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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • C07D241/28—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
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    • 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
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    • 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
    • C07D403/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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 two hetero rings
    • C07D405/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D487/08—Bridged systems
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    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • 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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Application Number Priority Date Filing Date Title
JP2012007525 2012-01-17

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AR089727A1 true AR089727A1 (es) 2014-09-10

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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)
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 (2) SMT201700094T1 (es)
TW (1) TWI532727B (es)
UA (1) UA111010C2 (es)
WO (1) WO2013108754A1 (es)
ZA (1) ZA201405045B (es)

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