PENG LI,HAILIN ZHENG,JUN ZHAO,LAWRENCE P. WENNOGLE
申请号：
ARP140101051
公开号：
AR095347A1
申请日:
2014.03.14
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
Provides PDE1 Inhibitors, processes for their production, their use as Pharmaceuticals and Pharmaceutical compositions that compriseUseful for the treatment of Parkinson's disease, Psychosis, Schizophrenia, etc., which are defined as PDE1 Family I phosphodiesterases.Claim 1: a compound of formula (1) wherein R is H or alkyl) r u00b9 c u2081 u208b u2084 (e.g., Methyl or ethyl)； (ii) R u00b2 and r u00b3 are independently H or alkyl c u2081 u208b u2086 (e.g.Methyl or ethyl)； (iii) r u2074 is H or alkyl c u2081 u208b u2084 (e.g., Methyl or ethyl)； (iv) is r u2075 aryl (e.g.) phenyl optionally substituted with one or more selected groups of C (= o) - alkyl c u2081 u208b u2086 (For example, C (= o) ch u2083) and hidroxialquilo c u2081 u208b u2086 (e.g.1 - hydroxyethyl)； (V) r u2076 and r u2077 are independently H or aryl (e.g. phenyl) optionally substituted with one or more selected from alkyl groups (For example, c u2081 u208b u2086Methyl or ethyl) and Halogen (e.g., F or CL), e.g. phenyl phenyl substituted or non substituted with one or more halogens (e.g.(f) or phenyl substituted with one or more alkyl c u2081 u208b u2086 and one or more alkyl or phenyl substituted with a Halogen and Halogen c u2081 u208b u2086, for example - fluorofenilo 4 or 3,4 - or difluorofenilo 4-fluoro-3 - methylphenyl； and (VI) n is 1, 2, 3, or 4； in free form or in Salt.Se proporciona inhibidores de PDE1, procesos para su producción, su uso como productos farmacéuticos, y composiciones farmacéuticas que las comprenden, útiles para el tratamiento de enfermedades de Parkinson, psicosis, esquizofrenia, etc., donde PDE1 se define como fosfodiesterasas de familia I. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque (i) R¹ es H o alquilo C₁₋₄ (por ejemplo, metilo o etilo)； (ii) R² y R³ son de modo independiente H o alquilo C₁₋₆ (por ejemplo, metilo o etilo)； (iii) R⁴ es H o alquilo C₁₋₄ (por ejemplo, metilo o etilo)； (iv) R⁵ es arilo (por ejemplo, fenilo) opcionalmente sustituido co
