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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JP2017514801A (ja
JP2017514801A5 (cg-RX-API-DMAC7.html
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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (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)
  • Hematology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Emergency Medicine (AREA)
  • Pregnancy & Childbirth (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)
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
EP14163697.7 2014-04-07
EP14163697 2014-04-07
PCT/EP2015/057442 WO2015155151A1 (en) 2014-04-07 2015-04-07 Double-acylated glp-1 compounds

Publications (3)

Publication Number Publication Date
JP2017514801A JP2017514801A (ja) 2017-06-08
JP2017514801A5 JP2017514801A5 (cg-RX-API-DMAC7.html) 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 (cg-RX-API-DMAC7.html)
EP (1) EP3129041B1 (cg-RX-API-DMAC7.html)
JP (1) JP6768515B2 (cg-RX-API-DMAC7.html)
CN (1) CN106132985B (cg-RX-API-DMAC7.html)
ES (1) ES2741507T3 (cg-RX-API-DMAC7.html)
WO (1) WO2015155151A1 (cg-RX-API-DMAC7.html)

Families Citing this family (23)

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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
JP7053480B2 (ja) 2016-03-03 2022-04-12 ノヴォ ノルディスク アー/エス Glp-1誘導体及びその使用
AR112015A1 (es) 2017-06-09 2019-09-11 Novo Nordisk As Composiciones sólidas para administración oral
EP4360651A3 (en) 2017-08-24 2024-07-17 Novo Nordisk A/S Glp-1 compositions and uses thereof
RS64643B1 (sr) 2018-02-02 2023-10-31 Novo Nordisk As Čvrste kompozicije koje sadrže glp-1 agonist i so n-(8-(2-hidroksibenzoil)amino)kaprilne kiseline i lubrikant
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
BR112022002189A2 (pt) * 2019-09-02 2022-04-26 Novo Nordisk As Processo de produção de um comprimido, e, comprimido
WO2021089678A1 (en) 2019-11-06 2021-05-14 Novo Nordisk A/S Glp-1 receptor agonists in dementia
US20220395559A1 (en) 2019-11-07 2022-12-15 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
KR20220143036A (ko) 2020-02-18 2022-10-24 노보 노르디스크 에이/에스 약학적 제형
CN115461044B (zh) 2020-04-29 2025-06-10 诺和诺德股份有限公司 包含glp-1激动剂和组氨酸的固体组合物
JP2023542867A (ja) * 2020-09-11 2023-10-12 グリンプス バイオ, インコーポレイテッド 疾患の検出/診断、病期分類、モニタリング及び処置のための生体外でのプロテアーゼ活性検出
CN115925994B (zh) 2020-09-30 2023-09-22 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
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
IL128332A0 (en) 1996-08-30 2000-01-31 Novo Nordisk As GLP-1 derivatives
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
DE69942306D1 (de) 1998-02-27 2010-06-10 Novo Nordisk As Abkömmlinge von glp-1 analogen
PL202367B1 (pl) 1998-12-07 2009-06-30 Sod Conseils Rech Applic Związki stanowiące analogi GLP-1, kompozycje zawierające te związki oraz zastosowanie tych związków
JP2003516322A (ja) 1999-11-12 2003-05-13 ノボ ノルディスク アクティーゼルスカブ ベータ細胞変性抑制のためのglp−1アゴニストの使用
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
WO2009030771A1 (en) 2007-09-05 2009-03-12 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
CN102686607B (zh) * 2009-12-16 2014-10-29 诺沃—诺迪斯克有限公司 双酰化glp-1衍生物
US9006178B2 (en) * 2010-11-09 2015-04-14 Novo Nordisk A/S Double-acylated GLP-1 derivatives with a linker
EP2665470A1 (en) * 2011-01-19 2013-11-27 Novo Nordisk A/S Glp-1 particles and compositions
EP3225631B1 (en) 2011-04-12 2019-01-09 Novo Nordisk A/S Double-acylated glp-1 derivatives
JP6126097B2 (ja) * 2011-09-06 2017-05-10 ノヴォ ノルディスク アー/エス Glp−1誘導体
EP2846823B1 (en) 2012-05-08 2019-12-04 Novo Nordisk A/S Double-acylated glp-1 derivatives
WO2013167455A1 (en) * 2012-05-08 2013-11-14 Novo Nordisk A/S Double-acylated glp-1 derivatives
HK1217443A1 (zh) * 2013-01-29 2017-01-13 奥莎迪药品管理有限公司 用於糖尿病的口服治疗的药物组合物

Also Published As

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

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