Aminomethylpyrimidines as allosteric enhancers of the GABA B...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S217060, C514S218000, C514S235800, C514S252140, C514S269000, C540S472000, C540S544000, C540S575000, C540S601000, C544S122000, C544S295000, C544S315000, C544S316000

Reexamination Certificate

active

07351700

ABSTRACT:
The present invention relates to compounds of formulawhereinX is —S— or —NH—;R3/R4together 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, —NR2, —CONR2, —CO-lower alkyl or benzyl; or R3/R4form 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; andR, R1, R2, and R5are 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 GABABreceptor 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.

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