| 摘要 |
The invention relates to compounds of general formula (I), or a salt or solvate thereof;
in which:
X and Y are each N;
A is an optionally substituted phenyl group or an optionally substituted sulphur containing heterocycle;
Z is a single bond or a linking group which is a carbon atom carrying substituents R4 and R5, wherein R4 and R5 are independently selected from hydrogen, optionally substituted C 1-6 alkyl and another group A, provided that no more than one of R4 or R5 are hydrogen;
R1 is hydrogen, or a substituent group selected from C 1-10 alkyl, C 2-10 alkenyl, benzyl, piperidine-methyl, thienyl-methyl, furyl-methyl or C 3-10 cycloalkyl, any of which is optionally substituted by hydroxy, halogen, carboxamide, halo C 1-4 alkyl, C 1-6 alkyl or C 1-6 alkoxy; or the Y nitrogen is unsubstituted;
R2 is amino or a substituent group selected from optionally substituted alkyl or phenyl groups; and
N* is =NH when R1 is hydrogen or a substituent group; or
N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or
N* is an optionally substituted piperazinyl ring. The compounds can be used to treat disorders in mammals that are susceptible to sodium channel blockers and antifolates, particularly disorders such as epilepsy, multiple sclerosis, glaucoma and uveitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motor neurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria. |
