AR085352A1 - Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv - Google Patents

Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv

Info

Publication number
AR085352A1
AR085352A1 ARP120100432A ARP120100432A AR085352A1 AR 085352 A1 AR085352 A1 AR 085352A1 AR P120100432 A ARP120100432 A AR P120100432A AR P120100432 A ARP120100432 A AR P120100432A AR 085352 A1 AR085352 A1 AR 085352A1
Authority
AR
Argentina
Prior art keywords
heterocyclyl
nr1br1c
nrfrg
nrbrc
aralkyl
Prior art date
Application number
ARP120100432A
Other languages
English (en)
Original Assignee
Idenix Pharmaceuticals 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 Idenix Pharmaceuticals Inc filed Critical Idenix Pharmaceuticals Inc
Publication of AR085352A1 publication Critical patent/AR085352A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • 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
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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

Abstract

Compuestos macrocíclicos inhibidores de serina proteasa, por ejemplo, de la formula (1) y sus composiciones farmacéuticas y sus procesos de preparación. También métodos de su uso para el tratamiento de una infección de HCV en un huésped que lo necesita.Reivindicación 1: Un compuesto caracterizado por la fórmula (1) o una de sus variantes isotópicas; o una de sus sales, solvatos o profármacos farmacéuticamente aceptables; en donde: RA es (i) hidrógeno o halógeno; o (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; y RB es un resto seleccionado del grupo de fórmulas (2) a (5) en donde: cada Z es, de modo independiente, CR1 o N; U1, V1, W1 y X1 son cada uno, de modo independiente, O, N, S, CR9 o NR9; Y1 es C o N; R1, R2, R3, R4, R5, R6, R7, R8 y R9 son cada uno, de modo independiente, (i) hidrógeno, halo, ciano, trifluorometilo o nitro; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (iii) -C(O)R1a, C(O)OR1a, -C(O)NR1bR1c, -C(NR1a)NR1bR1c, -OR1a, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1bR1c, -NR1aS(O)2NR1bR1c, -P(O)R1aR1d, -P(O)(OR1a)R1d, -P(O)(OR1a)(OR1d), -SR1a, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c o -S(O)2NR1bR1c; y cada R1a, R1b, R1c y R1d es, de modo independiente, hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o R1a y R1c junto con los átomos de C y N a los que están unidos forman heterociclilo; o R1b y R1c junto con el átomo de N a los que están unidos forman heterociclilo; en donde cada alquilo, alquenilo, alquinilo, cicloalquilo, arilo, aralquilo, heteroarilo y heterociclilo está opcionalmente sustituido con uno o varios sustituyentes Q, donde cada Q está seleccionado, de modo independiente, de (a) oxo, ciano, halo y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo, cada uno de los cuales está opcionalmente sustituido con uno o varios, en una forma de realización, uno, dos, tres o cuatro sustituyentes Qa; y (c) -C(O)Ra, -C(O)ORa, -C(O)NRbRc, -C(NRa)NRbRc, -ORa, -OC(O)Ra, -OC(O)ORa, -OC(O)NRbRc, -OC(=NRa)NRbRc, -OS(O)Ra, -OS(O)2Ra, -OS(O)NRbRc, -OS(O)2NRbRc, -NRbRc, -NRaC(O)Rd, -NRaC(O)ORd, NRaC(O)NRbRc, -NRaC(=NRd)NRbRc, -NRaS(O)Rd, -NRaS(O)2Rd, -NRaS(O)NRbRc, -NRaS(O)2NRbRc, -P(O)RaRd, -P(O)(ORa)Rd, -P(O)(ORa)(ORd), -SRa, -S(O)Ra, -S(O)2Ra, -S(O)NRbRc y -S(O)2NRbRc, en donde cada Ra, Rb, Rc y Rd es, de modo independiente, (i) hidrógeno; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo, cada uno opcionalmente sustituido con uno o varios, en una forma de realización, uno, dos, tres o cuatro sustituyentes Qa; o (iii) Rb y Rc junto con el átomo de N a los que están unidos forman heterociclilo, opcionalmente sustituido con uno o varios, en una forma de realización, uno, dos, tres o cuatro sustituyentes Qa; en donde cada Qa está seleccionado, de modo independiente, del grupo que consiste en (a) oxo, ciano, halo y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo; y (c) -C(O)Re, -C(O)ORe, -C(O)NRfRg, -C(NRe)NRfRg, -ORe, -OC(O)Re, -OC(O)ORe, -OC(O)NRfRg, -OC(=NRe)NRfRg, -OS(O)Re, -OS(O)2Re, -OS(O)NRfRg, -OS(O)2NRfRg, -NRfRg, -NReC(O)Rh, -NReC(O)ORf, -NReC(O)NRfRg, -NReC(=NRh)NRfRg, -NReS(O)Rh, -NReS(O)2Rh, -NReS(O)NRfRg, -NReS(O)2NRfRg, -P(O)ReRh, -P(O)(ORe)Rh, -P(O)(ORe)(ORh), -SRe, -S(O)Re, -S(O)2Re, -S(O)NRfRg y -S(O)2NRfRg; en donde cada Re, Rf, Rg y Rh es, de modo independiente, (i) hidrógeno; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (iii) Rf y Rg junto con el átomo de N a los que están unidos forman heterociclilo.
ARP120100432A 2011-02-10 2012-02-09 Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv AR085352A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161441563P 2011-02-10 2011-02-10

Publications (1)

Publication Number Publication Date
AR085352A1 true AR085352A1 (es) 2013-09-25

Family

ID=45814652

Family Applications (1)

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ARP120100432A AR085352A1 (es) 2011-02-10 2012-02-09 Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv

Country Status (4)

Country Link
US (1) US9353100B2 (es)
AR (1) AR085352A1 (es)
TW (1) TW201309690A (es)
WO (1) WO2012109398A1 (es)

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
TW201040181A (en) 2009-04-08 2010-11-16 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitors
JP2013501068A (ja) 2009-08-05 2013-01-10 アイディニックス ファーマシューティカルズ インコーポレイテッド 大環状セリンプロテアーゼ阻害剤
AR085352A1 (es) 2011-02-10 2013-09-25 Idenix Pharmaceuticals Inc Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
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