AR055041A1 - Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas. - Google Patents

Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas.

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Publication number
AR055041A1
AR055041A1 ARP060100953A ARP060100953A AR055041A1 AR 055041 A1 AR055041 A1 AR 055041A1 AR P060100953 A ARP060100953 A AR P060100953A AR P060100953 A ARP060100953 A AR P060100953A AR 055041 A1 AR055041 A1 AR 055041A1
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Argentina
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alkyl
group
atoms
substituted
membered aromatic
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ARP060100953A
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Merck Frosst Canada Ltd
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Application filed by Merck Frosst Canada Ltd filed Critical Merck Frosst Canada Ltd
Publication of AR055041A1 publication Critical patent/AR055041A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

Composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de formula estructural (1) y las sales, ésteres y solvatos farmacéuticamente aceptables de la misma, en los que: -------- se selecciona de un enlace simple y un enlace doble; ôAö se selecciona a partir de un grupo que consta de (a) un anillo aromático de 5 miembros que contiene (i) uno o más átomos de C, (ii) un heteroátomo seleccionado a partir de O y S, y (iii) 0, 1, 2 o 3 átomos de N; (b) un anillo aromático de 5 miembros que contiene uno o más átomos de C y de uno a cuatro átomos de N, (c) un anillo aromático de 6 miembros que contiene átomos de C y 1, 2 o 3 átomos de N; (d) un sistema anillo bicíclico seleccionado de benzotienilo, indolilo, quinolinilo y naftalenilo; (e) fenilo, y (f) -CH2-fenil; y en los que A está opcionalmente mono- o di-sustituida con un sustituyente independientemente seleccionado en cada aparicion del grupo consistente en (i) -F, (ii) -Cl, (iii) -alquilo C1-3 opcionalmente sustituido con uno o más grupos halo, (iv) -Oalquil C1-3 opcionalmente sustituido con uno o más grupos halo, (v) -Ocicloalquil C3-6, (vi) -CH2OH, (vii) -COOR1, (viii) -CN y (ix) -NR10R11; X se selecciona de -O- y -S-; Y se selecciona de (a) -NR6- CHR7 y -NR8-C(O)- en los que el N en Y está unido al resto heterocíclico de 5 miembros de formula (1) y el C en Y está unido al resto heterocíclico bicíclico de formula (1), (b) -S- y (c) -O-; R1 se selecciona del grupo consistente en - H, alquil C1- 6 y -cicloalquil C3-6; R2 se selecciona del grupo consistente en -H, -OH, -F, -alquil C1-3, -Oalquil C1-3 y -OC(O)-alquil C1-3; R3 se selecciona del grupo consistente en -H, -alquil C1-6, -alquil C1-6 sustituido con uno o más grupos fluoro, -alquil C1-6 sustituido con R9, -alquenil C2-6, -cicloalquil C3-6, -cicloalquenil C5-7 y -Z; R4 se selecciona del grupo consistente en -H, -alquil C1-6, -alquil C1-6 sustituido con uno o más grupos fluoro, -alquil C1-6 sustituido con R9, -alquenil C2-6, - cicloalquil C3-6, -cicloalquenil C5-7 y -Z; o R3 y R4 representan conjuntamente oxo; o R3 y R4 se articulan conjuntamente con el C al cual están unidos para formar un anillo seleccionado del grupo consistente en un anillo - cicloalquil C3-6 y un anillo -cicloalquenil C5-7, dado que cuando R3 y R4 se articulan conjuntamente con el C al cual están unidos para formar un anillo -cicloalquenil C5-7, no hay doble enlace en la posicion C-1 en el anillo; o R2, R3 y R4 se articulan conjuntamente con el C al cual están unidos para formar un anillo cicloalquenilo seleccionado de las formulas (2), R5 está ausente o es un sustituyente seleccionado a partir del grupo consistente en -alquil C1-6, cicloalquil C3-6 y halo; R6 se selecciona del grupo consistente en (a) -H, (b) -alquil C1-4, (c) -C(O)alquil C1-4 y (d) -C(O)fenil opcionalmente sustituido con -alquil C1-4; R7 se selecciona del grupo consistente en (a) -h, (b) alquilo C1-4, (c) -cicloalquil C3-6 y (d) fenilo opcionalmente mono- o di- sustituido con un sustituyente independientemente seleccionado en cada aparicion del grupo consistente en -alquil C1-4, -F y -Cl, y (e) un anillo aromático de 5 miembros que contiene (i) uno o más átomos de C, (ii) un heteroátomo seleccionado a partir de O y S; y (iii) 0, 1, 2 o 3 átomos de N; R8 se selecciona del grupo consistente en -H y -alquil C1-4; R9 se selecciona del grupo consistente en -COOR1, -C(O)H, -CN, -CR1R1OH, -OR1, -S-alquil C1-6 y -S-cicloalquil C3-6; R10 se selecciona del grupo consistente en -H, - alquil C1-6, -cicloalquil C3-6 y -COOR1; R11 se selecciona del grupo consistente en -H, -alquil C1-6 y -cicloalquil C3-6; y Z se selecciona del grupo consistente en (a) un anillo aromático de 5 miembros que contiene (i) uno o más átomos de C, (ii) un heteroátomo seleccionado a partir de O y S, y (iii) 0, 1, 2 o 3 átomos de N; (b) un anillo aromático de 5 miembros que contiene uno o más átomos de C y de uno a cuatro átomos de N, (c) un anillo aromático de 6 miembros que contiene átomos de C y 1, 2 o 3 átomos de N; (d) fenilo, y (e) -CH2-fenil y -CH2-dioxolanil, y en el que Z está opcionalmente mono- o di-sustituida con un sustituyente independientemente seleccionado en cada aparicion del grupo consistente en (i) - F, (ii) -Cl, (iii) -alquil C1-3 opcionalmente sustituido con uno o más grupos halo que incluye por ejemplo -CF3, (iv) -Oalquil C1-3 opcionalmente sustituido con uno o más grupos halo, (v) -Ocicloalquil C3-6, (vi) -CH2OH, (vii) -COOR1, (viii) -CN y (ix) -NR10R11.
ARP060100953A 2005-03-23 2006-03-13 Tiadiazoles y oxadiazoles como inhibidores de la sintesis de leucotrienos. composiciones farmaceuticas. AR055041A1 (es)

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US (3) US20090227638A1 (es)
EP (1) EP1869031B1 (es)
JP (2) JP4109316B1 (es)
KR (1) KR20070113259A (es)
CN (2) CN102627638A (es)
AR (1) AR055041A1 (es)
AU (1) AU2006227524B2 (es)
BR (1) BRPI0609687A2 (es)
CA (1) CA2600727C (es)
CR (1) CR9442A (es)
DO (1) DOP2006000069A (es)
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IL (1) IL185724A0 (es)
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AU2006299671A1 (en) * 2005-10-05 2007-04-12 Merck Frosst Canada Ltd Substituted quinolines as inhibitors of leukotriene biosynthesis
AR065093A1 (es) * 2007-02-05 2009-05-13 Merck Frosst Canada Ltd Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos
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