BLEICHER, KONRAD,FLOHR, ALEXANDER,ZBINDEN, KATRIN GROEBKE,GRUBER, FELIX,KOERNER, MATTHIAS,KUHN, BERND,PETERS, JENS-UWE,RODRIGUEZ SARMIENTO, ROSA MARIA
申请号：
PE0022982012
公开号：
PE02792013A1
申请日:
2011.06.06
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Heteroaryl nitrogen relates to compounds of formula (i) where n is CH or A1 A2 is cr19 or n, where R19 is H or tetrahydrofuran-2-ylmethyl - ilo 2 b is aryl or heteroaryl alkyl alkoxy optionally substituted Lower, Lower, Lower haloalquilo, CN, among others r1 is lower alkyl, Lac Oxy CN, halogen, LowerAmong others, R2 and R3 are each H or lower alkyl R4 is optionally substituted aryl or heteroaryl with hydroxyl, halogen, CN, among others R5 and R6 are each less than h, alkyl, cycloalkyl, cianoalquilo, among others.Preferred compounds are: (DIMETHYLCARBAMOYL - 3 - 1 - methyl - 1h-pyrazol-4-yl) - 6 - cyclopropyl amide acid - 3 - (5 - ilamino - pyrimidin-2-yl) - pyridin - 2 - carboxylic acid (1 - methyl - 3 - metilcarbamoil - 1h-pyrazol-4-yl) - amide acid - cyclopropyl - (3 - 6 - 5 - ilamino pyrimidin-2-yl) - pyridin - carboxylic acid (- 2 - carbamoyl - 1 - 3 - methyl) - 1H pyrazole 4 - il) - 6 - cyclopropyl amide acid - 3 - (5 - ilamino - pyrimidin-2-yl) - pyridin - 2 - carboxylic acid among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are inhibitors of phosphodiesterase pde10a being useful in the treatment of schizophrenia, Anxiety Disorder, depressionSE REFIERE A COMPUESTOS HETEROARILO NITROGENADOS DE FORMULA (I) DONDE A1 ES CH O N A2 ES CR19 O N, EN DONDE R19 ES H O TETRAHIDROFURAN-2-ILO B ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS CON ALQUILO INFERIOR, ALCOXI INFERIOR, HALOALQUILO INFERIOR, CN, ENTRE OTROS R1 ES ALQUILO INFERIOR, ALCOXI INFERIOR, CN, HALOGENO, ENTRE OTROS R2 Y R3 SON CADA UNO H O ALQUILO INFERIOR R4 ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS CON HIDROXILO, HALOGENO, CN, ENTRE OTROS R5 Y R6 SON CADA UNO H, ALQUILO INFERIOR, CIANOALQUILO INFERIOR, CICLOALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (3-DIMETILCARBAMOIL-1-METIL-1H-PIRAZOL-4-IL)-AMIDA DE ACIDO 6-CICLOPROPIL-3-(PIRIMIDIN-5-ILAMINO)-PIRIDIN-2-CARBOXILICO (1-METIL-3-METILCARBAMOIL-1H-PIRAZOL-4-IL)-AMIDA DE ACIDO 6-CICLOPROPIL
