ES2683372T3 - Derivados de GLP-1 acilados con un conector nuevo - Google Patents

Derivados de GLP-1 acilados con un conector nuevo Download PDF

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Publication number
ES2683372T3
ES2683372T3 ES11779674T ES11779674T ES2683372T3 ES 2683372 T3 ES2683372 T3 ES 2683372T3 ES 11779674 T ES11779674 T ES 11779674T ES 11779674 T ES11779674 T ES 11779674T ES 2683372 T3 ES2683372 T3 ES 2683372T3
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glp
integer
range
residue
acylated
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Jacob Kofoed
Jesper Lau
Lars Linderoth
Patrick William Garibay
Thomas Kruse
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Novo Nordisk AS
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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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Cardiology (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)

Abstract

Un derivado de un análogo de GLP-1, cuyo análogo comprende un primer residuo K en una posición correspondiente a la posición 18 de GLP-1(7-37) (sec. con núm. de ident.: 1), un segundo residuo K en otra posición y un máximo de doce cambios de aminoácidos en comparación con GLP-1(7-37), cuyo derivado comprende dos porciones de prolongación unidas a dicho residuo K primero y segundo, respectivamente, mediante un conector, en donde la porción de prolongación se selecciona de Quím. 2 y Quím. 1: Quím. 2: HOOC-C6H4-O-(CH2)y-CO-* Quím. 1: HOOC-(CH2)x-CO-*, en donde x es un número entero en el intervalo de 6-18 y y es un número entero en el intervalo de 3-17; y el conector comprende Quím. 3: *-NH-(CH2)q-CH[(CH2)w-NH2]-CO-*, en donde q es un número entero en el intervalo de 0-5 y w es un número entero en el intervalo de 0-5; o una sal farmacéuticamente aceptable, amida, o éster del mismo.
ES11779674T 2010-11-09 2011-11-09 Derivados de GLP-1 acilados con un conector nuevo Active ES2683372T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP10190515 2010-11-09
US41422110P 2010-11-16 2010-11-16
EP11169276 2011-06-09
US201161497123P 2011-06-15 2011-06-15
PCT/EP2011/069743 WO2012062804A1 (en) 2010-11-09 2011-11-09 Double-acylated glp-1 derivatives with a linker

Publications (1)

Publication Number Publication Date
ES2683372T3 true ES2683372T3 (es) 2018-09-26

Family

ID=46050422

Family Applications (2)

Application Number Title Priority Date Filing Date
ES11779456T Active ES2913803T3 (es) 2010-11-09 2011-11-09 Derivados de GLP-1 diacilados
ES11779674T Active ES2683372T3 (es) 2010-11-09 2011-11-09 Derivados de GLP-1 acilados con un conector nuevo

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES11779456T Active ES2913803T3 (es) 2010-11-09 2011-11-09 Derivados de GLP-1 diacilados

Country Status (6)

Country Link
US (3) US9708383B2 (es)
EP (2) EP2637699B1 (es)
JP (3) JP6039569B2 (es)
CN (3) CN103209711B (es)
ES (2) ES2913803T3 (es)
WO (2) WO2012062803A1 (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5750341A (en) 1995-04-17 1998-05-12 Lynx Therapeutics, Inc. DNA sequencing by parallel oligonucleotide extensions
EP2454282B1 (en) 2009-07-13 2015-03-04 Zealand Pharma A/S Acylated glucagon analogues
EP2637699B1 (en) * 2010-11-09 2018-05-16 Novo Nordisk A/S Double-acylated glp-1 derivatives with a linker
EP2753642B8 (en) 2011-09-06 2017-12-13 Novo Nordisk A/S Glp-1 derivatives
EP2844669B1 (en) 2012-05-03 2018-08-01 Zealand Pharma A/S Gip-glp-1 dual agonist compounds and methods
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
CN104411322B (zh) * 2012-05-08 2017-05-24 诺和诺德股份有限公司 双酰化glp‑1衍生物
EA033399B1 (ru) 2012-07-23 2019-10-31 Zealand Pharma As Аналоги глюкагона с повышенной растворимостью и/или стабильностью и их применение
TWI608013B (zh) 2012-09-17 2017-12-11 西蘭製藥公司 升糖素類似物
WO2014199397A2 (en) * 2013-06-11 2014-12-18 Mylan Laboratories Ltd Process for the preparation of liraglutide
KR20160021183A (ko) 2013-06-20 2016-02-24 노보 노르디스크 에이/에스 Glp-1 유도체 및 그것의 용도
BR112015032875A2 (pt) 2013-07-04 2017-11-07 Novo Nordisk As derivados de peptídeos do tipo glp-1, e usos dos mesmos
CN105451776B (zh) * 2013-08-15 2020-04-17 诺和诺德股份有限公司 Glp-1衍生物及其用途
KR102569036B1 (ko) 2013-10-17 2023-08-23 질랜드 파마 에이/에스 아실화된 글루카곤 유사체
US9988429B2 (en) 2013-10-17 2018-06-05 Zealand Pharma A/S Glucagon analogues
EA035688B1 (ru) 2013-11-06 2020-07-27 Зилэнд Фарма А/С Соединения, которые представляют собой тройные агонисты глюкагона, glp-1 и gip
WO2015067715A2 (en) 2013-11-06 2015-05-14 Zealand Pharma A/S Gip-glp-1 dual agonist compounds and methods
US10221315B2 (en) * 2013-11-08 2019-03-05 Ppg Industries Ohio, Inc. Curable film-forming composition comprising catalyst associated with a carrier
CN106132985B (zh) * 2014-04-07 2020-10-13 诺和诺德股份有限公司 双酰化glp-1化合物
JP6898231B6 (ja) 2014-10-29 2021-07-28 ジーランド ファーマ アクティーゼルスカブ Gipアゴニスト化合物及び方法
JP6730278B2 (ja) 2014-11-27 2020-07-29 ノヴォ ノルディスク アー/エス Glp−1誘導体及びその使用
JP6691125B2 (ja) 2014-12-17 2020-04-28 ノヴォ ノルディスク アー/エス Glp−1誘導体及びその使用
US10336802B2 (en) 2015-04-16 2019-07-02 Zealand Pharma A/S Acylated glucagon analogue
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
US11358994B2 (en) 2017-07-27 2022-06-14 Saint Louis University Fatty acid modified human epidermal growth factor
AR112480A1 (es) 2017-08-24 2019-10-30 Novo Nordisk As Composiciones de glp-1 y sus usos
HUE060135T2 (hu) 2018-04-05 2023-02-28 Sun Pharmaceutical Ind Ltd Új GLP-1 analógok
CN113214381B (zh) * 2018-04-19 2024-01-19 杭州先为达生物科技股份有限公司 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
CN113597434B (zh) 2019-12-31 2022-07-01 北京质肽生物医药科技有限公司 Glp-1和gdf15的融合蛋白以及其缀合物
US20230082544A1 (en) 2020-02-18 2023-03-16 Novo Nordisk A/S Pharmaceutical formulations
EP4222176A4 (en) 2020-09-30 2024-02-28 Beijing Ql Biopharmaceutical Co Ltd POLYPEPTIDE CONJUGATES AND METHODS OF USE
AU2021374823A1 (en) 2020-11-06 2023-05-25 Novo Nordisk A/S Glp-1 prodrugs and uses hereof
CN117279657A (zh) 2021-05-18 2023-12-22 日本株式会社Ltt生物医药 用于治疗或预防伴随抗癌剂给药的障碍的医药组合物
WO2022266927A1 (zh) * 2021-06-24 2022-12-29 深圳翰宇药业股份有限公司 一种利拉鲁肽变构体及其制备方法、应用
TW202346324A (zh) 2022-05-10 2023-12-01 丹麥商諾佛 儂迪克股份有限公司 前藥及其用途

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5336782A (en) 1991-04-24 1994-08-09 Kuraray Co., Ltd. Long chain carboxylic acid imide ester
SE9102652D0 (sv) * 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5512549A (en) * 1994-10-18 1996-04-30 Eli Lilly And Company Glucagon-like insulinotropic peptide analogs, compositions, and methods of use
PT944648E (pt) 1996-08-30 2007-06-26 Novo Nordisk As Derivados do glp-1.
DE69942306D1 (de) * 1998-02-27 2010-06-10 Novo Nordisk As Abkömmlinge von glp-1 analogen
MY155270A (en) * 1998-09-24 2015-09-30 Lilly Co Eli Use of glp-1 or analogs in treatment of stroke
AU2004273573B2 (en) 2003-09-19 2010-04-22 Novo Nordisk A/S Albumin-binding derivatives of therapeutic peptides
US8067362B2 (en) 2005-02-02 2011-11-29 Novo Nordisk As Insulin derivatives
TWI362392B (en) 2005-03-18 2012-04-21 Novo Nordisk As Acylated glp-1 compounds
EP2514406A1 (en) 2007-06-01 2012-10-24 Novo Nordisk A/S Spontaneously dispersible preconcentrates including a peptide drug in a solid or semisolid carrier
JP5476304B2 (ja) 2007-09-05 2014-04-23 ノボ・ノルデイスク・エー/エス グルカゴン様ペプチド−1誘導体及びそれらの医薬用途
WO2009030771A1 (en) * 2007-09-05 2009-03-12 Novo Nordisk A/S Peptides derivatized with a-b-c-d- and their therapeutical use
US8598314B2 (en) 2007-09-27 2013-12-03 Amylin Pharmaceuticals, Llc Peptide-peptidase-inhibitor conjugates and methods of making and using same
US20100317057A1 (en) 2007-12-28 2010-12-16 Novo Nordisk A/S Semi-recombinant preparation of glp-1 analogues
ES2561208T3 (es) 2008-09-12 2016-02-25 Novo Nordisk A/S Método de acilación de un péptido o una proteína
EP2513140B1 (en) 2009-12-16 2015-11-04 Novo Nordisk A/S Double-acylated glp-1 derivatives
EP2637699B1 (en) * 2010-11-09 2018-05-16 Novo Nordisk A/S Double-acylated glp-1 derivatives with a linker

Also Published As

Publication number Publication date
EP2637698B1 (en) 2022-04-20
US20130288960A1 (en) 2013-10-31
JP6039569B2 (ja) 2016-12-07
CN103200966A (zh) 2013-07-10
JP6231386B2 (ja) 2017-11-15
CN103209711B (zh) 2016-04-13
CN103209711A (zh) 2013-07-17
JP2014501712A (ja) 2014-01-23
EP2637698A1 (en) 2013-09-18
US9708383B2 (en) 2017-07-18
US9006178B2 (en) 2015-04-14
ES2913803T3 (es) 2022-06-06
CN105601729A (zh) 2016-05-25
EP2637699B1 (en) 2018-05-16
CN103200966B (zh) 2016-10-12
JP2016188246A (ja) 2016-11-04
US20150210745A1 (en) 2015-07-30
EP2637699A1 (en) 2013-09-18
WO2012062803A1 (en) 2012-05-18
JP2013543853A (ja) 2013-12-09
US20130338068A1 (en) 2013-12-19
WO2012062804A1 (en) 2012-05-18

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