公开(公告)号：US5744452A

公开(公告)日：1998-04-28

申请号：US634718

申请日：1996-04-18

申请人： Alexander A. Kolobov ,  Andrey S. Simbirtsev ,  Sergey V. Kulikov ,  Alexey N. Prusakov ,  Natalia M. Kalinina ,  Natalia V. Pigareva ,  Alexander U. Kotov ,  Vladimir M. Shpen ,  Oleg A. Kaurov ,  Sergey A. Ketlinsky

发明人： Alexander A. Kolobov ,  Andrey S. Simbirtsev ,  Sergey V. Kulikov ,  Alexey N. Prusakov ,  Natalia M. Kalinina ,  Natalia V. Pigareva ,  Alexander U. Kotov ,  Vladimir M. Shpen ,  Oleg A. Kaurov ,  Sergey A. Ketlinsky

IPC分类号： A61K31/305 ,  A61K31/381 ,  C07D209/20 ,  C07D333/22 ,  A61K38/00 ,  A61K31/38 ,  A61K31/40

CPC分类号： C07D333/22 ,  A61K31/305 ,  A61K31/381 ,  C07D209/20

摘要： The new class of synthetic immunomodulatory molecules having a .gamma.-L-glutamyl- moiety at the amino terminus are provided as illustrated by Formula 1. ##STR1## In Formula 1, the Greek symbols designate the noted carbon atoms, R is hydrogen, acyl or alkyl, and X is an aromatic or heterocyclic amino acid or its derivative. Included as members of the new class (in addition to Bestim, .gamma.-L-glutamyl-L-tryptophan) are those compounds where R=hydrogen and X=L-tryptophan, such as .gamma.-L-glutamyl-N.sub.in -formyl-L-tryptophan, N-methyl-.gamma.-L-glutamyl-L-tryptophan, N-acetyl-.gamma.-L-glutamyl-L-tryptophan, and .gamma.-L-glutamyl-.beta.-thienyl-D-alanylamide. A preferred embodiment, termed "BESTIM," has the chemical structure of .gamma.-L-glutamyl-L-tryptophan.

摘要翻译： 提供了在氨基末端具有γ-L-谷氨酰基部分的新一类合成免疫调节分子，如式1所示。式1中，希腊符号表示所述碳原子，R为氢， 酰基或烷基，X是芳族或杂环氨基酸或其衍生物。 作为新类的成员（除了Bestim，γ-L-谷氨酰-L-色氨酸之外）包括R =氢和X = L-色氨酸的那些化合物，例如γ--L-谷氨酰 - in - 甲酰基-L 色氨酸，N-甲基-γ-L-谷氨酰-L-色氨酸，N-乙酰基-γ-L-谷氨酰-L-色氨酸和γ--L-谷氨酰基-β-噻吩基-D-丙氨酰胺。 称为“BESTIM”的优选实施方案具有γ-L-谷氨酰-L-色氨酸的化学结构。