| abstract |
The present invention provides compounds of formula (I) wherein X is —S— or —NH—; R 1 is alkyl, alkenyl, arylalkyl, arylalkenyl or aryl-O-alkyl, wherein aryl The group is optionally substituted with one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen or lower halogen-alkyl; R 2 is hydrogen, lower alkyl or cycloalkyl; R 3 / R 4 together with the N atom to which they are attached may form a non-aromatic 5-, 6- or 7-membered ring, in addition to the N atom, It may contain one additional heteroatom selected from the group consisting of S or N, wherein the ring is hydroxy, lower alkyl, lower alkoxy, —NR 2 , —CONR 2 , —CO—lower. Alkyl or May be optionally substituted with benzyl; or together with the N atom to which they are attached, may form a heterocyclic ring system containing at least two rings, which is a group consisting of N or O 1 or 2 additional heteroatoms selected from R; R is hydrogen or lower alkyl; R 5 is hydrogen or lower alkyl], and pharmaceutically It relates to suitable acid addition salts thereof. This compound is active against the GABA B receptor and thus anxiety, depression, epilepsy, schizophrenia, cognitive impairment, spasticity and skeletal muscle stiffness, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, Useful for the treatment of cerebral palsy, neuropathic pain and cocaine and nicotine related addiction, psychosis, panic disorder, post-traumatic stress disorder or gastrointestinal disorder. |