AU2008218116B2 - Triazole macrocycle systems - Google Patents

Triazole macrocycle systems Download PDF

Info

Publication number
AU2008218116B2
AU2008218116B2 AU2008218116A AU2008218116A AU2008218116B2 AU 2008218116 B2 AU2008218116 B2 AU 2008218116B2 AU 2008218116 A AU2008218116 A AU 2008218116A AU 2008218116 A AU2008218116 A AU 2008218116A AU 2008218116 B2 AU2008218116 B2 AU 2008218116B2
Authority
AU
Australia
Prior art keywords
alkyl
macrocycle
methyl
compound
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.)
Ceased
Application number
AU2008218116A
Other languages
English (en)
Other versions
AU2008218116A1 (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 AU2008218116A1 publication Critical patent/AU2008218116A1/en
Application granted granted Critical
Publication of AU2008218116B2 publication Critical patent/AU2008218116B2/en
Priority to AU2012203906A priority Critical patent/AU2012203906A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters 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
    • C07C271/22—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/006—General 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General 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
    • C07K1/1072—General 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
    • C07K1/1075—General 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General 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
    • C07K1/113—General 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • 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
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4748—Tumour specific antigens; Tumour rejection antigen precursors [TRAP], e.g. MAGE
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K4/00—Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56—Cyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- 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
    • C07C2603/18—Fluorenes; 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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
AU2008218116A 2007-02-23 2008-02-25 Triazole macrocycle systems Ceased AU2008218116B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2012203906A AU2012203906A1 (en) 2007-02-23 2012-07-04 Triazole macrocycle systems

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2012203906A Division AU2012203906A1 (en) 2007-02-23 2012-07-04 Triazole macrocycle systems

Publications (2)

Publication Number Publication Date
AU2008218116A1 AU2008218116A1 (en) 2008-08-28
AU2008218116B2 true AU2008218116B2 (en) 2012-04-05

Family

ID=39710801

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2008218116A Ceased AU2008218116B2 (en) 2007-02-23 2008-02-25 Triazole macrocycle systems

Country Status (10)

Country Link
US (6) US7981999B2 (enExample)
EP (4) EP2564862B1 (enExample)
JP (2) JP4997293B2 (enExample)
CN (3) CN104086641A (enExample)
AU (1) AU2008218116B2 (enExample)
BR (1) BRPI0807578A2 (enExample)
CA (1) CA2678941C (enExample)
ES (3) ES2648687T3 (enExample)
IL (2) IL200532A (enExample)
WO (1) WO2008104000A2 (enExample)

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
CN103467588B (zh) 2003-11-05 2016-12-28 达纳-法伯癌症研究所股份有限公司 稳定的α螺旋肽及其用途
WO2005118620A2 (en) 2004-05-27 2005-12-15 New York University Methods for preparing internally constraied peptides and peptidomimetics
EP2091552A4 (en) 2006-11-15 2010-01-06 Dana Farber Cancer Inst Inc STABILIZED MAML-PEPTIDES AND ITS USES
US7981998B2 (en) * 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
EP3170835A1 (en) * 2006-12-14 2017-05-24 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
EP2564862B1 (en) 2007-02-23 2017-08-02 Aileron Therapeutics, Inc. Substituted amino acids for preparing triazole linked macrocyclic peptides
EP2508531B1 (en) 2007-03-28 2016-10-19 President and Fellows of Harvard College Stitched polypeptides
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
WO2009110952A2 (en) * 2007-12-31 2009-09-11 New York University Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices
AU2014201269B2 (en) * 2008-02-08 2016-09-15 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles
CN104474529A (zh) * 2008-02-08 2015-04-01 爱勒让治疗公司 治疗性的拟肽大环化合物
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
EP2285970A4 (en) * 2008-06-03 2011-10-12 Aileron Therapeutics Inc COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES
WO2010011313A2 (en) 2008-07-23 2010-01-28 President And Fellows Of Harvard College Ligation of stapled polypeptides
EP2334317B1 (en) * 2008-09-16 2017-06-14 The Research Foundation Of State University Of New York Stapled peptides and method of synthesis
CA2737918A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN102482336B (zh) * 2008-09-22 2015-05-06 爱勒让治疗公司 拟肽大环化合物
BRPI0920889A2 (pt) * 2008-09-22 2017-10-10 Aileron Therapeutics Inc macrociclos peptidomiméticos.
CA2737914A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034032A2 (en) 2008-09-22 2010-03-25 Aileron Therapeutic, Inc. Methods for preparing purified polypeptide compositions
EP2342214A1 (en) * 2008-09-22 2011-07-13 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP2012509902A (ja) 2008-11-24 2012-04-26 エルロン・セラピューティクス・インコーポレイテッド 改善された特性を有するペプチド模倣大環状分子
WO2010083347A2 (en) 2009-01-14 2010-07-22 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP5677980B2 (ja) * 2009-01-23 2015-02-25 パシフィック・サイエンティフィック・エナジェティック・マテリアルズ・カンパニー 鉛フリー起爆薬の調合
CN102333537B (zh) * 2009-02-27 2014-08-13 米梅托根药物公司 用于治疗色素性视网膜炎的模拟肽环状化合物
WO2011008260A2 (en) 2009-07-13 2011-01-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
CA2774973A1 (en) 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2777700A1 (en) * 2009-10-14 2011-04-21 Aileron Therapeutics, Inc. Improved peptidomimetic macrocycles
CN102666565B (zh) * 2009-11-16 2016-01-20 国家科学研究中心 用于纯化由固相肽合成法制备的肽的化合物和方法
US9227995B2 (en) * 2010-04-23 2016-01-05 Øyvind Jacobsen Peptides
RU2016111360A (ru) 2010-08-13 2018-11-27 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
US8957026B2 (en) 2010-09-22 2015-02-17 President And Fellows Of Harvard College Beta-catenin targeting peptides and uses thereof
WO2012051405A1 (en) 2010-10-13 2012-04-19 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
AU2011325910B2 (en) 2010-11-12 2016-03-24 Dana Farber Cancer Institute, Inc. Cancer therapies and diagnostics
EP2651964B1 (en) 2010-12-15 2018-02-28 The Research Foundation of 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
CN108929375A (zh) 2011-10-18 2018-12-04 爱勒让治疗公司 拟肽大环化合物
US8987274B2 (en) 2011-10-28 2015-03-24 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
EP2809660B1 (en) 2012-02-02 2016-01-20 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
RU2017145921A (ru) 2012-02-15 2019-02-21 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
US9278984B2 (en) 2012-08-08 2016-03-08 Pacific Scientific Energetic Materials Company Method for preparation of a lead-free primary explosive
EP2920197B1 (en) 2012-09-26 2021-03-17 President and Fellows of Harvard College Proline-locked stapled peptides and uses thereof
CN104812384B (zh) 2012-11-01 2020-09-18 爱勒让治疗公司 二取代的氨基酸及其制备和使用方法
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
WO2014138429A2 (en) 2013-03-06 2014-09-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating hif1alpha
JP6568515B2 (ja) 2013-03-13 2019-08-28 プレジデント アンド フェローズ オブ ハーバード カレッジ ステープルドおよびステッチドポリペプチドならびにその使用
MX2015017274A (es) 2013-06-14 2016-08-04 Harvard College Moduladores del receptor del polipéptido insulina estabilizados.
ES2927607T3 (es) 2013-09-13 2022-11-08 Scripps Research Inst Agentes terapéuticos modificados y composiciones de los mismos
MX378668B (es) * 2013-10-28 2025-03-10 Naurex Inc Profarmacos y moduladores de receptores nmda, sales y usos de estos.
US10039809B2 (en) 2013-12-18 2018-08-07 The California Institute For Biomedical Research Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof
JP6759109B2 (ja) 2014-05-21 2020-09-23 プレジデント アンド フェローズ オブ ハーバード カレッジ Ｒａｓ抑制性ペプチドおよびその使用
PT3900742T (pt) * 2014-09-11 2024-08-21 Seagen Inc Entrega direcionada de fármacos contendo uma amina terciária
JP2017533889A (ja) 2014-09-24 2017-11-16 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
MX389354B (es) 2014-09-24 2025-03-20 Aileron Therapeutics Inc Macrociclos peptidomimeticos y formulaciones de los mismos.
US10253067B2 (en) 2015-03-20 2019-04-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
CN108367043A (zh) 2015-12-04 2018-08-03 西雅图基因公司 季铵化的微管溶素化合物的缀合物
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
BR112019006301A2 (pt) * 2016-09-30 2019-07-30 Fujifilm Corp peptídeo cíclico, suporte de cromatografia de afinidade, anticorpo marcado, conjugado anticorpo - fármaco, e preparação farmacêutica
CN111601803A (zh) 2017-09-08 2020-08-28 西雅图基因公司 微管溶素及其中间体的制备方法
WO2019118893A1 (en) 2017-12-15 2019-06-20 Dana-Farber Cancer Institute, Inc. Stabilized peptide-mediated targeted protein degradation
US11091522B2 (en) 2018-07-23 2021-08-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
WO2020060975A1 (en) * 2018-09-17 2020-03-26 Massachusetts Institute Of Technology Peptides selective for bcl-2 family proteins
IL309067A (en) 2021-06-09 2024-02-01 Scripps Research Inst Long-acting dual gip/glp-1 peptide conjugates and methods of use

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
WO1989009233A1 (en) 1988-03-24 1989-10-05 Terrapin Technologies, 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
CA2286867A1 (en) 1997-04-11 1998-10-22 Eli Lilly And Company Combinatorial libraries of peptidomimetic macrocycles and processes therefor
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
NZ514141A (en) 1999-03-29 2004-01-30 Procter & Gamble Melanocortin receptor ligands
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
US6703382B2 (en) 2000-08-16 2004-03-09 Georgetown University Medical Center Small molecule inhibitors targeted at Bcl-2
WO2002072597A2 (en) 2001-03-09 2002-09-19 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
IL162604A0 (en) 2002-01-03 2005-11-20 Yissum Res Dev Co Conformationally constrained c-backbone cyclic peptides
US7432242B2 (en) 2002-02-15 2008-10-07 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
KR101138643B1 (ko) 2002-05-30 2012-04-26 더 스크립스 리서치 인스티튜트 구리 촉매 작용하에서의 아지드와 아세틸렌과의 리게이션
WO2004022766A1 (ja) 2002-09-06 2004-03-18 Kaneka Corporation Ｌ−αーメチルシステイン誘導体の製造方法
EP1590363A4 (en) 2002-09-09 2006-11-02 Dana Farber Cancer Inst Inc BH3-PEPTIDES AND METHOD FOR THEIR USE
EP2135867B1 (en) * 2002-11-07 2013-09-25 Kosan Biosciences Incorporated Trans-9, 10-dehydroepothilone C and trans-9, 10-dehydroepothilone D, analogs thereof and methods of making the same
US20070032417A1 (en) 2002-12-24 2007-02-08 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
JP4649413B2 (ja) * 2003-10-03 2011-03-09 メルク・シャープ・エンド・ドーム・コーポレイション アルツハイマー病の治療用のベンジルエーテル及びベンジルアミノβ−セクレターゼ阻害薬
WO2005040202A2 (en) 2003-10-16 2005-05-06 Aplagen Gmbh Stabilized alpha-helical peptides
CN103467588B (zh) 2003-11-05 2016-12-28 达纳-法伯癌症研究所股份有限公司 稳定的α螺旋肽及其用途
WO2005090388A1 (en) 2004-03-19 2005-09-29 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
EP1602663A1 (en) * 2004-06-04 2005-12-07 Chiralix B.V. Triazole-linked glycoamino acids and glycopeptides
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
JP4762995B2 (ja) 2004-10-29 2011-08-31 シェーリング コーポレイション 抗ウイルス物質としての置換５−カルボキシアミドピラゾールおよび置換［１，２，４］トリアゾール
PL1844337T3 (pl) 2005-01-24 2013-12-31 Pepscan Systems Bv Związki wiążące, związki immunogenne i peptydomimetyki
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
EP2091552A4 (en) 2006-11-15 2010-01-06 Dana Farber Cancer Inst Inc STABILIZED MAML-PEPTIDES AND ITS USES
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
EP3170835A1 (en) 2006-12-14 2017-05-24 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
EP2564862B1 (en) 2007-02-23 2017-08-02 Aileron Therapeutics, Inc. Substituted amino acids for preparing triazole linked macrocyclic peptides
EP2508531B1 (en) 2007-03-28 2016-10-19 President and Fellows of Harvard College Stitched polypeptides
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
WO2009110952A2 (en) 2007-12-31 2009-09-11 New York University Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices
SI2235064T1 (sl) 2008-01-07 2016-04-29 Amgen Inc. Metoda za izdelavo heterodimernih molekul - protitelesa fc z uporabo elektrostatičnih usmerjevalnih učinkov
CN104474529A (zh) 2008-02-08 2015-04-01 爱勒让治疗公司 治疗性的拟肽大环化合物
US20110144303A1 (en) 2008-04-08 2011-06-16 Aileron Therapeutics, Inc. Biologically Active Peptidomimetic Macrocycles
WO2009126292A2 (en) 2008-04-08 2009-10-15 Aileron Therapeutics, Inc. Biologically active peptidomimetic macrocycles
EP2285970A4 (en) 2008-06-03 2011-10-12 Aileron Therapeutics Inc COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES
WO2010011313A2 (en) 2008-07-23 2010-01-28 President And Fellows Of Harvard College Ligation of stapled polypeptides
JP2012503013A (ja) 2008-09-18 2012-02-02 ニューヨーク ユニバーシティ ＨＩＦ−１αと水素結合代替ヘリックスを有するｐ３００／ＣＢＰの間の相互作用の阻害
BRPI0920889A2 (pt) 2008-09-22 2017-10-10 Aileron Therapeutics Inc macrociclos peptidomiméticos.
CA2737918A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2737914A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
EP2342214A1 (en) 2008-09-22 2011-07-13 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN102482336B (zh) 2008-09-22 2015-05-06 爱勒让治疗公司 拟肽大环化合物
WO2010034032A2 (en) 2008-09-22 2010-03-25 Aileron Therapeutic, Inc. Methods for preparing purified polypeptide compositions
JP2012509902A (ja) 2008-11-24 2012-04-26 エルロン・セラピューティクス・インコーポレイテッド 改善された特性を有するペプチド模倣大環状分子
WO2010083347A2 (en) 2009-01-14 2010-07-22 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2011008260A2 (en) 2009-07-13 2011-01-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
CA2774973A1 (en) 2009-09-22 2011-03-31 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2777700A1 (en) 2009-10-14 2011-04-21 Aileron Therapeutics, Inc. Improved peptidomimetic macrocycles
RU2016111360A (ru) 2010-08-13 2018-11-27 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
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
WO2013033645A1 (en) 2011-08-31 2013-03-07 New York University Thioether-,ether-, and alkylamine-linked hydrogen bond surrogate pertidomimentics
CN108929375A (zh) 2011-10-18 2018-12-04 爱勒让治疗公司 拟肽大环化合物
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
RU2017145921A (ru) 2012-02-15 2019-02-21 Эйлерон Терапьютикс, Инк. Пептидомиметические макроциклы
CN104812384B (zh) 2012-11-01 2020-09-18 爱勒让治疗公司 二取代的氨基酸及其制备和使用方法
WO2014138429A2 (en) 2013-03-06 2014-09-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating hif1alpha
US20170037086A1 (en) 2014-04-09 2017-02-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles with pth activity
JP2017533889A (ja) 2014-09-24 2017-11-16 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
MX389354B (es) 2014-09-24 2025-03-20 Aileron Therapeutics Inc Macrociclos peptidomimeticos y formulaciones de los mismos.
US10253067B2 (en) 2015-03-20 2019-04-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2989311A1 (en) 2015-07-02 2017-01-05 Dana-Farber Cancer Institute, Inc. Stabilized anti-microbial peptides
WO2017023933A2 (en) 2015-08-03 2017-02-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
AU2016315878A1 (en) 2015-09-03 2018-03-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
QSAR & Combinatorial Science, 2004, vol. 23, pp. 662-673 *

Also Published As

Publication number Publication date
US10030049B2 (en) 2018-07-24
ES2649941T3 (es) 2018-01-16
EP3301108A1 (en) 2018-04-04
EP2564863A2 (en) 2013-03-06
US8637686B2 (en) 2014-01-28
US9957296B2 (en) 2018-05-01
JP2012144555A (ja) 2012-08-02
JP2015107966A (ja) 2015-06-11
WO2008104000A3 (en) 2008-11-27
IL241729A (en) 2017-09-28
US20080262200A1 (en) 2008-10-23
JP6046686B2 (ja) 2016-12-21
CA2678941C (en) 2018-11-27
JP4997293B2 (ja) 2012-08-08
EP2564862A2 (en) 2013-03-06
US7981999B2 (en) 2011-07-19
ES2398310T3 (es) 2013-03-15
US20120190818A1 (en) 2012-07-26
US9493509B2 (en) 2016-11-15
CN101663044A (zh) 2010-03-03
US20160304564A1 (en) 2016-10-20
US20110263815A1 (en) 2011-10-27
BRPI0807578A2 (pt) 2021-06-15
ES2648687T3 (es) 2018-01-05
CN101663044B (zh) 2014-07-23
AU2008218116A1 (en) 2008-08-28
JP5657594B2 (ja) 2015-01-21
CN109627287A (zh) 2019-04-16
US20160031936A1 (en) 2016-02-04
JP2010519318A (ja) 2010-06-03
IL200532A0 (en) 2010-04-29
US20160289274A1 (en) 2016-10-06
CN104086641A (zh) 2014-10-08
WO2008104000A2 (en) 2008-08-28
EP2114428B1 (en) 2012-10-31
IL241729A0 (en) 2015-11-30
CA2678941A1 (en) 2008-08-28
EP2564863A3 (en) 2013-07-03
US9023988B2 (en) 2015-05-05
IL200532A (en) 2015-10-29
EP2564863B1 (en) 2017-08-23
EP2114428A2 (en) 2009-11-11
EP2114428A4 (en) 2010-03-31
EP2564862A3 (en) 2013-07-10
EP2564862B1 (en) 2017-08-02

Similar Documents

Publication Publication Date Title
AU2008218116B2 (en) Triazole macrocycle systems
EP2342222B1 (en) Peptidomimetic macrocycles
AU2007333846B2 (en) Bis-sulfhydryl macrocyclization systems
AU2009294875C1 (en) Methods for preparing purified polypeptide compositions
AU2016216698A1 (en) Peptidomimetic macrocycles with improved properties
AU2012203906A1 (en) Triazole macrocycle systems
AU2017201310A1 (en) Bis-sulfhydryl macrocyclization systems

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired