AR063226A1 - Bifenilsulfonilos y fenil heteroaril sulfonilos como moduladores del receptor h3 de histamina, su uso en medicamentos para el tratamiento de los trastornos relacionados con dicho receptor y una composicion farmaceutica que los comprende. - Google Patents

Bifenilsulfonilos y fenil heteroaril sulfonilos como moduladores del receptor h3 de histamina, su uso en medicamentos para el tratamiento de los trastornos relacionados con dicho receptor y una composicion farmaceutica que los comprende.

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AR063226A1
AR063226A1 ARP070104474A ARP070104474A AR063226A1 AR 063226 A1 AR063226 A1 AR 063226A1 AR P070104474 A ARP070104474 A AR P070104474A AR P070104474 A ARP070104474 A AR P070104474A AR 063226 A1 AR063226 A1 AR 063226A1
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ring
haloalkyl
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Arena Pharm Inc
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    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/10—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 carbon chain containing aromatic rings

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Abstract

Estos compuestos y sus composiciones farmacéuticas están dirigidos a la preparacion de medicamentos utiles en el tratamiento de trastornos asociados al receptor H3 histamina, como trastornos cognitivos, epilepsia, lesion cerebral, depresion, obesidad, trastornos del sueno y la vigilia como narcolepsia, trastornos del sueno por cambio de turno de trabajo, somnolencia como efecto colateral de un medicamento, mantenimiento del estado de alerta para ayudar a completar tareas y similares, cataplejía, hipersomnia, síndrome de somnolencia, síndrome de cambio rápido de husos horarios o jet lag, apnea del sueno y similares, trastorno de hiperactividad por déficit atencional (THDA), esquizofrenia, alergias, respuestas alérgicas en las vías respiratorias superiores, rinitis alérgica, congestion nasal, demencia, enfermedad de Alzheimer y similares. Reivindicacion 1: Un compuesto seleccionado entre los compuestos de formula (1) y sus sales, hidratos y solvatos farmacéuticamente aceptables donde: R1 se selecciona del grupo que consiste en H, acilo C1-6, aciloxi C1-6, alquenilo C2-8, alcoxi C1-6, alquilo C1-8, alquilcarboxamida C1-8, alquinilo C2-8, alquilsulfonamida C1-8, alquilsulfinilo C1-8, alquilsulfonilo C1-8, alquiltio C1-8, alquilureilo C1-8, amino, alquilamino C1-8, dialquilamino C2-8, carboC1-6-alcoxi, carboxamida, carboxi, ciano, cicloalquilo C3-7, dialquilcarboxamida C2-8, dialquilsulfonamida C2-8, halogeno, haloalcoxi C1-6, haloalquilo C1-6, haloalquilsulfinilo C1-6, haloalquilsulfonilo C1-6, haloalquiltio C1-6, heterociclilo C3-7, hidroxilo, tiol, nitro, fenilo y sulfonamida, y cada uno está opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-8, alcoxi C1-6, alquilo C1-8, alquilcarboxamida C1-8, alquinilo C2-8, alquilsulfonamida C1-8, alquilsulfinilo C1-8, alquilsulfonilo C1-8, alquiltio C1-8, alquilureilo C1-8, amino, alquilamino C1-8, dialquilamino C2-8, carboC1-6-alcoxi, carboxamida, carboxi, ciano, cicloalquilo C3-7, dialquilcarboxamida C2-8, dialquilsulfonamida C2-8, halogeno, haloalcoxi C1-6, haloalquilo C1-6, haloalquilsulfinilo C1-6, haloalquilsulfonilo C1- 6, haloalquiltio C1-6, hidroxilo, tiol, nitro y sulfonamida; o R1 junto con el grupo W-SO2 y el átomo del anillo al cual está unido el grupo W-SO2 forman un anillo het4rocíclico C5-7 con el anillo A por lo cual dicho anillo heterocíclico C5-7 y el anillo A comparten dos átomos del anillo adyacentes y dicho anillo heterocíclico C5-7 está opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes seleccionados independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-8, alcoxi C1-6, alquilo C1-8, alquilcarboxamida C1-8, alquinilo C2-8, alquilsulfonamida C1-8, alquilsulfinilo C1-8, alquilsulfonilo C1-8, alquiltio C1-8, alquilureilo C1-8, amino, alquilamino C1-8, dialquilamino C2-8, carboC1-6-alcoxi, carboxamida, carboxi, ciano, cicloalquilo C3-7, dialquilcarboxamida C2-8, dialquilsulfonamida C2-8, halogeno, haloalcoxi C1-6, haloalquilo C1-6, haloalquilsulfinilo C1-6, haloalquilsulfonilo C1-6, haloalquiltio C1-6, hidroxilo, tiol, nitro, oxo y sulfonamida; W es alquileno C1-4, alquenileno C2-4, cicloalquileno C3-7, heterociclileno C3-7 o fenileno, cada uno opcionalmente sustituido con 1, 2, 3, 4, 5, 6, 7 u 8 sustituyentes seleccionados independientemente del grupo que consiste en alquilo C1-3, alcoxi C1- 4, carboxi, ciano, haloalquilo C1-3, halogeno, hidroxilo y oxo; El anillo A es 1,3-fenileno o 1,4-fenileno, cada uno sustituido con R12, R13, R14 y R15, donde R12, R13, R14 y R15 se seleccionan cada uno independientemente del grupo que consiste en H, acilo C1-6, aciloxi C1-6, alquenilo C2-8, alcoxi C1-6, alquilo C1-8, alquilcarboxamida C1-8, alquinilo C2-8, alquilsulfonamida C1-8, alquilsulfinilo C1-8, alquilsulfonilo C1-8, alquiltio C1-8, alquilureilo C1-8, amino, alquilamino C1-8, dialquilamino C2-8, carboC1-6-alcoxi, carboxamida, carboxi, ciano, cicloalquilo C3-7, dialquilcarboxamida C2-8, dialquilsulfonamida C2-8, halogeno, haloalcoxi C1-6, haloalquilo C1-6, haloalquilsulfinilo C1-6, haloalquilsulfonilo C1-6, haloalquiltio C1-6, hidroxilo, tiol, nitro y sulfonamida; o el anillo A es un heteroarileno e 6 miembros o un heteroarileno de 5 miembros cada uno opcionalmente sustituido con R16, R17 y R18, donde R16, R17 y R18 se seleccionan cada uno independientemente del grupo que consiste en acilo C1-6, aciloxi C1-6, alquenilo C2-8, alcoxi C1-6, alquilo C1-8, alquilcarboxamida C1-8, alquinilo C2-8, alquilsulfonamida C1-8, alquilsulfinilo C1-8, alquilsulfonilo C1-8, alquiltio C1-8, alquilureilo C1-8, amino, alquilamino C1-8, dialquilamino C2-8, carboC1-6-alcoxi, carboxamida, carboxi, ciano, cicloalquilo C3-7, dialquilcarboxamida C2-8, dialquilsulfonamida C2-8, halogeno, haloalcoxi C1-6, haloalquilo C1-6, haloalquilsulfinilo C1-6, haloalquilsulfonilo C1- 6, haloalquiltio C1-6, hidroxilo, tiol, nitro y sulfonamida; R2, R3, R4 y R5 se seleccionan cada uno independientemente del grupo que consiste en H, acilo C1-6, aciloxi C1-6, alquenilo C2-8, alcoxi C1-6, alquilo C1-8, alquilcarboxamida C1-8, alquinilo C2-8, alquilsulfonamida C1-8, alquilsulfinilo C1-8, alquilsulfonilo C1-8, alquiltio C1-8, alquilureilo C1-8, amino, alquilamino C1-8, dialquilamino C2-8, carboC1-6-alcoxi, carboxamida, carboxi, ciano, cicloalquilo C3-7, dialquilcarboxamida C2-8, dialquilsulfonamida C2-8, halogeno, haloalcoxi C1-6, haloalquilo C1-6, haloalquilsulfinilo C1-6, haloalquilsulfonilo C1-6, haloalquiltio C1-6, hidroxilo, tiol, nitro y sulfonamida; R6, R7, R8 y R9 se selecciona cada uno independientemente del grupo que consiste en H, alquilo C1-3, alcoxi C1-4, carboxi, ciano, haloalquilo C1-3, halogeno e hidroxilo; y R10 y R11 junto con el átomo de N al cual están ambos unidos forman 2-metil-pirrolidin-1-ilo; siempre que 1) el anillo B y el azufre del grupo R1-W-S(O)2- no estén unidos a átomos del anillo A adyacentes; y 2) si el anillo A es 1,3-fenileno o 1,4-fenileno, y W es heterociclileno C3-7, entonces el átomo del anillo de W que está directamente unido al azufre del grupo R1-W-S(O)2- es diferente de N.
ARP070104474A 2006-10-17 2007-10-10 Bifenilsulfonilos y fenil heteroaril sulfonilos como moduladores del receptor h3 de histamina, su uso en medicamentos para el tratamiento de los trastornos relacionados con dicho receptor y una composicion farmaceutica que los comprende. AR063226A1 (es)

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US85261006P 2006-10-17 2006-10-17
US93435807P 2007-06-11 2007-06-11

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US (1) US20100240653A1 (es)
EP (1) EP2074086B1 (es)
JP (1) JP2010506918A (es)
KR (1) KR20090069333A (es)
AR (1) AR063226A1 (es)
AT (1) ATE512948T1 (es)
AU (1) AU2007313180A1 (es)
CA (1) CA2665204A1 (es)
CL (1) CL2007002977A1 (es)
EA (1) EA200970386A1 (es)
IL (1) IL197892A0 (es)
MX (1) MX2009004071A (es)
PA (1) PA8750901A1 (es)
PE (1) PE20081462A1 (es)
TW (1) TW200823204A (es)
WO (1) WO2008048609A1 (es)

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