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    • 69. 发明公开
    • SULFONYLOXAZOLAMINE ALS THERAPEUTISCHE WIRKSTOFFE
    • 磺酰氧胺唑啉ALS THERAPEUTISCHE WIRKSTOFFE
    • EP1140875A1
    • 2001-10-10
    • EP99962190.7
    • 1999-12-01
    • MERCK PATENT GmbH
    • GREINER, HartmutBARTOSZYK, GerdBÖTTCHER, HenningBARNICKEL, GerhardCEZANNE, Bertram
    • C07D263/48A61K31/42A61P25/16A61P25/18A61P25/28A61P25/24
    • C07D263/48
    • The present invention relates to sulphonyloxazolamines of general formula (I), wherein R1, R2 represent independently from each other H, A, -(CH¿2?)n-Ar or alkenyl with 2-6 C atoms, R?1 and R2¿ together also represent a mononuclear saturated heterocycle with 1-2 N, O and/or S atoms, Z is H, A, CF¿3?, NO2, Hal, OH, OA, NH2, NHA or NA2, A represents alkyl with 1-6 C atoms, Ar is Z-monosubstituted or Z-disubstituted phenyl, Hal is F, Cl, Br or I, n is 1 or 2 or the physiologically acceptable salts or solvates thereof. Said sulphonyloxazolamines are used as therapeutic active ingredients. The invention also relates to the use of sulphonyloxazolamines as therapeutic active ingredients and/or to the production of pharmaceutical preparations to combat diseases of the central nervous system. The invention further relates to a pharmaceutical preparation and the production thereof.
    • 本发明涉及通式(I)的磺酰基恶唑胺,其中R 1,R 2彼此独立地代表H,A, - (CH 2 2)n -Ar或具有2-6个C原子的烯基,R 1和R 2 A一起代表具有1-2个N,O和/或S原子的单核饱和杂环,Z代表H,A,CF 3,NO 2,Hal,OH,OA,NH 2,NHA或NA 2, Ar为Z-单取代或Z-二取代苯基,Hal为F,Cl,Br或I,n为1或2或其生理上可接受的盐或溶剂合物。 所述磺酰恶唑胺用作治疗活性成分。 本发明还涉及磺酰基恶唑胺作为治疗活性成分和/或用于制备抗中枢神经系统疾病的药物制剂的用途。 本发明还涉及药物制剂及其制备。