AR085990A1 - Derivados de 1-oxido de 3-hidroxiisotiazol utiles en el tratamiento de la diabetes y composiciones farmaceuticas que los contienen - Google Patents

Derivados de 1-oxido de 3-hidroxiisotiazol utiles en el tratamiento de la diabetes y composiciones farmaceuticas que los contienen

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Publication number
AR085990A1
AR085990A1 ARP120101245A ARP120101245A AR085990A1 AR 085990 A1 AR085990 A1 AR 085990A1 AR P120101245 A ARP120101245 A AR P120101245A AR P120101245 A ARP120101245 A AR P120101245A AR 085990 A1 AR085990 A1 AR 085990A1
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Argentina
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group
optionally substituted
substituents
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alkyl
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ARP120101245A
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Mochida Pharm Co Ltd
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    • C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
    • C07D275/03—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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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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    • 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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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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  • Thiazole And Isothizaole Compounds (AREA)
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Abstract

Reivindicación 1: Un compuesto de la fórmula (1) (caracterizado porque p es un entero de 0 hasta 4; j es un entero de 0 hasta 2; k es 0 ó 1; un anillo A es un grupo arilo C6-14 que está opcionalmente sustituido con 1 hasta 5 sustituyentes L, un grupo heterocíclico de 3 hasta 14 miembros que está opcionalmente sustituido con 1 hasta 5 sustituyentes L, un grupo cicloalquilo C5-7 que está opcionalmente sustituido con 1 hasta 5 sustituyentes L, un grupo cicloalquenilo C5-7 que está opcionalmente sustituido con 1 hasta 5 sustituyentes L, un grupo espirocíclico de 6 hasta 14 miembros que está opcionalmente sustituido con 1 hasta 5 sustituyentes L, o un grupo 2-fenilamino-2-oxoacetilo que está opcionalmente sustituido con 1 hasta 5 sustituyentes L; un anillo B es grupo arilo C6-14 o grupo heteroarilo de 5 hasta 14 miembros; X es un átomo de oxígeno o -NR7-; R1s son independientemente un grupo seleccionado arbitrariamente de un átomo de halógeno, un grupo alquilo C1-6 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alquenilo C2-6 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alquinilo C2-6 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alcoxi C1-6 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI y un grupo ciano; R2 es un átomo de hidrógeno, un átomo de halógeno, un grupo alquilo C1-6, un grupo alquenilo C2-6, un grupo alquinilo C2-6, un grupo alcoxi C1-6 o un grupo ciano; R3, R4, R5, R6, y R7 son independientemente un átomo de hidrógeno o un grupo alquilo C1-6; los sustituyentes L son independientemente un grupo seleccionados arbitrariamente de un átomo de halógeno, -OH, un grupo oxo, un grupo ciano, un grupo alquilo C1-10 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alquenilo C2-10 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alquinilo C2-10 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alcoxi C1-10 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alqueniloxi C2-10 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo alquiniloxi C2-10 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI, un grupo arilo que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo heterocíclico que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo aralquilo que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo heteroarilalquilo que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo alquilo heterocíclico no aromático que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo ariloxi que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo heteroariloxi que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo oxi heterocíclico no aromático que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo aralquiloxi que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, un grupo heteroarilalquiloxi que está opcionalmente sustituido con 1 hasta 5 sustituyentes RII, -SH, -SF5, un grupo: -S(O)iRa (i es un entero de 0 hasta 2), un grupo: -NRbRc y un grupo espiropiperidinilmetilo sustituido; Ra es un grupo seleccionados arbitrariamente de un grupo alquilo C1-6 y un grupo alquilo C1-6 halogenado; Rb y Rc son independientemente un grupo seleccionados arbitrariamente de un átomo de hidrógeno, un grupo alquilo C1-6, un grupo alquilo C1-6 halogenado, un grupo alquenilo C2-6, un grupo alquinilo C2-6, un grupo alcanoilo C2-7 (el grupo alcanoilo está opcionalmente sustituido con -OH o un grupo alcoxi C1-6), un grupo alquilsulfonilo C1-6, un grupo arilcarbonilo y un grupo carbonilo heterocíclico, o Rb y Rc forman opcionalmente en conjunto con un átomo de nitrógeno al cual Rb y Rc se unen, un grupo cíclico de 3 hasta 8 miembros, donde en el grupo cíclico, uno o dos átomos de carbono están opcionalmente sustituidos con un átomo seleccionados arbitrariamente de un átomo de oxígeno, un átomo de azufre, y un átomo de nitrógeno (el átomo de nitrógeno está opcionalmente sustituido con un grupo alquilo C1-6 que está opcionalmente sustituido con 1 hasta 5 sustituyentes RI) o con un grupo carbonilo, y el grupo cíclico está opcionalmente sustituido además con 1 hasta 5 sustituyentes RII; los sustituyentes RI antes mencionado son el mismo como o diferente uno del otro y son cada uno un grupo seleccionado arbitrariamente de un átomo de halógeno, -OH, un grupo ciano, un grupo alcoxi C1-6 (el grupo alcoxi C1-6 está opcionalmente sustituido con 1 hasta 5 átomos de halógeno, 1 hasta 5 -OH, 1 hasta 5 grupos alcoxi C1-6, 1 hasta 5 grupos arilo (el grupo arilo opcionalmente está arbitrariamente sustituido con 1 hasta 3 átomos de halógeno), 1 hasta 5 grupos heterocíclico (el grupo heterocíclico opcionalmente está arbitrariamente sustituido con 1 hasta 3 grupos alquilo C1-6 o 1 hasta 3 grupos oxo), 1 hasta 5 grupos: -S(O)iRa (i es un entero de 0 hasta 2), 1 hasta 5 grupos: -SO2NRdRe, 1 hasta 5 grupos: -CONRdRe o 1 hasta 5 grupos: -NRb1Rc1), un grupo: -NRb1Rc1 y un grupo oxi heterocíclico (el grupo oxi heterocíclico opcionalmente está arbitrariamente sustituido con 1 hasta 3 grupos alquilo C1-6 o 1 hasta 3 grupos oxo); los sustituyentes RII antes mencionado son el mismo como o diferente uno del otro y son cada uno un grupo seleccionado arbitrariamente del sustituyente RI antes mencionado, un grupo alquilo C1-6 (el grupo alquilo C1-6 opcionalmente está arbitrariamente sustituido con 1 hasta 5 átomos de halógeno, 1 hasta 5 -OH, 1 hasta 5 grupos alcoxi C1-6, 1 hasta 5 grupos: -S(O)iRa (i es un entero de 0 hasta 2), 1 hasta 5 grupos: -SO2NRdRe, 1 hasta 5 grupos: -CONRdRe o 1 hasta 5 grupos: -NRb1Rc1), un grupo alquenilo C2-6, un grupo alcanoilo C2-7, un grupo aralquiloxi, un grupo heterocíclico (el grupo heterocíclico opcionalmente está arbitrariamente sustituido con 1 hasta 3 grupos alquilo C1-6 o 1 hasta 3 grupos oxo), un grupo carbonilo heterocíclico (el grupo carbonilo heterocíclico opcionalmente está arbitrariamente sustituido con 1 hasta 3 grupos alquilo C1-6 o 1 hasta 3 grupos oxo), un grupo: -S(O)iRa (i es un entero de 0 hasta 2), un grupo: -CONRdRe1, y un grupo: -CONRdRe1; Rd y Re son independientemente un átomo de hidrógeno o un grupo alquilo C1-6 (el grupo alquilo C1-6 está opcionalmente sustituido con 1 hasta 5 átomos de halógeno, 1 hasta 5 -OH o 1 hasta 5 grupos alcoxilo C1-6); Re1 es un grupo alquilo C1-6 (el grupo alquilo C1-6 está opcionalmente sustituido con 1 hasta 5 -OH, 1 hasta 5 grupos alcoxilo C1-6, 1 hasta 5 grupos arilo (el grupo arilo está opcionalmente sustituido con 1 hasta 3 átomos de halógeno), 1 hasta 5 grupos heterocíclico (el grupo heterocíclico está opcionalmente sustituido con 1 hasta 3 grupo alquilo C1-6 o 1 hasta 3 grupos oxo), 1 hasta 5 grupos -S(O)iRa (i es un entero de 0 hasta 2), 1 hasta 5 grupos -SO2NRdRe, 1 hasta 5 grupos -CONRdRe o 1 hasta 5 grupos -NRb1Rc1; Rb1 y Rc1 son independientemente un grupo seleccionados arbitrariamente de un átomo de hidrógeno, un grupo alquilo C1-6, un grupo alcanoilo C2-7 y un grupo alquilsulfonilo C1-6, o Rb1 y Rc1 forman opcionalmente en conjunto con un átomo de nitrógeno al cual Rb1 y Rc1 se unen, un grupo cíclico de 3 hasta 8 miembros, donde en el grupo cíclico, uno o dos átomos de carbono están opcionalmente sustituidos con un átomo seleccionado arbitrariamente de un átomo de oxígeno, un átomo de azufre, y un átomo de nitrógeno (el átomo de nitrógeno está opcionalmente sustituido con un grupo alquilo C1-6) o con un grupo carbonilo; en un grupo isotiazolilo, en un caso donde el anillo B se une en la posición 5, R2 se une en la posición 4, y en un caso donde el anillo B se une en la posición 4, R2 se une en la posición 5), o una sal farmacéuticamente aceptable del compuesto, o un solvato farmacéuticamente aceptable de la sal o un solvato farmacéuticamente aceptable del compuesto.
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