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1. WO2020108228 - EXENATIDE ANALOG

Publication Number WO/2020/108228
Publication Date 04.06.2020
International Application No. PCT/CN2019/115200
International Filing Date 03.11.2019
IPC
C07K 14/605 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
A61K 38/26 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
26Glucagons
A61P 5/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
48of the pancreatic hormones
CPC
A61K 38/26
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17from animals; from humans
22Hormones
26Glucagons
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 5/48
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5Drugs for disorders of the endocrine system
48of the pancreatic hormones
C07K 14/605
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
14Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435from animals; from humans
575Hormones
605Glucagons
Applicants
  • 鲁南贝特制药有限公司 LUNAN BETTER PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 张贵民 ZHANG, Guimin
  • 李铁健 LI, Tiejian
  • 刘东 LIU, Dong
Priority Data
201811432450.228.11.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) EXENATIDE ANALOG
(FR) ANALOGUE D'EXÉNATIDE
(ZH) 艾塞纳肽类似物
Abstract
(EN)
The present invention belongs to the field of biomedicine, and specifically discloses an exenatide analog. The present invention makes a design for several amino acid structures at the C-terminus of the amino acid sequence of exenatide Exendin-4, including the addition or deletion of amino acids, amino acid sequence mutations and addition of sites that can be used for site-directed modification to obtain an exenatide analog. The activity of this analog to stimulate insulin secretion from mouse islet tumor cells is significantly higher than exenatide Ex-4, and the glucose-lowering activity in vivo in diabetic model mouse C57BL/KsJ-db/db is significantly better than exenatide Ex-4, which can be used to prevent, treat or reduce diabetes and obesity and/or related complications thereof and other diseases.
(FR)
La présente invention se rapporte au domaine de la biomédecine, et concerne particulièrement un analogue d'exénatide. La présente invention permet de concevoir plusieurs structures d'acides aminés à l'extrémité C-terminale de la séquence d'acides aminés de l'exendine-4 d'exénatide, comprenant l'addition ou la délétion d'acides aminés, des mutations de séquence d'acides aminés et l'addition de sites qui peuvent être utilisés pour une modification dirigée sur un site afin d'obtenir un analogue d'exénatide. L'activité de cet analogue pour stimuler la sécrétion d'insuline à partir de cellules tumorales d'îlots de souris est significativement supérieure que l'exénatide Ex-4, et l'activité de réduction de glucose in vivo dans un modèle de souris diabétique C57BL/KsJ-db/db est nettement meilleure que l'exénatide Ex-4, l'analogue fourni par l'invention peut être utilisé pour prévenir, traiter ou réduire le diabète et l'obésité et/ou des complications associées correspondantes ainsi que d'autres maladies.
(ZH)
本发明属于生物医药领域,具体公开了一类艾塞纳肽类似物。本发明对艾塞纳肽Exendin-4的氨基酸序列C端的几个氨基酸结构设计,包括氨基酸的添加或缺失、氨基酸序列突变和增加可用于定点修饰的位点得到一类艾塞纳肽类似物。该类似物刺激小鼠胰岛瘤细胞分泌胰岛素的活性明显高于艾塞纳肽Ex-4,且糖尿病模型小鼠C57BL/KsJ-db/db体内降糖活性也显著优于艾塞纳肽Ex-4,可用于预防、治疗或减轻糖尿病和肥胖症和/或其相关并发症等其他疾病。
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Latest bibliographic data on file with the International Bureau