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AR119206A1 - DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR - Google Patents

DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR

Info

Publication number
AR119206A1
AR119206A1 ARP200101745A ARP200101745A AR119206A1 AR 119206 A1 AR119206 A1 AR 119206A1 AR P200101745 A ARP200101745 A AR P200101745A AR P200101745 A ARP200101745 A AR P200101745A AR 119206 A1 AR119206 A1 AR 119206A1
Authority
AR
Argentina
Prior art keywords
pyrrolo
imidazole derivatives
egfr inhibitors
egfr
pyrazole
Prior art date
Application number
ARP200101745A
Other languages
English (en)
Inventor
Annick Goergler
Cosimo Dolente
David Stephen Hewings
Georg Jaeschke
Bernd Kuhn
Yvonne Alice Nagel
Christa Ulrike Obst-Sander
Antonio Ricci
Daniel Rueher
Sandra Steiner
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 AR119206A1 publication Critical patent/AR119206A1/es

Links

Classifications

    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • C07D519/00—Heterocyclic 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

Compuestos derivados de 5H-pirrolo[1,2-c]pirazol como inhibidores allostéricos de EGFR, composiciones farmacéuticas que los comprenden y el uso de los mismos para el tratamiento de cáncer de pulmón microcítico. Reivindicación 1: Un compuesto de fórmula (1) o sales farmacéuticamente aceptables.
ARP200101745A 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR AR119206A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP19181754 2019-06-21

Publications (1)

Publication Number Publication Date
AR119206A1 true AR119206A1 (es) 2021-12-01

Family

ID=67139601

Family Applications (4)

Application Number Title Priority Date Filing Date
ARP200101749A AR119210A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR
ARP200101745A AR119206A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR
ARP200101747A AR119208A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR
ARP200101748A AR119209A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP200101749A AR119210A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP200101747A AR119208A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR
ARP200101748A AR119209A1 (es) 2019-06-21 2020-06-19 DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR

Country Status (30)

Country Link
US (5) US12344613B2 (es)
EP (4) EP3986898B1 (es)
JP (4) JP7550800B2 (es)
CN (4) CN113993873B (es)
AR (4) AR119210A1 (es)
AU (1) AU2020295703A1 (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) TW202115074A (es)
UA (1) UA129328C2 (es)
WO (4) WO2020254565A1 (es)

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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 (en) * 2022-05-13 2023-11-16 F. Hoffmann-La Roche Ag New indazole derivatives
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 (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
WO2025255438A1 (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
WO2026015801A1 (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
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

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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
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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 (en) 2019-06-21 2023-08-30 F. Hoffmann-La Roche AG New egfr inhibitors
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 (en) 2022-05-13 2023-11-16 F. Hoffmann-La Roche Ag New indazole derivatives

Also Published As

Publication number Publication date
JP7550798B2 (ja) 2024-09-13
ES2961187T3 (es) 2024-03-08
MA56508B1 (fr) 2023-11-30
EP3986895B1 (en) 2023-03-15
EP3986895A1 (en) 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 (en) 2022-04-27
EP3986897A1 (en) 2022-04-27
KR20220024105A (ko) 2022-03-03
US20220315592A1 (en) 2022-10-06
AR119208A1 (es) 2021-12-01
TW202115071A (zh) 2021-04-16
EP3986896A1 (en) 2022-04-27
WO2020254565A1 (en) 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 (en) 2023-03-15
JP2022537769A (ja) 2022-08-29
US20220315593A1 (en) 2022-10-06
JP2022538403A (ja) 2022-09-02
CN114008049A (zh) 2022-02-01
IL288522B2 (en) 2025-02-01
WO2020254562A1 (en) 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 (en) 2023-03-15
WO2020254572A1 (en) 2020-12-24
CN113993873A (zh) 2022-01-28
SI3986897T1 (sl) 2023-12-29
CN113993872B (zh) 2024-09-24
CA3140485A1 (en) 2020-12-24
PT3986897T (pt) 2023-10-23
TW202115074A (zh) 2021-04-16
EP3986897B1 (en) 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 (en) 2020-12-24
TW202115072A (zh) 2021-04-16

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