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    • 8. 发明授权
    • Method of using certain substituted aliphatic secondary amines or their
salts for easing breathing
    • 使用某些取代的脂族仲胺或其盐来缓解呼吸的方法
    • US4448776A
    • 1984-05-15
    • US341035
    • 1982-01-20
    • Karl BucherMax MatterBernhard BrunnerAlfred Frey
    • Karl BucherMax MatterBernhard BrunnerAlfred Frey
    • A61K31/13A61K31/135A61K31/195A61K31/215A61P11/10C07C67/00C07C209/00C07C209/08C07C209/52C07C211/27C07C229/36C07C229/38A61K31/24A61K31/495
    • C07C229/38
    • Compounds of the formula IR.sub.1 --CH(R.sub.2)--N(R.sub.3)--R.sub.4 (I)in which R.sub.1 is unsubstituted or substituted phenyl, R.sub.2 is hydrogen lower alkyl, unsubstituted or substituted phenyl or free or esterified carboxy, and in which R.sub.3 is hydrogen or lower alkyl and R.sub.4 is a group of the formula --alk.sub.1 --X--alk.sub.2 --R.sub.5, or R.sub.3 and R.sub.4 together are a group of the formula --alk.sub.3 --NH--alk.sub.4 --, alk.sub.1 and alk.sub.2 being lower alkylidene, alk.sub.3 and alk.sub.4 lower alkylene, X a direct bond, methylene or unsubstituted or substituted phenylene and R.sub.5 being hydroxy, amino or substituted amino of the formula --N(R.sub.6)--CH(R.sub.7)--R.sub.8 in which R.sub.6 is hydrogen, or, provided that R.sub.3 is hydrogen, it may alternatively be lower alkyl or unsubstituted or substituted phenyl-lower alkyl, R.sub.7 is hydrogen, lower alkyl, unsubstituted or substituted phenyl or free or esterified carboxy and R.sub.8 is unsubstituted or substituted phenyl, and their pharmaceutically acceptable salts have properties that ease breathing and are suitable for combating respiratory disorders, preferably as active ingredients in and/or for the manufacture of pharmaceutical preparations that ease breathing.
    • 其中R 1为未取代或取代的苯基,R 2为氢低级烷基,未取代或取代的苯基或游离的或酯化的羧基,其中R 1,R 2,R 3, 是氢或低级烷基,R4是式-alk1-X-alk2-R5的基团,或R3和R4一起是式-alk3-NH-alk4-,alk1和alk2是低级亚烷基,alk3和 烷基,低级亚烷基,X为直接键,亚甲基或未取代或取代的亚苯基,R5为羟基,式-N(R6)-CH(R7)-R8的氨基或取代的氨基,其中R6为氢,或 可以是低级烷基或未取代的或取代的苯基 - 低级烷基,R7是氢,低级烷基,未取代或取代的苯基或游离或酯化的羧基,R8是未取代或取代的苯基,其药学上可接受的盐具有 舒适呼吸,适合对抗呼吸系统疾病,优先 可以作为促进呼吸的药物制剂的制造和/或制造中的活性成分。