AR120697A1 - Inhibidores de braf como rompedores de la paradoja - Google Patents

Inhibidores de braf como rompedores de la paradoja

Info

Publication number
AR120697A1
AR120697A1 ARP200103415A ARP200103415A AR120697A1 AR 120697 A1 AR120697 A1 AR 120697A1 AR P200103415 A ARP200103415 A AR P200103415A AR P200103415 A ARP200103415 A AR P200103415A AR 120697 A1 AR120697 A1 AR 120697A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
cyano
halogen
braf inhibitors
Prior art date
Application number
ARP200103415A
Other languages
English (en)
Inventor
Cosimo Dolente
David Hewings
Daniel Hunziker
Daniela Krummenacher
Piergiorgio 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 AR120697A1 publication Critical patent/AR120697A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/90Oxygen atoms with acyclic radicals attached in position 2 or 3
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Glass Compositions (AREA)
  • Luminescent Compositions (AREA)

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) en donde R¹ es C₁₋₆-alquilo; X se selecciona de i) -NH- y ii) -O-; R² se selecciona de iii) H, iv) ciano y v) halógeno; R³ se selecciona de vi) NR⁴R⁵ y vii) CHR⁶R⁷; R⁴ se selecciona de viii) C₁₋₆-alquilo, ix) C₃₋₈-cicloalquilo y x) C₃₋₈-cicloalquil-C₁₋₆-alquilo; R⁵ se selecciona de xi) C₁₋₆-alquilo, xii) C₃₋₈-cicloalquilo y xiii) C₃₋₈-cicloalquil-C₁₋₆-alquilo; o R⁴ y R⁵, junto con el átomo de nitrógeno al que están unidos, forman un heterocicloalquilo opcionalmente sustituido con R⁸, en donde el heterocicloalquilo se selecciona de pirrolidinilo y piperidinilo; R⁶ se selecciona de xiv) C₁₋₆-alquilo, xv) C₃₋₈-cicloalquilo y xvi) C₃₋₈-cicloalquil-C₁₋₆-alquilo; R⁷ se selecciona de xvii) C₁₋₆-alquilo, xviii) C₃₋₈-cicloalquilo y xix) C₃₋₈-cicloalquil-C₁₋₆-alquilo; o R⁶ y R⁷, junto con el átomo de carbono al que están unidos, forman un C₃₋₈-cicloalquilo opcionalmente sustituido con R⁸; R⁸ es halógeno; siempre que N-[2-ciano-4-fluoro-3-(3-metil-4-oxo-quinazolin-6-il)oxi-fenil]-3-fluoropirrolidin-1-sulfonamida se excluya, o una sal de aquel aceptable desde el punto de vista farmacéutico.
ARP200103415A 2019-12-10 2020-12-09 Inhibidores de braf como rompedores de la paradoja AR120697A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP19214867 2019-12-10

Publications (1)

Publication Number Publication Date
AR120697A1 true AR120697A1 (es) 2022-03-09

Family

ID=68848068

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP200103415A AR120697A1 (es) 2019-12-10 2020-12-09 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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20220251A (es) * 2019-12-10 2022-07-11 Hoffmann La Roche Nuevos derivados de metilquinazolinona
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
WO2024126634A1 (en) 2022-12-15 2024-06-20 F. Hoffmann-La Roche Ag Process for the preparation of a quinazolinone derivative
WO2024126660A1 (en) 2022-12-15 2024-06-20 F. Hoffmann-La Roche Ag Combination therapy for cancer treatment

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2972138A1 (en) * 2008-03-17 2009-09-24 Ambit Biosciences Corporation Raf kinase modulator compounds and methods of use thereof
WO2012118492A1 (en) * 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
CN104640865B (zh) * 2012-09-19 2018-05-11 诺华股份有限公司 作为激酶抑制剂的二氢吡咯烷子基-嘧啶
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
PE20231651A1 (es) * 2020-06-09 2023-10-17 Array Biopharma Inc Compuestos para el tratamiento de enfermedades y trastornos asociados a braf

Also Published As

Publication number Publication date
PE20221027A1 (es) 2022-06-16
KR20220112777A (ko) 2022-08-11
CN114746405B (zh) 2024-03-26
AU2020403082A1 (en) 2022-05-12
EP4073044A1 (en) 2022-10-19
CL2022001492A1 (es) 2023-02-24
MX2022006711A (es) 2022-07-12
TW202136218A (zh) 2021-10-01
CA3158541A1 (en) 2021-06-17
BR112022010633A2 (pt) 2022-08-16
US20220298145A1 (en) 2022-09-22
IL292349A (en) 2022-06-01
CO2022007621A2 (es) 2022-08-30
CR20220252A (es) 2022-07-11
JP2023505300A (ja) 2023-02-08
CN114746405A (zh) 2022-07-12
WO2021116050A1 (en) 2021-06-17
ZA202204092B (en) 2022-12-21

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