AR060872A1 - Antagonistas de los receptores cgrp monociclicos sustituidos - Google Patents

Antagonistas de los receptores cgrp monociclicos sustituidos

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AR060872A1
AR060872A1 ARP070101991A ARP070101991A AR060872A1 AR 060872 A1 AR060872 A1 AR 060872A1 AR P070101991 A ARP070101991 A AR P070101991A AR P070101991 A ARP070101991 A AR P070101991A AR 060872 A1 AR060872 A1 AR 060872A1
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Argentina
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substituted
halo
nrbrc
unsubstituted
ora
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ARP070101991A
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Merck & Co Inc
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Abstract

Reivindicacion 1: Un compuesto de la formula (1 )en la que A1 se selecciona de: -O-, -S(O)v-, -Si(Ora)-alquil C1-4-, donde el alquilo está sustituido o no sustituido con 1-5 halo, -Si(alquilo C1-4)2, donde cada alquilo independientemente no está sustituido o está sustituido con 1-5 halo-, -CR6R7-, -N(R8)-, -(C=O)-, -C(R8)(Ra)-, -C(N(Rb)-SO2Rd(Ra)-, -C(N(Rb)(C=O)Ra)(Ra)-, -C(N(Rb)(C=O)ORa)(Ra)-, -CR10R11-, y -N(R11)-; A2 se selecciona de entre -CR6R7-, -CR10R11-, y -(C=O)-, A3 se selecciona de entre: -CR6R7-, -N(R8)-, -CR10R11-, y -N(R11)-; A4 se selecciona de entre: -CR6R7-, -(C=O)-, -N(R8)-, -CR10R11-, -N(R11)-, y un enlace entre A2 y A3; Ea se selecciona de entre: -C(R5a)=, -N=, y -(N+-O-)=; Eb se selecciona de entre: -C(R5b)=, -N=, y -(N+-O-)=; Ec se selecciona de entre: -C(R5c)=, -N=, y -(N+-O-)=; Q se selecciona de entre: -(C=O)-, -SO2-, -SO-, y -C(Ra)2-; R4 se selecciona de entre: H, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -cicloalquilo C3-6, -CF3, y -O-Ra, -cicloalquilo C3-6, bencilo, y fenilo; R5a, R5b y R5c se seleccionan cada uno independientemente de entre: H, -alquilo C1-6, que no está sustituido o está sustituido con 1-6 halo, halo, -ORa, y -CN; R6 y R7 se seleccionan cada uno independientemente de entre: H, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -ORa, -cicloalquilo C3-6, fenilo o heterociclo, estando dicho heterociclo seleccionado de: piridilo, pirimidinilo, pirazinilo, piridazinilo, piperidinilo, piperazinilo, pirrolidinilo, tienilo, morfolinilo, tiazolilo, indolilo, indazolilo, bencimidazolilo y oxazolilo, estando dicho fenilo o heterociclo no sustituido o sustituido con 1-5 sustituyentes seleccionados cada uno independientemente de: halo, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 halo, -ORa, -NRbRc, - CN, y oxo; -CO2Ra, -C(=O)NRbRc, -S(O)vRd, -CN, -NRbRc, -N(Rb)C(=O)Ra, -N(Rb)SO2Rd, -CF3, -O-CO2Rd, -O-(C=O)-NRbRc, -C(=O)Ra, -cicloalquilo C3-8, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -CN, -alquilo C1-4, que no está sustituido o está sustituido con 1-3 halo, y -ORa, fenilo o heterociclo, estando dicho heterociclo seleccionado de: piridilo, pirimidinilo, pirazinilo, piridazinilo, piperidinilo, piperazinilo, pirrolidinilo, tienilo, morfolinilo, tiazolilo y oxazolilo, estando dicho fenilo o heterociclo no sustituido o sustituido con 1-5 sustituyentes seleccionados cada uno independientemente de: halo, -ORa, -cicloalquilo C3-6, fenilo, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -alquilo C1-6, que no está sustituido o está sustituido con 1-6 halo, y -ORa, -CO2Ra, -C(=O)NRbRc, -S(O)vRd, -CN, -NRbRc, - N(Rb)C(=O)Ra, -N(Rb)SO2Rd, -O-CO2Rd, -O(C=O)NRbRc, -NRb-(C=O)-NRbRc, -C(=O)Ra, -alquilo C1-6, que no está sustituido o está sustituido con 1-6 halo, y oxo; halo, -ORa, -CN, -CO2Ra, -N(Rb)C(=O)Ra, -NRbRc, -C(=O)NRbRc, y -O(C=O)Ra; o R6 y R7 y el átomo o átomos de carbono al que (a los que) están unidos se unen formando un anillo que se selecciona de entre ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo, cicloheptilo, ciclooctilo, ciclononilo, ciclobutenilo, ciclopentenilo, ciclohexenilo, cicloheptenilo, ciclooctenilo, dioxolanilo, dioxanilo, aziridinilo, azetidinilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, tetrahidrofuranilo, tetrahidropiranilo, tetrahidrotiapiranilo, oxetanilo, tietanilo y tetrahidrotienilo, en los que el azufre está opcionalmente oxidado dando la sulfona o sulfoxido, y dicho anillo no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: -alquilo C1-6, que no está sustituido o está sustituido con 1-3 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -ORa, -cicloalquilo C3-6, -CO2Ra, -NRbRc, -S(O)vRd, -C(=O)NRbRc, fenilo, -cicloalquilo C3-6, estando el grupo cicloalquilo C3-6 opcionalmente condensado con el anillo, y estando el grupo C3-6 no sustituido o sustituido con 1-3 sustituyentes seleccionados cada uno independientemente de entre: halo, -ORa, -cicloalquilo C3-6, -CO2Ra, -NRbRc, -S(O)vRd, -C(=O)NRbRc, y fenilo, fenilo o heterociclo, estando dicho heterociclo seleccionado de: piridilo, pirimidinilo, pirazinilo, piridazinilo, piperidinilo, piperazinilo, pirrolidinilo, tienilo, morfolinilo, imidazolilo, furanilo, tetrahidrofuranilo, tiazolilo y oxazolilo, estando el fenilo o heterociclo opcionalmente condensado con el anillo, y dicho fenilo o heterociclo no está sustituido o está sustituido con 1-5 sustituyentes seleccionados cada uno independientemente de: halo, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 halo, -ORa, -CO2Ra, -O(C=O)Ra, -CN, -NRbRc, oxo, -C(=O)NRbRc, -N(Rb)C(=O)Ra, -N(Rb)CO2Ra, -O(C=O)NRbRc, y -S(O)vRd, -ORa, -CO2Ra, -C(=O)NRbRc, -S(O)vRd, -CN, halo, -NRbRc, -N(Rb)C(=O)Ra, -N(Rb)SO2Rd, -O-CO2Rd, -O(C=O)- NRbRc, -NRb-(C=O)-NRbRc, -C(=O)Ra, y oxo; R8 se selecciona independientemente de entre: H, -C(=O)Ra, -CO2Ra, -S(=O)Rd, -SO2Rd, -C(=O)NRbRc, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -ORa, -cicloalquilo C3-6, fenilo o heterociclo, en el que dicho heterociclo seleccionado de: piridilo, pirimidinilo, pirazinilo, piridazinilo, piperidinilo, piperazinilo, pirrolidinilo, tienilo, morfolinilo, tiazolilo y oxazolilo, estando dicho fenilo o heterociclo no sustituido o sustituido con 1-5 sustituyentes seleccionados cada uno independientemente de: halo, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 halo, y -ORa, -NRbRc, - C(=O)Ra, -CO2Ra, y oxo, -CO2Ra, -C(=O)NRbRc, -S(O)vRd, -CN, -NRbRc, -N(Rb)C(=O)Ra, -N(Rb)SO2Rd, -CF3, -O-CO2Rd, -O(C=O)NRbRc, -NRb-(C=O)-NRbRc, y -C(=O)Ra, -cicloalquilo C3-6, que no está sustituido o está sustituido con 1-6 sustituyentes que se seleccionan cada uno independientemente de entre: halo; -CN, -ORa, y -alquilo C1-6, que no está sustituido o está sustituido con 1-6 halo; o R7 y R8 y los átomos a los que están unidos se unen formando un anillo alquilo o heteroalquilo de 4, 5, 6 o 7 miembros que opcionalmente contiene un heteroátomo adicional que se selecciona de entre N, O, y S, en el que el azufre está opcionalmente oxidado dando la sulfona o sulfoxido, y dicho anillo no está sustituido o está sustituido con 1-4 sustituyentes que se seleccionan cada uno independientemente de entre: halo, fenilo, que no está sustituido o está sustituido con 1-3 sustituyentes que se seleccionan cada uno independientemente de entre: halo, ORa, CN y -C(=O)ORa, -Ora, y -alquilo C1-6, que no está sustituido o está sustituido con 1-6 halo; R10 se selecciona independientemente de entre: H, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -ORa, -CN, fenilo, y -cicloalquilo C3-6, que no está sustituido o está sustituido con 1-6 halo, -cicloalquilo C3-6, que no está sustituido o está sustituido con 1-6 halo; R11 se selecciona independientemente del grupo constituido por: fenilo, naftilo, tetrahidronaftilo, indanilo, bifenilo, fenantrilo, antrilo, azepinilo, azepanilo, azetidinilo, bencimidazolilo, bencisoxazolilo, benzofuranilo, benzofurazanilo, benzopiranilo, benzotiopiranilo, benzofurilo, 1,3-benzodioxolilo, benzotiazolilo, benzotienilo, benzoxazolilo, benzopirazolilo, benzotriazolilo, cromanilo, cinolinilo, dibenzofuranilo, dihidrobenzofurilo, dihidrobenzotienilo, dihidrobenzotiopiranilo, dihidrobenzotiopiranilsulfona, furilo, furanilo, imidazolidinilo, imidazolinilo, imidazolilo, indolinilo, indolilo, isocromanilo, isoindolinilo, isoquinolinilo, isotiazolidinilo, isotiazolilo, morfolinilo, naftiridinilo, oxadiazolilo, 2-oxoazepinilo, 4-oxonaftiridinilo, 2-oxopiperazinilo, 2- oxopiperidinilo, 2-oxopirrolidinilo, 2-oxopiridilo, 2-oxoquinolinilo, piperidilo, piperazinilo, pirazinilo, pirazolidinilo, pirazolilo, piridazinilo, piridinilo, piridilo, pirimidinilo, pirimidilo, pirrolidinilo, pirrolilo, quinazolinilo, quinolinilo, quinoxalinilo, tetrahidrofuranilo, tetrahidrofurilo, tetrahidroimidazopiridinilo, tetrahidroisoquinolinilo, tetrahidroquinolinilo, tetrazolilo, tiamorfolinilo, tiamorfolinilsulfoxido, tiamorfolinilsulfona, tiazolilo, tiazolinilo, tienofurilo, tienotienilo, tienilo, triazolilo, isoxazolilo, tetrahidrotienilo, tetrahidropiranilo, oxetanilo, tetrahidrotiapiranilo, y tietanilo, donde R11 no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre R12, R13, R14, R15a y R15b; R12, R13, R14, R15a y R15b se seleccionan cada uno independientemente de entre: -alquilo C1-6, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -ORa, -cicloalquilo C3-6, fenilo o heterociclo, estando dicho heterociclo seleccionado de: piridilo, pirimidinilo, pirazinilo, piridazinilo, piperidinilo, piperazinilo, pirrolidinilo, tienilo, morfolinilo, tiazolilo y oxazolilo, estando dicho fenilo o heterociclo no sustituido o sustituido con 1-5 sustituyentes seleccionados cada uno independientemente de: halo, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 halo, y -ORa; -CO2Ra, - C(=O)NRbRc, -S(O)vRd, -CN, -NRbRc, -N(Rb)C(=O)Ra, -N(Rb)SO2Rd, -CF3, -O-CO2Rd, -O-(C=O)-NRbRc, -NRb-(C=O)-NRbRc, y -C(=O)Ra, -cicloalquilo C1-6, que no está sustituido o está sustituido con 1-5 sustituyentes que se seleccionan cada uno independientemente de entre: halo, -CN, -alquilo C1-6, que no está sustituido o está sustituido con 1-5 halo, -ORa, y fenilo, que no está sustituido o está sustituido con 1-5 sustituyentes donde los sustituyentes se seleccionan
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