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ES2504090T3 - Compuestos de aril bencilamina - Google Patents

Compuestos de aril bencilamina Download PDF

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Publication number
ES2504090T3
ES2504090T3 ES11701825.9T ES11701825T ES2504090T3 ES 2504090 T3 ES2504090 T3 ES 2504090T3 ES 11701825 T ES11701825 T ES 11701825T ES 2504090 T3 ES2504090 T3 ES 2504090T3
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carbon atoms
halogen
alkyl
optionally substituted
alkoxy
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Daniela Angst
Birgit Bollbuck
Philipp Janser
Jean Quancard
Nikolaus Johannes Stiefl
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Novartis AG
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Novartis AG
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Abstract

Un compuesto de fórmula (l), o una sal farmacéuticamente aceptable del mismo; en donde, R1 es hidrógeno, halógeno, o alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno; R2 es halógeno, alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno, ciano, o alcoxi de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno; o R1 y R2, junto con los átomos de carbono a los que están unidos, forman un anillo arilo con 6 a 10 átomos de carbono, el cual puede estar opcionalmente sustituido por 1 a 4 sustituyentes seleccionados a partir de ciano, alquilo de 1 a 4 átomos de carbono opcionalmente sustituido por halógeno, alcoxi de 1 a 4 átomos de carbono opcionalmente sustituido por halógeno, halógeno; R3 es hidrógeno, halógeno, o alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno; R4 es hidrógeno, cicloalquilo de 3 a 6 átomos de carbono, o alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno; R5 es hidrógeno o alquilo de 1 a 6 átomos de carbono; R6 y R7 se seleccionan independientemente a partir de H y alquilo de 1 a 6 átomos de carbono, o R8 y R9 pueden formar, junto con el átomo de carbono al que están unidos, un anillo carbocíclico saturado de 3 a 7 miembros; R8 y R9 se seleccionan independientemente a partir de H y alquilo de 1 a 6 átomos de carbono, o pueden formar, junto con los átomos con los que están unidos, un anillo heterocíclico de 4 a 7 miembros opcionalmente sustituido una o más veces por alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno, trifluorometilo, hidroxilo, alcoxi de 1 a 6 átomos de carbono, amino; n >= 1, 2, 3 o 4; R10 es hidrógeno, alquilo de 1 a 6 átomos de carbono, amino, hidroxilo, o alcoxi de 1 a 6 átomos de carbono; R se selecciona a partir de H; fenilo que está opcionalmente sustituido por alquilo de 1 a 6 átomos de carbono, alcoxi de 1 a 6 átomos de carbono, halógeno o hidroxilo; y alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por alcoxi de 1 a 6 átomos de carbono, halógeno, hidroxilo, o fenilo opcionalmente sustituido por alquilo de 1 a 6 átomos de carbono, alcoxi de 1 a 6 átomos de carbono, halógeno o hidroxilo, X1, X2, X3 y X4, se seleccionan cada uno independientemente a partir de N o CR11, R11 en cada caso se selecciona independientemente a partir de H, halógeno, ciano, alcoxi de 1 a 6 átomos de carbono, alquilo de 1 a 6 átomos de carbono opcionalmente sustituido por halógeno; o -SO2 - alquilo de 1 a 6 átomos de carbono; y Y representa independientemente en cada caso que se presente, CR12R13, en donde R12 y R13 se seleccionan independientemente a partir de H y alquilo de 1 a 6 átomos de carbono.

Description

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isoflurano. Se utilizan de dos a tres animales en cada grupo. Las muestras de sangre entera se someten a análisis hematológico. Los recuentos de linfocitos periféricos se determinan utilizando un analizador automatizado. El Sistema de Hematología utiliza una combinación de dispersión de luz, tinción citoquímica, y densidad nuclear en dos canales independientes, para medir los recuentos totales y diferenciales de glóbulos blancos. La reducción de
5 linfocitos provocada por cada compuesto de prueba se calcula comparando los recuentos de linfocitos medidos después de cada tratamiento, con los recuentos de linfocitos promedio medidos en cinco a ocho ratones o ratas no tratados, respectivamente. Los datos se presentan como el promedio ± STDEV (desviación estándar).
Como ejemplo, la Tabla 2 muestra el efecto sobre los recuentos de linfocitos en los puntos del tiempo indicados en horas después de administración oral de una dosis dada en mg/kg de algunos compuestos de fórmula (l) a las
10 especies indicadas, comparado con los recuentos de linfocitos promedio de los animales no tratados.
Tabla 2:
Ejemplo No.
Especie Dosis (mg/kg) Puto de tiempo (horas) Recuentos de linfocitos residuales 24 horas después la dosificación por vía oral
21
Ratones C57BL/6NCrl 30 24 17,8 % ± 2,3
55
Ratones C57BL/6NCrl 30 24 43,6 % ± 4,6
43
Ratones C57BL/6NCrl 30 24 21,8% ± 3,4
29
Ratones C57BL/6NCrl 30 24 35,6 % ± 4,6
34
Ratones C57BL/6NCrl 30 24 24,2 % ± 2,3
62
Ratones C57BL/6NCrl 30 24 31,5 % ± 8,0
42
Ratones C57BL/6NCrl 30 24 19,4 % ± 2,3
42
Ratas Lewis 30 24 22,2 % ± 6,7
65
Ratones C57BL/6NCrl 30 24 22,6% ± 11,4
66
Ratones C57BL/6NCrl 30 24 19,4 % ± 2,3
41
Ratones C57BL/6NCrl 30 24 20,2 % ± 8,0
30
Ratones C57BL/6NCrl 30 24 19,4 % ± 2,3
30
Ratas Lewis 30 24 26,9 % ± 13,0
32
Ratones C57BL/6NCrl 30 24 17,0 % ± 3,4
33
Ratones C57BL/6NCrl 30 24 16,2 % ± 2,3
23
Ratones C57BL/6NCrl 30 24 25,1 % ± 3,4
70
Ratones C57BL/6NCrl 30 24 20,2 % ± 5,7
31
Ratones C57BU6NCrl 30 24 23,4 % ± 3,4
61
Ratones C57BU6NCrl 30 24 16,2 % ± 4,6
84
Ratas Lewis 30 24 16,8 % ± 7,2
85
Ratas Lewis 30 24 11,6% ± 0,3
75
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