和治疗用途
US20230391785A1 (en) 2021-05-24 2023-12-07 280 Bio, Inc. 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
IL308438A (en) 2021-05-28 2024-01-01 Redx Pharma Plc Pyrido[3,4-D]pyrimidine compounds inhibit mutant KRAS proteins
WO2022261154A1 (en) 2021-06-09 2022-12-15 Eli Lilly And Company Substituted fused azines as kras g12d inhibitors
EP4352061A1 (en) 2021-06-10 2024-04-17 Redx Pharma Plc Quinazoline derivatives useful as ras inhibitiors
WO2022262686A1 (en) * 2021-06-13 2022-12-22 Jingrui Biopharma Co., Ltd. Kras g12d inhibitors
WO2022266167A1 (en) * 2021-06-16 2022-12-22 Erasca, Inc. Amide and urea-containing tricyclic kras inhibitors
WO2022266069A1 (en) * 2021-06-16 2022-12-22 Erasca, Inc. Tricyclic kras g12d inhibitors
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
CN117255793A (zh) 2021-06-21 2023-12-19 江苏恒瑞医药股份有限公司 稠合四环类化合物、其制备方法及其在医药上的应用
WO2022271823A1 (en) * 2021-06-23 2022-12-29 Newave Pharmaceutical Inc. Mutant kras modulators and uses thereof
CN117642407A (zh) 2021-06-30 2024-03-01 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
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
WO2023284730A1 (en) * 2021-07-14 2023-01-19 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
WO2023001141A1 (en) * 2021-07-23 2023-01-26 Shanghai Zion Pharma Co. Limited Kras g12d inhibitors and uses thereof
CA3228579A1 (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
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
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
WO2023020519A1 (en) * 2021-08-18 2023-02-23 Jacobio Pharmaceuticals Co., Ltd. 1, 4-oxazepane derivatives and uses 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
CN117794930A (zh) * 2021-09-03 2024-03-29 苏州亚盛药业有限公司 Kras抑制剂
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
CN115785124A (zh) * 2021-09-10 2023-03-14 润佳（苏州）医药科技有限公司 Kras g12d抑制剂及其用途
WO2023039240A1 (en) 2021-09-13 2023-03-16 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
AU2022359880A1 (en) * 2021-10-05 2024-04-11 Mirati Therapeutics, Inc. COMBINATION THERAPIES OF KRAS G12D INHIBITORS WITH Pan ErbB FAMILY INHIBITORS
WO2023059598A1 (en) * 2021-10-05 2023-04-13 Mirati Therapeutics, Inc. Combination therapies of kras g12d inhibitors with shp-2 inhibitors
WO2023059597A1 (en) * 2021-10-05 2023-04-13 Mirati Therapeutics, Inc. Combination therapies of kras g12d inhibitors with sos1 inhibitors
AU2022361219A1 (en) * 2021-10-05 2024-04-11 Mirati Therapeutics, Inc. Combinations of kras g12d inhibitors with irinotecan and related methods of treatment
AU2022359282A1 (en) * 2021-10-05 2024-04-11 Mirati Therapeutics, Inc. Combinations of kras g12d inhibitors with pi3ka inhibitors 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
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
WO2023101928A1 (en) * 2021-11-30 2023-06-08 Beta Pharma, Inc. Fused pyrimidine derivatives as kras oncoprotein inhibitors
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
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
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
WO2023138583A1 (zh) * 2022-01-21 2023-07-27 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
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
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
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
US20240043451A1 (en) 2022-03-25 2024-02-08 Eli Lilly And Company Kras inhibitors
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
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
WO2023198191A1 (zh) * 2022-04-15 2023-10-19 杭州多域生物技术有限公司 一种六元并六元化合物、制备方法、药物组合物和应用
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
US20230374036A1 (en) 2022-04-21 2023-11-23 Gilead Sciences, Inc. Kras g12d modulating compounds
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
WO2023213269A1 (en) * 2022-05-06 2023-11-09 Zai Lab (Shanghai) Co., Ltd. Amide-substituted heterocyclic compounds as kras g12d modulators and uses thereof
US20230365595A1 (en) * 2022-05-13 2023-11-16 Ranok Therapeutics (Hangzhou) Co. Ltd. Inhibitors of kras(g12d)
US20240025919A1 (en) * 2022-05-19 2024-01-25 Genentech, Inc. Aza-tetracyclic oxazepine compounds 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
WO2024009191A1 (en) 2022-07-05 2024-01-11 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
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
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
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
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
WO2024051852A1 (zh) * 2022-09-09 2024-03-14 上海翰森生物医药科技有限公司 含嘧啶多环类生物抑制剂、其制备方法和应用
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

Family Cites Families (207)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1363899B1 (en) 2001-01-02 2005-05-11 F.Hoffmann-La Roche Ag Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
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
WO2008080056A2 (en) 2006-12-21 2008-07-03 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
PE20110403A1 (es) 2008-07-31 2011-07-04 Genentech Inc Compuestos biciclicos fusionados de pirimidina en el tratamiento del cancer
WO2010120996A1 (en) 2009-04-17 2010-10-21 Wyeth Llc 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
EP2421823B1 (en) 2009-04-22 2015-01-14 Janssen Pharmaceutica N.V. Azetidinyl diamides as monoacylglycerol lipase inhibitors
US20130029978A1 (en) 2009-12-25 2013-01-31 Mochida Pharmaceutical Co., Ltd. Novel aryl urea derivative
CA2785738A1 (en) 2009-12-30 2011-07-07 Avila Therapeutics, Inc. Ligand-directed covalent modification of protein
US20150087628A1 (en) 2012-04-10 2015-03-26 The Regents Of The University Of California Compositions and methods for treating cancer
EP2858647B1 (en) * 2012-06-08 2018-05-23 Sensorion H4 receptor inhibitors for treating tinnitus
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
EP2970121B1 (en) 2013-03-15 2017-12-13 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
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
BR112016008016B8 (pt) 2013-10-10 2023-09-26 Araxes Pharma Llc Compostos inibidores de kras g12c, composição farmacêutica compreendendo ditos compostos, métodos para regular a atividade e para preparar uma proteína mutante kras, hras ou nras g12c, método para inibir a proliferação de uma população de células e usos terapêuticos dos ditos compostos
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
EP3148981A4 (en) 2014-05-30 2017-11-08 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
US10011600B2 (en) 2014-09-25 2018-07-03 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
CN107849022A (zh) 2015-04-10 2018-03-27 亚瑞克西斯制药公司 取代的喹唑啉化合物和其使用方法
EP3283462B1 (en) 2015-04-15 2020-12-02 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
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (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
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
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 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
EP3365686A4 (en) 2015-10-22 2019-03-27 The Scripps Research Institute CYSTEINE-RESPONSIVE PROBES AND USES THEREOF
WO2017080980A1 (en) 2015-11-09 2017-05-18 Astrazeneca Ab Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer
WO2017079864A1 (en) 2015-11-12 2017-05-18 Hangzhou Yier Biotech Co., Ltd. Treatment of cancers related to chronically active ras
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US20170283445A1 (en) 2016-04-05 2017-10-05 University Of South Carolina Small Molecule Inhibitors Selective For Polo-Like Kinase Proteins
KR102444509B1 (ko) 2016-05-18 2022-09-19 미라티 테라퓨틱스, 인크. Kras g12c 억제제
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
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
EP3548024A2 (en) 2016-11-30 2019-10-09 Bantam Pharmaceutical, LLC Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
JP7373992B2 (ja) 2016-11-30 2023-11-06 バンタム、ファーマシューティカル、リミテッド、ライアビリティー、カンパニー 過剰増殖性疾患の治療のための置換ピラゾール化合物およびそれらの使用方法
WO2018112420A1 (en) 2016-12-15 2018-06-21 The Regents Of The University Of California Compositions and methods for treating cancer
CR20190338A (es) 2016-12-22 2019-09-09 Amgen Inc Inhibidores de kras g12c y métodos para su uso
US10898487B2 (en) 2016-12-22 2021-01-26 Boehringer Ingelheim International Gmbh Benzylamino substituted quinazolines and derivatives as SOS1 inhibitors
US10344026B2 (en) 2017-01-18 2019-07-09 Nantbio, Inc. Compositions and methods of targeting mutant K-ras
JP2020505395A (ja) 2017-01-26 2020-02-20 アラクセス ファーマ エルエルシー 縮合ｎ−複素環式化合物およびその使用方法
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3573967A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused hetero-hetero bicyclic compounds and methods of use thereof
WO2018140514A1 (en) 2017-01-26 2018-08-02 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
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
BR112019021899A2 (pt) 2017-04-20 2020-08-18 The Regents Of The University Of California moduladores de k-ras
SG11202001499WA (en) 2017-09-08 2020-03-30 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
JP2022517222A (ja) 2019-01-10 2022-03-07 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
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
KR20200100429A (ko) 2019-02-18 2020-08-26 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
US20220313700A1 (en) 2019-02-26 2022-10-06 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
WO2020178282A1 (en) 2019-03-05 2020-09-10 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
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
CN113924365A (zh) 2019-03-29 2022-01-11 迪克纳制药公司 用于治疗kras相关疾病或病症的组合物和方法
WO2020205486A1 (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
EP3964516A4 (en) 2019-04-28 2023-01-11 Genfleet Therapeutics (Shanghai) Inc. OXAAZACHUINAZOLINE-7( 8H)-KETONE COMPOUND, PROCESS FOR ITS PRODUCTION AND ITS PHARMACEUTICAL APPLICATION
MX2021013662A (es) 2019-05-10 2022-03-11 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de heteroarilaminopirimidina amida y metodos de uso de estos.
RS65019B1 (sr) 2019-05-10 2024-01-31 Deciphera Pharmaceuticals Llc Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primene
MX2021013817A (es) 2019-05-13 2021-12-14 Novartis Ag Nuevas formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinop iridin-4-il)-4-metilfenil)-2-(trifluorometil)isonicotinamida como inhibidores de raf para el tratamiento del cancer.
JOP20210304A1 (ar) 2019-05-14 2023-01-30 Janssen Biotech Inc علاجات مركبة باستخدام الأجسام المضادة ثنائية النوعية المضادة لمستقبل عامل نمو البشرة (EGFR)/ مستقبل عامل نمو خلايا الكبد (c-Met) ومثبطات كيناز التيروسين الخاصة بمستقبل عامل نمو البشرة (EGFR) من الجيل الثالث
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
WO2020236940A1 (en) 2019-05-20 2020-11-26 California Institute Of Technology Kras g12c inhibitors and uses thereof
US20220227729A1 (en) 2019-05-21 2022-07-21 Bayer Aktiengesellschaft Identification and use of kras inhibitors
AU2020279287A1 (en) 2019-05-21 2021-12-16 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
AU2020280024A1 (en) 2019-05-21 2021-12-09 Amgen Inc. Solid state forms
CA3140394A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
WO2020247914A1 (en) 2019-06-07 2020-12-10 Emory University Kras g12v mutant binds to jak1, inhibitors, pharmaceutical compositions, and methods related thereto
EP3983377A1 (en) 2019-06-12 2022-04-20 Vanderbilt University Dibenzylamines as amino acid transport inhibitors
AU2020291464A1 (en) 2019-06-12 2022-02-03 Vanderbilt University Amino acid transport inhibitors and the uses thereof
CN114040914A (zh) 2019-07-01 2022-02-11 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
WO2021023154A1 (zh) 2019-08-02 2021-02-11 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
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
US20220363681A1 (en) 2019-08-16 2022-11-17 Genfleet Therapeutics (Shanghai) Inc. Oxo six-membered cyclopyrimidine compound, preparation method and medical use thereof
CN114286676A (zh) 2019-08-22 2022-04-05 密歇根大学董事会 治疗kras相关癌症的方法
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
JP2022546043A (ja) 2019-08-29 2022-11-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
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
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
CA3149872A1 (en) 2019-09-10 2021-03-18 Eric Alejandro Sweet-Cordero Methods of treating kras mutant cancers
WO2021051034A1 (en) 2019-09-13 2021-03-18 Biotheryx, Inc. Ras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
WO2021055728A1 (en) 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
BR112022005193A2 (pt) 2019-09-20 2022-08-16 Shanghai Jemincare Pharmaceuticals Co Ltd Composto de piridona fundido, método de preparação do mesmo e uso do mesmo
WO2021061515A1 (en) 2019-09-23 2021-04-01 Synblia Therapeutics, Inc. Shp2 inhibitors and uses thereof
KR20220091480A (ko) 2019-09-24 2022-06-30 미라티 테라퓨틱스, 인크. 병용 요법
WO2021057832A1 (en) 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
WO2021058018A1 (en) 2019-09-29 2021-04-01 Beigene, Ltd. Inhibitors of kras g12c
CN112574224A (zh) 2019-09-30 2021-03-30 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
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
EP4045047A1 (en) 2019-10-15 2022-08-24 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
JP6754125B1 (ja) 2019-10-15 2020-09-09 学校法人東京理科大学 Ｂｒａｐ２作用増強剤
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
EP4050006A4 (en) 2019-10-23 2023-11-01 SK Biopharmaceuticals Co., Ltd. BICYCLIC COMPOUND AND ITS USE
CA3155857A1 (en) 2019-10-24 2021-04-29 Amgen Inc. PYRIDOPYRIMIDINE DERIVATIVES USEFUL AS KRAS G12C AND KRAS G12D INHIBITORS IN THE TREATMENT OF CANCER
WO2021086833A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
KR20220106765A (ko) 2019-10-30 2022-07-29 젠플리트 테라퓨틱스 (상하이) 아이엔씨. 치환된 헤테로환형 융합된 환형 화합물, 이의 제조 방법 및 이의 약학적 용도
JP2023515235A (ja) 2019-10-31 2023-04-12 大鵬薬品工業株式会社 ４－アミノブタ－２－エンアミド誘導体及びその塩
WO2021084765A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
TW202132316A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ｒａｓ抑制劑
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
EP4055028A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
EP4054720A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
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
SG10202111127YA (en) 2019-11-07 2021-11-29 Chugai Pharmaceutical Co Ltd Cyclic Peptide Compound Having Kras Inhibitory Action
TWI760919B (zh) 2019-11-15 2022-04-11 大陸商四川海思科製藥有限公司 一種嘧啶並環衍生物及其在醫藥上的應用
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US20230061083A1 (en) 2019-11-29 2023-03-02 Evopoint Biosciences Co., Ltd. Kras g12c inhibitor compound and use thereof
US20230049402A1 (en) 2019-11-29 2023-02-16 Taiho Pharmaceutical Co., Ltd. Novel phenol compound or salt thereof
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
AU2020395397A1 (en) 2019-12-02 2022-06-09 Shanghai Yingli Pharmaceutical Co., Ltd Oxygen-containing heterocyclic compound, preparation method and application thereof
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
EP4076493A4 (en) 2019-12-18 2024-01-03 Merck Sharp & Dohme Llc MACROCYCLIC PEPTIDES AS POWERFUL INHIBITORS OF K-RAS MUTANT G12D
TW202128691A (zh) 2019-12-19 2021-08-01 大陸商北京加科思新藥研發有限公司 Ｋｒａｓ 突變蛋白抑制劑
CN114761408B (zh) 2019-12-19 2023-09-15 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
WO2021121397A1 (zh) 2019-12-19 2021-06-24 首药控股(北京)股份有限公司 取代的炔基杂环化合物
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
EP4076667A1 (en) 2019-12-20 2022-10-26 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
MX2022006609A (es) 2019-12-27 2022-07-05 Wigen Biomedicine Tech Shanghai Co Ltd Compuesto de quinazolina que contiene anillo espiro.
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
KR20220125287A (ko) 2020-01-10 2022-09-14 인사이트 코포레이션 Kras 억제제로서 트리사이클릭 화합물
CN115175908A (zh) 2020-01-13 2022-10-11 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
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
CN113637005A (zh) 2020-02-24 2021-11-12 泰励生物科技（上海）有限公司 用于癌症治疗的kras抑制剂
WO2021169963A1 (zh) 2020-02-24 2021-09-02 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
WO2021173923A1 (en) 2020-02-28 2021-09-02 Erasca, Inc. Pyrrolidine-fused heterocycles
CN114901663A (zh) 2020-03-02 2022-08-12 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
WO2021177721A1 (ko) 2020-03-03 2021-09-10 웰마커바이오 주식회사 Kras 돌연변이 및 활성화된 ron이 존재하는 암의 예방 또는 치료용 약학 조성물
US20230098205A1 (en) 2020-03-05 2023-03-30 The Regents Of The University Of Michigan Inhibitors of egfr, kras, braf, and other targets and use of the same
CA3172812A1 (en) 2020-03-05 2021-09-10 The Regents Of The University Of Michigan Inhibitors of egfr, kras, braf, and other targets and use of the same
EP4105211A4 (en) 2020-03-12 2023-09-06 D3 Bio(Wuxi) Co., Ltd. PYRIMIDOHETEROCYCLIC COMPOUNDS AND THEIR APPLICATION
WO2021185233A1 (en) 2020-03-17 2021-09-23 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CN115335379B (zh) 2020-03-25 2024-03-29 微境生物医药科技(上海)有限公司 含螺环的喹唑啉化合物
AU2021248363B2 (en) 2020-04-03 2024-02-15 Medshine Discovery Inc. Octahydropyrazinodiazanaphthyridine dione compounds
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
CN115244058A (zh) 2020-04-08 2022-10-25 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
JP2023522202A (ja) 2020-04-16 2023-05-29 インサイト・コーポレイション 融合三環式ｋｒａｓ阻害剤
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
EP4139299A1 (en) 2020-04-24 2023-03-01 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
CA3177261A1 (en) 2020-04-29 2021-11-04 Shanghai Ringene Biopharma Co., Ltd. Benzothiazolyl biaryl compound, and preparation method and use
CN115151532B (zh) 2020-04-29 2023-06-06 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
CN116194456A (zh) 2020-04-30 2023-05-30 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
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
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
CR20220614A (es) 2020-06-02 2023-05-08 Univ Vanderbilt 2-amino-3-cianotiofenos anulados y derivados para el tratamiento del cáncer
BR112022024300A2 (pt) 2020-06-04 2023-01-24 Pillai Universal Llc Moléculas pequenas para degradação direcionada de kras não direcionado na terapia de câncer
EP4161934A1 (en) 2020-06-04 2023-04-12 Antengene Discovery Limited Inhibitors of kras g12c protein and uses thereof
WO2021248079A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248082A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
US20230026856A1 (en) 2020-06-05 2023-01-26 Sparcbio Llc Heterocyclic compounds and methods of use thereof
US20230023009A1 (en) 2020-06-05 2023-01-26 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021248083A1 (en) 2020-06-05 2021-12-09 Sparcbio Llc Heterocyclic compounds and methods of use thereof
WO2021252339A1 (en) 2020-06-08 2021-12-16 Accutar Biotechnology, Inc. Substituted purine-2,6-dione compounds as kras inhibitors
WO2021249563A1 (zh) 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
WO2021257828A1 (en) 2020-06-18 2021-12-23 Shy Therapeutics, Llc Substituted thienopyrimidines that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2021259331A1 (zh) 2020-06-24 2021-12-30 南京明德新药研发有限公司 八元含n杂环类化合物
EP4175947A1 (en) 2020-06-30 2023-05-10 InventisBio Co., Ltd. Quinazoline compounds, preparation methods and uses thereof
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
EP4194452A1 (en) 2020-08-02 2023-06-14 Shanghai Zheye Biotechnology Co., Ltd. Aromatic compound and application thereof in antitumor drug
EP4192585A1 (en) 2020-08-04 2023-06-14 Mirati Therapeutics, Inc. Kras g12d inhibitors
US20230322788A1 (en) 2020-08-05 2023-10-12 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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