AR039695A1 - Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit) - Google Patents

Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit)

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Publication number
AR039695A1
AR039695A1 ARP030102149A ARP030102149A AR039695A1 AR 039695 A1 AR039695 A1 AR 039695A1 AR P030102149 A ARP030102149 A AR P030102149A AR P030102149 A ARP030102149 A AR P030102149A AR 039695 A1 AR039695 A1 AR 039695A1
Authority
AR
Argentina
Prior art keywords
replaced
groups
hal
atoms
independently
Prior art date
Application number
ARP030102149A
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English (en)
Inventor
Eggenweiler Hans-Michael Dr
Wolf Michael Dr
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Merck Patent Gmbh
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Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR039695A1 publication Critical patent/AR039695A1/es

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    • C07D417/02—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
    • C07D417/06—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 only aliphatic carbon atoms
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Abstract

Estos derivados de fórmula (1), actúan como inhibidores de la fosfodiesterasa IV y pueden emplearse para el tratamiento de osteoporosis, tumores, caquexia, aterosclerosis, artritis reumatoidea, esclerosis múltiple, diabetes mellitus, procesos inflamatorios, alergias, asma, enfermedades, autoinmunes, enfermedades miocárdicas y SIDA. Reivindicación 1: Compuestos de la fórmula (1) donde: R1, R2 son en cada caso, independientemente entre sí, H, OH, OR8, -SR8, -SOR8, -SO2R8, o Hal; R1 y R2 también son juntos -OCH2O- u -OCH2CH2O-; R3, R3' son en cada caso, independientemente entre sí, H, A"R7, COA"R7, COOA"R7, CONH2, CONHA''R7, CON(A"R7)(A"')R7, CONR10Het, NH2, NHA"R7, N(A"R7)(A"'R7), NCOA''R7 o NCOOA''R7; V, W son oxígeno, o sustituyentes de hidrógeno, con la condición de que, cuando V significa O, W es H, H, y viceversa; B es un radical isocíclico o heterocíclico aromático, que esta insustituido o que puede estar mono, di o trisustituido por R4, R5 y/o R6; X es N o CR3, R4, R5, R6 son en cada caso, independientemente entre sí, H, A''R7, OH, OA''R7, NO2, NH2, NHA''R7, N(A''R7)(A'''R7), NHCOA''R7, NHCOOA''R7, NHCONH2, NHCONHA''R7, NHCON(A''R7)(A'''R7), Hal, COOH, COOA''R7, CONH2, CONHA''R7, CON(A''R7)(A'''R7); o un resto del grupo de fórmulas (2); R7 es H, COOH, COOA, CONH2, CONHA, CONAA', NH2, NHA, NAA', NCOA, NCOOA, OH u OA; R8 es A, cicloalquilo C3-7, alquilencicloalquilo C4-8 o alquenilo C2-8; R9 es alquilo C1-10, cicloalquilo C3-7, alquilencicloalquilo C4-8 o alquenilo C2-8, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH, NMe, NEt y/o por grupos -CH=CH- y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; Y es alquileno C1-10 o alquenileno C2-8, donde uno, dos o tres grupos CH2 pueden estar reemplazado por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; A, A' son en cada caso, independientemente entre sí, alquilo C1-10 o alquenilo C2-8, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl, o arilo o Het; A y A' también son juntos una cadena de alquileno C2-7, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9, NCOR9 o NCOOR9; A'', A''' en cada caso, independientemente entre sí, están ausentes, son alquileno C1-10, alquenileno C2-8 o cicloalquileno C3-7, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9 y/o 1-7 átomos de H pueden estar reemplazados por F y/o Cl; A'' y A''' también son juntos una cadena de alquileno C2-7, donde uno, dos o tres grupos CH2 pueden estar reemplazados por O, S, SO, SO2, NH o NR9, NCOR9 o NCOOR9; arilo es fenilo, naftilo, fluorenilo, o bifenilo insustituido o mono, di o trisustituido por Hal, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2A, COR10, SO2N(R10)2, S(O)mR11, R10 es H o alquilo C1-6; R11 es alquilo C1-6; Het es un heterociclo mono o bicíclico saturado, no saturado o aromático con 1 ó 2 átomos de N, O y/o S, que está insustituido o mono o disustituido por el oxígeno del carbonilo, Hal, R11, OR10, N(R10)2, NO2, CN, COOR10, CON(R10)2, NR10COR10, NR10CON(R10)2, NR10SO2R11, COR10, SO2NR10 y/o S(O)mR11; Hal es F, Cl, Br o I; m es 0, 1 ó 2; así como los derivados, solvatos y estereoisómeros de los mismos de uso farmacéutico, incluyendo las mezclas de los mismos en todas las proporciones.
ARP030102149A 2002-06-19 2003-06-18 Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit) AR039695A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10227269A DE10227269A1 (de) 2002-06-19 2002-06-19 Thiazolderivate

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AR039695A1 true AR039695A1 (es) 2005-03-09

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ARP030102149A AR039695A1 (es) 2002-06-19 2003-06-18 Derivados de tiazol, uso de los mismos para preparar un medicamento y conjunto en envases (kit)

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US (1) US7790723B2 (es)
EP (1) EP1513837B1 (es)
JP (1) JP4555076B2 (es)
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CA2489902C (en) 2011-11-22
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MXPA04012428A (es) 2005-04-19
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