AR117194A1 - Compuestos de anillos fusionados - Google Patents

Compuestos de anillos fusionados

Info

Publication number
AR117194A1
AR117194A1 ARP190103302A ARP190103302A AR117194A1 AR 117194 A1 AR117194 A1 AR 117194A1 AR P190103302 A ARP190103302 A AR P190103302A AR P190103302 A ARP190103302 A AR P190103302A AR 117194 A1 AR117194 A1 AR 117194A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
alkoxy
haloalkyl
halo
Prior art date
Application number
ARP190103302A
Other languages
English (en)
Inventor
Jack Terrett
Steven Do
Jianfeng Xin
Sushant Malhotra
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 AR117194A1 publication Critical patent/AR117194A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este; caracterizado porque R¹ es un resto electrofílico capaz de formar un enlace covalente con un residuo de cisteína en la posición 12 de una proteína mutante K-Ras G12C; R² se selecciona del grupo que consiste en H, OH, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, ciclopropilo y -NHR, donde R se selecciona del grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₆, alcanoilo C₁₋₆, hidroxialcanoilo C₁₋₆, cianoalquilo C₁₋₆, alquilamino C₁₋₆, -(alquilenilo C₁₋₆)NH(CH₃)-(alquilenilo C₁₋₆)N(CH₃)₂ y -(alquilenilo C₁₋₃)(heterociclilo de 3 - 7 miembros); R³ y R⁴ se seleccionan cada uno independientemente del grupo que consiste en H, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquilamino C₁₋₆ y ciclopropilo; R⁵ se selecciona del grupo que consiste en H, NH₂, halo, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquilamino C₁₋₆ y cicloalquilo C₃₋₇, en donde al menos uno de R², R³, R⁴ y R⁵ es diferente de H; o R² y R³, R³ y R⁴, o R⁴ y R⁵, junto con los átomos a los cuales están unidos, forman un cicloalquilo C₃₋₇, heterocicloalquilo de 3 a 7 miembros, arilo C₆₋₁₄ o heteroarilo de 5 a 10 miembros; cada uno de los cuales está opcionalmente sustituido con 1 a 4 sustituyentes, en donde cada sustituyente se selecciona independientemente del grupo que consiste en OH, NH₂, halo, alquilo C₁₋₃, haloalquilo C₁₋₃, alcoxi C₁₋₃ y haloalcoxi C₁₋₃; X se selecciona del grupo que consiste en NH₂, alcoxi C₁₋₆, alquilo C₁₋₆, alquilamino C₁₋₆, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, cicloalquilo C₃₋₇, heterociclilo de 4 a 7 miembros y heterociclilamino de 4 a 7 miembros; cada uno de los cuales está opcionalmente sustituido con 1 a 4 sustituyentes, en donde cada sustituyente se selecciona independientemente del grupo que consiste en OH, NH₂, halo, ciano, carboxi, carbamoilo, alquilo C₁₋₆, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆ y heterociclilo de 4 a 7 miembros; en donde dos sustituyentes geminales se pueden tomar juntos para formar espirocicloalquilo C₃₋₇ o espiroheterociclilo de 4 a 7 miembros; Y se selecciona del grupo que consiste en -L-Y¹ o Y¹; Y¹ se selecciona del grupo que consiste en H, NH₂, halo, ciano, carbamoilo, alquenilo C₂₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con un heterociclilo de 4 a 10 miembros que se sustituye opcionalmente con 1 - 4 sustituyentes Y¹ᵃ, alquilo C₁₋₆ sustituido con un sustituyente dialquilamino C₁₋₆, alquilo C₁₋₆ sustituido con un dialquilamino ciclopropilo C₁₋₆, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, alquinilo C₂₋₆, alquilamino C₁₋₆, arilo C₆₋₁₄, arilo C₆₋₁₄ sustituido con un alquilo C₁₋₆, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇ sustituido con un dialquilamino C₁₋₆, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo de 5 a 10 miembros, heterociclilo de 4 a 10 miembros, un heterociclilo de 4 a 10 miembros sustituido con metilo, hidroxi y oxo; cada Y¹ᵃ se selecciona independientemente del grupo que consiste en halo, alquilo C₁₋₆, alcoxi C₁₋₆, heterociclilo de 3 a 7 miembros, alcoxi C₁₋₆alquilo C₁₋₆, haloalquilo C₁₋₆, oxo, hidroxi, NH₂, ciano, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, hidroxialquilo C₁₋₆ y haloalcoxi C₁₋₆; L se selecciona del grupo que consiste en un enlace, O, S y N(Lᵃ); Lᵃ se selecciona del grupo que consiste en hidrógeno y alquilo C₁₋₃; U es C(R⁶ᵃ); V es C(R⁶ᵇ); W es C(R⁶ᶜ) o N; cada uno de R⁶ᵃ, R⁶ᵇ y R⁶ᶜ se selecciona independientemente del grupo que consiste en H, OH, NH₂, halo, ciano, carbamoilo, alquenilo C₂₋₆, alcoxi C₁₋₆, alquilo C₁₋₆, alquilo C₁₋₆ sustituido con un sustituyente heterociclilo de 4 a 10 miembros, alquilsulfanilo C₁₋₆, alquilsulfonilo C₁₋₆, alquiltio C₁₋₆, haloalquiltio C₁₋₆, alquinilo C₂₋₆, alquilamino C₁₋₆, arilo C₆₋₁₄, aminoalquilo C₁₋₆, carbamoilalquilo C₁₋₆, carboxialquilo C₁₋₆, cianoalquilo C₁₋₆, cicloalquilo C₃₋₇, haloalcoxi C₁₋₆, haloalquilo C₁₋₆, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros; y n se selecciona del grupo que consiste en 0, 1 y 2.
ARP190103302A 2018-11-09 2019-11-08 Compuestos de anillos fusionados AR117194A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2018114788 2018-11-09

Publications (1)

Publication Number Publication Date
AR117194A1 true AR117194A1 (es) 2021-07-21

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Family Applications (1)

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US (2) US11236068B2 (es)
EP (1) EP3735299A2 (es)
JP (3) JP6941241B2 (es)
KR (2) KR20230147742A (es)
CN (5) CN118084867A (es)
AR (1) AR117194A1 (es)
AU (3) AU2019377130B2 (es)
BR (1) BR112021008986A2 (es)
CA (1) CA3087089C (es)
CL (2) CL2021001171A1 (es)
CO (1) CO2021005987A2 (es)
CR (1) CR20210229A (es)
IL (2) IL311187A (es)
MA (1) MA51530A (es)
MX (1) MX2021005428A (es)
MY (1) MY196726A (es)
PE (1) PE20211504A1 (es)
PH (1) PH12021551065A1 (es)
SG (1) SG11202103298QA (es)
TW (2) TWI784209B (es)
UA (1) UA127930C2 (es)
WO (1) WO2020097537A2 (es)

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CR20210229A (es) 2021-06-30
US11236068B2 (en) 2022-02-01
JP2021512136A (ja) 2021-05-13
PH12021551065A1 (en) 2021-11-22
CO2021005987A2 (es) 2021-05-20
CL2022000698A1 (es) 2022-10-21
TW202325703A (zh) 2023-07-01
PE20211504A1 (es) 2021-08-11
CN118084867A (zh) 2024-05-28
KR20200119824A (ko) 2020-10-20
AU2019377130B2 (en) 2022-03-17
TWI784209B (zh) 2022-11-21
AU2022201413B2 (en) 2024-02-29
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