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DERIVADOS DE PIRAZINA COMO INHIBIDORES DE BACE
专利权人:
NOVARTIS AG
发明人:
TINTELNOT-BLOMLEY, MARINA,VEENSTRA, SIEM JACOB
申请号:
PE0008972012
公开号:
PE16402012A1
申请日:
2010.12.22
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Referring to a pyrazine Derivative of formula (i), wherein R1 is H, halogen, alkyl, cyano, C1, C8, among others R2 is an aryl, heteroaryl, among others R3 is H, halogen, alkyl, cyano, C1, C8, among others R4 cn is H, alkyl, halogen, C1 - C8, among others R5 is H, CN, halogen, alkyl of C1 C8 Other R6 is H, alkyl C8 haloalquilo C1 C1, C8, among others R7 is H, alkyl C1 C8Haloalquiloc1 - C8, among others E1 is C (R8) (R9) or C (R8) (R9) - C (R10) (R11) E2 is C (R12) (R13) or C (R12) (R13) - C (R14) (R15) R8 and R9 are H CN, halogen, alkyl, C1, C8, among others, R10 and R11 are h, CN, halogen, alkyl of C1 - C8, among others R12 and R13) is H, alkyl, halogen, C1, C8, among others R14 and R 15 ns is H, alkyl, halogen, C1, C8, among others.Preferred compounds are: [3 - (6 - amino - 2.4 - dimethyl - 3 - oxo - pirazin 2,3,4,5 - tetrahydro - 2 - 4 - fluoro - il) phenyl] - amide acid 5 - bromo carboxylic pyridin - 2 - [3 - (6 - amino - 2,4 Dimethyl 2,3,4,5 - tetrahydro - pirazin - 2 - 4 - fluoro - il) phenyl] - amide acid 5 - bromo carboxylic pyridin - 2 - [3 - (6 - amino - 2.4 - dimethyl - 3 - or XO 2,3,4,5 - tetrahydro - pirazin - 2 - il) - 4 - phenyl] - amide acid 5 - bromo - pyridin - 2 - carboxylic acid.Among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of bace and are useful in the treatment of Neurological Disorders such as Alzheimers diseaseREFERIDA A UN DERIVADO DE PIRAZINA DE FORMULA (I), DONDE R1 ES H, CIANO, HALOGENO, ALQUILO C1-C8, ENTRE OTROS R2 ES ARILO, HETEROARILO, ENTRE OTROS R3 ES H, CIANO, HALOGENO, ALQUILO C1-C8, ENTRE OTROS R4 ES H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS R5 ES H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS R6 ES H, ALQUILO C1-C8, HALOALQUILO C1-C8, ENTRE OTROS R7 ES H, ALQUILO C1-C8, HALOALQUILOC1-C8, ENTRE OTROS E1 ES C(R8)(R9) O C(R8)(R9)-C(R10)(R11) E2 ES C(R12)(R13) O C(R12)(R13)-C(R14)(R15) R8 Y R9 SON H, CN, HALOGENO, ALQUILO C1-C8, ENTRE OTROS R10 Y R11 SON H, CN, HALOGENO, ALQUILO C1-C8, E
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