Peptide structures useful for competitive modulation of dipeptidyl peptidase IV catalysis
申请人:——
公开号:US20030135023A1
公开(公告)日:2003-07-17
This invention involves a compound represented by the general formula (I):
1
and pharmaceutically acceptable salts thereof,
wherein
A is any amino acid except a D-amino acid;
B is an amino acid selected from Pro, Ala, Ser, Gly, Hyp, acetidine-(2)-carboxylic acid and pipecolic acid,
C is any amino acid except Pro, Hyp, acetidine-(2)-carboxylic acid, pipecolic acid and except N-alkylated amino acids, e.g. N-methyl valine and sarcosine,
D is any amino acid or missing, and
E is any amino acid or missing;
or
wherein
C is any amino acid except Pro, Hyp, acetidine-(2)-carboxylic acid, pipecolic acid, except N-alkylated amino acids, e.g. N-methyl valine and sarcosine and except a D-amino acid,
D is an amino acid selected from Pro, Ala, Ser, Gly, Hyp, acetidine-(2)-carboxylic acid and pipecolic acid, and
E is any amino acid except Pro, Hyp, acetidine-(2)-carboxylic acid, pipecolic acid and except N-alkylated amino acids, e.g. N-methyl valine and sarcosine and methods of manufacture and use.
本发明涉及一种由通式(I)表示的化合物:
1
及其药学上可接受的盐类、
其中
A 是除 D-
氨基酸以外的任何
氨基酸;
B 是选自 Pro、Ala、Ser、Gly、Hyp、
乙脒-(2)-
羧酸和
哌啶醇酸的
氨基酸、
C 是任何
氨基酸,但 Pro、Hyp、
乙脒-(2)-
羧酸、
哌啶醇酸和 N-烷基化
氨基酸(如
N-甲基缬氨酸和
肌氨酸)除外、
D 是任何
氨基酸或缺如,以及
E 为任何
氨基酸或缺失;
或
其中
C 是任何
氨基酸,但 Pro、Hyp、
乙脒-(2)-
羧酸、
哌啶醇酸除外,N-烷基化
氨基酸(如
N-甲基缬氨酸和
肌氨酸)除外,D-
氨基酸除外、
D 是选自 Pro、Ala、Ser、Gly、Hyp、
乙脒-(2)-
羧酸和
哌啶酸的
氨基酸,以及
E 是除 Pro、Hyp、
乙脒-(2)-
羧酸、
哌啶醇酸和 N-烷基化
氨基酸(如
N-甲基缬氨酸和
肌氨酸)以外的任何
氨基酸,以及制造和使用方法。