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1. 发明授权

US5371099A Phenyl carboxamide isoxazoles 失效
标题翻译：苯基甲酰胺异恶唑
公开(公告)号：US5371099A
公开(公告)日：1994-12-06
申请号：US54893
申请日：1993-04-28
申请人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
发明人： Robert R. Bartlett , Matharu S. Singh , Elizabeth A. Kuo , Rudolf Schleyerbach , Robert Westwood
IPC分类号： A61K31/42 , A61P29/00 , C07C235/78 , C07C235/80 , C07C255/60 , C07C323/41 , C07D207/06 , C07D261/18 , C07D295/145 , C07D261/08 , C07D261/12
CPC分类号： C07D295/145 , C07C235/80 , C07C255/60 , C07C323/41 , C07D261/18 , C07C2101/02
摘要： A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.2 is alkyl of 1 to 3 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, R.sub.3 is --COOR.sub.6, R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms, R.sub.4 is selected from the group consisting of halogen, --CN, --NO.sub.2, --SCH.sub.3, alkylcarbonyl of 1 to 6 alkyl carbon atoms, --CX.sub.3, --WCX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --W--(CX.sub.2).sub.n --CX.sub.3, and --W--(CH.sub.2).sub.n --CX.sub.3, X is halogen, W is --O-- or --S--, n is 1, 2 or 3, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms and cycloalkyl of 3 to 6 carbon atoms and their salts with non-toxic pharmaceutically acceptable bases with the proviso that if R.sub.2 is alkyl of 1 to 3 carbon atoms, R.sub.1 is hydrogen and R.sub.4 is selected from the group consisting of halogen, --CX.sub.3, --(CH.sub.2).sub.n --CX.sub.3, --(CX.sub.2).sub.n --CX.sub.3, --OCX.sub.3, --O--(CX.sub.2).sub.n --CX.sub.3, and --O--(CH.sub.2).sub.n --CX.sub.3, X is halogen and n is 1, 2 or 3, R.sub.5 cannot be hydrogen having anti-inflammatory activity and their preparation and intermediates.
摘要翻译：选自下式的化合物的化合物其中R 1为氢或1至3个碳原子的烷基，R 2为1至3个碳原子的烷基或3至6个碳原子的环烷基，R 3为 -COOR 6，R 6是氢或1至3个碳原子的烷基，R 4选自卤素，-CN，-NO 2，-SCH 3，1至6个烷基碳原子的烷基羰基，-CX 3，-WCX 3，（CH 2）n -CX 3， - （CX 2）n -CX 3，-W-（CX 2）n -CX 3和-W-（CH 2）n -CX 3，X是卤素，W是-O-或-S-， n为1,2或3，R5选自氢，1至3个碳原子的烷基和3至6个碳原子的环烷基及其与无毒的药学上可接受的碱的盐，条件是如果R2为 1至3个碳原子的烷基，R1是氢，R4选自卤素，-CX3， - （CH2）n -CX3， - （CX2）n -CX3，-OCX3，-O-（CX2） n -CX3和-O-（CH2）n -CX3，X是卤素，n是1,2或3，R5不能是具有抗炎活性的氢及其制备和中间体。

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