AR035440A1 - Compuestos antagonistas del receptor h3, el uso de los mismos solos o en combinacion para la manufactura de medicamentos y composiciones farmaceuticas - Google Patents

Compuestos antagonistas del receptor h3, el uso de los mismos solos o en combinacion para la manufactura de medicamentos y composiciones farmaceuticas

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Publication number
AR035440A1
AR035440A1 ARP020100884A ARP020100884A AR035440A1 AR 035440 A1 AR035440 A1 AR 035440A1 AR P020100884 A ARP020100884 A AR P020100884A AR P020100884 A ARP020100884 A AR P020100884A AR 035440 A1 AR035440 A1 AR 035440A1
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Argentina
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alkyl
aryl
independently selected
phenyl
ring
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ARP020100884A
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English (en)
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Pharmacopeia Drug Discovery
Schering Corp
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Application filed by Pharmacopeia Drug Discovery, Schering Corp filed Critical Pharmacopeia Drug Discovery
Publication of AR035440A1 publication Critical patent/AR035440A1/es

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Abstract

Un compuesto no imidazol, donde comprende la fórmula (1) o una sal o solvato farmacéuticamente aceptable del mismo, en el cual (A) R1 está seleccionado entre: arilo, heteroarilo, heterocicloalquilo, alquilo, -C(O)N(R4B)2, cicloalquilo, arilalquilo, heteroarilheteroarilo; o un grupo seleccionado de: fórmulas (2), (3), (4), (4A), (4B), (4C), (4D), dichos arilo, heteroarilo, porción arilo de arilalquilo, anillo fenilo de fórmula (2), anillo fenilo de fórmula (3), anillos fenilo de fórmula (4B), o anillos fenilo de fórmula (4D) están opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados de: halógeno, hidroxilo, alcoxi inferior, O arilo, -SR22, -CF3, -OCF3, -OCHF2, -NR4R5, fenilo, -NO2, -CO2R4, -CON(R4)2 donde cada R4 es igual o diferente, -S(O)2R22, -S(O)2N(R20)2 donde cada R20 es igual o diferente, -N(R24)S(O)2R22, -CN, -CH2OH, -OCH2CH2OR22, alquilo, fenilo sustituido donde dicho fenilo tiene de 1 a 3 sustituyentes independientemente seleccionados entre alquilo, halógeno, -CN, -NO2, -OCHF2, -O alquilo, O alquilarilo donde dicho grupo arilo está opcionalmente sustituido con 1 a 3 halógenos independientemente seleccionados; o fenilo; (B) X está seleccionado entre alquilo o -S(O)2-; (C) (1)Y representa: un enlace simple, o (2)Y está seleccionado entre -C(O)-, -C(S)-, -(CH2)q-, o -NR4C(O)-, con las condiciones de que: (a) cuando M1 es N, entonces Y no es -NR4C(O)-, y (b) cuando Y es un enlace, entonces M1 y M2 son ambos carbono; (D) M1 y M2 están independientemente seleccionados de C o N; (E) Z está seleccionado entre: alquilo C1-6, -SO2-, -C(O)- o -C(O)NR4-; (F) R2 está seleccionado entre: (1) un anillo heteroarilo de 6 miembros que tiene 1 o 2 heteroátomos independientemente seleccionados entre N o N-O, siendo los átomos de anillo remanentes carbono; (2) un anillo heteroarilo de 5 miembros que tiene 1 a 3 heteroátomos seleccionados entre nitrógeno, oxígeno, o azufre siendo los átomos de anillo remanentes carbono; o (3) un grupo alquilo; (4) un grupo arilo donde dicho fenilo sustituido está sustituido con 1 a 3 sustituyentes independientemente seleccionados entre: halógeno, -O alquilo, -OCF3, -CF3, -CN, -NO2, -NHC(O)CH3, u -(CH2)qN(R10A)2; (5) -N(R11A)2 donde cada R11A está independientemente seleccionado entre: H, alquilo o arilo; (6) un grupo de la fórmula (5); o (7) un grupo heteroarilheteroarilo; donde dicho anillo heteroarilo de 5 miembros (((F)(2) anterior) o anillo heteroarilo de 6 miembros ((F)(1)anterior) está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados entre; halógeno, hidroxilo, alquilo inferior, alcoxi inferior, -CF3, -NR4R5, fenilo, -NO2, -C(O)N(R4)2 (donde cada R4 es igual o diferente), -C(O)2R4, o fenilo sustituido con 1 a 3 sustituyentes independientemente seleccionados entre: halógeno, -O alquilo, -OCF3, -CF3, -CN, -NO2 u -O(CH2)qN(R10A)2; (G) R3 está seleccionado entre: arilo, heteroarilo, heterocicloalquilo, alquilo, o cicloalquilo, donde dichos grupos R3 arilo o heteroarilo están opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados entre: halógeno, hidroxilo, alcoxi inferior, -O arilo, -SR22, -CF3, -OCF3, -OCHF2, -NR4R5, fenilo, -NO2, -CO2R4, -CON(R4)2 donde cada R4 es igual o diferente, -S(O)2R22, -S(O)2N(R20)2 donde cada R20 es igual o diferente, -N(R24)S(O)2R22, -CN, -CH2OH, -OCH2CH2OR22, o alquilo; (H) R4 está seleccionado de: hidrógeno, alquilo C1-6, cicloalquilo, cicloalquilalquilo, heterocicloalquilalquilo, un anillo cicloalquilo bicíclico puenteado, arilo que tiene un anillo heterocicloalquilo fusionado unido a dicho anillo arilo, arilo, arilalquilo, alquilarilo, -(CH2)d(CH(R12A)2 donde d es 1 a 3 y cada R12A está independientemente seleccionado entre fenilo o fenilo sustituido, estando dicho fenilo sustituido con 1 a 3 sustituyentes independientemente seleccionados de: halógeno, -O alquilo, -OCF3, -CF3, -CN, o -NO2, heterocicloalquilheteroarilo, o alquileno C1-6 -O-R22, donde el grupo R4 arilo, la porción arilo del grupo R4 arilalquilo, o la porción arilo del grupo R4 alquilarilo está opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de: halógeno, hidroxilo, alquilo inferior, alcoxi inferior, -CF3, -N(R20)R24), fenilo, -NO2, -C(O)N(R20)2 (donde cada R20 es igual o diferente), -C(O)R22, -(CH2)k-cicloalquilo, -(CH2)q-arilo, o -(CH2)m-OR22; (I) cada R4B esta independientemente seleccionado entre: H, heteroarilo, alquilo, alquenilo, un grupo de la fórmula (6), arilalquilo, o arilalquilo donde la porción arilo está sustituido con 1-3 sustituyentes independientemente seleccionados de: halógeno; (J) R5 está seleccionado entre: hidrógeno, alquilo C1-6, -C(O)R20, -C(O)2R20, -C(O)N(R20)2 (donde cada r20 es igual o diferente); (K) cada R10A esta independientemente seleccionado entre H o alquilo C1-6, o cada R10A tomado conjuntamente con el átomo de nitrógeno al cual están unidos forma un anillo heterocicloalquilo de 4 a 7 miembros; (L) R12 está: (1) seleccionado entre alquilo, hidroxilo, alcoxi, o flúor, con la condición de que cuando R12 es hidroxi o flúor entonces R12 no está unido a un carbono adyacente a un nitrógeno; o (2) R12 forma un puente alquilo a partir de un carbono del anillo a otro carbono del anillo; (M) R13 está: (1) seleccionado entre alquilo, hidroxilo, alcoxi, o flúor, con la condición de que cuando R13 es hidroxi o flúor entonces R13 no está unido a un carbono adyacente a un nitrógeno; o (2) R13 forma un puente alquilo a partir de un carbono del anillo a otro carbono del anillo; (N) R20 está seleccionado entre hidrógeno, alquilo, o arilo, donde dicho grupo arilo está opcionalmente sustituido con desde 1 a 3 grupos independientemente seleccionados entre: halógeno, -CF3, -OCF3, hidroxilo, o metoxi; o cuando dos grupos R20 están presentes dichos dos grupos R20 tomados conjuntamente con el nitrógeno al cual están unidos forman un anillo heterocíclico de 5 a 6 miembros; (O) R22 está seleccionado entre: heterocicloalquilo, alquilo o arilo, donde dicho grupo arilo está opcionalmente sustituido con 1 a 3 grupos independientemente seleccionados entre halógeno, -CF3, -OCF3, hidroxilo, o metoxi; (P) R24 está seleccionado entre: hidrógeno, alquilo, -SO2R22, o arilo, donde dicho grupo arilo está opcionalmente sustituido con 1 a 3 grupos independientemente seleccionados entre halógeno, -CF3, -OCF3, hidroxilo, o metoxi; (Q) a es 0 a 2; (R) b es 0 a 2; (S) k es 1 a 5; (T) m es 2 a 5; (U) n es 1, 2 o 3 con la condición de que cuando M1 es N, entonces n no es 1; (V) p es 1, 2, o 3 con la condición de que cuando M2 es N, entonces p no es 1; (W) q es 1 a 5; y (X) r es 1, 2, o 3 con la condición de que cuando r es 2 o 3, entonces M2 es C y p es 1; el uso de los mismos, solos o en combinación de un antagonista del receptor H1 para la manufactura de medicamentos para varias enfermedades o alergia, respuestas de las vías respiratorias inducidas por alergia, congestión, hipotensión, enfermedad cardiovascular, enfermedad del tracto GI, hiper e hipo motilidad y secreción ácida del tracto gastro-intestinal, obesidad, desórdenes del sueno, desórdenes del sistema nervioso central, desórdenes de hiperactividad con déficit de atención, hipo e hiperactividad del sistema nervioso central, enfermedad de Alzheimer, esquizofrenia, migrana y composiciones farmacéuticas.
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