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AR116474A1 - DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV - Google Patents

DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV

Info

Publication number
AR116474A1
AR116474A1 ARP190102685A ARP190102685A AR116474A1 AR 116474 A1 AR116474 A1 AR 116474A1 AR P190102685 A ARP190102685 A AR P190102685A AR P190102685 A ARP190102685 A AR P190102685A AR 116474 A1 AR116474 A1 AR 116474A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alternatively
taken together
double bonds
ring containing
Prior art date
Application number
ARP190102685A
Other languages
English (en)
Inventor
Joseph Panarese
Yat Sun Or
Katherine Chong
Dexter Davis
Samuel Bartlett
Original Assignee
Enanta Pharm 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 Enanta Pharm Inc filed Critical Enanta Pharm Inc
Publication of AR116474A1 publication Critical patent/AR116474A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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 three hetero rings
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos derivados del ácido 6,7-dihidro-2H-benzofuro[2,3-a]quinolizin-3-carboxílico como agentes antivirales para el tratamiento o prevención de una infección con el virus de la hepatitis B (HBV), utilizando los mismos en terapias combinadas con otros agentes con actividad antiviral. Se provee además una composición farmacéutica que comprende éstos compuestos. Reivindicación 1: Un compuesto representado por la fórmula (1), o una sal de uso farmacéutico aceptable del mismo, donde: Z¹ es O, NR¹ o S; Z² es N o CR²; Z³ es N o CR³; Z⁴ es N o CR⁴, Z⁵ es N o CR⁵; R¹ es hidrógeno, alquilo C₁₋₈ opcionalmente sustituido, alquenilo C₂₋₈ opcionalmente sustituido, cicloalquilo C₃₋₈ opcionalmente sustituido, heterocicloalquilo de 3- a 8- miembros opcionalmente sustituido, arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R², R³, R⁴ y R⁵ se seleccionan independientemente: 1) hidrógeno; 2) halógeno; 3) -NO₂; 4) ciano; 5) alquilo C₁₋₈ opcionalmente sustituido; 6) alquenilo C₂₋₈ opcionalmente sustituido; 7) alquinilo C₂₋₈ opcionalmente sustituido; 8) cicloalquilo C₃₋₈ opcionalmente sustituido; 9) heterocicloalquilo de 3- a 8- miembros opcionalmente sustituido; 10) arilo opcionalmente sustituido; 11) arilalquilo opcionalmente sustituido; 12) heteroarilo opcionalmente sustituido; 13) heteroarilalquilo opcionalmente sustituido; 14) -SR¹¹; 15) -S(O)₂R¹¹; 16) -S(O)₂N(R¹¹)(R¹²); 17) -C(O)R¹¹; 18) -C(O)OR¹¹; 19) -C(O)N(R¹¹)(R¹²); 20) -C(O)N(R¹¹)S(O)₂(R¹²); 21) -N(R¹¹)(R¹²); 22) -N(R¹³)C(O)N(R¹¹)(R¹²); 23) -N(R¹¹)C(O)(R¹²); 24) -N(R¹¹)C(O)₂(R¹²); 25) -N(R¹³)S(O)₂N(R¹¹)(R¹²); 26) -N(R¹¹)S(O)₂(R¹²); 27) -OR¹¹; 28) -OC(O)R¹¹; 29) -OC(O)OR¹¹; y 30) -OC(O)N(R¹¹)(R¹²); donde R¹¹, R¹² y R¹³ es cada uno independientemente seleccionado de hidrógeno, alquilo C₁₋₈ opcionalmente substituido, alquenilo C₂₋₈ opcionalmente substituido, cicloalquilo C₃₋₈ opcionalmente substituido, heterocicloalquilo de 3- a 8- miembros opcionalmente substituido, arilo opcionalmente substituido y heteroarilo opcionalmente sustituido; alternativamente, R¹¹ y R¹² están tomados junto con el átomo de nitrógeno al cual están unidos para formar un anillo heterocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 dobles enlaces; alternativamente, Z² es CR², Z³ es CR³, y R² y R³ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Z³ es CR³, Z⁴ es CR⁴, y R³ y R⁴ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Z⁴ es CR⁴, Z⁵ es CR⁵, y R⁴ y R⁵ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; Q¹, Q², Q³, y Q⁴ son cada uno independientemente seleccionado de hidrógeno, halo, NR¹¹, alquilo C₁₋₆ opcionalmente sustituido, alcoxi C₁₋₆ opcionalmente sustituido, cicloalquilo C₃₋₈ opcionalmente sustituido; heterocicloalquilo de 3- a 8- miembros opcionalmente sustituido; arilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; alternativamente, Q¹ se toma junto con Q² o Q³ para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Q² se toma junto con Q⁴ para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; alternativamente, Q³ y Q⁴ se toman juntos para formar un anillo heterocíclico o carbocíclico de 3 - 8 miembros opcionalmente sustituido que contiene 0, 1, 2 ó 3 enlaces dobles; Y¹ es hidrógeno, halo, o alquilo C₁₋₆ opcionalmente sustituido; Y² es O, NR¹¹, N(OR¹¹), o N(NR¹¹); Y³ es -COOR¹¹, -C(O)NHSO₂R¹¹, -C(O)NHSO₂NR¹¹R¹², 5-tetrazolilo o 1,2,4-oxadiazol-3-il-5(4H)-ona; e Y⁴ es hidrógeno o metilo opcionalmente sustituido; alternativamente, Y² e Y³ se toman juntos para formar un anillo heterocíclico de 5 - 12 miembros opcionalmente sustituido que contiene 1, 2 ó 3 enlaces dobles.
ARP190102685A 2018-09-21 2019-09-20 DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV AR116474A1 (es)

Applications Claiming Priority (1)

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US201862734424P 2018-09-21 2018-09-21

Publications (1)

Publication Number Publication Date
AR116474A1 true AR116474A1 (es) 2021-05-12

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ARP190102685A AR116474A1 (es) 2018-09-21 2019-09-20 DERIVADOS DEL ÁCIDO 6,7-DIHIDRO-2H-BENZOFURO[2,3-a]QUINOLIZIN-3-CARBOXÍLICO COMO AGENTES ANTIVIRALES PARA EL TRATAMIENTO O PREVENCIÓN DE UNA INFECCIÓN POR HBV

Country Status (14)

Country Link
US (2) US10865211B2 (es)
EP (1) EP3852751A4 (es)
JP (1) JP2022500466A (es)
KR (1) KR20210065965A (es)
CN (1) CN112955142A (es)
AR (1) AR116474A1 (es)
AU (1) AU2019342750A1 (es)
BR (1) BR112021005091A2 (es)
CA (1) CA3113235A1 (es)
IL (1) IL281564A (es)
MX (1) MX2021003253A (es)
TW (1) TW202024093A (es)
UY (1) UY38383A (es)
WO (1) WO2020061435A1 (es)

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