AR089727A1 - Compuesto de pirazin-carboxamida - Google Patents

Compuesto de pirazin-carboxamida

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Publication number
AR089727A1
AR089727A1 ARP130100118A ARP130100118A AR089727A1 AR 089727 A1 AR089727 A1 AR 089727A1 AR P130100118 A ARP130100118 A AR P130100118A AR P130100118 A ARP130100118 A AR P130100118A AR 089727 A1 AR089727 A1 AR 089727A1
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AR
Argentina
Prior art keywords
substituted
lower alkyl
alkylene
egfr
mutation
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ARP130100118A
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English (en)
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Astellas Pharma Inc
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Application filed by Astellas Pharma Inc filed Critical Astellas Pharma Inc
Publication of AR089727A1 publication Critical patent/AR089727A1/es

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    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
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    • 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
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    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • C07D491/10Spiro-condensed systems
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Steroid Compounds (AREA)

Abstract

El compuesto de pirazin-carboxamida de la presente tiene una acción inhibidora sobre una quinasa con mutación T790M en el EGFR, y se puede usar como agente para prevenir y/o tratar el cáncer positivo con mutación T790M en el EGFR; en otra forma de realización, cáncer de pulmón positivo con mutación T790M en el EGRF; aún en otra forma de realización, cáncer de pulmón de células no pequeñas positivo con mutación T790M en el EGFR; también en otra forma de realización, cáncer de proteínas positivo con mutación T790M en el EGRF; en una forma de realización diferente, cáncer de pulmón de proteínas positivo con mutación T790M en el EGRF; aún en una forma de realización diferente, cáncer resistente al inhibidor de la tirosina quinasa en el EGFR; aún en una forma de realización diferente, cáncer de pulmón resistente al inhibidor de la tirosina quinasa en el EGFR; y también en otra forma de realización diferente, cáncer de pulmón de células no pequeñas resistente al inhibidor de la tirosina quinasa en el EGFR y similares. Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales, donde R¹ representa alquilo inferior que puede estar sustituido, -O-alquilo inferior que puede estar sustituido, -NH₂, -NH-alquilo inferior que puede estar sustituido, -N(alquilo inferior que puede estar sustituido)₂, -L⁴-cicloalquilo que puede estar sustituido, -L⁴-arilo que puede estar sustituido, -L⁴-grupo heterocíclico aromático que puede estar sustituido, o -L⁴-grupo heterocíclico no aromático que puede estar sustituido; el anillo A representa areno que puede estar sustituido o un heterociclo aromático que puede estar sustituido; L¹ representa -O- o -NH-; R² representa H, halógeno, -OH, -NR⁵R⁶, -CONH₂, -CN, -L⁴-cicloalquilo que puede estar sustituido, -L⁴-arilo que puede estar sustituido, -L⁴-grupo heterocíclico aromático que puede estar sustituido, -L⁴-grupo heterocíclico no aromático que puede estar sustituido, alquilo inferior que puede estar sustituido, alquenilo inferior que puede estar sustituido, o alquinilo inferior que puede estar sustituido; L² representa -O-, -S(O)ₚ-, -NH-, -N(CH₃)-, -NHCH₂-, -NHCH₂CH₂-, -OCH₂- o una unión; Y representa anillo X o una unión; el anillo X representa cicloalcano que puede estar sustituido, areno que puede estar sustituido, un heterociclo aromático que puede estar sustituido, o un heterociclo no aromático que puede estar sustituido; L³ representa -O-, -NH-, -N(alquilo inferior que puede estar sustituido)-, -N(cicloalquilo que puede estar sustituido), -alquileno inferior que puede estar sustituido-, -alquileno inferior que puede estar sustituido-NH-, -NH-alquileno inferior que puede estar sustituido-, -alquileno inferior que puede estar sustituido-N(alquilo inferior que puede estar sustituido)-, -N(alquilo inferior que puede estar sustituido)-alquileno inferior que puede estar sustituido- o una unión; M representa -C(O)- o -S(O)₂-; R³ representa H o alquilo inferior que puede estar sustituido; R⁴ representa alquilo inferior que puede estar sustituido con uno o más sustituyentes que se seleccionan del grupo que consiste de -OH, halógeno, -NH₂, -NH-(alquilo inferior que puede estar sustituido), -N(alquilo inferior que puede estar sustituido)₂, y un grupo heterocíclico no aromático que puede estar sustituido, o H; R⁵ y R⁶ son iguales o diferentes entre sí, y representan H o alquilo inferior que puede estar sustituido; L⁴s son iguales o diferentes entre sí, y representan alquileno inferior que puede estar sustituido-, -NH-, -O-, -O-alquileno inferior que puede estar sustituido-, -alquileno inferior que puede estar sustituido-O- o una unión; y p representa 0, 1 ó 2.
ARP130100118A 2012-01-17 2013-01-15 Compuesto de pirazin-carboxamida AR089727A1 (es)

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JP2012007525 2012-01-17

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US (1) US9085540B2 (es)
EP (1) EP2805940B1 (es)
JP (1) JP5532366B2 (es)
KR (1) KR101985050B1 (es)
CN (1) CN104080774B (es)
AR (1) AR089727A1 (es)
AU (1) AU2013210438B2 (es)
BR (1) BR112014017466A8 (es)
CA (1) CA2860765C (es)
CY (1) CY1118644T1 (es)
DK (1) DK2805940T3 (es)
EA (1) EA026353B1 (es)
ES (1) ES2613399T3 (es)
HK (1) HK1203491A1 (es)
HR (1) HRP20170226T1 (es)
HU (1) HUE033177T2 (es)
IL (1) IL233437A (es)
LT (1) LT2805940T (es)
ME (1) ME02648B (es)
MX (1) MX355434B (es)
PH (1) PH12014501456A1 (es)
PL (1) PL2805940T3 (es)
PT (1) PT2805940T (es)
RS (1) RS55704B1 (es)
SI (1) SI2805940T1 (es)
SM (1) SMT201700094B (es)
TW (1) TWI532727B (es)
UA (1) UA111010C2 (es)
WO (1) WO2013108754A1 (es)
ZA (1) ZA201405045B (es)

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