JP6768515B2 - 二重アシル化glp−1化合物 - Google Patents

二重アシル化glp−1化合物 Download PDF

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Publication number
JP6768515B2
JP6768515B2 JP2016561311A JP2016561311A JP6768515B2 JP 6768515 B2 JP6768515 B2 JP 6768515B2 JP 2016561311 A JP2016561311 A JP 2016561311A JP 2016561311 A JP2016561311 A JP 2016561311A JP 6768515 B2 JP6768515 B2 JP 6768515B2
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xaa
chem
glp
derivative
ethoxy
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JP2017514801A5 (enExample
JP2017514801A (ja
Inventor
ラルス・リンデロート
ヤコブ・コフォード
イェスパ・ラウ
パウ・ブロク
パトリック・ウィリアム・ガリバイ
ヤノス・ティボル・コドラ
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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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Child & Adolescent Psychology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2016561311A 2014-04-07 2015-04-07 二重アシル化glp−1化合物 Active JP6768515B2 (ja)

Applications Claiming Priority (3)

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

Publications (3)

Publication Number Publication Date
JP2017514801A JP2017514801A (ja) 2017-06-08
JP2017514801A5 JP2017514801A5 (enExample) 2018-05-10
JP6768515B2 true JP6768515B2 (ja) 2020-10-14

Family

ID=50434120

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016561311A Active JP6768515B2 (ja) 2014-04-07 2015-04-07 二重アシル化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)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN111050750B (zh) 2017-08-24 2024-09-24 诺和诺德股份有限公司 Glp-1组合物及其用途
EP4299118A3 (en) 2018-02-02 2024-04-10 Novo Nordisk A/S Solid compositions comprising a glp-1 agonist, a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant
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
WO2020077129A1 (en) 2018-10-11 2020-04-16 Intarcia Therapeutics, Inc. Human amylin analog polypeptides and methods of use
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
JP7670698B2 (ja) 2019-11-06 2025-04-30 ノヴォ ノルディスク アー/エス 認知症におけるglp-1受容体作動薬
EP4054536A1 (en) 2019-11-07 2022-09-14 Novo Nordisk A/S Solid compositions comprising a glp-1 agonist, an sglt2 inhibitor and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid
JP7761567B2 (ja) 2020-02-18 2025-10-28 ノヴォ ノルディスク アー/エス 医薬製剤
US20230165939A1 (en) 2020-04-29 2023-06-01 Novo Nordisk A/S Solid compositions comprising a glp-1 agonist and histidine
WO2022056313A2 (en) * 2020-09-11 2022-03-17 Glympse Bio, Inc. Ex vivo protease activity detection for disease detection/diagnostic, staging, monitoring and treatment
EP4222176A4 (en) 2020-09-30 2024-02-28 Beijing QL Biopharmaceutical Co., Ltd. POLYPEPTIDE CONJUGATES AND METHODS OF USE
WO2023012263A1 (en) 2021-08-04 2023-02-09 Novo Nordisk A/S Solid oral peptide formulations
KR20240163717A (ko) 2022-03-30 2024-11-19 베이징 큐엘 바이오파마슈티컬 컴퍼니 리미티드 폴리펩티드 접합체의 액체 약학 조성물 및 그의 사용 방법
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2264243C (en) * 1996-08-30 2004-10-05 Novo Nordisk A/S Glp-1 derivatives
AU2610699A (en) 1998-02-27 1999-09-15 Novo Nordisk A/S Derivatives of glp-1 analogs
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
CN1495198A (zh) 1998-12-07 2004-05-12 �о���Ӧ�ÿ�ѧЭ��ɷ����޹�˾ 胰高血糖素样肽-1的类似物
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
US7291594B2 (en) 2002-10-11 2007-11-06 Sanwa Kagaku Kenkyusho Co., Ltd. GLP-1 derivative and preparation thereof absorbable via mucous membrane
US20060286129A1 (en) 2003-12-19 2006-12-21 Emisphere Technologies, Inc. Oral GLP-1 formulations
TWI362392B (en) 2005-03-18 2012-04-21 Novo Nordisk As Acylated glp-1 compounds
CN101842109B (zh) 2007-09-05 2014-01-29 诺沃-诺迪斯克有限公司 用a-b-c-d-衍生的肽和它们的治疗用途
CN111560060A (zh) * 2009-12-16 2020-08-21 诺沃—诺迪斯克有限公司 双酰化glp-1衍生物
CN105601729A (zh) * 2010-11-09 2016-05-25 诺沃—诺迪斯克有限公司 双-酰化的glp-1衍生物
CN103298456A (zh) * 2011-01-19 2013-09-11 诺沃—诺迪斯克有限公司 Glp-1颗粒和组合物
KR101972836B1 (ko) * 2011-04-12 2019-04-29 노보 노르디스크 에이/에스 이중 아실화된 glp-1 유도체
ES2626013T3 (es) * 2011-09-06 2017-07-21 Novo Nordisk A/S Derivados de GLP-1
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
EP2846823B1 (en) 2012-05-08 2019-12-04 Novo Nordisk A/S Double-acylated glp-1 derivatives
AU2014210751A1 (en) * 2013-01-29 2015-08-06 Oshadi Drug Administration Ltd. Pharmaceutical compositions for oral treatment of diabetes

Also Published As

Publication number Publication date
US20170114116A1 (en) 2017-04-27
WO2015155151A1 (en) 2015-10-15
EP3129041B1 (en) 2019-06-12
ES2741507T3 (es) 2020-02-11
JP2017514801A (ja) 2017-06-08
EP3129041A1 (en) 2017-02-15
CN106132985A (zh) 2016-11-16
CN106132985B (zh) 2020-10-13
US10689429B2 (en) 2020-06-23

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