TWI726889B - 蛋白酶抗性之脂化肽 - Google Patents

蛋白酶抗性之脂化肽 Download PDF

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Publication number
TWI726889B
TWI726889B TW105118294A TW105118294A TWI726889B TW I726889 B TWI726889 B TW I726889B TW 105118294 A TW105118294 A TW 105118294A TW 105118294 A TW105118294 A TW 105118294A TW I726889 B TWI726889 B TW I726889B
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Taiwan
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res
mod
peptide
peg
phe
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TW105118294A
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English (en)
Chinese (zh)
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TW201710287A (zh
Inventor
傑佛森D 瑞維爾
瑪利亞A 班德那克
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英商梅迪繆思有限公司
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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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Toxicology (AREA)
  • Hematology (AREA)
  • Obesity (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)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
TW105118294A 2015-06-10 2016-06-08 蛋白酶抗性之脂化肽 TWI726889B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW201710287A TW201710287A (zh) 2017-03-16
TWI726889B true TWI726889B (zh) 2021-05-11

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Family Applications (1)

Application Number Title Priority Date Filing Date
TW105118294A TWI726889B (zh) 2015-06-10 2016-06-08 蛋白酶抗性之脂化肽

Country Status (25)

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

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AU2017277594A1 (en) * 2016-06-09 2019-02-07 Medimmune Limited Protease-resistant mono-lipidated peptides
CR20200185A (es) * 2017-10-31 2020-06-19 Medimmune Ltd Administración oral de análogos del péptido glp-1
RS63523B1 (sr) 2018-04-05 2022-09-30 Sun Pharmaceutical Ind Ltd Novi glp-1 analozi
WO2022159395A1 (en) 2021-01-20 2022-07-28 Viking Therapeutics, Inc. Compositions and methods for the treatment of metabolic and liver disorders
MX2024003236A (es) 2021-09-15 2024-06-19 Viking Therapeutics Inc Composiciones y metodos para el tratamiento de trastornos metabolicos y hepaticos.
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

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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
JP2006501820A (ja) 2002-09-06 2006-01-19 バイエル・フアーマシユーチカルズ・コーポレーシヨン 修飾glp−1受容体アゴニストおよびそれらの薬理学的使用法
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
ATE444741T1 (de) * 2006-05-10 2009-10-15 Biocompatibles Uk Ltd Glp-1 peptide enthaltende kugelförmige mikrokapseln, deren produktion und deren verwendung
US20100022457A1 (en) 2006-05-26 2010-01-28 Bristol-Myers Squibb Company Sustained release glp-1 receptor modulators
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ATE502114T1 (de) 2007-06-21 2011-04-15 Univ Muenchen Tech Biologisch aktive proteine mit erhöhter in-vivo- und/oder in-vitro-stabilität
WO2009125424A2 (en) 2007-12-11 2009-10-15 Cadila Healthcare Limited Peptidomimetics with glucagon antagonistic and glp-1 agonistic activities
KR101740066B1 (ko) * 2008-12-05 2017-05-25 글락소 그룹 리미티드 프로테아제 저항성 폴리펩티드를 선택하는 방법
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Brian D. Green et al:Degradation, receptor binding, insulin secreting and antihyperglycaemic actions of palmitate-derivatised native and Ala8-substituted GLP-1 analogues. Biol. Chem., Vol. 385, pp. 169–177, February 2004.
Hongxiang Hui et al:Structure and function studies of glucagon-like peptide-1 (GLP-1): the designing of a novel pharmacological agent for the treatment of diabetes. DIABETES/METABOLISM RESEARCH AND REVIEWS REVIEW ARTICLE Diabetes Metab Res Rev 2005; 21: 313–331.
Hongxiang Hui et al:Structure and function studies of glucagon-like peptide-1 (GLP-1): the designing of a novel pharmacological agent for the treatment of diabetes. DIABETES/METABOLISM RESEARCH AND REVIEWS REVIEW ARTICLE Diabetes Metab Res Rev 2005; 21: 313–331. Brian D. Green et al:Degradation, receptor binding, insulin secreting and antihyperglycaemic actions of palmitate-derivatised native and Ala8-substituted GLP-1 analogues. Biol. Chem., Vol. 385, pp. 169–177, February 2004. *

Also Published As

Publication number Publication date
MX2017015482A (es) 2018-02-09
NZ738909A (en) 2019-08-30
JP2018518485A (ja) 2018-07-12
CA2988841C (en) 2023-06-06
US20210221866A1 (en) 2021-07-22
CO2017012675A2 (es) 2018-02-28
DOP2017000287A (es) 2018-04-15
SG10201911837SA (en) 2020-01-30
EP3865504A1 (en) 2021-08-18
US10414811B2 (en) 2019-09-17
CN108271373B (zh) 2021-12-28
CR20170559A (es) 2018-05-11
IL255978A (en) 2018-01-31
EP3307769A1 (en) 2018-04-18
AU2016277449A1 (en) 2018-02-01
KR20180016441A (ko) 2018-02-14
JP6811190B2 (ja) 2021-01-13
CA2988841A1 (en) 2016-12-15
ES2849950T3 (es) 2021-08-24
WO2016198544A1 (en) 2016-12-15
TN2017000519A1 (en) 2019-04-12
AU2016277449B2 (en) 2019-06-20
US20180162920A1 (en) 2018-06-14
EA036415B1 (ru) 2020-11-09
MX389407B (es) 2025-03-20
NI201700156A (es) 2018-10-18
IL255978B (en) 2021-04-29
EP3307769B1 (en) 2020-12-02
CL2017003144A1 (es) 2018-04-13
PH12017502259A1 (en) 2018-06-25
EA201792640A1 (ru) 2018-06-29
PE20180659A1 (es) 2018-04-17
AU2019229424A1 (en) 2019-10-03
CN108271373A (zh) 2018-07-10
TW201710287A (zh) 2017-03-16
SV2017005585A (es) 2018-05-22
US20200079833A1 (en) 2020-03-12
MY185816A (en) 2021-06-10

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