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COMPUESTOS HETEROCICLICOS DE NITROGENO UTILES COMO INHIBIDORES DE PDE10
专利权人:
AMGEN INC.
发明人:
ALLEN, JENNIFER R.,CHEN, JIAN J.,FROHN, MICHAEL J.,HARRINGTON, ESSA HU,LIU, QINGYIAN,PICKERELL, ALEXANDER J.,RUMFELT, SHANNON,RZASA, ROBERT M.,ZHONG, WENGE
申请号:
PE0021592012
公开号:
PE05762013A1
申请日:
2011.05.11
申请国别(地区):
PE
年份:
2013
代理人:
摘要:
Relates to Heterocyclic compounds of formula (i) wherein x1 and X4 are each n is n or Cr6 x2 or X3 is n or CR2 and Cr3, where R2 and R3 are each h, Halo, CN, o, among others R6, R1 is alkyl, Halo, CN, (C1 - C4), among others R1 - ORC or alkyl (C0 - C4) - L1, where RC is alkyl (C0 - C4) - L1 or L2 is Monociclico n Ring 3 to 7 members, among others L2 is a bicyclic ring 6 to 12 members,Among others, R4A is H, o, F, cl or Methyl r4b is Halo, CN, o, or alkyl (c1-c4), among others, and is (C0 C4 alkyl -, - C = o, so or SO2 R5 is pyridine, pyrimidine, benzimidazole, among others M is 0 to 4 P and q are each of 0 to 6, where the sum of P and q is from 2 to 6.Preferred compounds are: (1h served - 2 - il) - [3 - (3-phenyl pyridin-2-yl) - azetidin - triazin-1-yl] - methanone [3 - (3 - phenyl - 2 - pirazin - il) - azetidin - triazin-1-yl] - [1 - (2,2,2 trifluoro ethyl) - 1H - served - 2 - yl] - methanone 1 - (3 - (3 - [1 - (1H - served - 2 - carbonyl) - azetidin - 3 - yl] - pirazin il} - 2 - phenyl) - ethanone among others . It also relates to a Pharmaceutical composition.These compounds are inhibitors of phosphodiesterase 10 being useful in the treatment of Obesity, Huntingtons disease, Schizophrenia, bipolar disorderSE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE X1 Y X4 SON CADA UNO N O CR6 X2 ES N O CR2 X3 ES N O CR3, EN DONDE R2 Y R3 SON CADA UNO H, HALO, CN, OH, ENTRE OTROS R6 ES R1, HALO, CN, ALQUILO(C1-C4), ENTRE OTROS R1 -ORc O ALQUILO(C0-C4)-L1, EN DONDE Rc ES ALQUILO(C0-C4)-L2 L1 ES UN ANILLO MONOCICLICO DE 3 A 7 MIENBROS, ENTRE OTROS L2 ES UN ANILLO BICICLICO DE 6 A 12 MIEMBROS, ENTRE OTROS R4a ES H, OH, F, Cl O METILO R4b ES HALO, CN, OH, O-ALQUILO(C1-C4), ENTRE OTROS Y ES ALQUILO(C0-C4), -C=O, SO O SO2 R5 ES PIRIDINA, PIRIMIDINA, BENZIMIDAZOL, ENTRE OTROS m ES DE 0 A 4 p Y q SON CADA UNO DE 0 A 6 DONDE LA SUMA DE p Y q ES DE 2 HASTA 6. SON COMPUESTOS PREFERIDOS: (1H-BENZOIMIDAZOL-2-IL)-[3-(3-FENIL-PIRIDIN-2-IL)-AZETIDIN-1-IL]-METANONA [3-(3-FENIL-PIRA
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