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    • 24. 发明授权
    • Cyclohexane derivatives
    • 环己烷衍生物
    • US5708026A
    • 1998-01-13
    • US448470
    • 1996-07-15
    • Roger CrossleyAlbert Opalko
    • Roger CrossleyAlbert Opalko
    • C07D521/00A61K31/13A61K31/135A61K31/215A61P25/00A61P25/04A61P25/08A61P25/20A61P25/24A61P25/26A61P25/28C07C211/39C07C211/44C07C211/54C07C211/57C07C215/42C07C217/52C07C217/74C07C225/20C07C227/16C07C229/46A61K31/24C07C211/25C07C229/34
    • C07C217/74C07C229/46C07C2101/14
    • This invention concerns compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted line represents an optional bond, one of R.sup.1 and R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.16 aralkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8, --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH wherein n is 0 or 1, R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7)alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl; the other of R.sup.1 and R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl; R.sup.3 is C.sub.6 -C.sub.10 aryl or heteroaryl group optionally substituted by one or more substituents the same or differnet, R.sup.2 and R.sup.4 independently represent hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl or R.sup.2 also represents COR.sup.11 where R.sup.11 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; one of Y and Y.sub.1 is ##STR2## where R.sup.13 represents hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl; the other of Y and Y.sub.1 is --CHR.sup.12 -- where R.sup.12 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl,which compounds have pharmaceutical uses conferred by their ability to block voltage gated potassium channels.
    • PCT No.PCT / GB95 / 00280 Sec。 371日期:1996年7月15日 102(e)日期1996年7月15日PCT提交1995年2月10日PCT公布。 出版物WO95 / 21813 日期:1995年8月17日本发明涉及以下通式的化合物:其中虚线代表任选的键,R1和R5之一表示氢,C1-C6烷基,C7- C16芳烷基, - (CHR6)nCHR7CN, - (CHR6)nCHR7CONH2, - (CHR6)nCHR7COOR8, - (CHR6)nCHR7CH2OH其中n是0或1,R6和R7独立地表示氢,C1-C6烷基或C7-C16芳烷基 - ,和R 7还表示羟基(C 1 -C 6)烷基 - ,(C 2 -C 7)烷酰氧基(C 1 -C 6)烷基 - ,(C 1 -C 6烷氧基)羰基 - ,R 8是氢或C 1 -C 6烷基; R 1和R 5中的另一个是氢,C 1 -C 6烷基或C 7 -C 16芳烷基; R3是任选被一个或多个相同或不同取代基取代的C 6 -C 10芳基或杂芳基,R 2和R 4独立地表示氢,或式-CR a R b R c基团,其中R a,R b和R c独立地选自氢,C 1 -C 6 烷基,任选取代的C 6 -C 10芳基,任选取代的杂芳基,被任选取代的C 6 -C 10芳基或杂芳基或R 2取代的C 1 -C 6烷基也表示COR 11,其中R 11是C 1 -C 6烷基,C 1 -C 6烷氧基或任选取代的(C 6 -C 10芳基)烷基或杂芳基烷基; Y和Y1之一是,其中R13表示氢,C1-C6烷基或C7-C16芳烷基; Y和Y1中的另一个是-CHR12-,其中R12是氢,C1-C6烷基或C7-C16芳烷基,这些化合物具有通过其阻挡电压门控钾通道的能力赋予的药学用途。