AR037352A1 - Compuestos ligandos de los receptores de los cannabinoides, una composicion farmaceutica , y el uso de dichos compuestos para la manufactura de medicamentos - Google Patents

Compuestos ligandos de los receptores de los cannabinoides, una composicion farmaceutica , y el uso de dichos compuestos para la manufactura de medicamentos

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AR037352A1
AR037352A1 ARP020104334A ARP020104334A AR037352A1 AR 037352 A1 AR037352 A1 AR 037352A1 AR P020104334 A ARP020104334 A AR P020104334A AR P020104334 A ARP020104334 A AR P020104334A AR 037352 A1 AR037352 A1 AR 037352A1
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Argentina
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alkyl
group
haloalkyl
cycloalkyl
aryl
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Schering Corp
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Abstract

Un compuesto ligando de receptores de los cannabinoides de la fórmula (1), o una sal o solvato farmacéuticamente aceptables de dicho compuesto, en la cual; L1 es un enlace covalente, -CH2-, -C(O)-; -C(O)O-, -S(O2)-, -S(O)-, -S-, -O-, -NH-, o N(R7)-; L2 es -CH2, -C(H)(alquilo)-, -C(alquilo)2, -C(O)-; -SO-; -S(O2)-, -C(=NR7)-, -C(=N-CN)-, o -C(=N-OR7); L3 es enlace covalente, -C(O)-, o -S(O2); R1 está seleccionado entre el grupo consistente en H, halógeno, alquilo, haloalquilo, cicloalquilo, cicloalquilalquilo, heterociclilalquilo, -NHR7, -N(R7)2, -C(O)R7, -C(O)OR7, -S(O2)R7, -Si(alquilo)n(arilo)3-n, arilo, y heteroarilo, pudiendo cada uno de dichos arilo o heteroarilo estar no sustituido u opcionalmente sustituido independientemente con 1 a 5 partes que pueden ser iguales o diferentes entre sí y están independientemente seleccionados entre el grupo consistente en halógeno, alquilo, cicloalquilo, cicloalquilalquilo, haloalquilo, haloalcoxi, alcoxi, -N(R7)2, -C(O)OR7, -C(O)N(R7)2, -NC(O)OR7, -NC(O)N(R7)2, -NO2, -CN, S(O2)R7, S(O2)N(R7)2, NC(=N-CN)NHR7, y OH, con la condición de que: e) cuando R1 es halógeno, L1 es un enlace covalente; f) cuando R1 es -NHR7 o -N(R7)2, L1 es un enlace covalente, -CH2-, -C(O)-, S(O2)- o -SO-; g) cuando R1 es -C(O)R7 o -C(O)OR7, L1 es un enlace covalente, -CH2, -NH- o -N(alquilo)- y h) cuando R1 es -S(O2)R7 o -C(O)OR7, L1 es un enlace covalente, -CH2-, -NH-; o -N(alquilo)-; R2 es H; -OH, halógeno, -N(R7)2, -CF3, alcoxi, alquilo, haloalquilo, cicloalquilo, o cicloalquilalquilo; R3 y R4 , son iguales o diferentes entre sí y están independientemente seleccionados entre el grupo consistente en H o alquilo, o R3 y R4 tomados conjuntamente forman un grupo carbonilo, es decir, C(=O); R5 es H, o alquilo; R6 está seleccionado de entre el grupo consistente en H, alquilo, haloalquilo, cicloalquilo, NHR7, N(R7)2, arilo y heteroarilo, pudiendo cada arilo y heteroarilo no estar sustituido o estar opcionalmente sustituido con uno a cinco partes las cuales partes pueden ser iguales o diferentes entre sí y estan independientemente seleccionados entre el grupo consistente en halógeno, alquilo, cicloalquilo, haloalquilo, haloalcoxi, alcoxi, y OH; R7 es seleccionado entre el grupo consistente en H, alquilo, haloalquilo, cicloalquilo, heterocicloalquilo, arilo y heteroarilo, pudiendo cada arilo y heteroarilo no estar sustituido o estar opcionalmente sustituido con uno a cinco partes las cuales pueden ser iguales o diferentes entre sí y están independientemente seleccionados entre el grupo consistente en halógeno, alquilo, cicloalquilo, haloalquilo, haloalcoxi, alcoxi, y OH; A está seleccionado entre el grupo consistente en fenilo, naftilo, piridilo, tienilo, tiazolilo e indolilo, quinolilo, isoquinolilo, pirazinilo, piridazinilo, furanilo, pirrolilo, pirimidilo, linolinilo, quinazolinilo, quinoxalinilo, ftalazinilo, benzofuranilo, benzotienilo; X está independientemente seleccionado entre el grupo que consiste en H, halógeno, alquilo, cicloalquilo, haloalquilo, hidroxi, alcoxi, alcoxicarbonilo, haloalcoxi, -N(R7)2, -N(R7)(C(O)R7), -N(R7)(C(O)OR7), -NO2 y -CN, y cuando A está seleccionado entre el grupo consistente en piridilo, tienilo, tiazolilo, indolilo, quinolilo, isoquinolilo, pirazinilo, piridazinilo, pirrolilo, pirimidilo, cinolinilo, quinazolinilo, quinoxalinilo, ftalazinilo, y benzotienilo, X puede ser óxido; y n es de 0 a 3; con la condición de que (i) dos partes R7 en -N(R7)2 pueden ser iguales o diferentes entre sí, y están independientemente seleccionados, e (ii) la parte -N(R5)-L3-R6 puede formar opcionalmente un sistema de anillo. También se revelan composiciones farmacéuticas que contienen dichos compuestos y el uso de dichos compuestos para la manufactura de medicamentos que presentan una actividad anti-inflamatoria e inmunomoduladora.
ARP020104334A 2001-11-14 2002-11-12 Compuestos ligandos de los receptores de los cannabinoides, una composicion farmaceutica , y el uso de dichos compuestos para la manufactura de medicamentos AR037352A1 (es)

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CN (2) CN100567266C (es)
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US7868204B2 (en) * 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
WO2003024448A2 (en) * 2001-09-14 2003-03-27 Methylgene, Inc. Inhibitors of histone deacetylase
JP2005509032A (ja) 2001-11-14 2005-04-07 シェーリング　コーポレイション カンナビノイドレセプターリガンド
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