AR099345A2 - MACROCYCLIC INHIBITORS OF THE HEPATITIS C VIRUS, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USE OF THE SAME AND PROCESS TO PREPARE THEM - Google Patents

MACROCYCLIC INHIBITORS OF THE HEPATITIS C VIRUS, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USE OF THE SAME AND PROCESS TO PREPARE THEM

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Publication number
AR099345A2
AR099345A2 ARP140101796A ARP140101796A AR099345A2 AR 099345 A2 AR099345 A2 AR 099345A2 AR P140101796 A ARP140101796 A AR P140101796A AR P140101796 A ARP140101796 A AR P140101796A AR 099345 A2 AR099345 A2 AR 099345A2
Authority
AR
Argentina
Prior art keywords
alkyl
het
optionally substituted
cycloalkyl
alkoxy
Prior art date
Application number
ARP140101796A
Other languages
Spanish (es)
Original Assignee
Janssen Sciences Ireland Uc
Medivir Ab
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 Janssen Sciences Ireland Uc, Medivir Ab filed Critical Janssen Sciences Ireland Uc
Publication of AR099345A2 publication Critical patent/AR099345A2/en

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Classifications

    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones farmacéuticas que contienen compuestos de fórmula (1) y procesos para preparar compuestos de fórmula (1). También se proporcionan combinaciones biodisponibles de los inhibidores del VHC de fórmula (1) con ritonavir. Reivindicación 1: Un compuesto que posee la fórmula (1) o una sal del mismo, en donde cada línea punteada (representada por - - - - -) representa un doble enlace opcional; X es N, CH y cuando X posee un doble enlace es C; R¹ es -OR⁷, -NH-SO₂R⁸; R² es hidrógeno y cuando X es C o CH, R² también puede ser alquilo C₁₋₆; R³ es hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, cicloalquilo C₃₋₇; R⁴ es arilo o Het; n es 3, 4, 5 ó 6; R⁵ representa halo, alquilo C₁₋₆, hidroxi, alcoxi C₁₋₆, polihaloalquilo C₁₋₆, fenilo o Het; R⁶ representa alcoxi C₁₋₆ o dimetilamino; R⁷ es hidrógeno; arilo; Het; cicloalquilo C₃₋₇; sustituido opcionalmente con alquilo C₁₋₆; o alquilo C₁₋₆ sustituido opcionalmente con cicloalquilo C₃₋₇, arilo o con Het; R⁸ es arilo; Het; cicloalquilo C₃₋₇ sustituido opcionalmente con alquilo C₁₋₆; o alquilo C₁₋₆ sustituido opcionalmente con cicloalquilo C₃₋₇, arilo o con Het; arilo como grupo o parte de un grupo es fenilo sustituido opcionalmente con uno, dos o tres sustituyentes seleccionados de halo, hidroxi, nitro, ciano, carboxilo, alquilo C₁₋₆, alcoxi C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, alquilcarbonilo C₁₋₆, amino, mono- o di-alquilamino C₁₋₆, azido, mercapto, polihaloalquilo C₁₋₆, polihaloalcoxi C₁₋₆, cicloalquilo C₃₋₇, pirrolidinilo, piperidinilo, piperazinilo, 4-alquil C₁₋₆-piperazinilo, 4-alquilcarbonil C₁₋₆-piperazinilo y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituidos opcionalmente con uno o con dos radicales alquilo C₁₋₆; Het como grupo o parte de un grupo es un anillo heterocíclico saturado, parcialmente no saturado o completamente no saturado de 5 ó 6 miembros que contiene 1 a 4 heteroátomos, cada uno seleccionado independientemente de nitrógeno, oxígeno y azufre, estando dicho anillo heterocíclico opcionalmente condensado con un anillo bencénico; y donde dicho het como un todo está sustituido opcionalmente con uno, dos o tres sustituyentes, cada uno seleccionado independientemente del grupo que consiste en halo, hidroxi, nitro, ciano, carboxilo, alquilo C₁₋₆, alcoxi C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, alquilcarbonilo C₁₋₆, amino, mono- o di-alquilamino C₁₋₆, azido, mercapto, polihaloalquilo C₁₋₆, polihaloalcoxi C₁₋₆, cicloalquilo C₃₋₇, pirrolidinilo, piperidinilo, piperazinilo, 4-alquil C₁₋₆-piperazinilo, 4-alquilcarbonil C₁₋₆-piperazinilo y morfolinilo; donde los grupos morfolinilo y piperidinilo pueden estar sustituidos opcionalmente con uno o con dos radicales alquilo C₁₋₆; caracterizado porque es un compuesto de fórmula (2) o una sal del mismo.Pharmaceutical compositions containing compounds of formula (1) and processes for preparing compounds of formula (1). Bioavailable combinations of the HCV inhibitors of formula (1) with ritonavir are also provided. Claim 1: A compound having the formula (1) or a salt thereof, wherein each dotted line (represented by - - - - -) represents an optional double bond; X is N, CH and when X has a double bond it is C; R¹ is -OR⁷, -NH-SO₂R⁸; R² is hydrogen and when X is C or CH, R² can also be C₁₋₆ alkyl; R³ is hydrogen, C₁₋₆ alkyl, C₁₋₆ alkoxy-C₁₋₆ alkyl, C₃₋₇ cycloalkyl; R⁴ is aryl or Het; n is 3, 4, 5 or 6; R⁵ represents halo, C₁₋₆ alkyl, hydroxy, C₁₋₆ alkoxy, C₁₋₆ polyhaloalkyl, phenyl or Het; R⁶ represents C₁₋₆ alkoxy or dimethylamino; R⁷ is hydrogen; aryl; Het; C₃₋₇ cycloalkyl; optionally substituted with C₁₋₆ alkyl; or C₁₋₆ alkyl optionally substituted with C₃₋₇ cycloalkyl, aryl or with Het; R⁸ is aryl; Het; C₃₋₇ cycloalkyl optionally substituted with C₁₋₆ alkyl; or C₁₋₆ alkyl optionally substituted with C₃₋₇ cycloalkyl, aryl or with Het; aryl as a group or part of a group is phenyl optionally substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, carboxyl, C₁₋₆ alkyl, C alco alkoxy, C₁₋₆ alkoxy-C₁₋₆ alkyl , C₁₋₆ alkylcarbonyl, amino, mono- or di-C₁₋₆ alkylamino, azido, mercapto, C₁₋₆ polyhaloalkyl, C₁₋₆ polyhaloalkoxy, C₃₋₇ cycloalkyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-C₁₋₆ alkyl piperazinyl, 4-alkylcarbonyl Cin-piperazinyl and morpholinyl; wherein the morpholinyl and piperidinyl groups may be optionally substituted with one or two C₁₋₆ alkyl radicals; Het as a group or part of a group is a saturated, partially unsaturated or completely unsaturated 5 or 6-membered heterocyclic ring containing 1 to 4 heteroatoms, each independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally condensed with a benzene ring; and wherein said het as a whole is optionally substituted with one, two or three substituents, each independently selected from the group consisting of halo, hydroxy, nitro, cyano, carboxyl, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋ alkoxy ₆-C₁₋₆ alkyl, C₁₋₆ alkylcarbonyl, amino, mono- or di-Cila alkylamino, azido, mercapto, C₁₋₆ polyhaloalkyl, C₁₋₆ polyhaloalkoxy, C₃₋₇ cycloalkyl, pyrrolidinyl, piperidinyl, piperazinyl, 4 -C₁₋₆-piperazinyl, 4-C₁₋₆-piperazinyl and morpholinyl alkyl; wherein the morpholinyl and piperidinyl groups may be optionally substituted with one or two C₁₋₆ alkyl radicals; characterized in that it is a compound of formula (2) or a salt thereof.

ARP140101796A 2005-07-29 2014-04-30 MACROCYCLIC INHIBITORS OF THE HEPATITIS C VIRUS, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USE OF THE SAME AND PROCESS TO PREPARE THEM AR099345A2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05107074 2005-07-29

Publications (1)

Publication Number Publication Date
AR099345A2 true AR099345A2 (en) 2016-07-20

Family

ID=44050753

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140101796A AR099345A2 (en) 2005-07-29 2014-04-30 MACROCYCLIC INHIBITORS OF THE HEPATITIS C VIRUS, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USE OF THE SAME AND PROCESS TO PREPARE THEM

Country Status (3)

Country Link
AR (1) AR099345A2 (en)
ES (1) ES2360473T3 (en)
UA (1) UA95245C2 (en)

Also Published As

Publication number Publication date
UA95245C2 (en) 2011-07-25
ES2360473T3 (en) 2011-06-06

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