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    • 19. 发明申请
    • NOVEL QUINOXALINE- AND QUINOXALINYLALKANE-PHOSPHONIC ACIDS
    • 新型喹喔啉 - 和喹喔啉酮 - 磷酸
    • WO1997003079A1
    • 1997-01-30
    • PCT/EP1996002866
    • 1996-07-01
    • CIBA-GEIGY AGMORETTI, RobertALLGEIER, Hans
    • CIBA-GEIGY AG
    • C07F09/6509
    • C07F9/650994C07D241/44
    • Quinoxaline- and quinoxalinylalkane-phosphonic acids of formula (I), wherein R1 is free or esterified carboxy or free or partially esterified phosphono, R2 and R3 are each independently of the other hydrogen or an aliphatic radical, the radicals R4, R5 and R6 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, free or etherified mercapto or oxidised free or etherified mercapto, unsubstituted or aliphatically substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl and X is a divalent aliphatic radical, and their tautomers and/or salts have NMDA-antagonistic properties and can be used in the treatment of pathological conditions that are responsive to blocking of NMDA-sensitive receptors.
    • 式(I)的喹喔啉和喹喔啉基烷烃膦酸,其中R1是游离的或酯化的羧基或游离的或部分酯化的膦酰基,R2和R3各自独立地是另一个氢或脂族基团,基团R4,R5和R6是 游离或醚化的羟基,游离的或醚化的巯基或被氧化的游离的或醚化的巯基,未取代或脂族取代的氨基,硝基,游离或酯化或酰胺化的羧基,氰基,游离或酰胺基氨磺酰基, 卤素或三氟甲基,X是二价脂族基团,其互变异构体和/或盐具有NMDA-拮抗性质,并且可用于治疗对阻断NMDA敏感受体有反应的病理状况。