Pharmacologically active peptides, their preparation and pharmaceutical compositions containing them
申请人:ELI LILLY AND COMPANY
公开号:EP0030845A2
公开(公告)日:1981-06-24
Compounds of the formula
and pharmaceutically acceptable non-toxic acid addition salts thereof, in which Land D define the chirality;
R1 is hydrogen or C1-C3 primary alkyl;
R2 is C1-C4 primary or secondary alkyl,
allyl, cyclopropylmethyl, C1-C2 hydroxyalkyl, or -(CH2)m-U-CH3 in which U is -S- or S-0 and mis 1 or 2; R3 is hydrogen, C1-C4 primary or secondary alkyl, cyclopropylmethyl, allyl or propargyl; and
in which R, is hydrogen, acetyl, or acetoxymethyl and R5 is C1-C3 alkyl; are useful analgesic agents. These compounds are prepared by deblocking the correspondingly blocked compound of formula I with a deblocking agent.
式化合物
及其药学上可接受的无毒酸加成盐,其中 Land D 定义了手性;
R1 是氢或 C1-C3 伯烷基;
R2 是 C1-C4 伯烷基或仲烷基、
烯丙基、环丙基甲基、C1-C2 羟基烷基或-(CH2)m-U-CH3,其中 U 是-S-或 S-0 且误为 1 或 2;R3 是氢、C1-C4 伯或仲烷基、环丙基甲基、烯丙基或丙炔基;以及
其中 R,是氢、乙酰基或乙酰氧甲基,R5 是 C1-C3 烷基;这些都是有用的镇痛剂。这些化合物的制备方法是用解嵌剂对相应的式 I 嵌段化合物进行解嵌。