摘要 |
Use of sulfonylguanidines (I), optionally as racemates, pure, or mixed stereoisomers (particularly enantiomers or diastereoisomers), and/or salts with acids or bases, and/or as solvates, especially hydrates, for treating a wide variety of disorders. The disorders are: pain (especially neuropathic, chronic or acute) epilepsy and/or migraine; hyperalgesia (thermal or mechanical), (cold) allodynia or inflammatory or post-operative pain; hot flushes, post-menopausal pain, amyotropic lateral sclerosis, reflex sympasthetic dystrophy, spastic paralysis, restless leg syndrome, inherited nystagmus, psychiatric or neuropathological conditions (bipolar disorders, anxiety, panic attacks, mood fluctuations, mania, depression, manic-depressive states, painful diabetic neuropathy, multiple sclerosis, Parkinson's , Alzheimer's or Huntington's diseases), gastrointestinal injury, erythromelalgic or post-poliomyelotic pain, trigeminal or post-herpetic neuralgia. (I) have formula R1-SO2-N=C(NH2)-NR2R3 and/or the tautomeric form R1-SO2-NH-C(=NH)-NH2, with the preferred tautomer depending on the status of aggregation or solvent used. R1 = 1-10C alkyl (linear or branched, saturated or unsaturated, optionally substituted one or more times), 3-8C cycloalkyl or bicyclic alkylene (saturated or unsaturated, optionally substituted one or more times), (hetero)aryl (both optionally substituted one or more times), or 3-9C cycloalkyl or (hetero)aryl, all optionally substituted one or more times, linked through 1-4C alkyl, linear or branched, saturated or unsaturated; R2 = R1 but not bicyclic alkylene, and the optionally substituted 3-9C cycloalkyl or (hetero)aryl may be linked through 1-3C alkyl (saturated or unsaturated), sulfonyl or NH or R<2> = NR<4>R<5> or SO2R<6>; R<4> and R<5> = R1, but not bicyclic alkylene, also hydrogen or 11-18C alkyl, or together form CH2CH2(O or NR<7>)CH2CH2; R<6> and R<7> = R<5> but not hydrogen; R<3> = hydrogen or R<2>, but not NR<4>R<5> or SO2R<6>, or R<2> and R<3> together form (CH2)n or CH2CH2(O or NR<8>)CH2CH2; n = 4 or 5; R<8> = R<7> or bicyclic alkylene . An Independent claim is also included for (I) as new compounds where R<1> = optionally substituted (hetero)aryl; R<2> = optionally substituted (hetero)aryl attached through optionally unsaturated 1-3C alkyl, and R<3> = hydrogen, except where R<2> = benzyl and R<1> = phenyl (optionally as part of fused ring system), optionally substituted by Me or amino.
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