AR091079A1 - Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak - Google Patents

Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak

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Publication number
AR091079A1
AR091079A1 ARP130101717A ARP130101717A AR091079A1 AR 091079 A1 AR091079 A1 AR 091079A1 AR P130101717 A ARP130101717 A AR P130101717A AR P130101717 A ARP130101717 A AR P130101717A AR 091079 A1 AR091079 A1 AR 091079A1
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Argentina
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alkyl
heterocycloalkyl
cycloalkyl
heteroaryl
aryl
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ARP130101717A
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English (en)
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Incyte Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Abstract

Compuestos útiles para el tratamiento de las enfermedades relacionadas con la actividad de las JAK, como trastornos inflamatorios, trastornos autoinmunitarios, cáncer y otras enfermedades. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este; en donde: X es N o CH; L es O ó NR²ᵃ; (a) en donde cuando L es O, entonces: Y es CH; R¹ es -C(=O)NR³R⁴, -CH₂CH₂OH, -CH₂NR³R⁴ o un anillo de oxetano, en donde el anillo de oxetano está opcionalmente sustituido con R⁵; R² es CF₃; R³ es -[CH(R⁶ᵃ)]ₙ-OR⁶ᵇ, ciclopropilo, ciclobutilo, anillo de tetrahidro-2H-pirano, anillo de tetrahidrofurano, o anillo de oxetano, en donde cada ciclopropilo, ciclobutilo, anillo de tetrahidro-2H-pirano, anillo de tetrahidrofurano y anillo de oxetano está opcionalmente sustituido con 1 ó 2 grupos seleccionados independientemente de CN, OH, metilo, etilo, n-propilo, isopropilo, metoxilo, etoxilo y propoxilo; R⁴ es H, CH₃, o -[CH(R⁶ᵃ)]ₙ-OR⁶ᵇ; o alternativamente, R³ y R⁴, tomados junto con el átomo de nitrógeno al cual están unidos, forman un grupo acetidinilo, 1H-pirazolilo, un grupo 1H-imidazolilo o un grupo 1H-triazolilo, en donde dicho grupo acetidinilo está opcionalmente sustituido con 1 ó 2 grupos R³ᵃ seleccionados independientemente; cada R³ᵃ es independientemente CN, OH, metilo, etilo, n-propilo, isopropilo, metoxilo, etoxilo, propoxilo o -CH₂-OH; o alternativamente, dos grupos R³ᵃ, tomados junto con el átomo de carbono al cual ambos están unidos, forman un anillo de oxetano; R⁵ es OH o NH₂; cada R⁶ᵃ y R⁶ᵇ es independientemente H o CH₃; y cada n es independientemente 2 ó 3; cuando X es N, NR³R⁴ no es NHCH₂CH₂-OH, NHCH₂CH₂CH₂-OH, o un resto de fórmula (2) ó (3); o alternativamente, (b) en donde cuando L es NR²ᵃ, entonces: Y es CH o N; R¹ es halo, ciano, nitro, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquilo C₃₋₁₀-alquilo C₁₋₄, heterocicloalquilo C₂₋₁₀, heterocicloalquilo C₂₋₁₀-alquilo C₁₋₄, arilo C₆₋₁₀, arilo C₆₋₁₀-alquilo C₁₋₄, heteroarilo C₁₋₁₀, heteroarilo C₁₋₁₀-alquilo C₁₋₄, -ORᵃ, -SRᵃ, -S(=O)Rᵇ, -S(=O)₂Rᵇ, -S(=O)₂NRᵉRᶠ, -C(=O)Rᵇ, -C(=O)ORᵃ, -C(=O)NRᵉRᶠ, -OC(=O)Rᵇ, -OC(=O)NRᵉRᶠ, -NRᵉRᶠ, -NRᶜC(=O)Rᵈ, -NRᶜC(=O)ORᵈ, NRᶜC(=O)NRᵈ, -NRᶜS(=O)₂Rᵈ o -NRᶜS(=O)₂NRᵉRᶠ; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquilo C₃₋₁₀-alquilo C₁₋₄, heterocicloalquilo C₂₋₁₀, heterocicloalquilo C₂₋₁₀-alquilo C₁₋₄, arilo C₆₋₁₀, arilo C₆₋₁₀-alquilo C₁₋₄, heteroarilo C₁₋₁₀ y heteroarilo C₁₋₁₀-alquilo C₁₋₄ opcionalmente sustituido por 1, 2, 3 ó 4 grupos Rᵍ seleccionados independientemente; R² es H, halo, ciano, nitro, alquilo C₁₋₄ o haloalquilo C₁₋₄; R²ᵃ es H o CH₃; cada Rᵃ, Rᶜ, Rᵈ, Rᵉ y Rᶠ se selecciona independientemente de H, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquilo C₃₋₁₀-alquilo C₁₋₄, heterocicloalquilo C₂₋₁₀, heterocicloalquilo C₂₋₁₀-alquilo C₁₋₄, arilo C₆₋₁₀, arilo C₆₋₁₀-alquilo C₁₋₄, heteroarilo C₁₋₁₀ y heteroarilo C₁₋₁₀-alquilo C₁₋₄; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquilo C₃₋₁₀-alquilo C₁₋₄, heterocicloalquilo C₂₋₁₀, heterocicloalquilo C₂₋₁₀-alquilo C₁₋₄, arilo C₆₋₁₀, arilo C₆₋₁₀-alquilo C₁₋₄, heteroarilo C₁₋₁₀ y heteroarilo C₁₋₁₀-alquilo C₁₋₄ está opcionalmente sustituido por 1, 2, 3 ó 4 grupos Rᵍ seleccionados independientemente; cada Rᵇ se selecciona independientemente de alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquilo C₃₋₁₀-alquilo C₁₋₄, heterocicloalquilo C₂₋₁₀, heterocicloalquilo C₂₋₁₀-alquilo C₁₋₄, arilo C₆₋₁₀, arilo C₆₋₁₀-alquilo C₁₋₄, heteroarilo C₁₋₁₀ y heteroarilo C₁₋₁₀-alquilo C₁₋₄; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₁₀, cicloalquilo C₃₋₁₀-alquilo C₁₋₄, heterocicloalquilo C₂₋₁₀, heterocicloalquilo C₂₋₁₀-alquilo C₁₋₄, arilo C₆₋₁₀, arilo C₆₋₁₀-alquilo C₁₋₄, heteroarilo C₁₋₁₀ y heteroarilo C₁₋₁₀-alquilo C₁₋₄ está opcionalmente sustituido por 1, 2, 3 ó 4 grupos Rᵍ seleccionados independientemente; cada Rᵍ se selecciona independientemente de halo, ciano, nitro, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇-alquilo C₁₋₃, heterocicloalquilo C₂₋₇, heterocicloalquilo C₂₋₇-alquilo C₁₋₃, fenilo, fenilo-alquilo C₁₋₃, heteroarilo C₁₋₇, heteroarilo C₁₋₇-alquilo C₁₋₃, -ORᵃ¹, -SRᵃ¹, -S(=O)Rᵇ¹, -S(=O)₂Rᵇ¹, -S(=O)₂NRᵉ¹Rᶠ¹, -C(=O)Rᵇ¹, -C(=O)ORᵃ¹, -C(=O)NRᵉ¹Rᶠ¹, -OC(=O)Rᵇ¹, -OC(=O)NRᵉ¹Rᶠ¹, -NRᵉ¹Rᶠ¹, -NRᶜ¹C(=O)Rᵈ¹, -NRᶜ¹C(=O)ORᵈ¹, -NRᶜ¹C(=O)NRᵈ¹, -NRᶜ¹S(=O)₂Rᵈ¹ y -NRᶜ¹S(=O)₂NRᵉ¹Rᶠ¹; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇-alquilo C₁₋₃, heterocicloalquilo C₂₋₇, heterocicloalquilo C₂₋₇-alquilo C₁₋₃, fenilo, fenilo-alquilo C₁₋₃, heteroarilo C₁₋₇ y heteroarilo C₁₋₇-alquilo C₁₋₃ está opcionalmente sustituido con 1, 2, 3 ó 4 grupos Rʰ seleccionados independientemente; cada Rᵃ¹, Rᶜ¹, Rᵈ¹, Rᵉ¹ y Rᶠ¹ se selecciona independientemente de H, alquilo C₁₋₆, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇-alquilo C₁₋₃, heterocicloalquilo C₂₋₇, heterocicloalquilo C₂₋₇-alquilo C₁₋₃, fenilo, fenil-alquilo C₁₋₃, heteroarilo C₁₋₇ y heteroarilo C₁₋₇-alquilo C₁₋₃; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₇, cicloalquilo C₃₋₇-alquilo C₁₋₃, heterocicloalquilo C₂₋₇, heterocicloalquilo C₂₋₇-alquilo C₁₋₃, fenilo, fenil-alquilo C₁₋₃, heteroarilo C₁₋₇ y heteroarilo C₁₋₇-alquilo C₁₋₃ está opcionalmente sustituido por 1, 2, 3 ó 4 grupos Rʰ seleccionados independientemente; cada Rᵇ¹ se selecciona independientemente de alquilo C₁₋₆, haloalquilo C₁
ARP130101717A 2012-05-18 2013-05-17 Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak AR091079A1 (es)

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