公开(公告)号：US4407746A

公开(公告)日：1983-10-04

申请号：US330614

申请日：1981-12-14

申请人： Robert H. Mazur ,  David A. Tyner ,  Eleanor A. Hallinan

发明人： Robert H. Mazur ,  David A. Tyner ,  Eleanor A. Hallinan

IPC分类号： C07K14/655 ,  A61K38/00 ,  A61K38/22 ,  A61P25/04 ,  C07K5/10 ,  C07K5/107 ,  C07K14/575 ,  C07K14/70 ,  C07C103/52 ,  A61K37/00

CPC分类号： C07K5/1016

摘要： The invention discloses cyclohexyl and phenyl substituted enkephalin derivatives of the formula: ##STR1## Where R.sub.1, R.sub.2, R.sub.4, and R.sub.8 is hydrogen or alkyl of R.sub.3 is alkylthioalkyl or alkylsulfinylalkyl, X is: ##STR2## R.sub.5 is cyclohexylmethyl, phenylmethyl, optionally substituted by --NO.sub.2, R.sub.6 is cyclohexyl or phenyl optionally substituted by R.sub.7 and R.sub.7 is hydrogen, an alkyl ester of carboxylic acid or hydroxyalkyl and the pharmaceutically acceptable salts, which are useful as analgesic agents.

摘要翻译： 本发明公开了下式的环己基和苯基取代的脑啡肽衍生物：其中R1，R2，R4和R8是氢或R3的烷基是烷硫基烷基或烷基亚磺酰基烷基，X是：环己基甲基，苯甲基， 通过-NO 2，R 6是任选被R 7取代的环己基或苯基，R 7是氢，羧酸或羟烷基的烷基酯和药学上可接受的盐，其可用作止痛剂。