CN101636407B - 双巯基大环化系统 - Google Patents

双巯基大环化系统 Download PDF

Info

Publication number
CN101636407B
CN101636407B CN200780050407.3A CN200780050407A CN101636407B CN 101636407 B CN101636407 B CN 101636407B CN 200780050407 A CN200780050407 A CN 200780050407A CN 101636407 B CN101636407 B CN 101636407B
Authority
CN
China
Prior art keywords
alkyl
peptidomimetic
amino acid
macrocycle
substituted
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
CN200780050407.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN101636407A (zh
Inventor
H·M·纳什
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
Priority to CN201510441012.2A priority Critical patent/CN105061577A/zh
Publication of CN101636407A publication Critical patent/CN101636407A/zh
Application granted granted Critical
Publication of CN101636407B publication Critical patent/CN101636407B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • C07K1/1133General 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 by redox-reactions involving cystein/cystin side chains
    • 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
    • C07K14/4747Apoptosis related proteins
    • 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
    • C07K14/665Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • C07K14/68Melanocyte-stimulating hormone [MSH]
    • 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
    • C07K14/705Receptors; Cell surface antigens; Cell surface determinants

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Analytical Chemistry (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Cell Biology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CN200780050407.3A 2006-12-14 2007-12-14 双巯基大环化系统 Expired - Fee Related CN101636407B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510441012.2A CN105061577A (zh) 2006-12-14 2007-12-14 双巯基大环化系统

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87481906P 2006-12-14 2006-12-14
US60/874,819 2006-12-14
PCT/US2007/087615 WO2008076904A1 (en) 2006-12-14 2007-12-14 Bis-sulfhydryl macrocyclization systems

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510441012.2A Division CN105061577A (zh) 2006-12-14 2007-12-14 双巯基大环化系统

Publications (2)

Publication Number Publication Date
CN101636407A CN101636407A (zh) 2010-01-27
CN101636407B true CN101636407B (zh) 2015-08-26

Family

ID=39536693

Family Applications (2)

Application Number Title Priority Date Filing Date
CN200780050407.3A Expired - Fee Related CN101636407B (zh) 2006-12-14 2007-12-14 双巯基大环化系统
CN201510441012.2A Pending CN105061577A (zh) 2006-12-14 2007-12-14 双巯基大环化系统

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201510441012.2A Pending CN105061577A (zh) 2006-12-14 2007-12-14 双巯基大环化系统

Country Status (9)

Country Link
US (5) US7960506B2 (https=)
EP (2) EP3170835A1 (https=)
JP (3) JP5656407B2 (https=)
CN (2) CN101636407B (https=)
AU (1) AU2007333846B2 (https=)
BR (1) BRPI0720306A2 (https=)
CA (1) CA2686827C (https=)
IL (1) IL199301A (https=)
WO (1) WO2008076904A1 (https=)

Families Citing this family (65)

* 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
ES2586387T3 (es) 2003-11-05 2016-10-14 Dana-Farber Cancer Institute, Inc. Péptidos alfa helicoidales adecuados para activar o inhibir la muerte celular
US7202332B2 (en) * 2004-05-27 2007-04-10 New York University Methods for preparing internally constrained peptides and peptidomimetics
EP2997973A1 (en) 2006-11-15 2016-03-23 Dana-Farber Cancer Institute, Inc. Stabalized 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
DK2118123T3 (en) 2007-01-31 2016-01-25 Dana Farber Cancer Inst Inc Stabilized p53 peptides and uses thereof
ES2649941T3 (es) 2007-02-23 2018-01-16 Aileron Therapeutics, Inc. Aminoácidos sustituidos para preparar péptidos macrocíclicos unidos a triazol
US8592377B2 (en) 2007-03-28 2013-11-26 President And Fellows Of Harvard College Stitched polypeptides
CA2685568A1 (en) * 2007-05-02 2008-11-13 Dana-Farber Cancer Institute, Inc. Methods of treating diabetes using bad bh3 domain peptide
WO2009110952A2 (en) * 2007-12-31 2009-09-11 New York University Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices
DE112009000300T5 (de) * 2008-02-08 2011-01-20 Aileron Therapeutics, Inc., Cambridge Therapeutische Peptidomimetische Makrocyclen
US20110144303A1 (en) * 2008-04-08 2011-06-16 Aileron Therapeutics, Inc. Biologically Active Peptidomimetic Macrocycles
EP2310407A4 (en) * 2008-04-08 2011-09-14 Aileron Therapeutics Inc BIOLOGIC EFFECTIVE PEPTIDOMIMETIC MACROCYCLES
WO2009149214A2 (en) * 2008-06-03 2009-12-10 Aileron Therapeutics, Inc. Compositions and methods for enhancing cellular transport of biomolecules
EP2356139A4 (en) 2008-07-23 2013-01-09 Harvard College LIGURE COMBINED POLYPEPTIDES
US8586707B2 (en) 2008-09-16 2013-11-19 The Research Foundation Of State University Of New York Stapled peptides and method of synthesis
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
US20120115783A1 (en) * 2008-09-22 2012-05-10 Alleron therapeutics, Inc Peptidomimetic macrocycles
CN102203126A (zh) 2008-09-22 2011-09-28 爱勒让治疗公司 用于制备纯化的多肽组合物的方法
CA2737922A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN102197048A (zh) * 2008-09-22 2011-09-21 爱勒让治疗公司 拟肽大环化合物
BRPI0920899A2 (pt) 2008-11-24 2016-04-26 Aileron Therapeutics Inc macrociclos peptidomiméticos com propriedades melhoradas
US9175047B2 (en) 2009-01-14 2015-11-03 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2752891C (en) * 2009-02-27 2018-08-21 Mimetogen Pharmaceuticals Inc. Peptidomimetic cyclic compounds for treating retinitis pigmentosa
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
CN102712675A (zh) 2009-09-22 2012-10-03 爱勒让治疗公司 拟肽大环化合物
US20110223149A1 (en) * 2009-10-14 2011-09-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
ES2711526T3 (es) 2010-08-13 2019-05-06 Aileron Therapeutics Inc Macrociclos peptidomiméticos
WO2012040459A2 (en) 2010-09-22 2012-03-29 President And Fellows Of Harvard College Beta-catenin targeting peptides and uses thereof
CA2817568A1 (en) 2010-11-12 2012-05-18 The Salk Institute For Biological Studies Intellectual Property And Tech Nology Transfer Cancer therapies and diagnostics
WO2012083078A2 (en) 2010-12-15 2012-06-21 The Research Foundation Of State University Of New York Croos-linked peptides and proteins, methods of making same, and uses thereof
CN103347532A (zh) * 2011-02-04 2013-10-09 爱奇司治疗公司 口服可生物利用肽药物组合物及其方法
US9487562B2 (en) 2011-06-17 2016-11-08 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
BR112014020103A2 (pt) * 2012-02-15 2018-10-09 Aileron Therapeutics, Inc. macrociclos peptidomiméticos
EP2819688A4 (en) 2012-02-15 2015-10-28 Aileron Therapeutics Inc TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES
WO2013126703A1 (en) * 2012-02-22 2013-08-29 New York University Reversibly crosslinked helical hydrogen bond surrogate macrocycles
WO2013173755A1 (en) 2012-05-18 2013-11-21 The Regents Of The University Of California Modification of peptides using a bis(thioether)arylbridge approach
WO2014052647A2 (en) 2012-09-26 2014-04-03 President And Fellows Of Harvard College Proline-locked stapled peptides and uses thereof
WO2014071241A1 (en) 2012-11-01 2014-05-08 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
EP3391898A3 (en) 2013-03-13 2019-02-13 President and Fellows of Harvard College Stapled and stitched polypeptides and uses thereof
CA2907454C (en) 2013-03-21 2021-05-04 Sanofi-Aventis Deutschland Gmbh Synthesis of hydantoin containing peptide products
US10450343B2 (en) 2013-03-21 2019-10-22 Sanofi-Aventis Deutschland Gmbh Synthesis of cyclic imide containing peptide products
JP2016523241A (ja) 2013-06-14 2016-08-08 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 安定化されたポリペプチドインスリン受容体調節剤
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
US9745342B2 (en) * 2013-10-28 2017-08-29 Naurex, Inc. NMDA receptor modulators and prodrugs, salts, and uses thereof
KR102455171B1 (ko) 2013-12-18 2022-10-14 더 스크립스 리서치 인스티튜트 변형된 치료제, 스테이플드 펩티드 지질 접합체, 및 이의 조성물
EP3126375B1 (en) * 2014-04-02 2023-12-13 University of Rochester Macrocyclic peptidomimetics for alpha-helix mimicry
CA2949535C (en) 2014-05-21 2023-09-12 President And Fellows Of Harvard College Ras inhibitory peptides and uses thereof
EP3197478A4 (en) 2014-09-24 2018-05-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
AU2015320545C1 (en) 2014-09-24 2020-05-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
WO2016154058A1 (en) 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US11155577B2 (en) 2015-06-22 2021-10-26 University Of Utah Research Foundation Thiol-ene based peptide stapling and uses thereof
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2017044633A1 (en) 2015-09-10 2017-03-16 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of mcl-1
US11034720B2 (en) 2016-07-17 2021-06-15 University Of Utah Research Foundation Thiol-yne based peptide stapling and uses thereof
US11091522B2 (en) 2018-07-23 2021-08-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
MX2021001943A (es) 2018-08-20 2021-07-15 Fog Pharmaceuticals Inc Colecciones de péptidos, agentes peptídicos y métodos de uso de los mismos.
US11345725B2 (en) 2019-09-16 2022-05-31 Research Foundation Of The City University Of New York Bis-thioether stapled peptides as inhibitors of PRC2 function
MX2022006861A (es) 2019-12-04 2022-07-11 Scripps Research Inst Agonistas del receptor glp2 y metodos de uso.
KR20240032010A (ko) 2021-06-09 2024-03-08 더 스크립스 리서치 인스티튜트 장기 지속형 이중 gip/glp-1 펩타이드 접합체 및 사용 방법
WO2025040657A1 (en) * 2023-08-21 2025-02-27 Medizinische Universität Wien Selective cyclized peptide kappa-opioid receptor antagonists

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998046631A1 (en) * 1997-04-11 1998-10-22 Eli Lilly And Company Combinatorial libraries of peptidomimetic macrocycles and processes therefor
US20050119167A1 (en) * 2003-06-02 2005-06-02 Giovanni Abbenante Process for the preparation of cyclic peptides

Family Cites Families (117)

* 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
WO1992013878A2 (en) 1991-02-07 1992-08-20 Board Of Trustees Of The University Of Illinois Conformationally restricted mimetics of beta turns and beta bulges and peptides containing the same
CA2084061A1 (en) 1991-04-09 1992-10-10 Arthur M. Felix Growth hormone releasing factor analogs
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
AU6770794A (en) 1993-04-23 1994-11-21 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
DK0832096T3 (da) 1995-05-04 2001-10-01 Scripps Research Inst Syntese af proteiner ved nativ kemisk ligering
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
US5955893A (en) * 1996-12-16 1999-09-21 Macronix International Co., Ltd. Power saving buffer circuit buffer bias voltages
EP0989136A4 (en) 1997-05-15 2002-10-09 Kyowa Hakko Kogyo Kk PEPTIDES WITH CYCLIC STRUCTURES THAT CAN RECOVER THE ACTIVITY OF MUTED P53 PROTEINS.
EP1015578A4 (en) 1997-09-17 2004-12-01 Walker And Eliza Hall Inst Of THERAPEUTIC MOLECULES
US6326354B1 (en) 1998-08-19 2001-12-04 Washington University Modulation of apoptosis with bid
JP2003503008A (ja) 1999-03-01 2003-01-28 バリアジェニックス インコーポレーテッド Rna分子をターゲティングする方法
CA2368431C (en) 1999-03-29 2006-01-24 The Procter & Gamble Company 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
WO2002013833A2 (en) 2000-08-16 2002-02-21 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
WO2003057158A2 (en) 2001-12-31 2003-07-17 Dana-Farber Cancer Institute, Inc. Method of treating apoptosis and compositions thereof
EP1468013A4 (en) 2002-01-03 2005-03-16 Yissum Res Dev Co CYCLIC PEPTIDES WITH CARBON SKELETON HAVING RESTRICTED CONFORMATION
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
JP4638225B2 (ja) 2002-05-30 2011-02-23 ザ スクリプス リサーチ インスティテュート 銅を触媒とするアジドとアセチレンのライゲーション
AU2003261774A1 (en) * 2002-09-06 2004-03-29 Kaneka Corporation PROCESS FOR PRODUCING L-Alpha-METHYLCYSTEINE DERIVATIVE
US20040171809A1 (en) 2002-09-09 2004-09-02 Korsmeyer Stanley J. BH3 peptides and method of use thereof
WO2004026896A2 (en) 2002-09-23 2004-04-01 Medivir Ab Hcv ns-3 serine protease inhibitors
EP1562941B1 (en) 2002-11-07 2009-12-23 Kosan Biosciences, Inc. Trans-9,10-dehydroepothilone c and d, analogs thereof and methos of making the same
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
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
EP1673078B1 (en) 2003-10-03 2008-05-28 Merck & Co., Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
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
ES2586387T3 (es) 2003-11-05 2016-10-14 Dana-Farber Cancer Institute, Inc. Péptidos alfa helicoidales adecuados para activar o inhibir la muerte celular
WO2005090388A1 (en) 2004-03-19 2005-09-29 The University Of Queensland Alpha helical mimics, their uses and methods for their production
US7202332B2 (en) 2004-05-27 2007-04-10 New York University Methods for preparing internally constrained 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
ES2326750T3 (es) 2004-10-29 2009-10-19 Schering Corporation 5-carboxiamido pirazoles y (1,2,4) triazoles como agentes antivirales.
WO2006078161A1 (en) 2005-01-24 2006-07-27 Pepscan Systems B.V. Binding compounds, immunogenic compounds and peptidomimetics
US20070020620A1 (en) 2005-07-14 2007-01-25 Finn M G Compositions and methods for coupling a plurality of compounds to a scaffold
JP2009544697A (ja) 2006-07-26 2009-12-17 ペプスキャン システムズ ベー.フェー. 免疫原性化合物及びタンパク質擬態物
US20080213175A1 (en) 2006-09-15 2008-09-04 Kolb Hartmuth C Click chemistry-derived cyclic peptidomimetics as integrin markers
EP2997973A1 (en) 2006-11-15 2016-03-23 Dana-Farber Cancer Institute, Inc. Stabalized maml peptides and uses thereof
US7981998B2 (en) 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
BRPI0720306A2 (pt) 2006-12-14 2014-02-04 Aileron Therapeutics Inc Sistemas de macrociclização da bis-sufidrila
EP2121007A1 (en) 2006-12-21 2009-11-25 Cytos Biotechnology AG Circular ccr5 peptide conjugates and uses thereof
DK2118123T3 (en) 2007-01-31 2016-01-25 Dana Farber Cancer Inst Inc Stabilized p53 peptides and uses thereof
ES2649941T3 (es) 2007-02-23 2018-01-16 Aileron Therapeutics, Inc. Aminoácidos sustituidos para preparar péptidos macrocíclicos unidos a triazol
US8592377B2 (en) 2007-03-28 2013-11-26 President And Fellows Of Harvard College Stitched polypeptides
CA2685568A1 (en) 2007-05-02 2008-11-13 Dana-Farber Cancer Institute, Inc. Methods of treating diabetes using bad bh3 domain peptide
WO2009110952A2 (en) 2007-12-31 2009-09-11 New York University Control of viral-host membrane fusion with hydrogen bond surrogate-based artificial helices
JP6157046B2 (ja) 2008-01-07 2017-07-05 アムジェン インコーポレイテッド 静電的ステアリング(electrostaticsteering)効果を用いた抗体Fcヘテロ二量体分子を作製するための方法
DE112009000300T5 (de) 2008-02-08 2011-01-20 Aileron Therapeutics, Inc., Cambridge Therapeutische Peptidomimetische Makrocyclen
EP2310407A4 (en) 2008-04-08 2011-09-14 Aileron Therapeutics Inc BIOLOGIC EFFECTIVE 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
EP2356139A4 (en) 2008-07-23 2013-01-09 Harvard College LIGURE COMBINED POLYPEPTIDES
WO2010033879A2 (en) 2008-09-18 2010-03-25 New York University Inhibiting interaction between hif-1a and p300/cbp with hydrogen bond surrogate-based helices
WO2010034026A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN102203126A (zh) 2008-09-22 2011-09-28 爱勒让治疗公司 用于制备纯化的多肽组合物的方法
CN102197048A (zh) 2008-09-22 2011-09-21 爱勒让治疗公司 拟肽大环化合物
CA2737922A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20120115783A1 (en) 2008-09-22 2012-05-10 Alleron therapeutics, Inc Peptidomimetic macrocycles
BRPI0920889A2 (pt) 2008-09-22 2017-10-10 Aileron Therapeutics Inc macrociclos peptidomiméticos.
BRPI0920899A2 (pt) 2008-11-24 2016-04-26 Aileron Therapeutics Inc macrociclos peptidomiméticos com propriedades melhoradas
US9175047B2 (en) 2009-01-14 2015-11-03 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
CN102712675A (zh) 2009-09-22 2012-10-03 爱勒让治疗公司 拟肽大环化合物
US20110223149A1 (en) 2009-10-14 2011-09-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
ES2711526T3 (es) 2010-08-13 2019-05-06 Aileron Therapeutics Inc Macrociclos peptidomiméticos
ES2586411T3 (es) 2011-03-04 2016-10-14 New York University Macrociclos sustitutos de enlace de hidrógeno como moduladores de Ras
WO2012173846A2 (en) 2011-06-06 2012-12-20 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN103889437A (zh) 2011-08-31 2014-06-25 纽约大学 硫醚、醚和烷基胺连接的氢键替代物肽模拟物
WO2013059530A2 (en) 2011-10-18 2013-04-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
TW201806968A (zh) 2011-10-18 2018-03-01 艾利倫治療公司 擬肽巨環化合物
BR112014020103A2 (pt) 2012-02-15 2018-10-09 Aileron Therapeutics, Inc. macrociclos peptidomiméticos
EP2819688A4 (en) 2012-02-15 2015-10-28 Aileron Therapeutics Inc TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES
WO2014071241A1 (en) 2012-11-01 2014-05-08 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
EP3197478A4 (en) 2014-09-24 2018-05-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
AU2015320545C1 (en) 2014-09-24 2020-05-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
WO2016154058A1 (en) 2015-03-20 2016-09-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
EP3317294B1 (en) 2015-07-02 2023-03-15 Dana-Farber Cancer Institute, Inc. Stabilized anti-microbial peptides
US20170037105A1 (en) 2015-08-03 2017-02-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20170114098A1 (en) 2015-09-03 2017-04-27 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
WO2017044633A1 (en) 2015-09-10 2017-03-16 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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998046631A1 (en) * 1997-04-11 1998-10-22 Eli Lilly And Company Combinatorial libraries of peptidomimetic macrocycles and processes therefor
US20050119167A1 (en) * 2003-06-02 2005-06-02 Giovanni Abbenante Process for the preparation of cyclic peptides

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Peter L.Barker et al.Cyclic RGD Peptide Analogues as Antiplatelet Antithrombotics.《J.Med.Chem》.1992,第35卷2040-2048. *

Also Published As

Publication number Publication date
US8609809B2 (en) 2013-12-17
AU2007333846B2 (en) 2014-01-23
US20140135473A1 (en) 2014-05-15
BRPI0720306A2 (pt) 2014-02-04
IL199301A (en) 2014-09-30
US20090047711A1 (en) 2009-02-19
AU2007333846A1 (en) 2008-06-26
JP5656407B2 (ja) 2015-01-21
EP3170835A1 (en) 2017-05-24
EP2094721A4 (en) 2011-01-19
EP2094721A1 (en) 2009-09-02
CN105061577A (zh) 2015-11-18
CA2686827C (en) 2014-09-16
US20170296620A1 (en) 2017-10-19
CA2686827A1 (en) 2008-06-26
JP2014231516A (ja) 2014-12-11
US10328117B2 (en) 2019-06-25
US20160095896A1 (en) 2016-04-07
EP2094721B1 (en) 2018-02-14
JP2016199546A (ja) 2016-12-01
JP6259861B2 (ja) 2018-01-10
WO2008076904A1 (en) 2008-06-26
JP2010513314A (ja) 2010-04-30
JP5931975B2 (ja) 2016-06-08
US7960506B2 (en) 2011-06-14
US20100184628A1 (en) 2010-07-22
US9675661B2 (en) 2017-06-13
US9175056B2 (en) 2015-11-03
HK1137184A1 (en) 2010-07-23
CN101636407A (zh) 2010-01-27
WO2008076904A9 (en) 2017-04-27

Similar Documents

Publication Publication Date Title
CN101636407B (zh) 双巯基大环化系统
US7981998B2 (en) Bis-sulfhydryl macrocyclization systems
CN101663044B (zh) 三唑大环系统
AU2009316288B2 (en) Peptidomimetic macrocycles with improved properties
HK1137184B (en) Bis-sulfhydryl macrocyclization systems
AU2017201310A1 (en) Bis-sulfhydryl macrocyclization systems
AU2012203906A1 (en) Triazole macrocycle systems

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1137184

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1137184

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20150826

Termination date: 20211214

CF01 Termination of patent right due to non-payment of annual fee