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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
Other languages
English (en)
Inventor
Eggenweiler Hans-Michael Dr
Wolf Michael Dr
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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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    • C07D417/00—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
    • 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

Publications (1)

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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)

Country Status (15)

Country Link
US (1) US7790723B2 (es)
EP (1) EP1513837B1 (es)
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AU2003232215B2 (en) 2009-04-30
US7790723B2 (en) 2010-09-07
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