| 摘要 |
<p>1,2,3,6-Tetrahydroisonicotinic acid and derivatives thereof, methods and starting products for their preparation, and pharmaceutical compositions containing them. Compounds of formula …<CHEM>… is which R sec is hydrogen, acetyl or a group… ……R1-O-@-… wherein R1 is C1-8 alkyl; phenyl; substituted phenyl, phenylalkyl in which the phenyl group may be substituted. R min is hydrogen; C1-8 alkyl; phenyl; substituted phenyl, phenylalkyl, substituted phenylalkyl or idanyl; or R min is a group wherein R2 and R3 are hydrogen; C1-6 alkyl; or phenylalkyl and R4 designates C1-8 alkyl; phenyl; substituted phenyl or phenylalkyl and salts thereof. Intermediates for preparing (I) are …<CHEM>… in which Z is hydrogen or a protecting group and W is hydrogen or a readily removable group and salts thereof which are subjected to dehydration and …<CHEM>… in which Z min and W min have the same meaning as Z and W and salts thereof, which are reacted with appropriate reagents. …<??>The compounds (I) exhibit gamma -aminobutyric acid related activity and are useful as active ingredients in pharmaceutical compositions. They may additionally contain a minor tranquilizer or a neuroleptic.</p> |
