公开(公告)号：US20160058881A1

公开(公告)日：2016-03-03

申请号：US14775985

申请日：2014-03-14

Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION

Inventor： RICHARD D. DIMARCHI ,  Binbin KOU

IPC: A61K47/48 ,  A61K45/06 ,  A61K38/26

CPC classification number: A61K38/22 ,  A61K38/26 ,  A61K45/06 ,  A61K47/542 ,  C07K14/605 ,  A61K2300/00

Abstract: A prodrug derivative of a bioactive peptide (or polypeptide) is provided that exhibits prolonged half-life in serum and prolonged action in vivo, compared to the parent peptide or polypeptide. In some embodiments, the peptide is selected from the group consisting of glucagon, exendin-4, GLP-1, GLP-2, GIP, vasoactive intestinal peptide (VIP), Pituitary adenylate cyclase-activating polypeptide 27 (PACAP-27), peptide histidine methionine (PHM), oxyntomodulin, secretin, osteocalcin, growth hormone releasing hormone, as well as analogs, derivatives and conjugates.

Abstract translation: 与母体肽或多肽相比，提供生物活性肽（或多肽）的前药衍生物，其在血清中表现出延长的半衰期和体内延长的作用。 在一些实施方案中，肽选自胰高血糖素，毒蜥外泌肽-4，GLP-1，GLP-2，GIP，血管活性肠肽（VIP），垂体腺苷酸环化酶活化多肽27（PACAP-27），肽 组氨酸甲硫氨酸（PHM），胃泌酸调节素，促胰液素，骨钙素，生长激素释放激素，以及类似物，衍生物和缀合物。

公开(公告)号：US20170283479A1

公开(公告)日：2017-10-05

申请号：US15513762

申请日：2015-09-23

Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION

Inventor： Richard D. DIMARCHI ,  Binbin KOU ,  Fa ZHANG ,  John P. MAYER

IPC: C07K14/62 ,  A61K38/28

CPC classification number: C07K14/62 ,  A61K38/00 ,  A61K38/28 ,  A61K47/00 ,  A61K47/54 ,  A61K47/543 ,  A61K47/6911

Abstract: Prodrug formulations of insulin and insulin analogs are provided wherein the insulin peptide has been modified by an amide bond linkage of a dipeptide prodrug element. The prodrugs disclosed herein have extended half-lives and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.