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
formula
ring
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

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

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 (28)

Country Link
US (4) US20220315592A1 (es)
EP (4) EP3986895B1 (es)
JP (4) JP2022537191A (es)
KR (1) KR20220024105A (es)
CN (4) CN113993873A (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) IL288522A (es)
LT (1) LT3986897T (es)
MA (1) MA56508B1 (es)
MX (1) MX2021015464A (es)
PE (1) PE20220576A1 (es)
PL (1) PL3986897T3 (es)
PT (1) PT3986897T (es)
RS (1) RS64720B1 (es)
SI (1) SI3986897T1 (es)
TW (4) TW202115072A (es)
WO (4) WO2020254568A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023217924A1 (en) * 2022-05-13 2023-11-16 F. Hoffmann-La Roche Ag Combination of allosteric and orthosteric egfr inhibitors for the treatment of cancer
WO2023217923A1 (en) * 2022-05-13 2023-11-16 F. Hoffmann-La Roche Ag New indazole derivatives

Family Cites Families (12)

* 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
US20110212078A1 (en) 2008-06-25 2011-09-01 Reddy Panduranga Adulla P Synthesis and use of heterocyclic antibacterial agents
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
WO2015095807A1 (en) * 2013-12-20 2015-06-25 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of egfr and erk inhibitors
WO2016000615A1 (en) * 2014-07-02 2016-01-07 Sunshine Lake Pharma Co., Ltd. Heteroaryl compounds and pharmaceutical applications thereof
JP6639497B2 (ja) * 2014-11-10 2020-02-05 ジェネンテック， インコーポレイテッド ブロモドメインインヒビターおよびその使用
CN107848964B (zh) 2015-05-14 2021-03-19 威斯塔解剖学和生物学研究所 Ebna1抑制剂和使用其的方法
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
WO2019046668A1 (en) * 2017-08-31 2019-03-07 Kezar Life Sciences AMIDE-SUBSTITUTED THIAZOLES AS INHIBITORS OF SECRETIC PROTEIN
KR20210025535A (ko) * 2018-06-29 2021-03-09 에프. 호프만-라 로슈 아게 화합물

Also Published As

Publication number Publication date
EP3986897A1 (en) 2022-04-27
MA56508A (fr) 2022-04-27
FI3986897T3 (fi) 2023-10-20
TW202115053A (zh) 2021-04-16
HRP20231276T1 (hr) 2024-02-02
EP3986898B1 (en) 2023-03-15
PE20220576A1 (es) 2022-04-20
TW202115074A (zh) 2021-04-16
WO2020254565A1 (en) 2020-12-24
JP2022537769A (ja) 2022-08-29
LT3986897T (lt) 2023-11-10
WO2020254562A1 (en) 2020-12-24
EP3986898A1 (en) 2022-04-27
AU2020295703A1 (en) 2022-01-06
CN113993872A (zh) 2022-01-28
TW202115072A (zh) 2021-04-16
TW202115071A (zh) 2021-04-16
US20220315593A1 (en) 2022-10-06
JP2022537191A (ja) 2022-08-24
CN113993873A (zh) 2022-01-28
US20220135571A1 (en) 2022-05-05
AR119210A1 (es) 2021-12-01
CO2021017173A2 (es) 2022-01-17
PT3986897T (pt) 2023-10-23
SI3986897T1 (sl) 2023-12-29
KR20220024105A (ko) 2022-03-03
CN113966335A (zh) 2022-01-21
RS64720B1 (sr) 2023-11-30
CA3140485A1 (en) 2020-12-24
AR119209A1 (es) 2021-12-01
WO2020254568A1 (en) 2020-12-24
ES2961187T3 (es) 2024-03-08
US20220315592A1 (en) 2022-10-06
WO2020254572A1 (en) 2020-12-24
CN114008049A (zh) 2022-02-01
JP2022538055A (ja) 2022-08-31
MA56508B1 (fr) 2023-11-30
BR112021025445A2 (pt) 2022-02-01
JP2022538403A (ja) 2022-09-02
MX2021015464A (es) 2022-01-24
AR119208A1 (es) 2021-12-01
DK3986897T3 (da) 2023-10-30
EP3986895A1 (en) 2022-04-27
EP3986897B1 (en) 2023-08-30
BR112021025445B1 (pt) 2024-02-27
IL288522A (en) 2022-01-01
PL3986897T3 (pl) 2024-01-22
EP3986895B1 (en) 2023-03-15
HUE063676T2 (hu) 2024-01-28
CL2021003408A1 (es) 2022-10-14
AR119206A1 (es) 2021-12-01
EP3986896B1 (en) 2023-03-15
US20230054473A1 (en) 2023-02-23
EP3986896A1 (en) 2022-04-27

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