JP6811190B2 - プロテアーゼ耐性脂質付加glp−1類似体 - Google Patents

プロテアーゼ耐性脂質付加glp−1類似体 Download PDF

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JP6811190B2
JP6811190B2 JP2017563292A JP2017563292A JP6811190B2 JP 6811190 B2 JP6811190 B2 JP 6811190B2 JP 2017563292 A JP2017563292 A JP 2017563292A JP 2017563292 A JP2017563292 A JP 2017563292A JP 6811190 B2 JP6811190 B2 JP 6811190B2
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peptide
lipid
peg
polypeptide
amino acid
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JP2018518485A5 (enExample
JP2018518485A (ja
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レヴェル,ジェファーソン,ディー
ベドナレク,マリア,エー
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MedImmune Ltd
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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
    • 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
    • A61K38/26Glucagons
    • 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
    • A61K38/28Insulins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P3/08Drugs 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Toxicology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
JP2017563292A 2015-06-10 2016-06-09 プロテアーゼ耐性脂質付加glp−1類似体 Active JP6811190B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562173631P 2015-06-10 2015-06-10
US62/173,631 2015-06-10
US201662343390P 2016-05-31 2016-05-31
US62/343,390 2016-05-31
PCT/EP2016/063206 WO2016198544A1 (en) 2015-06-10 2016-06-09 Protease-resistant lipidated glp-1 analogs

Publications (3)

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JP2018518485A JP2018518485A (ja) 2018-07-12
JP2018518485A5 JP2018518485A5 (enExample) 2019-05-23
JP6811190B2 true JP6811190B2 (ja) 2021-01-13

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JP2017563292A Active JP6811190B2 (ja) 2015-06-10 2016-06-09 プロテアーゼ耐性脂質付加glp−1類似体

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US (3) US10414811B2 (enExample)
EP (2) EP3865504A1 (enExample)
JP (1) JP6811190B2 (enExample)
KR (1) KR20180016441A (enExample)
CN (1) CN108271373B (enExample)
AU (2) AU2016277449B2 (enExample)
CA (1) CA2988841C (enExample)
CL (1) CL2017003144A1 (enExample)
CO (1) CO2017012675A2 (enExample)
CR (1) CR20170559A (enExample)
DO (1) DOP2017000287A (enExample)
EA (1) EA036415B1 (enExample)
ES (1) ES2849950T3 (enExample)
IL (1) IL255978B (enExample)
MX (1) MX389407B (enExample)
MY (1) MY185816A (enExample)
NI (1) NI201700156A (enExample)
NZ (1) NZ738909A (enExample)
PE (1) PE20180659A1 (enExample)
PH (1) PH12017502259A1 (enExample)
SG (1) SG10201911837SA (enExample)
SV (1) SV2017005585A (enExample)
TN (1) TN2017000519A1 (enExample)
TW (1) TWI726889B (enExample)
WO (1) WO2016198544A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3025592A1 (en) * 2016-06-09 2017-12-14 Medimmune Limited Protease-resistant mono-lipidated peptides
MA50047A (fr) * 2017-10-31 2020-07-08 Medimmune Ltd Administration orale d'analogues peptidiques de glp-1
PE20211417A1 (es) 2018-04-05 2021-08-02 Sun Pharmaceutical Ind Ltd Analogos novedosos de glp-1
CA3204051A1 (en) 2021-01-20 2022-07-28 Brian Lian Compositions and methods for the treatment of metabolic and liver disorders
WO2023044290A1 (en) 2021-09-15 2023-03-23 Viking Therapeutics, Inc. Compositions and methods for the treatment of metabolic and liver disorders
TW202346323A (zh) * 2022-02-07 2023-12-01 英商梅迪繆思有限公司 具有改善的生物穩定性的glp—1及升糖素雙重激動肽

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0154316B1 (en) 1984-03-06 1989-09-13 Takeda Chemical Industries, Ltd. Chemically modified lymphokine and production thereof
EP0401384B1 (en) 1988-12-22 1996-03-13 Kirin-Amgen, Inc. Chemically modified granulocyte colony stimulating factor
CA2497794A1 (en) 2002-09-06 2004-03-18 Bayer Pharmaceuticals Corporation Modified glp-1 receptor agonists and their pharmacological methods of use
CN101010339B (zh) * 2004-07-02 2011-11-09 布里斯托尔-迈尔斯斯奎布公司 人类胰高血糖素样肽-1调节剂及它们在治疗糖尿病及相关病况中的用途
BRPI0615573A2 (pt) * 2005-09-08 2011-05-24 Tufts College análogos de glp-1 estabilizados
EP1854455B1 (en) * 2006-05-10 2009-10-07 Biocompatibles UK Limited Spherical microcapsules comprising GLP-1 peptides, their production and use
EP2021014A1 (en) 2006-05-26 2009-02-11 Brystol-Myers Squibb Company Sustained release glp-1 receptor modulators
WO2008023050A1 (en) 2006-08-25 2008-02-28 Novo Nordisk A/S Acylated exendin-4 compounds
DE602008005596D1 (de) 2007-06-21 2011-04-28 Univ Muenchen Tech Biologisch aktive proteine mit erhöhter in-vivo- und/oder in-vitro-stabilität
CA2707448C (en) 2007-12-11 2014-10-14 Cadila Healthcare Limited Peptidomimetics with glucagon antagonistic and glp-1 agonistic activities
US8685895B2 (en) * 2008-12-05 2014-04-01 Carolyn Enever Methods for selecting protease resistant polypeptides
CN102459325B (zh) 2009-06-16 2015-03-25 印第安纳大学科技研究有限公司 胃抑胜肽受体活化的胰高血糖素化合物
WO2011048614A2 (en) 2009-10-22 2011-04-28 Cadila Healthcare Limited Short chain peptidomimetics based orally active glp-1 agonist and glucagon receptor antagonist
EP2569000B1 (en) 2010-05-13 2017-09-27 Indiana University Research and Technology Corporation Glucagon superfamily peptides exhibiting nuclear hormone receptor activity
US20130143800A1 (en) 2011-11-07 2013-06-06 Research Development Foundation Combination therapies to treat diabetes
AR092873A1 (es) 2012-09-26 2015-05-06 Cadila Healthcare Ltd Peptidos como agonistas triples de los receptores de gip, glp-1 y glugagon
WO2014088631A1 (en) * 2012-12-06 2014-06-12 Stealth Peptides International, Inc. Peptide therapeutics and methods for using same
HK1220383A1 (zh) * 2013-03-14 2017-05-05 Medimmune Limited 用於治疗肥胖症的聚乙二醇化的胰高血糖素和glp-1共激动剂
SG10201805039UA (en) 2013-12-13 2018-07-30 Medimmune Ltd Protease resistant peptides

Also Published As

Publication number Publication date
SV2017005585A (es) 2018-05-22
AU2019229424A1 (en) 2019-10-03
IL255978B (en) 2021-04-29
EP3307769B1 (en) 2020-12-02
CO2017012675A2 (es) 2018-02-28
EP3307769A1 (en) 2018-04-18
CN108271373A (zh) 2018-07-10
PH12017502259A1 (en) 2018-06-25
EP3865504A1 (en) 2021-08-18
NZ738909A (en) 2019-08-30
CA2988841A1 (en) 2016-12-15
TWI726889B (zh) 2021-05-11
EA036415B1 (ru) 2020-11-09
CN108271373B (zh) 2021-12-28
KR20180016441A (ko) 2018-02-14
CL2017003144A1 (es) 2018-04-13
TN2017000519A1 (en) 2019-04-12
AU2016277449B2 (en) 2019-06-20
US20180162920A1 (en) 2018-06-14
CR20170559A (es) 2018-05-11
NI201700156A (es) 2018-10-18
TW201710287A (zh) 2017-03-16
MY185816A (en) 2021-06-10
SG10201911837SA (en) 2020-01-30
MX2017015482A (es) 2018-02-09
US20200079833A1 (en) 2020-03-12
DOP2017000287A (es) 2018-04-15
US10414811B2 (en) 2019-09-17
ES2849950T3 (es) 2021-08-24
AU2016277449A1 (en) 2018-02-01
MX389407B (es) 2025-03-20
CA2988841C (en) 2023-06-06
EA201792640A1 (ru) 2018-06-29
IL255978A (en) 2018-01-31
US20210221866A1 (en) 2021-07-22
PE20180659A1 (es) 2018-04-17
JP2018518485A (ja) 2018-07-12
WO2016198544A1 (en) 2016-12-15

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