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发明授权
US4670541A Use of diamino alcohols as analgesic agents 失效
二氨基醇用作止痛剂

Use of diamino alcohols as analgesic agents
摘要：
An enkephalin-degrading aminopeptidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15;A.sub.2, A.sub.3, A.sub.4 and A.sub.5 each is independently glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, or prolyl, norleucyl, or norvalyl; andn.sub.1, n.sub.2, n.sub.3, n.sub.4 and n.sub.5 each is independently 0 or 1.
摘要（中）：

脑啡肽降解氨基肽酶被具有式（IMAGE）+ TR（A2）n2（A3）n3（A4）n4（A5）n5R3的化合物及其药学上可接受的盐抑制，其中R 1和R 2各自独立地为氢， 烷基，羧基烷基，卤素取代的烷基，羟基烷基，氨基烷基，巯基烷基，烷硫基烷基，（环烷基）烷基，（杂芳基）烷基，芳基烷基，氨基甲酰基烷基，胍基烷基或杂芳基; R3是羟基，烷氧基，（取代的烷基）氧基，芳基烷氧基，（杂芳基）烷氧基或-NY1Y2，其中Y1和Y2各自独立地是氢，烷基，芳基或芳烷基或Y1是氢，Y2是取代的烷基或（杂芳基） 烷基; A1是甘氨酰基，丙氨酰基，亮氨酰基，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺基，赖氨酰，谷氨酰，组氨酸，色氨酸，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰，脯氨酰， 其中n6为2至15的整数; A2，A3，A4和A5各自独立地是甘氨酰，丙氨酰，亮氨酰，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺酰基，赖氨酰，谷氨酰，组氨酸，色氨酸，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰或脯氨酰 ，正亮酰基或诺瓦尔基; n1，n2，n3，n4和n5各自独立地为0或1。

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