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1. 发明授权

US06939871B2 Benzoxazinone derivatives, their preparation and use 失效
公开(公告)号：US06939871B2
公开(公告)日：2005-09-06
申请号：US10415119
申请日：2001-10-22
申请人： Christopher Norbert Johnson , Harshad Kantilal Rami , Geoffrey Stemp , Kevin Thewlis , Mervyn Thompson , Antonio Keuok Keong Vong
发明人： Christopher Norbert Johnson , Harshad Kantilal Rami , Geoffrey Stemp , Kevin Thewlis , Mervyn Thompson , Antonio Keuok Keong Vong
IPC分类号： A61K31/538 , A61P25/00 , A61P25/22 , A61P25/24 , C07D413/12 , C07D413/14 , C07D413/10 , A61P25/18
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is phenyl, naphthyl, a monocyclic heteroaromatic group or a bicyclic heteroaromatic group, said Ar group being optionally substituted by 1-4 substituents, which may be the same or different, and which are selected from the group consisting of: halogen, hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-6alkyl, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-6alkoxy, arylC1-6alkoxy, C1-6alkylthio, C1-6alkoxyC1-6-alkyl, C3-7cycloalkylC1-6alkoxy, C1-6alkanoyl, C1-6alkoxycarbonyl, C1-6alkylsulfonyl, C1-6alkylsulfinyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, C1-6alkylsulfonamido, C1-6alkylamido, C1-6alkylsulfonamidoC1-6alkyl, C1-6alkylamidoC1-6alkyl, arylsulfonamido, arylcarboxamido, alkylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, arolC1-6alkyl, arylC1-6alkanoyl, a group R OCO(CH2)s, R CON(R )(CH2)s, R R NCO(CH2)s or R R NSO2(CH2) where each of R and R independently represents a hydrogen atom or C1-4alkyl or R and R form part of a C3-6azacyloalkane or C3-6(2-oxo)azacycloalkane ring and s represents zero or an integer from 1 to 4, and a group Ar Z, wherein Z represents a single bond, O, S or CH2 and Ar represents a phenyl or a monocyclic heteroaromatic group, said Ar group being optionally substituted by 1-3 substituents, which may be the same or different, and which are selected from the group consisting of a halogen, hydroxy, cyano, trifluoromethyl, C1-6alkyl, C1-6alkoxy or C1-6alkanoyl; when Ar is a phenyl or a monocyclic heteroaromatic group, substitutents positioned ortho to one another may be linked to form a 5- or 6-membered ring; R is hydrogen, C1-6alkyl, C3-6alkenyl, C3-6alkynyl or arylC1-6alkyl; R is halogen, C1-6alkyl, cyano, CF3, C1-6alkanoyl, C1-6alkoxy or hydroxy; X is CH or N; Y is a single bond, O, or C═O; p is 0, 1 or 2; r is 0, 1, 2 or 3; m is 2, 3 or 4; n and q are independently 1 or 2. Processes for preparing the compounds, pharmaceutical compositions containing them and their use as medicaments for various CNS disorders, including deression and/or anxiety, are also disclosed.

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