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 (https=
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 (https=) 2017-04-20

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ID=51535727

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

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
EP3160513B1 (en) 2014-06-30 2020-02-12 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
EP3973958A3 (en) * 2015-03-20 2022-06-22 Aarhus Universitet Inhibitors of pcsk9 for treatment of lipoprotein metabolism disorders
EP4067368A1 (en) 2016-06-01 2022-10-05 Athira Pharma, Inc. Compounds
BR112018076242A2 (pt) 2016-06-24 2019-03-26 Hoffmann La Roche inibidores de pcsk9, pcsk9 inibido, composição farmacêutica, métodos para modular a atividade de pcsk9, para inibir a ligação de pcsk9 a ldlr, para aumentar a disponibilidade de ldlr, para reduzir um nível de ldl-c, para reduzir o nível sérico de ldl-c, para o tratamento de um distúrbio relacionado com colesterol, métodos para o tratamento de um distúrbio associado a um nível anormal de ldl-c, de uma condição associada a um nível elevado de ldl-c, de dislipidemia, de hipercolesterolemia, usos de um inibidor de pcsk9 e método para identificar um composto candidato como um inibidor de pcsk9 que liga um epítopo da seq id nº 1
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
SG11202107614PA (en) 2019-01-18 2021-08-30 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

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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998013461A1 (en) * 1996-09-24 1998-04-02 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
AU2003228793B2 (en) * 2002-04-30 2008-01-03 Trustees Of Tufts College Smart Pro-Drugs of Serine Protease Inhibitors
CN101679527A (zh) * 2007-04-13 2010-03-24 诺瓦提斯公司 用于调节前蛋白转化酶枯草杆菌蛋白酶/kexin9型(pcsk9)的分子和方法
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
CA2791651C (en) * 2010-03-01 2019-08-20 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
EP2961765A4 (en) 2016-11-09
AU2014231330A1 (en) 2015-10-01
CA2905237A1 (en) 2014-09-18
HK1222864A1 (zh) 2017-07-14
CN105431447A (zh) 2016-03-23
KR20150132362A (ko) 2015-11-25
BR112015023761A2 (pt) 2017-07-18
WO2014139008A1 (en) 2014-09-18
US20160031935A1 (en) 2016-02-04
EP2961765A1 (en) 2016-01-06

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