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DERIVADOS DE PIRAZOLO[3,4-d]PIRIMIDINA COMO INHIBIDORES PDE1
专利权人:
INTRA-CELLULAR THERAPIES; INC.
发明人:
LI, PENG,WENNOGLE, LAWRENCE P.,ZHAO, JUN,ZENG, HAILIN
申请号:
PE0011652011
公开号:
PE09442011A1
申请日:
2009.12.07
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Referring to a Derivative of pyrazole compounds of formula (ii), where q is c = C (S) = N (r6) or C (R14) (R15) r1 is H or c1-c6 alkyl R2 is H, alkyl haloalquilo C1 - C6 C1 - C6, among others R3 is D - e - F -, heteroalquilo of 1 to 6 carbon Atoms replaced with haloalquilo C1 - C6, among others d is an enl Ace or alquileno C1 - C6 and is a Link, alquileno c1-c4, amino, among others f is H, haloC1 - C6 alkyl, phenyl, among others R4 and R5 are C1 - C6 h, alkyl, cycloalkyl, phenyl C3, C8, among others R6 is H, alkyl or cycloalkyl C3 - C1 - C6 C8.Preferred compounds are: 7 - isobutyl - 5 - methyl - 3 - (phenylamino) - 2 - (4 - (pyridin-2-yl) benzyl) - 4 - tioxo - 4,5-dihydro-2h - pyrazolo [3,4-d] pyrimidine 6 (7H) - One, - isobutyl - 5 - 7 Methyl 4 - (metilimino) - 3 - (phenylamino) - 2 - (4 - (pyridin-2-yl) benzyl) - 4,5-dihydro-2h - pyrazolo [3,4-d] pyrimidine 6 (7H) - One, 2 - (4 - (1H - 1,2,4 - triazole - 1 - IL) benzyl) - 5 - methyl - 3 - 7 - Neopentyl - (phenylamino) - 4 - tioxo - 4,5-dihydro-2h - pyrazolo [3,4 - d] pyrimidine 6 (7H) - One, among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of phosphodiesterase 1 (PDE1) and are useful in the treatment of Parkinsons disease, narcolepsy, Schizophrenia, among othersREFERIDA A UN COMPUESTOS DERIVADO DE PIRAZOL DE FORMULA (II), DONDE Q ES C(=S), C(=N(R6)) O C(R14)(R15) R1 ES H O ALQUILO C1-C6 R2 ES H, ALQUILO C1-C6, HALOALQUILO C1-C6, ENTRE OTROS R3 ES D-E-F-, HETEROALQUILO DE 1 A 6 ATOMOS DE CARBONO SUSTITUIDO CON HALOALQUILO C1-C6, ENTRE OTROS D ES UN ENLACE O ALQUILENO C1-C6 E ES UN ENLACE, ALQUILENO C1-C4, AMINO, ENTRE OTROS F ES H, HALO, ALQUILO C1-C6, FENILO, ENTRE OTROS R4 Y R5 SON H, ALQUILO C1-C6, FENILO, CICLOALQUILO C3-C8, ENTRE OTROS R6 ES H, ALQUILO C1-C6 O CICLOALQUILO C3-C8. SON COMPUESTOS PREFERIDOS: 7-ISOBUTIL-5-METIL-3-(FENILAMINO)-2-(4-(PIRIDIN-2-IL)BENCIL)-4-TIOXO-4,5-DIHIDRO-2H-PIRAZOLO[3,4-d]PIRIMIDIN-6(7H)-ONA, 7-ISOBUTIL-5-METIL-4-(METILIMINO)-3-(FENIL
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