AR100327A1 - Inhibidores de quinasa relacionados con tropomiosina - Google Patents

Inhibidores de quinasa relacionados con tropomiosina

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Publication number
AR100327A1
AR100327A1 ARP150101378A ARP150101378A AR100327A1 AR 100327 A1 AR100327 A1 AR 100327A1 AR P150101378 A ARP150101378 A AR P150101378A AR P150101378 A ARP150101378 A AR P150101378A AR 100327 A1 AR100327 A1 AR 100327A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
cycloalkyl
het
alkoxy
Prior art date
Application number
ARP150101378A
Other languages
English (en)
Inventor
Scott Warmus Joseph
Ian Storer Robert
Elizabeth Skerratt Sarah
Omoto Kiyoyuki
Ninkovik Sacha
Nagata Asako
Elizabeth Greasley Samantha
Jean Cui Jingrong
Kaur Bagal Sharanjeet
James Malpine Indrawan
Ann Lunney Elizabeth
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of AR100327A1 publication Critical patent/AR100327A1/es

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Classifications

    • 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
    • C07D401/14—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D405/14—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
    • C—CHEMISTRY; METALLURGY
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o uno de sus profármacos o una de sus sales farmacéuticamente aceptables, en donde R¹ es CN, CO₂Rˣ, CO-(NHet), CONRˣ¹-(cicloalquilo C₃₋₈, Ar, Het o Rˣ²), CONRˣ¹(CRˣRʸ)ₘ(NHet, NRˣ¹Rˣ², cicloalquilo C₃₋₈, Ar, Het o Rˣ²), CONRˣ¹(CRYRX)ₘCO(NHet, NRˣ¹Rˣ², cicloalquilo C₃₋₈, Ar, Het o Rˣ²), CONRˣ¹(CRYRX)ₘNRˣ¹CO(NHet, NRˣ¹Rˣ², cicloalquilo C₃₋₈, Ar, Het o Rˣ²), CONRˣ¹CO(NHet, NRˣ¹Rˣ², cicloalquilo C₃₋₈, Ar, Het o Rˣ²), CONRˣ¹CO-(CRˣRʸ)ₘ(NHet, NRˣ¹Rˣ², cicloalquilo C₃₋₈, Ar, Het o Rˣ²), CONRˣ¹(CRˣRʸ)ₘCONRˣ¹-(NHet, NRˣ¹Rˣ², cicloalquilo C₃₋₈, Ar, Het o Rˣ²); Rˣ¹ y Rˣ² son cada uno, de modo independiente, H, alquilo C₁₋₆ opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, OH, NH₂, NH(alquilo C₁₋₆), N(alquilo C₁₋₆)₂, CN, (alcoxi C₁₋₆ opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, OH, NH₂, NH(alquilo CN, opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, OH, NH₂), N(alquilo C₁₋₆ opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, OH, NH₂)₂ y alcoxi C₁₋₆) y alcoxi C₁₋₆) y (alquilo C₁₋₆ opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, NH₂, NH(alquilo C₁₋₆), N(alquilo C₁₋₆)₂ y alcoxi C₁₋₆), o, junto con el átomo de nitrógeno al que están unidos, Rˣ¹ y Rˣ² forman un anillo NHet; NHet es un anillo heterocíclico saturado o insaturado de 4 a 8 miembros con un átomo de N del anillo directamente ligado con el resto ligado, que tiene de 0 a 2 otros heteroátomos del anillo seleccionados, de modo independiente, de N, O y S; Het es un anillo heterocíclico saturado o insaturado de 4 a 8 miembros que tiene al menos 1 y hasta 3 heteroátomos del anillo seleccionados, de modo independiente, de N, O y S; los grupos cicloalquilo C₃₋₈, NHet y Het pueden ser monocíclicos, bicíclicos, en puente o espirocíclicos si lo permite la cantidad de átomos del anillo; Ar es fenilo, en donde cada uno de cicloalquilo C₃₋₈, Ar, NHet y Het están opcionalmente sustituidos, donde lo permita la valencia, con hasta 5 sustituyentes seleccionados, de modo independiente, de alquilo C₁₋₆ opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, OH, CN, NRˣ¹Rˣ², NHCORˣ¹, NHCO(CRˣRʸ)ₘNRˣ¹Rˣ², CONRˣ¹Rˣ², alcoxi C₁₋₆, alcoxi C₁₋₆-C(O)-, CONRˣ¹Rˣ², alquil C₁₋₆-tio, hidroxi-alquilo C₁₋₆, alquil C₁₋₆-SO₂-, CO₂Rˣ y alcoxi C₁₋₃-alquil C₁₋₃-O-C(O)-; halógeno, CN, alcoxi C₁₋₆, alcoxi C₁₋₆-C(O)-, CONRˣ¹Rˣ², alquil C₁₋₆-tio, hidroxi-alquilo C₁₋₆, alquil C₁₋₆-SO₂-, CO₂Rˣ, alcoxi C₁₋₃-alquil C₁₋₃-O-C(O)-, OH, =O, O(alquilo C₁₋₆ opcionalmente sustituido con uno o varios F), C(O)(alquilo C₁₋₆ opcionalmente sustituido con uno o varios F), alquilo C₁₋₆, opcionalmente sustituido con uno o varios F, alquilo C₁₋₆ sustituido con CN, alquilo C₁₋₆, sustituido con hasta 3 OH, alquilo C₁₋₆ sustituido con CO₂(alquilo C₁₋₄), alquilo C₁₋₆ sustituido con uno o varios alcoxi C₁₋₃, SO₂(alquilo C₁₋₆ opcionalmente sustituido con uno o varios F), CO₂(alquilo C₁₋₆), cicloalquilo C₃₋₆, C₍O₎₍ᶜⁱᶜₗₒₐₗqᵘⁱₗₒ C₃₋₆), N(H o alquil C₁₋₃)CO(alquilo C₁₋₃) y N(H o alquil C₁₋₃)(H o alquilo C₁₋₃); m es un número entero de 1 a 4; R²ᵃ, R²ᵇ, R²ᶜ, R²ᵈ y R²ᵉ se seleccionan cada uno, de modo independiente, de H, OH, halógeno, NH₂ o metilo opcionalmente sustituido con hasta 3 F; X¹, X², R¹ᵃ, R⁴, R⁴ᵃ y R⁵ se seleccionan cada uno, de modo independiente, de H, cicloalquilo C₃₋₆, alquilo C₀₋₆ opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de halógeno, CN, CO₂H, OH, (alcoxi C₁₋₆ opcionalmente sustituido con hasta 3 F), S(O)ₚ(alquilo C₁₋₆ opcionalmente sustituido con hasta 3 F), C(O)(alcoxi C₁₋₆ opcionalmente sustituido con hasta 3 F o con alcoxi C₁₋₃), C(O)NRˣ¹Rˣ², NRˣ¹Rˣ², O(cicloalquilo C₃₋₆), Ar, Het, CO₂(alquilo C₁₋₆ opcionalmente sustituido con hasta 3 F), NRˣ¹C(O)(alquilo C₁₋₆ opcionalmente sustituido con hasta 3 F), NRˣ¹C(O)NRˣ²(alquilo C₁₋₆ opcionalmente sustituido con hasta 3 F), OC(O)(alquilo C₁₋₆ opcionalmente sustituido con hasta 3 F) y OC(O)NRˣ¹Rˣ²; p es 0, 1 ó 2; R³ es H, alquilo C₀₋₃ opcionalmente sustituido con CN, N(H o alquilo C₁₋₃ opcionalmente sustituido con uno o varios F)(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F), Het, OH, SH, Ar, OAr, uno o varios halógenos, CONRXRY, CO₂CRXRY, CONRXRY, S(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F), S-(CRXRY)₀₋₂Het, S-(CRXRY)₀₋₂Ar, S-(CRXRY)₀₋₂(cicloalquilo C₃₋₆), SONRXRY, SO₂CRXRY, O(CRXRY)ₘ(CO)NRXRY, NHSO₂(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F o con Ar o Het o (cicloalquilo C₃₋₆)), NHSO₂NRXRY, CONHSO₂CRXRY, alquino C₂₋₆, alqueno C₂₋₆, cicloalquilo C₃₋₆ opcionalmente sustituido con uno o varios F o con O(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F), o R³ es NH(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F), NH(cicloalquilo C₃₋₆), NH-Het, NHCO(alquilo C₁₋₄ opcionalmente sustituido con uno o varios F), NHCOCRˣRʸHet, NHCOCRˣRʸAr, NHSO₂-(alquilo C₁₋₆), NHCONH-(H o alquilo C₁₋₆), NHCONH-(cicloalquilo C₃₋₆), NHSO₂-(cicloalquilo C₃₋₆), CRˣRʸO(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F, Het, arilo o cicloalquilo C₃₋₆), CH₂O-Het, CH₂O-(cicloalquilo C₃₋₆), O(alquilo C₁₋₃ opcionalmente sustituido con uno o varios F), O(cicloalquilo C₃₋₆), O-Het, NHCO(cicloalquilo C₃₋₆, Ar o Het), cicloalquilo C₃₋₆, Het, C(O)N(H o alquilo C₁₋₃ opcionalmente sustituido con uno o varios F)(H o alquilo C₁₋₃ opcionalmente sustituido con uno o varios F) o NH(alquilo C₂₋₃ opcionalmente sustituido con uno o varios F o alquil C₁₋₃)NHCO(alquilo C₁₋₆ opcionalmente sustituido con uno o varios F); y Rˣ y Rʸ son cada uno, de modo independiente, H, alquilo C₁₋₃ (opcionalmente sustituido con hasta 3 sustituyentes seleccionados, de modo independiente, de F, OH y OCH₃), alcoxi C₁₋₃ opcionalmente sustituido con hasta 3 F o junto con el C al que están unidos, son cicloalquilo C₃₋₆.
ARP150101378A 2014-05-07 2015-05-06 Inhibidores de quinasa relacionados con tropomiosina AR100327A1 (es)

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US (1) US9328096B2 (es)
EP (1) EP3140298A1 (es)
AR (1) AR100327A1 (es)
TW (1) TW201546060A (es)
UY (1) UY36110A (es)
WO (1) WO2015170218A1 (es)

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