AR057408A1 - Agonistas del receptor de niacina composiciones que contienen tales compuestos y procedimientos para tratamiento - Google Patents

Agonistas del receptor de niacina composiciones que contienen tales compuestos y procedimientos para tratamiento

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AR057408A1
AR057408A1 ARP060102740A ARP060102740A AR057408A1 AR 057408 A1 AR057408 A1 AR 057408A1 AR P060102740 A ARP060102740 A AR P060102740A AR P060102740 A ARP060102740 A AR P060102740A AR 057408 A1 AR057408 A1 AR 057408A1
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Argentina
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alkyl
groups
halo
optionally substituted
group
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Merck & Co Inc
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Abstract

También se incluyen composiciones farmacéuticas y procedimientos de uso. Reivindicacion 1: Se describe un compuesto representado por la formula (1) o una sal o solvato farmacéuticamente aceptable del mismo en la que: X representa CH2, O, S, S(O), SO2 o NH, de tal forma que cuando X representa NH, el átomo de N puede estar opcionalmente sustituido con R6, C(O)R6, o SO2R6, donde: R6 representa alquilo C1-3 opcionalmente sustituido con 1-3 grupos, 0-3 de los cuales son halo, y 0-1 de los cuales se seleccionan entre el grupo constituido por: O-alquilo C1-3, OH, NH2, NH-alquilo C1-3, N(alquilo C1-3)2, CN, Hetci, Arilo y HAR; estando dicho Arilo y HAR opcionalmente sustituidos adicionalmente con 1-3 grupos, 1-3 de los cuales son halo, y 0-1 de los cuales se seleccionan entre el grupo constituido por: grupos OH, NH2, alquilo C1-3, alcoxi C1-3, haloalquilo C1-3 y haloalcoxi C1-3; cada uno de a y b es el numero entero 1, 2 o 3, de tal forma que la suma de a y b es 2, 3 o 4; el anillo A representa un arilo de 6-10 miembros, un heteroarilo de 5-13 miembros o un grupo heterocíclico parcialmente aromático, conteniendo dicho heteroarilo y dicho grupo heterocíclico parcialmente aromático al menos un heteroátomo seleccionado entre O, S, S(O), S(O)2, y N, y conteniendo opcionalmente 1 heteroátomo diferente seleccionado entre O y S, y conteniendo opcionalmente 1-3 átomos N adicionales, estando presentes hasta 5 heteroátomos; cada R2 y R3 es independientemente H, alquilo C1-3, haloalquilo C1-3, O-alquilo C1-3, haloalcoxi C1-3, OH o F; n representa un numero entero de 1 a 5; cada R4 es H o se selecciona independientemente entre halo y R6; R5 representa -CO2H, un resto de formula (2) o -C(O)NHSO2Re donde Re representa alquilo C1-4 o fenilo, estando dicho alquilo C1-4 y dicho fenilo opcionalmente sustituidos con 1-3 grupos, 1-3 de los cuales se seleccionan entre halo, y alquilo C1-3, y 1-2 de los cuales se seleccionan entre el grupo constituido por: O-alquilo C1- 3, haloalquilo C1-3, haloalcoxi C1-3, OH, NH2 y NH-alquilo C1-3; y cada R1 es H o se selecciona independientemente entre el grupo constituido por: a) halo, OH, CO2H, CN, NH2, S(O)0-2Re, C(O)Re, OC(O)Re y CO2Re, donde Re es como se ha definido anteriormente; b) alquilo C1-6 y O-alquilo C1-6, estando dicho alquilo C1-6 y dicha porcion alquilo del O-alquilo C1-6 opcionalmente sustituidos con 1-3 grupos, 1-3 de los cuales son halo y 1-2 de los cuales se seleccionan entre: OH, CO2H, CO2alquilo C1-4, CO2haloalquilo C1-4, OCO2alquilo C1-4, NH2, NH-alquilo C1-4, N(alquilo C1-4)2, Hetci y CN; c) NH-alquilo C1-4 y N(alquilo C1-4)2, cuyas porciones alquilo están opcionalmente sustituidas como se ha indicado anteriormente en (b); d) C(O)NH2, C(O)NH-alquilo C1-4, C(O)N(alquilo C1-4)2, C(O)Hetci, C(O)NHO-alquilo C1-4 y C(O)N(alquilo C1-4)(O-alquilo C1-4), cuyas porciones alquilo están opcionalmente sustituidas como se ha indicado anteriormente en (b); e) NR'C(O)Rö, NR'SO2Rö, NR'CO2Rö y NR'C(O)NRöR'ö donde: R' representa H, alquilo C1-3 o haloalquilo C1-3, Rö representa (a) alquilo C1-8 opcionalmente sustituido con 1-4 grupos, 0-4 de los cuales son halo, y 0-1 de los cuales se seleccionan entre el grupo constituido por: O-alquilo C1-6, OH, CO2H, CO2alquilo C1-4, CO2haloalquilo C1-4, NH2, NH-alquilo C1-4, N(alquilo C1-4)2, CN, Hetci, Arilo y HAR, estando dichos grupos Hetci, Arilo y HAR opcionalmente sustituidos adicionalmente con 1-3 grupos halo, alquilo C1-4, alcoxi C1-4, haloalquilo C1-4 o haloalcoxi C1-4; (b) Hetci, Arilo o HAR, estando cada uno opcionalmente sustituido con 1-3 miembros seleccionados entre el grupo constituido por: grupos halo, alquilo C1-4, alcoxi C1-4, haloalquilo C1-4 y haloalcoxi C1-4; y R'ö que representa H o Rö; f) fenilo o un heteroarilo de 5-6 miembros o un grupo Hetci unido en cualquier átomo disponible del anillo y estando cada uno opcionalmente sustituido con 1-3 grupos, 1-3 de los cuales se seleccionan entre grupos halo, alquilo C1-3 y haloalquilo C1-3, y 1-2 de los cuales se seleccionan entre grupos O-alquilo C1-3 y halo-O-alquilo C1-3, y 0-1 de los cuales se seleccionan entre el grupo constituido por: i) OH, CO2H, CN, NH2 y S(O)0-2Re donde Re es como se ha descrito anteriormente; ii) NH-alquilo C1-4 y N(alquilo C1-4)2, cuyas porciones alquilo están opcionalmente sustituidas con 1-3 grupos, 1-3 de los cuales son halo y 1-2 de los cuales se seleccionan entre: OH. CO2H, CO2alquilo C1-4, CO2haloalquilo C1- 4, NH2, NH-alquilo C1-4, N(alquilo C1-4)2 y CN; iii) C(O)NH2, C(O)NH-alquilo C1-4, C(O)N(alquilo C1-4)2, C(O)NHO-alquilo C1-4 y C(O)N(alquilo C1-4)(O-alquilo C1-4), cuyas porciones alquilo están opcionalmente sustituidas como se ha indicado anteriormente en b); y iv) NR'C(O)Rö, NR'SO2Rö, NR'CO2Rö y NR'C(O)NRöR'ö donde R', Rö y R'ö son como se ha descrito anteriormente.
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