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COMPOSÉS CHIMIQUES
专利权人:
ROTTAPHARM SPA
发明人:
STASI, Luigi Piero,ROVATI, Lucio Claudio,ARTUSI, Roberto,COLACE, Fabrizio,MANDELLI, Stefano,PERUGINI, Lorenzo
申请号:
EPEP2012/076447
公开号:
WO2013/092893A1
申请日:
2012.12.20
申请国别(地区):
EP
年份:
2013
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 bicylic 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.L'invention concerne un nouveau composé de formule (I) ou un stéréoisomère, ou un racémate ou un mélange ou un sel pharmaceutiquement acceptable de ceux-ci : formule dans laquelle : R représente phényle ou un cycle hétéroaryle à 5 ou 6 chaînons, contenant 1 à 3 hétéroatomes choisis parmi S, N et O, de tels cycles pouvant être éventuellement substitués par n groupes Q ; Q est choisi dans un groupe consistant en : alkyle en C1-C4, halogène, halo-alkyle
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