JP2016519072A5 - - Google Patents

Download PDF

Info

Publication number
JP2016519072A5
JP2016519072A5 JP2016502462A JP2016502462A JP2016519072A5 JP 2016519072 A5 JP2016519072 A5 JP 2016519072A5 JP 2016502462 A JP2016502462 A JP 2016502462A JP 2016502462 A JP2016502462 A JP 2016502462A JP 2016519072 A5 JP2016519072 A5 JP 2016519072A5
Authority
JP
Japan
Prior art keywords
pharmaceutically acceptable
compound according
stereoisomer
tautomer
prodrug
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
JP2016502462A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016519072A (ja
JP6473133B2 (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2014/027504 external-priority patent/WO2014152588A1/en
Publication of JP2016519072A publication Critical patent/JP2016519072A/ja
Publication of JP2016519072A5 publication Critical patent/JP2016519072A5/ja
Application granted granted Critical
Publication of JP6473133B2 publication Critical patent/JP6473133B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2016502462A 2013-03-15 2014-03-14 Krasg12cの共有結合性阻害剤 Expired - Fee Related JP6473133B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361852123P 2013-03-15 2013-03-15
US61/852,123 2013-03-15
US201361889480P 2013-10-10 2013-10-10
US61/889,480 2013-10-10
JOP20140098 2014-03-13
JO98/2014 2014-03-13
PCT/US2014/027504 WO2014152588A1 (en) 2013-03-15 2014-03-14 Covalent inhibitors of kras g12c

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2019010309A Division JP6849711B2 (ja) 2013-03-15 2019-01-24 Kras g12cの共有結合性阻害剤

Publications (3)

Publication Number Publication Date
JP2016519072A JP2016519072A (ja) 2016-06-30
JP2016519072A5 true JP2016519072A5 (https=) 2017-04-13
JP6473133B2 JP6473133B2 (ja) 2019-02-20

Family

ID=54251765

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2016502462A Expired - Fee Related JP6473133B2 (ja) 2013-03-15 2014-03-14 Krasg12cの共有結合性阻害剤
JP2019010309A Active JP6849711B2 (ja) 2013-03-15 2019-01-24 Kras g12cの共有結合性阻害剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2019010309A Active JP6849711B2 (ja) 2013-03-15 2019-01-24 Kras g12cの共有結合性阻害剤

Country Status (8)

Country Link
EP (2) EP3401314B1 (https=)
JP (2) JP6473133B2 (https=)
CN (1) CN105189456B (https=)
AU (2) AU2014239542A1 (https=)
CA (1) CA2904393A1 (https=)
MX (1) MX364438B (https=)
TW (1) TW201524952A (https=)
WO (1) WO2014152588A1 (https=)

Families Citing this family (173)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2836482B1 (en) 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer
MX394360B (es) 2013-03-14 2025-03-24 Sumitomo Pharma Oncology Inc Inhibidores de jak2 y alk2 y metodos para su uso.
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
US9745319B2 (en) 2013-03-15 2017-08-29 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
WO2015188073A1 (en) 2014-06-06 2015-12-10 Research Triangle Institute Apelin receptor (apj) agonists and uses thereof
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
ES2826443T3 (es) * 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
MX373656B (es) 2015-03-30 2020-04-02 Mission Therapeutics Ltd Compuestos de 1-ciano-pirrolidina como inhibidores de las enzimas desubiquitinantes, como la hidrolasa 30 de la c-terminal de la ubiquitina (usp30), y el uso de los mismos en el tratamiento de condiciones de disfunción mitocondrial y tratamiento de cancér.
JP2018513853A (ja) 2015-04-10 2018-05-31 アラクセス ファーマ エルエルシー 置換キナゾリン化合物およびその使用方法
JP6789239B2 (ja) * 2015-04-15 2020-11-25 アラクセス ファーマ エルエルシー Krasの縮合三環系インヒビターおよびその使用の方法
BR112017023821A2 (pt) 2015-05-06 2018-07-31 Leidos Biomedical Res Inc moduladores de k-ras
WO2016200726A1 (en) * 2015-06-08 2016-12-15 Texas Tech University System Inhibitors of mci-1 as drugs to overcome resistance to braf inhibitors and mek inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
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
WO2017058807A1 (en) * 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 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
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
JP2018533939A (ja) 2015-10-19 2018-11-22 アラクセス ファーマ エルエルシー Rasの阻害剤をスクリーニングするための方法
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
CN108602806B (zh) 2015-12-09 2022-07-12 研究三角协会 改进的爱帕琳肽受体(apj)激动剂及其用途
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
JP7039489B2 (ja) 2016-05-18 2022-03-22 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
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
TW201825458A (zh) 2016-09-20 2018-07-16 英商葛蘭素史克智慧財產(第二)有限公司 Trpv4拮抗劑
US10590077B2 (en) 2016-09-20 2020-03-17 Glaxosmithkline Intellectual Property Development Limited TRPV4 antagonists
CN109790116B (zh) 2016-09-20 2022-10-28 葛兰素史密斯克莱知识产权(第2 号)有限公司 Trpv4拮抗剂
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
WO2018098352A2 (en) 2016-11-22 2018-05-31 Jun Oishi Targeting kras induced immune checkpoint expression
BR112019012263A2 (pt) * 2016-12-15 2020-01-28 The Regents Of The University Of California composições e métodos para tratar câncer
JP7219218B2 (ja) 2016-12-22 2023-02-07 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 新規のベンジルアミノ置換キナゾリンおよびsos1阻害剤としての誘導体
WO2018119183A2 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
US11986480B2 (en) 2017-02-03 2024-05-21 Tohoku University Heterocyclic compound
ES2747768T3 (es) 2017-03-20 2020-03-11 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)
BR112019021899A2 (pt) 2017-04-20 2020-08-18 The Regents Of The University Of California moduladores de k-ras
EA201992781A1 (ru) 2017-05-22 2020-04-01 Эмджен Инк. Ингибиторы g12c kras и способы их применения
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
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
EP3700901A1 (en) 2017-10-24 2020-09-02 Genentech, Inc. (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
HRP20230377T1 (hr) 2017-11-15 2023-06-23 Mirati Therapeutics, Inc. Inhibitori mutacije kras g12c
RS64167B1 (sr) 2017-12-21 2023-05-31 Boehringer Ingelheim Int Benzilamino supstituisani piridopirimidinoni i derivati kao sos1 inhibitori
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
CN112533602A (zh) 2018-04-05 2021-03-19 大日本住友制药肿瘤公司 Axl激酶抑制剂及其用途
TW202012396A (zh) * 2018-04-18 2020-04-01 美商德洛斯股份有限公司 具乙烯磺醯胺部分之k-ras調節劑
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES2995514T3 (en) 2018-05-04 2025-02-10 Amgen Inc Kras g12c inhibitors and methods of using the same
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
EP3790886B1 (en) 2018-05-10 2024-06-26 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
US20190375749A1 (en) 2018-06-11 2019-12-12 Amgen Inc. Kras g12c inhibitors and methods of using the same
ES3060664T3 (en) 2018-06-12 2026-03-27 Amgen Inc Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
MX2021000977A (es) 2018-07-26 2021-04-12 Sumitomo Pharma Oncology Inc Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos.
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
CA3112043A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
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
SMT202500028T1 (it) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Terapie combinate
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
EP3628664A1 (en) 2018-09-25 2020-04-01 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Irreversible inhibitors of kras g12c mutant
WO2020086739A1 (en) * 2018-10-24 2020-04-30 Araxes Pharma Llc 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(1h-indazol-4-yl)-benzonitrile derivatives and related compounds as inhibitors of g12c mutant kras protein for inhibiting tumor metastasis
WO2020085504A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法
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
US11053226B2 (en) 2018-11-19 2021-07-06 Amgen Inc. KRAS G12C inhibitors and methods of using the same
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
CN113164418A (zh) 2018-12-05 2021-07-23 米拉蒂治疗股份有限公司 组合疗法
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
CN109646680B (zh) * 2019-01-31 2020-02-11 四川大学华西医院 一种治疗kras突变型肠癌的联合用药物
WO2020165732A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
WO2020173935A1 (en) 2019-02-26 2020-09-03 Boehringer Ingelheim International Gmbh New isoindolinone substituted indoles and derivatives as ras inhibitors
ES3010507T3 (en) 2019-03-05 2025-04-03 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
CN111662232B (zh) * 2019-03-06 2022-08-02 中国科学院上海药物研究所 具有2h-吲唑结构的小分子化合物及其合成和应用
AU2020256166A1 (en) 2019-04-02 2021-10-14 Aligos Therapeutics, Inc. Compounds targeting PRMT5
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
NZ782284A (en) 2019-05-21 2024-11-29 Amgen Inc Solid state forms
WO2020239123A1 (zh) * 2019-05-31 2020-12-03 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
CN113993860B (zh) * 2019-06-25 2023-08-01 正大天晴药业集团股份有限公司 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
US20220378756A1 (en) 2019-09-19 2022-12-01 Forma Therapeutics, Inc. Activating pyruvate kinase r
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
CN112225734B (zh) * 2019-10-25 2021-12-07 南京瑞捷医药科技有限公司 Kras g12c抑制剂及其用途
CN114867726B (zh) 2019-10-28 2023-11-28 默沙东有限责任公司 Kras g12c突变体的小分子抑制剂
WO2021085653A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
CN120699039A (zh) 2019-11-04 2025-09-26 锐新医药公司 Ras抑制剂
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
CN110698378B (zh) * 2019-11-19 2021-03-19 上海皓元生物医药科技有限公司 2-(羟基-(甲基环丙基)苯基氨基)-1-哌嗪基乙酮衍生物的制备方法
MX2022006052A (es) * 2019-11-22 2022-08-15 Univ California Inhibidores de la caspasa 6 y usos de los mismos.
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
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
WO2021215545A1 (en) 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Anticancer combination therapy with n-(1-acryloyl-azetidin-3-yl)-2-((1h-indazol-3-yl)amino)methyl)-1h-imidazole-5-carboxamide inhibitor of kras-g12c
WO2021215544A1 (en) * 2020-04-24 2021-10-28 Taiho Pharmaceutical Co., Ltd. Kras g12d protein inhibitors
CN115135636B (zh) * 2020-04-29 2024-08-23 北京泰德制药股份有限公司 喹喔啉酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
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
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
WO2022056307A1 (en) 2020-09-11 2022-03-17 Mirati Therapeutics, Inc. Crystalline forms of a kras g12c inhibitor
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
AU2021347232A1 (en) 2020-09-23 2023-04-27 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN114249703B (zh) * 2020-09-25 2023-10-13 四川科瑞德制药股份有限公司 适合工业放大的医药中间体的制备方法
WO2022132200A1 (en) 2020-12-15 2022-06-23 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2022133345A1 (en) 2020-12-18 2022-06-23 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
US20240051956A1 (en) 2020-12-22 2024-02-15 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
EP4329750A4 (en) 2021-04-27 2025-06-18 Merck Sharp & Dohme LLC Small-molecule inhibitors of the KRAS G12C mutant
CA3217393A1 (en) 2021-05-05 2022-11-10 Elena S. Koltun Ras inhibitors
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
US20240317721A1 (en) 2021-06-23 2024-09-26 Novartis Ag Pyrazolyl derivatives as inhibitors of the kras mutant protein
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
EP4373822A2 (en) 2021-07-23 2024-05-29 Theras Inc. Compositions and methods for inhibition of ras
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CN113956233B (zh) * 2021-10-22 2023-06-06 南方医科大学 一种酰胺类化合物或其药学上可接受的盐及其制备方法和应用
WO2023066371A1 (zh) 2021-10-22 2023-04-27 江苏恒瑞医药股份有限公司 含氮的四环化合物、其制备方法及其在医药上的应用
CN114380682A (zh) * 2021-10-27 2022-04-22 上海毕得医药科技股份有限公司 一种2,3-二氟-4-甲氧基苯乙酸合成方法
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
WO2023152255A1 (en) 2022-02-10 2023-08-17 Bayer Aktiengesellschaft Fused pyrimidines as kras inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
JP2026504244A (ja) 2022-11-09 2026-02-04 レヴォリューション・メディスンズ,インコーポレイテッド 化合物、複合体、ならびにそれらの調製方法及びそれらの使用方法
WO2024182447A1 (en) * 2023-02-28 2024-09-06 Vividion Therapeutics, Inc. Compounds and methods for modulating ras-pi3k
WO2024201691A1 (ja) 2023-03-28 2024-10-03 国立大学法人東北大学 オートファジーを誘導する化合物のスクリーニング方法
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
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
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024248123A1 (ja) 2023-06-02 2024-12-05 第一三共株式会社 抗her3抗体-薬物コンジュゲートとrasg12c阻害剤の組み合わせ
GB2631397A (en) 2023-06-28 2025-01-08 Sevenless Therapeutics Ltd New treatments for pain
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
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
GB2633813A (en) 2023-09-21 2025-03-26 Sevenless Therapeutics Ltd New treatments for pain
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025085748A1 (en) 2023-10-20 2025-04-24 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2025083426A1 (en) 2023-10-20 2025-04-24 Sevenless Therapeutics Limited New treatments for pain
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
WO2025146548A1 (en) 2024-01-04 2025-07-10 Sevenless Therapeutics Limited Sos1 inhibitors useful to treat pain and cancer
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (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
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
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
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and 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
CN119039303A (zh) * 2024-09-20 2024-11-29 上海信诺维生物医药有限公司 一种螺环化合物
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
IL111730A (en) * 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
DK0821671T3 (da) 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
US6011029A (en) * 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
EP0923585B1 (en) 1996-07-18 2002-05-08 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
WO1998007697A1 (en) 1996-08-23 1998-02-26 Pfizer Inc. Arylsulfonylamino hydroxamic acid derivatives
WO1998030566A1 (en) 1997-01-06 1998-07-16 Pfizer Inc. Cyclic sulfone derivatives
EP0977733B1 (en) 1997-02-03 2003-09-03 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EA002546B1 (ru) 1997-02-11 2002-06-27 Пфайзер Инк. Производные арилсульфонилгидроксамовой кислоты
EP0968201A2 (en) * 1997-02-17 2000-01-05 Fujisawa Pharmaceutical Co., Ltd. New aminopiperazine derivatives
IL133389A0 (en) * 1997-06-17 2001-04-30 Schering Corp Novel n-substituted urea inhibitors of farnesyl-protein transferase
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
IL136637A0 (en) * 1997-12-22 2001-06-14 Du Pont Pharm Co Nitrogen containing heteroaromatics with ortho-substituted pi'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
TWI227231B (en) * 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
US7429599B2 (en) * 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
WO2002080928A1 (en) * 2001-04-03 2002-10-17 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists
EP1348434A1 (en) * 2002-03-27 2003-10-01 Fujisawa Deutschland GmbH Use of pyridyl amides as inhibitors of angiogenesis
CA2501611A1 (en) * 2002-10-11 2004-04-22 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors
BRPI0408284B8 (pt) * 2003-03-12 2021-05-25 Kudos Pharm Ltd compostos derivados de ftalazinona, seu uso e composição farmacêutica compreendendo os mesmos
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
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
KR20080066949A (ko) * 2005-10-11 2008-07-17 인터뮨, 인크. 바이러스 복제 억제제
EP2133334A1 (en) * 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
US8455476B2 (en) * 2009-04-22 2013-06-04 Janssen Pharmaceutica, Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
EP2475375A4 (en) * 2009-09-09 2013-02-20 Avila Therapeutics Inc PI3 KINASE INHIBITORS AND USES THEREOF
US8658131B2 (en) * 2010-06-21 2014-02-25 Washington University Compounds comprising 4-benzoylpiperidine as a sigma-1-selective ligand
WO2012054716A1 (en) * 2010-10-22 2012-04-26 Janssen Pharmaceutica Nv. Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
EP2731940B1 (en) * 2011-07-13 2015-08-19 Novartis AG 4 - piperidinyl compounds for use as tankyrase inhibitors
CN104254533B (zh) * 2012-01-13 2017-09-08 百时美施贵宝公司 用作激酶抑制剂的噻唑或噻二唑取代的吡啶基化合物
EP2836482B1 (en) * 2012-04-10 2019-12-25 The Regents of The University of California Compositions and methods for treating cancer

Similar Documents

Publication Publication Date Title
JP2016519072A5 (https=)
JP2019529484A5 (https=)
JP2016506960A5 (https=)
JP2017528498A5 (https=)
JP2015520769A5 (https=)
JP2017514855A5 (https=)
JP2020521740A5 (https=)
JP2018520195A5 (https=)
JP2015523383A5 (https=)
JP2014503567A5 (https=)
JP2018524390A5 (https=)
JP2018533611A5 (https=)
JP2016512520A5 (https=)
JP2013529649A5 (https=)
RU2015143717A (ru) 2-Аминопиримидин-6-оны и аналоги, проявляющие противораковые и антипролиферативные действия
JP2018511631A5 (https=)
JP2018528261A5 (https=)
JP2016530283A5 (https=)
JP2017526677A5 (https=)
JP2016506962A5 (https=)
RU2012151012A (ru) Циклопропиловые дикарбоксамиды и аналоги, обладающие противораковым и антипролиферативным действием
BR112014019478A2 (pt) composto ou um sal farmacologicamente aceitável do mesmo, composição farmacêutica, uso de um composto ou de um sal farmacologicamente aceitável do mesmo, formulação inibidor do canal de sódio, métodos para tratamento e/ou prevenção de dor e de uma doença.
JP2013509431A5 (https=)
RU2015147447A (ru) Производные доластатина 10 и ауристатинов
JP2017511321A5 (https=)