AR070750A1 - Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento - Google Patents

Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento

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Publication number
AR070750A1
AR070750A1 ARP080103747A ARP080103747A AR070750A1 AR 070750 A1 AR070750 A1 AR 070750A1 AR P080103747 A ARP080103747 A AR P080103747A AR P080103747 A ARP080103747 A AR P080103747A AR 070750 A1 AR070750 A1 AR 070750A1
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Argentina
Prior art keywords
alkyl
substituted
group
fluorine atoms
cycloalkyl
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ARP080103747A
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English (en)
Inventor
Angelo Ceci
Ingo Konetzki
Juergen Mack
Henning Priepke
Norbert Hauel
Enzo Cereda
Annette Schuler-Metz
Henri Doods
Walter Rainer
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Boehringer Ingelheim Int
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Publication of AR070750A1 publication Critical patent/AR070750A1/es

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    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having 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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    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
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Abstract

Reivindicacion 1: Compuestos caracterizados porque tienen la formula general (1) en la cual R1 es (a) un grupo alquilo C1-6 eventualmente sustituido con un radical R1,1, (b) un grupo alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (c) un grupo cicloalquilo C3-6 eventualmente sustituido con un radical R1,2, (d) un grupo alquenilo C2-6, (e) un grupo alquinilo C2-6, (f) un grupo aril-alquileno C0-2 eventualmente sustituido con 1, 2 o 3 radicales R1,3, (g) un radical heteroarilo de cinco miembros eventualmente sustituido con 1, 2 o 3 radicales R1,4, que al menos contiene un átomo de N, O o S y que eventualmente contiene además uno, dos o tres otros átomos de N y que además puede estar benzocondensado, (h) un radical heteroarilo de seis miembros eventualmente sustituido con un radical R1,4, que contiene uno, dos o tres átomos de N y que además puede estar benzocondensado, (i) -O-R1,1,1 o (j) -NR1,1,2R1,1,4; R1,1 es halogeno, -NO2, -CN, cicloalquilo C3-6, -OR1,1,1, -SR1,1,1, -C(O)R1,1,1, -S(O)2-R1,1,2, -OS(O)2-R1,1,1, -CO2R1,1,1, -OC(O)-R1,1,1, NR1,1,3R1,1,4, -NR1,1,3-C(O)R1,1,1, -NR1,1,3-C(O)-R1,1,1, -NR1,1,3-C(O)2-R1,1,1 o -C(O)-NR1,1,3R1,1,4; R1,1,1 es (a) H, (b) alquilo C1-4, (c) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (d) un grupo fenilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,1, (e) cicloalquilo C3-6 o (f) un grupo piridilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,2; R1,1,1,1 de modo independiente entre sí, es (a) halogeno, -NO2, -CN, -OH, -O-alquilo C1-4, cicloalquilo C3-6, alquilo C1-4 o (b) alquilo C1-3 en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R1,1,1,2 de modo independiente entre sí, es halogeno o alquilo C1-4; R1,1,2 es (a) alquilo C1-4, (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (c) -O-alquilo C1-4 o (d) un grupo fenilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,1; R1,1,3, R1,1,4 son, de modo independiente entre sí, (a) H, (b) un grupo alquilo C1-4 eventualmente sustituido con 1, 2 o 3 radicales R1,1,4,1, (c) un grupo fenilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,1, (d) cicloalquilo C3-6; o R1,1,3 y R1,1,4 junto con el átomo de N, al que están unidos, forman un anillo heterocíclico de 4, 5 o 6 miembros que puede contener adicionalmente otro heteroátomo seleccionado de N, O y S, o R1,1,3 y R1,1,4 junto con el átomo de N, al que están unidos, forman una imida cíclica; R1,1,4,1 de modo independiente entre sí, halogeno, -NH2, -NH(alquilo C1-4), -N(alquilo C1-4)2 o -SO2-R1,1,2; R1,2 es halogeno, -NO2, -CN o fenilo; R1,3 es (a) halogeno, -NO2, -CN, -OR1,1,1, -SR1,1,1, -CO2R1,1,1, alquilo C1-6 o (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R1,4 es, de modo independiente entre sí, (a) halogeno, -NO2, -CN, -OR1,1,1, -SR1,1,1, -S(O)-R1,1,2, -S(O)2-R1,1,2, -NR1,1,3R1,1,4, alquilo C1-6, (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, o (c) un grupo oxo; R2 es (a) H, alquilo C1-4 o (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R3 es, de modo independiente entre sí, (a) H, halogeno, -CN, -OH, alquilo C1-6, cicloalquilo C3-7, -O-alquilo C1-4, -O-CF3, -O-cicloalquilo C3-6, -N(alquilo C1-3)2, -C(O)-NH2, -(SO2)NH2, -SO2-alquilo C1-3, o (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R4, R5, R6, R7, R8 son, de modo independiente entre sí, (a) H, halogeno, -CN, -OH, (b) alquilo C1-6, en donde dos sustituyentes adyacentes pueden representar juntos un grupo trimetileno o tetrametileno, (c) alquilo C1-3 en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (d) cicloalquilo C3-7, (e) -O-alquilo C1-6, en donde dos sustituyentes adyacentes pueden representar un grupo metilendioxi o etilendioxi, (f) -O-CF3, -O-cicloalquilo C3-7, (g) -NH2, -NH(alquilo C1-3), -N(alquilo C1-3)2, (h) -C(O)-R8,1, (i) -SO2R8,2, (j) un grupo heteroarilo de cinco miembros eventualmente sustituido con uno o dos grupos alquilo C1-3, que está seleccionado del grupo compuesto por pirrolilo, oxazolilo, isoxazolilo, oxadiazolilo, tiazolilo, isotiazolilo, tiadiazolilo, imidazolilo, pirazolilo, triazolilo y tetrazolilo o (k) un grupo heteroarilo de seis miembros eventualmente sustituido con uno o dos grupos alquilo C1-3, que está seleccionado del grupo compuesto por piridilo, pirimidinilo, pirazinilo, piridazinilo y triazinilo; R8,1 es -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, N-acetidinilo, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, -OH, -O-alquilo C1-8 u -O-cicloalquilo C3-7; R8,2 es -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, N-acetidinilo, N-pirrolidinilo, N-piperidinilo o N-morfolinilo; y n es una de las cifras 0, 1, 2, 3 o 4; sus enantiomeros, sus diastereoisomeros, sus mezclas y sus sales, en particular sus sales fisiologicamente compatibles con ácidos o bases orgánicos o inorgánicos. Reivindicacion 16: Sales fisiologicamente compatibles de los compuestos segun una de las reivindicaciones 1 a 15 caracterizadas porque son sales con ácidos o bases inorgánicos u orgánicos. Reivindicacion 17: Medicamento, caracterizado porque contiene un compuesto segun al menos una de las reivindicaciones 1 a 15 o una sal fisiologicamente compatible segun la reivindicacion 16, eventualmente junto a una o varias sustancias de soporte y/o agentes diluyentes inertes. Reivindicacion 18: Uso de un compuesto de acuerdo con al menos una de las reivindicaciones 1 a 16 caracterizado porque es para preparar un medicamento para el tratamiento agudo y preventivo de dolores agudos, dolores viscerales, dolores neuropáticos, dolores inflamatorios / mediados por el receptor del dolor, dolores tumorales y afecciones de cefaleas. Reivindicacion 19: Procedimiento para la preparacion de un medicamento segun la reivindicacion 17, caracterizado porque, por vía no química, un compuesto segun al menos una de las reivindicaciones 1 a 16 se incorpora en una o varias sustancias de soporte y/o agentes diluyentes inertes.
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