KR20150132362A - Pcsk9의 소분자 조절물질 및 그것의 사용 방법 - Google Patents

Pcsk9의 소분자 조절물질 및 그것의 사용 방법 Download PDF

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KR20150132362A
KR20150132362A KR1020157029032A KR20157029032A KR20150132362A KR 20150132362 A KR20150132362 A KR 20150132362A KR 1020157029032 A KR1020157029032 A KR 1020157029032A KR 20157029032 A KR20157029032 A KR 20157029032A KR 20150132362 A KR20150132362 A KR 20150132362A
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South Korea
Prior art keywords
alkyl
substituted
unsubstituted
phenyl
compound
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Korean (ko)
Inventor
다니엘 구아이
쉘던 크레인
니콜라스 라샹스
진-프랑수아 치아손
보우이 린 트루옹
패트릭 라콩브
캐서린 스코리
나빌 지 세이다
Original Assignee
에이다에레이타, 리미티드 파트너쉽
아모르캠 홀딩스 아이엔씨.
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Publication of KR20150132362A publication Critical patent/KR20150132362A/ko
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Crystallography & Structural Chemistry (AREA)
KR1020157029032A 2013-03-15 2014-03-14 Pcsk9의 소분자 조절물질 및 그것의 사용 방법 Withdrawn KR20150132362A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361792249P 2013-03-15 2013-03-15
US61/792,249 2013-03-15
PCT/CA2014/050255 WO2014139008A1 (en) 2013-03-15 2014-03-14 Small molecule modulators of pcsk9 and methods of use thereof

Publications (1)

Publication Number Publication Date
KR20150132362A true KR20150132362A (ko) 2015-11-25

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ID=51535727

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020157029032A Withdrawn KR20150132362A (ko) 2013-03-15 2014-03-14 Pcsk9의 소분자 조절물질 및 그것의 사용 방법

Country Status (10)

Country Link
US (1) US20160031935A1 (OSRAM)
EP (1) EP2961765A4 (OSRAM)
JP (1) JP2016511274A (OSRAM)
KR (1) KR20150132362A (OSRAM)
CN (1) CN105431447A (OSRAM)
AU (1) AU2014231330A1 (OSRAM)
BR (1) BR112015023761A2 (OSRAM)
CA (1) CA2905237A1 (OSRAM)
HK (1) HK1222864A1 (OSRAM)
WO (1) WO2014139008A1 (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016001485A1 (en) 2014-06-30 2016-01-07 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
WO2016029037A1 (en) 2014-08-21 2016-02-25 Srx Cardio, Llc Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(pcsk9) protein activity
US20170290806A1 (en) * 2014-09-08 2017-10-12 Temple University-Of The Commonwealth System Of Higher Education PCSK9 Inhibitors and Methods of Use Thereof
JP6869894B2 (ja) * 2015-03-20 2021-05-12 オーフス ウニベルシテット リポタンパク質代謝障害の治療のためのｐｃｓｋ９阻害剤
PL3464336T3 (pl) 2016-06-01 2022-05-16 Athira Pharma, Inc. Związki
WO2017220701A1 (en) 2016-06-24 2017-12-28 F. Hoffmann-La Roche Ag Compositions and methods for treating cardiovascular disease
GB2567210B (en) 2017-10-06 2020-01-15 Rolls Royce Plc A bladed disk
CN109096247A (zh) * 2018-08-15 2018-12-28 上海罕道医药科技有限公司 一种3h双吖丙啶基双取代吡啶衍生物的制备方法
EP4470609A3 (en) 2019-01-18 2025-03-12 Astrazeneca AB Pcsk9 inhibitors and methods of use thereof
LV15544A (lv) * 2019-07-01 2021-01-20 Latvijas Organiskās Sintēzes Institūts Jauni borskābi saturoši peptidomimētiķi kā malārijas serīna proteāzes inhibitori
WO2024163598A2 (en) * 2023-01-31 2024-08-08 Brandeis University Peptides comprising thioester groups, including depsipeptide thioesters, methods of making, and use thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6180586B1 (en) * 1996-09-24 2001-01-30 The Procter & Gamble Company Liquid laundry detergent compositions containing proteolytic enzyme and protease inhibitors
GB9623908D0 (en) * 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
US6358491B1 (en) * 1999-08-27 2002-03-19 Berlex Laboratories, Inc. Somatostatin analogs
EP2204181A3 (en) * 2002-04-30 2010-09-22 Trustees Of Tufts College Protease inhibitors
US20100233177A1 (en) * 2007-04-13 2010-09-16 David Langdon Yowe Molecules and methods for modulating proprotein convertase subtilisin/kexin type 9 (pcsk9)
AR079344A1 (es) * 2009-12-22 2012-01-18 Lilly Co Eli Analogo peptidico de oxintomodulina, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para tratar diabetes no insulinodependiente y/u obesidad
AU2011223795B2 (en) * 2010-03-01 2015-11-05 Onyx Therapeutics, Inc. Compounds for immunoproteasome inhibition
MX357561B (es) * 2012-02-16 2018-07-13 Rqx Pharmaceuticals Inc Antibióticos peptídicos lineales.

Also Published As

Publication number Publication date
EP2961765A1 (en) 2016-01-06
CA2905237A1 (en) 2014-09-18
JP2016511274A (ja) 2016-04-14
CN105431447A (zh) 2016-03-23
HK1222864A1 (zh) 2017-07-14
US20160031935A1 (en) 2016-02-04
WO2014139008A1 (en) 2014-09-18
BR112015023761A2 (pt) 2017-07-18
AU2014231330A1 (en) 2015-10-01
EP2961765A4 (en) 2016-11-09

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PA0105 International application

Patent event date: 20151013

Patent event code: PA01051R01D

Comment text: International Patent Application

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WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid