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    • 4. 发明申请
    • [1,2,4]TRIAZOLO[4,3-a]QUINOXALINE COMPOUNDS, THEIR PREPARATION AND USE
    • [1,2,4]三唑[4,3-a]喹啉化合物,其制备和使用
    • WO1994026746A1
    • 1994-11-24
    • PCT/DK1994000170
    • 1994-04-28
    • NOVO NORDISK A/S
    • NOVO NORDISK A/SJACOBSEN, PoulNIELSEN, Flemming, ElmelundJEPPESEN, Lone
    • C07D487/04
    • C07D487/04
    • [1,2,4]triazolo[4,3-a]quinoxaline derivatives of general formula (I) wherein one of R and R is a 5- or 6-membered N-containing heterocyclic ring optionally substituted, or a fused ring system comprising a 5- or 6-membered N-containing heterocyclic ring optionally substituted; and the other of R and R is H, alkyl, alkoxy, halogen, NO2, NH2, CN, CF3, COC1-6-alkyl or SO2NR'R", wherein R' and R" are independently H or alkyl and X is O or S; and pharmaceutically acceptable salts thereof have affinity for the AMPA receptors and are antagonists in connection with this type of receptors which makes them useful in the treatment of CNS ailments, especially in the treatment of any of the numerous indications caused by hyperactivity of excitatory amino acids.
    • [1,2,4]通式(I)的三唑并[4,3-a]喹喔啉衍生物,其中R 1和R 2之一是任选取代的5-或6-元含N杂环 或包含任选取代的5或6元含氮杂环的稠环体系; R 1和R 2中的另一个为H,烷基,烷氧基,卤素,NO 2,NH 2,CN,CF 3,COC 1-6 - 烷基或SO 2 NR'R“,其中R'和R”独立地为H 或烷基,X是O或S; 和其药学上可接受的盐对AMPA受体具有亲和力,并且是与这种类型的受体有关的拮抗剂,这使得它们可用于治疗CNS疾病,特别是治疗由兴奋性氨基酸的多动症引起的许多适应症中的任何一种。