公开(公告)号：US4235906A

公开(公告)日：1980-11-25

申请号：US7952

申请日：1979-01-31

申请人： John J. Savarese ,  Richard J. Kitz ,  Sara Ginsburg

发明人： John J. Savarese ,  Richard J. Kitz ,  Sara Ginsburg

IPC分类号： C07C51/41 ,  C07D217/10 ,  C07D217/20 ,  C07F1/00 ,  A61K31/47

CPC分类号： C07F1/005 ,  C07C51/412 ,  C07D217/10 ,  C07D217/20

摘要： Intermediate-duration reversible neuromuscular blocking agents of the formula (I) ##STR1## where B and C are preferably para or may be meta and are each ##STR2## where W is CH.sub.2 or most preferably CH.dbd.CH R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are each hydrogen or lower alkoxy of 1 to 4 carbon atoms and preferably methoxy, Y is lower alkyl of 1 to 4 carbon atoms and preferably methyl, Z is hydrogen, lower alkyl of 1 to 4 carbon atoms, cyclopentyl, cyclohexyl, benzyl, or ##STR3## where ALKYL has 1 to 4 carbon atoms preferably where the O-ALKYL is at the 2, 3, 4 or 5 positions such as 4-methoxy benzyl and is most preferably 3,4-dimethoxy benzyl or 3, 4, 5-trimethoxybenzyl, n is 2, 3 or 4, most preferably 2 or 3 provided that at least one of R.sub.1 to R.sub.4 is lower alkoxy and most preferably where R.sub.1 and R.sub.4 is hydrogen and R.sub.2 and R.sub.3 are methoxy and X is a pharmaceutically acceptable anion.The neuromuscular blocking agents of formula I are useful for administration to a patient to cause skeletal muscle relaxation during surgery and are normally administered intravenously in a pharmaceutically acceptable carrier.

摘要翻译： 其中B和C优选为对位或可以是间位的，并且各自为“IMAGE”，其中W为CH 2或最优选CH = CHR 1，R 2， R 3和R 4相同或不同，各自为氢或1至4个碳原子的低级烷氧基，优选甲氧基，Y为1至4个碳原子的低级烷基，优选甲基，Z为氢，1至4碳的低级烷基 原子，环戊基，环己基，苄基或者IMAGE，其中ALKYL具有1至4个碳原子，优选O-ALKYL在2,3,4或5位如4-甲氧基苄基，最优选为3,4 二甲氧基苄基或3,4,5-三甲氧基苄基，n为2,3或4，最优选2或3，条件是R 1至R 4中的至少一个为低级烷氧基，最优选其中R 1和R 4为氢，且R 2和R 3为 是甲氧基，X是药学上可接受的阴离子。 式I的神经肌肉阻滞剂可用于给予患者在手术期间引起骨骼肌松弛，并且通常在药学上可接受的载体中静脉内施用。

公开(公告)号：US4192877A

公开(公告)日：1980-03-11

申请号：US921713

申请日：1978-07-03

申请人： John J. Savarese ,  Richard J. Kitz ,  Sara Ginsburg

发明人： John J. Savarese ,  Richard J. Kitz ,  Sara Ginsburg

IPC分类号： C07D217/20 ,  A61K31/47 ,  C07D217/10

CPC分类号： C07D217/20

摘要： Short acting reversible neuromuscular blocking agents of the formula (I) ##STR1## where B and C is preferably meta or maybe para ##STR2## where m is 2, 3 or 4 and is preferably 2,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen or lower alkoxy of 1 to 4 carbon atomsY is lower alkyl of 1 to 4 carbon atomsn is 2, 3 or 4, most preferably 3, provided that at least one of R.sub.1 to R.sub.4 and one of R.sub.5 to R.sub.7 is lower alkoxy and X is a pharmaceutically acceptable anion. These neuromuscular blocking agents of formula I are useful upon administration to a patient in providing muscular relaxation in the patient during surgery and are normally intravenously administered in a pharmaceutically acceptable carrier.

摘要翻译： 式（I）的短效可逆神经肌肉阻滞剂其中B和C优选为间位或可能对位，其中m为2,3或4，优选为2，R 1，R 2，R 3， R 4，R 5，R 6和R 7相同或不同，为氢或1至4个碳原子的低级烷氧基。Y为1至4个碳原子的低级烷基，n为2,3或4，最优选为3，条件是至少 R 1至R 4中的一个和R 5至R 7中的一个为低级烷氧基，X为药学上可接受的阴离子。 式I的神经肌肉阻滞剂在给予患者时在用于在手术期间在患者中提供肌肉松弛时是有用的，并且通常在药学上可接受的载体中静脉内施用。