PE20221027A1 - Nuevos inhibidores de braf como rompedores de la paradoja - Google Patents

Nuevos inhibidores de braf como rompedores de la paradoja

Info

Publication number
PE20221027A1
PE20221027A1 PE2022000850A PE2022000850A PE20221027A1 PE 20221027 A1 PE20221027 A1 PE 20221027A1 PE 2022000850 A PE2022000850 A PE 2022000850A PE 2022000850 A PE2022000850 A PE 2022000850A PE 20221027 A1 PE20221027 A1 PE 20221027A1
Authority
PE
Peru
Prior art keywords
alkyl
paradox
cycloalkyl
optionally substituted
compound
Prior art date
Application number
PE2022000850A
Other languages
English (en)
Inventor
Cosimo Dolente
David Stephen Hewings
Daniel Hunziker
Daniela Krummenacher
Piergiorgio Francesco Tommaso Pettazzoni
Juergen Wichmann
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 PE20221027A1 publication Critical patent/PE20221027A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

La presente invencion se refiere a un compuesto de formula (I) o una sal farmaceuticamente aceptable, donde: R1 es alquil C1-6; X es NH u O; R2 es H, ciano y halogeno; R3 es NR4R5 y CHR6R7; R4, R5, R6 y R7 son alquil C1-6, cicloalquilo C3-8 o cicloalquilC3-8-alquilC1-6, o R4 y R5 juntos con el atomo de nitrogeno al que estan unidos forman un heterocicloalquilo opcionalmente sustituido, o R6 y R7 juntos con el atomo de carbono al que estan unidos forman un cicloalquiloC3-8 opcionalmente sustituido. Tambien se refiere a una composicion farmaceutica. Dicho compuesto es un inhibidor de BRAF rompedor de la paradoja, que es uno de los tres miembros de la clase fibrosarcoma de rapida aceleracion de serina-treonina quinasas (RAF), siendo util en el tratamiento del cancer.
PE2022000850A 2019-12-10 2020-12-08 Nuevos inhibidores de braf como rompedores de la paradoja PE20221027A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19214867 2019-12-10
PCT/EP2020/084969 WO2021116050A1 (en) 2019-12-10 2020-12-08 New braf inhibitors as paradox breakers

Publications (1)

Publication Number Publication Date
PE20221027A1 true PE20221027A1 (es) 2022-06-16

Family

ID=68848068

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000850A PE20221027A1 (es) 2019-12-10 2020-12-08 Nuevos inhibidores de braf como rompedores de la paradoja

Country Status (18)

Country Link
US (1) US20220298145A1 (es)
EP (1) EP4073044A1 (es)
JP (1) JP2023505300A (es)
KR (1) KR20220112777A (es)
CN (1) CN114746405B (es)
AR (1) AR120697A1 (es)
AU (1) AU2020403082A1 (es)
BR (1) BR112022010633A2 (es)
CA (1) CA3158541A1 (es)
CL (1) CL2022001492A1 (es)
CO (1) CO2022007621A2 (es)
CR (1) CR20220252A (es)
IL (1) IL292349A (es)
MX (1) MX2022006711A (es)
PE (1) PE20221027A1 (es)
TW (1) TW202136218A (es)
WO (1) WO2021116050A1 (es)
ZA (1) ZA202204092B (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010010172A (es) * 2008-03-17 2010-11-25 Ambit Biosciences Corp Derivados de quinazolina como moduladores de quinasa raf y metodos de uso de los mismos.
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
US9546173B2 (en) * 2012-09-19 2017-01-17 Novartis Ag Substituted pyrrolo[3,4-d]pyrimidines as kinase inhibitors
TWI817018B (zh) * 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療ｂｒａｆ相關的疾病和失調症之化合物
IL298300A (en) * 2020-06-09 2023-01-01 Array Biopharma Inc 4-oxo-3,4-dihydroquinazolinone compounds for the treatment of braf-related diseases and disorders

Also Published As

Publication number Publication date
KR20220112777A (ko) 2022-08-11
TW202136218A (zh) 2021-10-01
EP4073044A1 (en) 2022-10-19
CL2022001492A1 (es) 2023-02-24
CN114746405A (zh) 2022-07-12
IL292349A (en) 2022-06-01
CR20220252A (es) 2022-07-11
US20220298145A1 (en) 2022-09-22
BR112022010633A2 (pt) 2022-08-16
AR120697A1 (es) 2022-03-09
ZA202204092B (en) 2022-12-21
CA3158541A1 (en) 2021-06-17
AU2020403082A1 (en) 2022-05-12
CN114746405B (zh) 2024-03-26
JP2023505300A (ja) 2023-02-08
CO2022007621A2 (es) 2022-08-30
MX2022006711A (es) 2022-07-12
WO2021116050A1 (en) 2021-06-17

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