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    • 9. 发明授权
    • Propanobicyclic amine derivatives for CNS disorders
    • 中枢神经系统疾病的丙酰胆碱胺衍生物
    • US5098916A
    • 1992-03-24
    • US501216
    • 1990-03-29
    • Nancy M. GrayBrian K. Cheng
    • Nancy M. GrayBrian K. Cheng
    • A61K31/445A61K31/495A61P9/10A61P25/00C07C211/38C07C211/42C07D295/02C07D295/03C07D295/033C07D295/08C07D295/088
    • C07D295/088C07C211/42C07D295/03C07D295/033C07C2103/78
    • Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.17 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R.sup.3, R.sup.4, ring-position two, ring-position three and ring-position four; or the pharmaceutically-acceptable salts thereof.