AR045033A1 - Derivados de malonamida, metodo de obtencion y composiciones farmaceuticas que los contienen. - Google Patents

Derivados de malonamida, metodo de obtencion y composiciones farmaceuticas que los contienen.

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Publication number
AR045033A1
AR045033A1 ARP040102386A ARP040102386A AR045033A1 AR 045033 A1 AR045033 A1 AR 045033A1 AR P040102386 A ARP040102386 A AR P040102386A AR P040102386 A ARP040102386 A AR P040102386A AR 045033 A1 AR045033 A1 AR 045033A1
Authority
AR
Argentina
Prior art keywords
halogen
atoms
substituted
group
optionally
Prior art date
Application number
ARP040102386A
Other languages
English (en)
Inventor
Chem David Bruge
Buchstaller Hans-Peter Dr
Wiesner Matthias Dr
Finsinger Dirk Dr
Manfred Baumgarth
Sirrenberg Christian Dr
Zenke Frank Dr
Amendt Christiane Dr
Grell Matthias 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 AR045033A1 publication Critical patent/AR045033A1/es

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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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Abstract

La presente se refiere a derivados de malonamida de la fórmula (1) A-D-B en donde D es un resto de malonamida bivalente sustituido o insustituido o uno de sus derivados: A es un resto insustituido o sustituido de hasta 40 átomos de C de la fórmula -L-(M-L´)a´ en donde L es una estructura cíclica de 5, 6 o 7 miembros seleccionada, con preferencia, del grupo integrado por arilo, heteroarilo, arileno y heteroarileno, unida directamente con D; L´ comprende un resto cíclico opcionalmente sustituido que tiene al menos 5 miembros seleccionado, con preferencia, del grupo integrado por arilo, heteroarilo, aralquilo, cicloalquilo y heterociclilo, M es un enlace o un grupo puente que tiene al menos un átomo, a es un número entero de 1 a 4; y cada estructura cíclica de L y L´ contiene 0-4 miembros del grupo integrado por N, O y S, en donde L´ está sustituido, con preferencia, con al menos un sustituyente seleccionado del grupo integrado por SObRx, -C(O)Rx y -C(NRy)Rz; B es un resto arilo o heteroarilo sustituido o insustituido hasta tricíclico de hasta 30 átomos de C, con preferencia, de hasta 20 átomos de C, que comprende al menos una estructura cíclica de 5, 6 o 7 miembros, con preferencia, una estructura cíclica de 5 o 6 miembros, unida directamente con D que contiene 0-4 miembros del grupo integrado por N, O y S, en donde dicha estructura cíclica directamente unida a D está seleccionada, con preferencia, del grupo integrado por arilo, heteroarilo y heterociclilo; Ry es H o un resto carbonado de hasta 24 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, s y O que está opcionalmente halosustituido, hasta perhalo; Rz es H o u resto carbonado de hasta 30 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halógeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halógeno; Rx es Rz o NRaRb, en donde Ra y Rb son a) de forma independiente, H, un resto carbonado de hasta 30 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halógeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halógeno, u -OSi(Rf)3, en donde Rf es H o un resto carbonado de hasta 24 átomos de C que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halógeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halógeno; o b) Ra y Rb forman juntos una estructura heterocíclica de 5-7 miembros de 1-3 heteroátomos seleccionados de N, S y O, o una estructura heterocíclica sustituida de 5-7 miembros de 1-3 heteroátomos seleccionados de N, S y O sustituida con halógeno, hidroxi o sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halógeno; o c) uno de Ra o Rb es -C(O)-, un grupo alquileno C1-5 divalente o un grupo alquileno C1-5 divalente sustituido unido con el resto L para formar una estructura cíclica con al menos 5 miembros, en donde los sustituyentes del grupo alquileno C1-5 divalente sustituido están seleccionados del grupo integrado por halógeno, hidroxi y sustituyentes carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con halógeno; en donde B está sustituido, L está sustituido o L´ está adicionalmente sustituido, los sustituyentes están seleccionados del grupo integrado por halógeno, hasta perhalo, y Wg, en donde g es 0-3; en donde cada W está seleccionado, de forma independiente, del grupo integrado por -CN, -CO2R, -C(O)NR5R6, -C(O)-R5, -NO2, -OR5, -SR5, SO2R5, -SO3H, -NR5R5, -NR5C(O)OR5, -NR5C(O)R5, -Q-Ar, y restos carbonados de hasta 24 átomos de C, que opcionalmente contienen heteroátomos seleccionados de N, S y O y que están opcionalmente sustituidos con uno o varios sustituyentes seleccionados, de forma independiente, de los grupos integrados por -CN, -CO2R, -C(O)NR5R5, -C(O)-R5, -NO2, -OR5, -SR5, -SO2R5, -SO3H, -NR5R5, -NR5C(O)OR5, -NR5C(O)R5 y halógeno hasta perhalo; con cada R5 seleccionado, de forma independiente, de H o un resto carbonado de hasta 24 átomos de C, que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con halógeno, en donde Q es -O-, -S-, -N(R5)-, -(CH2)b, -C(O)-,-CH(OH)-, -(CH2)b-O-, -(CH2)b-S-, -(CH2)bN(R5), -O(CH2)b, -CHHal-, -CHal2-,-S-(CH2)- y -N(R5)(CH2)b-, en donde b = 1-3, y Hal es halógeno; y Ar es una estructura aromática de 5 o 6 miembros que contiene 0-2 miembros seleccionados del grupo integrado por N, O y S, que está opcionalmente sustituida con halógeno, hasta perhalo, y opcionalmente sustituida con Zd1, en donde d1 es 0 a 3 y cada Z está seleccionado, de forma independiente, del grupo integrado por -CN, -CO2R5, -C(O)NR5R5, -C(O)-R5, -NO2,-OR5, -SR5, -SO2R5, -SO3H, -NR5R5, -NR5C(O)OR5, -NR5C(O)R5, y un resto carbonado de hasta 24 átomos de C, que opcionalmente contiene heteroátomos seleccionados de N, S y O y que está opcionalmente sustituido con uno o varios sustituyentes seleccionados del grupo integrado por -CN, -CO2R5, -C(O)NR5R5, -C(O)-R5, -NO2, -OR5, -SR5, -SO2R5, -SO2R5, -SO3H., -NR5R5, -NR5C(O)OR5, -NR5C(O)R5, y sus derivados, sales y solvatos fisiológicamente aceptables. Al uso de los compuestos de la fórmula (1) para preparar una composición farmacéutica y a un método de tratamiento que comprende la administración de dicha composición farmacéutica a un paciente.
ARP040102386A 2003-07-07 2004-07-07 Derivados de malonamida, metodo de obtencion y composiciones farmaceuticas que los contienen. AR045033A1 (es)

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