ES2534222T3 - Compuestos que contienen haloalquilo como inhibidores de la cisteína proteasa - Google Patents

Compuestos que contienen haloalquilo como inhibidores de la cisteína proteasa Download PDF

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ES2534222T3
ES2534222T3 ES04784332.1T ES04784332T ES2534222T3 ES 2534222 T3 ES2534222 T3 ES 2534222T3 ES 04784332 T ES04784332 T ES 04784332T ES 2534222 T3 ES2534222 T3 ES 2534222T3
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methyl
fluorophenyl
methylphenyl
fluoro
ethyl
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John O. Link
Craig J. Mossman
Soon H. Woo
Sheila M. Zipfel
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Virobay Inc
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Virobay Inc
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Abstract

Un compuesto de la Fórmula (I):**Fórmula** en donde: R1 y R2 tomados junto con el átomo de carbono al que tanto R1 como R2 están unidos, forman (i) cicloalquileno opcionalmente sustituido con uno o dos Rb seleccionados independientemente entre alquilo, halo, alquilamino, dialquilamino, arilo, aralquilo, cicloalquilo, cicloalquilalquilo, heteroarilo, heteroaralquilo, alcoxicarbonilo, o ariloxicarbonilo, (ii) heterociclilalquileno opcionalmente sustituido con uno a cuatro Rc independientemente seleccionados entre alquilo, haloalquilo, hidroxi, hidroxialquilo, alcoxialquilo, alcoxialquiloxialquilo, ariloxialquilo, heteroariloxialquilo, aminoalquilo, acilo, arilo, aralquilo, heteroarilo, heteroaralquilo, heterociclilo, heterociclilalquilo, cicloalquilo, cicloalquilalquilo, -S(O)n2R14, -alquileno-S(O)n2-R15, -COOR16, -alquileno-COOR17, -CONR18R19, o - alquileno-CONR20R21 donde n2 es 0-2 y R14-R17, R18 y R20 son independientemente hidrógeno, alquilo, haloalquilo, arilo, aralquilo, heteroarilo, heteroaralquilo, cicloalquilo, cicloalquilalquilo, o heterociclilo y R19 y R21 son independientemente hidrógeno o alquilo en donde el anillo aromático o alicíclico en los grupos unidos a cicloalquileno o heterociclilalquileno está opcionalmente sustituido con uno, dos, o tres sustituyentes seleccionados independientemente entre alquilo, haloalquilo, alcoxi, hidroxi, haloalcoxi, halo, carboxi, alcoxicarbonilo, amino, amino monosustituido, amino disustituido, o acilo; R3 es hidrógeno; R5 es hidrógeno; donde cicloalquilo es un anillo monocíclico monovalente saturado o parcialmente insaturado que comprende de tres a ocho átomos de carbono en el anillo y cicloalquileno se refiere a un anillo monocíclico divalente saturado o parcialmente insaturado que contiene de tres a ocho átomos de carbono; y en donde R4 es etiltiometilo, etilsulfinilmetilo, etilsulfonilmetilo, isopropiltiometilo, 2-metiltioetilo, 2-metilsulfiniletilo, 2- metisulfoniletilo, 2-metilpropilsulfonilmetilo, isobutilsulfanilmetilo, terc-butiltiometilo, bencenosulfonilmetilo, 2-fenil- sulfaniletilo, 2-fenilsulfoniletilo, naft-2-ilmetanosulfonilmetilo, bifenil-2-ilmetanosulfonilmetilo, bifenil-4-ilmetanosulfonil- metilo, fenilmetanosulfanilmetilo, fenilmetanosulfinilmetilo, fenilmetanosulfonilmetilo, 2-fenilmetanosulfoniletilo, 4-terc- butilfenilmetanosulfonilmetilo, 2-fluorofenilmetanosulfanilmetilo, 2-fluorofenilmetanosulfonilmetilo, 3-fluorofenil- metanosulfonilmetilo, 4-fluorofenilmetanosulfonilmetilo, 2-clorofenilmetanosulfanilmetilo, 2-clorofenilmetano- sulfonilmetilo, 3-clorofenilmetanosulfonilmetilo, 4-clorofenilmetanosulfonilmetilo, 2-metoxifenilmetanosulfonilmetilo, 4- metoxifenilmetanosulfonilmetilo, 2-trifluorometoxifenilmetanosulfonilmetilo, 3-trifluorometoxifenilmetanosulfonilmetilo, 30 4-trifluorometoxifenilmetanosulfonilmetilo, 2-trifluorometilfenilmetanosulfanilmetilo, 2-trifluorometilfenilmetano- sulfonilmetilo, 3-trifluorometilfenilmetanosulfonilmetilo, 4-trifluorometilfenilmetanosulfonilmetilo, 2-cianofenilmetano- sulfanilmetilo, 2-cianofenilmetanosulfonilmetilo, 3-cianofenilmetanosulfonilmetilo, 2-bromofenilmetanosulfonilmetilo, 2-nitrofenilmetanosulfanilmetilo, 2-nitrofenilmetanosulfonilmetilo, 2-metilfenilmetanosulfonilmetilo, 3-metilfenilmetano- sulfonilmetilo, 4-metilfenilmetanosulfonilmetilo, 2-(4-trifluormetoxibencenosulfonil)etilo, 2-(3-trifluorometoxibenceno- sulfonil)etilo, 2-(2-trifluorometoxi-bencenosulfonil)-etilo, 2-difluorometoxifenilmetanosulfonilmetilo, 3-difluorometoxi- fenilmetanosulfonilmetilo, 4-difluorometoxifenilmetano-sulfonilmetilo, 2- (4-difluorometoxibenzenesulfonil) etilo, 2- (2- difluorometoxibenzene-sulfonil)etilo, 2-(3-difluorometoxibenzenesulfonil)etilo, 3-cloro-2-fluorofenilmetano-sulfonil- metilo, 3,5-dimetilfenilmetanosulfonilmetilo, 3,5-bis-trifluorometilfenilmetanosulfonilmetilo, 2,5-difluorofenilmetano- sulfonilmetilo, 2,6-difluorofenilmetanosulfonilmetilo, 2,3-difluorofenilmetano-sulfonilmetilo, 3,4-difluorofenilmetano- 40 sulfonilmetilo, 2,4-difluorofenilmetanosulfonilmetilo, 2,5-diclorofenilmetanosulfonilmetilo, 3,4-diclorofenilmetano- sulfonilmetilo, 2,6-diclorofenilmetanosulfonilmetilo, 2-fluoro-3-metilfenilmetanosulfonilmetilo, 4-fluoro-2-trifluoro- metoxifenilmetanosulfonilmetilo, 2-fluoro-6-trifluorometilfenilmetanosulfonilmetilo, 2-fluoro-3-trifluorometilfenilmetano- sulfonilmetilo, 2-fluoro-4-trifluorometilfenilmetanosulfonilmetilo, 2-fluoro-5-trifluorometilfenilmetanosulfonilmetilo, 4- fluoro-3-trifluorometil-fenilmetanosulfonilmetilo, 2-cloro-5-trifluorometilfenilmetanosulfonilmetilo, 2,4,6-trifluorofenil- metanosulfonilmetilo, 2,4,5-trifluorofenilmetanosulfonilmetilo, 2,3,4-trifluorofenilmetanosulfonilmetilo, 2,3,5-trifluoro- fenilmetanosulfonilmetilo, 2,5,6-trifluorofenilmetanosulfonilmetilo, 3,4,5-trimetoxifenilmetanosulfonilmetilo, piridin-2- ilmetanosulfonilmetilo, piridin-3-ilmetanosulfonilmetilo, piridin-4-ilmetanosulfonilmetilo, 2-(piridin-2-ilsulfonil)etilo, 2- (piridin-4-ilsulfonil)etilo, oxipiridin-2-ilmetanosulfonilmetilo, ciclohexilmetanosulfanilmetilo, ciclohexilsulfiniltiometilo, ciclohexilmetanosulfonilmetilo, ciclohexilmetanosulfonilmetilo, ciclopropilmetanosulfonilmetilo, tiofeno-2-sulfonilmetilo, 5-clorotien-2-ilmetanosulfonilmetilo, o 3,5-dimetil-isoxazol-4-ilmetanosulfonilmetilo; donde R6 es fenilo, 4-metoxifenilo, 4-clorofenilo, 4-fluorofenilo, 2-fluorofenilo, 2-fluoro-4-clorofenilo, naftilo, piperidin-4-ilo, morfolin-4-ilo, furanilo, tienilo, piridin-4-ilo, o pirazinilo; y, en donde: R7 es trifluorometilo y R8 es hidrógeno.

Description

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ES04784332.1T 2003-09-18 2004-09-17 Compuestos que contienen haloalquilo como inhibidores de la cisteína proteasa Expired - Lifetime ES2534222T3 (es)

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