KUDUDK, SCOTT D.,SCHLEGEL, KELLY-ANN,YANG, ZHI-QIANG
申请号：
PE0008302012
公开号：
PE16132012A1
申请日:
2010.12.13
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a quinoline derivative Compound of formula (i), where X1 is n o n - o x2 X3 is - CH2 - CH2 -, - or - CH2 - CH2 -, or - or CH2 x4, X5, X6 and X7 are n, N or CH, or r1 is H, halogen, alkyl of C1 - C6 2a, among others and R2B are h, Oh, halogen, or together form = R3 is Halogen, alkyl or c1-c6 alkyl, S C1 - C6, among others R4 is Oh, halogen, alkyl of C1 - C6 or c1-c6 alkyl, among others.Preferred compounds are: 4 - [(3 - 6 - cloropiridin - yl) methyl] - N - [(1S, 2S) - 2 - hidroxiciclohexil] quinoline carboxamide - 2 -, N - [(1S, 2S) - 2 - hidroxiciclohexil] - [4 - (6-methylpyridin-3-yl) methyl - 2 -] quinoline carboxamide, N - [(1S, 2S) - 2 - hidroxiciclohexil] - 4 - (pyridin - 3 - methyl - 2 -) quinoline carboxamide, among others. It also relates to a Pharmaceutical composition.These compounds are positive allosteric modulators of M1 Receptors and are useful in the treatment of disorders such as Alzheimers disease, Schizophrenia, pain or Sleep DisordersREFERIDA A UN COMPUESTO DERIVADO DE QUINOLINA DE FORMULA (I), DONDE X1 ES N O N-O X2-X3 ES -CH2-CH2-, -O-CH2, -CH2-O- O CH2 X4, X5, X6 Y X7 SON N, N-O, CH, O R1 ES H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS R2A Y R2B SON H, OH, HALOGENO, JUNTOS FORMAN =O R3 ES HALOGENO, O-ALQUILO C1-C6, S-ALQUILO C1-C6, ENTRE OTROS R4 ES OH, HALOGENO, ALQUILO C1-C6, O-ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-[(6-CLOROPIRIDIN-3-IL)METIL]-N-[(1S,2S)-2-HIDROXICICLOHEXIL]QUINOLINA-2-CARBOXAMIDA, N-[(1S,2S)-2-HIDROXICICLOHEXIL]-4-[(6-METILPIRIDIN-3-IL)METIL]QUINOLINA-2-CARBOXAMIDA, N-[(1S,2S)-2-HIDROXICICLOHEXIL]-4-(PIRIDIN-3-ILMETIL)QUINOLINA-2-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES ALOSTERICOS POSITIVOS DE LOS RECEPTORES M1 Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS TALES COMO LA ENFERMEDAD DE ALZHEIMER, ESQUIZOFRENIA, TRASTORNOS DEL DOLOR O DEL SUENO
