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MA56508B1 - Inhibiteur de l'egfr pour le traitement du cancer - Google Patents

Inhibiteur de l'egfr pour le traitement du cancer

Info

Publication number
MA56508B1
MA56508B1 MA56508A MA56508A MA56508B1 MA 56508 B1 MA56508 B1 MA 56508B1 MA 56508 A MA56508 A MA 56508A MA 56508 A MA56508 A MA 56508A MA 56508 B1 MA56508 B1 MA 56508B1
Authority
MA
Morocco
Prior art keywords
cancer treatment
egfr inhibitor
formula
cancer
ring
Prior art date
Application number
MA56508A
Other languages
English (en)
Other versions
MA56508A (fr
Inventor
Bernd Kuhn
Daniel Rueher
Georg Jaeschke
Antonio Ricci
Cosimo Dolente
Sander Ulrike Obst
Sandra Steiner
Annick Goergler
David Hewings
Yvonne 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 MA56508A publication Critical patent/MA56508A/fr
Publication of MA56508B1 publication Critical patent/MA56508B1/fr

Links

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

L'invention concerne un composé de formule (i) contenant un cycle thiazole, un cycle indazole et un système cyclique 6,7-dihydro-5h-pyrrolo[l,2- c]imidazole, des compositions pharmaceutiques le contenant et son utilisation médicale. Les composés sont décrits en tant qu'inhibiteurs allostériques sélectifs de t790m/l858r, t790m/l858r/c797s, l858r, l858r/c797s contenant des mutants egfr et sont donc utiles pour le traitement du cancer, en particulier du cancer du poumon non à petites cellules. (formule i)
MA56508A 2019-06-21 2020-06-19 Inhibiteur de l'egfr pour le traitement du cancer MA56508B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19181754 2019-06-21
PCT/EP2020/067076 WO2020254562A1 (fr) 2019-06-21 2020-06-19 Inhibiteur d'egfr pour le traitement du cancer

Publications (2)

Publication Number Publication Date
MA56508A MA56508A (fr) 2022-04-27
MA56508B1 true MA56508B1 (fr) 2023-11-30

Family

ID=67139601

Family Applications (1)

Application Number Title Priority Date Filing Date
MA56508A MA56508B1 (fr) 2019-06-21 2020-06-19 Inhibiteur de l'egfr pour le traitement du cancer

Country Status (30)

Country Link
US (5) US12344613B2 (fr)
EP (4) EP3986898B1 (fr)
JP (4) JP7550800B2 (fr)
CN (4) CN113993873B (fr)
AR (4) AR119210A1 (fr)
AU (1) AU2020295703A1 (fr)
BR (1) BR112021025445B1 (fr)
CA (1) CA3140485A1 (fr)
CL (1) CL2021003408A1 (fr)
CO (1) CO2021017173A2 (fr)
CR (1) CR20210624A (fr)
DK (1) DK3986897T3 (fr)
ES (1) ES2961187T3 (fr)
FI (1) FI3986897T3 (fr)
HR (1) HRP20231276T1 (fr)
HU (1) HUE063676T2 (fr)
IL (1) IL288522B2 (fr)
LT (1) LT3986897T (fr)
MA (1) MA56508B1 (fr)
MX (1) MX2021015464A (fr)
MY (1) MY209340A (fr)
PE (1) PE20220576A1 (fr)
PH (1) PH12021553190A1 (fr)
PL (1) PL3986897T3 (fr)
PT (1) PT3986897T (fr)
RS (1) RS64720B1 (fr)
SI (1) SI3986897T1 (fr)
TW (4) TW202115074A (fr)
UA (1) UA129328C2 (fr)
WO (4) WO2020254565A1 (fr)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113993873B (zh) * 2019-06-21 2024-08-02 豪夫迈·罗氏有限公司 用于治疗癌症的egfr抑制剂
TW202115070A (zh) * 2019-06-21 2021-04-16 瑞士商赫孚孟拉羅股份公司 新穎的egfr抑制劑
JOP20220107A1 (ar) 2019-11-11 2023-01-30 Dana Farber Cancer Inst Inc مثبطات egfr تفارغية وطرق استخدامها
US20240059692A1 (en) * 2020-12-01 2024-02-22 Hoffmann-La Roche Inc. New indazole derivatives
JP7798887B2 (ja) * 2020-12-01 2026-01-14 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
TW202313025A (zh) * 2021-05-26 2023-04-01 美商C4醫藥公司 治療腦或cns癌症轉移之egfr降解藥物
CN119173253A (zh) * 2022-05-13 2024-12-20 豪夫迈·罗氏有限公司 用于治疗癌症的变构和正构egfr抑制剂的组合产品
WO2023217923A1 (fr) * 2022-05-13 2023-11-16 F. Hoffmann-La Roche Ag Nouveaux dérivés d'indazole
CR20250458A (es) 2023-03-30 2025-11-21 Revolution Medicines Inc Composiciones para inducir la hidrólisis de ras gtp y sus usos
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (fr) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Inhibiteurs de ras
WO2025240847A1 (fr) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Inhibiteurs de ras
WO2025255438A1 (fr) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Procédés de traitement d'une maladie ou d'un trouble lié à la protéine ras
WO2025265060A1 (fr) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Compositions thérapeutiques et procédés de gestion d'effets liés au traitement
WO2026006747A1 (fr) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Inhibiteurs de ras
WO2026015801A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble liés à ras
WO2026015790A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble lié à ras
WO2026015825A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Utilisation d'un inhibiteur de ras pour traiter le cancer du pancréas
WO2026015796A1 (fr) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Méthodes de traitement d'une maladie ou d'un trouble lié à ras

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0508715D0 (en) * 2005-04-29 2005-06-08 Astrazeneca Ab Chemical compounds
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
EP2307365B1 (fr) 2008-06-25 2013-03-27 Merck Sharp & Dohme Corp. Synthèse et utilisation d agents antibactériens hétérocycliques
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
DK2964638T3 (en) 2013-03-06 2017-10-30 Astrazeneca Ab QUINAZOLIN INHIBITORS TO ACTIVATE MUTANEOUS FORMS OF EPIDERMAL GROWTH FACTOR RECEPTOR
WO2015095807A1 (fr) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Traitements du cancer au moyen de combinaisons d'inhibiteurs de l'egfr et de l'erk
WO2016000615A1 (fr) * 2014-07-02 2016-01-07 Sunshine Lake Pharma Co., Ltd. Composés hétéroaryles et leurs applications pharmaceutiques
WO2016077375A1 (fr) * 2014-11-10 2016-05-19 Genentech, Inc. Inhibiteurs de bromodomaines et leurs utilisations
BR112017024481B1 (pt) 2015-05-14 2020-11-17 The Wistar Institute Of Anatomy And Biology composto inibidor de ebna1, composição farmacêutica compreendendo dito composto e usos terapêuticos do mesmo
EP3317273B1 (fr) 2015-06-30 2021-12-29 Dana-Farber Cancer Institute, Inc. Inhibiteurs d'egfr et méthodes d'utilisation de ceux-ci
TW201834651A (zh) 2016-12-22 2018-10-01 瑞士商赫孚孟拉羅股份公司 化合物
AR113299A1 (es) * 2017-06-02 2020-04-08 Hoffmann La Roche Compuestos de isoindolina
CN110753691B (zh) 2017-06-02 2024-02-02 豪夫迈·罗氏有限公司 用于治疗性和/或预防性治疗癌症的化合物
WO2019046668A1 (fr) * 2017-08-31 2019-03-07 Kezar Life Sciences Thiazoles à substitution amide utilisés en tant qu'inhibiteurs de la sécrétine protéique
MA53003A (fr) 2018-06-29 2021-05-05 Hoffmann La Roche Composés
TW202115070A (zh) 2019-06-21 2021-04-16 瑞士商赫孚孟拉羅股份公司 新穎的egfr抑制劑
CN113993873B (zh) 2019-06-21 2024-08-02 豪夫迈·罗氏有限公司 用于治疗癌症的egfr抑制剂
EP3986565B1 (fr) 2019-06-21 2023-08-30 F. Hoffmann-La Roche AG Nouveaux inhibiteurs de l'egfr
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
JP7798887B2 (ja) 2020-12-01 2026-01-14 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
CR20230218A (es) 2020-12-01 2023-07-07 Hoffmann La Roche Nuevos derivados de indazol acetileno
US20240059692A1 (en) 2020-12-01 2024-02-22 Hoffmann-La Roche Inc. New indazole derivatives
CN119173253A (zh) 2022-05-13 2024-12-20 豪夫迈·罗氏有限公司 用于治疗癌症的变构和正构egfr抑制剂的组合产品
WO2023217923A1 (fr) 2022-05-13 2023-11-16 F. Hoffmann-La Roche Ag Nouveaux dérivés d'indazole

Also Published As

Publication number Publication date
JP7550798B2 (ja) 2024-09-13
ES2961187T3 (es) 2024-03-08
EP3986895B1 (fr) 2023-03-15
EP3986895A1 (fr) 2022-04-27
US20230054473A1 (en) 2023-02-23
AR119210A1 (es) 2021-12-01
CO2021017173A2 (es) 2022-01-17
JP2022538055A (ja) 2022-08-31
PH12021553190A1 (en) 2022-11-07
EP3986898A1 (fr) 2022-04-27
EP3986897A1 (fr) 2022-04-27
KR20220024105A (ko) 2022-03-03
US20220315592A1 (en) 2022-10-06
AR119208A1 (es) 2021-12-01
TW202115071A (zh) 2021-04-16
EP3986896A1 (fr) 2022-04-27
WO2020254565A1 (fr) 2020-12-24
TW202115053A (zh) 2021-04-16
TWI869416B (zh) 2025-01-11
IL288522B1 (en) 2024-10-01
DK3986897T3 (da) 2023-10-30
CL2021003408A1 (es) 2022-10-14
PE20220576A1 (es) 2022-04-20
CN113993873B (zh) 2024-08-02
RS64720B1 (sr) 2023-11-30
IL288522A (en) 2022-01-01
CN113966335A (zh) 2022-01-21
CN114008049B (zh) 2024-07-05
JP7550800B2 (ja) 2024-09-13
BR112021025445A2 (pt) 2022-02-01
CN113966335B (zh) 2024-08-02
FI3986897T3 (fi) 2023-10-20
JP7530391B2 (ja) 2024-08-07
HRP20231276T1 (hr) 2024-02-02
EP3986898B1 (fr) 2023-03-15
JP2022537769A (ja) 2022-08-29
US20220315593A1 (en) 2022-10-06
JP2022538403A (ja) 2022-09-02
CN114008049A (zh) 2022-02-01
AR119206A1 (es) 2021-12-01
IL288522B2 (en) 2025-02-01
WO2020254562A1 (fr) 2020-12-24
JP2022537191A (ja) 2022-08-24
CR20210624A (es) 2022-02-14
LT3986897T (lt) 2023-11-10
AU2020295703A1 (en) 2022-01-06
AR119209A1 (es) 2021-12-01
HUE063676T2 (hu) 2024-01-28
BR112021025445B1 (pt) 2024-02-27
EP3986896B1 (fr) 2023-03-15
WO2020254572A1 (fr) 2020-12-24
CN113993873A (zh) 2022-01-28
SI3986897T1 (sl) 2023-12-29
CN113993872B (zh) 2024-09-24
CA3140485A1 (fr) 2020-12-24
PT3986897T (pt) 2023-10-23
TW202115074A (zh) 2021-04-16
EP3986897B1 (fr) 2023-08-30
US12479849B2 (en) 2025-11-25
MX2021015464A (es) 2022-01-24
JP7550799B2 (ja) 2024-09-13
US20250289824A1 (en) 2025-09-18
MY209340A (en) 2025-07-03
CN113993872A (zh) 2022-01-28
US12344613B2 (en) 2025-07-01
MA56508A (fr) 2022-04-27
US20220135571A1 (en) 2022-05-05
UA129328C2 (uk) 2025-03-19
PL3986897T3 (pl) 2024-01-22
WO2020254568A1 (fr) 2020-12-24
TW202115072A (zh) 2021-04-16

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