CR20210624A - Inhibidor de egfr para el tratamiento de cáncer - Google Patents

Inhibidor de egfr para el tratamiento de cáncer

Info

Publication number
CR20210624A
CR20210624A CR20210624A CR20210624A CR20210624A CR 20210624 A CR20210624 A CR 20210624A CR 20210624 A CR20210624 A CR 20210624A CR 20210624 A CR20210624 A CR 20210624A CR 20210624 A CR20210624 A CR 20210624A
Authority
CR
Costa Rica
Prior art keywords
cancer
treatment
egfr inhibitor
ring
microcytic
Prior art date
Application number
CR20210624A
Other languages
English (en)
Inventor
Annick Goergler
Cosimo Dolente
Daniel Rueher
Georg Jaeschke
Sandra Steiner
Sander Christa Ulrike Obst
Antonio Ricci
David Hewings
Bernd Kuhn
Yvonne Alice Nagel
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CR20210624A publication Critical patent/CR20210624A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/485Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto de fórmula (I) que contiene un anillo tiazol, un anillo indazol y un sistema de anillo 6,7-dihidro-5H-pirrolo [1,2-c]imidazol, a las composiciones farmacéuticas que lo contienen y a su uso médico. Los compuestos se describen como inhibidores alostéricos selectivos de T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S que contienen mutantes de EGFR y, de este modo, son útiles para el tratamiento de cáncer, en particular, cáncer de pulmón no microcítico.
CR20210624A 2019-06-21 2020-06-19 Inhibidor de egfr para el tratamiento de cáncer CR20210624A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19181754 2019-06-21
PCT/EP2020/067076 WO2020254562A1 (en) 2019-06-21 2020-06-19 Egfr inhibitor for the treatment of cancer

Publications (1)

Publication Number Publication Date
CR20210624A true CR20210624A (es) 2022-02-14

Family

ID=67139601

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20210624A CR20210624A (es) 2019-06-21 2020-06-19 Inhibidor de egfr para el tratamiento de cáncer

Country Status (31)

Country Link
US (5) US12344613B2 (es)
EP (4) EP3986898B1 (es)
JP (4) JP7550799B2 (es)
KR (1) KR102913816B1 (es)
CN (4) CN114008049B (es)
AR (4) AR119210A1 (es)
AU (1) AU2020295703B2 (es)
BR (1) BR112021025445B1 (es)
CA (1) CA3140485A1 (es)
CL (1) CL2021003408A1 (es)
CO (1) CO2021017173A2 (es)
CR (1) CR20210624A (es)
DK (1) DK3986897T3 (es)
ES (1) ES2961187T3 (es)
FI (1) FI3986897T3 (es)
HR (1) HRP20231276T1 (es)
HU (1) HUE063676T2 (es)
IL (1) IL288522B2 (es)
LT (1) LT3986897T (es)
MA (1) MA56508B1 (es)
MX (1) MX2021015464A (es)
MY (1) MY209340A (es)
PE (1) PE20220576A1 (es)
PH (1) PH12021553190A1 (es)
PL (1) PL3986897T3 (es)
PT (1) PT3986897T (es)
RS (1) RS64720B1 (es)
SI (1) SI3986897T1 (es)
TW (4) TW202115053A (es)
UA (1) UA129328C2 (es)
WO (4) WO2020254562A1 (es)

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CN114008049B (zh) * 2019-06-21 2024-07-05 豪夫迈·罗氏有限公司 用于癌症治疗的egfr抑制剂
CN113993591A (zh) * 2019-06-21 2022-01-28 豪夫迈·罗氏有限公司 新egfr抑制剂
IL326879A (en) 2019-11-11 2026-04-01 Dana Farber Cancer Inst Inc EGFR allosteric inhibitors and methods of using them
CN116600806A (zh) * 2020-12-01 2023-08-15 豪夫迈·罗氏有限公司 新的吲唑衍生物
JP7840324B2 (ja) 2020-12-01 2026-04-03 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規インダゾール誘導体
JP2024521791A (ja) * 2021-05-26 2024-06-04 シーフォー セラピューティクス, インコーポレイテッド 脳又はcnsへの癌転移を治療するためのegfrデグレーダー
JP2025515833A (ja) * 2022-05-13 2025-05-20 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規インダゾール誘導体
JP2025516543A (ja) * 2022-05-13 2025-05-30 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のためのアロステリックおよびオルソステリックegfr阻害剤の組み合わせ
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
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

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CN101273033A (zh) * 2005-09-20 2008-09-24 阿斯利康(瑞典)有限公司 作为治疗癌症的erbb受体酪氨酸激酶抑制剂的4-(1h-吲哚-5-基-氨基)-喹唑啉化合物
ES2408932T3 (es) 2008-06-25 2013-06-24 Merck Sharp & Dohme Corp. Síntesis y uso de agentes antibacterianos heterocíclicos
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
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CN113993591A (zh) 2019-06-21 2022-01-28 豪夫迈·罗氏有限公司 新egfr抑制剂
JP7561777B2 (ja) * 2019-06-21 2024-10-04 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規egfr阻害剤
CN114008049B (zh) 2019-06-21 2024-07-05 豪夫迈·罗氏有限公司 用于癌症治疗的egfr抑制剂
AR120800A1 (es) 2019-12-20 2022-03-16 Hoffmann La Roche Derivados de 6,7-dihidro-5h-pirrolo[1,2-c]imidazol como inhibidores de egfr
AR120799A1 (es) 2019-12-20 2022-03-16 Hoffmann La Roche 2-[4-cloro-6-[2-[4-[[4-(hidroximetil)-1-piperidil]metil]fenil]etinil]-1-oxoisoindolin-2-il]-2-(6,7-dihidro-5h-pirrolo[1,2-c]imidazol-1-il)-n-tiazol-2-il-acetamida como inhibidor de egfr
JP7840324B2 (ja) 2020-12-01 2026-04-03 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規インダゾール誘導体
PE20240099A1 (es) 2020-12-01 2024-01-18 Hoffmann La Roche Nuevos derivados de indazol acetileno
CN116600806A (zh) 2020-12-01 2023-08-15 豪夫迈·罗氏有限公司 新的吲唑衍生物
JP2025516543A (ja) 2022-05-13 2025-05-30 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のためのアロステリックおよびオルソステリックegfr阻害剤の組み合わせ
JP2025515833A (ja) 2022-05-13 2025-05-20 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 新規インダゾール誘導体

Also Published As

Publication number Publication date
PE20220576A1 (es) 2022-04-20
US20230054473A1 (en) 2023-02-23
US20220315592A1 (en) 2022-10-06
KR102913816B1 (ko) 2026-01-16
TW202115074A (zh) 2021-04-16
HRP20231276T1 (hr) 2024-02-02
CO2021017173A2 (es) 2022-01-17
IL288522B2 (en) 2025-02-01
MA56508A (fr) 2022-04-27
ES2961187T3 (es) 2024-03-08
AR119208A1 (es) 2021-12-01
JP7550799B2 (ja) 2024-09-13
CN113993872B (zh) 2024-09-24
JP2022537191A (ja) 2022-08-24
CN113993872A (zh) 2022-01-28
CN113966335B (zh) 2024-08-02
CA3140485A1 (en) 2020-12-24
IL288522A (en) 2022-01-01
TW202115072A (zh) 2021-04-16
CN114008049B (zh) 2024-07-05
WO2020254565A1 (en) 2020-12-24
WO2020254572A1 (en) 2020-12-24
MY209340A (en) 2025-07-03
RS64720B1 (sr) 2023-11-30
EP3986895A1 (en) 2022-04-27
EP3986896B1 (en) 2023-03-15
SI3986897T1 (sl) 2023-12-29
EP3986896A1 (en) 2022-04-27
CL2021003408A1 (es) 2022-10-14
CN114008049A (zh) 2022-02-01
US20250289824A1 (en) 2025-09-18
AU2020295703B2 (en) 2026-02-12
JP7550800B2 (ja) 2024-09-13
JP7530391B2 (ja) 2024-08-07
WO2020254562A1 (en) 2020-12-24
CN113993873A (zh) 2022-01-28
DK3986897T3 (da) 2023-10-30
EP3986897A1 (en) 2022-04-27
EP3986898B1 (en) 2023-03-15
BR112021025445A2 (pt) 2022-02-01
MX2021015464A (es) 2022-01-24
WO2020254568A1 (en) 2020-12-24
LT3986897T (lt) 2023-11-10
IL288522B1 (en) 2024-10-01
JP2022538403A (ja) 2022-09-02
US20220315593A1 (en) 2022-10-06
FI3986897T3 (fi) 2023-10-20
EP3986898A1 (en) 2022-04-27
JP7550798B2 (ja) 2024-09-13
UA129328C2 (uk) 2025-03-19
HUE063676T2 (hu) 2024-01-28
AR119209A1 (es) 2021-12-01
CN113966335A (zh) 2022-01-21
TW202115053A (zh) 2021-04-16
TWI869416B (zh) 2025-01-11
KR20220024105A (ko) 2022-03-03
TW202115071A (zh) 2021-04-16
JP2022537769A (ja) 2022-08-29
MA56508B1 (fr) 2023-11-30
JP2022538055A (ja) 2022-08-31
PL3986897T3 (pl) 2024-01-22
AU2020295703A1 (en) 2022-01-06
AR119206A1 (es) 2021-12-01
PH12021553190A1 (en) 2022-11-07
EP3986897B1 (en) 2023-08-30
US12479849B2 (en) 2025-11-25
CN113993873B (zh) 2024-08-02
AR119210A1 (es) 2021-12-01
BR112021025445B1 (pt) 2024-02-27
PT3986897T (pt) 2023-10-23
EP3986895B1 (en) 2023-03-15
US12344613B2 (en) 2025-07-01
US20220135571A1 (en) 2022-05-05

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