[EN] REVERSIBLE NONDEPOLARIZING NEUROMUSCULAR BLOCKADE AGENTS AND METHODS FOR THEIR USE<br/>[FR] AGENTS DE BLOCAGE NEUROMUSCULAIRES NON DÉPOLARISANTS RÉVERSIBLES ET LEUR MÉTHODE
申请人:UNIV CORNELL
公开号:WO2010107488A1
公开(公告)日:2010-09-23
The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.
该发明提供了一种非去极化型神经肌肉阻滞剂,几乎没有任何循环效应。该发明的化合物包括富马酸、马来酸、琥珀酸和乙炔二羧酸的双(异喹啉基烷醇)二酯;适用于这些化合物作为手术辅助麻醉剂的静脉给药组合物,以及这些化合物的制备方法。该发明的化合物可以产生短暂或中等持续时间的神经肌肉阻滞,对于各种化合物,可以通过给予硫醇化合物如L-半胱氨酸、D-半胱氨酸或谷胱甘肽来逆转。对于该发明的各种化合物,神经肌肉阻滞效应可以迅速、高效地逆转,而且没有明显的副作用。