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

Moduladores de enpp1 y usos de los mismos

Info

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
Authority
AR
Argentina
Prior art keywords
optionally substituted
halogen
alkyl
independently selected
carbocycle
Prior art date
Application number
ARP210101325A
Other languages
English (en)
Inventor
Roland D Saito
Winston C Tse
Original Assignee
Vir Biotechnology Inc
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 Vir Biotechnology Inc filed Critical Vir Biotechnology Inc
Publication of AR122090A1 publication Critical patent/AR122090A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/47064-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/44Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • 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.
ARP210101325A 2020-05-14 2021-05-13 Moduladores de enpp1 y usos de los mismos AR122090A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202063024937P 2020-05-14 2020-05-14

Publications (1)

Publication Number Publication Date
AR122090A1 true AR122090A1 (es) 2022-08-10

Family

ID=76250495

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP210101325A AR122090A1 (es) 2020-05-14 2021-05-13 Moduladores de enpp1 y usos de los mismos

Country Status (13)

Country Link
US (1) US20230183188A1 (es)
EP (1) EP4149927A1 (es)
JP (1) JP2023526050A (es)
KR (1) KR20230012535A (es)
CN (1) CN116348451A (es)
AR (1) AR122090A1 (es)
AU (1) AU2021273001A1 (es)
BR (1) BR112022023112A2 (es)
CA (1) CA3178372A1 (es)
IL (1) IL298169A (es)
MX (1) MX2022014126A (es)
TW (1) TW202208336A (es)
WO (1) WO2021231726A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023086638A1 (en) * 2021-11-15 2023-05-19 Vir Biotechnology, Inc. Enpp1 modulators and uses thereof
WO2023220402A1 (en) * 2022-05-13 2023-11-16 Gossamer Bio Services, Inc. Enpp1 modulators and products and uses thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
KR20040068613A (ko) 1994-03-25 2004-07-31 이소테크니카 인코포레이티드 중수소화된 화합물 이를 포함하는 고혈압 치료용 조성물
KR20190126283A (ko) * 2016-12-22 2019-11-11 마브파마, 인크. 포스포디에스테라아제 저해제 및 미생물 치료 방법
AU2020353005A1 (en) * 2019-09-23 2022-04-14 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use

Also Published As

Publication number Publication date
BR112022023112A2 (pt) 2023-01-17
CN116348451A (zh) 2023-06-27
WO2021231726A1 (en) 2021-11-18
US20230183188A1 (en) 2023-06-15
EP4149927A1 (en) 2023-03-22
MX2022014126A (es) 2023-04-10
KR20230012535A (ko) 2023-01-26
TW202208336A (zh) 2022-03-01
JP2023526050A (ja) 2023-06-20
IL298169A (en) 2023-01-01
CA3178372A1 (en) 2021-11-18
AU2021273001A1 (en) 2022-12-15

Similar Documents

Publication Publication Date Title
AR122090A1 (es) Moduladores de enpp1 y usos de los mismos
AR114793A1 (es) Moduladores de enzimas modificadoras de metilo, composiciones y usos de los mismos
AR119770A1 (es) Proceso de elaboración de moduladores de cftr
AR111407A1 (es) Compuestos inhibidores de ask1 y usos de los mismos
AR114254A1 (es) Moduladores del regulador de conductancia transmembrana de fibrosis quística, composiciones farmacéuticas, métodos de tratamiento y proceso de preparación de los moduladores
AR129635A2 (es) Moduladores de tetrahidropiridopirazina de gpr6
AR117617A1 (es) Compuestos de sulfonilurea como inhibidores de la actividad de interleuquina 1
AR090945A1 (es) Moduladores de la via del complemento y usos de los mismos
AR088565A1 (es) Inhibidor de cetp de oxazolidinona biciclico fusionado
AR108709A1 (es) Compuestos moduladores de fxr (nr1h4)
AR114044A1 (es) Composiciones y métodos para el tratamiento de trastornos en el sistema nervioso central
AR114236A1 (es) Inhibidores de la gcn2 y usos de los mismos
AR088175A1 (es) 3-pirimidin-4-il-oxazolidin-2-onas utiles para tratar cancer y composiciones farmaceuticas que las contienen
AR117616A1 (es) Compuestos anti-vih
AR099890A1 (es) Inhibidores de histona demetilasas
AR094790A1 (es) Derivados sustituidos del ácido bisfenil butanóico fosfónico como inhibidores de la nep
AR120773A1 (es) Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona como reductor de la actividad de la proteína wiz
AR111248A1 (es) Derivados de ciclopropilmetilamida activos como pesticida
AR094497A1 (es) Compuestos tetracíclicos sustituidos con tiofeno y métodos de uso de los mismos para el tratamiento de enfermedades víricas
AR112794A1 (es) Compuestos heteroaromáticos sustituidos con cicloolefinas y su uso en el tratamiento de enfermedades inducidas por mutaciones idh
AR120377A1 (es) Derivados heteroaromáticos de sulfiliminas o sulfoximinas con actividad fungicida
AR104533A1 (es) Derivados de ácido ciclopropano carboxílico y sus usos como inhibidores de leucotrieno c₄ sintasa
AR096827A1 (es) Uso de piridoncarboxamidas seleccionadas o sus sales como ingredientes activos contra estrés abiótico en plantas
AR111282A1 (es) Inhibidores de cdpk1 ii, composiciones y métodos relacionados con los mismos
AR105060A1 (es) Concentrado emulsionable que comprende un herbicida de ácido fenoxi-alcanoico