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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derivative
ethoxy
amino
glp
xaa
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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/605Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02Carboxylic 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
    • C07C235/04Carboxylic 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
    • C07C235/18Carboxylic 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
    • C07C235/20Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic 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
    • C07C237/22Carboxylic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Child & Adolescent Psychology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (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 (enExample)
EP (1) EP3129041B1 (enExample)
JP (1) JP6768515B2 (enExample)
CN (1) CN106132985B (enExample)
ES (1) ES2741507T3 (enExample)
WO (1) WO2015155151A1 (enExample)

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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
TWI797133B (zh) 2017-06-09 2023-04-01 丹麥商諾佛 儂迪克股份有限公司 用於經口投予的固體組成物
EP3474820B1 (en) 2017-08-24 2024-02-07 Novo Nordisk A/S Glp-1 compositions and uses thereof
BR112020014624A2 (pt) 2018-02-02 2020-12-08 Novo Nordisk A/S Composições sólidas compreendendo agonista de glp-1, sal de ácido n-(8-(2-hidroxibenzoil) amino)caprílico e lubrificante
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
BR112021006823A2 (pt) 2018-10-11 2021-07-27 Intarcia Therapeutics, Inc. polipeptídeos análogos de amilina humana e 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
JP7767264B2 (ja) * 2019-09-02 2025-11-11 ノヴォ ノルディスク アー/エス Glp-1ペプチドを含む錠剤を生成するためのプロセス
RS65780B1 (sr) 2019-11-06 2024-08-30 Novo Nordisk As Semaglutid u lečenju alchajmerove demencije
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
JP7777085B2 (ja) 2020-04-29 2025-11-27 ノヴォ ノルディスク アー/エス Glp-1作動薬およびヒスチジンを含む固形組成物
CA3194956A1 (en) * 2020-09-11 2022-03-17 Glympse Bio, Inc. Ex vivo protease activity detection for disease detection/diagnostic, staging, monitoring and treatment
JP2023545684A (ja) 2020-09-30 2023-10-31 ベイジン キューエル バイオファーマシューティカル カンパニー,リミテッド ポリペプチドコンジュゲートおよび使用の方法
WO2023012263A1 (en) 2021-08-04 2023-02-09 Novo Nordisk A/S Solid oral peptide formulations
CA3252113A1 (en) 2022-03-30 2023-10-05 Beijing Ql Biopharmaceutical Co Ltd Liquid pharmaceutical compositions of polypeptide conjugates and their methods of use
WO2024110614A1 (en) 2022-11-25 2024-05-30 Novo Nordisk A/S Oral administration of peptide therapeutics, such as glp-1
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
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2283025T3 (es) * 1996-08-30 2007-10-16 Novo Nordisk A/S Derivados de glp-1.1.
WO1999043708A1 (en) 1998-02-27 1999-09-02 Novo Nordisk A/S Glp-1 derivatives of glp-1 and exendin with protracted profile of action
ATE466027T1 (de) 1998-02-27 2010-05-15 Novo Nordisk As Abkömmlinge von glp-1 analogen
SG125915A1 (en) 1998-12-07 2006-10-30 Sod Conseils Rech Applic Analogues of glp-1
AU1269501A (en) 1999-11-12 2001-05-30 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
EP1559724A4 (en) * 2002-10-11 2006-02-08 Sanwa Kagaku Kenkyusho Co GLP-1 DERIVATIVES AND TRANSMUCOSAL 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
WO2009030771A1 (en) 2007-09-05 2009-03-12 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
JP6006118B2 (ja) 2009-12-16 2016-10-12 ノヴォ ノルディスク アー/エス Glp−1アナログ及び誘導体
US9708383B2 (en) * 2010-11-09 2017-07-18 Novo Nordisk A/S Double-acylated GLP-1 derivatives
WO2012098188A1 (en) * 2011-01-19 2012-07-26 Novo Nordisk A/S Glp-1 particles and compositions
CA2832811A1 (en) 2011-04-12 2012-10-18 Novo Nordisk A/S Double-acylated glp-1 derivatives
ES2626013T3 (es) 2011-09-06 2017-07-21 Novo Nordisk A/S Derivados de GLP-1
WO2013167454A1 (en) * 2012-05-08 2013-11-14 Novo Nordisk A/S Double-acylated glp-1 derivatives
JP6366575B2 (ja) * 2012-05-08 2018-08-01 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
CA2899220A1 (en) * 2013-01-29 2014-08-07 Oshadi Drug Administration Ltd. Pharmaceutical compositions for oral treatment of diabetes

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

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