AR088630A1 - Inhibidores del virus de la hepatitis c - Google Patents

Inhibidores del virus de la hepatitis c

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Publication number
AR088630A1
AR088630A1 ARP120104114A ARP120104114A AR088630A1 AR 088630 A1 AR088630 A1 AR 088630A1 AR P120104114 A ARP120104114 A AR P120104114A AR P120104114 A ARP120104114 A AR P120104114A AR 088630 A1 AR088630 A1 AR 088630A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
hydrogen
orh
heterocycle
Prior art date
Application number
ARP120104114A
Other languages
English (en)
Inventor
Zhang Weijiang
ogawa Gavin
D Long Daniel
Huang Xiaojun
Lepack Kassandra
Loo Mandy
Murray Mkinnell Robert
Jean Van Orden Lori
Jiang Lan
Original Assignee
Theravance 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 Theravance Inc filed Critical Theravance Inc
Publication of AR088630A1 publication Critical patent/AR088630A1/es

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Classifications

    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/14Heterocyclic 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
    • 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde R¹ se selecciona entre alquilo C₁₋₆, alcoxi C₁₋₆, fenilo, cicloalquilo C₃₋₆, heterociclo, y heteroarilo, donde alquilo C₁₋₆ está opcionalmente sustituido con -ORᵃ, amino, -SRᵉ, heterociclo, o heteroarilo, alcoxi C₁₋₆ está opcionalmente sustituido con -ORᵃ, y heterociclo está opcionalmente sustituido con -ORᵃ, amino, o -C(O)O-alquilo C₁₋₆, o con uno o dos alquilo C₁₋₃ o =O; R² se selecciona entre hidrógeno y alquilo C₁₋₆; R³ se selecciona entre hidrógeno, alquilo C₁₋₆, -C(O)O-alquilo C₁₋₆, -C(O)NRᵐRⁿ, -C(O)cicloalquilo C₃₋₆, y -S(O)₂alquilo C₁₋₃; o R² y R³ junto con el átomo de nitrógeno al cual están unidos forman un heterociclo; R⁴ se selecciona entre alquilo C₁₋₆, -NRᵇRᶜ, -ORᵈ, -SRᵉ, -S(O)alquilo C₁₋₃, -S(O)₂alquilo C₁₋₃, -CN, C(O)NRᵃRᵇ, heterociclo, heteroarilo, y halo, donde alquilo C₁₋₆ está opcionalmente sustituido con -ORᵃ; y R⁵ y R⁶ son hidrógeno; o R⁴ y R⁵ son en forma independiente alquilo C₁₋₆ o halo y R⁶ es hidrógeno; o R⁴ y R⁵ tomados juntos forman -(CH₂)ₙ-, donde n es 2, 3, 4, ó 5; y R⁶ es hidrógeno; o R⁴ y R⁵ tomados juntos forman -O-(CH₂)₂-O- y R⁶ es hidrógeno; o R⁴ es hidrógeno y R⁵ y R⁶ tomados juntos forman -(CH₂)ₘ-, donde m es 1, 2, 3, ó 4; o R⁴ y R⁵ son cada uno hidrógeno y R⁶ es alquilo C₁₋₆; R⁷ se selecciona entre halo, alquilo C₁₋₃, y alcoxi C₁₋₃ donde alquilo C₁₋₃ y alcoxi C₁₋₃ están opcionalmente sustituidos con uno, dos, tres, cuatro, o cinco halo; R⁸ es alquilo C₁₋₃, opcionalmente sustituido con -ORʰ; R⁹ se selecciona entre alquilo C₁₋₆, cicloalquilo C₃₋₆, alcoxi C₁₋₆, -NRᶠRᵍ, heteroarilo, heterociclo, y -CH₂-heteroarilo; donde: alquilo C₁₋₆ está opcionalmente sustituido con uno o dos sustituyentes seleccionados en forma independiente entre -ORʰ, -NRʲRᵏ, -NHC(O)alquilo C₁₋₃, -NHC(O)O-alquilo C₁₋₃, -NHC(O)cicloalquilo C₃₋₆, cicloalquilo C₃₋₆, halo, -NHC(O)alquilo C₁₋₃(O)ORʰ, -NHC(O)alquilo C₁₋₃Rʰ, -NHC(O)NH-alquilo C₁₋₃, -NHS(O)₂alquilo C₁₋₃, y heterociclo; alcoxi C₁₋₆ está opcionalmente sustituido con -ORʰ; cualquier cicloalquilo C₃₋₆ está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados en forma independiente entre alquilo C₁₋₃, halo, NRᵃRᵇ, -ORʰ, y -CD₃, donde cualquier alquilo C₁₋₃ está opcionalmente sustituido con uno, dos o tres halo; cualquier heterociclo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados en forma independiente entre alquilo C₁₋₃, halo, -C(O)O-alquilo C₁₋₃, -C(O)alquilo C₁₋₆, -C(O)cicloalquilo C₃₋₆, -C(O)NH-alquilo C₁₋₆, -C(O)NH-cicloalquilo C₃₋₆, -S(O)₂alquilo C₁₋₆, y -C(O)NH₂; donde cualquier -C(O)alquilo C₁₋₆ está opcionalmente sustituido con -NHC(O)O-alquilo C₁₋₃, -ORʰ, -NRʲRᵏ, o heterociclo, cualquier -C(O)cicloalquilo C₃₋₆ está opcionalmente sustituido con uno o dos alquilo C₁₋₃, y cualquier -C(O)NH-alquilo C₁₋₆ está opcionalmente sustituido con -ORʰ o cicloalquilo C₃₋₆; cualquier heteroarilo está opcionalmente sustituido con uno o dos alquilo C₁₋₃; Rᵃ, Rᵇ, Rᵉ, Rʰ, Rʲ, Rᵏ, Rᵐ, y Rⁿ son en forma independiente entre sí hidrógeno o alquilo C₁₋₃; Rᶜ es hidrógeno o alquilo C₁₋₆, donde alquilo C₁₋₆ está opcionalmente sustituido con -ORᵃ o amino; Rᵈ es hidrógeno o alquilo C₁₋₆, donde alquilo C₁₋₆ está opcionalmente sustituido con -ORʰ o con heteroarilo opcionalmente sustituido con alquilo C₁₋₃; Rᶠ es hidrógeno o alquilo C₁₋₆, donde alquilo C₁₋₆ está opcionalmente sustituido con -ORʰ; Rᵍ se selecciona entre hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, cicloalquilo C₃₋₆, NRᵃRᵇ, y heterociclo, donde alquilo C₁₋₆ está opcionalmente sustituido con -ORʰ y heterociclo está opcionalmente sustituido con uno o dos =O; R¹⁰ se selecciona entre hidrógeno, halo, y alquilo C₁₋₃, donde alquilo C₁₋₃ está opcionalmente sustituido con uno, dos o tres halo, o con -ORʰ; Aₘ es -NHC(O)- ó -C(O)NH-; a es 0, 1 ó 2; y b es 0, 1 ó 2; o una sal o estereoisómero farmacéuticamente aceptable del mismo.
ARP120104114A 2011-11-03 2012-11-02 Inhibidores del virus de la hepatitis c AR088630A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555056P 2011-11-03 2011-11-03
US201261600089P 2012-02-17 2012-02-17
US201261637961P 2012-04-25 2012-04-25

Publications (1)

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AR088630A1 true AR088630A1 (es) 2014-06-25

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Country Status (19)

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US (2) US9212168B2 (es)
EP (1) EP2773634B1 (es)
JP (2) JP6082747B2 (es)
KR (1) KR20140091036A (es)
CN (1) CN103946220B (es)
AR (1) AR088630A1 (es)
AU (1) AU2012332358B2 (es)
BR (1) BR112014010401A8 (es)
CA (1) CA2852700A1 (es)
CL (1) CL2014001110A1 (es)
CO (1) CO6940424A2 (es)
HK (1) HK1200812A1 (es)
IL (1) IL232042A (es)
MX (1) MX347692B (es)
RU (1) RU2625787C2 (es)
SG (1) SG11201401891RA (es)
TW (1) TWI577672B (es)
WO (1) WO2013067267A1 (es)
ZA (1) ZA201403198B (es)

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AU2012332358A1 (en) 2014-05-29
EP2773634A1 (en) 2014-09-10
IL232042A0 (en) 2014-05-28
RU2014122340A (ru) 2015-12-10
CN103946220B (zh) 2017-12-22
IL232042A (en) 2017-07-31
NZ623846A (en) 2016-07-29
JP6082747B2 (ja) 2017-02-15
MX2014005342A (es) 2014-08-08
TW201326156A (zh) 2013-07-01
RU2625787C2 (ru) 2017-07-19
CN103946220A (zh) 2014-07-23
ZA201403198B (en) 2017-04-26
WO2013067267A1 (en) 2013-05-10
HK1200812A1 (en) 2015-08-14
BR112014010401A8 (pt) 2017-12-19
JP2014532716A (ja) 2014-12-08
MX347692B (es) 2017-05-09
TWI577672B (zh) 2017-04-11
SG11201401891RA (en) 2014-05-29
AU2012332358B2 (en) 2017-07-13
US9669027B2 (en) 2017-06-06
EP2773634B1 (en) 2018-06-06
CL2014001110A1 (es) 2014-08-22
US9212168B2 (en) 2015-12-15
BR112014010401A2 (pt) 2017-04-25
JP2017048248A (ja) 2017-03-09
CA2852700A1 (en) 2013-05-10
CO6940424A2 (es) 2014-05-09
US20160038483A1 (en) 2016-02-11
US20130115194A1 (en) 2013-05-09
KR20140091036A (ko) 2014-07-18

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