申请人:Ciba-Geigy Corporation
公开号:US05281747A1
公开(公告)日:1994-01-25
P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.B.sup.- agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.
P-取代氨基磷酸类化合物的化学式为##STR1##其中R代表可选的氟代甲基基团,R.sub.1代表氢、较低的烷基、较低的烷氧基、羟基、卤素或氟代甲基基团,R.sub.2和R.sub.3代表氢或R.sub.2代表羟基、较低的烷氧基或卤素,而R.sub.3是氢或R.sub.2和R.sub.3一起代表氧基团。它们的药学上可接受的盐作为GABA.sub.B.sup.-激动剂具有活性,可用于治疗脊髓痉挛、多发性硬化、脑瘫、三叉神经痛、药物戒断综合征和/或疼痛症状。它们可以通过已知的方法制备,适当的方法已经描述。