AR075835A1 - Compuestos bis-aromaticos para su uso como inhibvidores de ltc4 sintasa - Google Patents

Compuestos bis-aromaticos para su uso como inhibvidores de ltc4 sintasa

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Publication number
AR075835A1
AR075835A1 ARP100100797A ARP100100797A AR075835A1 AR 075835 A1 AR075835 A1 AR 075835A1 AR P100100797 A ARP100100797 A AR P100100797A AR P100100797 A ARP100100797 A AR P100100797A AR 075835 A1 AR075835 A1 AR 075835A1
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Argentina
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optionally substituted
substituents selected
alkyl
independently represent
hydrogen
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ARP100100797A
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Peter Nilsson
Benjamin Pelcman
Martins Katkevics
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Biolipox Ab
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Publication of AR075835A1 publication Critical patent/AR075835A1/es

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Abstract

Dichos compuestos son de utilidad en el tratamiento de enfermedades en donde se desea, y/o requiere inhibir la leucotrieno C4 sintasa y, en particular, en el tratamiento de un trastorno respiratorio y/o de una inflamacion. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula 1, donde uno de E2a, E2b y E2c representa -C(-L3-Y3)= y los otros dos respectivamente representan E2 y E3; Y representa -C(O)- o -C(=N-OR28)-; R28 representa hidrogeno o C1-6 alquilo opcionalmente sustituido con uno o más átomos de fluor; uno o dos de D1, D2 y D3 representa(n) -N=; y/o uno o dos de E1, E2, E3 y E4 representa(n) -N=; y los demás grupos D1, D2 y D3 representan cada uno en forma independiente -C(R1)=; y los demás grupos E1, E2, E3 y E4 representan cada uno en forma independiente -C(R2)=; cada R1 representa en forma independiente, en cada ocasion en que se lo usa en la presente, hidrogeno o un sustituyente seleccionado entre X1; cada R2 representa en forma independiente, en cada ocasion en que se lo usa en la presente, hidrogeno o un sustituyente seleccionado entre X2; Y1 representa -C(O)OR9a o 5-tetrazolilo; R9a representa: (i) hidrogeno; o (ii) C1-8 alquilo o un grupo heterocicloalquilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre G1 y/o Z1; uno de Y2 e Y3 representa un grupo arilo o un grupo heteroarilo (de los cuales ambos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre A) y el otro representa: (a) un grupo arilo o un grupo heteroarilo (de los cuales ambos grupos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre A); o (b) C1-12 alquilo o un grupo heterocicloalquilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre G1 y/o Z1; A representa, en cada ocasion en que se lo usa en la presente: I) un grupo arilo o un grupo heteroarilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre B; II) C1-8 alquilo o un grupo heterocicloalquilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre G1 y/o Z1; o III) un grupo G1; X1, X2, G1 y B representan en forma independiente halo, -R5a, -C(O)R5b, -CN, -NO2, -C(O)N(R6a)R7a, -N(R6b)R7b, -N(R5c)C(O)R6c, -N(R5b)C(O)OR6d, -OR5e, -OS(O)2R5f, -S(O)mR5g, -OC(O)R5h o -S(O)2N(R6e)R7e; R5b a R5e, R5g, R5h, R6a a R6c, R6e, R7a, R7b y R7e representan en forma independiente, en cada ocasion en que se lo usa en la presente, H o R5a; o cualquiera de los pares R6a y R7a, R6b y R7b, o R6e y R7e se pueden unir para formar, junto con el o los átomos a los cuales se encuentran unidos, un anillo de 3 a 6 miembros, cuyo anillo contiene opcionalmente un heteroátomo adicional (como por ejemplo nitrogeno u oxigeno) además del átomo de nitrogeno al cual estos sustituyentes se encuentran necesariamente unidos, y cuyo anillo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro, =O, -OR y/o R5a; R5f y R6d representan en forma independiente R5a; R5a representa, en cada ocasion en que se lo usa en la presente: (i) C1-6 alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro, -CN, =O, -OR8a, -N(R8b)R8c, -S(O)nR8d y/o -S(O)2N(R8e)R8f; o (ii) arilo o heteroarilo, de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre halo, -CN, -OR8a, -N(R8b)R8C, -S(O)nR8d y/o -S(O)2N(R8e)R8f; n representa 0, 1 o 2; cada R8a, R8b, R8d y R8d representa en forma independiente H o C1-6 alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro, =O, -OR11a y/o -N(R12a)R12b; cada R8c y R8f representa en forma independiente H o C1-3 alquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre F, =O, -OR13a, -N(R14a)R14b, -S(O)2CH3, -S(O)-2CHF2 y/o -S(O)2CF3; o R8b y R8c y/o R8e y R8f se pueden unir para formar, junto con el o los átomos a los cuales se encuentran unidos, un anillo de 3 a 6 miembros, opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro y C1-2 alquilo; R11a y R13a representan en forma independiente H o C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; R12a, R12b, R14a y R14b representan en forma independiente H, -CH3 o -CH2CH3; Z1 representa, en cada ocasion en que se lo usa en la presente, =O o =NOR16b; representa hidrogeno o C1-6 alquilo opcionalmente sustituido con uno o más átomos de fluor; L1 representa una union simple o -(CH2)p-Q-(CH2)q-; Q representa -C(Ry1)(Ry2)-, -C(O)-, -N(Ry3)- o -O-; p y q representan en forma independiente 0, 1 o 2, pero donde la suma de p y q no excede 2; L2 y L3 representan en forma independiente una union simple o un grupo separador seleccionado entre -S(O)n1-, -C(Ry4)(Ry5)-, -N(R17a)-A16-, -OA17- y -C(O)-A17; n1 representa 0, 1 o 2; A16 representa una union directa, -C(Ry6)(Ry7)-, -C(O)-, C(O)N(R17b), -C(O)C(Ry6)(Ry7)- o -S(O)2-; A17 representa una union directa o -C(Ry8)(Ry9)-; cada Ry1, Ry2, Ry4, Ry5, Ry6, Ry7, Ry8 y Ry9 representa en forma independiente H, fluoro o C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; o Ry1, Ry2, Ry4, Ry5, Ry6, Ry7, Ry8 y Ry9 pueden estar unidos para formar un anillo de 3 a 6 miembros opcionalmente sustituido con uno o más sustituyentes seleccionados entre fluoro y C1-2 alquilo; Ry3 representa hidrogeno o C1-3 alquilo; R17a y R17b representan en forma independiente hidrogeno, C1-6 alquilo (opcionalmente sustituido con uno o más sustituyentes seleccionados entre heterocicloalquilo, arilo, fluoro, -CN, -OR19 y/o =O), arilo o heteroarilo (de los cuales ambos están opcionalmente sustituidos con uno o más sustituyentes seleccionados entre halo, -R18a, -C(O)R18b, -CN, -C(O)N(R18c)R18d, -N(R18e)R18f, -N(R18g)C(O)R18h, -N(R18i)C(O)OR18j, -OR18k, -OS(O)2R18m, -S(O)mR18n, -OC(O)R18p y/o -S(O)2N(R18q)(R18r); m representa 0, 1 o 2; R18a, R18b, R18C, R18d, R18e, R18f, R18g, R18h, R18i, R18k, R18n, R18p, R18q y R18r representan en forma independiente hidrogeno o C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; R18j y R18m representan en forma independiente C1-3 alquilo opcionalmente sustituido con uno o más átomos de fluor; R19 representa hidrogeno o C1-6 alquilo opcionalmente sustituido con uno o más átomos de fluor; o una sal aceptable farmacéuticamente del mismo.
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