CN110494145A - 治疗脂蛋白代谢障碍的化合物 - Google Patents

治疗脂蛋白代谢障碍的化合物 Download PDF

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Publication number
CN110494145A
CN110494145A CN201780069925.3A CN201780069925A CN110494145A CN 110494145 A CN110494145 A CN 110494145A CN 201780069925 A CN201780069925 A CN 201780069925A CN 110494145 A CN110494145 A CN 110494145A
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CN
China
Prior art keywords
formula
compound
composition according
pcsk9
substituted
Prior art date
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Pending
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CN201780069925.3A
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English (en)
Chinese (zh)
Inventor
C·古斯塔夫森
S·P·马德森
G·S·彼得森
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Aarhus Universitet
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Aarhus Universitet
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/727—Heparin; Heparan
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/554—Medicinal 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 the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/62—Medicinal 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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • A61K47/6455—Polycationic oligopeptides, polypeptides or polyamino acids, e.g. for complexing nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Biochemistry (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Botany (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
CN201780069925.3A 2016-09-20 2017-09-20 治疗脂蛋白代谢障碍的化合物 Pending CN110494145A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA201670733 2016-09-20
DKPA201670733 2016-09-20
PCT/EP2017/073747 WO2018054959A1 (en) 2016-09-20 2017-09-20 Compounds for treatment of lipoprotein metabolism disorders

Publications (1)

Publication Number Publication Date
CN110494145A true CN110494145A (zh) 2019-11-22

Family

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Family Applications (1)

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CN201780069925.3A Pending CN110494145A (zh) 2016-09-20 2017-09-20 治疗脂蛋白代谢障碍的化合物

Country Status (9)

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US (2) US11173177B2 (https=)
EP (1) EP3515455B1 (https=)
JP (1) JP7046381B2 (https=)
CN (1) CN110494145A (https=)
AU (1) AU2017329799A1 (https=)
CA (1) CA3035875A1 (https=)
DK (1) DK3515455T3 (https=)
ES (1) ES2871783T3 (https=)
WO (1) WO2018054959A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116270507A (zh) * 2023-03-02 2023-06-23 青岛海洋生物医药研究院股份有限公司 一种含脂蛋白脂酶刺激剂的舌下含片及其制备方法和应用
WO2023185505A1 (zh) * 2022-03-28 2023-10-05 南开大学 肝素三糖结构化合物及其制药应用
CN119708089A (zh) * 2023-09-27 2025-03-28 南开大学 一种磺酸化三糖及其制备方法和治疗应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3973958A3 (en) * 2015-03-20 2022-06-22 Aarhus Universitet Inhibitors of pcsk9 for treatment of lipoprotein metabolism disorders
KR102137147B1 (ko) * 2018-07-16 2020-07-24 경희대학교 산학협력단 벤질 알파-d-갈락토피라노사이드 또는 (-)-세코이소라리시레시놀-9'-o-베타-d-글루코피라노사이드를 포함하는 당뇨병 예방 또는 치료용 조성물
SE543275C2 (en) * 2019-03-07 2020-11-10 Tx Medic Ab Treatment efficiency evaluation
WO2021122793A1 (en) * 2019-12-17 2021-06-24 Norinvent Ab Sulfated disaccharides as enhancers of transmucosal drug uptake
US12378557B2 (en) 2020-08-25 2025-08-05 Regeneron Pharmaceuticals, Inc. Treatment of sepsis with PCSK9 and LDLR modulators

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107531798A (zh) * 2015-03-20 2018-01-02 奥胡斯大学 Pcsk9的抑制剂用于脂蛋白代谢病症的治疗

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4602003A (en) * 1982-05-17 1986-07-22 Medical Research Foundation Of Oregon Synthetic compounds to inhibit intestinal absorption of cholesterol in the treatment of hypercholesterolemia
ES2114948T3 (es) * 1991-10-04 1998-06-16 Procter & Gamble Compuestos disminuidores del colesterol y procedimiento para prepararlos.
DE69232137T2 (de) 1991-11-25 2002-05-29 Enzon Inc Multivalente antigen-bindende proteine
US5366473A (en) 1992-08-18 1994-11-22 Ultrasonic Sensing And Monitoring Systems, Inc. Method and apparatus for applying vascular grafts
GB9221657D0 (en) 1992-10-15 1992-11-25 Scotgen Ltd Recombinant bispecific antibodies
WO1994013806A1 (en) 1992-12-11 1994-06-23 The Dow Chemical Company Multivalent single chain antibodies
CN1487996B (zh) 2000-11-30 2010-06-16 米德列斯公司 用于生产人类抗体的转基因转染色体啮齿动物
US7754208B2 (en) 2001-01-17 2010-07-13 Trubion Pharmaceuticals, Inc. Binding domain-immunoglobulin fusion proteins
US20030133939A1 (en) 2001-01-17 2003-07-17 Genecraft, Inc. Binding domain-immunoglobulin fusion proteins
US8828952B2 (en) 2007-10-16 2014-09-09 Progen Pharmaceuticals Limited Sulfated oligosaccharide derivatives
TWI516501B (zh) 2008-09-12 2016-01-11 禮納特神經系統科學公司 Ｐｃｓｋ９拮抗劑類
CN102656153B (zh) 2009-10-29 2015-02-18 延世大学校产学协力团 新型血管渗漏阻断剂
WO2013091103A1 (en) 2011-12-20 2013-06-27 Adaerata, Limited Partnership Single domain antibodies as inhibitors of pcsk9
WO2013148284A1 (en) 2012-03-29 2013-10-03 Genentech, Inc. Antibodies that bind to a pcsk9 cleavage site and methods of use
US9255154B2 (en) 2012-05-08 2016-02-09 Alderbio Holdings, Llc Anti-PCSK9 antibodies and use thereof
CA2874244A1 (en) 2012-05-25 2013-11-28 Catabasis Pharmaceuticals, Inc. Methods of lowering proprotein convertase subtilisin/kexin type 9 (pcsk9)
US20150190369A1 (en) 2012-07-03 2015-07-09 Majambu Mbikay Quercetin-3-glucoside and uses thereof
HK1210953A1 (en) 2012-08-02 2016-05-13 Stealth Peptides International, Inc. Methods for treatment of atherosclerosis
JP2016514668A (ja) 2013-03-15 2016-05-23 アムジエン・インコーポレーテツド プロタンパク質コンベルターゼスブチリシンケクシン９型に結合するヒト抗原結合タンパク質
EP3197492A1 (en) 2014-09-23 2017-08-02 Pfizer Inc Treatment with anti-pcsk9 antibodies

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107531798A (zh) * 2015-03-20 2018-01-02 奥胡斯大学 Pcsk9的抑制剂用于脂蛋白代谢病症的治疗

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
CAMILLA GUSTAFSEN 等: "Heparan sulfate proteoglycans present PCSK9 to the LDL receptor", 《NATURE COMMUNICATIONS》 *
JOSE L. DE PAZ 等: "Potentiation of Fibroblast Growth Factor Activity by Synthetic Heparin Oligosaccharide Glycodendrimers", 《CHEMISTRY & BIOLOGY》 *
JOSE L. DE PAZ 等: "Profiling Heparin–Chemokine Interactions Using Synthetic Tools", 《ACS CHEMICAL BIOLOGY》 *
MARIE-LYN HECHT 等: "Natural Cytotoxicity Receptors NKp30, NKp44 and NKp46 Bind to Different Heparan Sulfate/Heparin Sequences", 《JOURNAL OF PROTEOME RESEARCH》 *
梅齐建 等: "低分子肝素对老年人血脂的影响", 《医药导报》 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023185505A1 (zh) * 2022-03-28 2023-10-05 南开大学 肝素三糖结构化合物及其制药应用
CN116854752A (zh) * 2022-03-28 2023-10-10 南开大学 肝素三糖结构化合物及其制药应用
CN116270507A (zh) * 2023-03-02 2023-06-23 青岛海洋生物医药研究院股份有限公司 一种含脂蛋白脂酶刺激剂的舌下含片及其制备方法和应用
CN119708089A (zh) * 2023-09-27 2025-03-28 南开大学 一种磺酸化三糖及其制备方法和治疗应用

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Publication number Publication date
EP3515455B1 (en) 2021-04-14
US11173177B2 (en) 2021-11-16
US20190275074A1 (en) 2019-09-12
EP3515455A1 (en) 2019-07-31
US20220054530A1 (en) 2022-02-24
JP7046381B2 (ja) 2022-04-04
CA3035875A1 (en) 2018-03-29
ES2871783T3 (es) 2021-11-02
WO2018054959A1 (en) 2018-03-29
JP2019529402A (ja) 2019-10-17
DK3515455T3 (da) 2021-07-05
AU2017329799A1 (en) 2019-04-11

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