UA129778C2 - Низькомолекулярні інгібітори g12c-мутантного kras - Google Patents

Низькомолекулярні інгібітори g12c-мутантного kras

Info

Publication number
UA129778C2
UA129778C2 UAA202201759A UAA202201759A UA129778C2 UA 129778 C2 UA129778 C2 UA 129778C2 UA A202201759 A UAA202201759 A UA A202201759A UA A202201759 A UAA202201759 A UA A202201759A UA 129778 C2 UA129778 C2 UA 129778C2
Authority
UA
Ukraine
Prior art keywords
mmol
ipi
tert
oxy
formula
Prior art date
Application number
UAA202201759A
Other languages
English (en)
Ukrainian (uk)
Inventor
Інду Бхаратхан
Инду Бхаратхан
Симон Ґатіака
Симон Гатиака
Томас Г. Ґрегем
Томас Х. Грехем
Юнсинь Гань
Юнсинь ХАНЬ
Тімоті Гендерсон
Тимоти Хендерсон
Елізабет Геннессі
Элизабет Хеннесси
Сяошень Ма
Райан Отте
Анандан Палані
Анандан ПАЛАНИ
Девід Л. Сломан
Девид Л. Сломан
Original Assignee
Мерк Шарп Енд Доум Елелсі
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 Мерк Шарп Енд Доум Елелсі filed Critical Мерк Шарп Енд Доум Елелсі
Publication of UA129778C2 publication Critical patent/UA129778C2/uk

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
UAA202201759A 2019-10-28 2020-10-27 Низькомолекулярні інгібітори g12c-мутантного kras UA129778C2 (uk)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962926879P 2019-10-28 2019-10-28
US202063030014P 2020-05-26 2020-05-26
PCT/US2020/057496 WO2021086833A1 (en) 2019-10-28 2020-10-27 Small molecule inhibitors of kras g12c mutant

Publications (1)

Publication Number Publication Date
UA129778C2 true UA129778C2 (uk) 2025-07-30

Family

ID=73598936

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA202201759A UA129778C2 (uk) 2019-10-28 2020-10-27 Низькомолекулярні інгібітори g12c-мутантного kras

Country Status (22)

Country Link
US (3) US11697657B2 (https=)
EP (1) EP4051678B1 (https=)
JP (2) JP7340100B2 (https=)
KR (1) KR20220106980A (https=)
CN (1) CN114867726B (https=)
AU (1) AU2020372881A1 (https=)
BR (1) BR112022007783A8 (https=)
CA (1) CA3158793A1 (https=)
CO (1) CO2022006858A2 (https=)
CR (1) CR20220230A (https=)
DO (1) DOP2022000090A (https=)
EC (1) ECSP22033597A (https=)
GE (2) GEP20247710B (https=)
IL (1) IL292438B2 (https=)
JO (1) JOP20220101A1 (https=)
MX (1) MX2022005053A (https=)
PE (1) PE20221253A1 (https=)
PH (1) PH12022551027A1 (https=)
TW (1) TWI911172B (https=)
UA (1) UA129778C2 (https=)
WO (1) WO2021086833A1 (https=)
ZA (1) ZA202205938B (https=)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210006356A (ko) 2018-04-04 2021-01-18 아비나스 오퍼레이션스, 인코포레이티드 단백질분해 조절제 및 연관된 사용 방법
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
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
WO2020055761A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
SMT202500028T1 (it) 2018-09-10 2025-03-12 Mirati Therapeutics Inc Terapie combinate
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
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
MX2021014961A (es) 2019-06-06 2022-01-24 Hutchison Medipharma Ltd Compuestos triciclicos y su uso.
EP3990448A4 (en) * 2019-06-24 2023-08-02 Guangdong Newopp Biopharmaceuticals Co., Ltd. HETEROCYCLIC COMPOUNDS AS INHIBITORS OF KRAS G12C
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
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
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
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
WO2021147965A1 (zh) * 2020-01-21 2021-07-29 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
CN113248521B (zh) * 2020-02-11 2023-07-18 上海和誉生物医药科技有限公司 一种k-ras g12c抑制剂及其制备方法和应用
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
WO2022111521A1 (zh) * 2020-11-24 2022-06-02 杭州多域生物技术有限公司 一种芳香化合物、其制备方法及应用
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
CN116249703A (zh) * 2020-12-21 2023-06-09 上海和誉生物医药科技有限公司 一种大环k-ras g12c抑制剂,其制备方法和用途
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
CN117177980A (zh) * 2021-05-06 2023-12-05 上海齐鲁制药研究中心有限公司 十二元大环类化合物
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
US20240327929A1 (en) * 2021-08-12 2024-10-03 Merck Sharp & Dohme Llc Dosage regimen for administration of belzutifan
CN115894520A (zh) * 2021-09-23 2023-04-04 上海和誉生物医药科技有限公司 一种大环k-ras g12c抑制剂及其制备方法和在药学上的应用
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CN116375746B (zh) * 2021-12-23 2025-08-05 上海馨远医药科技有限公司 一种(2-氟-6-羟基苯基)三氟硼酸钾的制备方法
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
CN116063211B (zh) * 2023-02-14 2023-11-10 斯坦德药典标准物质研发(湖北)有限公司 一种Belzutifan的制备方法
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
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
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
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
WO2025090809A1 (en) * 2023-10-25 2025-05-01 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
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
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras 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
WO2026015796A1 (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
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
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
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (225)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4034075A (en) 1972-07-03 1977-07-05 Allen & Hanburys Limited Quinaldic acid derivatives
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
JP3560609B2 (ja) 1992-11-13 2004-09-02 イミュネックス・コーポレーション Elkリガンドと呼ばれる新規なサイトカイン
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
US5912253A (en) 1993-12-17 1999-06-15 Novartis Ag Rapamycin derivatives
EP0756627A1 (en) 1994-04-15 1997-02-05 Amgen Inc. Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
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
EP0833828B1 (en) 1995-06-09 2002-11-20 Novartis AG Rapamycin derivatives
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
US6258823B1 (en) 1996-07-12 2001-07-10 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
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
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
AU730248B2 (en) 1997-08-08 2001-03-01 Pfizer Products Inc. Aryloxyarylsulfonylamino hydroxamic acid derivatives
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
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
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
ES2262518T5 (es) 1999-06-07 2009-05-08 Immunex Corporation Antagonistas de tek.
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
CA2400040A1 (en) 2000-02-25 2001-08-30 Immunex Corporation Integrin antagonists
US6861424B2 (en) 2001-06-06 2005-03-01 Schering Aktiengesellschaft Platelet adenosine diphosphate receptor antagonists
EP1442039A1 (en) 2001-10-31 2004-08-04 Bayer HealthCare AG Pyrimido (4,5-b) indole derivatives
AU2004255340B2 (en) 2003-07-08 2008-05-01 Novartis Ag Use of rapamycin and rapamycin derivatives for the treatment of bone loss
EP1648900A4 (en) 2003-07-11 2010-02-10 Ariad Pharma Inc PHOSPHORUS MACROCYCLES
AR045134A1 (es) 2003-07-29 2005-10-19 Smithkline Beecham Plc Compuesto de 1h - imidazo [4,5-c] piridin-ilo, composicion farmaceutica que lo comprende, proceso para prepararla, su uso para preparar dicha composicion farmaceutica, combinacion farmaceutica, uso de la combinacion farmaceutica para la preparacion de un medicamento, procedimientos para preparar dic
WO2005019177A1 (en) 2003-08-14 2005-03-03 Icos Corporation Aminopiperidine amide derivatives as vla-1 integrin antagonists and uses thereof
BR122020017756B1 (pt) 2004-08-26 2022-02-15 Pfizer Inc Uso de compostos de aminoeteroarila enantiomericamente puros na preparação de um medicamento para o tratamento de crescimento celular anormal em um mamífero
PE20060608A1 (es) 2004-10-13 2006-08-22 Wyeth Corp Analogos de 17-hidroxiwortmanina como inhibidores de pi3k
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CN101267824A (zh) 2005-09-20 2008-09-17 辉瑞产品公司 使用酪氨酸激酶抑制剂的治疗剂型和方法
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
US8278313B2 (en) 2008-03-11 2012-10-02 Abbott Laboratories Macrocyclic spiro pyrimidine derivatives
WO2010064705A1 (ja) 2008-12-05 2010-06-10 大日本住友製薬株式会社 H4受容体アンタゴニスト作用を有する新規7位置換ジヒドロピラノピリミジン誘導体
SG176959A1 (en) 2009-06-24 2012-01-30 Genentech Inc Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
KR101658274B1 (ko) 2011-04-06 2016-09-22 다이호야쿠힌고교 가부시키가이샤 신규 이미다조 옥사진 화합물 또는 그의 염
AR090037A1 (es) 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
EP3378476A1 (en) 2012-06-08 2018-09-26 Sensorion H4 receptor inhibitors for treating tinnitus
JP6460991B2 (ja) 2012-09-12 2019-01-30 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 抗菌剤として使用するための三環式ジャイレース阻害剤
KR20150130389A (ko) 2013-03-13 2015-11-23 더 리젠츠 오브 더 유니버시티 오브 미시간 티에노피리미딘 및 티에노피리딘 화합물을 포함하는 조성물 및 이의 사용 방법
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
JP6473133B2 (ja) 2013-03-15 2019-02-20 アラクセス ファーマ エルエルシー Krasg12cの共有結合性阻害剤
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
PL2981963T3 (pl) 2013-04-05 2017-06-30 Dolby Int Ab Urządzenie kompandujące i sposób redukcji szumu kwantyzacji stosujący zaawansowane rozszerzenie spektralne
WO2015035223A1 (en) 2013-09-09 2015-03-12 Peloton Therapeutics, Inc. Aryl ethers and uses thereof
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
AU2014331794C1 (en) 2013-10-10 2019-09-12 Araxes Pharma Llc Inhibitors of KRAS G12C
CN106029648A (zh) 2013-12-19 2016-10-12 拜耳制药股份公司 作为肾上腺素能受体α2C拮抗剂的取代的联哌啶基衍生物
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
WO2016029454A1 (en) 2014-08-29 2016-03-03 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US10011600B2 (en) 2014-09-25 2018-07-03 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
ES2826443T3 (es) 2014-09-25 2021-05-18 Araxes Pharma Llc Inhibidores de proteínas mutantes KRAS G12C
MX383691B (es) 2015-03-06 2025-03-14 Beyondspring Pharmaceuticals Inc Método de tratamiento de cáncer asociado con una mutación de ras.
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
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
MX388781B (es) 2015-07-22 2025-03-20 Araxes Pharma Llc Compuestos de quinazolina sustituido y su uso como inhibidores de proteínas kras, hras y/o nras mutantes g12c.
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
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 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
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
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
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
KR102398941B1 (ko) 2016-07-27 2022-05-17 패들락 테라퓨틱스, 인코포레이티드 Pad4의 공유결합성 억제제
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
WO2018119183A2 (en) 2016-12-22 2018-06-28 Amgen Inc. Kras g12c inhibitors and methods of using the same
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic 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
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
US20200385364A1 (en) 2017-01-26 2020-12-10 Araxes Pharma Llc Fused n-heterocyclic 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
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JOP20190186A1 (ar) 2017-02-02 2019-08-01 Astellas Pharma Inc مركب كينازولين
WO2018206539A1 (en) 2017-05-11 2018-11-15 Astrazeneca Ab Heteroaryl compounds that inhibit g12c mutant ras proteins
EA201992781A1 (ru) 2017-05-22 2020-04-01 Эмджен Инк. Ингибиторы g12c kras и способы их применения
US11639346B2 (en) 2017-05-25 2023-05-02 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS
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
CN107556289A (zh) 2017-06-22 2018-01-09 天津国际生物医药联合研究院 一种氯苯‑吡啶类化合物及其应用
MA50077A (fr) 2017-09-08 2020-07-15 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
MX2020003242A (es) 2017-09-22 2020-09-18 Jubilant Epipad LLC Compuestos heterociclicos como inhibidores de pad.
GB201715342D0 (en) 2017-09-22 2017-11-08 Univ Nottingham Compounds
AU2018352142B2 (en) 2017-10-18 2022-08-25 Jubilant Epipad LLC Imidazo-pyridine compounds as PAD inhibitors
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
WO2019099703A1 (en) 2017-11-16 2019-05-23 Sidecar Therapeutics, Inc. Apoptosis signal-regulating kinase 1 (ask 1) inhibitor compounds
WO2019110751A1 (en) 2017-12-08 2019-06-13 Astrazeneca Ab Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents
TW201942116A (zh) 2018-02-09 2019-11-01 美商輝瑞股份有限公司 作為抗癌劑之四氫喹唑啉衍生物
NZ766835A (en) 2018-03-02 2023-09-29 Otsuka Pharma Co Ltd Pharmaceutical compounds
CA3095233A1 (en) 2018-03-28 2019-10-03 Bayer Pharma Aktiengesellschaft 4-(3-amino-6-fluoro-1h-indazol-5-yl)-1,2,6-trimethyl-1,4-dihydropyridine-3,5-dic arbonitrile compounds for treating hyperproliferative disorders
WO2019213516A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
TW202012415A (zh) 2018-05-08 2020-04-01 瑞典商阿斯特捷利康公司 化學化合物
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
JP7174143B2 (ja) 2018-07-24 2022-11-17 大鵬薬品工業株式会社 Shp2活性を阻害するヘテロ二環性化合物
WO2020035031A1 (en) 2018-08-16 2020-02-20 Genentech, Inc. Fused ring compounds
EP3841100A1 (en) 2018-08-20 2021-06-30 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
TW202033518A (zh) 2018-10-15 2020-09-16 美商美國禮來大藥廠 Kras g12c 抑制劑
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
PT3735299T (pt) 2018-11-09 2024-11-25 Hoffmann La Roche Compostos de anéis fundidos
US11053226B2 (en) 2018-11-19 2021-07-06 Amgen Inc. KRAS G12C inhibitors and methods of using the same
AU2019388998A1 (en) 2018-11-29 2021-06-03 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3919483A4 (en) 2019-01-29 2022-02-09 Brightgene Bio-medical Technology Co., Ltd. HETEROCYCLIC BENZOPYRIDONE COMPOUND AND USE THEREOF
WO2020177629A1 (zh) 2019-03-01 2020-09-10 劲方医药科技(上海)有限公司 螺环取代的嘧啶并环类化合物,其制法与医药上的用途
ES3010507T3 (en) 2019-03-05 2025-04-03 Astrazeneca Ab Fused tricyclic compounds useful as anticancer agents
US20220251109A1 (en) 2019-04-28 2022-08-11 Genfleet Therapeutics (Shanghai) Inc. Oxaazaquinazoline-7(8h)-ketone compound, preparation method therefor and pharmaceutical application thereof
CN114096544B (zh) 2019-05-20 2025-08-12 加州理工学院 Kras g12c抑制剂及其用途
CN118359609A (zh) 2019-05-21 2024-07-19 益方生物科技(上海)股份有限公司 杂环化合物,其制备方法和用途
WO2020234103A1 (en) 2019-05-21 2020-11-26 Bayer Aktiengesellschaft Identification and use of kras inhibitors
WO2020238791A1 (zh) 2019-05-24 2020-12-03 江苏恒瑞医药股份有限公司 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
KR20220027879A (ko) 2019-05-29 2022-03-08 상하이 한서 바이오메디컬 컴퍼니 리미티드 질소 함유 헤테로사이클릭 유도체의 조절제, 이의 제조방법 및 용도
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
MX2021014961A (es) 2019-06-06 2022-01-24 Hutchison Medipharma Ltd Compuestos triciclicos y su uso.
EP3990448A4 (en) 2019-06-24 2023-08-02 Guangdong Newopp Biopharmaceuticals Co., Ltd. HETEROCYCLIC COMPOUNDS AS INHIBITORS OF KRAS G12C
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
CN110256421A (zh) 2019-06-26 2019-09-20 微境生物医药科技(上海)有限公司 Kras-g12c抑制剂
TW202115089A (zh) 2019-07-01 2021-04-16 大陸商江蘇恆瑞醫藥股份有限公司 喹唑啉酮類衍生物、其製備方法及其在醫藥上的應用
MX2022001421A (es) 2019-08-02 2022-06-08 Shanghai Jemincare Pharmaceuticals Co Ltd Compuesto tetracíclico, método de preparación y uso del mismo.
TWI752580B (zh) 2019-08-07 2022-01-11 大陸商北京加科思新藥研發有限公司 Kras突變蛋白抑制劑
WO2021027943A1 (zh) 2019-08-14 2021-02-18 正大天晴药业集团南京顺欣制药有限公司 哒嗪酮并嘧啶类衍生物及其医药用途
CN112390797A (zh) 2019-08-15 2021-02-23 微境生物医药科技(上海)有限公司 新型螺环类K-Ras G12C抑制剂
US20220363681A1 (en) 2019-08-16 2022-11-17 Genfleet Therapeutics (Shanghai) Inc. Oxo six-membered cyclopyrimidine compound, preparation method and medical use thereof
CN114269735B (zh) 2019-08-26 2024-02-23 南京创济生物医药有限公司 二氢或四氢喹唑啉类化合物及其中间体、制备方法和应用
CN112430234B (zh) 2019-08-26 2023-04-28 信达生物制药(苏州)有限公司 一种新型kras g12c蛋白抑制剂及其制备方法和用途
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2021043322A1 (zh) 2019-09-06 2021-03-11 正大天晴药业集团南京顺欣制药有限公司 氮杂环庚烷并嘧啶类衍生物及其医药用途
EP4031542B1 (en) 2019-09-18 2025-10-15 Merck Sharp & Dohme LLC Small molecule inhibitors of kras g12c mutant
CA3155066A1 (en) 2019-09-20 2021-03-25 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
US20210094919A1 (en) 2019-09-25 2021-04-01 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
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
EP4684786A3 (en) 2019-10-24 2026-04-08 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
JP7651464B2 (ja) 2019-10-28 2025-03-26 日本曹達株式会社 2,6-ジオキソ-3,6-ジヒドロピリミジン化合物並びに農園芸用殺菌剤、殺線虫剤、および医療用・動物用抗真菌剤
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
PT4053118T (pt) 2019-10-30 2024-12-05 Genfleet Therapeutics Shanghai Inc Composto cíclico fundido heterocíclico substituído, método de preparação deste e utilização farmacêutica deste
WO2021084765A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd 4-aminobut-2-enamide derivatives and salts thereof
WO2021085653A1 (en) 2019-10-31 2021-05-06 Taiho Pharmaceutical Co., Ltd. 4-aminobut-2-enamide derivatives and salts thereof
WO2021088458A1 (en) 2019-11-04 2021-05-14 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
WO2021093758A1 (zh) 2019-11-15 2021-05-20 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
CN112824410A (zh) 2019-11-21 2021-05-21 苏州泽璟生物制药股份有限公司 氮杂七元环类抑制剂及其制备方法和应用
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
US20230061083A1 (en) 2019-11-29 2023-03-02 Evopoint Biosciences Co., Ltd. Kras g12c inhibitor compound and use thereof
WO2021106231A1 (en) 2019-11-29 2021-06-03 Taiho Pharmaceutical Co., Ltd. A compound having inhibitory activity against kras g12d mutation
BR112022010254A2 (pt) 2019-12-02 2022-09-06 Shanghai Yingli Pharm Co Ltd Composto heterocíclico contendo oxigênio representado pela fórmula i, método para preparar o composto heterocíclico contendo oxigênio, composto, composição farmacêutica e uso composto heterocíclico contendo oxigênio
WO2021113595A1 (en) 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
ES2929700T3 (es) 2019-12-11 2022-12-01 Lilly Co Eli Inhibidores de KRas g12c
WO2021120045A1 (en) 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
CA3165238A1 (en) 2019-12-19 2021-06-24 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
WO2021121371A1 (zh) 2019-12-19 2021-06-24 贝达药业股份有限公司 Kras g12c抑制剂及其在医药上的应用
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
EP4076667A1 (en) 2019-12-20 2022-10-26 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN113045565A (zh) 2019-12-27 2021-06-29 微境生物医药科技(上海)有限公司 新型K-Ras G12C抑制剂
WO2021147965A1 (zh) 2020-01-21 2021-07-29 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
US20220370416A1 (en) 2020-04-06 2022-11-24 Arvinas Operations, Inc. Compounds and methods for targeted degradation of kras
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
CN116194456B (zh) 2020-04-30 2025-08-29 上海科州药物股份有限公司 作为kras抑制剂的杂环化合物的制备及其应用方法
EP4216951B1 (en) 2020-09-22 2026-04-01 Mirati Therapeutics, Inc. Kras g12d inhibitors
UY39526A (es) 2020-11-20 2022-06-30 Jacobio Pharmaceuticals Co Ltd Inhibidores de kras g12d
EP4247807A4 (en) 2020-11-23 2024-10-16 Merck Sharp & Dohme LLC 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT
US20240124478A1 (en) 2020-11-23 2024-04-18 Merck Sharp & Dohme Llc SPIROCYCLIC-SUBSTITUTED 6,7-DIHYDRO-PYRANO[2,3-d]PYRIMIDINE INHIBITORS OF KRAS G12C MUTANT
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
WO2022173870A1 (en) 2021-02-09 2022-08-18 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
AU2022224511A1 (en) 2021-02-16 2023-08-10 Lawrence Livermore National Security, Llc Compositions and methods for inhibition of ras
WO2022221739A1 (en) 2021-04-16 2022-10-20 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12d mutant
US20240262842A1 (en) 2021-04-27 2024-08-08 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12c mutant
EP4329750A4 (en) 2021-04-27 2025-06-18 Merck Sharp & Dohme LLC Small-molecule inhibitors of the KRAS G12C mutant
WO2022250170A1 (en) 2021-05-28 2022-12-01 Taiho Pharmaceutical Co., Ltd. Small molecule inhibitors of kras mutated proteins
US20240417408A1 (en) 2021-05-28 2024-12-19 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
WO2022256459A1 (en) 2021-06-01 2022-12-08 Quanta Therapeutics, Inc. Kras modulators and uses thereof
CN118019746A (zh) 2021-09-27 2024-05-10 北京加科思新药研发有限公司 多环稠环衍生物及其用途
JP2024543879A (ja) 2021-11-24 2024-11-26 メルク・シャープ・アンド・ドーム・エルエルシー Kras変異型タンパク質の小分子阻害剤
WO2023103523A1 (zh) 2021-12-09 2023-06-15 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
MA71388A (fr) 2022-07-05 2025-04-30 Pfizer Inc. Composés pyrido[4,3-d]pyrimidines
WO2024015262A1 (en) 2022-07-09 2024-01-18 Blossomhill Therapeutics, Inc. Fused ring kras inhibitors for treating disease
TW202416982A (zh) 2022-08-11 2024-05-01 英屬開曼群島商百濟神州有限公司 雜環化合物、其組成物及用其進行治療之方法
WO2024041573A1 (en) 2022-08-25 2024-02-29 Zai Lab (Shanghai) Co., Ltd. Fused multi-heterocyclic compounds as kras g12d modulators and uses thereof
WO2024044667A2 (en) 2022-08-26 2024-02-29 Merck Sharp & Dohme Llc Small molecule inhibitors of kras proteins
WO2024063578A1 (ko) 2022-09-23 2024-03-28 일동제약(주) 신규한 테트라헤테로사이클 화합물
JP2025535367A (ja) 2022-10-19 2025-10-24 ジェネンテック, インコーポレイテッド 6-アザ部分を含むオキサゼピン化合物およびその使用
EP4615847A1 (en) 2022-11-11 2025-09-17 Merck Sharp & Dohme LLC Small molecule inhibitors of kras proteins
KR20250120376A (ko) 2022-12-07 2025-08-08 자코바이오 파마슈티칼스 컴퍼니 리미티드 축합환 화합물 및 이의 응용
WO2024209339A1 (en) 2023-04-05 2024-10-10 Pfizer Inc. Pyrido[4,3-d]pyrimidine compounds
WO2024213979A1 (en) 2023-04-10 2024-10-17 Pfizer Inc. Pyrido[4,3-d]pyrimidine compounds
WO2024233776A1 (en) 2023-05-09 2024-11-14 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12d mutant
KR20260009841A (ko) 2023-05-12 2026-01-20 블로썸힐 테라퓨틱스, 인크. 질병 치료를 위한 융합 고리 kras 억제제

Also Published As

Publication number Publication date
CO2022006858A2 (es) 2022-06-10
WO2021086833A1 (en) 2021-05-06
KR20220106980A (ko) 2022-08-01
CR20220230A (es) 2022-06-15
PH12022551027A1 (en) 2023-05-29
WO2021086833A8 (en) 2022-07-14
JP7340100B2 (ja) 2023-09-06
ZA202205938B (en) 2024-02-28
BR112022007783A2 (pt) 2022-07-05
ECSP22033597A (es) 2022-05-31
US20240043448A1 (en) 2024-02-08
GEAP202415960A (en) 2024-08-12
US12291538B2 (en) 2025-05-06
US20210122764A1 (en) 2021-04-29
US20240083913A1 (en) 2024-03-14
JP7595127B2 (ja) 2024-12-05
JP2022553994A (ja) 2022-12-27
BR112022007783A8 (pt) 2023-04-11
MX2022005053A (es) 2022-05-18
US12297208B2 (en) 2025-05-13
TW202130645A (zh) 2021-08-16
EP4051678B1 (en) 2026-03-04
CA3158793A1 (en) 2021-05-06
DOP2022000090A (es) 2022-06-30
JOP20220101A1 (ar) 2023-01-30
PE20221253A1 (es) 2022-08-16
CN114867726A (zh) 2022-08-05
TWI911172B (zh) 2026-01-11
US11697657B2 (en) 2023-07-11
IL292438B2 (en) 2025-11-01
JP2023159395A (ja) 2023-10-31
CN114867726B (zh) 2023-11-28
IL292438B1 (en) 2025-07-01
AU2020372881A1 (en) 2022-06-09
GEP20247710B (en) 2024-12-25
EP4051678A1 (en) 2022-09-07
IL292438A (en) 2022-06-01

Similar Documents

Publication Publication Date Title
UA129778C2 (uk) Низькомолекулярні інгібітори g12c-мутантного kras
JP7754865B2 (ja) Tlr7/8アンタゴニストおよびそれらの使用
ES2944573T3 (es) Antagonistas de TLR7/8 y usos de los mismos
KR102653190B1 (ko) 고 활성 sting 단백질 작용제 화합물
EP3693375A1 (en) Compositions and methods for inhibiting arginase activity
UA127968C2 (uk) Інгібітори g12c kras і способи їх застосування
JP7495790B2 (ja) Mdm2-p53相互作用のイソインドリノン阻害剤およびそれを作製するためのプロセス
UA124474C2 (uk) БЕНЗІЗОТІАЗОЛЬНІ, ІЗОТІАЗОЛО[3,4-b]ПІРИДИНОВІ, ХІНАЗОЛІНОВІ, ФТАЛАЗИНОВІ, ПІРИДО[2,3-d]ПІРИДАЗИНОВІ Й ПІРИДО[2,3-d]ПІРИМІДИНОВІ ПОХІДНІ ЯК ІНГІБІТОРИ G12C KRAS ДЛЯ ЛІКУВАННЯ РАКУ ЛЕГЕНІ, РАКУ ПІДШЛУНКОВОЇ ЗАЛОЗИ АБО КОЛОРЕКТАЛЬНОГО РАКУ
BR112019020459A2 (pt) compostos que inibem a proteína mcl-1
RS65319B1 (sr) 8-cijano-5-piperidino-hinolini kao tlr7/8 antagonisti i njihova upotreba u lečenju imunoloških poremećaja
JP7365332B2 (ja) Cdk8/19阻害薬としての新規ヘテロ環式化合物
BR122023023308A2 (pt) Antagonistas tlr7/8, seus usos, composição farmacêutica, e kit
EP3826723B1 (en) Boronic acid derivatives
EP3929188A1 (en) Pd-l1 antagonist compound
CN116806220B (zh) 一种Wnt通路抑制剂化合物
EA047571B1 (ru) Низкомолекулярные ингибиторы g12c-мутантного kras
RU2833035C2 (ru) Антагонисты tlr7/8 и их применение
HK40058270A (en) Pd-l1 antagonist compound