CA2678941C - Triazole macrocycle systems - Google Patents

Triazole macrocycle systems Download PDF

Info

Publication number
CA2678941C
CA2678941C CA2678941A CA2678941A CA2678941C CA 2678941 C CA2678941 C CA 2678941C CA 2678941 A CA2678941 A CA 2678941A CA 2678941 A CA2678941 A CA 2678941A CA 2678941 C CA2678941 C CA 2678941C
Authority
CA
Canada
Prior art keywords
independently
macrocycle
peptidomimetic macrocycle
alkyl
peptidomimetic
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CA2678941A
Other languages
English (en)
French (fr)
Other versions
CA2678941A1 (en
Inventor
Huw M. Nash
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Rein Therapeutics Inc
Original Assignee
Aileron Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Aileron Therapeutics Inc filed Critical Aileron Therapeutics Inc
Publication of CA2678941A1 publication Critical patent/CA2678941A1/en
Application granted granted Critical
Publication of CA2678941C publication Critical patent/CA2678941C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/006General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length of peptides containing derivatised side chain amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1075General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of amino acids or peptide residues
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/113General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4748Tumour specific antigens; Tumour rejection antigen precursors [TRAP], e.g. MAGE
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K4/00Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/08Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18Fluorenes; Hydrogenated fluorenes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CA2678941A 2007-02-23 2008-02-25 Triazole macrocycle systems Expired - Fee Related CA2678941C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US90307307P 2007-02-23 2007-02-23
US60/903,073 2007-02-23
PCT/US2008/054922 WO2008104000A2 (en) 2007-02-23 2008-02-25 Triazole macrocycle systems

Publications (2)

Publication Number Publication Date
CA2678941A1 CA2678941A1 (en) 2008-08-28
CA2678941C true CA2678941C (en) 2018-11-27

Family

ID=39710801

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2678941A Expired - Fee Related CA2678941C (en) 2007-02-23 2008-02-25 Triazole macrocycle systems

Country Status (10)

Country Link
US (6) US7981999B2 (cg-RX-API-DMAC7.html)
EP (4) EP3301108A1 (cg-RX-API-DMAC7.html)
JP (2) JP4997293B2 (cg-RX-API-DMAC7.html)
CN (3) CN109627287A (cg-RX-API-DMAC7.html)
AU (1) AU2008218116B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0807578A2 (cg-RX-API-DMAC7.html)
CA (1) CA2678941C (cg-RX-API-DMAC7.html)
ES (3) ES2649941T3 (cg-RX-API-DMAC7.html)
IL (2) IL200532A (cg-RX-API-DMAC7.html)
WO (1) WO2008104000A2 (cg-RX-API-DMAC7.html)

Families Citing this family (74)

* Cited by examiner, † Cited by third party
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
CA2830063C (en) * 2003-11-05 2017-10-31 Dana-Farber Cancer Institute, Inc. Stabilized alpha helical peptides and uses thereof
WO2005118620A2 (en) 2004-05-27 2005-12-15 New York University Methods for preparing internally constraied peptides and peptidomimetics
AU2007319193A1 (en) 2006-11-15 2008-05-22 Dana-Farber Cancer Institute, Inc. Stabilized MAML peptides and uses thereof
BRPI0720306A2 (pt) * 2006-12-14 2014-02-04 Aileron Therapeutics Inc Sistemas de macrociclização da bis-sufidrila
US7981998B2 (en) * 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
CA2677045C (en) 2007-01-31 2016-10-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
CA2678941C (en) 2007-02-23 2018-11-27 Aileron Therapeutics, Inc. Triazole macrocycle systems
KR20160061439A (ko) * 2007-03-28 2016-05-31 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
JP5883220B2 (ja) * 2007-05-02 2016-03-09 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド 細胞のホメオスタシス経路および細胞の生存を調節する方法
JP5653219B2 (ja) * 2007-12-31 2015-01-14 ニューヨーク ユニバーシティ 水素結合サロゲートをベースとする人工ヘリックスによるウイルス宿主膜融合の制御
JP2011511076A (ja) * 2008-02-08 2011-04-07 エイルロン セラピューティクス,インコーポレイテッド 治療用ペプチド模倣大環状分子
AU2014201269B2 (en) * 2008-02-08 2016-09-15 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles
WO2009126292A2 (en) * 2008-04-08 2009-10-15 Aileron Therapeutics, Inc. Biologically active peptidomimetic macrocycles
US20110144303A1 (en) * 2008-04-08 2011-06-16 Aileron Therapeutics, Inc. Biologically Active Peptidomimetic Macrocycles
WO2009149214A2 (en) * 2008-06-03 2009-12-10 Aileron Therapeutics, Inc. Compositions and methods for enhancing cellular transport of biomolecules
US20110144306A1 (en) * 2008-07-23 2011-06-16 President And Fellows Of Harvard College Ligation of stapled polypeptides
WO2010033617A2 (en) * 2008-09-16 2010-03-25 The Research Foundation Of State University Of New York Stapled peptides and method of synthesis
BRPI0918833A2 (pt) * 2008-09-22 2015-12-08 Aileron Therapeutics Inc macrociclos peptidomiméticos
US9206223B2 (en) 2008-09-22 2015-12-08 Aileron Therapeutics, Inc. Methods for preparing purified polypeptide compositions
EP2331567A1 (en) * 2008-09-22 2011-06-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034034A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
BRPI0920889A2 (pt) * 2008-09-22 2017-10-10 Aileron Therapeutics Inc macrociclos peptidomiméticos.
WO2010034026A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
BRPI0920899A2 (pt) 2008-11-24 2016-04-26 Aileron Therapeutics Inc macrociclos peptidomiméticos com propriedades melhoradas
BRPI1006139A2 (pt) 2009-01-14 2017-05-30 Aileron Therapeutics Inc macrociclos peptidomiméticos
ES2684169T3 (es) * 2009-01-23 2018-10-01 Pacific Scientific Energetic Materials Company Preparación de un explosivo primario exento de plomo
US8653036B2 (en) 2009-02-27 2014-02-18 Mimetogen Pharmaceuticals Inc. Methods of treating retinitis pigmentosa
JP2012532929A (ja) 2009-07-13 2012-12-20 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二機能性のステープリングされたポリペプチドおよびそれらの使用
US20130072439A1 (en) 2009-09-22 2013-03-21 Huw M. Nash Peptidomimetic macrocycles
US20110223149A1 (en) * 2009-10-14 2011-09-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2780142C (en) 2009-11-16 2018-07-17 Centre National De La Recherche Scientifique - Cnrs Compounds and methods for purifying peptides produced by solid phase peptide synthesis
US9227995B2 (en) * 2010-04-23 2016-01-05 Øyvind Jacobsen Peptides
MX355543B (es) 2010-08-13 2018-04-20 Aileron Therapeutics Inc Star Macrociclos peptidomiméticos.
US8957026B2 (en) 2010-09-22 2015-02-17 President And Fellows Of Harvard College Beta-catenin targeting peptides and uses thereof
EP2627662B1 (en) 2010-10-13 2015-09-16 Bristol-Myers Squibb Company Methods for preparing macrocycles and macrocycle stabilized peptides
FR2967072B1 (fr) 2010-11-05 2013-03-29 Univ Dundee Procede pour ameliorer la production de virus et semences vaccinales influenza
US10822374B2 (en) 2010-11-12 2020-11-03 Dana-Farber Cancer Institute, Inc. Cancer therapies and diagnostics
US9029332B2 (en) 2010-12-15 2015-05-12 The Research Foundation For The State University Of New York Cross-linked peptides and proteins, methods of making same, and uses thereof
WO2012173846A2 (en) * 2011-06-06 2012-12-20 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2012174423A1 (en) 2011-06-17 2012-12-20 President And Fellows Of Harvard College Stabilized polypeptides as regulators of rab gtpase function
RU2639523C2 (ru) 2011-10-18 2017-12-21 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы и их применение
WO2013062923A1 (en) * 2011-10-28 2013-05-02 Merck Sharp & Dohme Corp. MACROCYCLES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF
WO2013071039A1 (en) * 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
US9284283B2 (en) 2012-02-02 2016-03-15 Ensemble Therapeutics Corporation Macrocyclic compounds for modulating IL-17
HK1205454A1 (en) * 2012-02-15 2015-12-18 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
JP6450191B2 (ja) * 2012-02-15 2019-01-09 エイルロン セラピューティクス,インコーポレイテッド ペプチドミメティック大環状化合物
US9278984B2 (en) 2012-08-08 2016-03-08 Pacific Scientific Energetic Materials Company Method for preparation of a lead-free primary explosive
DK2920197T3 (da) 2012-09-26 2021-05-31 Harvard College Prolinlåste sammenhæftede peptider og anvendelser deraf
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
MX373639B (es) 2012-12-20 2020-05-04 Merck Sharp & Dohme Imidazopiridinas sustituidas como inhibidores de doble minuto 2 humana.
WO2014138429A2 (en) 2013-03-06 2014-09-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating hif1alpha
BR112015022872A2 (pt) 2013-03-13 2017-11-07 Harvard College polipeptídeos grampeados e costurados, seu uso, seu método de preparação, composição que os compreende e aminoácido
WO2014201370A1 (en) 2013-06-14 2014-12-18 President And Fellows Of Harvard College Stabilized polypeptide insulin receptor modulators
JP6822839B2 (ja) 2013-09-13 2021-01-27 ザ・スクリップス・リサーチ・インスティテュート 修飾された治療剤、及びその組成物
BR112016009443A8 (pt) * 2013-10-28 2020-03-24 Naurex Inc moduladores do receptor de nmda, pró-drogas e seus sais
CA2933701C (en) 2013-12-18 2022-05-31 The California Institute For Biomedical Research Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof
AU2015264122B2 (en) 2014-05-21 2021-02-04 President And Fellows Of Harvard College Ras inhibitory peptides and uses thereof
CN107108694B (zh) * 2014-09-11 2022-05-03 西雅图基因公司 含叔胺药物物质的靶向递送
SG11201702223UA (en) * 2014-09-24 2017-04-27 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
WO2016049355A1 (en) 2014-09-24 2016-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
EP3294318A4 (en) 2015-03-20 2019-04-03 Aileron Therapeutics, Inc. PEPTIDOMIMETIC MACROCYCLES AND USES THEREOF
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP2018528217A (ja) 2015-09-10 2018-09-27 エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. Mcl−1のモジュレーターとしてのペプチド模倣大環状分子
CA3006000A1 (en) 2015-12-04 2017-06-08 Seattle Genetics, Inc. Conjugates of quaternized tubulysin compounds
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
US20170360881A1 (en) * 2016-06-17 2017-12-21 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US11198715B2 (en) 2016-07-22 2021-12-14 Massachusetts Institute Of Technology Selective Bfl-1 peptides
WO2018061509A1 (ja) * 2016-09-30 2018-04-05 富士フイルム株式会社 環状ペプチド、アフィニティクロマトグラフィー担体、標識化抗体、抗体薬物複合体および医薬製剤
MA50124A (fr) 2017-09-08 2020-07-15 Seattle Genetics Inc Procédé de préparation de tubulysines et d'intermédiaires de celles-ci
CN112119085B (zh) 2017-12-15 2025-04-01 丹娜-法伯癌症研究院有限公司 稳定肽-介导的靶向蛋白降解
US11091522B2 (en) 2018-07-23 2021-08-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
EP3852783A1 (en) * 2018-09-17 2021-07-28 Massachusetts Institute of Technology Peptides selective for bcl-2 family proteins
JP2024522196A (ja) 2021-06-09 2024-06-11 ザ スクリプス リサーチ インスティテュート 長時間作用型デュアルgip/glp-1ペプチドコンジュゲートおよび使用方法

Family Cites Families (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4000259A (en) 1975-06-16 1976-12-28 American Home Products Corporation Cyclic dodecapeptide analogs of somatostatin and intermediates
US4438270A (en) 1977-07-11 1984-03-20 Merrell Toraude Et Compagnie α-Halomethyl derivatives of α-amino acids
US4191754A (en) 1979-02-28 1980-03-04 Merck & Co., Inc. Bicyclic somatostatin analogs
AU3439589A (en) 1988-03-24 1989-10-16 Terrapin Diagnostics, Inc. Molecular sticks for controlling protein conformation
US5650133A (en) 1990-01-19 1997-07-22 Nycomed Salutar Macrocyclic polyaza dichelates linked through ring nitrogens via an amide or ester functionality
CA2047042A1 (en) 1990-07-19 1992-01-20 John Hannah Cyclic hiv principal neutralizing determinant peptides
US5364851A (en) 1991-06-14 1994-11-15 International Synthecon, Llc Conformationally restricted biologically active peptides, methods for their production and uses thereof
GB9114949D0 (en) 1991-07-11 1991-08-28 Smithkline Beecham Plc Novel compounds
US5411860A (en) 1992-04-07 1995-05-02 The Johns Hopkins University Amplification of human MDM2 gene in human tumors
CA2161108A1 (en) 1993-04-23 1994-11-10 Herbert J. Evans Polypeptides that include conformation-constraining groups which flank a protein-protein interaction site
US5446128A (en) 1993-06-18 1995-08-29 The Board Of Trustees Of The University Of Illinois Alpha-helix mimetics and methods relating thereto
US5622852A (en) 1994-10-31 1997-04-22 Washington University Bcl-x/Bcl-2 associated cell death regulator
US6287787B1 (en) * 1993-11-24 2001-09-11 Torrey Pines Institute For Molecular Studies Dimeric oligopeptide mixture sets
US5824483A (en) 1994-05-18 1998-10-20 Pence Inc. Conformationally-restricted combinatiorial library composition and method
US5770377A (en) 1994-07-20 1998-06-23 University Of Dundee Interruption of binding of MDM2 and P53 protein and therapeutic application thereof
US6169073B1 (en) 1995-02-16 2001-01-02 Bayer Corporation Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function
US5675001A (en) 1995-03-14 1997-10-07 Hoffman/Barrett, L.L.C. Heteroatom-functionalized porphyrazines and multimetallic complexes and polymers derived therefrom
DE69521815T2 (de) 1995-05-04 2002-04-04 The Scripps Research Institute, La Jolla Proteinsynthese mittels nativer chemischer ligation (07.01.97)
US5811515A (en) 1995-06-12 1998-09-22 California Institute Of Technology Synthesis of conformationally restricted amino acids, peptides, and peptidomimetics by catalytic ring closing metathesis
US5840833A (en) 1995-10-27 1998-11-24 Molecumetics, Ltd Alpha-helix mimetics and methods relating thereto
US5849954A (en) * 1996-01-18 1998-12-15 Research Corporation Technologies, Inc. Method of peptide synthesis
US5849691A (en) 1996-02-20 1998-12-15 The United States Of America As Represented By The Department Of Health And Human Services Peptidomimetic inhibitors of cathepsin D and plasmepsins I and II
US5817752A (en) 1996-06-06 1998-10-06 La Jolla Pharmaceutical Company Cyclic polypeptides comprising a thioether linkage and methods for their preparation
US5663316A (en) 1996-06-18 1997-09-02 Clontech Laboratories, Inc. BBC6 gene for regulation of cell death
US7083983B2 (en) 1996-07-05 2006-08-01 Cancer Research Campaign Technology Limited Inhibitors of the interaction between P53 and MDM2
US5955593A (en) 1996-09-09 1999-09-21 Washington University BH3 interacting domain death agonist
US5965703A (en) 1996-09-20 1999-10-12 Idun Pharmaceuticals Human bad polypeptides, encoding nucleic acids and methods of use
US5856445A (en) 1996-10-18 1999-01-05 Washington University Serine substituted mutants of BCL-XL /BCL-2 associated cell death regulator
US6271198B1 (en) 1996-11-06 2001-08-07 Genentech, Inc. Constrained helical peptides and methods of making same
JP2002506423A (ja) 1997-04-11 2002-02-26 イーライ・リリー・アンド・カンパニー ペプチド模倣型大員環のコンビナトリアルライブラリーとそのための方法
US7064193B1 (en) 1997-09-17 2006-06-20 The Walter And Eliza Hall Institute Of Medical Research Therapeutic molecules
US6326354B1 (en) 1998-08-19 2001-12-04 Washington University Modulation of apoptosis with bid
WO2000052210A2 (en) 1999-03-01 2000-09-08 Variagenics, Inc. Methods for targeting rna molecules
TR200102765T2 (tr) 1999-03-29 2002-05-21 The Procter & Gamble Company Melanokortin reseptör ligandları
US6713280B1 (en) 1999-04-07 2004-03-30 Thomas Jefferson University Enhancement of peptide cellular uptake
US7192713B1 (en) 1999-05-18 2007-03-20 President And Fellows Of Harvard College Stabilized compounds having secondary structure motifs
DE10009341A1 (de) * 2000-02-22 2001-09-06 Florian Kern Verfahren zur antigen-spezifischen Stimulation von T-Lymphozyten
WO2002013833A2 (en) 2000-08-16 2002-02-21 Georgetown University Medical Center SMALL MOLECULE INHIBITORS TARGETED AT Bcl-2
AU2002252246A1 (en) 2001-03-09 2002-09-24 University Of Louisville Helicomimetics and stabilized lxxll peptidomimetics
US20040106548A1 (en) 2001-09-07 2004-06-03 Schmidt Michelle A Conformationally constrained labeled peptides for imaging and therapy
US7247700B2 (en) 2001-12-31 2007-07-24 Dana Farber Cancer Institute, Inc. BID polypeptides and methods of inducing apoptosis
WO2003059933A2 (en) 2002-01-03 2003-07-24 Yissum Research Development Company Of The Hebrew University Of Jerusalem Conformationally constrained c-backbone cyclic peptides
AU2003211093A1 (en) 2002-02-15 2003-09-09 The Regents Of The University Of Michigan Inhibitors of rgs proteins
US20030166138A1 (en) * 2002-02-21 2003-09-04 Todd Kinsella Cyclic peptides and analogs useful to treat allergies
CA2487424C (en) 2002-05-30 2011-01-04 The Scripps Research Institute Copper-catalysed ligation of azides and acetylenes
JPWO2004022766A1 (ja) 2002-09-06 2005-12-22 株式会社カネカ L−α−メチルシステイン誘導体の製造方法
JP2006516383A (ja) 2002-09-09 2006-07-06 デイナ−ファーバー キャンサー インスティチュート,インコーポレイテッド Bh3ペプチドおよびその使用方法
ES2436296T3 (es) 2002-11-07 2013-12-30 Kosan Biosciences Incorporated Trans-9,10-dehidroepotilona C y trans-9,10-dehidroepotilona D, sus análogos y procedimientos de fabricación de las mismas
WO2004058804A1 (en) 2002-12-24 2004-07-15 Walter And Eliza Hall Institute Of Medical Research Peptides and therapeutic uses thereof
EP1452868A2 (en) 2003-02-27 2004-09-01 Pepscan Systems B.V. Method for selecting a candidate drug compound
AU2003902743A0 (en) 2003-06-02 2003-06-19 Promics Pty Limited Process for the preparation of cyclic peptides
WO2005007675A2 (en) * 2003-07-09 2005-01-27 The Scripps Research Institute TRIAZOLE ϵ-AMINO ACIDS
GB0317815D0 (en) 2003-07-30 2003-09-03 Amersham Health As Imaging agents
CN1859904A (zh) * 2003-10-03 2006-11-08 默克公司 用于治疗阿尔茨海默氏病的苄醚和苄氨基β-分泌酶抑制剂
JP2007537989A (ja) 2003-10-16 2007-12-27 アプラーゲン ゲゼルシャフト ミット ベシュレンクテル ハフツング 安定化ペプチド
CA2830063C (en) 2003-11-05 2017-10-31 Dana-Farber Cancer Institute, Inc. Stabilized alpha helical peptides and uses thereof
EP1737884B1 (en) 2004-03-19 2016-10-19 The University Of Queensland Alpha helical mimics, their uses and methods for their production
WO2005118620A2 (en) 2004-05-27 2005-12-15 New York University Methods for preparing internally constraied peptides and peptidomimetics
CN100335467C (zh) 2004-06-04 2007-09-05 中国科学院上海有机化学研究所 一锅法区域选择性合成5-碘代-1,4-二取代-1,2,3-三氮唑化合物
EP1602663A1 (en) * 2004-06-04 2005-12-07 Chiralix B.V. Triazole-linked glycoamino acids and glycopeptides
MX2007005176A (es) 2004-10-29 2007-06-25 Schering Corp 5-carboxiamida pirazoles y [1,2,4]triazoles sustituidos como agentes antivirales.
CA2595902C (en) 2005-01-24 2017-08-22 Pepscan Systems B.V. Binding compounds, immunogenic compounds and peptidomimetics of the beta-3 hairpin loop of cystine-knot growth factors
US20070020620A1 (en) * 2005-07-14 2007-01-25 Finn M G Compositions and methods for coupling a plurality of compounds to a scaffold
WO2008033557A2 (en) * 2006-09-15 2008-03-20 Siemens Medical Solutions Usa, Inc. Click chemistry-derived cyclic peptidomimetics as integrin markers
AU2007319193A1 (en) 2006-11-15 2008-05-22 Dana-Farber Cancer Institute, Inc. Stabilized MAML peptides and uses thereof
BRPI0720306A2 (pt) 2006-12-14 2014-02-04 Aileron Therapeutics Inc Sistemas de macrociclização da bis-sufidrila
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
CA2677045C (en) 2007-01-31 2016-10-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
CA2678941C (en) 2007-02-23 2018-11-27 Aileron Therapeutics, Inc. Triazole macrocycle systems
KR20160061439A (ko) 2007-03-28 2016-05-31 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
JP5883220B2 (ja) 2007-05-02 2016-03-09 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド 細胞のホメオスタシス経路および細胞の生存を調節する方法
JP5653219B2 (ja) 2007-12-31 2015-01-14 ニューヨーク ユニバーシティ 水素結合サロゲートをベースとする人工ヘリックスによるウイルス宿主膜融合の制御
DK2235064T3 (en) 2008-01-07 2016-01-11 Amgen Inc A process for the preparation of heterodimeric Fc molecules using electrostatic control effects
JP2011511076A (ja) * 2008-02-08 2011-04-07 エイルロン セラピューティクス,インコーポレイテッド 治療用ペプチド模倣大環状分子
WO2009126292A2 (en) 2008-04-08 2009-10-15 Aileron Therapeutics, Inc. Biologically active peptidomimetic macrocycles
US20110144303A1 (en) 2008-04-08 2011-06-16 Aileron Therapeutics, Inc. Biologically Active Peptidomimetic Macrocycles
WO2009149214A2 (en) 2008-06-03 2009-12-10 Aileron Therapeutics, Inc. Compositions and methods for enhancing cellular transport of biomolecules
US20110144306A1 (en) 2008-07-23 2011-06-16 President And Fellows Of Harvard College Ligation of stapled polypeptides
EP2344520B1 (en) 2008-09-18 2013-11-13 New York University Inhibiting interaction between hif-1a and p300/cbp with hydrogen bond surrogate-based helices
BRPI0920889A2 (pt) 2008-09-22 2017-10-10 Aileron Therapeutics Inc macrociclos peptidomiméticos.
WO2010034034A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
BRPI0918833A2 (pt) 2008-09-22 2015-12-08 Aileron Therapeutics Inc macrociclos peptidomiméticos
EP2331567A1 (en) 2008-09-22 2011-06-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034026A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9206223B2 (en) 2008-09-22 2015-12-08 Aileron Therapeutics, Inc. Methods for preparing purified polypeptide compositions
BRPI0920899A2 (pt) 2008-11-24 2016-04-26 Aileron Therapeutics Inc macrociclos peptidomiméticos com propriedades melhoradas
BRPI1006139A2 (pt) 2009-01-14 2017-05-30 Aileron Therapeutics Inc macrociclos peptidomiméticos
JP2012532929A (ja) 2009-07-13 2012-12-20 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二機能性のステープリングされたポリペプチドおよびそれらの使用
US20130072439A1 (en) 2009-09-22 2013-03-21 Huw M. Nash Peptidomimetic macrocycles
US20110223149A1 (en) 2009-10-14 2011-09-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
MX355543B (es) 2010-08-13 2018-04-20 Aileron Therapeutics Inc Star Macrociclos peptidomiméticos.
CA2828889A1 (en) 2011-03-04 2012-09-13 New York University Hydrogen bond surrogate macrocycles as modulators of ras
WO2012173846A2 (en) 2011-06-06 2012-12-20 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20130123196A1 (en) 2011-08-31 2013-05-16 New York University Thioether-, ether-, and alkylamine-linked hydrogen bond surrogate peptidomimetics
RU2639523C2 (ru) 2011-10-18 2017-12-21 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы и их применение
WO2013059530A2 (en) 2011-10-18 2013-04-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
HK1205454A1 (en) 2012-02-15 2015-12-18 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
JP6450191B2 (ja) 2012-02-15 2019-01-09 エイルロン セラピューティクス,インコーポレイテッド ペプチドミメティック大環状化合物
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
WO2014138429A2 (en) 2013-03-06 2014-09-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating hif1alpha
WO2015157508A1 (en) 2014-04-09 2015-10-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles with pth activity
WO2016049355A1 (en) 2014-09-24 2016-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
SG11201702223UA (en) 2014-09-24 2017-04-27 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof
EP3294318A4 (en) 2015-03-20 2019-04-03 Aileron Therapeutics, Inc. PEPTIDOMIMETIC MACROCYCLES AND USES THEREOF
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
MX2017016251A (es) 2015-07-02 2018-04-20 Dana Farber Cancer Inst Inc Peptidos anti-microbianos estabilizados.
WO2017023933A2 (en) 2015-08-03 2017-02-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP6971970B2 (ja) 2015-09-03 2021-11-24 エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics, Inc. ペプチド模倣大環状分子およびその使用
JP2018528217A (ja) 2015-09-10 2018-09-27 エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. Mcl−1のモジュレーターとしてのペプチド模倣大環状分子
JP2019520304A (ja) 2016-03-21 2019-07-18 エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. ペプチド模倣大環状分子に関するコンパニオン診断ツール
WO2017205786A1 (en) 2016-05-27 2017-11-30 Aileron Therapeutics, Inc. Cell permeable peptidomimetic macrocycles
US20170360881A1 (en) 2016-06-17 2017-12-21 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof

Also Published As

Publication number Publication date
CN104086641A (zh) 2014-10-08
JP6046686B2 (ja) 2016-12-21
US8637686B2 (en) 2014-01-28
US9023988B2 (en) 2015-05-05
JP2015107966A (ja) 2015-06-11
IL241729A (en) 2017-09-28
US9493509B2 (en) 2016-11-15
EP2114428A4 (en) 2010-03-31
US10030049B2 (en) 2018-07-24
ES2649941T3 (es) 2018-01-16
ES2648687T3 (es) 2018-01-05
CN101663044B (zh) 2014-07-23
AU2008218116A1 (en) 2008-08-28
CN109627287A (zh) 2019-04-16
EP2564863A3 (en) 2013-07-03
IL200532A (en) 2015-10-29
EP2114428B1 (en) 2012-10-31
US20110263815A1 (en) 2011-10-27
EP2564862A3 (en) 2013-07-10
EP2564862B1 (en) 2017-08-02
ES2398310T3 (es) 2013-03-15
US20120190818A1 (en) 2012-07-26
EP2564863B1 (en) 2017-08-23
WO2008104000A3 (en) 2008-11-27
EP3301108A1 (en) 2018-04-04
US9957296B2 (en) 2018-05-01
JP5657594B2 (ja) 2015-01-21
JP4997293B2 (ja) 2012-08-08
IL241729A0 (en) 2015-11-30
AU2008218116B2 (en) 2012-04-05
US20160289274A1 (en) 2016-10-06
US20080262200A1 (en) 2008-10-23
US20160304564A1 (en) 2016-10-20
BRPI0807578A2 (pt) 2021-06-15
JP2012144555A (ja) 2012-08-02
CA2678941A1 (en) 2008-08-28
EP2564862A2 (en) 2013-03-06
US20160031936A1 (en) 2016-02-04
EP2114428A2 (en) 2009-11-11
WO2008104000A2 (en) 2008-08-28
CN101663044A (zh) 2010-03-03
IL200532A0 (en) 2010-04-29
JP2010519318A (ja) 2010-06-03
US7981999B2 (en) 2011-07-19
EP2564863A2 (en) 2013-03-06

Similar Documents

Publication Publication Date Title
CA2678941C (en) Triazole macrocycle systems
EP2342222B1 (en) Peptidomimetic macrocycles
US9394336B2 (en) Methods for preparing purified polypeptide compositions
AU2016216698A1 (en) Peptidomimetic macrocycles with improved properties
WO2008076904A9 (en) Bis-sulfhydryl macrocyclization systems
EP2488193A1 (en) Improved peptidomimetic macrocycles
EP2310407A2 (en) Biologically active peptidomimetic macrocycles
AU2012203906A1 (en) Triazole macrocycle systems
AU2017201310A1 (en) Bis-sulfhydryl macrocyclization systems

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20130213

MKLA Lapsed

Effective date: 20210831

MKLA Lapsed

Effective date: 20200225