AR065133A1 - Derivados de tetrahidroisoquinolina, composiciones farmaceuticas que los contienen y usos de los mismos para tratar o prevenir enfermedades o trastornos asociados a la actividad de gpr119, tales como diabetes, obesidad y trastornos cardiovasculares, entre otros. - Google Patents

Derivados de tetrahidroisoquinolina, composiciones farmaceuticas que los contienen y usos de los mismos para tratar o prevenir enfermedades o trastornos asociados a la actividad de gpr119, tales como diabetes, obesidad y trastornos cardiovasculares, entre otros.

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AR065133A1
AR065133A1 ARP080100423A ARP080100423A AR065133A1 AR 065133 A1 AR065133 A1 AR 065133A1 AR P080100423 A ARP080100423 A AR P080100423A AR P080100423 A ARP080100423 A AR P080100423A AR 065133 A1 AR065133 A1 AR 065133A1
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Argentina
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alkyl
halo
substituted
aryl
independently selected
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ARP080100423A
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Irm Llc
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Publication of AR065133A1 publication Critical patent/AR065133A1/es

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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07D217/08—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
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    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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Abstract

Reivindicacion 1: Un compuesto de formula (1) en la cual: B se selecciona de arilo C6-10, heteroarilo C1-10 cicloalquilo C3-12 y heterocicloalquilo C3-8; donde dicho arilo, heteroarilo, cicloalquilo o heterocicloalquilo de B está sustituido con uno a tres radicales seleccionados de -R3 y -OXaR3; donde Xa se selecciona de un enlace y alquileno C1-3; y donde cualquier heterocicloalquilo de B puede tener a CH2 grupo reemplazado con C(O); n y p se seleccionan independientemente de 0, 1, 2 y 3; q se selecciona de 0, 1 y 2; m se selecciona de 1, 2 y 3; L es -X1-A-X2-B1-X3-; donde A y B1 se seleccionan independientemente de un enlace, -O-, -S(O)0-2-, -C(O)-, -C(O)O-, -OC(O)-, -NR4-, -C(O)NR4-, -C(S)NR4, -NR4C(O)-, -CR4(NR4C(O)R4)-, -C(=NOR4)-, -CR4(NR4R4)-, -CR4(OR4)-, -CR4R4C(O)OR4-, -N(C(O)R4)- y -NR4C(S)-; donde X1, X2 y X3 se seleccionan independientemente de un enlace, alquileno C1-6, alquenileno C2-6, cicloalquilo C3-8, arilo C6-10, heterocicloalquilo C3-8 y heteroarileno C1-6; donde dicho cicloalquilo, arilo, heterocicloalquilo o heteroarilo de L pueden estar opcionalmente sustituidos con hasta 3 radicales independientemente seleccionados de hidroxilo, halo, alquilo C1-6, alcoxi C1-6, alquilo C1-6 sustituido con halo y alcoxi C1-6 sustituido con halo; cada R4 se selecciona independientemente de hidrogeno, hidroxilo, halo, alquilo C1-6, alquilo C1-6 sustituido con halo y alcoxi C1-6 sustituido con halo; con la condicion de que cuando A y B sean el mismo resto, X2 no puede ser un enlace; donde cualquier metileno de L puede tener los hidrogenos reemplazados por un radical seleccionado de halo, hidroxi, alquilo C1-4, alcoxi C1-4, alquilo C1-4 sustituido con hidroxi, -CR4R4C(O)OR4, -X4OR4a, -X4NR4aR4a, - X4NR4aX4OR4a, -X4C(O)OR4a y -X4C(O)R4a donde X4 se selecciona de un enlace y alquileno C1-4; R4a se selecciona de hidrogeno y alquilo C1-4; R1 se selecciona de alquilo C1-10, alquilo C1-10 sustituido con halo, arilo C6-10, heteroarilo C1-10, -S(O)0- 2R5a, -C(O)OR5a, -C(O)R5a, y -C(O)NR5aR5b; donde R5a y R5b se seleccionan independientemente de hidrogeno, alquilo C1-6, cicloalquilo C3-12, alquilo C1-6 sustituido con halo, arilo C6-10-alquilo C0-4 y heteroarilo C1-10; donde dicho alquilo, cicloalquilo, arilo o heteroarilo de R5a o R5b pueden estar opcionalmente sustituidos con 1 a 3 radicales independientemente seleccionados de hidrogeno, hidroxi, alquilo C1-6, alquenilo C2-6, alquilo C1-6 sustituido con halo, alcoxi C1-6 sustituido con halo, -NR5cR5d, -C(O)OR5c y arilo C6-10-alquilo C0-4 donde R5c y R5d se seleccionan independientemente de hidrogeno y alquilo C1-6; R2a y R2b se seleccionan independientemente de halo, ciano, hidroxi, alquilo C1-4, amino, nitro, -C(O)OR5e, - C(O)R5e y -NR5eR5f donde R5e y R5f se seleccionan independientemente de hidrogeno, alquilo C1-6, cicloalquilo C3-12, alquilo C1-6 sustituido con halo, cicloalquilo C1-6 sustituido con halo, arilo C6-10 y heteroarilo C1-10; donde dicho arilo o heteroarilo de R5e o R5f pueden estar opcionalmente sustituidos con 1 a 3 radicales independientemente seleccionados de alquilo C1-6, alcoxi C1-6, alquilo C1-6 sustituido con halo y alcoxi C1-6 sustituido con halo; R3 se selecciona de hidrogeno, heteroarilo C1-10, arilo C6-10, heterocicloalquilo C3-8, -C(O)OR6a, -C(O)R6a, -S(O)0-2R6a, -C(O)R7, -C(O)X5NR6aC(O)OR6b, -C(S)OR6a, -C(S)R6a, -C(S)R7 y -C(S)X5NR6aC(O)OR6b; donde X5 se selecciona de un enlace y alquileno C1-6; R6a y R6b se seleccionan independientemente de hidrogeno, alquilo C1-6, alquilo C1-6 sustituido con halo, cicloalquilo C3-12 opcionalmente sustituido con alquilo C1-4, cicloalquilo C1-6 sustituido con halo; R7 se selecciona de alquilo C1-8, cicloalquilo C3-8, arilo C6-10, heteroarilo C1-10 alquilo C1-8 sustituido con halo, cicloalquilo C3-8 sustituido con halo, arilo C6-10 sustituido con halo y heteroarilo C6-10 sustituido con halo; donde dicho arilo, heteroarilo o heterocicloalquilo de R3 está opcionalmente sustituido con 1 a 3 radicales independientemente seleccionados de halo, ciano, -X5aNR8aR8b, -X5aNR8aR9, -X5aNR8aC(O)OR8b, -X5aC(O)OR8a, -X5aOR8a, -X5aOX5bOR8a, -X5aC(O)R8a, -X5aR9, alquilo C1-6, alcoxi C1-6, alquilo C1-6 sustituido con halo y alcoxi C1-6 sustituido con halo; donde R8a y R8b se seleccionan independientemente de hidrogeno y alquilo C1-6; X5a y X5b se seleccionan independientemente de un enlace y alquileno C1-4; R9 se selecciona de cicloalquilo C3-12, heterocicloalquilo C3-8, heteroarilo C1-10 y arilo C6-10; donde dicho arilo, heteroarilo, cicloalquilo o heterocicloalquilo de R9 está opcionalmente sustituido con 1 a 3 radicales independientemente seleccionados de halo, alquilo C1-4 y alcoxi C1-4; o sus sales aceptables para uso farmacéutico.
ARP080100423A 2007-02-02 2008-02-01 Derivados de tetrahidroisoquinolina, composiciones farmaceuticas que los contienen y usos de los mismos para tratar o prevenir enfermedades o trastornos asociados a la actividad de gpr119, tales como diabetes, obesidad y trastornos cardiovasculares, entre otros. AR065133A1 (es)

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EP (1) EP2114890A2 (es)
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CN (1) CN101663278A (es)
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