JP2014520120A - 安定化した変異型ｍａｍｌペプチドおよびその使用 - Google Patents

安定化した変異型ｍａｍｌペプチドおよびその使用 Download PDF

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Publication number
JP2014520120A
JP2014520120A JP2014516044A JP2014516044A JP2014520120A JP 2014520120 A JP2014520120 A JP 2014520120A JP 2014516044 A JP2014516044 A JP 2014516044A JP 2014516044 A JP2014516044 A JP 2014516044A JP 2014520120 A JP2014520120 A JP 2014520120A
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Japan
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xaa
amino acid
amino acids
modified polypeptide
substituted
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JP2014516044A
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Japanese (ja)
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JP2014520120A5 (enExample
Inventor
アール メラーリング、レイモンド
エル． バーダイン、グレゴリー
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Harvard University
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Harvard University
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • 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
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • 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
    • A61K47/55—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 also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551—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 also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0056—Peptides, proteins, polyamino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Rheumatology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2014516044A 2011-06-17 2012-06-15 安定化した変異型ｍａｍｌペプチドおよびその使用 Pending JP2014520120A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161498477P 2011-06-17 2011-06-17
US61/498,477 2011-06-17
PCT/US2012/042719 WO2012174409A1 (en) 2011-06-17 2012-06-15 Stabilized variant maml peptides and uses thereof

Publications (2)

Publication Number Publication Date
JP2014520120A true JP2014520120A (ja) 2014-08-21
JP2014520120A5 JP2014520120A5 (enExample) 2015-07-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014516044A Pending JP2014520120A (ja) 2011-06-17 2012-06-15 安定化した変異型ｍａｍｌペプチドおよびその使用

Country Status (4)

Country Link
US (1) US20140256912A1 (enExample)
EP (1) EP2721061A4 (enExample)
JP (1) JP2014520120A (enExample)
WO (1) WO2012174409A1 (enExample)

Families Citing this family (28)

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Publication number Priority date Publication date Assignee Title
US7192713B1 (en) 1999-05-18 2007-03-20 President And Fellows Of Harvard College Stabilized compounds having secondary structure motifs
PT2332968T (pt) 2003-11-05 2016-08-17 Harvard College Péptidos alfa-helicoidais adequados para a activação ou inibição da morte celular
EP3159352B1 (en) 2007-03-28 2023-08-02 President and Fellows of Harvard College Stitched polypeptides
WO2010011313A2 (en) 2008-07-23 2010-01-28 President And Fellows Of Harvard College Ligation of stapled polypeptides
JP2012515172A (ja) 2009-01-14 2012-07-05 エルロン・セラピューティクス・インコーポレイテッド ペプチド模倣大環状分子
WO2011008260A2 (en) 2009-07-13 2011-01-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
AU2010298338A1 (en) 2009-09-22 2012-04-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
KR102104762B1 (ko) 2010-08-13 2020-04-24 에일러론 테라퓨틱스 인코포레이티드 펩티도미메틱 거대고리
WO2012174423A1 (en) 2011-06-17 2012-12-20 President And Fellows Of Harvard College Stabilized polypeptides as regulators of rab gtpase function
TW201806968A (zh) 2011-10-18 2018-03-01 艾利倫治療公司 擬肽巨環化合物
CA2864120A1 (en) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
NZ627528A (en) 2012-02-15 2016-05-27 Aileron Therapeutics Inc Peptidomimetic macrocycles
EP2920197B1 (en) 2012-09-26 2021-03-17 President and Fellows of Harvard College Proline-locked stapled peptides and uses thereof
BR112015009470A2 (pt) 2012-11-01 2019-12-17 Aileron Therapeutics Inc aminoácidos dissubstituídos e seus métodos de preparação e uso
EP2991665A4 (en) 2013-03-13 2016-11-09 Harvard College STACKED AND GRAFTED POLYPEPTIDES AND USES THEREOF
US10308926B2 (en) 2013-03-15 2019-06-04 Dana-Farber Cancer Institute, Inc. Stablized EZH2 peptides
KR20160019547A (ko) 2013-06-14 2016-02-19 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 안정화된 폴리펩티드 인슐린 수용체 조절제
CN111620940A (zh) 2014-05-21 2020-09-04 哈佛大学的校长及成员们 Ras抑制肽和其用途
MX389354B (es) 2014-09-24 2025-03-20 Aileron Therapeutics Inc Macrociclos peptidomimeticos y formulaciones de los mismos.
KR20170058424A (ko) 2014-09-24 2017-05-26 에일러론 테라퓨틱스 인코포레이티드 펩티드모방 거대고리 및 이의 용도
SG11201707750YA (en) 2015-03-20 2017-10-30 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
WO2017004548A1 (en) 2015-07-01 2017-01-05 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1
US20190135868A1 (en) * 2016-04-29 2019-05-09 The University Of Chicago Synthetic dna binding domain peptides and uses thereof
KR20200064075A (ko) 2017-09-07 2020-06-05 포그 파마슈티컬스 인코포레이티드 베타-카테닌 기능을 조절하는 제제 및 이의 방법
WO2019136209A1 (en) * 2018-01-05 2019-07-11 President And Fellows Of Harvard College Stabilized polypeptides and uses thereof
CN113039195A (zh) 2018-08-20 2021-06-25 弗格制药有限公司 肽集合、肽试剂及其使用方法
EP4600411A3 (en) 2019-04-09 2025-09-10 The University of Chicago Versatile peptide and protein macrocyclization and multimerization with diels-alder cycloadditions

Citations (3)

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WO2010034034A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034029A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP2010510236A (ja) * 2006-11-15 2010-04-02 ダナ−ファーバー キャンサー インスティテュート インク． 安定化させたｍａｍｌペプチドおよびその使用法

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
JP2010510236A (ja) * 2006-11-15 2010-04-02 ダナ−ファーバー キャンサー インスティテュート インク． 安定化させたｍａｍｌペプチドおよびその使用法
WO2010034034A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034029A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles

Non-Patent Citations (3)

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JPN6016018148; Ｅｕｒｏｐｅａｎ　Ｊｏｕｒｎａｌ　ｏｆ　Ｃａｎｃｅｒ．　Ｓｕｐｐｌｅｍｅｎｔ Ｖｏｌ．８，　Ｎｏ．７, 2010, ｐ．３０ *
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Also Published As

Publication number Publication date
WO2012174409A1 (en) 2012-12-20
EP2721061A1 (en) 2014-04-23
US20140256912A1 (en) 2014-09-11
EP2721061A4 (en) 2014-11-05

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