CN106132985B - 双酰化glp-1化合物 - Google Patents

双酰化glp-1化合物 Download PDF

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Publication number
CN106132985B
CN106132985B CN201580018073.6A CN201580018073A CN106132985B CN 106132985 B CN106132985 B CN 106132985B CN 201580018073 A CN201580018073 A CN 201580018073A CN 106132985 B CN106132985 B CN 106132985B
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China
Prior art keywords
ethoxy
amino
derivative
acetyl
glp
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CN201580018073.6A
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Chinese (zh)
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CN106132985A (zh
Inventor
L.林德罗思
J.科福埃德
J.刘
P.布洛赫
P.W.加里贝
J.T.科德拉
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Novo Nordisk AS
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Novo Nordisk AS
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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Zoology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201580018073.6A 2014-04-07 2015-04-07 双酰化glp-1化合物 Active CN106132985B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14163697.7 2014-04-07
EP14163697 2014-04-07
PCT/EP2015/057442 WO2015155151A1 (en) 2014-04-07 2015-04-07 Double-acylated glp-1 compounds

Publications (2)

Publication Number Publication Date
CN106132985A CN106132985A (zh) 2016-11-16
CN106132985B true CN106132985B (zh) 2020-10-13

Family

ID=50434120

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580018073.6A Active CN106132985B (zh) 2014-04-07 2015-04-07 双酰化glp-1化合物

Country Status (6)

Country Link
US (1) US10689429B2 (https=)
EP (1) EP3129041B1 (https=)
JP (1) JP6768515B2 (https=)
CN (1) CN106132985B (https=)
ES (1) ES2741507T3 (https=)
WO (1) WO2015155151A1 (https=)

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WO2016168388A2 (en) 2015-04-14 2016-10-20 Palatin Technologies, Inc. Therapies for obesity, diabetes and related indications
WO2017149070A1 (en) 2016-03-03 2017-09-08 Novo Nordisk A/S Glp-1 derivatives and uses thereof
AR112015A1 (es) 2017-06-09 2019-09-11 Novo Nordisk As Composiciones sólidas para administración oral
HRP20240485T1 (hr) 2017-08-24 2024-07-05 Novo Nordisk A/S Pripravci glp-1 i njihova upotreba
PL3746111T3 (pl) 2018-02-02 2024-01-15 Novo Nordisk A/S Stałe kompozycje zawierające agonistę glp-1 i sól kwasu n-(8-(2- hydroksybenzoilo)amino kaprylowego i substancję poślizgową
WO2019200594A1 (zh) * 2018-04-19 2019-10-24 杭州先为达生物科技有限公司 酰化的glp-1衍生物
TWI829687B (zh) 2018-05-07 2024-01-21 丹麥商諾佛 儂迪克股份有限公司 包含glp-1促效劑與n-(8-(2-羥基苯甲醯基)胺基)辛酸之鹽的固體組成物
AR116632A1 (es) 2018-10-11 2021-05-26 Intarcia Therapeutics Inc Polipéptidos análogos de la amilina humana y sus métodos de uso
CN111378027B (zh) * 2018-12-29 2022-04-15 万新医药科技(苏州)有限公司 一种索玛鲁肽前体的制备方法
CN114340655A (zh) * 2019-09-02 2022-04-12 诺和诺德股份有限公司 生产包含glp-1肽的片剂的方法
CA3154744A1 (en) 2019-11-06 2021-05-14 Sarah FRIEDRICH Glp-1 receptor agonists in dementia
CN114641276A (zh) 2019-11-07 2022-06-17 诺和诺德股份有限公司 包含glp-1激动剂、sglt2抑制剂和n-(8-(2-羟基苯甲酰基)氨基)辛酸的盐的固体组合物
PE20230819A1 (es) 2020-02-18 2023-05-19 Novo Nordisk As Composiciones y usos de glp-1
EP4142695B1 (en) 2020-04-29 2025-11-05 Novo Nordisk A/S Solid compositions comprising a glp-1 agonist and histidine
EP4211468A4 (en) * 2020-09-11 2024-10-09 Glympse Bio, Inc. DETECTION OF EX VIVO PROTEASE ACTIVITY FOR DETECTION/DIAGNOSTIC, STAGING, MONITORING AND TREATMENT OF DISEASES
CN114729060B (zh) 2020-09-30 2022-11-25 北京质肽生物医药科技有限公司 多肽缀合物和使用方法
WO2023012263A1 (en) 2021-08-04 2023-02-09 Novo Nordisk A/S Solid oral peptide formulations
EP4323413A4 (en) 2022-03-30 2025-10-15 Beijing Ql Biopharmaceutical Co Ltd LIQUID PHARMACEUTICAL COMPOSITIONS OF POLYPEPTIDE CONJUGATES AND METHODS OF USE THEREOF
CA3266547A1 (en) 2022-08-29 2024-03-07 Eli Lilly And Company COMPOSITIONS FOR ORAL ADMINISTRATION
TW202421645A (zh) 2022-11-25 2024-06-01 丹麥商諾佛 儂迪克股份有限公司 如ｇｌｐ—１之肽治療劑的口服投與
WO2024165571A2 (en) 2023-02-06 2024-08-15 E-Therapeutics Plc Inhibitors of expression and/or function
WO2025125576A2 (en) 2023-12-15 2025-06-19 E-Therapeutics Plc Inhibitors of expression and/or function
EP4686757A1 (en) 2024-07-31 2026-02-04 e-therapeutics PLC Inhibitors of expression and/or function
WO2025133348A1 (en) 2023-12-22 2025-06-26 E-Therapeutics Plc Inhibitors of expression and/or function
WO2025196502A1 (en) 2024-03-20 2025-09-25 North Carolina Agricultural & Technical State University Choline kinase inhibitors as a therapeutic treatment for obesity

Family Cites Families (18)

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IL128332A0 (en) * 1996-08-30 2000-01-31 Novo Nordisk As GLP-1 derivatives
JP2002512175A (ja) 1998-02-27 2002-04-23 ノボ ノルディスク アクティーゼルスカブ Ｇｌｐ−１類似体の誘導体類
JP2003522099A (ja) 1998-02-27 2003-07-22 ノボ ノルディスク アクティーゼルスカブ 遅延作用プロファイルを有するｇｌｐ−１のｇｌｐ−１誘導体及びエキセンジン
DE69922043T2 (de) 1998-12-07 2005-11-24 Société de Conseils de Recherches et d'Applications Scientifiques S.A.S. Glp-1 analoge
EP1239871A1 (en) 1999-11-12 2002-09-18 Novo Nordisk A/S Use of glp-1 agonists for the inhibition of beta cell degeneration
US6693094B2 (en) * 2001-03-22 2004-02-17 Chrono Rx Llc Biguanide and sulfonylurea formulations for the prevention and treatment of insulin resistance and type 2 diabetes mellitus
CA2502118A1 (en) 2002-10-11 2004-05-06 Sanwa Kagaku Kenkyusho Co., Ltd. Glp-1 derivatives and transmicosal absorption preparations thereof
US20060286129A1 (en) 2003-12-19 2006-12-21 Emisphere Technologies, Inc. Oral GLP-1 formulations
TWI372629B (en) 2005-03-18 2012-09-21 Novo Nordisk As Acylated glp-1 compounds
US20100261637A1 (en) 2007-09-05 2010-10-14 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
EP2512518A1 (en) 2009-12-16 2012-10-24 Novo Nordisk A/S Glp-1 receptor agonist compounds with a modified n-terminus
EP2637698B1 (en) 2010-11-09 2022-04-20 Novo Nordisk A/S Double-acylated glp-1 derivatives
US20140004198A1 (en) * 2011-01-19 2014-01-02 Novo Nordisk A/S Glp-1 particles and compositions
RU2602601C2 (ru) * 2011-04-12 2016-11-20 Ново Нордиск А/С Дважды ацилированные производные glp-1
EP2753642B8 (en) * 2011-09-06 2017-12-13 Novo Nordisk A/S Glp-1 derivatives
JP6250034B2 (ja) * 2012-05-08 2017-12-20 ノヴォ ノルディスク アー／エス 二重アシル化されたｇｌｐ−１誘導体
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Also Published As

Publication number Publication date
JP6768515B2 (ja) 2020-10-14
EP3129041A1 (en) 2017-02-15
CN106132985A (zh) 2016-11-16
EP3129041B1 (en) 2019-06-12
US20170114116A1 (en) 2017-04-27
WO2015155151A1 (en) 2015-10-15
ES2741507T3 (es) 2020-02-11
US10689429B2 (en) 2020-06-23
JP2017514801A (ja) 2017-06-08

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