WO2017181452A8 - Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化 - Google Patents

Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化 Download PDF

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WO2017181452A8
WO2017181452A8 PCT/CN2016/081741 CN2016081741W WO2017181452A8 WO 2017181452 A8 WO2017181452 A8 WO 2017181452A8 CN 2016081741 W CN2016081741 W CN 2016081741W WO 2017181452 A8 WO2017181452 A8 WO 2017181452A8
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polypeptide
glp
hyperlipidemia
atherosclerosis
fatty liver
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PCT/CN2016/081741
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English (en)
French (fr)
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WO2017181452A1 (zh
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蒋先兴
王锐
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深圳市图微安创科技开发有限公司
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Priority to JP2018555579A priority Critical patent/JP6846055B2/ja
Priority to US16/089,228 priority patent/US11197914B2/en
Priority to EP16899039.8A priority patent/EP3447067B1/en
Priority to CA3021933A priority patent/CA3021933A1/en
Publication of WO2017181452A1 publication Critical patent/WO2017181452A1/zh
Publication of WO2017181452A8 publication Critical patent/WO2017181452A8/zh

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
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  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Obesity (AREA)
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  • Immunology (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)

Abstract

本发明提供了一类具有胰高血糖素样肽-1受体(Glucagon-like peptide-1receptor，GLP-1R)和胰高血糖素受体(Glucagon receptor，GCGR)双激动效应的多肽化合物的用途，其具有高酶解稳定性、高生物活性、无不良反应等特点，能够降低因糖尿病以及高脂膳食诱发的血中总胆固醇和甘油三酯水平异常升高，降低肝酶水平，改善肝脏损伤和纤维化程度，并可用于预防或治疗非酒精性脂肪肝病、高脂血症、动脉硬化等疾病。
PCT/CN2016/081741 2016-04-22 2016-05-11 Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化 WO2017181452A1 (zh)

Priority Applications (4)

Application Number Priority Date Filing Date Title
JP2018555579A JP6846055B2 (ja) 2016-04-22 2016-05-11 脂肪性肝疾患、高脂血症及び動脈硬化治療用のｇｌｐ−１ｒ／ｇｃｇｒデュアルアゴニストペプチド
US16/089,228 US11197914B2 (en) 2016-04-22 2016-05-11 GLP-1R/GCGR dual target agonist polypeptide for treatment of fatty liver diseases, hyperlipemia and arteriosclerosis
EP16899039.8A EP3447067B1 (en) 2016-04-22 2016-05-11 Glp-1r/gcgr dual target agonist polypeptide for treating non-alcoholic fatty liver diseases
CA3021933A CA3021933A1 (en) 2016-04-22 2016-05-11 Glp-1r/gcgr dual target agonist polypeptide for treatment of fatty liver diseases, hyperlipemia and arteriosclerosis

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610255395.9 2016-04-22
CN201610255395.9A CN106046145B (zh) 2016-04-22 2016-04-22 Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化

Publications (2)

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WO2017181452A1 WO2017181452A1 (zh) 2017-10-26
WO2017181452A8 true WO2017181452A8 (zh) 2018-07-19

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PCT/CN2016/081741 WO2017181452A1 (zh) 2016-04-22 2016-05-11 Glp-1r/gcgr双靶点激动剂多肽治疗脂肪肝病、高脂血症和动脉硬化

Country Status (7)

Country Link
US (1) US11197914B2 (zh)
EP (1) EP3447067B1 (zh)
JP (1) JP6846055B2 (zh)
CN (2) CN106046145B (zh)
CA (1) CA3021933A1 (zh)
TW (1) TW201737937A (zh)
WO (1) WO2017181452A1 (zh)

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CN106986924A (zh) * 2017-03-23 2017-07-28 中国药科大学 胃泌酸调节素（oxm）类似物及其应用
AU2018314773A1 (en) * 2017-08-09 2020-03-26 Sanofi GLP-1/glucagon receptor agonists in the treatment of fatty liver disease and steatohepatitis
WO2019085773A1 (zh) * 2017-11-06 2019-05-09 中山大学 基于胃泌酸调节素类似物glp-1r/gcgr双靶点激动剂多肽治疗特发性肺间质纤维化
CN114920818B (zh) * 2017-11-06 2024-02-27 深圳市图微安创科技开发有限公司 基于胃泌酸调节素类似物glp-1r/gcgr双靶点激动剂多肽治疗胆汁性肝硬化
CN109836503B (zh) * 2017-11-24 2022-09-16 浙江道尔生物科技有限公司 一种治疗代谢疾病的多重活性蛋白
CA3086918A1 (en) * 2018-01-03 2019-07-11 Mederis Diabetes, Llc Improved peptide pharmaceuticals for treatment of nash and other disorders
CN111068042B (zh) * 2018-10-18 2023-10-13 中山大学 一种多肽化合物在制备治疗非酒精性肝病、特发性肺间质纤维化和动脉硬化药物中的应用
WO2020098657A1 (zh) * 2018-11-12 2020-05-22 天津药物研究院有限公司 具有双重受体激动作用的胰高血糖素衍生肽及其用途
CN111171134B (zh) * 2018-11-12 2023-08-15 天津药物研究院有限公司 胰高血糖素衍生肽及其用途
CN111423506B (zh) * 2019-11-08 2023-06-27 成都奥达生物科技有限公司 一种glp-1化合物
CN111138552A (zh) * 2020-01-15 2020-05-12 中国药科大学 一种降脂多肽及其制药应用
CN114945589B (zh) * 2020-02-24 2024-05-24 深圳市图微安创科技开发有限公司 多肽化合物及其在预防或治疗糖尿病或糖尿病并发症中的应用
KR20230039604A (ko) * 2020-04-17 2023-03-21 아이투오 테라퓨틱스, 인코포레이티드 지속형 글루카곤 수용체 선택적 펩타이드 및 사용 방법
EP4219539A4 (en) * 2020-09-28 2024-06-26 Shenzhen Turier Biotech Co., Ltd. GLP-1R/GCGR DUAL-TARGETED AGONIST PEPTIDE DERIVATIVES FOR THE TREATMENT OF VIRAL HEPATITIS-RELATED HEPATIC FIBROSIS
CN112472794A (zh) * 2020-11-17 2021-03-12 深圳市图微安创科技开发有限公司 双靶点激动剂多肽治疗anit介导的pbc及其相关的肝纤维化
CN112625093B (zh) * 2020-12-29 2022-12-23 清远市图微安创科技开发有限公司 用于预防和/或治疗非酒精性脂肪肝炎的多肽化合物
CN112898405B (zh) * 2021-01-22 2023-02-28 深圳市图微安创科技开发有限公司 多肽化合物及其在预防或治疗糖尿病或糖尿病并发症中的应用
CN112791178A (zh) * 2021-01-22 2021-05-14 深圳市图微安创科技开发有限公司 Glp-1r/gcgr双激动剂多肽衍生物预防或治疗肾纤维化
EP4289860A1 (en) * 2021-01-22 2023-12-13 Shenzhen Turier Biotech Co., Ltd. Use of polypeptide compound in prevention or treatment of inflammatory bowel disease and intestinal fibrosis related thereto
CN115073582A (zh) * 2021-03-16 2022-09-20 深圳市图微安创科技开发有限公司 多肽化合物及其在预防或治疗糖尿病或糖尿病并发症中的应用
CN115806593B (zh) * 2022-09-23 2023-09-05 成都普康生物科技有限公司 一种脂肪酸链修饰的双受体激动剂及其用途
CN115975057B (zh) * 2023-03-16 2023-05-16 杭州信海医药科技有限公司 一种可妥度肽的固相合成方法

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CN106046145A (zh) 2016-10-26
CA3021933A1 (en) 2017-10-26
CN115181175A (zh) 2022-10-14
TW201737937A (zh) 2017-11-01
JP2019520314A (ja) 2019-07-18
US11197914B2 (en) 2021-12-14
EP3447067A1 (en) 2019-02-27
CN106046145B (zh) 2022-11-04
JP6846055B2 (ja) 2021-03-24
EP3447067B1 (en) 2021-06-23
US20190117737A1 (en) 2019-04-25
WO2017181452A1 (zh) 2017-10-26
EP3447067A4 (en) 2020-01-01

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