AR039684A1 - Moduladores de receptor activado de proliferador de peroxisoma con union amida - Google Patents

Moduladores de receptor activado de proliferador de peroxisoma con union amida

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Publication number
AR039684A1
AR039684A1 ARP030102136A ARP030102136A AR039684A1 AR 039684 A1 AR039684 A1 AR 039684A1 AR P030102136 A ARP030102136 A AR P030102136A AR P030102136 A ARP030102136 A AR P030102136A AR 039684 A1 AR039684 A1 AR 039684A1
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AR
Argentina
Prior art keywords
alkyl
group
aryl
arylalkyl
cycloalkyl
Prior art date
Application number
ARP030102136A
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English (en)
Original Assignee
Lilly Co Eli
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Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR039684A1 publication Critical patent/AR039684A1/es

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Abstract

La presente se refiere a compuestos, composiciones y uso de compuestos de fórmula estructural (1). Reivindicación 1: Un compuesto de fórmula estructural (1), donde: (a) R1 se selecciona del grupo formado por hidrógeno, alquilo (C1-8), cicloalquilo (C3-6), arilalquilo (C0-4), heteroarilalquilo (C0-4), aminoalquilo (C1-4), cicloalquil(C3-6)-arilalquilo(C0-2), arilheteroalquilo (C1-8), -CHC(O)-alcoxi (C1-4), alquil(C0-4)-C(O)-heteroalquilo(C1-8) y -CH2-C(O)-R15-R16; y estando dichos alquilo (C1-8), cicloalquilo (C3-6), arilalquilo (C0-4), heteroarilalquilo (C0-4), aminoalquilo (C1-4), cicloalquil(C3-6)-arilalquilo(C0-2), arilheteroalquilo (C1-8), -CHC(O)-alcoxi (C1-4), alquil(C0-4)-C(O)-heteroalquilo (C1-8) y -CH2-C(O)-R15-R16 cada uno independientemente no sustituido o sustituido con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R1'; y en la que R15 es O ó NH y R16 es bencilo, estando no sustituido o sustituido el bencilo con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R16'; (b) R1' y R2' son independientemente cada uno un grupo formado por alquilo (C1-5), cicloalquilo (C3-6), alcoxi (C1-5), arilalcoxi (C0-2), haloalquilo (C1-3), halo, arilo, -C(O)-alquilo (C1-5), -C(O)-arilo, haloalquil(C1-5)oxi, arilalquilo(C1-5) y biarilalquilo (C1-5); y estando no sustituido o sustituido dicho -C(O)-arilo con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por halo, alquilo (C1-5), haloalquilo (C1-5), alcoxi (C1-5) y -C(O)-alquilo (C1-5); y estando independientemente no sustituidos o sustituidos cada uno de arilalquilo (C1-5), biarilalquilo (C1-5) y arilo con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por halo, alquilo (C1-8), arilo, haloalquilo (C1-5), trihaloalquilo (C1-3), alcoxi (C1-5) y arilalquilo (C1-5); (c) R2 se selecciona del grupo formado por alquilo (C1-8), cicloalquilo (C3-6), arilalquilo (C0-4), heteroarilalquilo (C0-4), heterocicloalquil(C1-6)arilo, heterocicloalquil(C1-6)-arilalquilo(C1-4), aminoalquilo (C1-4), cicloalquil(C3-6)-arilalquilo(C0-2), arilheteroalquilo (C1-8), alquil(C0-4)-C(O)-heteroalquilo(C1-8)-, -CH(C(O)OCH3)bencilo y -CH2-C(O)-R15''-R16'', y estando independientemente no sustituidos o sustituidos dichos alquilo (C1-8), cicloalquilo (C3-6), arilalquilo (C0-4), heterocicloalquil(C1-6)-arilalquilo(C1-4), heteroarilalquilo (C0-4), aminoalquilo (C1-4), cicloalquil(C3-6)-arilalquilo(C0-2), arilheteroalquilo (C1-8), alquil(C0-4)-C(O)-heteroalquilo (C1-8) y -CH2-C(O)-R15''-R16'' cada uno con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R2'; (d) R15'' es O ó NH; (e) R16'' es bencilo, estando no sustituido o sustituido dicho bencilo con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R16'; (f) R1 y R2 pueden formar conjuntamente un anillo heterocíclico, estando no sustituido o sustituido dicho anillo heterocíclico con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R1'; (g) E se selecciona del grupo formado por C(R3)(R4)A, (CH2)nCOOR13, arilalquilo (C0-4), tioalquilo (C1-4), tioarilo, arialcoxi (C1-4), alcoxi(C1-4)-alquilo(C1-4), aminoarilo, y aminoalquilo (C1-4); y estando independientemente no sustituidos o sustituidos dichos (CH2)nCOOR13, arilalquilo (C0-4), tioalquilo (C1-4), tioarilo, alcoxi(C1-4)arilo, alcoxi(C1-4)-alquilo(C1-4), aminoarilo, y aminoalquilo (C1-4) cada uno con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por E'; (h) R7' y R7'' se seleccionan independientemente cada uno del grupo formado por alquilo (C1-4) y haloalquilo (C1-4); (i) n y m se seleccionan independientemente cada uno del grupo formado por 0, 1, 2 y 3; (j) A se selecciona del grupo formado por (CH2)mCOOR14, alquil(C1-3)nitrilo, carboxamida, sulfonamida, acilsulfonamida y tetrazol, estando independientemente no sustituidos o sustituidos dichos sulfonamida, acilsulfonamida y tetrazol con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por A'; (k) A' es un grupo formado por alquilo (C1-4), haloalquilo (C1-4), heteroarilo y arilo, y en el que heteroarilo y arilo están independientemente no sustituidos o sustituidos cada uno con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por halo, alquilo (C1-5), haloalquilo (C1-5), alcoxi (C1-5) y -C(O)alquilo (C1-5); (l) R3 se selecciona del grupo formado por H, alquilo (C1-5), alquenilo (C1-5) y alcoxi (C1-6); (m) R4 se selecciona del grupo formado por H, halo, alquilo (C1-5), alcoxi (C1-6), cicloalquilo (C3-6), arilalquilo (C0-4) y alcoxi(C1-4)arilo, y estando independientemente no sustituidos o independientemente sustituidos dichos alquilo (C1-5), alcoxi (C1-6), cicloalquilo (C3-6), arilalquilo (C0-4) y alcoxi(C1-4)arilo cada uno con uno a cuatro sustituyentes independientemente seleccionados cada uno de R4'; o R3 y R4 se combinan para formar un cicloalquilo (C3-6); (n) R5 y R6 se seleccionan independientemente cada uno del grupo formado por hidrógeno, alquilo (C1-8), arilalquilo (C0-4), heteroarilalquilo (C0-4), cicloalquil(C3-6)-arilalquilo(C0-2), cicloalquil(C3-6)-alquilo(C0-2) y -CH2-C(O)-R17-R18, y estando independientemente no sustituidos o sustituidos dichos alquilo (C1-8), arilalquilo (C0-4), heteroarilalquilo (C0-4), cicloalquil(C3-6)-arilalquilo(C0-2), cicloalquil(C3-6)-alquilo(C0-2) y -CH2-C(O)-R17-R18 con uno a cuatro sustituyentes independientemente seleccionados cada uno del grupo formado por R5'; (o) E', R4', R5' y R13'' son cada uno independientemente un grupo formado por alquilo (C1-5), alcoxi (C1-5), haloalquilo (C1-5), haloalcoxi (C1-5), nitro, ciano, CHO, hidroxi, ácido alcanoico (C1-4), fenilo, ariloxi, SO2R7', SR7'', arilalcoxi (C0-2), alquil (C1-6)carboxamido y COOH; (p) R16' es un grupo formado por halo, alquilo (C1-8), arilo, haloalquilo, trihaloalquilo (C1-3), alcoxi (C1-5) y arilalquilo (C1-5); (q) R17 y R18 se seleccionan independientemente cada uno de alquilo (C1-8), arilalquilo (C0-4), heteroarilalquilo (C0-4), cicloalquil(C3-6)-arilalquilo(C0-2) y cicloalquil(C3-6)-alquilo(C0-2); (r) R13 y R14 se seleccionan independientemente cada uno del grupo formado por hidrógeno, alquilo (C1-4), arilo, y arilmetilo, y estando independientemente no sustituido o sustituido el citado alquilo (C1-4) cada uno con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R13', y estando independientemente no sustituidos o sustituidos dichos arilmetilo y arilo cada uno con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R14'; (s) R13' es un grupo formado por alquilo (C1-5), cicloalquilo (C3-6), haloalquilo (C1-5), alcoxi (C1-5), ariloxi, halo, arilo, -C(O)-alquilo (C1-5), -C(O)-arilo, haloalquil(C1-5)oxi, arilalquilo (C1-5) y alquil(C1-5)biarilo, y estando independientemente no sustituidos o sustituidos dichos -C(O)-arilo, arilo, arilalquilo (C1-5) y alquil(C1-5)biarilo cada uno con uno a tres sustituyentes independientemente seleccionados cada uno del grupo formado por R13''; y (t) R14' es un grupo formado por halo, alquilo (C1-8), haloalquilo (C1-5), alcoxi (C1-5) y arilalquilo (C0-4); o (u) una de sus sales farmacéuticamente aceptables.
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