AR082628A1 - Compuestos heterociclicos antivirales - Google Patents

Compuestos heterociclicos antivirales

Info

Publication number
AR082628A1
AR082628A1 ARP110102919A ARP110102919A AR082628A1 AR 082628 A1 AR082628 A1 AR 082628A1 AR P110102919 A ARP110102919 A AR P110102919A AR P110102919 A ARP110102919 A AR P110102919A AR 082628 A1 AR082628 A1 AR 082628A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
independently
hydrogen
Prior art date
Application number
ARP110102919A
Other languages
English (en)
Inventor
Francisco Xavier Talamas
Jim Li
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR082628A1 publication Critical patent/AR082628A1/es

Links

Classifications

    • 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
    • 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
    • C07D401/10—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 carbon chain containing aromatic 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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Inhibidores de la polimerasa NS5b del virus de la hepatitis C. Se describen también composiciones y métodos para tratar una infección del HCV e inhibir la replicación del HCV.Reivindicación 1: Un compuesto de la fórmula (1), en la que: R1 es 2-oxo-1,2-dihidro-piridin-3-ilo opcionalmente sustituido por halógeno, alquilo C1-6, haloalquilo C1-3, alcoxi C1-6 o hidroxi; o 2,4-dioxo-tetrahidro-pirimidin-1-ilo, 2,4-dioxo-3,4-dihidro-2H-pirimidin-1-ilo o 2,4-dioxo-1,2,3,4-tetrahidro-pirimidin-5-ilo; R2 es (a) arilo, (b) heteroarilo o (c) NRaRb, dichos arilo o heteroarilo están opcionalmente sustituidos con independencia entre sí de una a tres veces por sustituyentes elegidos entre el grupo formado por hidroxi, alcoxi C1-6, alquilo C1-6, hidroxialquilo C1-6, halógeno, (CH2)nNRcRd, ciano, alcoxi C1-6-carbonilo, carbamoilo, N-alquil-carbamoilo, N,N-dialquil-carbamoilo, (CH2)0-2CO2H, SO2NH2, alquilsulfinilo C1-6 y alquilsulfonilo C1-6; Ra y Rb junto con el nitrógeno al que están unidos forman una amina cíclica sustituida con independencia por (CH2)nNRcRd, en el que n es un número de cero a dos, y además está opcionalmente sustituida por uno o dos grupos elegidos con independencia entre alquilo C1-6 y halógeno; Rc y Rd son con independencia hidrógeno, alquilo C1-6, haloalquilo C1-6, acilo C1-6, O2SR4, en el que R4 es alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-3, alcoxi C1-6-alquilo C1-6, -SO-NReRf; Re y Rf son (i) con independencia hidrógeno, alquilo C1-3 o (CH2)2-6NRgRh o (ii) junto con el átomo de nitrógeno al que están unidos son (CH2)2X5(CH2)2, en el que X5 es O ó NRg y Rg es hidrógeno, alquilo C1-3, acilo C1-3 o alquilsulfonilo C1-3; R3 es CF3, CH2CF3, cicloalquilo C3-5, halógeno, alcoxi C1-6, haloalcoxi C1-3, CHR3aR3b o CR3aR3bR3c, en los que: (i) R3a, R3b y R3c se eligen con independencia entre alquilo C1-3, CD3, alcoxi C1-2, fluoroalquilo C1-2, hidroxialquilo C1-3, ciano e hidroxi; o (ii) tomados juntos, R3a y R3b juntos son alquileno C2-4 y R3c es hidrógeno, alquilo C1-3, CD3, alcoxi C1-2, halógeno, hidroxialquilo C1-3, ciano o fluoroalquilo C1-2, o R3a y R3b junto con el átomo de carbono al que están unidos son 3-oxetanilo o tetrahidrofuran-2-ilo.
ARP110102919A 2010-08-13 2011-08-11 Compuestos heterociclicos antivirales AR082628A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37343410P 2010-08-13 2010-08-13

Publications (1)

Publication Number Publication Date
AR082628A1 true AR082628A1 (es) 2012-12-19

Family

ID=44503829

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102919A AR082628A1 (es) 2010-08-13 2011-08-11 Compuestos heterociclicos antivirales

Country Status (14)

Country Link
US (1) US8734777B2 (es)
EP (1) EP2603501B1 (es)
JP (1) JP5617036B2 (es)
KR (1) KR101382730B1 (es)
CN (1) CN103068819B (es)
AR (1) AR082628A1 (es)
BR (1) BR112013003113A2 (es)
CA (1) CA2806547A1 (es)
ES (1) ES2477342T3 (es)
HK (1) HK1184452A1 (es)
MX (1) MX2013001273A (es)
RU (1) RU2572835C2 (es)
TW (1) TW201210598A (es)
WO (1) WO2012020037A1 (es)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0489480A1 (en) * 1990-12-05 1992-06-10 Nissan Chemical Industries Ltd. Uracil derivatives and herbicides containing the same as active ingredient
GB0201179D0 (en) * 2002-01-18 2002-03-06 Angeletti P Ist Richerche Bio Therapeutic agents
WO2009039127A1 (en) 2007-09-17 2009-03-26 Abbott Laboratories Uracil or thymine derivative for treating hepatitis c
WO2010100178A1 (en) * 2009-03-06 2010-09-10 F. Hoffmann-La Roche Ag Heterocyclic antiviral compounds
JP5571167B2 (ja) * 2009-03-25 2014-08-13 アッヴィ・インコーポレイテッド 抗ウイルス組成物およびこの使用
CA2986195A1 (en) * 2009-03-25 2010-09-30 Abbvie Inc. Substituted aryl antivrial compounds and uses thereof
TWI428332B (zh) * 2009-06-09 2014-03-01 Hoffmann La Roche 雜環抗病毒化合物
CA2801670A1 (en) * 2010-07-07 2012-01-12 Leanna Renee Staben Heterocyclic antiviral compounds

Also Published As

Publication number Publication date
RU2572835C2 (ru) 2016-01-20
BR112013003113A2 (pt) 2019-09-24
KR20130069763A (ko) 2013-06-26
US20130209397A1 (en) 2013-08-15
KR101382730B1 (ko) 2014-04-08
RU2013108055A (ru) 2014-09-20
TW201210598A (en) 2012-03-16
CN103068819A (zh) 2013-04-24
CA2806547A1 (en) 2012-02-16
JP5617036B2 (ja) 2014-10-29
HK1184452A1 (en) 2014-01-24
CN103068819B (zh) 2014-08-13
ES2477342T3 (es) 2014-07-16
WO2012020037A1 (en) 2012-02-16
JP2013537537A (ja) 2013-10-03
EP2603501B1 (en) 2014-05-14
MX2013001273A (es) 2013-04-10
EP2603501A1 (en) 2013-06-19
US8734777B2 (en) 2014-05-27

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