AR049502A1 - Derivados de carbonilo heterociclicos - Google Patents

Derivados de carbonilo heterociclicos

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Publication number
AR049502A1
AR049502A1 ARP050102034A ARP050102034A AR049502A1 AR 049502 A1 AR049502 A1 AR 049502A1 AR P050102034 A ARP050102034 A AR P050102034A AR P050102034 A ARP050102034 A AR P050102034A AR 049502 A1 AR049502 A1 AR 049502A1
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AR
Argentina
Prior art keywords
mono
hal
coor2
con
trisubstituted
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ARP050102034A
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English (en)
Inventor
Rolf Gericke
Norbert Beier
Werner Mederski
Florian Lang
Dieter Dorsch
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Merck Patent Gmbh
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Publication of AR049502A1 publication Critical patent/AR049502A1/es

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract

Los compuestos heterocíclicos de la formula (1), en donde: R1, R1a son cada uno, de modo independiente entre sí, un carbociclo o heterociclo mono o bicíclico saturado, insaturado o aromático con 0 a 4 átomos de N, O y/o S, que puede estar mono, di o trisustituido con R2, Hal, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, OR2, N(R2)2, NO2, CN, -[C(R3)2]nCOOR2, -[C(R3)2]nCON(R2)2, -[C(R3)2]nCONR2N(R2)2, O-[C(R3)2]oCON(R2)2, O-[C(R3)2]oCONR2N(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2, S(O)mA, =S, =NR3 y/u =O (oxígeno del carbonilo); D es O, NH o S; W es CX o N; T es CX, N o CR; T' es CX, N o CR; con la condicion de que uno de los radicales T o T' sea CR y el otro sea distinto de CR; R es -C(=O)-N(R2)[C(R2)2]nR1a; X es H, Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, COR2 o SO2NR2; R2 es H, A, -[C(R3)2]n-Ar', -[C(R3)2]n-Het', -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-OR3, -[C(R3)2]n-COOA o -[C(R3)2]nN(R3)2; R3 es H o A; A es alquilo no ramificado o ramificado C1-10, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2N(R2)2, S(O)mA, -[C(R3)2]n-COOR2 u -O-[C(R3)2]o-COOR2; Ar' es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)mA, -[C(R3)2]n-COOR3 u -O-[C(R3)2]o-COOR3; Het es un heterociclo mono o bicíclico, saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono, di o trisustituido con Hal, A, - [C(R3)2]n-Ar, -[C(R3)2]n-Het', -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-OR2, -[C(R3)2]n-N(R3)2, NO2, CN, -[C(R3)2]n-COOR2, O-[C(R3)2]n-COOR2, -[C(R3)2]n-CON(R2)2, -[C(R3)2]n-CONR2N(R2)2, O-[C(R3)2]o-CON(R2)2, O-[C(R3)2]o-CONR2N(R2)2, -[C(R3)2]n-NR2COA, NR2CON(R2)2, -[C(R3)2]n-NR2SO2A, COR2, SO2NR2, S(O)mA, =S, =NR2 y/u =O (oxígeno del carbonilo); Het' es un heterociclo mono o bicíclico, saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar mono, di o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3, S(O)mA, =S, =NR3 y/u =O (oxígeno del carbonilo); Hal es F, Cl, Br o I; m es 0, 1 o 2; n es 0, 1, 2 o 3; o es 1, 2 o 3; así como sus derivados, sales, solvatos y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, son inhibidores de la SGK y pueden ser utilizados para el tratamiento de enfermedades y dolencias causadas por las SGK y tales como diabetes, obesidad, síndrome metabolico (dislipidemia), hipertonía sistémica y pulmonar, enfermedades cardiocirculatorias y renales, en general para todo tipo de fibrosis y procesos inflamatorios.
ARP050102034A 2004-10-21 2005-05-18 Derivados de carbonilo heterociclicos AR049502A1 (es)

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AU2005299112B2 (en) 2011-10-27
JP5420839B2 (ja) 2014-02-19
CA2584465C (en) 2013-08-06
US8815924B2 (en) 2014-08-26
DE102004051277A1 (de) 2006-04-27
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WO2006045350A1 (de) 2006-05-04

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