The present invention relates to compounds of formula I ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification. Compounds of the invention are active on the GABAB receptor and are useful for treating a variety of CNS disorders, including anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity-and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.

Hoffmann-La Roche Inc.

Thieno-pyridine derivatives as allosteric enhancers of the GABA.sub.B receptors

The present invention provides novel compounds of formula I wherein W.sub.1, W.sub.2, W.sub.3, W.sub.4, W.sub.5, B, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B ("GABA.sub.B") positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome. ##STR00001##

Addex Pharma S.A.

Triazinedione derivatives as GABA.sub.B receptor modulators

The present invention relates to compounds of formula ##STR00001## wherein X is --S-- or --NH--; R.sup.3/R.sup.4 together with the N-atom to which they are attached form a non aromatic 5, 6 or 7 membered ring, which optionally contains in addition to the N-atom one additional heteroatom selected from the group consisting of O, S and N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, --NR.sub.2, --CONR.sub.2, --CO-lower alkyl or benzyl; or R.sup.3/R.sup.4 form together with the N-atom to which they are attached a heterocyclic ring system, containing two or three rings and which optionally contains one or two additional heteroatoms selected from the group consisting of N and O and which has no more than 20 carbon atoms; and R, R.sup.1, R.sup.2, and R.sup.5 are as defined herein and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds of the invention are active on the GABA.sub.B receptor and therefore are useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders and gastro-intestinal disorders.

tuberous sclerosis/− nicotin

Thieno-pyridine derivatives as allosteric enhancers of the GABA.sub.B receptors

Triazinedione derivatives as GABA.sub.B receptor modulators

Triazinedione derivatives as GABA.sub.B receptor modulators

Aminomethylpyrimidines as allosteric enhancers of the GABA.sub.B receptors

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