JP2013505300A - ペプチド模倣大環状分子 - Google Patents

ペプチド模倣大環状分子 Download PDF

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Publication number
JP2013505300A
JP2013505300A JP2012531010A JP2012531010A JP2013505300A JP 2013505300 A JP2013505300 A JP 2013505300A JP 2012531010 A JP2012531010 A JP 2012531010A JP 2012531010 A JP2012531010 A JP 2012531010A JP 2013505300 A JP2013505300 A JP 2013505300A
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Japan
Prior art keywords
amino acid
peptidomimetic macrocycle
peptidomimetic
macrocycle
independently
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Pending
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JP2012531010A
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Japanese (ja)
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JP2013505300A5 (enExample
Inventor
ヒュー エム. ナッシュ,
ロザナ カペラー−リバーマン,
ジア−ウェン ハン,
トミ ケー. ソーヤー,
ジャスティン ノーエレ,
ノリユキ カワハタ,
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Rein Therapeutics Inc
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Aileron Therapeutics Inc
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Publication of JP2013505300A publication Critical patent/JP2013505300A/ja
Publication of JP2013505300A5 publication Critical patent/JP2013505300A5/ja
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2012531010A 2009-09-22 2010-09-22 ペプチド模倣大環状分子 Pending JP2013505300A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24481909P 2009-09-22 2009-09-22
US61/244,819 2009-09-22
PCT/US2010/049892 WO2011038049A1 (en) 2009-09-22 2010-09-22 Peptidomimetic macrocycles

Publications (2)

Publication Number Publication Date
JP2013505300A true JP2013505300A (ja) 2013-02-14
JP2013505300A5 JP2013505300A5 (enExample) 2013-12-12

Family

ID=43796193

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012531010A Pending JP2013505300A (ja) 2009-09-22 2010-09-22 ペプチド模倣大環状分子

Country Status (7)

Country Link
US (3) US20130072439A1 (enExample)
EP (1) EP2480565A4 (enExample)
JP (1) JP2013505300A (enExample)
CN (1) CN102712675A (enExample)
AU (1) AU2010298338A1 (enExample)
CA (1) CA2774973A1 (enExample)
WO (1) WO2011038049A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017513826A (ja) * 2014-04-02 2017-06-01 ユニバーシティー オブ ロチェスター アルファヘリックスを模倣した大環状ペプチドミメティック
CN110833549A (zh) * 2018-08-15 2020-02-25 广西梧州制药(集团)股份有限公司 吡唑并嘧啶衍生物在治疗慢性盆腔炎的用途
JP2022510606A (ja) * 2018-11-21 2022-01-27 エンドメット バイオサイエンシーズ,インク. 子宮内膜症を処置するための組成物および方法

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008076904A1 (en) 2006-12-14 2008-06-26 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
US7981999B2 (en) 2007-02-23 2011-07-19 Aileron Therapeutics, Inc. Triazole macrocycle systems
KR101623985B1 (ko) 2007-03-28 2016-05-25 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
CA2737922A1 (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
JP2012515172A (ja) 2009-01-14 2012-07-05 エルロン・セラピューティクス・インコーポレイテッド ペプチド模倣大環状分子
AU2010298338A1 (en) * 2009-09-22 2012-04-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
KR102104762B1 (ko) 2010-08-13 2020-04-24 에일러론 테라퓨틱스 인코포레이티드 펩티도미메틱 거대고리
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
CN108929375A (zh) 2011-10-18 2018-12-04 爱勒让治疗公司 拟肽大环化合物
US20140275295A1 (en) * 2011-10-19 2014-09-18 Hiroyuki Kouji Method for treating type i and type ii diabetes
EP2819688A4 (en) 2012-02-15 2015-10-28 Aileron Therapeutics Inc PEPTIDOMIMETIC MACROCYCLES CROSS-LINKED WITH TRIAZOLE AND THIOETHER
KR102112373B1 (ko) 2012-02-15 2020-05-18 에일러론 테라퓨틱스 인코포레이티드 펩티드모방체 마크로사이클
WO2013126703A1 (en) * 2012-02-22 2013-08-29 New York University Reversibly crosslinked helical hydrogen bond surrogate macrocycles
KR20150082307A (ko) 2012-11-01 2015-07-15 에일러론 테라퓨틱스 인코포레이티드 이치환 아미노산 및 이의 제조 및 사용 방법
WO2014138429A2 (en) 2013-03-06 2014-09-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating hif1alpha
SG10201902598VA (en) 2014-09-24 2019-04-29 Aileron Therapeutics Inc Peptidomimetic macrocycles and formulations thereof
CN106999541A (zh) 2014-09-24 2017-08-01 艾瑞朗医疗公司 拟肽大环化合物及其用途
EP3247378B8 (en) 2015-01-09 2023-08-23 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
TW201629069A (zh) 2015-01-09 2016-08-16 霍普驅動生物科技股份有限公司 參與協同結合之化合物及其用途
MX2017011834A (es) 2015-03-20 2018-04-11 Aileron Therapeutics Inc Macrociclos peptidomimeticos y usos de los mismos.
WO2017004548A1 (en) * 2015-07-01 2017-01-05 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
WO2017059207A1 (en) 2015-10-01 2017-04-06 Warp Drive Bio, Inc. Methods and reagents for analyzing protein-protein interfaces
US10907188B2 (en) 2016-04-12 2021-02-02 Ginkgo Bioworks, Inc. Compositions and methods for the production of compounds
JP2020501519A (ja) 2016-10-28 2020-01-23 ギンゴー バイオワークス, インコーポレイテッド 化合物の生産のための組成物および方法
WO2020023502A1 (en) 2018-07-23 2020-01-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
EP4054720A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
US11566007B2 (en) 2019-11-04 2023-01-31 Revolution Medicines, Inc. Ras inhibitors
US11608346B2 (en) 2019-11-04 2023-03-21 Revolution Medicines, Inc. Ras inhibitors
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002505255A (ja) * 1998-02-21 2002-02-19 マックス−デルブルック−セントラム フュール モレクラーレ メディツィン βカテニンに基づくヒトの疾患の治療薬、その製造及び使用
WO2009099677A2 (en) * 2008-02-08 2009-08-13 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles

Family Cites Families (202)

* 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
US4191754A (en) 1979-02-28 1980-03-04 Merck & Co., Inc. Bicyclic somatostatin analogs
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
AU550730B2 (en) 1982-03-09 1986-04-10 Commonwealth Of Australia, The Automated metal detection
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US4730006A (en) 1986-01-27 1988-03-08 Merrell Dow Pharmaceuticals Inc. Derivatives of 2,6-diamino-3-haloheptanedioic acid
CA1283827C (en) 1986-12-18 1991-05-07 Giorgio Cirelli Appliance for injection of liquid formulations
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
WO1989009233A1 (en) 1988-03-24 1989-10-05 Terrapin Technologies, Inc. Molecular sticks for controlling protein conformation
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5120859A (en) 1989-09-22 1992-06-09 Genentech, Inc. Chimeric amino acid analogues
US5650133A (en) 1990-01-19 1997-07-22 Nycomed Salutar Macrocyclic polyaza dichelates linked through ring nitrogens via an amide or ester functionality
US5712418A (en) 1989-10-23 1998-01-27 Research Corporation Technologies, Inc. Synthesis and use of amino acid fluorides as peptide coupling reagents
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5245009A (en) 1990-03-23 1993-09-14 The Salk Institute For Biological Studies CRF antagonists
CA2047042A1 (en) 1990-07-19 1992-01-20 John Hannah Cyclic hiv principal neutralizing determinant peptides
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
EP0488258B1 (en) 1990-11-27 1996-04-17 Fuji Photo Film Co., Ltd. Propenamide derivatives, polymers, copolymers and use thereof
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
US5364851A (en) 1991-06-14 1994-11-15 International Synthecon, Llc Conformationally restricted biologically active peptides, methods for their production and uses thereof
CA2072249C (en) 1991-06-28 2003-06-17 Saiko Hosokawa Human monoclonal antibody specifically binding to surface antigen of cancer cell membrane
GB9114949D0 (en) 1991-07-11 1991-08-28 Smithkline Beecham Plc Novel compounds
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
EP1251135A3 (en) 1992-04-03 2004-01-02 California Institute Of Technology High activity ruthenium or osmium metal carbene complexes for olefin metathesis reactions and synthesis thereof
US5411860A (en) 1992-04-07 1995-05-02 The Johns Hopkins University Amplification of human MDM2 gene in human tumors
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
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
US5536814A (en) 1993-09-27 1996-07-16 La Jolla Cancer Research Foundation Integrin-binding peptides
US6287787B1 (en) 1993-11-24 2001-09-11 Torrey Pines Institute For Molecular Studies Dimeric oligopeptide mixture sets
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
US5824483A (en) 1994-05-18 1998-10-20 Pence Inc. Conformationally-restricted combinatiorial library composition and method
IL109943A (en) 1994-06-08 2006-08-01 Develogen Israel Ltd Conformationally constrained backbone cyclized peptide analogs
US6407059B1 (en) 1994-06-08 2002-06-18 Peptor Limited Conformationally constrained backbone cyclized peptide analogs
US5807746A (en) 1994-06-13 1998-09-15 Vanderbilt University Method for importing biologically active molecules into cells
US7553929B2 (en) 1994-06-13 2009-06-30 Vanderbilt University Cell permeable peptides for inhibition of inflammatory reactions and methods of use
US5770377A (en) 1994-07-20 1998-06-23 University Of Dundee Interruption of binding of MDM2 and P53 protein and therapeutic application thereof
EP1956374A1 (en) 1994-09-19 2008-08-13 Ricardo J. Moro Detection and treatment of cancer
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US6169073B1 (en) 1995-02-16 2001-01-02 Bayer Corporation Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function
EP0729972A1 (de) 1995-02-28 1996-09-04 F. Hoffmann-La Roche Ag Tetrahydronaphthalin-Peptidderivate
US5675001A (en) 1995-03-14 1997-10-07 Hoffman/Barrett, L.L.C. Heteroatom-functionalized porphyrazines and multimetallic complexes and polymers derived therefrom
US6054556A (en) 1995-04-10 2000-04-25 The Arizona Board Of Regents On Behalf Of The University Of Arizona Melanocortin receptor antagonists and agonists
US5731408A (en) 1995-04-10 1998-03-24 Arizona Board Of Regents On Behalf Of The University Of Arizona Peptides having potent antagonist and agonist bioactivities at melanocortin receptors
US5672584A (en) 1995-04-25 1997-09-30 The University Of Kansas Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane permeability
US6184344B1 (en) 1995-05-04 2001-02-06 The Scripps Research Institute Synthesis of proteins by native chemical ligation
MX9708500A (es) 1995-05-04 1998-02-28 Scripps Research Inst Sintesis de proteinas mediante ligacion quimica nativa.
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5817789A (en) 1995-06-06 1998-10-06 Transkaryotic Therapies, Inc. Chimeric proteins for use in transport of a selected substance into cells
US6051554A (en) 1995-06-07 2000-04-18 Peptor Limited Conformationally constrained backbone cyclized somatostatin analogs
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
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
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
WO1998001467A2 (en) 1996-07-05 1998-01-15 Novartis Ag Inhibitors of the interaction between p53 and mdm2
US20020168761A1 (en) * 2000-01-24 2002-11-14 Gour Barbara J. Peptidomimetic modulators of cell adhesion
AU722985B2 (en) * 1996-07-12 2000-08-17 Mcgill University Compounds and methods for modulating cell adhesion
US5955593A (en) 1996-09-09 1999-09-21 Washington University BH3 interacting domain death agonist
US20020064546A1 (en) 1996-09-13 2002-05-30 J. Milton Harris Degradable poly(ethylene glycol) hydrogels with controlled half-life and precursors therefor
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
DE69735241T2 (de) 1996-11-21 2006-11-02 Promega Corp., Madison Alkyl peptidamide für topische verwendung
JP2001512475A (ja) 1997-02-20 2001-08-21 イエダ リサーチ アンド デベロップメント カンパニー リミテッド 抗病原性合成ペプチドおよびこれらを含む組成物
US6849428B1 (en) 1997-03-05 2005-02-01 New England Biolabs, Inc. Intein-mediated protein ligation of expressed proteins
US5851775A (en) * 1997-03-20 1998-12-22 Johns Hopkins University β-catenin, Tcf-4, and APC interact to prevent cancer
CA2286867A1 (en) 1997-04-11 1998-10-22 Eli Lilly And Company Combinatorial libraries of peptidomimetic macrocycles and processes therefor
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
JP2001524301A (ja) 1997-09-17 2001-12-04 ザ・ワルター・アンド・エリザ・ホール・インスティテュート・オヴ・メディカル・リサーチ 新規治療用分子
US6165732A (en) 1997-10-14 2000-12-26 Washington University Method for identifying apoptosis modulating compounds
US6875594B2 (en) 1997-11-13 2005-04-05 The Rockefeller University Methods of ligating expressed proteins
US6362276B1 (en) 1998-01-07 2002-03-26 Debio Recherche Pharmaceutique S.A. Degradable heterobifunctional poly(ethylene glycol) acrylates and gels and conjugates derived therefrom
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US6030997A (en) 1998-01-21 2000-02-29 Eilat; Eran Acid labile prodrugs
AU767185B2 (en) 1998-03-23 2003-11-06 President And Fellows Of Harvard College Synthesis of compounds and libraries of compounds
CA2325572A1 (en) 1998-04-15 1999-10-21 Aventis Pharmaceuticals Products Inc. Process for the preparation of resin-bound cyclic peptides
US6277824B1 (en) * 1998-07-10 2001-08-21 Adherex Technologies Compounds and methods for modulating adhesion molecule function
US6326354B1 (en) 1998-08-19 2001-12-04 Washington University Modulation of apoptosis with bid
US7173005B2 (en) 1998-09-02 2007-02-06 Antyra Inc. Insulin and IGF-1 receptor agonists and antagonists
US6572856B1 (en) 1998-09-10 2003-06-03 The University Of Virginia Patent Foundation Methods for the prevention and treatment of cancer using anti-C3b(i) antibodies
WO2000052210A2 (en) 1999-03-01 2000-09-08 Variagenics, Inc. Methods for targeting rna molecules
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
CA2284459C (en) * 1999-10-04 2012-12-11 Neokimia Inc. Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
US6348558B1 (en) 1999-12-10 2002-02-19 Shearwater Corporation Hydrolytically degradable polymers and hydrogels made therefrom
DE10009341A1 (de) 2000-02-22 2001-09-06 Florian Kern Verfahren zur antigen-spezifischen Stimulation von T-Lymphozyten
US6495674B1 (en) 2000-02-25 2002-12-17 The Salk Institute For Biological Studies Evectins and their use
US7049290B2 (en) 2000-07-28 2006-05-23 Universität Zürich Essential downstream component of the wingless signaling pathway and therapeutic and diagnostic applications based thereon
AU2001284942A1 (en) 2000-08-16 2002-02-25 Georgetown University Medical Center Small molecule inhibitors targeted at bcl-2
WO2002044378A2 (en) * 2000-11-28 2002-06-06 Curis, Inc. Wnt signalling assay, methods and uses thereof
WO2002064790A2 (en) 2000-12-19 2002-08-22 The Johns Hopkins University Jfy1 protein induces rapid apoptosis
US20050054770A1 (en) 2001-03-09 2005-03-10 Spatola Arno F. Helicomimetics and stabilized lxxll peptidomimetics
US20040106548A1 (en) 2001-09-07 2004-06-03 Schmidt Michelle A Conformationally constrained labeled peptides for imaging and therapy
CA2471719A1 (en) 2001-12-31 2003-07-17 Dana-Farber Cancer Institute, Inc. Method of treating apoptosis and compositions thereof
AU2003207940A1 (en) 2002-01-03 2003-07-30 Yissum Research Development Company Of The Hebrew University Of Jerusalem Conformationally constrained c-backbone cyclic peptides
WO2003070892A2 (en) 2002-02-15 2003-08-28 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
DE60320780D1 (de) 2002-04-22 2008-06-19 Univ Florida Funktionalisierte nanopartikel und verwendungsverfahren
DK2226316T3 (en) 2002-05-30 2016-04-11 Scripps Research Inst Copper catalyzed ligation of azides and acetylenes
SE0201863D0 (en) 2002-06-18 2002-06-18 Cepep Ab Cell penetrating peptides
US20060051846A1 (en) 2002-09-06 2006-03-09 Kaneka Corporation Process for producing l-alpha-methylcysteine derivative
WO2004022580A2 (en) 2002-09-09 2004-03-18 Dana-Farber Cancer Institute, Inc. Bh3 peptides and method of use thereof
KR100996996B1 (ko) 2002-11-07 2010-11-25 코산 바이오사이언시즈, 인코포레이티드 트랜스-9,10-디히드로에포틸론 c 및 d, 그것의 유사체 및 그것의 제조 방법
ES2295692T3 (es) 2002-11-08 2008-04-16 F. Hoffmann-La Roche Ag Nuevos derivados de 4-alcoxioxazol sustituido como agonistas de ppar.
US7166575B2 (en) 2002-12-17 2007-01-23 Nastech Pharmaceutical Company Inc. Compositions and methods for enhanced mucosal delivery of peptide YY and methods for treating and preventing obesity
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
DE602004014170D1 (de) 2003-10-03 2008-07-10 Merck & Co Inc Benzylether- und benzylamino-beta-sekretase-hemmer zur behandlung von alzheimer-krankheit
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
WO2005044839A2 (en) 2003-11-05 2005-05-19 Dana-Farber Cancer Institute, Inc. Stabilized alpha helical peptides and uses thereof
GB0404731D0 (en) 2004-03-03 2004-04-07 Indp Administrative Inst Nims Method and products for the selective degradation of proteins
US8193310B2 (en) 2004-03-19 2012-06-05 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
WO2005118634A2 (en) 2004-06-04 2005-12-15 The Brigham And Women's Hospital, Inc. Helical peptidomimetics with enhanced activity against beta-amyloid production
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
DE602005014804D1 (de) 2004-10-29 2009-07-16 Schering Corp Substituierte 5-carboxyamidpyrazoles und ä1,2,4ütriazole als viruzide
WO2006069001A2 (en) 2004-12-20 2006-06-29 Baylor College Of Medicine Structural requirements for stat3 binding and recruitment to phosphototyrosine ligands
EP1844337B1 (en) 2005-01-24 2013-07-03 Pepscan Systems B.V. Binding compounds, immunogenic compounds and peptidomimetics
WO2006103666A2 (en) 2005-03-28 2006-10-05 Yeda Research And Development Co. Ltd. Isolated bid polypeptides, polynucleotides encoding same and antibodies directed thereagainst and methods of using same for inducing cell cycle arrest or apoptosis
US20070020620A1 (en) 2005-07-14 2007-01-25 Finn M G Compositions and methods for coupling a plurality of compounds to a scaffold
US20070161544A1 (en) 2006-01-06 2007-07-12 Peter Wipf Selective targeting agents for mitcochondria
US7538190B2 (en) 2006-02-17 2009-05-26 Polychip Pharmaceuticals Pty Ltd Methods for the synthesis of two or more dicarba bridges in organic compounds
US7745573B2 (en) 2006-02-17 2010-06-29 Polychip Pharmaceuticals Pty Ltd. Conotoxin analogues and methods for synthesis of intramolecular dicarba bridge-containing peptides
GB0611405D0 (en) 2006-06-09 2006-07-19 Univ Belfast FKBP-L: A novel inhibitor of angiogenesis
US20080213175A1 (en) 2006-09-15 2008-09-04 Kolb Hartmuth C Click chemistry-derived cyclic peptidomimetics as integrin markers
US7897394B2 (en) 2006-09-21 2011-03-01 Intrexon Corporation Endoplasmic reticulum localization signals
JP2010510236A (ja) 2006-11-15 2010-04-02 ダナ−ファーバー キャンサー インスティテュート インク. 安定化させたmamlペプチドおよびその使用法
WO2008076904A1 (en) 2006-12-14 2008-06-26 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
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
US7981999B2 (en) 2007-02-23 2011-07-19 Aileron Therapeutics, Inc. Triazole macrocycle systems
KR101623985B1 (ko) 2007-03-28 2016-05-25 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 스티칭된 폴리펩티드
EP2152294B1 (en) 2007-05-02 2017-07-26 Dana-Farber Cancer Institute, Inc. A bad bh3 domain peptide for use in treating or delaying the onset of diabetes.
WO2009042237A2 (en) 2007-09-26 2009-04-02 Dana Farber Cancer Institute Methods and compositions for modulating bcl-2 family polypeptides
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
ES2563027T3 (es) 2008-01-07 2016-03-10 Amgen Inc. Método para fabricación de moléculas heterodímeras Fc de anticuerpos utilizando efectos de conducción electrostática
US20090326192A1 (en) 2008-04-08 2009-12-31 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
CN102216322A (zh) 2008-09-18 2011-10-12 纽约大学 用基于氢键替代的螺旋抑制HIF-1α和p300/CBP之间的相互作用
AU2009294875C1 (en) 2008-09-22 2015-05-14 Aileron Therapeutics, Inc. Methods for preparing purified polypeptide compositions
CN102884074A (zh) 2008-09-22 2013-01-16 爱勒让治疗公司 拟肽大环化合物
JP2012503024A (ja) 2008-09-22 2012-02-02 エルロン・セラピューティクス・インコーポレイテッド ペプチド模倣大環状分子
WO2010034026A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2737918A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CA2737922A1 (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
JP5731986B2 (ja) 2008-12-09 2015-06-10 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Mcl−1の特異的調節の方法及び組成物
JP2012515172A (ja) 2009-01-14 2012-07-05 エルロン・セラピューティクス・インコーポレイテッド ペプチド模倣大環状分子
CA2768299C (en) 2009-07-13 2018-03-20 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
AU2010298338A1 (en) * 2009-09-22 2012-04-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20110223149A1 (en) 2009-10-14 2011-09-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US20130177979A1 (en) 2010-06-22 2013-07-11 University Of Central Florida Research Foundation, Inc. Methods and compositions for cell permeable stat3 inhibitor
KR102104762B1 (ko) 2010-08-13 2020-04-24 에일러론 테라퓨틱스 인코포레이티드 펩티도미메틱 거대고리
US8957026B2 (en) 2010-09-22 2015-02-17 President And Fellows Of Harvard College Beta-catenin targeting peptides and uses thereof
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
US9487562B2 (en) 2011-06-17 2016-11-08 President And Fellows Of Harvard College Stabilized polypeptides as regulators of RAB GTPase function
US20140256912A1 (en) 2011-06-17 2014-09-11 President And Fellows Of Harvard College Stabilized Variant MAML Peptides and Uses Thereof
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
US8796257B2 (en) 2011-12-02 2014-08-05 Naeja Pharmaceutical Inc. Bicyclic compounds and their use as antibacterial agents and β-lactamase inhibitors
EP2819688A4 (en) 2012-02-15 2015-10-28 Aileron Therapeutics Inc PEPTIDOMIMETIC MACROCYCLES CROSS-LINKED WITH TRIAZOLE AND THIOETHER
KR102112373B1 (ko) 2012-02-15 2020-05-18 에일러론 테라퓨틱스 인코포레이티드 펩티드모방체 마크로사이클
PT2920197T (pt) 2012-09-26 2021-06-11 Harvard College Péptidos agrafados com bloqueio de prolina e suas utilizações
US20150225471A1 (en) 2012-10-01 2015-08-13 President And Fellows Of Harvard College Stabilized polypeptide insulin receptor modulators
KR20150082307A (ko) 2012-11-01 2015-07-15 에일러론 테라퓨틱스 인코포레이티드 이치환 아미노산 및 이의 제조 및 사용 방법
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
CN106999541A (zh) 2014-09-24 2017-08-01 艾瑞朗医疗公司 拟肽大环化合物及其用途
SG10201902598VA (en) 2014-09-24 2019-04-29 Aileron Therapeutics Inc Peptidomimetic macrocycles and formulations thereof
MX2017011834A (es) 2015-03-20 2018-04-11 Aileron Therapeutics Inc Macrociclos peptidomimeticos y usos de los mismos.
WO2017004548A1 (en) 2015-07-01 2017-01-05 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
AU2016287754B2 (en) 2015-07-02 2021-02-25 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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002505255A (ja) * 1998-02-21 2002-02-19 マックス−デルブルック−セントラム フュール モレクラーレ メディツィン βカテニンに基づくヒトの疾患の治療薬、その製造及び使用
WO2009099677A2 (en) * 2008-02-08 2009-08-13 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
JPN6014053258; Chemical Biology & Drug design Vol.73, No.1, 200901, p.3-6 *
JPN6014053260; Bioorganic & Medicinal Chemistry Letters Vol.19, No.9, 200905, p.2533-2536 *
JPN6014053262; Proceedings of the National Academy of Sciences Vol.109, No.44, 2012, p.17942-17947 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017513826A (ja) * 2014-04-02 2017-06-01 ユニバーシティー オブ ロチェスター アルファヘリックスを模倣した大環状ペプチドミメティック
CN110833549A (zh) * 2018-08-15 2020-02-25 广西梧州制药(集团)股份有限公司 吡唑并嘧啶衍生物在治疗慢性盆腔炎的用途
JP2022510606A (ja) * 2018-11-21 2022-01-27 エンドメット バイオサイエンシーズ,インク. 子宮内膜症を処置するための組成物および方法
US11884749B2 (en) 2018-11-21 2024-01-30 Endomet Biosciences, Inc. Compositions and methods for treating endometriosis
JP2025063040A (ja) * 2018-11-21 2025-04-15 エンドメット バイオサイエンシーズ,インク. 子宮内膜症を処置するための組成物および方法
US12441768B2 (en) 2018-11-21 2025-10-14 Endomet Biosciences, Inc. Compositions and methods for treating endometriosis

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