CN103415300B - N‑末端修饰的fgf21化合物 - Google Patents

N‑末端修饰的fgf21化合物 Download PDF

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Publication number
CN103415300B
CN103415300B CN201180045216.4A CN201180045216A CN103415300B CN 103415300 B CN103415300 B CN 103415300B CN 201180045216 A CN201180045216 A CN 201180045216A CN 103415300 B CN103415300 B CN 103415300B
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China
Prior art keywords
fgf21
formula
derivative
ethoxy
compound
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Expired - Fee Related
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CN201180045216.4A
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English (en)
Chinese (zh)
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CN103415300A (zh
Inventor
T.M.塔格莫塞
P.W.加里拜
X.张
H.托格森
P.K.尼尔森
B.安德森
J.王
K.S.巴克詹森
H.F.维迪科
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Novo Nordisk AS
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Novo Nordisk AS
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    • 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
    • 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
    • A61K38/18Growth factors; Growth regulators
    • A61K38/1825Fibroblast growth factor [FGF]
    • 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
    • A61K47/545Heterocyclic compounds
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CN201180045216.4A 2010-07-20 2011-07-18 N‑末端修饰的fgf21化合物 Expired - Fee Related CN103415300B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CNPCT/CN2010/001087 2010-07-20
CN2010001087 2010-07-20
US37407210P 2010-08-16 2010-08-16
US61/374072 2010-08-16
US61/374,072 2010-08-16
PCT/EP2011/062238 WO2012010553A1 (en) 2010-07-20 2011-07-18 N-terminal modified fgf21 compounds

Publications (2)

Publication Number Publication Date
CN103415300A CN103415300A (zh) 2013-11-27
CN103415300B true CN103415300B (zh) 2018-02-23

Family

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CN201180045216.4A Expired - Fee Related CN103415300B (zh) 2010-07-20 2011-07-18 N‑末端修饰的fgf21化合物

Country Status (5)

Country Link
US (1) US9655974B2 (https=)
EP (1) EP2595647A1 (https=)
JP (1) JP6069198B2 (https=)
CN (1) CN103415300B (https=)
WO (1) WO2012010553A1 (https=)

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CN105601748B (zh) 2011-07-01 2021-08-27 恩格姆生物制药公司 用于代谢病症和疾病治疗的组合物、应用和方法
US9290557B2 (en) 2012-11-28 2016-03-22 Ngm Biopharmaceuticals, Inc. Compositions comprising variants and fusions of FGF19 polypeptides
HK1214832A1 (zh) 2012-11-28 2016-08-05 恩格姆生物制药公司 用於代謝病症和疾病治療的組合物和方法
ES2915851T3 (es) 2012-12-27 2022-06-27 Ngm Biopharmaceuticals Inc Péptidos quiméricos de FGF19 para usar en el tratamiento de trastornos de ácidos biliares
US9273107B2 (en) 2012-12-27 2016-03-01 Ngm Biopharmaceuticals, Inc. Uses and methods for modulating bile acid homeostasis and treatment of bile acid disorders and diseases
AU2014340241B2 (en) 2013-10-21 2018-11-01 Salk Institute For Biological Studies Mutated fibroblast growth factor (FGF) 1 and methods of use
WO2015061331A1 (en) 2013-10-21 2015-04-30 Salk Institute For Biological Studies Chimeric fibroblast growth factor (fgf) 2/fgf1 peptides and methods of use
CA2927592C (en) 2013-10-28 2020-08-18 Ngm Biopharmaceuticals, Inc. Fgf-19 variants for treating a fgf-19 dependent cancer or tumor
TWI670283B (zh) 2013-12-23 2019-09-01 美商建南德克公司 抗體及使用方法
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US20170065678A1 (en) 2014-03-11 2017-03-09 Novartis Ag Methods of treating metabolic disorders associated with lipodystrophies and defects in insulin production or signaling
WO2015183890A2 (en) 2014-05-28 2015-12-03 Ngm Biopharmaceuticals, Inc. Methods and compositions for the treatment of metabolic disorders and diseases
AU2015277438B2 (en) 2014-06-16 2020-02-27 Ngm Biopharmaceuticals, Inc. Methods and uses for modulating bile acid homeostasis and treatment of bile acid disorders and diseases
RU2729161C2 (ru) 2014-10-23 2020-08-04 ЭнДжиЭм БАЙОФАРМАСЬЮТИКАЛЗ, ИНК. Фармацевтические композиции, содержащие варианты пептидов, и способы их применения
US10434144B2 (en) 2014-11-07 2019-10-08 Ngm Biopharmaceuticals, Inc. Methods for treatment of bile acid-related disorders and prediction of clinical sensitivity to treatment of bile acid-related disorders
AR103246A1 (es) * 2014-12-23 2017-04-26 Novo Nordiks As Derivados de fgf21 y sus usos
US10800843B2 (en) 2015-07-29 2020-10-13 Ngm Biopharmaceuticals, Inc. Beta klotho-binding proteins
AU2016326689A1 (en) * 2015-09-24 2018-03-22 Genentech, Inc. Methods for the treatment of epilepsy
KR102670157B1 (ko) 2015-10-28 2024-05-29 주식회사유한양행 이중 작용 단백질 및 이를 포함하는 약학적 조성물
KR102668200B1 (ko) * 2015-10-28 2024-05-23 주식회사유한양행 지속형 fgf21 융합 단백질 및 이를 포함하는 약학적 조성물
EP3368059A4 (en) 2015-10-30 2019-03-27 Salk Institute for Biological Studies TREATMENT OF STEROID-INDUCED HYPERGLYCEMIA WITH FIBROBLAST GROWTH FACTOR (FGF) -1 ANALOGUE
JP6728352B2 (ja) 2015-11-09 2020-07-22 エヌジーエム バイオファーマシューティカルス,インコーポレーテッド 胆汁酸に関係した障害の治療方法
WO2017220706A1 (en) 2016-06-22 2017-12-28 Novo Nordisk A/S Pharmaceutical compositions of fgf21 derivatives and uses thereof
US11123438B2 (en) 2016-08-19 2021-09-21 Ampsource Biopharma Shanghai Inc. Linker peptide for constructing fusion protein
CN106317226B (zh) 2016-08-19 2017-09-05 安源医药科技(上海)有限公司 用于构建融合蛋白的连接肽
CN106279437B (zh) 2016-08-19 2017-10-31 安源医药科技(上海)有限公司 高糖基化人凝血因子viii融合蛋白及其制备方法与用途
CA3034399A1 (en) 2016-08-26 2018-03-01 Ngm Biopharmaceuticals, Inc. Methods of treating fibroblast growth factor 19-mediated cancers and tumors
MX2019005380A (es) 2016-11-10 2019-08-12 Yuhan Corp Composicion farmaceutica que comprende proteinas de fusion para prevenir o tratar la hepatitis, la fibrosis hepatica y la cirrosis hepatica.
CN108619490A (zh) 2017-03-22 2018-10-09 天士力医药集团股份有限公司 一种长效化突变的人源成纤维生长因子的新用途
US11560416B2 (en) 2017-04-21 2023-01-24 Yuhan Corporation Method for producing dual function proteins and its derivatives
WO2019123427A1 (en) 2017-12-22 2019-06-27 Novartis Ag Methods of treating metabolic disorders with fgf21 variants
US11542309B2 (en) 2019-07-31 2023-01-03 Salk Institute For Biological Studies Fibroblast growth factor 1 (FGF1) mutant proteins that selectively activate FGFR1B to reduce blood glucose
CN113728013B (zh) 2020-01-11 2022-06-14 北京质肽生物医药科技有限公司 Glp-1和fgf21的融合蛋白的缀合物
US11981718B2 (en) 2020-05-27 2024-05-14 Ampsource Biopharma Shanghai Inc. Dual-function protein for lipid and blood glucose regulation
KR20220021207A (ko) 2020-08-13 2022-02-22 주식회사 나이벡 이소골 형성 부작용 경감으로 치료효과가 증진된 골형성 단백질-9, 10의 변이체 및 이를 포함하는 약학적 조성물
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Also Published As

Publication number Publication date
US20130190232A1 (en) 2013-07-25
US9655974B2 (en) 2017-05-23
CN103415300A (zh) 2013-11-27
JP6069198B2 (ja) 2017-02-01
WO2012010553A1 (en) 2012-01-26
EP2595647A1 (en) 2013-05-29
JP2013532644A (ja) 2013-08-19

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Granted publication date: 20180223

Termination date: 20190718