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DERIVADOS DE 2H-PIRAZOLO[3,4-d]PIRIMIDINA-4,6(5H,7H)-DIONA, COMO INHIBIDORES DE PDE1
专利权人:
INTRA-CELLULAR THERAPIES; INC.
发明人:
LI, PENG,WENNOGLE, LAWRENCE P.,ZHAO, JUN,ZENG, HAILIN
申请号:
PE0011712011
公开号:
PE01202012A1
申请日:
2009.12.07
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Refers to a compound of formula (ii) where: L is s, so and SO2 r1 is H, alkyl c1-c6 alkyl R2 is H, or C1 - C6 unsubstituted or substituted with Hydroxy Halo, c1-c4 alkyl, cycloalkyl C3 - C8 not replaced or substituted with one or more amino R3 is connected to one of the nitrogens in the portion of the Pyrazolo of formula (ii) and is preferably - trifluoromethyl benzyl 4 - 4 - metoxibencil (1,2,,,4 - triazol yl) 1 - Benzyl -, 4 - benzyl), among others R4 is H, alkyl, cycloalkyl - C1 - C6, C8 heterocicloalquilo C3, C3, C8, aryl or heteroaryl, among others.Preferred compounds are: 2 - (4 - (1H - 1,2,4 - triazole - 1 - il) benzyl) - 5 - methyl - 3 - (methylthio) - 7 - Neopentyl - 2H - [3,4-d] pyrazole pyrimidine 4.6 (5h, 7H) - dione 2 - (4 - metoxibencil) - 5 - Methyl - 3 - 7 - Neopentyl - (phenylthio) - 2H - pyrazolo [3,4-d] pyrimidine 4.6 (5h, 7H) - dione 5 - methyl - 3 - (methylthio) - 7 - Neopentyl - 2 - (4 - (trifluoromethyl) benzyl ) - 2H - pyrazolo [3,4-d] pyrimidine 4.6 (5h, 7H) - dione, among others.Also referred to a Pharmaceutical composition. This Compound is an inhibitor of phosphodiesterase 1 (PDE1) useful in the treatment of Neurodegenerative Diseases, mental disorders, Circulatory and caridovascularesSE REFIERE A UN COMPUESTO DE FORMULA (II) DONDE: L ES S, SO Y SO2 R1 ES H, ALQUILO C1-C6 R2 ES H, ALQUILO C1-C6 NO SUSTITUIDO O SUSTITUIDO CON HALO O HIDROXI, ALQUILO C1-C4, CICLOALQUILO C3-C8 NO SUSTITUIDO O SUSTITUIDO CON UNO O MAS AMINO R3 ESTA UNIDO A UNO DE LOS NITROGENOS EN LA PORCION DEL PIRAZOLO DE LA FORMULA (II) Y ES DE PREFERENCIA 4-TRIFLUOROMETIL-BENCIL, 4-METOXIBENCIL, (1,2,4-TRIAZOL-1-IL)BENCIL, 4-METILSULFONIL-BENCIL, ENTRE OTROS R4 ES H, ALQUILO C1-C6, CICLOALQUILO C3-C8, HETEROCICLOALQUILO C3-C8, ARILO O HETEROARILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-(4-(1H-1,2,4-TRIAZOL-1-IL)BENCIL)-5-METIL-3-(METILTIO)-7-NEOPENTIL-2H-PIRAZOL[3,4-d]PIRIMIDIN-4,6(5H,7H)-DIONA 2-(4-METOXIBENCIL)-5-METIL-7-NEOPENTIL-3-(FENILTIO)-2H-PIRAZOLO[3,4-d]PIRIM
来源网站:
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