EA202091186A1 - ИНГИБИТОРЫ KRas G12C - Google Patents

ИНГИБИТОРЫ KRas G12C

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Publication number
EA202091186A1
EA202091186A1 EA202091186A EA202091186A EA202091186A1 EA 202091186 A1 EA202091186 A1 EA 202091186A1 EA 202091186 A EA202091186 A EA 202091186A EA 202091186 A EA202091186 A EA 202091186A EA 202091186 A1 EA202091186 A1 EA 202091186A1
Authority
EA
Eurasian Patent Office
Prior art keywords
kras
inhibitors
compounds
relates
inhibit
Prior art date
Application number
EA202091186A
Other languages
English (en)
Inventor
Джеймс Ф. Блейк
Лоренс Е. Берджесс
Марк Джозеф Чикарелли
Джеймс Гейл Кристенсен
Адам Кук
Джэй Брэдфорд Фелл
Джон П. Фишер
Мэтью Арнольд Маркс
Македонио Дж. Мехия
Павел Савеченков
Гай П.А. Вайгерс
Кристофер Рональд Смит
Марта Е. Родригес
Original Assignee
Мирати Терапьютикс, Инк.
Эррэй Биофарма Инк.
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 Мирати Терапьютикс, Инк., Эррэй Биофарма Инк. filed Critical Мирати Терапьютикс, Инк.
Publication of EA202091186A1 publication Critical patent/EA202091186A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/08Bridged systems

Abstract

Данное изобретение относится к соединениям, которые ингибируют KRas G12C. В частности, данное изобретение относится к соединениям, которые необратимо ингибируют активность KRas G12C, к фармацевтическим композициям, содержащим соединения, и способам их применения.
EA202091186A 2017-11-15 2018-11-14 ИНГИБИТОРЫ KRas G12C EA202091186A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762586775P 2017-11-15 2017-11-15
PCT/US2018/061060 WO2019099524A1 (en) 2017-11-15 2018-11-14 Kras g12c inhibitors

Publications (1)

Publication Number Publication Date
EA202091186A1 true EA202091186A1 (ru) 2020-10-01

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA202091186A EA202091186A1 (ru) 2017-11-15 2018-11-14 ИНГИБИТОРЫ KRas G12C

Country Status (28)

Country Link
US (4) US10689377B2 (ru)
EP (2) EP3710439B1 (ru)
JP (2) JP7322019B2 (ru)
KR (1) KR20200100632A (ru)
AU (1) AU2018369759B2 (ru)
BR (1) BR112020009818A2 (ru)
CA (1) CA3082579A1 (ru)
CL (1) CL2020001271A1 (ru)
CO (1) CO2020007244A2 (ru)
DK (1) DK3710439T3 (ru)
EA (1) EA202091186A1 (ru)
ES (1) ES2944547T3 (ru)
FI (1) FI3710439T3 (ru)
HR (1) HRP20230377T1 (ru)
HU (1) HUE061599T2 (ru)
IL (1) IL274601B2 (ru)
LT (1) LT3710439T (ru)
MX (1) MX2020005063A (ru)
PH (1) PH12020550622A1 (ru)
PL (1) PL3710439T3 (ru)
PT (1) PT3710439T (ru)
RS (1) RS64182B1 (ru)
SG (1) SG11202004427TA (ru)
SI (1) SI3710439T1 (ru)
TW (1) TWI809005B (ru)
UA (1) UA125802C2 (ru)
WO (2) WO2019099524A1 (ru)
ZA (1) ZA202002105B (ru)

Families Citing this family (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017266911B2 (en) * 2016-05-18 2021-09-02 Array Biopharma, Inc. KRas G12C inhibitors
WO2019099524A1 (en) * 2017-11-15 2019-05-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
US20210230170A1 (en) * 2018-08-31 2021-07-29 Mirati Therapeutics, Inc. Kras g12c inhibitors
JP2022500388A (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
US20220040181A1 (en) * 2018-09-10 2022-02-10 Mirati Therapeutics, Inc. Combination therapies
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
AU2019377130B2 (en) 2018-11-09 2022-03-17 F. Hoffmann-La Roche Ag Fused ring compounds
KR20210113587A (ko) 2018-12-05 2021-09-16 미라티 테라퓨틱스, 인크. 병용 요법
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP4249000A3 (en) 2019-02-12 2023-12-27 Novartis AG Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
CN113874374A (zh) * 2019-05-24 2021-12-31 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
CA3139769A1 (en) * 2019-05-29 2020-12-03 Shiqiang Liu Nitrogen-containing heterocyclic derivative regulator, preparation method therefor and application thereof
CN112047939B (zh) * 2019-06-06 2023-05-02 江苏先声药业有限公司 一种具有抗肿瘤活性的四氢吡啶并嘧啶类化合物
CN112300153B (zh) * 2019-07-26 2023-06-13 博瑞生物医药(苏州)股份有限公司 一种杂环化合物、药物组合物和用途
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
WO2021023247A1 (en) * 2019-08-07 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
CN112390788A (zh) * 2019-08-13 2021-02-23 苏州闻天医药科技有限公司 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途
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
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
WO2021055728A1 (en) 2019-09-18 2021-03-25 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
MX2022003537A (es) * 2019-09-24 2022-07-11 Mirati Therapeutics Inc Terapias de combinacion.
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
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
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
JP7340100B2 (ja) 2019-10-28 2023-09-06 メルク・シャープ・アンド・ドーム・エルエルシー Kras g12c変異型の小分子阻害薬
EP4328229A2 (en) * 2019-10-30 2024-02-28 Genfleet Therapeutics (Shanghai) Inc. Substituted heterocyclic fused cyclic compound, preparation method therefor and pharmaceutical use thereof
CN115873020A (zh) 2019-11-04 2023-03-31 锐新医药公司 Ras抑制剂
WO2021091982A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021088458A1 (en) * 2019-11-04 2021-05-14 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
CA3160142A1 (en) 2019-11-04 2021-05-14 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
CN112824410A (zh) * 2019-11-21 2021-05-21 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
US11654145B2 (en) 2019-11-27 2023-05-23 Turning Point Therapeutics, Inc. Combination therapy involving diaryl macrocyclic compounds
WO2021108683A1 (en) 2019-11-27 2021-06-03 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
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
JOP20220142A1 (ar) 2019-12-11 2023-01-30 Lilly Co Eli مثبطات kras g12c
CN115192577B (zh) * 2019-12-19 2024-03-29 北京加科思新药研发有限公司 Kras突变蛋白抑制剂
CN113004269A (zh) * 2019-12-19 2021-06-22 首药控股(北京)有限公司 Kras-G12C抑制剂杂环化合物
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
WO2021120890A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
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
CN112094269B (zh) * 2020-01-01 2021-12-07 上海凌达生物医药有限公司 一类饱和六元环并杂环类化合物、制备方法和用途
TWI770760B (zh) * 2020-01-08 2022-07-11 大陸商蘇州亞盛藥業有限公司 螺環四氫喹唑啉
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
TW202140450A (zh) * 2020-02-24 2021-11-01 大陸商泰勵生物科技(上海)有限公司 用於癌症治療的kras抑制劑
WO2021218939A1 (zh) * 2020-04-28 2021-11-04 贝达药业股份有限公司 稠环化合物及其在医药上的应用
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
KR20230019462A (ko) 2020-06-02 2023-02-08 베링거 인겔하임 인터내셔날 게엠베하 암 치료용 고리형 2-아미노-3-시아노 티오펜 및 유도체
EP4161934A1 (en) * 2020-06-04 2023-04-12 Antengene Discovery Limited Inhibitors of kras g12c protein and uses thereof
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
JP2023531049A (ja) 2020-06-24 2023-07-20 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 Sos1阻害剤及びkras g12c阻害剤を含む抗がん剤併用療法
KR20230028798A (ko) * 2020-06-25 2023-03-02 톨레모 테라퓨틱스 아게 암 치료를 위한 CBP/p300 브로모도메인 억제제 및 KRAS 억제제의 조합물
CN113912608B (zh) * 2020-07-10 2023-07-14 江苏恒瑞医药股份有限公司 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用
CN113980014B (zh) * 2020-07-27 2023-05-12 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
EP4208261A1 (en) 2020-09-03 2023-07-12 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
EP4210833A1 (en) * 2020-09-11 2023-07-19 Mirati Therapeutics, Inc. Crystalline forms of a kras g12c inhibitor
CN116133662A (zh) 2020-09-11 2023-05-16 南京明德新药研发有限公司 氮杂环丁烷取代化合物的晶型
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
US20220112204A1 (en) * 2020-10-14 2022-04-14 Accutar Biotechnology Inc. Substituted dihydropyranopyrimidine compounds as kras inhibitors
EP4232039A1 (en) * 2020-10-23 2023-08-30 Mirati Therapeutics, Inc. Methods for treatment of lung cancers
TW202233607A (zh) * 2020-10-30 2022-09-01 瑞士商諾華公司 Kras g12c抑制劑化合物之新結晶形式
CN116867779A (zh) 2020-11-06 2023-10-10 泰励生物科技(上海)有限公司 用于癌症治疗的KRas抑制剂
WO2022132200A1 (en) * 2020-12-15 2022-06-23 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
WO2022133038A1 (en) * 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
PE20240545A1 (es) 2020-12-18 2024-03-19 Amphista Therapeutics Ltd Moleculas bifuncionales novedosas para la degradacion de proteinas dirigidas
TWI795129B (zh) * 2020-12-18 2023-03-01 大陸商正大天晴藥業集團股份有限公司 吡啶并嘧啶酮類化合物
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022140246A1 (en) 2020-12-21 2022-06-30 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
TW202241414A (zh) * 2020-12-22 2022-11-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合以及kras g12c抑制劑用於治療癌症之用途
AU2022212151A1 (en) * 2021-02-01 2023-08-17 Medshine Discovery Inc. Pyrimidopyran compound
WO2022187527A1 (en) * 2021-03-05 2022-09-09 Nikang Therapeutics, Inc Quinazoline nitrile derivatives as kras inhibitors
JP2024509625A (ja) 2021-03-15 2024-03-04 ノバルティス アーゲー ベンゾイソオキサゾール誘導体及びその使用
US20220331324A1 (en) 2021-04-08 2022-10-20 Mirati Therapeutics, Inc. Combination Therapies Using PRMT5 Inhibitors for the Treatment of Cancer
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
WO2022214594A1 (en) 2021-04-09 2022-10-13 Boehringer Ingelheim International Gmbh Anticancer therapy
IL308195A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors for cancer treatment
KR20240004960A (ko) 2021-05-05 2024-01-11 레볼루션 메디슨즈, 인크. Ras 억제제
AR125921A1 (es) * 2021-05-19 2023-08-23 Genentech Inc Terapia de combinación
WO2022251576A1 (en) * 2021-05-28 2022-12-01 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN117769554A (zh) * 2021-05-28 2024-03-26 大鹏药品工业株式会社 Kras突变蛋白的小分子抑制剂
CN117500799A (zh) 2021-06-09 2024-02-02 伊莱利利公司 作为kras g12d抑制剂的取代的稠合吖嗪
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
CN117529321A (zh) * 2021-06-18 2024-02-06 上海德琪医药科技有限公司 Erk抑制剂和kras抑制剂的组合及其用途
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途
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
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
KR20240041917A (ko) 2021-07-27 2024-04-01 도레이 카부시키가이샤 암의 치료 및/또는 예방을 위한 의약품
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
WO2023039020A1 (en) * 2021-09-09 2023-03-16 Mirati Therapeutics, Inc. Processes and intermediates for synthesis of adagrasib
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023097194A2 (en) 2021-11-24 2023-06-01 Genentech, Inc. Therapeutic compounds and methods of use
WO2023097195A1 (en) 2021-11-24 2023-06-01 Genentech, Inc. Therapeutic indazole compounds and methods of use in the treatment of cancer
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
WO2023117681A1 (en) 2021-12-22 2023-06-29 Boehringer Ingelheim International Gmbh Heteroaromatic compounds for the treatment of cancer
WO2023126822A1 (en) 2021-12-28 2023-07-06 Astrazeneca Uk Limited Combination of antibody-drug conjugate and rasg12c inhibitor
WO2023154528A1 (en) * 2022-02-11 2023-08-17 Wave Life Sciences Ltd. Stereoselective technologies for chiral compounds
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023183585A1 (en) 2022-03-25 2023-09-28 Eli Lilly And Company Kras inhibitors
WO2023194310A1 (en) 2022-04-04 2023-10-12 Sanofi Therapeutic combination of kras g12c inhibitor and tead inhibitor
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
WO2023205074A1 (en) * 2022-04-18 2023-10-26 Mirati Therapeutics, Inc. Processes and intermediates for synthesis of adagrasib
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CN117164580A (zh) * 2022-05-27 2023-12-05 苏州泽璟生物制药股份有限公司 一种kras g12c抑制剂的制备方法及其中间体
WO2023240189A1 (en) * 2022-06-10 2023-12-14 Bristol-Myers Squibb Company Tetrahydropyrido 3,4-d pyrimidine derivatives as kras inhibitors
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds
CN116478141B (zh) * 2023-06-20 2023-10-24 药康众拓(江苏)医药科技有限公司 氘代kras抑制剂药物及用途

Family Cites Families (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4031363B2 (ja) 2001-01-02 2008-01-09 エフ.ホフマン−ラ ロシュ アーゲー α−1A/Bアドレナリン作動性受容体拮抗薬としてのキナゾロン誘導体
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
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
KR20090130051A (ko) * 2007-03-14 2009-12-17 엑셀리시스, 인코포레이티드 헤지호그 경로의 억제제
US20100298289A1 (en) 2007-10-09 2010-11-25 Ucb Pharma, S.A. Heterobicyclic compounds as histamine h4-receptor antagonists
JP2011516494A (ja) 2008-04-07 2011-05-26 ギリアード サイエンシーズ, インコーポレイテッド ステアロイル−CoAデサチュラーゼの阻害剤として使用するための2H−ベンゾ[b][1,4]オキサジン−3(4H)−オン誘導体
KR20110046514A (ko) 2008-07-31 2011-05-04 제넨테크, 인크. 피리미딘 화합물, 조성물 및 사용 방법
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
CA2785284A1 (en) 2009-12-25 2011-06-30 Tomoyuki Kamino Novel aryl urea derivative
MX2012007684A (es) 2009-12-30 2012-10-05 Avila Therapeutics Inc Modificacion covalente ligando dirigida de proteina.
JP6399660B2 (ja) 2012-04-10 2018-10-03 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア 癌治療用組成物および方法
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
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Kras g12c之共價抑制劑
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
CN106488910B (zh) * 2013-10-10 2020-07-31 亚瑞克西斯制药公司 Kras g12c的抑制剂
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
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods 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
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
AU2016245864C1 (en) 2015-04-10 2021-09-09 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
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
EP3291813A4 (en) 2015-05-06 2019-01-02 The Regents of The University of California K-ras modulators
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
TW201723176A (zh) 2015-09-24 2017-07-01 Ionis製藥公司 Kras表現之調節劑
WO2017058807A1 (en) 2015-09-28 2017-04-06 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
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10858343B2 (en) 2015-09-28 2020-12-08 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
US10975071B2 (en) 2015-09-28 2021-04-13 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
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
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
AU2017266911B2 (en) * 2016-05-18 2021-09-02 Array Biopharma, Inc. KRas G12C inhibitors
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc 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
MX2019006296A (es) 2016-11-30 2019-11-12 Bantam Pharmaceutical Llc Métodos de uso de compuestos de pirazol y pirazol sustituido y para el tratamiento de enfermedades hiperproliferativas.
RU2019121922A (ru) 2016-12-15 2021-01-18 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Композиции и способы лечения рака
CR20190338A (es) 2016-12-22 2019-09-09 Amgen Inc Inhibidores de kras g12c y métodos para su uso
EP3558979B1 (en) 2016-12-22 2021-02-17 Boehringer Ingelheim International GmbH Novel 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
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
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
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
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US20200385364A1 (en) 2017-01-26 2020-12-10 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
SG11201909570PA (en) 2017-04-20 2019-11-28 Univ California K-ras modulators
ES2928576T3 (es) 2017-09-08 2022-11-21 Amgen Inc Inhibidores de KRAS G12C y métodos de uso de los mismos
WO2019099524A1 (en) 2017-11-15 2019-05-23 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2019110751A1 (en) 2017-12-08 2019-06-13 Astrazeneca Ab Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents
TW201942115A (zh) 2018-02-01 2019-11-01 美商輝瑞股份有限公司 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物

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