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    • 10. 发明授权
    • Cyclic motilin-like polypeptides with gastrointestinal motor stimulating
activity
    • 循环促胃动素样多肽与胃肠运动刺激活性
    • US5734012A
    • 1998-03-31
    • US648644
    • 1996-05-16
    • Ramalinga DharanipragadaMark J. MacielagJung Kim-DettelbackJames Florance
    • Ramalinga DharanipragadaMark J. MacielagJung Kim-DettelbackJames Florance
    • A61K38/00A61P1/00C07K14/63C07K5/12C07K7/00C07K7/08
    • C07K14/63A61K38/00
    • This invention pertains to cyclic polypeptides having gastrointestinal motor stimulating activity which may be represented by formula (1): ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein groups A and D are linked to from a cyclic structure; and R.sub.1 is lower alkyl; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is phenyl or substituted phenyl, wherein the phenyl group may be substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and lower alkoxy; R.sub.5 is --OH or --NH.sub.2 ; A is selected from the group consisting of L-glutamic acid, L-aspartic acid, L-lysine, L-ornithine, and L-2,4-diaminobutyric acid; B is L-alanine or L-glutamine; C is L-arginine or D-arginine; D is selected from the group consisting of L-lysine, L-ornithine, L-2,4-diaminobutyric acid, L-glutamic acid, and L-aspartic acid; E is a direct bond between group D and group R.sub.5 or is L-lysine or D-lysine; m is 0 or 1; the symbol * represents an asymmetric carbon atom which may be in the D or L configuration, with the proviso that: (a) when A is L-glutamic acid or L-aspartic acid, D is L-lysine, L-ornithine, or L-2,4-diaminobutyric acid; and (b) when A is L-lysine, L-ornithine, or L-2,4-diaminobutyric acid, D is L-glutamic acid or L-aspartic acid. This invention also pertains to methods for using the novel cyclic polypeptides.
    • 本发明涉及具有胃肠运动刺激活性的环状多肽,其可以由式(1)表示:(1)包括旋光异构体形式及其药学上可接受的酸加成盐,其中基团A和D与 循环结构; 且R 1为低级烷基; R2是氢或低级烷基; R3是氢或低级烷基; R4是苯基或取代的苯基,其中苯基可以被一个或多个选自卤素,羟基和低级烷氧基的取代基取代; R5是-OH或-NH2; A选自L-谷氨酸,L-天冬氨酸,L-赖氨酸,L-鸟氨酸和L-2,4-二氨基丁酸; B是L-丙氨酸或L-谷氨酰胺; C是L-精氨酸或D-精氨酸; D选自L-赖氨酸,L-鸟氨酸,L-2,4-二氨基丁酸,L-谷氨酸和L-天冬氨酸; E是D组和R5组之间的直接键,或是L-赖氨酸或D-赖氨酸; m为0或1; 符号*表示可以是D或L构型的不对称碳原子,条件是:(a)当A是L-谷氨酸或L-天冬氨酸时,D是L-赖氨酸,L-鸟氨酸或 L-2,4-二氨基丁酸; 和(b)当A是L-赖氨酸,L-鸟氨酸或L-2,4-二氨基丁酸时,D是L-谷氨酸或L-天冬氨酸。 本发明还涉及使用新型环状多肽的方法。