AR076866A1 - Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo y heterociclo y el uso de las mismas - Google Patents

Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo y heterociclo y el uso de las mismas

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AR076866A1
AR076866A1 ARP100101643A AR076866A1 AR 076866 A1 AR076866 A1 AR 076866A1 AR P100101643 A ARP100101643 A AR P100101643A AR 076866 A1 AR076866 A1 AR 076866A1
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Argentina
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alkyl
cycloalkyl
pyridinyl
halogen
haloalkyl
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Molecular Research Inc Albany
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Albany Molecular Res Inc
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

Estos compuestos se utilizan en el tratamiento de varios trastornos neurologicos y fisiologicos. Además se describen los métodos para preparar estos compuestos, y composicion farmacéutica. Reivindicacion 1: Un compuesto de formula (1) donde: el átomo de carbono designado * está en la configuracion R o S; R1 es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, cicloalquilalquilo C4-7, haloalquilo C1-6 o gem-dialquilo de los cuales cada alquilo es C1-4; R2 es H, halogeno, OR11, -S(O)nR12, -CN, -C(O)R12, -C(O)NR11R12, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, o cicloalquilalquilo C4-7, y donde cada uno de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, y cicloalquilalquilo C4-7 está opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados en cada aparicion de los mismos del grupo integrado por alquilo C1-3, halogeno, -CN, -OR9, -NR9R10, y fenilo que está opcionalmente sustituido 1 a 3 veces con halogeno, ciano, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, -CN, -OR9, o -NR9R10; R3 es un arilo seleccionado del grupo integrado por fenilo, naftilo, indanilo, e indenilo, o un heteroarilo seleccionado del grupo integrado por piridilo, 2-oxo-piridin-1-ilo, pirimidinilo, piridazinilo, pirazinilo, 1,2,4-triazinilo, 1,3,5-triazinilo, furanilo, pirrolilo, tiofenilo, pirazolilo, imidazolilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, 1,.,3-triazolilo, 1,2,4-triazolilo, 1,2,3-oxadiazolilo, 1,3, 4-oxadiazolilo, 1,2,3-tiadiazolilo, 1,3,4-tiadiazolilo, tetrazolilo, indolilo, isoindolilo, benzofuranilo, benzotiofenilo, indolinilo, oxoindolinilo, dihidrobenzofuranilo, dihidrobenzotiofenilo, indazolilo, bencimidazolilo, benzoxazolilo, benzotiazolilo, benzoisoxazolilo, benzoisotiazolilo, benzotriazolilo, benzo[1,3]dioxolilo, quinolinilo, isoquinolinilo, quinazolinilo, cinnolinilo, ptalazinilo, quinoxalinilo, 2,3-dihidro- benzo[1,4]dioxinilo, benzo[1,2,3]triazinilo, benzo[l12,4]triazinilo, 4H-cromenilo, indolizinilo, quinolizinilo, 6aH-tieno[2,3-d]imidazolilo, 1H-pirrolo[2,3-b]piridinilo, imidazo[1,2-a]piridinilo, pirazolo[1,5-a]piridinilo, [1,2,4]triazolo[4,3-a]piridinilo, [1,2,4]triazolo[1,5-a]piridinilo, tieno[2,3-b]furanilo, tieno[2,3-b]piridinilo, tieno[3,2-b]piridinilo, furo[2,3-b]piridinilo, furo[3,2-b]piridinilo, tieno[3,2-d]pirimidinilo, furo[3,2-d]pirimidinilo, tieno[2,3-b]pirazinilo, furo[2,3-b]pirazinilo, imidazo[1,2-a]pirazinilo, 5,6,7,8-tetrahidroimidazo[1,2-a]pirazinilo, 6,7-dihidro-4H-pirazolo[5,1-c][1,4]oxazinilo, 2-oxo-2,3-dihidrobenzo[d]oxazolilo, 2-oxo-2,3-dihidro-1H- benzo[d]imidazol, 3,3-dimetil-2-oxoindolinilo, 2-oxo-2,3-dihidro-1H-pirrolo[2,3-b]piridinilo, benzo[c][1,2,5] oxadiazolilo, benzo[c] [1,2,5]tiadiazolilo, 3,4-dihidro-2H- benzo[b][1,4]oxazinilo, 5,6,7,8-tetrahidro-[1,2,4]triazolo [4,3-a]pirazinilo, [1,2,4]triazolo[4,3-a]pirazinilo, y 3- oxo-[1,2,4]triazolo[4,3-a]piridinilo, o un heterociclo no aromático seleccionado del grupo integrado por pirrolidinilo, 2-oxopirrolidinilo, piperidinilo, 2-oxopiperidinilo, azepanilo, 2-oxoazepanilo, 2- oxoxazolidinilo, morfolino, 3-oxomorfolino, tiomorfolino, 1,1-dioxotiomorfolino, piperazinilo, y tetrahidro-2H-oxazinilo; donde el arilo, heteroarilo, o heterociclo no aromático está opcionalmente sustituido de 1 a 4 veces con sustituyentes como se define a continuacion en R14; R4, R5 y R6 y R7 son cada uno de ellos independientemente H o se seleccionan del grupo integrado por -OR11, -NR11R12, -NR11C(O)R12, -NR11C(O)2R12, -NR11C(O)NR12R13, -S(O)nR12, -CN, -C(O)R12, -C(O)NR11R12, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 y cicloalquilalquilo C4-7, y donde cada uno de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, cicloalquilalquilo C4-7 está opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados en cada aparicion de los mismos del grupo integrado por alquilo C1-3, halogeno, -CN, -OR9, -NR9R10, y fenilo que está opcionalmente sustituido 1 a 3 veces con halogeno, ciano, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, -CN, -OR9, o -NR9R10; R8 es H, alquilo C1-6, halogeno, o OR11; R9 y R10 son cada uno de ellos independientemente H, alquilo C1-4, haloalquilo C1-4, alcoxialquilo C1-4, cicloalquilo C3-6, cicloalquilalquilo C4-7, -C(O)R13, fenilo, o bencilo, donde fenilo o bencilo está opcionalmente sustituido de 1 a 3 veces con un sustituyente seleccionado independientemente en cada aparicion del mismo del grupo integrado por halogeno, ciano, alquilo C1-4, haloalquilo C1-4, y alcoxi C1-4; o R9 y R10 se toman juntos con el nitrogeno al cual están unidos para formar un anillo piperidina, pirrolidina, piperazina, N-metilpiperazina, morfolina, o tiomorfolina; R11 es H, alquilo C1-4, haloalquilo C1-4, alcoxialquilo C1-4, cicloalquilo C3-6, cicloalquilo C4-7, -C(O)R13, fenilo, o bencilo, donde fenilo o bencilo está opcionalmente sustituido 1 a 3 veces con halogeno, ciano, alquilo C1-4, haloalquilo C1-4, o alcoxi C1-4; R12 es H, alquilo C1-4, haloalquilo C1-4, alcoxialquilo C1-4, cicloalquilo C3-6, cicloalquilo C4-7, fenilo, o bencilo, donde fenilo o bencilo está opcionalmente sustituido 1 a 3 veces con halogeno, ciano, alquilo C1-4, haloalquilo C1-4, o alcoxi C1-4; o R11 y R12 se toman juntos con el nitrogeno al cual están unidos para formar un anillo piperidina, pirrolidina, piperazina, N-metilpiperazina, morfolina, o tiomorfolina, con la condicion de que solo uno de R9 y R10 o R11 y R12 se tome junto con el nitrogeno al cual están unidos para formar un anillo de piperidina, pirrolidina, piperazina, N-metilpiperazina, morfolina, o tiomorfolina; R13 es alquilo C1-4, haloalquilo C1-4, o fenilo; n es 0, 1, o 2; y R14 se selecciona independientemente en cada aparicion de un sustituyente seleccionado del grupo integrado por halogeno, -NO2, -OR11, -NR11R12, -NR11C(O)R12, -NR11C(O)2R12, -NR11C(O)NR12R13, -S(O)nR12, -CN, -C(O)R12, -C(O)NR11R12, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 y cicloalquilalquilo C4-7, donde alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 y cicloalquilalquilo C4-7, están opcionalmente sustituidos 1 a 3 sustituyentes independientemente seleccionados en cada aparicion del grupo integrado por alquilo C1-3, halogeno, Ar, -CN, -OR9, y -NR9R10, o un oxido del mismo, una sal aceptable para uso farmacéutico del mismo, un solvato del mismo, o una prodroga del mismo.
ARP100101643 2009-05-12 2010-05-12 Tetrahidroisoquinolinas sustituidas con arilo, heteroarilo y heterociclo y el uso de las mismas AR076866A1 (es)

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