AR059026A1 - Derivados triazolicos como ligandos analogos de ghrelina de receptores secretagogos de la hormona de crecimiento.composiciones farmaceuticas - Google Patents

Derivados triazolicos como ligandos analogos de ghrelina de receptores secretagogos de la hormona de crecimiento.composiciones farmaceuticas

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Publication number
AR059026A1
AR059026A1 ARP060103531A ARP060103531A AR059026A1 AR 059026 A1 AR059026 A1 AR 059026A1 AR P060103531 A ARP060103531 A AR P060103531A AR P060103531 A ARP060103531 A AR P060103531A AR 059026 A1 AR059026 A1 AR 059026A1
Authority
AR
Argentina
Prior art keywords
alkyl
arylalkyl
aryl
group
heteroarylalkyl
Prior art date
Application number
ARP060103531A
Other languages
English (en)
Original Assignee
Zentaris Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35589641&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR059026(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Zentaris Gmbh filed Critical Zentaris Gmbh
Publication of AR059026A1 publication Critical patent/AR059026A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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Abstract

Derivados triazolicos como ligandos análogos de ghrelina de receptores secretagogos de la hormona de crecimiento de acuerdo con la formula (1) que son utiles en el tratamiento o la profilaxis de afecciones fisiologicas y/o patofisiologicas en mamíferos, con preferencia humanos, que están mediadas por los receptores GHS. Además antagonistas del receptor GHS y agonistas que pueden usarse para la modulacion de estos receptores y son utiles para tratar las afecciones anteriores, en particular retraso en el crecimiento, caquexia, regulacion a corto, mediano y/o largo plazo del balance de energía; regulacion a corto, mediano y/o largo plazo (estimulacion y/o inhibicion) de la ingesta de alimentos; adipogénesis, adiposidad y/u obesidad; aumento y/o reduccion del peso corporal; diabetes, diabetes tipo I, diabetes tipo II, proliferacion de células tumorales; inflamacion, efectos inflamatorios, íleo gástrico post-operatorio, íleo post-operatorio y/o gasterectomía (terapia de reemplazo de ghrelina)ö. Reivindicacion 1: El uso de un compuesto de acuerdo con la formula (1) donde R1 y R2 se seleccionan, en forma independiente uno del otro, del grupo que consiste en ôátomo de hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, alquilsulfonilo, arilsulfonilo, arilalquilsulfoniloö que están sustituidos en forma opcional en el grupo alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo y/o heterociclilalquilo por hasta 3 sustituyentes seleccionados en forma independiente del grupo que consiste en ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, - OH, -NO2, alquilo, arilo, arilalquilo, -O-alquilo, -O-arilo, -O-arilalquiloö; y con preferencia se seleccionan del grupo que consiste en ôalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquiloö en forma opcional están sustituidos por hasta 3 sustituyentes seleccionados en forma independiente del grupo que consiste en ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alquilo, arilo, arilalquilo, -O-alquilo, -O-arilo, -O-arilalquiloö; uno de los radicales R3 y R4 es un átomo de hidrogeno, mientras que el otro radical se selecciona del grupo que consiste en ôátomo de hidrogeno, alquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, -alquil-O-arilo, -alquil-O-arilalquilo, -alquil-O- heteroarilo, -alquil-O-heteroarilalquilo, -alquil-O-heterociclilo, alquil-O-heterociclilalquilo, -alquil-CO-arilo, -alquil-CO-arilalquilo, alquil-CO-heteroariIo, alquil-CO-heteroarilalquilo, -alquil-CO-heterociclilo, -alquil-CO-heterociclilalquilo, - alquil-C(O)O-arilo, -alquil-C(O)O-arilalquilo, -alquil-C(O)O-heteroarilo, -alquil-C(O)O-heteroarilalquilo, -alquil-C(O)O-heterociclilo, alquil-C(O)O-heterociclilalquilo, -alquil-CO-NH2, - alquil-CO-OH, -alquil-NH2, -alquil-NH-C(NH)-NH2, alquilsulfonilo, arilsulfonilo, arilalquilsulfonilo, alquil-S-alquilo, alquil-S-Hö que están sustituidos en forma opcional en el grupo arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo y/o heterociclilalquilo por hasta 3 sustituyentes seleccionados en forma independiente del grupo que consiste en ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alquilo, arilo, arilalquilo, -O-alquilo, -O-arilo, -O-arilalquiloö y con preferencia se seleccionan del grupo que consiste en ôarilalquilo, heteroarilalquilo, heterociclilalquilo, -alquil-O-arilo, -alquil-O-arilalquilo, -alquil-O-heteroarilo, -alquil-O-heteroarilalquilo, -alquil-O-heterociclilo, alquil-O-heterociclilalquilo, -alquil-CO-arilo, -alquil-CO- arilalquilo, alquil-CO-heteroariIo, alquil-CO-heteroarilalquilo, -alquil-CO-heterociclilo, -alquil-CO-heterociclilalquilo, -alquil-C(O)O-arilo, -alquil-C(O)O-arilalquilo, -alquil-C(O)O-heteroarilo, -alquil-C(O)O-heteroarilalquilo, -alquil-C(O)O- heterociclilo, alquil-C(O)O-heterociclilalquilo, -alquil-CO-NH2, - alquil-CO-OH, -alquil-NH2, -alquil-NH-C(NH)-NH2ö, en forma opcional están sustituidos en el grupo arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo y/o heterociclilalquilo por hasta 3 sustituyentes seleccionados en forma independiente del grupo que consiste en ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alquilo, arilo, arilalquilo, -O-alquilo, -O-arilo, -O-arilalquiloö; R5 se selecciona del grupo que consiste en ôátomo de hidrogeno, alquilo, cicloalquilo, cicloalquilalquilo, arilo, heteroarilo, arilalquilo, heteroarilalquilo, heterociclilo, heterociclilalquilo, -CO-alquilo, -CO-cicloalquilo, -CO-cicloalquilalquilo, -CO- arilo, -CO-arilalquilo, -CO-heteroarilo, -CO-heteroarilalquilo, -CO-heterociclilo, -CO-heterociclilalquilo, -CO-C*(R9R10)-NH2, -CO-CH2-C*(R9R10)-NH2, -CO-C*(R9R10)-CH2-NH2, alquilsulfonilo, arilsulfonilo, arilalquilsulfoniloö que están sustituidos en forma opcional por hasta 3 sustituyentes seleccionados en forma independiente del grupo que consiste en ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alquilo, arilo, arilalquilo, -O-alquilo, -O-arilo, -O-arilalquiloö y con preferencia se selecciona del grupo que consiste en ôátomo de hidrogeno, -CO-alquilo, -CO-cicloalquilo, -CO-arilo, -CO-heteroarilo, -CO-arilalquilo, -CO- heteroarilalquilo, -CO-heterociclilo, -CO-C*(R9R10)-NH2, -CO-CH2-C*(R9R10)-NH2, -CO-C*(R9R10)-CH2-NH2, en forma opcional están sustituidos por hasta 3 sustituyentes seleccionados en forma independiente del grupo que consiste en ôhalogeno, -F, -CI, -Br, -I, -N3, -CN, -NR7R8, -OH, -NO2, alquilo, arilo, arilalquilo, -O-alquilo, -O-arilo, -O-arilalquiloö; R6 se selecciona del grupo que consiste en ôátomo de hidrogeno, alquilo, cicloalquilo, cicloalquilalquiloö y con preferencia es un átomo de hidrogeno; R7 y R8 se seleccionan, en forma independiente uno del otro, del grupo que consiste en ô átomo de H, alquilo, cicloalquilo, cicloalquilalquiloö y con preferencia son un átomo de H; R9 y R10 se seleccionan, en forma independiente uno del otro, del grupo que consiste en ôátomo de hidrogeno, alquilo, cadena lateral de alfa-aminoácido natural, cadena lateral de alfa-aminoácido no naturalö y con preferencia se seleccionan del grupo que consiste en ôátomo de hidrogeno, alquiloö; m es 0, 1 o 2 y con preferencia es 0; y * significa un átomo de carbono de configuracion R o S cuando es quiral; para la fabricacion de un medicamento para el tratamiento o la profilaxis de afecciones fisiologicas y/o patofisiologicas en mamíferos que están mediadas por los receptores GHS.
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