AR065354A1 - Derivados de 2-aminopirimidina, un metodo para su preparacion, una composicion farmaceutica que lo comprende y su uso en el tratamiento de enfermedades mediadas por el receptor de histamina h4. - Google Patents

Derivados de 2-aminopirimidina, un metodo para su preparacion, una composicion farmaceutica que lo comprende y su uso en el tratamiento de enfermedades mediadas por el receptor de histamina h4.

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Publication number
AR065354A1
AR065354A1 ARP080100637A ARP080100637A AR065354A1 AR 065354 A1 AR065354 A1 AR 065354A1 AR P080100637 A ARP080100637 A AR P080100637A AR P080100637 A ARP080100637 A AR P080100637A AR 065354 A1 AR065354 A1 AR 065354A1
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alkyl
methyl
formula
optionally substituted
taken together
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ARP080100637A
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Janssen Pharmaceutica Nv
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    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Animal Behavior & Ethology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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Abstract

Se describen los compuestos de 2-Aminopirimidina, que son utiles como moduladores del receptor H4. Dichos compuestos pueden utilizarse en composiciones farmacéuticas y para el tratamiento de enfermedades, trastornos y condiciones mediadas por laactividad del receptor de H4, tales como alergia, asma, enfermedades autoinmunes y pruritis. Reivindicacion 1: Una entidad química seleccionada de los compuestos de la formula (1), en donde R1 es: a) un grupo alquilo C1-6, opcionalmente sustituidocon -OH, -Oalquilo C1-4, -CF3, o -O-(cicloalquilo monocíclico); b) un grupo bencil, -CH2-(heteroaril monociclico), o fenetil, cada uno opcionalmente sustituido por halo; c) un grupo cicloalquilo monociclico, -(CH2)0-1-tetrahidrofuranil, o -(CH2)0-1-tetrahidropiranil, cada uno opcionalmente fusionado a un anillo de fenilo, y cada uno opcionalmente sustituido con alquilo C1-4 o fenilo; o d) un grupo adamantil; R2 es H, F, metil, o metoxi; o R1 y R2 tomados conjuntamente forman -(CH2)3-5- o -(CH2)2OCH2-; y -N(R3)R4 es uno de los siguientes sistemas de anillos acíclicos, monocíclicos, espirocíclicos, unidos o fusionados de formulas (2) en donde q es 0 o 1; R3 y R4 se toman en forma conjunta segun lo define la estructura de cada una dedichas mitades; Ra es H o OH; Rb y Rc son independientemente H o alquilo C1-3; y cada sustituto Rd es metil o dos sustitutos Rd tomados en forma conjunta son metileno o un puente de etileno; siempre que R1 sea metil, entonces -N(R3)R4 se seleccionade dichos sistemas de anillos espirocíclicos, de puente y fusionados; y sales farmacéuticamente aceptables de los compuestos de la formula (1), prodrogas farmacéuticamente aceptables de los compuestos de la formula (1) y metabolitosfarmacéuticamente aceptables de la formula (1). Reivindicacion 36: Un método para crear un compuesto de la formula (1) o una sal farmacéuticamente aceptable, en donde R1 es: a) un grupo alquilo C1-6, opcionalmente sustituido con -OH, -Oalquilo C1-4, -CF3, o -O-(cicloalquilo monocíclico); b) un grupo bencil, -CH2-(heteroaril monocíclico), o fenetil, cada uno opcionalmente sustituido por halo; c) un grupo cicloalquilo monocíclico, -(CH2)0-1-tetrahidrofuranil, o -(CH2)0-1-tetrahidropiranil,cada uno opcionalmente fusionado a un anillo de fenilo, y cada uno opcionalmente sustituido con alquilo C1-4 o fenilo; o d) un grupo adamantil; R2 es H, F, metil, o metoxi; o R1 y R2 tomados conjuntamente forman -(CH2)3-5- o -(CH2)2OCH2-; y -N(R3)R4es uno de los siguientes sistemas de anillos acíclicos, monocíclicos, espirocíclicos, unidos o fusionados de formulas (2), en donde q es 0 o 1; R3 y R4 se toman en forma conjunta segun lo define la estructura de cada una de dichas mitades; Ra es H oOH; Rb y Rc son independientemente H o alquilo C1-3; y cada sustituto Rd es metil o dos sustitutos Rd tomados en forma conjunta son metileno o un puente de etileno; siempre que R1 sea metil, entonces -N(R3)R4 se selecciona de dichos sistemas deanillos espirocíclicos, de puente y fusionados; comprendiendo la reaccion al cloro-pirimidina de la formula A3, con un diamino HNR3R4.
ARP080100637A 2007-02-14 2008-02-14 Derivados de 2-aminopirimidina, un metodo para su preparacion, una composicion farmaceutica que lo comprende y su uso en el tratamiento de enfermedades mediadas por el receptor de histamina h4. AR065354A1 (es)

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US88979807P 2007-02-14 2007-02-14

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AR065354A1 true AR065354A1 (es) 2009-06-03

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US (6) US7923451B2 (es)
EP (2) EP2124560A4 (es)
JP (1) JP5281586B2 (es)
KR (1) KR20090110877A (es)
CN (1) CN101668423B (es)
AR (1) AR065354A1 (es)
AU (1) AU2008216727B2 (es)
BR (1) BRPI0807815A2 (es)
CA (1) CA2678077A1 (es)
CL (1) CL2008000467A1 (es)
CO (1) CO6210771A2 (es)
CR (1) CR11027A (es)
EA (1) EA016133B1 (es)
EC (1) ECSP099582A (es)
GT (1) GT200900231A (es)
IL (1) IL200335A0 (es)
MX (1) MX2009008787A (es)
NI (1) NI200900159A (es)
NZ (1) NZ578977A (es)
PE (1) PE20081776A1 (es)
TW (1) TW200904437A (es)
UY (1) UY30917A1 (es)
WO (1) WO2008100565A1 (es)

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