AR040141A1 - Derivados de piridazina como inhibidores de fosfodiesterasa iv - Google Patents

Derivados de piridazina como inhibidores de fosfodiesterasa iv

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Publication number
AR040141A1
AR040141A1 ARP030101978A ARP030101978A AR040141A1 AR 040141 A1 AR040141 A1 AR 040141A1 AR P030101978 A ARP030101978 A AR P030101978A AR P030101978 A ARP030101978 A AR P030101978A AR 040141 A1 AR040141 A1 AR 040141A1
Authority
AR
Argentina
Prior art keywords
substituted
groups
atoms
conha
cooa
Prior art date
Application number
ARP030101978A
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 AR040141A1 publication Critical patent/AR040141A1/es

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Abstract

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 es H, A''R9, COA"R9, COOA''R9, CONH2, CONHA''R9, CON(A''R9)(A'''R9), NH2, NHA''R9, N(A''R9)(A'''R9), NCOA''R9 o NCOOA''R9; R4 es H, A''R9, COOA''R9, CONH2, CONHA''R9, o CON(A''R9)(A'''R9); B es un radical isocíclico o heterocíclico aromático que puede estar insustituido o mono, di o trisustituido por R5, R6 y / o R7; X es alquileno C1-10 o alquenileno C2-8, donde uno, dos o tres grupos CH2 pueden estar sustituidos por O, S, SO, SO2, NH o NA''R9, 1-7 átomos de H pueden estar sustituidos por F y / o Cl y / o 1 ó 2 átomos de H pueden estar sustituidos por R11 y / o R12; R5, R6, R7 son en cada caso, independientemente entre sí, H, A''R9, OH, OA''R9, NH2, NHA''R9, N(A''R9)(A'''R9), NHCOA''R9, NHCOOA''R9, NHCONH2, NHCONHA''R9, NHCON(A''R9)(A'''R9), Hal, COOH, COOA''R9, CONH2, CONHA''R9, CON(A''R9)(A'''R9), y un grupo de resto de fórmula (2); R8 es A, cicloalquilo C3-7 o alquilencicloalquilo C4-8; R9 es H, COOH, COOA, CONH2, CONHA, CONAA', NH2, NHA, NAA', NCOA, NCOOA, OH, OA, (CH2)narilo, o (CH2)nHet; R10 es alquilo C1-10, cicloalquilo C3-7, alquilencicloalquilo C4-8 o alquenilo C2-8, donde uno, dos o tres grupos CH2 pueden estar sustituidos por O, S, SO, SO2, NH, NMe, NEt y / o por grupos -CH=CH-; 1-7 átomos de H pueden estar sustituidos por F y / o Cl y / o 1 átomo de H puede estar sustituido por R9; R11 es H, A, COOA''R9, CONH2, CONHA''R9, CON(A''R9)(A'''R9), NH2, NHA''R9, N(A''R9)(A'''R9), NCOA''R9 NCOOA''R9, OH u OA''R9; R12 es H, A, COOA''R9, CONH2, CONHA''R9, o CON(A''R9)(A'''R9); Y es alquileno C1-10 o alquenileno C2-8, donde uno, dos o tres grupos CH2 pueden estar sustituidos por O, S, SO, SO2, NH o NR10 y / o 1-7 átomos de H pueden estar sustituidos 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 sustituidos por O, S, SO, SO2, NH o NR10 y / o 1-7 átomos de H pueden estar sustituidos 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 sustituidos por O, S, SO, SO2, NH, NR10, NCOR10 o NCOOR10; 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 sustituidos por O, S, SO, SO2, NH o NR10 y / o 1-7 átomos de H pueden estar sustituidos 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 sustituidos por O, S, SO, SO2, NH o NR10, NCOR10 o NCOOR10; arilo es fenilo, naftilo, fluorenilo, o bifenilo insustituido o mono, di o trisustituido por Hal, R14, OR13, N(R13)2, NO2, CN, COOR13, CON(R13)2, NR13COR13, NR13CON(R13)2, NR13SO2A, COR13, SO2N(R13)2, S(O)mR14, R13 es H o alquilo C1-6; R14 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, R14, OR13, N(R13)2, NO2, CN, COOR13, CON(R13)2, NR13COR13, NR13CON(R13)2, NR13SO2R14, COR13, SO2NR13 y / o S(O)2R14; Hal es F, Cl, Br o I; m es 0, 1 ó 2; n es 0, 1, 2, 3 ó 4, así como los derivados, solvatos y estereoisómeros de los mismos, incluyendo las mezclas de los mismos en todas las proporciones.
ARP030101978A 2002-06-05 2003-06-04 Derivados de piridazina como inhibidores de fosfodiesterasa iv AR040141A1 (es)

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RU2004139032A (ru) 2005-08-20
AU2003227746A1 (en) 2003-12-22

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