申请人:Kalthoff Christoph
公开号:US20130053311A1
公开(公告)日:2013-02-28
The invention relates to a GLP-1 analogue which comprises a histidine (H) residue at a position corresponding to position 31 of GLP-1 (7-37) (SEQ ID NO: 1), a glutamine (Q) residue at a position corresponding to position 34 of GLP-1 (7-37) (SEQ ID NO: 1), and a maximum of ten amino acid modifications as compared to GLP-1 (7-37) (SEQ ID NO: 1); wherein the H residue is designated H
31
, and the Q residue is designated Q
34
; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to derivatives thereof, as well as the pharmaceutical use of these analogues and derivatives, for example in the treatment and/or prevention of all forms of diabetes and related diseases. The invention furthermore relates to corresponding novel side chain intermediates. The derivatives are suitable for oral administration.
本发明涉及一种GLP-1类似物,其包括一个组氨酸(H)残基,该残基位于对应于GLP-1(7-37)(SEQ ID NO:1)的31位位置,一个谷氨酰胺(Q)残基,该残基位于对应于GLP-1(7-37)(SEQ ID NO:1)的34位位置,并且与GLP-1(7-37)(SEQ ID NO:1)相比最多具有十个氨基酸修饰;其中,H残基被指定为H31,Q残基被指定为Q34;或其药学上可接受的盐、酰胺或酯。本发明还涉及其衍生物,以及这些类似物和衍生物的药用,例如用于治疗和/或预防所有形式的糖尿病和相关疾病。本发明还涉及相应的新型侧链中间体。这些衍生物适合口服给药。