AR108396A1 - Compuestos heterocíclicos como inmunomoduladores - Google Patents

Compuestos heterocíclicos como inmunomoduladores

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Publication number
AR108396A1
AR108396A1 ARP170101185A ARP170101185A AR108396A1 AR 108396 A1 AR108396 A1 AR 108396A1 AR P170101185 A ARP170101185 A AR P170101185A AR P170101185 A ARP170101185 A AR P170101185A AR 108396 A1 AR108396 A1 AR 108396A1
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Argentina
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alkyl
cycloalkyl
membered heterocycloalkyl
aryl
substituents
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ARP170101185A
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Wenqing Yao
Zhenwu Li
Liangxing Wu
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Incyte Corp
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Publication of AR108396A1 publication Critical patent/AR108396A1/es

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Se describen compuestos, su uso como inmunomoduladores, y composiciones farmacéuticas que comprenden dichos compuestos. Los compuestos son útiles para tratar, prevenir o mejorar enfermedades o trastornos tales como cáncer o infecciones. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable o un estereoisómero de este, en donde: X¹ es O, S, N, NR¹ o CR¹; X² es N o C; X³ es O, S, N, NR³ o CR³; X⁴ es N o CR⁴; X⁵ es N o CR⁵; X⁶ es N o CR⁶; Y es C o N; al menos uno de X¹, X², X³ e Y es un heteroátomo seleccionado de N, O y S, en donde N se sustituye opcionalmente por R¹ o R³; Cy es arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 a 14 miembros o heterocicloalquilo de 4 a 10 miembros, cada uno sustituido opcionalmente con 1 a 5 sustituyentes R⁷ seleccionados independientemente; R¹, R³, R⁴, R⁵ y R⁶ se seleccionan, cada uno, independientemente de H, alquilo C₁₋₄, cicloalquilo C₃₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, halo, CN, OH, alcoxi C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, NH₂, alquilo -NH-C₁₋₄, -N(alquilo C₁₋₄)₂, NHOR¹⁰, C(O)R¹⁰, C(O)NR¹⁰R¹⁰, C(O)OR¹⁰, OC(O)R¹⁰, OC(O)NR¹⁰R¹⁰, NR¹⁰C(O)R¹⁰, NR¹⁰C(O)OR¹⁰, NR¹⁰C(O)NR¹⁰R¹⁰, C(=NR¹⁰)R¹⁰, C(=NR¹⁰)NR¹⁰R¹⁰, NR¹⁰C(=NR¹⁰)NR¹⁰R¹⁰, NR¹⁰S(O)R¹⁰, NR¹⁰S(O)₂R¹⁰, NR¹⁰S(O)₂NR¹⁰R¹⁰, S(O)R¹⁰, S(O)NR¹⁰R¹⁰, S(O)₂R¹⁰ y S(O)₂NR¹⁰R¹⁰, en donde cada R¹⁰ se selecciona independientemente de H y alquilo C₁₋₄ opcionalmente sustituido con 1 ó 2 grupos seleccionados independientemente de halo, OH, CN y alcoxi C₁₋₄; y en donde el alquilo C₁₋₄, cicloalquilo C₃₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄ y alcoxi C₁₋₄ de R¹, R³, R⁴, R⁵ y R⁶ están sustituidos, cada uno, opcionalmente con 1 ó 2 sustituyentes seleccionados independientemente de halo, OH, CN y alcoxi C₁₋₄; R⁹ es alquilo C₁₋₄, halo, CN, OH, ciclopropilo, alquenilo C₂₋₄, alquinilo C₂₋₄, alcoxi C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, NH₂, -NH-alquilo C₁₋₄, -N(alquilo C₁₋₄)₂, NHOR¹¹, C(O)R¹¹, C(O)NR¹¹R¹¹, C(O)OR¹¹, OC(O)R¹¹, OC(O)NR¹¹R¹¹, NR¹¹C(O)R¹¹, NR¹¹C(O)OR¹¹, NR¹¹C(O)NR¹¹R¹¹, C(=NR¹¹)R¹¹, C(=NR¹¹)NR¹¹R¹¹, NR¹¹C(=NR¹¹)NR¹¹R¹¹, NR¹¹S(O)R¹¹, NR¹¹S(O)₂R¹¹, NR¹¹S(O)₂NR¹¹R¹¹, S(O)R¹¹, S(O)NR¹¹R¹¹, S(O)₂R¹¹ y S(O)₂NR¹¹R¹¹, en donde alquilo C₁₋₄, ciclopropilo, alquenilo C₂₋₄, alquinilo C₂₋₄ y alcoxi C₁₋₄ de R⁹ están sustituidos, cada uno, opcionalmente, con 1 ó 2 sustituyentes seleccionados de halo, OH, CN y OCH₃ y cada R¹¹ se selecciona independientemente de H y alquilo C₁₋₄ sustituido opcionalmente con 1 ó 2 sustituyentes halo, OH, CN o OCH₃; cada R⁷, R¹³ y R¹⁴ se selecciona independientemente de H, halo, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 14 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 14 miembros)-alquilo C₁₋₄-, (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄-, CN, NO₂, ORᵃ, SRᵃ, NHORᵃ, C(O)Rᵃ, C(O)NRᵃRᵃ, C(O)ORᵃ, OC(O)Rᵃ, OC(O)NRᵃRᵃ, NHRᵃ, NRᵃRᵃ, NRᵃC(O)Rᵃ, NRᵃC(O)ORᵃ, NRᵃC(O)NRᵃRᵃ, C(=NRᵃ)Rᵃ, C(=NRᵃ)NRᵃRᵃ, NRᵃC(=NRᵃ)NRᵃRᵃ, NRᵃS(O)Rᵃ, NRᵃS(O)₂Rᵃ, NRᵃS(O)₂NRᵃRᵃ, S(O)Rᵃ, S(O)NRᵃRᵃ, S(O)₂Rᵃ y S(O)₂NRᵃRᵃ, en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 14 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 14 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄- de R⁷, R¹³ y R¹⁴ se sustituye opcionalmente con 1, 2, 3 ó 4 sustituyentes Rᵇ; o dos sustituyentes de R⁷ adyacentes en el anillo de Cy, tomados en conjunto con los átomos a los cuales están unidos, forman un anillo de fenilo fusionado, un anillo heterocicloalquilo de 5, 6 ó 7 miembros fusionado, un anillo heteroarilo de 5 ó 6 miembros fusionado o un anillo cicloalquilo de C₃₋₆ fusionado, en donde cada anillo heterocicloalquilo de 5, 6 ó 7 miembros fusionado y anillo heteroarilo de 5 ó 6 miembros fusionado tiene 1 - 4 heteroátomos como miembros de anillo seleccionados de N, O y S y en donde cada anillo fenilo fusionado, anillo heterocicloalquilo de 5, 6 ó 7 miembros fusionado, anillo heteroarilo de 5 ó 6 miembros fusionado y anillo cicloalquilo de C₃₋₆ fusionado se sustituye opcionalmente con 1, 2 ó 3 sustituyentes de Rᵇ seleccionados independientemente; o dos sustituyentes de R¹³ unidos al mismo átomo de carbono, tomados junto con el átomo de carbono al cual están unidos, forman un anillo cicloalquilo de C₃₋₆ o anillo heterocicloalquilo de 4, 5, 6 ó 7 miembros, en donde cada anillo cicloalquilo de C₃₋₆ y anillo heterocicloalquilo de 4, 5, 6 ó 7 miembros se sustituye opcionalmente con 1, 2 ó 3 sustituyentes de Rᵇ seleccionados independientemente; cada Rᵃ se selecciona independientemente de H, CN, alquilo C₁₋₆, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄-, en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄- de Rᵃ se sustituye opcionalmente con 1, 2, 3, 4 ó 5 sustituyentes de Rᵈ; cada Rᵈ se selecciona independientemente de alquilo C₁₋₄, haloalquilo C₁₋₄, halo, cicloalquilo C₃₋₁₀, heterocicloalquilo de 4 - 10 miembros, CN, NH₂, NHORᵉ, ORᵉ, SRᵉ, C(O)Rᵉ, C(O)NRᵉRᵉ, C(O)ORᵉ, OC(O)Rᵉ, OC(O)NRᵉRᵉ, NHRᵉ, NRᵉRᵉ, NRᵉC(O)Rᵉ, NRᵉC(O)NRᵉRᵉ, NRᵉC(O)ORᵉ, C(=NRᵉ)NRᵉRᵉ, NRᵉC(=NRᵉ)NRᵉRᵉ, S(O)Rᵉ, S(O)NRᵉRᵉ, S(O)₂Rᵉ, NRᵉS(O)₂Rᵉ, NRᵉS(O)₂NRᵉRᵉ y S(O)₂NRᵉRᵉ, en donde cada alquilo C₁₋₄, cicloalquilo C₃₋₁₀ y heterocicloalquilo de 4 - 10 miembros de Rᵈ se sustituye, además, opcionalmente con 1 - 3 sustituyentes de Rq seleccionados independientemente; cada sustituyente de Rᵇ se selecciona independientemente de halo, alquilo C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄-, (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄-, CN, OH, NH₂, NO₂, NHORᶜ, ORᶜ, SRᶜ, C(O)Rᶜ, C(O)NRᶜRᶜ, C(O)ORᶜ, OC(O)Rᶜ, OC(O)NRᶜRᶜ, C(=NRᶜ)NRᶜRᶜ, NRᶜC(=NRᶜ)NRᶜRᶜ, NHRᶜ, NRᶜRᶜ, NRᶜC(O)Rᶜ, NRᶜC(O)ORᶜ, NRᶜC(O)NRᶜRᶜ, NRᶜS(O)Rᶜ, NRᶜS(O)₂Rᶜ, NRᶜS(O)₂NRᶜRᶜ, S(O)Rᶜ, S(O)NRᶜRᶜ, S(O)₂Rᶜ y S(O)₂NRᶜRᶜ; en donde cada alquilo C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄- de Rᵇ se sustituye opcionalmente con 1 - 3 sustituyentes de Rᵈ seleccionados independientemente; cada Rᶜ se selecciona independientemente de H, alquilo C₆₋₁₀, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄-, en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄- de Rᶜ se sustituye opcionalmente con 1, 2, 3, 4 ó 5 sustituyentes de Rᶠ seleccionados independientemente de alquilo C₁₋₄, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄-, (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄-, halo, CN, NHORᵍ, ORᵍ, SRᵍ, C(O)Rᵍ, C(O)NRᵍRᵍ, C(O)ORᵍ, OC(O)Rᵍ, OC(O)NRᵍRᵍ, NHRᵍ, NRᵍRᵍ, NRᵍC(O)Rᵍ, NRᵍC(O)NRᵍRᵍ, NRᵍC(O)ORᵍ, C(=NRᵍ)NRᵍRᵍ, NRᵍC(=NRᵍ)NRᵍRᵍ, S(O)Rᵍ, S(O)NRᵍRᵍ, S(O)₂Rᵍ, NRᵍS(O)₂Rᵍ, NRᵍS(O)₂NRᵍRᵍ y S(O)₂NRᵍRᵍ; en donde cada alquilo C₁₋₄, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄- de Rᶠ se sustituye opcionalmente con 1, 2, 3, 4 ó 5 sustituyentes de Rⁿ seleccionados independientemente de alquilo C₁₋₄, haloalquilo C₁₋₄, halo, CN, NHORᵒ, ORᵒ, SRᵒ, C(O)Rᵒ, C(O)NRᵒRᵒ, C(O)ORᵒ, OC(O)Rᵒ, OC(O)NRᵒRᵒ, NHRᵒ, NRᵒRᵒ, NRᵒC(O)Rᵒ, NRᵒC(O)NRᵒRᵒ, NRᵒC(O)ORᵒ, C(=NRᵒ)NRᵒRᵒ, NRᵒC(=NRᵒ)NRᵒRᵒ, S(O)Rᵒ, S(O)NRᵒRᵒ, S(O)₂Rᵒ, NRᵒS(O)₂Rᵒ, NRᵒS(O)₂NRᵒRᵒ y S(O)₂NRᵒRᵒ; cada Rᵍ se selecciona independientemente de H, alquilo C₁₋₆, haloalquilo C₁₋₄, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄-, en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, arilo C₆₋₁₀, cicloalquilo C₃₋₁₀, heteroarilo de 5 - 10 miembros, heterocicloalquilo de 4 - 10 miembros, arilo C₆₋₁₀-alquilo C₁₋₄-, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 10 miembros)-alquilo C₁₋₄- y (heterocicloalquilo de 4 - 10 miembros)-alquilo C₁₋₄- de Rᵍ se sustituye opcionalmente con 1 - 3 sustituyentes de Rᵖ seleccionados independientemente; o dos sustituyentes de Rᵃ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6, 7, 8, 9 ó 10 miembros sustituidos opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente de alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo de 4 - 7 miembros, arilo C₆₋₁₀, heteroarilo de 5 - 6 miembros, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 6 miembros)-alquilo C₁₋₄-, (heterocicloalquilo de 4 - 7 miembros)-alquilo C₁₋₄-, haloalquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, halo, CN, ORⁱ, SRⁱ, NHORⁱ, C(O)Rⁱ, C(O)NRⁱRⁱ, C(O)ORⁱ, OC(O)Rⁱ, OC(O)NRⁱRⁱ, NHRⁱ, NRⁱRⁱ, NRⁱC(O)Rⁱ, NRⁱC(O)NRⁱRⁱ, NRⁱC(O)ORⁱ, C(=NRⁱ)NRⁱRⁱ, NRⁱC(=NRⁱ)NRⁱRⁱ, S(O)Rⁱ, S(O)NRⁱRⁱ, S(O)₂Rⁱ, NRⁱS(O)₂Rⁱ, NRⁱS(O)₂NRⁱRⁱ y S(O)₂NRⁱRⁱ, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heterocicloalquilo de 4 - 7 miembros, arilo C₆₋₁₀, heteroarilo de 5 - 6 miembros, cicloalquilo C₃₋₁₀-alquilo C₁₋₄-, (heteroarilo de 5 - 6 miembros)-alquilo C₁₋₄-, (heterocicloalquilo de 4 - 7 miembros)-alquilo C₁₋₄- de Rʰ se sustituye, además, opcionalmente por 1, 2 ó 3 sustituyentes de Rʲ seleccionados independientemente de cicloalquilo de C₃₋₆, arilo C₆₋₁₀, heteroarilo de 5 ó 6 miembros, alquenilo C₂₋₄, alquinilo C₂₋₄, halo, alquilo C₁₋₄, haloalquilo C₁₋₄, CN, NHORᵏ, ORᵏ, SRᵏ, C(O)Rᵏ, C(O)NRᵏRᵏ, C(O)ORᵏ, OC(O)Rᵏ, OC(O)NRᵏRᵏ, NHRᵏ, NRᵏRᵏ, NRᵏC(O)Rᵏ, NRᵏC(O)NRᵏRᵏ, NRᵏC(O)ORᵏ, C(=NRᵏ)NRᵏRᵏ, NRᵏC(=NRᵏ)NRᵏRᵏ, S(O)Rᵏ, S(O)NRᵏRᵏ, S(O)₂Rᵏ, NRᵏS(O)₂Rᵏ, NRᵏS(O)₂NRᵏRᵏ y S(O)₂NRᵏRᵏ; o dos grupos Rʰ unidos al mismo átomo de carbono de heterocicloalquilo de 4 a 10 miembros tomados junto con el átomo de carbono al cual están unidos forman un cicloalquilo de C₃₋₆ o un heterocicloalquilo de 4 a 6 miembros que tienen 1 - 2 heteroátomos como miembros de anillo seleccionados de O, N o S; o dos sustituyentes de Rᶜ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros sustituido opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente; o dos sustituyentes de Rᵉ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros sustituido opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente; o dos sustituyentes de Rᵍ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros sustituido opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente; o dos sustituyentes de Rⁱ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros sustituido opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente; o dos sustituyentes de Rᵏ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros sustituido opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente; o dos sustituyentes de Rᵒ junto con el átomo de nitrógeno al cual están unidos forman un grupo heterocicloalquilo de 4, 5, 6 ó 7 miembros sustituido opcionalmente con 1, 2 ó 3 sustituyentes de Rʰ seleccionados independientemente; y cada Rᵉ, Rⁱ, Rᵏ, Rᵒ o Rᵖ se selecciona independientemente de H, alquilo C₁₋₄, cicloalquilo de C₃₋₆, arilo C₆₋₁₀, heteroarilo de 5 ó 6 miembros, haloalquilo C₁₋₄, alquenilo C₂₋₄ y alquinilo C₂₋₄, en donde cada alquilo C₁₋₄, cicloalquilo de C₃₋₆, arilo C₆₋₁₀, heteroarilo de 5 ó 6 miembros, alquenilo C₂₋₄ y alquinilo C₂₋₄ de Rᵉ, Rⁱ, Rᵏ, Rᵒ o Rᵖ se sustituye opcionalmente con 1, 2 ó 3 sustituyentes de Rq; cada Rq se selecciona independientemente de OH, CN, -COOH, NH₂, halo, haloalquilo C₁₋₆, alquilo C₁₋₆, alcoxi C₁₋₆, haloalcoxi C₁₋₆, alquiltio C₁₋₆, fenilo, heteroarilo de 5 - 6 miembros, heterocicloalquilo de 4 - 6 miembros, cicloalquilo de C₃₋₆, NHR¹², NR¹²R¹² y haloalcoxi C₁₋₄, en donde cada alquilo C₁₋₆, fenilo, cicloalquilo de C₃₋₆, heterocicloalquilo de 4 - 6 miembros y heteroarilo de 5 - 6 miembros de Rq se sustituye opcionalmente con halo, OH, CN, -COOH, NH₂, alcoxi C₁₋₄, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, fenilo, cicloalquilo C₃₋₁₀ y heterocicloalquilo de 4 - 6 miembros y cada R¹² es independientemente alquilo C₁₋₆; ⁻ ⁻ ⁻ ⁻ ⁻ es un enlace simple o un enlace doble para que el anillo A se mantenga como un anillo aromático; el subíndice n es un entero de 1, 2, 3, 4, 5 ó 6; y cuando R⁹ es OH, Cy es distinto de 6-carbamimidoil-1H-benzo[d]imidazol-2-ilo.
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