JP2016511274A - Ｐｃｓｋ９の小分子モジュレータ及びその使用法 - Google Patents

Ｐｃｓｋ９の小分子モジュレータ及びその使用法 Download PDF

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JP2016511274A
JP2016511274A JP2015561865A JP2015561865A JP2016511274A JP 2016511274 A JP2016511274 A JP 2016511274A JP 2015561865 A JP2015561865 A JP 2015561865A JP 2015561865 A JP2015561865 A JP 2015561865A JP 2016511274 A JP2016511274 A JP 2016511274A
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compound
substituted
alkyl
amino
phenyl
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JP2016511274A5 (enExample
Inventor
ダニエル・ゲイ
シェルドン・クレイン
ニコラ・ラシャンス
ジャン−フランソワ・チアソン
ヴォイ・リン・トゥルン
パトリック・ラコーム
キャスリン・スコレイ
ナビル・ジェ・セイダ
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アデイラタ・リミテッド・パートナーシップ
アモールケム・ホールディングス・インコーポレイテッド
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Publication of JP2016511274A publication Critical patent/JP2016511274A/ja
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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
    • C07K5/04—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)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Diabetes (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)
JP2015561865A 2013-03-15 2014-03-14 Ｐｃｓｋ９の小分子モジュレータ及びその使用法 Pending JP2016511274A (ja)

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 (2)

Publication Number Publication Date
JP2016511274A true JP2016511274A (ja) 2016-04-14
JP2016511274A5 JP2016511274A5 (enExample) 2017-04-20

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JP2015561865A Pending JP2016511274A (ja) 2013-03-15 2014-03-14 Ｐｃｓｋ９の小分子モジュレータ及びその使用法

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017528448A (ja) * 2014-08-21 2017-09-28 エスアールエックス カーディオ，エル エル シー プロタンパク質コンバターゼであるスブチリシン／ケキシンタイプ９（ｐｃｓｋ９）のタンパク質活性のモジュレーションのための、結合リガンドとしての小分子の組成物およびその使用方法

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10973920B2 (en) 2014-06-30 2021-04-13 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
US20170290806A1 (en) * 2014-09-08 2017-10-12 Temple University-Of The Commonwealth System Of Higher Education PCSK9 Inhibitors and Methods of Use Thereof
EP3271405A1 (en) * 2015-03-20 2018-01-24 Aarhus Universitet Inhibitors of pcsk9 for treatment of lipoprotein metabolism disorders
SI3464336T1 (sl) 2016-06-01 2022-06-30 Athira Pharma, Inc. Spojine
AU2017281332A1 (en) 2016-06-24 2018-12-20 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
WO2020150473A2 (en) 2019-01-18 2020-07-23 Dogma Therapeutics, Inc. 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

Citations (2)

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Publication number Priority date Publication date Assignee Title
JP2000508344A (ja) * 1996-11-18 2000-07-04 エフ・ホフマン―ラ ロシュ アーゲー 抗ウイルス性ペプチド誘導体
WO2013123456A1 (en) * 2012-02-16 2013-08-22 Rqx Pharmaceuticals, Inc. Linear peptide antibiotics

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US6180586B1 (en) * 1996-09-24 2001-01-30 The Procter & Gamble Company Liquid laundry detergent compositions containing proteolytic enzyme and protease inhibitors
US6358491B1 (en) * 1999-08-27 2002-03-19 Berlex Laboratories, Inc. Somatostatin analogs
US7691967B2 (en) * 2002-04-30 2010-04-06 Trustees Of Tufts College Smart pro-drugs of serine protease inhibitors
AR066042A1 (es) * 2007-04-13 2009-07-22 Novartis Ag Moleculas y metodos para modular la proteina convertasa-subtilisina /quexina tipo 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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000508344A (ja) * 1996-11-18 2000-07-04 エフ・ホフマン―ラ ロシュ アーゲー 抗ウイルス性ペプチド誘導体
WO2013123456A1 (en) * 2012-02-16 2013-08-22 Rqx Pharmaceuticals, Inc. Linear peptide antibiotics

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
AROSIO, M. ET AL.: "LDL physical properties, lipoprotein and Lp(a) levels in acromegalic patients. Effects of octreotide", ATHEROSCLEROSIS, vol. 151, JPN6018005340, 2000, pages 551 - 557, XP000918773, ISSN: 0003740433, DOI: 10.1016/S0021-9150(99)00426-8 *
MORRIS, T. S. ET AL.: "In Vitro and Ex Vivo Inhibition of Hepatitis A Virus 3C Proteinase by a Peptidyl Monofluoromethyl Ke", BIOORAGANIC & MEDICINAL CHEISTRY, vol. 5, no. 5, JPN6018005338, 1997, pages 797 - 807, XP002403563, ISSN: 0003928866 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017528448A (ja) * 2014-08-21 2017-09-28 エスアールエックス カーディオ，エル エル シー プロタンパク質コンバターゼであるスブチリシン／ケキシンタイプ９（ｐｃｓｋ９）のタンパク質活性のモジュレーションのための、結合リガンドとしての小分子の組成物およびその使用方法
US11026957B2 (en) 2014-08-21 2021-06-08 Srx Cardio, Llc Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands
US11771710B2 (en) 2014-08-21 2023-10-03 Srx Cardio, Llc Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands

Also Published As

Publication number Publication date
WO2014139008A1 (en) 2014-09-18
EP2961765A1 (en) 2016-01-06
EP2961765A4 (en) 2016-11-09
BR112015023761A2 (pt) 2017-07-18
CA2905237A1 (en) 2014-09-18
HK1222864A1 (zh) 2017-07-14
US20160031935A1 (en) 2016-02-04
KR20150132362A (ko) 2015-11-25
CN105431447A (zh) 2016-03-23
AU2014231330A1 (en) 2015-10-01

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