Luigi Piero Stasi,Lucio Claudio Rovati,Roberto Artusi,Fabrizio Colace,Stefano Mandelli,Lorenzo Perugini
申请号：
US14366743
公开号：
US09062033B2
申请日:
2012.12.20
申请国别(地区):
US
年份:
2015
代理人:
摘要：
The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q； Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or a group —O[(CR1R2]pQ1； or Q may be a group Q2； Q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2； or corresponds to 2,2-difluoro-benzo[d][1,3]dioxol-4-yl； Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: C1 C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN； P is a 6-membered heteroaryl or a 8-1 1 membered bicyclic heteroaryl group, which may be substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN； R1 is hydrogen or C1-C3 alkyl； R2 is hydrogen or C1-C3 alkyl； n is 1, 2 or 3； p is 0, 1 or 2； and with the proviso that when R corresponds to phenyl, P is substituted by at least one CF3； processes for the preparation of those compounds, pharmaceutical compositions containing one or more compounds of formula (I) and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
