MX370661B - Derivados de indolin-2-ona o pirrolo-piridin/pirimidin-2-ona. - Google Patents

Derivados de indolin-2-ona o pirrolo-piridin/pirimidin-2-ona.

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Publication number
MX370661B
MX370661B MX2015017491A MX2015017491A MX370661B MX 370661 B MX370661 B MX 370661B MX 2015017491 A MX2015017491 A MX 2015017491A MX 2015017491 A MX2015017491 A MX 2015017491A MX 370661 B MX370661 B MX 370661B
Authority
MX
Mexico
Prior art keywords
lower alkyl
halogen
substituted
cycloalkyl
disorders
Prior art date
Application number
MX2015017491A
Other languages
English (en)
Other versions
MX2015017491A (es
Inventor
Hilpert Hans
Brunner Daniela
Malberg Jessica
G Shankar Bavani
Kolczewski Sabine
Limberg Anja
Prinssen Eric
Riemer Claus
Stoll Theodor
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2015017491A publication Critical patent/MX2015017491A/es
Publication of MX370661B publication Critical patent/MX370661B/es

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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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Abstract

La presente invención está relacionada con compuestos con la fórmula general (ver Fórmula) en los que Ar es un grupo heteroarilo, que contiene uno, dos o tres heteroátomos, seleccionados a partir de N, S o O; R1 es hidrógeno, alquilo inferior, halógeno, amino, dimetilamino, ciano, alquilo inferior sustituido por halógeno, alquilo inferior sustituido por hidroxi, CH(OH)CF3, (CH2) o-alcoxi inferior, cicloalquilo opcionalmente sustituido por CF3, o heterocicloalquilo opcionalmente sustituido por alquilo inferior; R2 es hidrógeno, alquilo inferior, (CH2) o-cicloalquilo, (CH2) o-O-cicloalquilo, (CH2) o-alcoxi inferior, CH2) o-alcoxi inferior sustituido por halógeno, (CH2) o-heterocicloalquilo opcionalmente sustituido por alquilo inferior, (CH2) o-S(O)2- cicloalquilo, alquilo inferior sustituido por uno o dos hidroxi, alquilo inferior sustituido por uno o dos alcoxi inferior, (CH2) o-S(O)2-alquilo inferior, alquilo inferior sustituido por halógeno o CH2CH(OH)CF3; R3 es halógeno o alquilo inferior; X es CH o N; X1 esCH o N; n es1 o 2; o es 0, 1. 2 o 3; m es 0, 1 o 2; y la línea de puntos es un enlace o puede no serlo; así como con sales farmacéuticamente aceptables de los mismos, con una mezcla racémica, o con su correspondiente enantiómero y / o isómero óptico y / o estereoisómero de los mismos. Los compuestos se pueden utilizar para el tratamiento de ciertos trastornos del sistema nervioso central que son síntomas positivos (psicosis) y negativos de la esquizofrenia, el abuso de sustancias, adicción al alcohol y las drogas, los trastornos obsesivo-compulsivos, deterioro cognitivo, trastornos bipolares, trastornos del estado de ánimo, depresión mayor, depresión resistente al tratamiento, trastornos de ansiedad, enfermedad de Alzheimer, autismo, enfermedad de Parkinson, dolor crónico, trastorno límite de la personalidad, trastornos del sueño, síndrome de fatiga crónica, rigidez, efectos antiinflamatorios en artritis y problemas de equilibrio.
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