AR122090A1 - Moduladores de enpp1 y usos de los mismos - Google Patents

Moduladores de enpp1 y usos de los mismos

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Publication number
AR122090A1
AR122090A1 ARP210101325A ARP210101325A AR122090A1 AR 122090 A1 AR122090 A1 AR 122090A1 AR P210101325 A ARP210101325 A AR P210101325A AR P210101325 A ARP210101325 A AR P210101325A AR 122090 A1 AR122090 A1 AR 122090A1
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AR
Argentina
Prior art keywords
optionally substituted
halogen
alkyl
independently selected
carbocycle
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ARP210101325A
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English (en)
Inventor
Roland D Saito
Winston C Tse
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Vir Biotechnology Inc
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Publication of AR122090A1 publication Critical patent/AR122090A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—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
    • 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
    • C07D413/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Radar Systems Or Details Thereof (AREA)
  • Ultra Sonic Daignosis Equipment (AREA)

Abstract

Compuestos derivados de quinolina con actividad moduladora de ENPP1, composición farmacéutica que comprende a uno de éstos compuestos y el uso de los mismos para inhibir ENPP1 y activar la actividad de STING in vivo como así también para la activación de la respuesta inmunitaria contra un patógeno. Reivindicación 1: Un compuesto representado por la estructura de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, donde: X¹ se selecciona de N y C(R³); X² está ausente o se selecciona de O, S, C(R⁸)₂, N(R⁴) y C₃₋₆ carbociclo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de R⁹; X³ se selecciona N y C(R³’); Y se selecciona de N y C(H); R¹ se selecciona de: halógeno, -OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, y -CN; y C₁₋₅ alquilo, C₂₋₅ alquenilo, C₂₋₅ alquinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, =O, =S, =N(R¹¹), -CN, C₃₋₆ carbociclo y heterociclo de 3 a 6 miembros; R² se selecciona de: hidrógeno, halógeno, -OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, y -CN; y C₁₋₅ alquilo, C₂₋₅ alquenilo, C₂₋₅ alquinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, =O, =S, =N(R¹¹), -CN, C₃₋₆ carbociclo y heterociclo de 3 a 6 miembros; R³ se selecciona de: hidrógeno, halógeno, -OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, y -CN; y C₁₋₅ alquilo, C₂₋₅ alquenilo, C₂₋₅ alquinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, =O, =S, =N(R¹¹), -CN, C₃₋₆ carbociclo y heterociclo de 3 a 6 miembros; R³’ se selecciona de: hidrógeno, halógeno, -OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, y -CN; y C₁₋₅ alquilo, C₂₋₅ alquenilo, C₂₋₅ alquinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, OR¹¹, -SR¹¹, -N(R¹¹)₂, -C(O)R¹¹, -C(O)N(R¹¹)₂, -N(R¹¹)C(O)R¹¹, -C(O)OR¹¹, -OC(O)R¹¹, -S(O)R¹¹, -S(O)₂R¹¹, -S(O)₂N(R¹¹)₂, -N(R¹¹)S(O)₂R¹¹, -S(O)(NR¹¹)R¹¹, -S(NR¹¹)₂R¹¹, -NO₂, =O, =S, =N(R¹¹), -CN, C₃₋₆ carbociclo y heterociclo de 3 a 6 miembros; L está ausente o se selecciona de metileno opcionalmente sustituidos con uno o más sustituyentes seleccionados de halógeno, -OR²¹, -SR²¹, -N(R²¹)₂, -C(O)R²¹, -C(O)N(R²¹)₂, -N(R²¹)C(O)R²¹, -C(O)OR²¹, -OC(O)R²¹, -S(O)R²¹, -S(O)₂R²¹, -NO₂, y -CN; el anillo A se selecciona de un C₃₋₁₀ carbociclo opcionalmente sustituido y heterociclo de 3 a 10 miembros opcionalmente sustituido, en donde los sustituyentes en el anillo A se seleccionan independientemente en cada aparición de: halógeno, -OR³¹, -SR³¹, -N(R³¹)₂, -C(O)R³¹, -C(O)N(R³¹)₂, -N(R³¹)C(O)R³¹, -C(O)OR³¹, -OC(O)R³¹, -S(O)R³¹, -S(O)₂R³¹, -NO₂, =O, -CN, y C₁₋₅ haloalquilo; y C₁₋₅ alquilo C₂₋₅ alquenilo, C₂₋₅ alquinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR³¹, -SR³¹, -N(R³¹)₂, -C(O)R³¹, -C(O)N(R³¹)₂, -N(R³¹)C(O)R³¹, -C(O)OR³¹, -OC(O)R³¹, -S(O)R³¹, -S(O)₂R³¹, -NO₂, =O, y -CN; R⁴ se selecciona de hidrógeno, C₁₋₅ alquilo y C₃₋₆ carbociclo, en donde C₁₋₅ alquilo y C₃₋₆ carbociclo están sustituidos opcionalmente con uno o más sustituyentes seleccionados independientemente de R⁹; R⁵, R⁶ y R⁷ se seleccionan cada uno independientemente de hidrógeno, C₁₋₆ alquilo opcionalmente sustituido, C₃₋₁₂ carbociclo opcionalmente sustituido y heterociclo de 3 a 12 miembros opcionalmente sustituido; o R⁵ y R⁶ se unen para formar un heterociclo opcionalmente sustituido de 5 a 8 miembros, y R⁷ se selecciona de hidrógeno, C₁₋₆ alquilo opcionalmente sustituido, C₃₋₁₂ carbociclo opcionalmente sustituido y heterociclo de 3 a 12 miembros opcionalmente sustituido; o R⁶ y R⁷ se unen para formar un heterociclo de 5 a 8 miembros opcionalmente sustituido, y R⁵ se selecciona de hidrógeno, C₁₋₆ alquilo opcionalmente sustituido, C₃₋₁₂ carbociclo opcionalmente sustituido y heterociclo de 3 a 12 miembros opcionalmente sustituido; en donde los sustituyentes en R⁵, R⁶ y R⁷ o anillos formados a partir de estos se seleccionan independientemente en cada aparición de: halógeno, -OR⁴¹, -SR⁴¹, -N(R⁴¹)₂, -C(O)R⁴¹,-C(O)N(R⁴¹)₂, -N(R⁴¹)C(O)R⁴¹, -N(R⁴¹)C(O)OR⁴¹, -C(O)OR⁴¹, -OC(O)R⁴¹, -S(O)R⁴¹, -S(O)₂R⁴¹, -S(O)₂N(R₄₁)₂, -N(R⁴¹)S(O)₂R⁴¹, -S(O)(NR⁴¹)R⁴¹, -S(NR⁴¹)₂R⁴¹, -NO₂, =O, =S, =N(R⁴¹), y -CN; y C₁₋₅ alquilo, C₂₋₅ alquenilo, C₂₋₅ alquinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR⁴¹, -SR⁴¹, -N(R⁴¹)₂, -C(O)R⁴¹, -C(O)N(R⁴¹)₂, -N(R⁴¹)C(O)R⁴¹, -N(R⁴¹)C(O)OR⁴¹, -C(O)OR⁴¹, -OC(O)R⁴¹, -S(O)R⁴¹, -S(O)₂R⁴¹, -S(O)₂N(R⁴¹)₂, -N(R⁴¹)S(O)₂R⁴¹, -S(O)(NR⁴¹)R⁴¹, -S(NR⁴¹)₂R⁴¹, -NO₂, =O, =S, =N(R⁴¹), -CN, C₃₋₁₂ carbociclo y heterociclo de 3 a 12 miembros; C₃₋₁₂ carbociclo y heterociclo de 3 a 12 miembros cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR⁴¹, -SR⁴¹, -N(R⁴¹)₂, -C(O)R⁴¹, -C(O)N(R⁴¹)₂, -N(R⁴¹)C(O)R⁴¹, -N(R⁴¹)C(O)OR⁴¹, -C(O)OR⁴¹, -OC(O)R⁴¹, -S(O)R⁴¹, -S(O)₂R⁴¹, -S(O)₂N(R⁴¹)₂, -N(R⁴¹)S(O)₂R⁴¹, -S(O)(NR⁴¹)R⁴¹, -S(NR⁴¹)₂R⁴¹, -NO₂, =O, =S, =N(R⁴¹), -CN, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₃₋₁₂ carbociclo y heterociclo de 3 a 12 miembros; cada R⁸ se selecciona independientemente de: hidrógeno, halógeno, -OR⁵¹, -SR⁵¹, -N(R⁵¹)₂, -NO₂ y -CN; y C₁₋₅ alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR⁵¹, -SR⁵¹, -N(R⁵¹)₂, -NO₂ y -CN; cada R⁹ se selecciona independientemente de: halógeno, -OR⁶¹, -SR⁶¹, -N(R⁶¹)₂, -NO₂ y -CN; y C₁₋₅ alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OR⁶¹, -SR⁶¹, -N(R⁶¹)₂, -NO₂ y -CN; cada R¹¹, R²¹, R³¹, R⁴¹, R⁵¹ y R⁶¹ se selecciona independientemente de: hidrógeno; y C₁₋₅ alquilo, C₂₋₅ alquenilo, C₂₋₅ alquinilo, C₃₋₈ carbociclo y 3 a 8 miembros heterociclo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente de halógeno, -OH, -CN, -NO₂, -NH₂, =O, =S, C₁₋₅ alquilo, -C₁₋₅ haloalquilo y -O-C₁₋₅ alquilo; y z se selecciona de 0 - 3.
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