CA2839410C - Pegylated analogues of exendin-4 - Google Patents

Pegylated analogues of exendin-4 Download PDF

Info

Publication number
CA2839410C
CA2839410C CA2839410A CA2839410A CA2839410C CA 2839410 C CA2839410 C CA 2839410C CA 2839410 A CA2839410 A CA 2839410A CA 2839410 A CA2839410 A CA 2839410A CA 2839410 C CA2839410 C CA 2839410C
Authority
CA
Canada
Prior art keywords
exendin
analogue
peg
derivative
cysteine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CA2839410A
Other languages
English (en)
French (fr)
Other versions
CA2839410A1 (en
Inventor
Sung Kwon Lee
Won Bae Kim
Seulki Lee
Tae Hyung Kim
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
D&D Pharmatech Inc
Original Assignee
D&D Pharmatech Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by D&D Pharmatech Inc filed Critical D&D Pharmatech Inc
Publication of CA2839410A1 publication Critical patent/CA2839410A1/en
Application granted granted Critical
Publication of CA2839410C publication Critical patent/CA2839410C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K47/02Inorganic compounds
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/2278Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • 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
    • A61K47/56Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • 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
    • 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
    • C07K14/57563Vasoactive intestinal peptide [VIP]; Related peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Vascular Medicine (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CA2839410A 2011-06-28 2012-06-28 Pegylated analogues of exendin-4 Active CA2839410C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR10-2011-0062858 2011-06-28
KR1020110062858A KR101357117B1 (ko) 2011-06-28 2011-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물
PCT/KR2012/005137 WO2013002580A2 (ko) 2011-06-28 2012-06-28 폴리에틸렌글라이콜 또는 이의 유도체로 페길화된 엑센딘-4 유사체, 이의 제조방법 및 이를 유효성분으로 함유하는 당뇨병 예방 또는 치료용 약학적 조성물

Publications (2)

Publication Number Publication Date
CA2839410A1 CA2839410A1 (en) 2013-01-03
CA2839410C true CA2839410C (en) 2019-05-14

Family

ID=47424684

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2839410A Active CA2839410C (en) 2011-06-28 2012-06-28 Pegylated analogues of exendin-4

Country Status (10)

Country Link
US (2) US20130217622A1 (enExample)
EP (1) EP2727605B1 (enExample)
JP (1) JP6084215B2 (enExample)
KR (1) KR101357117B1 (enExample)
CN (1) CN103338790B (enExample)
AU (1) AU2012276478B2 (enExample)
CA (1) CA2839410C (enExample)
DK (1) DK2727605T3 (enExample)
ES (1) ES2674581T3 (enExample)
WO (1) WO2013002580A2 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2851429B1 (en) 2012-05-18 2019-07-24 Adda Biotech Inc. Protein and protein conjugate for diabetes treatment, and applications thereof
UA116217C2 (uk) 2012-10-09 2018-02-26 Санофі Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону
HRP20181300T1 (hr) 2012-12-21 2018-10-05 Sanofi Derivati eksendina-4 kao dvostruki glp1/gip- ili trostruki glp1/gip/glukagon agonisti
CN105934257B (zh) 2013-12-06 2020-10-09 韩捷 用于含氮和羟基的药物的生物可逆引入基团
TW201609796A (zh) 2013-12-13 2016-03-16 賽諾菲公司 非醯化之艾塞那肽-4(exendin-4)胜肽類似物
WO2015086728A1 (en) 2013-12-13 2015-06-18 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
EP3080154B1 (en) 2013-12-13 2018-02-07 Sanofi Dual glp-1/gip receptor agonists
EP3080149A1 (en) 2013-12-13 2016-10-19 Sanofi Dual glp-1/glucagon receptor agonists
TW201625670A (zh) 2014-04-07 2016-07-16 賽諾菲公司 衍生自exendin-4之雙重glp-1/升糖素受體促效劑
TW201625669A (zh) 2014-04-07 2016-07-16 賽諾菲公司 衍生自艾塞那肽-4(Exendin-4)之肽類雙重GLP-1/升糖素受體促效劑
TW201625668A (zh) 2014-04-07 2016-07-16 賽諾菲公司 作為胜肽性雙重glp-1/昇糖素受體激動劑之艾塞那肽-4衍生物
US9932381B2 (en) 2014-06-18 2018-04-03 Sanofi Exendin-4 derivatives as selective glucagon receptor agonists
CN105985425B (zh) * 2014-12-11 2019-12-17 浙江海昶生物医药技术有限公司 一种聚乙二醇修饰的exendin类似物及其制备方法和应用
AR105319A1 (es) 2015-06-05 2017-09-27 Sanofi Sa Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico
AR105284A1 (es) 2015-07-10 2017-09-20 Sanofi Sa Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón
WO2017024182A1 (en) 2015-08-04 2017-02-09 Duke University Genetically encoded intrinsically disordered stealth polymers for delivery and methods of using same
US11752213B2 (en) 2015-12-21 2023-09-12 Duke University Surfaces having reduced non-specific binding and antigenicity
ES2968038T3 (es) 2015-12-23 2024-05-06 Univ Johns Hopkins Agonista GLP-1R de acción prolongada como terapia de afecciones neurológicas y neurodegenerativas
CN113546159B (zh) * 2015-12-29 2023-09-08 派格生物医药(苏州)股份有限公司 包含glp-1受体激动剂和胰高血糖素受体激动剂的组合物及其用途
US11467156B2 (en) 2016-06-01 2022-10-11 Duke University Nonfouling biosensors
WO2018057847A1 (en) 2016-09-23 2018-03-29 Duke University Unstructured non-repetitive polypeptides having lcst behavior
US11648200B2 (en) 2017-01-12 2023-05-16 Duke University Genetically encoded lipid-polypeptide hybrid biomaterials that exhibit temperature triggered hierarchical self-assembly
WO2018213320A1 (en) 2017-05-15 2018-11-22 Duke University Recombinant production of hybrid lipid-biopolymer materials that self-assemble and encapsulate agents
WO2019147954A1 (en) 2018-01-26 2019-08-01 Duke University Albumin binding peptide-drug (aibiped) conjugates and methods of making and using same
WO2019213150A1 (en) 2018-04-30 2019-11-07 Duke University Stimuli-responsive peg-like polymer-based drug delivery platform
KR20200135618A (ko) * 2019-05-23 2020-12-03 ㈜ 디앤디파마텍 폴리펩티드를 포함하는 비알코올성 지방간 질환의 예방 또는 치료용 약학 조성물
US11649275B2 (en) 2018-08-02 2023-05-16 Duke University Dual agonist fusion proteins
US11512314B2 (en) 2019-07-12 2022-11-29 Duke University Amphiphilic polynucleotides
KR102193211B1 (ko) * 2019-11-27 2020-12-18 (주)디앤디파마텍 비오틴 모이어티가 결합된 폴리펩티드 및 이를 포함하는 경구 투여용 약학적 조성물
US20240181013A1 (en) * 2021-04-01 2024-06-06 Duke University Poegma copolymer conjugates and methods of treating diseases
US20240374691A1 (en) 2021-08-25 2024-11-14 Neuraly, Inc. Glp-1r agonists for use in a treatment of neurologial impairment associated with viral infection
KR20240155737A (ko) 2023-04-20 2024-10-29 전북대학교산학협력단 폴리에틸렌글리콜을 이용한 분자 전달 방법
WO2024229006A1 (en) * 2023-05-01 2024-11-07 Neuraly, Inc. Glucagon-like peptide-1 receptor agonist variants and methods thereof

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2343072T3 (es) * 1999-01-14 2010-07-22 Amylin Pharmaceuticals, Inc. Exendina para la supresion del glucagon.
CN1191273C (zh) * 1999-05-17 2005-03-02 康久化学公司 长效促胰岛肽
EP1539210A4 (en) * 2002-09-06 2006-06-07 Bayer Pharmaceuticals Corp GLP-1 RECEPTOR MODIFIED AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
CA2529819A1 (en) * 2003-06-30 2004-09-23 Domantis Limited Pegylated single domain antibodies
JP2008516621A (ja) * 2004-10-18 2008-05-22 ノボ ノルディスク アクティーゼルスカブ 成長ホルモン結合体
WO2007075534A2 (en) * 2005-12-16 2007-07-05 Nektar Therapeutics Al, Corporation Polymer conjugates of glp-1
KR100890989B1 (ko) * 2006-06-01 2009-03-31 이강춘 폴리에틸렌글리콜 또는 이의 유도체로 단일 수식된 엑센딘,이의 제조방법 및 이의 용도
US8420598B2 (en) * 2007-04-20 2013-04-16 B & L Delipharm Corp. Mono modified exendin with polyethylene glycol or its derivatives and uses thereof
CN101870728A (zh) * 2009-04-23 2010-10-27 派格生物医药(苏州)有限公司 新型Exendin变体及其缀合物
KR101112578B1 (ko) * 2009-07-16 2012-02-16 성균관대학교산학협력단 엑센딘의 비강투여용 약제학적 조성물 및 이의 제조방법

Also Published As

Publication number Publication date
WO2013002580A2 (ko) 2013-01-03
KR101357117B1 (ko) 2014-02-06
JP2014520798A (ja) 2014-08-25
CN103338790B (zh) 2018-01-23
EP2727605B1 (en) 2018-04-04
ES2674581T3 (es) 2018-07-02
WO2013002580A3 (ko) 2013-04-11
CN103338790A (zh) 2013-10-02
EP2727605A4 (en) 2014-12-24
CA2839410A1 (en) 2013-01-03
DK2727605T3 (en) 2018-06-25
AU2012276478A1 (en) 2014-01-23
US10406230B2 (en) 2019-09-10
US20130217622A1 (en) 2013-08-22
JP6084215B2 (ja) 2017-02-22
KR20130008665A (ko) 2013-01-23
EP2727605A2 (en) 2014-05-07
US20170189545A1 (en) 2017-07-06
AU2012276478B2 (en) 2016-02-25

Similar Documents

Publication Publication Date Title
CA2839410C (en) Pegylated analogues of exendin-4
KR102449145B1 (ko) 지속형 인슐린 아날로그 결합체 및 지속형 인슐린 분비 펩타이드 결합체를 포함하는 당뇨병 치료용 조성물
CN102026666B (zh) 促胰岛素肽缀合物制剂
WO2021022149A1 (en) Insulin analogs and methods of using the same
EP2773672B1 (en) Method for preparing physiologically active polypeptide complex
EA018471B1 (ru) Слитые конструкции и конъюгаты лекарственного средства
US20140142037A1 (en) Site-directed mono-substituted pegylated exendin analog and preparation method therefor
KR100890989B1 (ko) 폴리에틸렌글리콜 또는 이의 유도체로 단일 수식된 엑센딘,이의 제조방법 및 이의 용도
CN111194223A (zh) 与白蛋白具有较佳结合亲和力的药物分子
WO2017152861A1 (en) Conjugates of islet neogenesis peptides and analogs, and methods thereof
CA2950266C (en) Composition for treating diabetes, comprising long-acting insulin analogue conjugate and long-acting insulinotropic peptide conjugate
KR20120104459A (ko) 페길화된 엑센딘-4 이량체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
HK1230958A1 (en) Composition for treating diabetes, containing long-acting insulin analog conjugate and long-acting insulin secretion peptide conjugate
NZ726959B2 (en) Composition for treating diabetes comprising long-acting insulin analogue conjugate and long-acting insulinotropic peptide conjugate
HK1230958B (en) Composition for treating diabetes, containing long-acting insulin analog conjugate and long-acting insulin secretion peptide conjugate

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20131213