JP2019529484A5 - - Google Patents

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JP2019529484A5
JP2019529484A5 JP2019516992A JP2019516992A JP2019529484A5 JP 2019529484 A5 JP2019529484 A5 JP 2019529484A5 JP 2019516992 A JP2019516992 A JP 2019516992A JP 2019516992 A JP2019516992 A JP 2019516992A JP 2019529484 A5 JP2019529484 A5 JP 2019529484A5
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JP2019516992A 2016-09-29 2017-09-29 Kras g12c変異体タンパク質の阻害剤 Pending JP2019529484A (ja)

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US201662401345P 2016-09-29 2016-09-29
US62/401,345 2016-09-29
PCT/US2017/054363 WO2018064510A1 (en) 2016-09-29 2017-09-29 Inhibitors of kras g12c mutant proteins

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JP2019529484A JP2019529484A (ja) 2019-10-17
JP2019529484A5 true JP2019529484A5 (ref) 2020-11-12

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US (2) US10280172B2 (ref)
EP (1) EP3519402A1 (ref)
JP (1) JP2019529484A (ref)
CN (1) CN110036010A (ref)
WO (1) WO2018064510A1 (ref)

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Publication number Priority date Publication date Assignee Title
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356347A1 (en) 2015-09-28 2018-08-08 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
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (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
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
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
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
FI3442977T3 (fi) * 2016-04-15 2023-09-26 Blueprint Medicines Corp Aktiviinireseptorin kaltaisen kinaasin estäjät
CN109843856B (zh) 2016-05-18 2023-05-02 米拉蒂治疗股份有限公司 Kras g12c抑制剂
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
CA3048217A1 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone 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
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
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
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
ES2905676T3 (es) 2017-05-22 2022-04-11 Amgen Inc Inhibidores de KRAS G12C y métodos para su uso
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
CN111051306B (zh) 2017-09-08 2023-01-03 美国安进公司 Kras g12c的抑制剂及其使用方法
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
KR102861303B1 (ko) 2017-11-15 2025-09-17 미라티 테라퓨틱스, 인크. Kras g12c 억제제
CN112442031B (zh) * 2018-01-19 2022-07-12 勤浩医药(苏州)有限公司 作为krasg12c突变蛋白抑制剂的吡啶酮并嘧啶类衍生物
WO2019178129A1 (en) * 2018-03-13 2019-09-19 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
MX2020010836A (es) 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
WO2019217307A1 (en) 2018-05-07 2019-11-14 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
EP3790886B1 (en) 2018-05-10 2024-06-26 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
AU2019278998B2 (en) 2018-06-01 2023-11-09 Amgen Inc. KRAS G12C inhibitors and methods of using the same
MX2020012204A (es) 2018-06-11 2021-03-31 Amgen Inc Inhibidores de kras g12c para tratar el cáncer.
CA3100390A1 (en) 2018-06-12 2020-03-12 Amgen Inc. Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
CR20210083A (es) 2018-08-16 2021-04-19 Hoffmann La Roche Compuestos de anillo fusionado
US20210230170A1 (en) * 2018-08-31 2021-07-29 Mirati Therapeutics, Inc. Kras g12c inhibitors
KR102871791B1 (ko) 2018-09-10 2025-10-15 미라티 테라퓨틱스, 인크. 병용 요법
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
ES3004338T3 (en) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Combination therapies
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
WO2020061103A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
TWI831855B (zh) 2018-10-26 2024-02-11 日商大鵬藥品工業股份有限公司 新穎吲唑化合物或其鹽
JP7516029B2 (ja) * 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
CA3117222A1 (en) 2018-11-19 2020-05-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
JP7592601B2 (ja) 2019-01-10 2024-12-02 ミラティ セラピューティクス, インコーポレイテッド Kras g12c阻害剤
US11390626B2 (en) * 2019-01-29 2022-07-19 Tosk, Inc. Pyrazolopyrimidine modulators of RAS GTPase
US20220152026A1 (en) 2019-02-12 2022-05-19 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
JP7426398B2 (ja) 2019-02-26 2024-02-01 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 Ras阻害剤としての新規イソインドリノン置換インドールおよび誘導体
PH12021552083A1 (en) 2019-03-05 2022-06-06 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
US12528796B2 (en) 2019-04-15 2026-01-20 Tosk, Inc. Modulators of RAS GTPase
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
US20220227729A1 (en) 2019-05-21 2022-07-21 Bayer Aktiengesellschaft Identification and use of kras inhibitors
CN114144414B (zh) 2019-05-21 2025-11-07 美国安进公司 固态形式
WO2020239077A1 (zh) * 2019-05-29 2020-12-03 上海翰森生物医药科技有限公司 含氮杂环类衍生物调节剂、其制备方法和应用
CN112047948B (zh) * 2019-06-06 2022-08-16 山东轩竹医药科技有限公司 Kras突变体抑制剂
CN110452180A (zh) * 2019-06-25 2019-11-15 南京普锐达医药科技有限公司 一种合成2-氯-5-氨基-6-嘧啶甲酸乙酯的方法
WO2020259573A1 (zh) * 2019-06-25 2020-12-30 南京明德新药研发有限公司 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物
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
CA3148745A1 (en) * 2019-08-29 2021-03-04 Xiaolun Wang Kras g12d inhibitors
US11370803B2 (en) 2019-09-18 2022-06-28 Takeda Pharmaceutical Company Limited Heteroaryl plasma kallikrein inhibitors
PT4031547T (pt) 2019-09-18 2024-08-27 Takeda Pharmaceuticals Co Inibidores de calicreína plasmática e utilizações dos mesmos
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
WO2021058018A1 (en) * 2019-09-29 2021-04-01 Beigene, Ltd. Inhibitors of kras g12c
WO2021063346A1 (zh) * 2019-09-30 2021-04-08 上海迪诺医药科技有限公司 Kras g12c抑制剂及其应用
CN112694475B (zh) * 2019-10-23 2025-09-23 苏州泽璟生物制药股份有限公司 环烷基类和杂环烷基类抑制剂及其制备方法和应用
CA3158793A1 (en) 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
CN114786777A (zh) 2019-11-04 2022-07-22 锐新医药公司 Ras抑制剂
PE20221277A1 (es) 2019-11-04 2022-09-05 Revolution Medicines Inc Inhibidores de ras
CN114867735A (zh) 2019-11-04 2022-08-05 锐新医药公司 Ras抑制剂
CN114630832A (zh) * 2019-11-15 2022-06-14 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
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
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
AU2020404319B2 (en) * 2019-12-19 2026-01-15 Jacobio Pharmaceuticals Co., Ltd. KRAS mutant protein inhibitors
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
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
GB202001344D0 (en) 2020-01-31 2020-03-18 Redx Pharma Plc Ras Inhibitors
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
US20210292330A1 (en) * 2020-02-28 2021-09-23 Erasca, Inc. Pyrrolidine-fused heterocycles
WO2021218110A1 (zh) * 2020-04-29 2021-11-04 上海凌达生物医药有限公司 一类苯并噻唑基联芳基类化合物、制备方法和用途
TW202210633A (zh) 2020-06-05 2022-03-16 法商昂席歐公司 用於治療癌症之dbait分子與kras抑制劑的組合
KR20230042600A (ko) 2020-06-18 2023-03-28 레볼루션 메디슨즈, 인크. Ras 억제제에 대한 획득된 저항성을 지연, 예방, 및 치료하는 방법
WO2022015375A1 (en) * 2020-07-16 2022-01-20 Mirati Therapeutics, Inc. Kras g12d inhibitors
JP7837952B2 (ja) * 2020-08-26 2026-03-31 インベンティスバイオ カンパニー リミテッド ヘテロアリール基化合物、その製造方法および使用
WO2022048545A1 (zh) * 2020-09-01 2022-03-10 勤浩医药(苏州)有限公司 一种吡啶并嘧啶化合物的晶型
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
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
US12286431B2 (en) 2020-09-11 2025-04-29 Mirati Therapeutics, Inc. Crystalline forms of a KRas G12C inhibitor
AU2021345111B2 (en) 2020-09-15 2025-11-27 Revolution Medicines, Inc. Indole derivatives as Ras inhibitors in the treatment of cancer
MX2023003338A (es) 2020-09-23 2023-06-14 Erasca Inc Piridonas y pirimidonas tricíclicas.
US12180220B2 (en) 2020-10-14 2024-12-31 Tosk, Inc. Heteroaryl modulators of RAS GTPase
US12398154B2 (en) 2020-12-15 2025-08-26 Mirati Therapeutics, Inc. Azaquinazoline pan-KRas inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
IL303661A (en) 2020-12-22 2023-08-01 Nikang Therapeutics Inc Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
WO2022152233A1 (en) * 2021-01-15 2022-07-21 Beigene, Ltd. Kras g12c inhibitors
WO2022192332A1 (en) * 2021-03-10 2022-09-15 Beta Pharma, Inc. Pyridopyrimidine derivatives as kras inhibitors
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
AR125782A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
WO2022246092A1 (en) * 2021-05-21 2022-11-24 Blossomhill Therapeutics, Inc. Macrocyclic compounds for treating disease
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
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
CN117980310A (zh) 2021-07-14 2024-05-03 尼坎治疗公司 作为kras抑制剂的亚烷基衍生物
CN117858878A (zh) * 2021-08-18 2024-04-09 北京加科思新药研发有限公司 N-环丙基吡啶并[4,3-d]嘧啶-4-胺衍生物及其用途
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
EP4395769A1 (en) 2021-09-01 2024-07-10 Novartis AG Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
EP4389751A1 (en) 2021-09-03 2024-06-26 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
US20250154170A1 (en) 2022-02-10 2025-05-15 Bayer Aktiengesellschaft Fused pyrimidines as kras inhibitors
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
KR20240167846A (ko) 2022-03-28 2024-11-28 니캉 테라퓨틱스 인코포레이티드 사이클린 의존적 키나제 2 억제제로서의 설폰아미도 유도체
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
AU2023267545A1 (en) * 2022-05-09 2024-11-14 Beta Pharma, Inc. 8- and 6-substituted pyridopyrimidine derivatives as kras inhibitors
EP4536363A1 (en) 2022-06-08 2025-04-16 Nikang Therapeutics, Inc. Sulfamide derivatives as cyclin-dependent kinase 2 inhibitors
AU2023285116A1 (en) 2022-06-10 2024-12-19 Revolution Medicines, Inc. Macrocyclic ras inhibitors
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds
CN120659773A (zh) 2022-11-09 2025-09-16 锐新医药公司 化合物、复合物以及其制备方法和用途
AU2023375457A1 (en) 2022-11-11 2025-05-01 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
EP4631948A1 (en) * 2022-12-07 2025-10-15 SK Biopharmaceuticals Co., Ltd. Novel tricyclic compound as kras g12d inhibitor, and use thereof
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
EP4688790A1 (en) 2023-04-07 2026-02-11 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024216016A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
CN121712509A (zh) 2023-05-04 2026-03-20 锐新医药公司 用于ras相关疾病或病症的组合疗法
EP4720059A1 (en) 2023-05-24 2026-04-08 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
CN121219016A (zh) 2023-06-02 2025-12-26 第一三共株式会社 抗-her3抗体-药物缀合物和rasg12c抑制剂的组合
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025016899A1 (en) 2023-07-19 2025-01-23 Bayer Aktiengesellschaft Spirocyclic compounds for the treatment of cancer
WO2025026903A1 (en) 2023-07-31 2025-02-06 Bayer Aktiengesellschaft Imidazo pyrimidine compounds for the treatment of cancer
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025072462A1 (en) 2023-09-27 2025-04-03 Nikang Therapeutics, Inc. Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors
IL327306A (en) 2023-10-12 2026-05-01 Revolution Medicines Inc Macrocyclic RAS inhibitors
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
TW202527955A (zh) 2023-11-27 2025-07-16 美商尼坎醫療公司 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶2和週期蛋白依賴性激酶4的含有2,5-取代的嘧啶衍生物的雙功能化合物
WO2025117981A1 (en) 2023-12-02 2025-06-05 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
WO2025171055A1 (en) 2024-02-06 2025-08-14 Kumquat Biosciences Inc. Heterocyclic conjugates and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025212828A1 (en) 2024-04-03 2025-10-09 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025230971A1 (en) 2024-04-30 2025-11-06 Kumquat Biosciences Inc. Macrocyclic heterocycles as anticancer agents
WO2025240536A1 (en) 2024-05-15 2025-11-20 Nikang Therapeutics, Inc. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025253326A1 (ko) * 2024-06-05 2025-12-11 에스케이바이오팜 주식회사 Kras 저해제로서 신규한 3환 화합물 및 이의 용도
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer

Family Cites Families (202)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB939516A (en) 1961-05-29 1963-10-16 British Drug Houses Ltd Sulphonyl ureas
US3702849A (en) 1967-10-26 1972-11-14 Pfizer 4-(isoquinolin-1-yl) piperazine-1-carboxylic acid esters
US3752660A (en) 1971-03-15 1973-08-14 Allied Chem Chlorophenoxyacetyloxazolidone herbicides and preparation thereof
US4439606A (en) 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
EP0094498A3 (en) 1982-05-06 1985-04-03 American Cyanamid Company Antiatherosclerotic 1-piperazine derivatives
US4656181A (en) 1982-11-24 1987-04-07 Cermol S.A. Esters of 1,4-dihydropyridines, processes for the preparation of the new esters, and medicaments containing the same
JPS59163372A (ja) 1983-03-09 1984-09-14 Showa Denko Kk ピラゾ−ル誘導体とその製造法及び除草剤
JPS60193955A (ja) 1984-03-13 1985-10-02 Mitsui Toatsu Chem Inc 環式不飽和アミド置換エ−テル化合物及びその製造方法
JPS6143190A (ja) 1984-08-06 1986-03-01 Mitsui Petrochem Ind Ltd ピリドピリミジン誘導体およびその製法
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5010175A (en) 1988-05-02 1991-04-23 The Regents Of The University Of California General method for producing and selecting peptides with specific properties
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5925525A (en) 1989-06-07 1999-07-20 Affymetrix, Inc. Method of identifying nucleotide differences
IE66205B1 (en) 1990-06-14 1995-12-13 Paul A Bartlett Polypeptide analogs
US5650489A (en) 1990-07-02 1997-07-22 The Arizona Board Of Regents Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6051380A (en) 1993-11-01 2000-04-18 Nanogen, Inc. Methods and procedures for molecular biological analysis and diagnostics
US6017696A (en) 1993-11-01 2000-01-25 Nanogen, Inc. Methods for electronic stringency control for molecular biological analysis and diagnostics
US5573905A (en) 1992-03-30 1996-11-12 The Scripps Research Institute Encoded combinatorial chemical libraries
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5288514A (en) 1992-09-14 1994-02-22 The Regents Of The University Of California Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5605798A (en) 1993-01-07 1997-02-25 Sequenom, Inc. DNA diagnostic based on mass spectrometry
US5858659A (en) 1995-11-29 1999-01-12 Affymetrix, Inc. Polymorphism detection
US6045996A (en) 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US6068818A (en) 1993-11-01 2000-05-30 Nanogen, Inc. Multicomponent devices for molecular biological analysis and diagnostics
US5538848A (en) 1994-11-16 1996-07-23 Applied Biosystems Division, Perkin-Elmer Corp. Method for detecting nucleic acid amplification using self-quenching fluorescence probe
IL111730A (en) 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
DE69531542T2 (de) 1994-02-07 2004-06-24 Beckman Coulter, Inc., Fullerton Ligase/polymerase-vermittelte analyse genetischer elemente von einzelnukleotid-polymorphismen und ihre verwendung in der genetischen analyse
US5593853A (en) 1994-02-09 1997-01-14 Martek Corporation Generation and screening of synthetic drug libraries
US5539083A (en) 1994-02-23 1996-07-23 Isis Pharmaceuticals, Inc. Peptide nucleic acid combinatorial libraries and improved methods of synthesis
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
EP0786997A4 (en) 1994-10-27 1998-03-11 Merck & Co Inc MUSCARINE ANTAGONISTS
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Mmpおよびtnf抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
FR2734816B1 (fr) 1995-05-31 1997-07-04 Adir Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE69638269D1 (de) 1995-06-14 2010-11-18 Univ California Hochaffine humane antikörper gegen tumorantigene
ATE225343T1 (de) 1995-12-20 2002-10-15 Hoffmann La Roche Matrix-metalloprotease inhibitoren
US6011029A (en) 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
CA2260898C (en) 1996-07-18 2002-05-14 Pfizer Limited Phosphinate based inhibitors of matrix metalloproteases
PL331895A1 (en) 1996-08-23 1999-08-16 Pfizer Arylosulphonylamino derivatives of hydroxamic acid
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
DE69730151T2 (de) 1997-01-06 2005-08-04 Pfizer Inc. Cyclische sulfonderivate
AU721748B2 (en) 1997-02-03 2000-07-13 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
CA2279863A1 (en) 1997-02-07 1998-08-13 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
WO1998034918A1 (en) 1997-02-11 1998-08-13 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
US6291464B1 (en) 1997-02-17 2001-09-18 Fujisawa Pharmaceutical Co., Ltd. Aminopiperazine derivatives
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US5919626A (en) 1997-06-06 1999-07-06 Orchid Bio Computer, Inc. Attachment of unmodified nucleic acids to silanized solid phase surfaces
AU8253598A (en) 1997-06-17 1999-01-04 Schering Corporation Novel n-substituted urea inhibitors of farnesyl-protein transferase
ID23668A (id) 1997-08-08 2000-05-11 Pfizer Prod Inc Turunan asam ariloksiarilsulfonilamino hidroksamat
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
DE19756236A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
CA2314401A1 (en) 1997-12-22 1999-07-01 Du Pont Pharmaceuticals Company Nitrogen containing heteroaromatics with ortho-substituted p1's as factor xa inhibitors
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
US7060431B2 (en) 1998-06-24 2006-06-13 Illumina, Inc. Method of making and decoding of array sensors with microspheres
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
US6429027B1 (en) 1998-12-28 2002-08-06 Illumina, Inc. Composite arrays utilizing microspheres
US6511993B1 (en) 1999-06-03 2003-01-28 Kevin Neil Dack Metalloprotease inhibitors
EP1081137A1 (en) 1999-08-12 2001-03-07 Pfizer Products Inc. Selective inhibitors of aggrecanase in osteoarthritis treatment
CA2384838C (en) 1999-09-13 2006-07-18 Nugen Technologies, Inc. Methods and compositions for linear isothermal amplification of polynucleotide sequences
SK13352002A3 (sk) 2000-03-21 2003-05-02 The Procter & Gamble Company Metaloproteázové inhibítory s vedľajším heterocyklickým reťazcom
BR0111280A (pt) 2000-06-05 2003-06-10 Dong A Pharm Co Ltd Novos derivados de oxazolidinona e um processo para a preparação dos mesmos
TWI227231B (en) 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
EP1964839A3 (en) 2000-08-18 2008-11-05 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as kinase inhibitors
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
US20020169300A1 (en) 2001-01-30 2002-11-14 Waterman Marian L. Method of detection and treatment of colon cancer by analysis of beta-catenin-sensitive isoforms of lymphoid enhancer factor-1
US7259157B2 (en) 2001-04-03 2007-08-21 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
JP4310109B2 (ja) 2001-04-26 2009-08-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 ピラゾリル基を置換基として有する含窒素縮合環化合物およびその医薬組成物
ATE449090T1 (de) 2001-07-02 2009-12-15 High Point Pharmaceuticals Llc Substituierte piperazin- und diazepanderivate zur verwendung als histamin h3 rezeptormodulatoren
EP1348434A1 (en) 2002-03-27 2003-10-01 Fujisawa Deutschland GmbH Use of pyridyl amides as inhibitors of angiogenesis
KR20050051691A (ko) 2002-10-11 2005-06-01 아스트라제네카 아베 1,4-이치환 피페리딘 유도체 및 11-베타hsd1억제제로서의 이들의 용도
JP4608852B2 (ja) 2002-10-15 2011-01-12 チッソ株式会社 液晶性ビニルケトン誘導体およびその重合体
CA2516234A1 (en) 2003-02-21 2004-09-02 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
AU2004220321B2 (en) 2003-03-12 2010-02-25 Kudos Pharmaceuticals Ltd Phthalazinone derivatives
US20050119266A1 (en) 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
JP4923380B2 (ja) 2003-12-22 2012-04-25 Jnc株式会社 低屈折率異方性化合物、組成物およびそれらの重合体または重合体組成物
JP4932495B2 (ja) 2004-01-23 2012-05-16 アムゲン インコーポレイテッド 化合物及び使用方法
WO2005082892A2 (en) 2004-02-17 2005-09-09 Dr. Reddy's Laboratories Ltd. Triazole compounds as antibacterial agents and pharmaceutical compositions containing them
WO2005095327A1 (ja) 2004-03-31 2005-10-13 Ajinomoto Co., Inc. アニリン誘導体
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
JP4955646B2 (ja) 2005-03-16 2012-06-20 エフ.ホフマン−ラ ロシュ アーゲー シス−2,4,5−トリアリール−イミダゾリン及びそれらの抗癌薬としての使用
JP2007016011A (ja) 2005-06-10 2007-01-25 Nippon Soda Co Ltd 抗酸化活性を有する新規な含窒素ヘテロ環化合物、及び該化合物を含有する抗酸化薬
JP2008543888A (ja) 2005-06-24 2008-12-04 ギリアード サイエンシーズ, インコーポレイテッド ピリド(3,2−d)ピリミジン、およびC型肝炎を治療するのに有用な医薬組成物
CN102304075A (zh) 2005-10-11 2012-01-04 因特蒙公司 病毒复制抑制剂
EP1966132A2 (en) 2005-12-15 2008-09-10 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
MX2008012617A (es) 2006-03-31 2008-10-10 Novartis Ag Compuestos organicos.
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
JP2009539937A (ja) 2006-06-16 2009-11-19 ハイ ポイント ファーマシューティカルズ,リミティド ライアビリティ カンパニー 置換型ピペリジンカルボキサミドの医薬的使用
US20080039450A1 (en) 2006-06-22 2008-02-14 Jensen Annika J Compounds
FR2903101B1 (fr) 2006-06-30 2008-09-26 Servier Lab Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
EP1903038A1 (de) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
CN101679261A (zh) 2007-03-09 2010-03-24 阿斯利康(瑞典)有限公司 哌嗪和哌啶mGluR5增效剂
EP2144606A2 (en) 2007-04-05 2010-01-20 Max-Delbrück-Centrum Für Molekulare Medizin Remedy for the treatment of cardio-vascular diseases or disorders
ES2705599T3 (es) 2007-04-16 2019-03-26 Abbvie Inc Indoles sustituidos en la posición 7 como inhibidores de mcl-1
EP3269824A1 (en) 2008-03-28 2018-01-17 Pacific Biosciences Of California, Inc. Compositions and methods for nucleic acid sequencing
EP2133334A1 (en) 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
CA2733533C (en) 2008-08-25 2013-12-17 Irm Llc Hedgehog pathway modulators
WO2010087399A1 (ja) 2009-01-30 2010-08-05 第一三共株式会社 ウロテンシンii受容体拮抗薬
NZ595073A (en) 2009-04-20 2012-11-30 Hoffmann La Roche Proline derivatives as cathepsin inhibitors
AU2010239188B2 (en) 2009-04-22 2016-03-31 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
EP2270002A1 (en) 2009-06-18 2011-01-05 Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2011016559A1 (ja) 2009-08-07 2011-02-10 武田薬品工業株式会社 複素環化合物およびその用途
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
RU2595718C2 (ru) 2009-09-09 2016-08-27 Селджен Авиломикс Рисерч,Инк. Ингибиторы pi3-киназы и их применение
EP3309152B1 (en) 2009-12-22 2020-09-09 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
AU2010339456A1 (en) 2009-12-30 2012-07-05 Celgene Avilomics Research, Inc. Ligand-directed covalent modification of protein
CN102791690B (zh) 2010-01-29 2015-12-02 大塚制药株式会社 作为抗癌药的二取代吡啶衍生物
EP2542893A2 (en) 2010-03-03 2013-01-09 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
MX2012010557A (es) 2010-03-16 2012-10-05 Merck Patent Gmbh Morfolinilquinazolinas.
CA2791020A1 (en) 2010-04-28 2011-11-03 Daiichi Sankyo Company, Limited [5,6] heterocyclic compound
TW201202230A (en) 2010-05-24 2012-01-16 Mitsubishi Tanabe Pharma Corp Novel quinazoline compound
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
CN103119439A (zh) 2010-06-08 2013-05-22 纽亘技术公司 用于多重测序的方法和组合物
US8658131B2 (en) 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
WO2012016082A1 (en) 2010-07-30 2012-02-02 Oncotherapy Science, Inc. Quinoline derivatives and melk inhibitors containing the same
CN103068798A (zh) 2010-09-03 2013-04-24 詹森药业有限公司 作为单酰甘油脂肪酶抑制剂的二-氮杂环丁烷二酰胺
BR112013006953A2 (pt) 2010-09-29 2016-07-26 Intervet Int Bv composto, composições farmacêutica e anti-helmíntica, uso de um composto, kit, e, método de tratamento de uma doença
CN103260703A (zh) 2010-10-22 2013-08-21 詹森药业有限公司 作为单酰甘油脂肪酶抑制剂的哌啶-4-基-氮杂环丁烷二酰胺
US20130225524A1 (en) 2010-11-05 2013-08-29 Deping Chai Chemical Compounds
WO2012174489A2 (en) 2011-06-15 2012-12-20 The Ohio State University Small molecule composite surfaces as inhibitors of protein-protein interactions
EA201490177A1 (ru) 2011-06-29 2014-08-29 Оцука Фармасьютикал Ко., Лтд. Хиназолины как терапевтические соединения и связанные с ними способы их применения
CN103087077B (zh) 2011-11-03 2016-05-18 上海希迈医药科技有限公司 噻吩并嘧啶和呋喃并嘧啶类衍生物、其制备方法及其在医药上的应用
JP2013107855A (ja) 2011-11-22 2013-06-06 Mitsubishi Tanabe Pharma Corp 医薬組成物
US9745631B2 (en) 2011-12-20 2017-08-29 Dana-Farber Cancer Institute, Inc. Methods for diagnosing and treating oncogenic kras-associated cancer
WO2013096151A1 (en) 2011-12-22 2013-06-27 Glaxosmithkline Llc Chemical compounds
ES2575604T3 (es) 2012-01-13 2016-06-29 Bristol-Myers Squibb Company Compuestos de piridilo sustituidos con tiazolilo o tiadiazolilo útiles como inhibidores cinasa
EP2828250B1 (en) 2012-03-19 2021-03-10 Imperial College Innovations Limited Quinazoline compounds and their use in therapy
WO2013155077A1 (en) 2012-04-09 2013-10-17 Board Of Regents,The University Of Texas System Response markers for src inhibitor therapies
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
CN104685055A (zh) 2012-05-09 2015-06-03 格兰达利斯有限公司 对单核苷酸KRAS突变特异的双功能短发夹RNA(bi-shRNA)
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
NZ703495A (en) 2012-07-11 2018-02-23 Blueprint Medicines Corp Inhibitors of the fibroblast growth factor receptor
US20150299188A1 (en) 2012-08-24 2015-10-22 Takeda Pharmaceutical Company Limited Heterocyclic compound
CN202931543U (zh) 2012-10-19 2013-05-08 深圳Tcl新技术有限公司 扬声器
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
WO2014159837A1 (en) 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
TW201524952A (zh) 2013-03-15 2015-07-01 Araxes Pharma Llc Kras g12c之共價抑制劑
JP6518656B2 (ja) 2013-06-13 2019-05-22 バイオデシー, インコーポレイテッド 標的生体実体を標的にする生化学実体候補をスクリーニングする方法
CN108440515B (zh) 2013-07-03 2022-05-03 卡尔约药物治疗公司 取代的苯并呋喃基和苯并噁唑基化合物及其用途
MX367085B (es) 2013-07-31 2019-08-05 Merck Patent Gmbh Piridinas, pirimidinas y pirazinas como inhibidores de tirosina cinasa de bruton e inhibidores y usos de las mismas.
CN104418860B (zh) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 嘧啶并杂环类化合物及其药用组合物和应用
JP6559123B2 (ja) * 2013-10-10 2019-08-14 アラクセス ファーマ エルエルシー Krasg12cの阻害剤
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
US9376559B2 (en) 2013-11-22 2016-06-28 Exxonmobil Chemical Patents Inc. Reverse staged impact copolymers
WO2015108992A1 (en) 2014-01-15 2015-07-23 Blueprint Medicines Corporation Heterobicyclic compounds and their use as fgfr4 receptor inhibitors
CN105916859A (zh) * 2014-02-03 2016-08-31 卡迪拉保健有限公司 杂环化合物
CA3175724C (en) 2014-03-20 2024-01-09 Capella Therapeutics, Inc. Benzimidazole derivatives, and pharmaceutical compositions and methods of use thereof
PE20170331A1 (es) 2014-03-24 2017-04-28 Guangdong Zhongsheng Pharmaceutical Co Ltd Derivados quinolina como inhibidores smo
MA40074A (fr) 2014-05-30 2015-12-03 Univ Columbia Composés liant ras multivalents
EP3160486B1 (en) 2014-06-27 2020-11-18 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
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
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
US20160219959A1 (en) 2015-01-23 2016-08-04 Bella Lash Extensions, Llc Tray for holding eyelash extensions and processes for applying eyelash extensions
HK1245677A1 (zh) * 2015-01-23 2018-08-31 Aclaris Therapeutics, Inc. 用於治疗炎症和癌症的杂环itk抑制剂
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
WO2017015562A1 (en) 2015-07-22 2017-01-26 Araxes Pharma Llc Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
WO2017058792A1 (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
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
US10457669B2 (en) 2015-10-21 2019-10-29 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
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
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
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
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
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
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer

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