TW201900633A - Kras之共價抑制劑 - Google Patents

Kras之共價抑制劑 Download PDF

Info

Publication number
TW201900633A
TW201900633A TW107117823A TW107117823A TW201900633A TW 201900633 A TW201900633 A TW 201900633A TW 107117823 A TW107117823 A TW 107117823A TW 107117823 A TW107117823 A TW 107117823A TW 201900633 A TW201900633 A TW 201900633A
Authority
TW
Taiwan
Prior art keywords
group
compound
alkyl
cancer
aminoalkyl
Prior art date
Application number
TW107117823A
Other languages
English (en)
Chinese (zh)
Inventor
李梁山
俊 方
吳濤
劉源
王禕
任平達
毅 劉
Original Assignee
美商亞瑞克西斯製藥公司
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 美商亞瑞克西斯製藥公司 filed Critical 美商亞瑞克西斯製藥公司
Publication of TW201900633A publication Critical patent/TW201900633A/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW107117823A 2017-05-25 2018-05-24 Kras之共價抑制劑 TW201900633A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762511163P 2017-05-25 2017-05-25
US62/511,163 2017-05-25
US201862625889P 2018-02-02 2018-02-02
US62/625,889 2018-02-02

Publications (1)

Publication Number Publication Date
TW201900633A true TW201900633A (zh) 2019-01-01

Family

ID=63586845

Family Applications (1)

Application Number Title Priority Date Filing Date
TW107117823A TW201900633A (zh) 2017-05-25 2018-05-24 Kras之共價抑制劑

Country Status (14)

Country Link
US (4) US10745385B2 (enExample)
EP (1) EP3630745A2 (enExample)
JP (1) JP2020521742A (enExample)
KR (1) KR20200010306A (enExample)
CN (1) CN110869358A (enExample)
AU (1) AU2018271990A1 (enExample)
BR (1) BR112019024674A2 (enExample)
CA (1) CA3063440A1 (enExample)
MX (1) MX2019013954A (enExample)
PH (1) PH12019550248A1 (enExample)
SG (1) SG10202113146UA (enExample)
TW (1) TW201900633A (enExample)
WO (1) WO2018218070A2 (enExample)
ZA (1) ZA202101138B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112707846A (zh) * 2019-10-25 2021-04-27 成都伊诺达博医药科技有限公司 一种达克替尼关键中间体的制备方法
TWI760919B (zh) * 2019-11-15 2022-04-11 大陸商四川海思科製藥有限公司 一種嘧啶並環衍生物及其在醫藥上的應用

Families Citing this family (132)

* Cited by examiner, † Cited by third party
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
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10858343B2 (en) 2015-09-28 2020-12-08 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
US10730867B2 (en) 2015-09-28 2020-08-04 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
EP3356339A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
TW201726656A (zh) 2015-11-16 2017-08-01 亞瑞克西斯製藥公司 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法
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
JP2019529484A (ja) 2016-09-29 2019-10-17 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阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
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
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
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
TW201900633A (zh) 2017-05-25 2019-01-01 美商亞瑞克西斯製藥公司 Kras之共價抑制劑
WO2018218071A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
JP2020521740A (ja) * 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体ｋｒａｓ、ｈｒａｓまたはｎｒａｓの調節因子としてのキナゾリン誘導体
JP7720698B2 (ja) 2018-04-04 2025-08-08 アルビナス・オペレーションズ・インコーポレイテッド タンパク質分解の調節因子および関連する使用方法
CN119954787A (zh) 2018-04-18 2025-05-09 星座制药公司 甲基修饰酶的调节剂、其组合物和用途
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
US11919912B2 (en) 2018-05-21 2024-03-05 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
WO2020085493A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 新規なインダゾール化合物又はその塩
US11236068B2 (en) 2018-11-09 2022-02-01 Genentech, Inc. Fused ring compounds
EP3908283A4 (en) * 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
CN113382774A (zh) 2019-02-12 2021-09-10 诺华股份有限公司 包含tno155和krasg12c抑制剂的药物组合
EP3935060B1 (en) 2019-03-05 2023-11-15 Astrazeneca AB Fused tricyclic compounds useful as anticancer agents
AU2020279253A1 (en) * 2019-05-20 2021-12-16 1200 Pharma Llc KRAS G12C inhibitors and uses thereof
JP7584451B2 (ja) * 2019-05-29 2024-11-15 上▲海▼翰森生物医▲薬▼科技有限公司 窒素含有複素環系誘導物レギュレーター、その製造方法及び使用
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
US12421236B2 (en) 2019-06-25 2025-09-23 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Seven-membered heterocyclic derivative acting as KRAS G12C mutant protein inhibitor
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
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
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
AU2020379731A1 (en) 2019-11-04 2022-05-05 Revolution Medicines, Inc. Ras inhibitors
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
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
WO2021106231A1 (en) * 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
EP4015520B1 (en) * 2019-12-02 2025-02-19 280 Bio, Inc. Oxygen-containing heterocyclic compound, preparation method and application thereof
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
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
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
WO2021216770A1 (en) * 2020-04-22 2021-10-28 Accutar Biotechnology Inc. Substituted tetrahydroquinazoline compounds as kras inhibitors
US20230174526A1 (en) * 2020-04-29 2023-06-08 Shanghai Ringene Biopharma Co., Ltd. Benzothiazolyl biaryl compound, and preparation method and use
TW202214253A (zh) 2020-06-18 2022-04-16 美商銳新醫藥公司 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法
WO2021259331A1 (zh) * 2020-06-24 2021-12-30 南京明德新药研发有限公司 八元含n杂环类化合物
CN115836055A (zh) * 2020-06-30 2023-03-21 益方生物科技(上海)股份有限公司 喹唑啉化合物、其制备方法和用途
EP4203952A4 (en) * 2020-08-28 2024-12-11 Kumquat Biosciences Inc. HETEROCYCLIC COMPOUNDS AND USES THEREOF
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
MX2023002942A (es) 2020-09-11 2023-05-22 Mirati Therapeutics Inc Formas cristalinas de un inhibidor de kras g12c.
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
KR20230094198A (ko) 2020-09-23 2023-06-27 에라스카, 아이엔씨. 3환식 피리돈 및 피리미돈
EP4223761A4 (en) * 2020-09-30 2025-03-12 Shanghai Pharmaceuticals Holding Co., Ltd. QUINAZOLINE COMPOUND AND ITS APPLICATION
WO2022087624A1 (en) * 2020-10-21 2022-04-28 Bioardis Llc Compounds as ras inhibitors and uses thereof
US20240034733A1 (en) * 2020-11-03 2024-02-01 Mirati Therapeutics, Inc. Kras g12d inhibitors
CN120887884A (zh) * 2020-11-06 2025-11-04 泰励生物科技（上海）有限公司 用于癌症治疗的KRas抑制剂
CN114920738B (zh) * 2020-11-06 2025-07-29 泰励生物科技（上海）有限公司 用于癌症治疗的KRas抑制剂
WO2022105855A1 (en) * 2020-11-20 2022-05-27 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
CN116490508A (zh) * 2020-11-20 2023-07-25 北京加科思新药研发有限公司 Kras g12d抑制剂
TWI880049B (zh) * 2020-12-04 2025-04-11 美商美國禮來大藥廠 Kras g12c抑制劑
CA3198885A1 (en) 2020-12-15 2022-06-23 Xiaolun Wang Azaquinazoline pan-kras inhibitors
US11999753B2 (en) 2020-12-16 2024-06-04 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
CN113999226B (zh) * 2020-12-22 2023-01-06 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
WO2022135470A1 (zh) * 2020-12-22 2022-06-30 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
WO2022135390A1 (zh) * 2020-12-25 2022-06-30 四川海思科制药有限公司 己酮糖激酶抑制剂及其用途
CN114685532A (zh) * 2020-12-31 2022-07-01 正大天晴药业集团股份有限公司 大环类化合物及其医药用途
US20240140957A1 (en) * 2021-01-08 2024-05-02 Beigene Switzerland Gmbh Bridged compounds as kras g12d inhibitor and degrader and the use thereof
WO2022152233A1 (en) * 2021-01-15 2022-07-21 Beigene, Ltd. Kras g12c inhibitors
WO2022184178A1 (en) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
AU2022232523A1 (en) * 2021-03-12 2023-11-16 Bristol-Myers Squibb Company Kras g12d inhibitors
WO2022194191A1 (en) * 2021-03-16 2022-09-22 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of kras g12d
WO2022232331A1 (en) * 2021-04-29 2022-11-03 Amgen Inc. Heterocyclic compounds and methods of use
EP4332105A4 (en) * 2021-04-30 2025-05-28 Genfleet Therapeutics (Shanghai) Inc. PYRIDINO- OR PYRIMIDO-CYCLIC COMPOUND, ITS PREPARATION PROCESS AND ITS MEDICAL USE
PE20240089A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cancer
MX2023013085A (es) 2021-05-05 2023-11-16 Revolution Medicines Inc Inhibidores de ras.
US20240300980A1 (en) * 2021-05-22 2024-09-12 Shanghai Kechow Pharma, Inc. Heterocyclic compounds as kras inhibitor, and preparation therefor and use thereof in treatment
AU2022288151A1 (en) * 2021-06-10 2024-01-18 Redx Pharma Plc Quinazoline derivatives useful as ras inhibitiors
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2022268051A1 (zh) * 2021-06-21 2022-12-29 江苏恒瑞医药股份有限公司 稠合四环类化合物、其制备方法及其在医药上的应用
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
AU2022303357A1 (en) * 2021-06-30 2023-12-14 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of kras g12d mutant
CN117460737A (zh) * 2021-07-05 2024-01-26 四川科伦博泰生物医药股份有限公司 杂芳环化合物、其制备方法及用途
AU2022315228A1 (en) * 2021-07-23 2024-02-08 Lawrence Livermore National Security, Llc Compositions and methods for inhibition of ras
WO2023020518A1 (en) * 2021-08-18 2023-02-23 Jacobio Pharmaceuticals Co., Ltd. N-cyclopropylpyrido [4, 3-d] pyrimidin-4-amine derivatives and uses thereof
WO2023031781A1 (en) 2021-09-01 2023-03-09 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
US20240408064A1 (en) * 2021-10-15 2024-12-12 Genetolead Inc. Ras inhibitors, compositions and methods of use thereof
CN116217591A (zh) * 2021-12-02 2023-06-06 思路迪生物医药(上海)有限公司 一类作为kras g12d突变抑制剂的吡啶并嘧啶类衍生物
CN116253748A (zh) * 2021-12-09 2023-06-13 苏州浦合医药科技有限公司 取代的双环杂芳基化合物作为kras g12d抑制剂
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
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
WO2023173016A1 (en) * 2022-03-09 2023-09-14 Blossomhill Therapeutics, Inc. Kras inhibitors for treating disease
WO2023199180A1 (en) 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
EP4540254A1 (en) * 2022-06-14 2025-04-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
JP2025525356A (ja) * 2022-06-15 2025-08-05 ミラティ セラピューティクス， インコーポレイテッド アザキナゾリン汎Ｋｒａｓ阻害剤
WO2024044667A2 (en) * 2022-08-26 2024-02-29 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
GB202212641D0 (en) 2022-08-31 2022-10-12 Jazz Pharmaceuticals Ireland Ltd Novel compounds
IL320639A (en) 2022-11-09 2025-07-01 Revolution Medicines Inc Compounds, complexes and methods for their preparation and use
WO2024158778A1 (en) * 2023-01-24 2024-08-02 Theras, Inc. Compositions and methods for inhibition of ras
TW202444727A (zh) 2023-01-26 2024-11-16 美商艾維納斯手術有限公司 基於cereblon之kras降解protac及其相關用途
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
AU2024253668A1 (en) 2023-04-07 2025-11-13 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
US20240352038A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
AR133028A1 (es) * 2023-06-22 2025-08-20 Astellas Pharma Inc Composición farmacéutica que comprende un degradador de todas las kras
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025019823A1 (en) * 2023-07-20 2025-01-23 Merck Sharp & Dohme Llc Small molecule protein degraders of kras g12d mutant
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
TW202535891A (zh) 2023-10-20 2025-09-16 美商默沙東有限責任公司 Ｋｒａｓ蛋白之小分子抑制劑
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
WO2025230971A1 (en) 2024-04-30 2025-11-06 Kumquat Biosciences Inc. Macrocyclic heterocycles as anticancer agents
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (232)

* 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
US4436748A (en) 1980-10-20 1984-03-13 Hoechst-Roussel Pharmaceuticals Inc. Benzo[b]thiophenes
EP0094498A3 (en) 1982-05-06 1985-04-03 American Cyanamid Company Antiatherosclerotic 1-piperazine derivatives
US4439606A (en) 1982-05-06 1984-03-27 American Cyanamid Company Antiatherosclerotic 1-piperazinecarbonyl compounds
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
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
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
EP0495421B1 (en) 1991-01-15 1996-08-21 Alcon Laboratories, Inc. Use of carrageenans in topical ophthalmic compositions
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
WO1995021271A1 (en) 1994-02-07 1995-08-10 Molecular Tool, Inc. Ligase/polymerase-mediated genetic bit analysistm of single nucleotide polymorphisms and its use in genetic analysis
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
CA2218503C (en) 1995-04-20 2001-07-24 Pfizer Inc. Arylsulfonyl hydroxamic acid derivatives
FR2734816B1 (fr) 1995-05-31 1997-07-04 Adir Nouveaux aryl (alkyl) propylamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
EP2258726A1 (en) 1995-06-14 2010-12-08 The Regents of the University of California High affinity human antibodies to c-erbB-2
EP0780386B1 (en) 1995-12-20 2002-10-02 F. Hoffmann-La Roche Ag Matrix metalloprotease inhibitors
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
KR20000067904A (ko) 1996-07-18 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 매트릭스 메탈로프로테아제의 포스피네이트계 억제제
BR9711223A (pt) 1996-08-23 1999-08-17 Pfizer Derivados de cido arilsulfonilamino-hidrox mico
US5777324A (en) 1996-09-19 1998-07-07 Sequenom, Inc. Method and apparatus for maldi analysis
EP0950059B1 (en) 1997-01-06 2004-08-04 Pfizer Inc. Cyclic sulfone derivatives
IL131042A0 (en) 1997-02-03 2001-01-28 Pfizer Prod Inc Arylsulfonylamino hydroxamic acid derivatives
GB9702194D0 (en) 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
BR9807824A (pt) 1997-02-07 2000-03-08 Pfizer Derivados de n-hidróxi-beta-sulfonil-propionamida e seu uso como inibidores de metaloproteinases de matriz
KR20000070923A (ko) 1997-02-11 2000-11-25 디. 제이. 우드, 스피겔 알렌 제이 아릴설포닐 하이드록삼산 유도체
JP2001511766A (ja) 1997-02-17 2001-08-14 藤沢薬品工業株式会社 新規アミノピペラジン誘導体
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
WO1998057948A1 (en) 1997-06-17 1998-12-23 Schering Corporation Novel n-substituted urea inhibitors of farnesyl-protein transferase
DE69822839T2 (de) 1997-08-08 2004-08-19 Pfizer Products Inc., Groton Derivate von aryloxyarylsulfonylamino hydroxyaminsäuren
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6903118B1 (en) 1997-12-17 2005-06-07 Klinge Pharma Gmbh Piperazinyl-substituted pyridylalkane, alkene and alkine carboxamides
DE19756236A1 (de) 1997-12-17 1999-07-01 Klinge Co Chem Pharm Fab Neue piperazinylsubstituierte Pyridylalkan-, alken- und -alkincarbonsäureamide
JP2001526268A (ja) 1997-12-22 2001-12-18 デュポン ファーマシューティカルズ カンパニー Ｘａ因子阻害剤としての、オルト−置換Ｐ１を有する、窒素含有複素環式芳香族化合物
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
WO1999067641A2 (en) 1998-06-24 1999-12-29 Illumina, Inc. Decoding of array sensors with microspheres
ES2213985T3 (es) 1998-11-05 2004-09-01 Pfizer Products Inc. Derivados de hidroxiamida de acido 5-oxo-pirrolidin-2-carboxilico.
US6429027B1 (en) 1998-12-28 2002-08-06 Illumina, Inc. Composite arrays utilizing microspheres
US6586447B1 (en) 1999-04-01 2003-07-01 Pfizer Inc 3,3-disubstituted-oxindole derivatives useful as anticancer agents
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
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
IL148091A0 (en) 1999-09-13 2002-09-12 Nugen Technologies Inc Methods and compositions for linear isothermal amplification of polynucleotide sequences
TWI271406B (en) 1999-12-13 2007-01-21 Eisai Co Ltd Tricyclic condensed heterocyclic compounds, preparation method of the same and pharmaceuticals comprising the same
US6849639B2 (en) 1999-12-14 2005-02-01 Amgen Inc. Integrin inhibitors and their methods of use
AU4545201A (en) 2000-03-13 2001-09-24 American Cyanamid Co Method of treating or inhibiting colonic polyps
SK13352002A3 (sk) 2000-03-21 2003-05-02 The Procter & Gamble Company Metaloproteázové inhibítory s vedľajším heterocyklickým reťazcom
US6689779B2 (en) 2000-06-05 2004-02-10 Dong A Pharm. Co., Ltd. Oxazolidinone derivatives and a process for the preparation thereof
TWI227231B (en) 2000-07-12 2005-02-01 Novartis Ag 4-benzoyl-piperidine derivatives for treating conditions mediated by CCR-3
MXPA03001359A (es) 2000-08-18 2004-12-13 Millennium Pharm Inc Derivados de quinazolina como inhibidores de cinasa.
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
AU2002338334B8 (en) 2001-04-03 2008-09-18 Merck & Co., Inc. N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B antagonists
EP1382603B1 (en) 2001-04-26 2008-07-23 Eisai R&D Management Co., Ltd. Nitrogenous fused-ring compound having pyrazolyl group as substituent and medicinal composition thereof
JP2002371078A (ja) 2001-06-12 2002-12-26 Sankyo Co Ltd キノリン誘導体及びキノロン誘導体
WO2003004480A2 (en) 2001-07-02 2003-01-16 Novo Nordisk A/S Substituted piperazine and diazepanes as histamine h3 receptor agonists
AU2002352444A1 (en) 2001-12-20 2003-07-09 Celltech R And D Limited Quinazolinedione derivatives
EP1348434A1 (en) 2002-03-27 2003-10-01 Fujisawa Deutschland GmbH Use of pyridyl amides as inhibitors of angiogenesis
US20050256159A1 (en) 2002-10-11 2005-11-17 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11,betahsd1 inhibitors
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
JP2004250329A (ja) 2002-12-26 2004-09-09 Dainippon Pharmaceut Co Ltd イサチン誘導体
EP1597256A1 (en) 2003-02-21 2005-11-23 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
MXPA05009661A (es) 2003-03-12 2006-03-08 Kudos Pharm Ltd Derivados de ftalazinona.
US20050119266A1 (en) 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
SE0302811D0 (sv) 2003-10-23 2003-10-23 Astrazeneca Ab Novel compounds
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
CN1933839A (zh) 2004-01-23 2007-03-21 安进公司 化合物和使用方法
WO2005082892A2 (en) 2004-02-17 2005-09-09 Dr. Reddy's Laboratories Ltd. Triazole compounds as antibacterial agents and pharmaceutical compositions containing them
EP1723146A1 (en) 2004-03-01 2006-11-22 Eli Lilly And Company Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms
GB0405628D0 (en) 2004-03-12 2004-04-21 Glaxo Group Ltd Novel compounds
EP1736465A4 (en) 2004-03-31 2009-06-17 Ajinomoto Kk ANILINE DERIVATIVES
US20060167044A1 (en) 2004-12-20 2006-07-27 Arnaiz Damian O Piperidine derivatives and their use as anti-inflammatory agents
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
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
TW200643015A (en) 2005-03-11 2006-12-16 Akzo Nobel Nv 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives
KR101139263B1 (ko) 2005-03-16 2012-05-16 에프. 호프만-라 로슈 아게 시스-２，４，５-트리아릴-이미다졸린 및 항암 약제로서의그의 용도
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
EP1899332A1 (en) 2005-06-24 2008-03-19 Gilead Sciences, Inc. Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for treating hepatitis c.
US20090099186A1 (en) 2005-10-11 2009-04-16 Leonid Beigelman Inhibitors of viral replication
TW200800201A (en) 2005-11-18 2008-01-01 Lilly Co Eli Pyrimidinyl benzothiophene compounds
EP1966132A2 (en) 2005-12-15 2008-09-10 Boehringer Ingelheim International Gmbh Compounds which modulate the cb2 receptor
JP2009526059A (ja) 2006-02-07 2009-07-16 ワイス １１−ベータｈｓｄ１阻害剤
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
WO2007113226A1 (en) 2006-03-31 2007-10-11 Novartis Ag Organic compounds
US20090124636A1 (en) 2006-04-12 2009-05-14 Pfizer Inc. Chemical compounds
CA2655282A1 (en) 2006-06-16 2007-12-21 High Point Pharmaceuticals, Llc Pharmaceutical use of substituted piperidine carboxamides
DE602007004618D1 (de) 2006-06-22 2010-03-18 Biovitrum Ab Publ Pyridin- und pyrazinderivate als mnk-kinaseinhibitoren
FR2903101B1 (fr) 2006-06-30 2008-09-26 Servier Lab Nouveaux derives naphtaleniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2658764A1 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
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
EP1903038A1 (de) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
WO2008033460A2 (en) 2006-09-15 2008-03-20 Schering Corporation Treating pain, diabetes, and lipid metabolism disorders
EP2134687A1 (en) 2007-03-09 2009-12-23 AstraZeneca AB Piperazine and piperidine mglur5 potentiators
JP5496877B2 (ja) 2007-04-16 2014-05-21 アッヴィ・インコーポレイテッド ７−置換インドールＭｃｌ−１阻害薬
CN102084001B (zh) 2008-03-28 2015-03-18 加利福尼亚太平洋生物科学股份有限公司 用于核酸测序的组合物和方法
EP2133334A1 (en) 2008-06-09 2009-12-16 DAC S.r.l. Heterocyclic derivatives as HDAC inhibitors
EP2328871B1 (en) 2008-08-25 2020-04-01 Novartis AG Hedgehog pathway modulators
WO2010054398A1 (en) 2008-11-10 2010-05-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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
PL2421826T3 (pl) 2009-04-20 2014-03-31 Hoffmann La Roche Pochodne proliny jako inhibitory katepsyn
WO2010124114A1 (en) 2009-04-22 2010-10-28 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
WO2010141817A1 (en) 2009-06-05 2010-12-09 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
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
WO2011031896A2 (en) 2009-09-09 2011-03-17 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
CA2785499C (en) 2009-12-22 2017-05-02 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
EA026042B1 (ru) 2010-01-29 2017-02-28 Оцука Фармасьютикал Ко., Лтд. Двузамещенные производные пиридина в качестве противораковых средств
US20110217309A1 (en) 2010-03-03 2011-09-08 Buck Elizabeth A Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
EA201201289A1 (ru) 2010-03-16 2013-08-30 Мерк Патент Гмбх Морфолинилхиназолины
MX2012012145A (es) 2010-04-28 2012-11-21 Daiichi Sankyo Co Ltd Compuestos [5, 6] heterociclico.
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
BR112013002182B8 (pt) 2010-07-30 2023-02-28 Oncotherapy Science Inc Compostos derivados de quinolina, composição farmacêutica, inibidor de melk, agente modulador de expressão de melk, agente antitumor, agente terapêutico e/ou preventivo para uma doença que envolve a superexpressão de melk contendo os mesmos e uso dos referidos compostos
BR112013005141A2 (pt) 2010-09-03 2016-05-10 Janssen Pharmaceutica Nv diazetidinil diamida como inibidores de monoacilglicerol lipase
HUE034347T2 (en) 2010-09-29 2018-02-28 Intervet Int Bv N-heteroaryl compounds with a cyclic bridge unit for the treatment of parasitic diseases
CA2815350A1 (en) 2010-10-22 2012-04-26 Janssen Pharmaceutica Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
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
AR086798A1 (es) 2011-06-29 2014-01-22 Otsuka Pharma Co Ltd Derivados quinazolinicos utiles para tratar trastornos del sistema nervioso central y composiciones farmaceuticas que los contienen
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
US20150087628A1 (en) 2012-04-10 2015-03-26 The Regents Of The University Of California Compositions and methods for treating cancer
EP2847333B1 (en) 2012-05-09 2025-07-30 Gradalis, Inc. Bi-functional short-hairpin rna (bi-shrna) specific for single-nucleotide kras mutations
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
US8802697B2 (en) 2012-07-11 2014-08-12 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
TW201414737A (zh) 2012-07-13 2014-04-16 必治妥美雅史谷比公司 作爲激酶抑制劑之咪唑并三□甲腈
US20150299188A1 (en) 2012-08-24 2015-10-22 Takeda Pharmaceutical Company Limited Heterocyclic compound
US20150283142A1 (en) 2013-03-15 2015-10-08 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
CN104955824B (zh) 2012-11-20 2017-09-22 豪夫迈·罗氏有限公司 作为含t790m的egfr突变体的抑制剂的氨基嘧啶化合物
BR112015022417A2 (pt) 2013-03-14 2017-07-18 Convergene Llc métodos e composições para inibição de proteínas contendo bromodomínio
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
AU2014239542A1 (en) 2013-03-15 2015-10-01 Araxes Pharma Llc Covalent inhibitors of KRas G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
EP2970219B1 (en) 2013-03-15 2019-02-27 Epizyme, Inc. Carm1 inhibitors and uses thereof
EP3008465B1 (en) 2013-06-13 2019-08-07 Biodesy, Inc. Method of screening candidate biochemical entities targeting a target biochemical entity
US20150005277A1 (en) 2013-06-28 2015-01-01 Beigene, Ltd. Protein Kinase Inhibitors and Uses Thereof
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
RU2712220C2 (ru) 2013-07-31 2020-01-27 Мерк Патент Гмбх Пиридины, пиримидины и пиразины в качестве ингибиторов тирозинкиназы брутона и их применение
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
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
WO2015054572A1 (en) 2013-10-10 2015-04-16 Araxes Pharma Llc Inhibitors of kras g12c
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
TWI542588B (zh) 2014-02-03 2016-07-21 卡迪拉保健有限公司 新穎雜環化合物
US10005765B2 (en) 2014-03-20 2018-06-26 Capella Therapeutics, Inc. Benzimidazole derivatives as ERBB tyrosine kinase inhibitors for the treatment of cancer
NZ724691A (en) 2014-03-24 2018-02-23 Guangdong Zhongsheng Pharmaceutical Co Ltd Quinoline derivatives as smo inhibitors
CA2950581A1 (en) 2014-05-30 2015-12-03 The Trustees Of Columbia University In The City Of New York Multivalent ras binding compounds
JP6640126B2 (ja) 2014-06-27 2020-02-05 セルジーン コーポレイション セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法
WO2016044604A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
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
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
WO2016049524A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
KR102550852B1 (ko) 2014-10-08 2023-07-05 에프. 호프만-라 로슈 아게 알도스테론 신타아제 억제제로서의 스피로다이아민 유도체
US9695200B2 (en) 2015-01-23 2017-07-04 Confluence Life Sciences, Inc. Heterocyclic ITK inhibitors for treating inflammation and cancer
EA201792214A1 (ru) 2015-04-10 2018-01-31 Араксис Фарма Ллк Соединения замещенного хиназолина
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
US10730867B2 (en) 2015-09-28 2020-08-04 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
US10647703B2 (en) 2015-09-28 2020-05-12 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
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356339A1 (en) 2015-09-28 2018-08-08 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
EP3365334B1 (en) 2015-10-21 2024-07-17 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
TW201726656A (zh) * 2015-11-16 2017-08-01 亞瑞克西斯製藥公司 包含經取代雜環基團之２－經取代喹唑啉化合物及其使用方法
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
JP2019529484A (ja) 2016-09-29 2019-10-17 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阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
EP3534899B1 (en) 2016-11-03 2022-06-01 Corvus Pharmaceuticals, Inc. Compounds and methods for modulating interleukin-2-inducible t-cell kinase
EP3573966A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused n-heterocyclic 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
EP3573971A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
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
US11274093B2 (en) 2017-01-26 2022-03-15 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
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
WO2018218071A1 (en) * 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
TW201900633A (zh) 2017-05-25 2019-01-01 美商亞瑞克西斯製藥公司 Kras之共價抑制劑
JP2020521740A (ja) * 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体ｋｒａｓ、ｈｒａｓまたはｎｒａｓの調節因子としてのキナゾリン誘導体
AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
US12134620B2 (en) 2018-08-01 2024-11-05 Araxes Pharma Llc Heterocyclic spiro compounds and methods of use thereof for the treatment of cancer
KR20210083286A (ko) 2018-10-24 2021-07-06 아락세스 파마 엘엘씨 종양 전이를 억제하기 위한 g12c 돌연변이 kras 단백질의 억제제로서 2-(2-아크릴로일-2,6-디아자스피로[3.4]옥탄-6-일)-6-(1h-인다졸-4-일)-벤조니트릴 유도체 및 관련 화합물
AU2019388998A1 (en) 2018-11-29 2021-06-03 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112707846A (zh) * 2019-10-25 2021-04-27 成都伊诺达博医药科技有限公司 一种达克替尼关键中间体的制备方法
CN112707846B (zh) * 2019-10-25 2023-04-21 成都伊诺达博医药科技有限公司 一种达克替尼关键中间体的制备方法
TWI760919B (zh) * 2019-11-15 2022-04-11 大陸商四川海思科製藥有限公司 一種嘧啶並環衍生物及其在醫藥上的應用

Also Published As

Publication number Publication date
KR20200010306A (ko) 2020-01-30
ZA202101138B (en) 2022-09-28
AU2018271990A1 (en) 2019-12-12
EP3630745A2 (en) 2020-04-08
SG10202113146UA (en) 2021-12-30
US20210024501A1 (en) 2021-01-28
US11377441B2 (en) 2022-07-05
MX2019013954A (es) 2020-08-31
US20190062313A1 (en) 2019-02-28
JP2020521742A (ja) 2020-07-27
CN110869358A (zh) 2020-03-06
US20250154133A1 (en) 2025-05-15
CA3063440A1 (en) 2018-11-29
US10745385B2 (en) 2020-08-18
WO2018218070A2 (en) 2018-11-29
WO2018218070A3 (en) 2019-02-07
PH12019550248A1 (en) 2021-01-11
US20230203018A1 (en) 2023-06-29
BR112019024674A2 (pt) 2020-06-16

Similar Documents

Publication Publication Date Title
US11377441B2 (en) Covalent inhibitors of KRAS
JP7628305B2 (ja) 腫瘍転移を阻害するためのｇ１２ｃ変異体ｋｒａｓタンパク質の阻害剤としての２－（２－アクリロイル－２，６－ジアザスピロ［３．４］オクタン－６－イル）－６－（１ｈ－インダゾール－４－イル）－ベンゾニトリル誘導体および関連化合物
US10723738B2 (en) Inhibitors of KRAS G12C mutant proteins
US10736897B2 (en) Compounds and methods of use thereof for treatment of cancer
US11279689B2 (en) 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
JP7327802B2 (ja) 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
US11274093B2 (en) Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US10428064B2 (en) Fused-tricyclic inhibitors of KRAS and methods of use thereof
US20230147053A1 (en) Fused n-heterocyclic compounds and methods of use thereof
US20220112192A1 (en) Compounds and methods of use thereof for treatment of cancer
US20200010454A1 (en) Substituted quinazoline and quinazolinone compounds and methods of use thereof
HK1249513B (en) Fused-tricyclic inhibitors of kras and methods of use thereof