WO2008104000A2 - Triazole macrocycle systems - Google Patents

Triazole macrocycle systems Download PDF

Info

Publication number
WO2008104000A2
WO2008104000A2 PCT/US2008/054922 US2008054922W WO2008104000A2 WO 2008104000 A2 WO2008104000 A2 WO 2008104000A2 US 2008054922 W US2008054922 W US 2008054922W WO 2008104000 A2 WO2008104000 A2 WO 2008104000A2
Authority
WO
WIPO (PCT)
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
PCT/US2008/054922
Other languages
English (en)
French (fr)
Other versions
WO2008104000A3 (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
Priority to AU2008218116A priority Critical patent/AU2008218116B2/en
Priority to CA2678941A priority patent/CA2678941C/en
Priority to JP2009551061A priority patent/JP4997293B2/ja
Priority to ES08730678T priority patent/ES2398310T3/es
Priority to EP08730678A priority patent/EP2114428B1/en
Priority to BRPI0807578-6A priority patent/BRPI0807578A2/pt
Priority to CN200880009510.8A priority patent/CN101663044B/zh
Application filed by Aileron Therapeutics Inc filed Critical Aileron Therapeutics Inc
Publication of WO2008104000A2 publication Critical patent/WO2008104000A2/en
Publication of WO2008104000A3 publication Critical patent/WO2008104000A3/en
Priority to IL200532A priority patent/IL200532A/en
Anticipated expiration legal-status Critical
Priority to IL241729A priority patent/IL241729A/en
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • 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

Definitions

  • Ri and R 2 are independently -H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroalkyl, or heterocycloalkyl, unsubstituted or substituted with halo-;
  • a secondary structure of the peptidomimetic macrocycle is more stable than a corresponding secondary structure of a corresponding non-macrocyclic polypeptide.
  • the peptidomimetic macrocycle comprises an ⁇ -helix.
  • the ⁇ -helix may comprise, for example, from 1 turn to 5 turns.
  • the ⁇ -helix is more stable than an ⁇ -helix of a corresponding non-macrocyclic polypeptide.
  • the macrocycle-forming linker may span, or examp e, om turn to 5 turns o t e ⁇ - e x, suc as approximately 1, 2, 3, 4 or 5 turns of the ⁇ -helix.
  • K is O, S, SO, SO 2 , CO, CO 2 , or CONR 3 ;
  • R 4 is alkylene, alkenylene, alkynylene, heteroalkylene, cycloalkylene, heterocycloalkylene, arylene, or heteroarylene; each R 5 is independently halogen, alkyl, -OR 6 , -N(Re) 2 , -SR 6 , -SOR 6 , -SO 2 R 6 , -CO 2 R 6 , a fluorescent moiety, a radioisotope or a therapeutic agent; each R 6 is independently -H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heterocycloalkyl, a fluorescent moiety, a radioisotope or a therapeutic agent;
  • compositions of this invention comprise a combination of a peptidomimetic macrocycle and one or more additional therapeutic or prophylactic agents
  • both the compound and the additional agent should be present at dosage levels of between about 1 to 100%, and more preferably between about 5 to 95% of the dosage normally administered in a monotherapy regimen.
  • the additional agents are administered separately, as part of a multiple dose regimen, from the compounds of this invention.
  • those agents are part of a single dosage form, mixed together with the compounds of this invention in a single composition.
  • metastatic tumor can arise from a multitude of primary tumor types, including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor types including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor types including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor types including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor growth including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • “Pathologic hyperproliferative" cells occur in disease states characterized by malignant tumor growth.
  • non-pathologic hyperproliferative cells include proliferation of cells associated with wound repair.
  • cellular proliferative and/or differentiative disorders include cancer, e.g., carcinoma, sarcoma, or metastatic disorders.
  • the peptidomimetics macrocycles are novel therapeutic agents for controlling breast cancer, ovarian cancer, colon cancer, lung cancer, metastasis

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)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Toxicology (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)
PCT/US2008/054922 2007-02-23 2008-02-25 Triazole macrocycle systems Ceased WO2008104000A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
CA2678941A CA2678941C (en) 2007-02-23 2008-02-25 Triazole macrocycle systems
JP2009551061A JP4997293B2 (ja) 2007-02-23 2008-02-25 トリアゾール大環状系
ES08730678T ES2398310T3 (es) 2007-02-23 2008-02-25 Péptidos macrocíclicos unidos a triazol
EP08730678A EP2114428B1 (en) 2007-02-23 2008-02-25 Triazole linked macrocyclic peptides
BRPI0807578-6A BRPI0807578A2 (pt) 2007-02-23 2008-02-25 macrociclo peptidomimético, composto, kit e métodos para sintetizar um macrociclo peptidomimético
AU2008218116A AU2008218116B2 (en) 2007-02-23 2008-02-25 Triazole macrocycle systems
CN200880009510.8A CN101663044B (zh) 2007-02-23 2008-02-25 三唑大环系统
IL200532A IL200532A (en) 2007-02-23 2009-08-20 Macrocyclic systems including triazole and a method for their preparation
IL241729A IL241729A (en) 2007-02-23 2015-09-20 Triazole macrocyclization systems

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US90307307P 2007-02-23 2007-02-23
US60/903,073 2007-02-23

Publications (2)

Publication Number Publication Date
WO2008104000A2 true WO2008104000A2 (en) 2008-08-28
WO2008104000A3 WO2008104000A3 (en) 2008-11-27

Family

ID=39710801

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/054922 Ceased WO2008104000A2 (en) 2007-02-23 2008-02-25 Triazole macrocycle systems

Country Status (10)

Country Link
US (6) US7981999B2 (https=)
EP (4) EP3301108A1 (https=)
JP (2) JP4997293B2 (https=)
CN (3) CN101663044B (https=)
AU (1) AU2008218116B2 (https=)
BR (1) BRPI0807578A2 (https=)
CA (1) CA2678941C (https=)
ES (3) ES2649941T3 (https=)
IL (2) IL200532A (https=)
WO (1) WO2008104000A2 (https=)

Cited By (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010034034A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034031A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034028A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic marcrocycles
WO2010034026A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034029A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010099436A1 (en) * 2009-02-27 2010-09-02 Mimetogen Pharmaceuticals, Inc. Methods of treating retinitis pigmentosa
WO2011058188A1 (en) * 2009-11-16 2011-05-19 Centre National De La Recherche Scientifique - Cnrs - Compounds and methods for purifying peptides produced by solid phase peptide synthesis
EP2285970A4 (en) * 2008-06-03 2011-10-12 Aileron Therapeutics Inc COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES
EP2334317A4 (en) * 2008-09-16 2012-03-14 Univ New York State Res Found CLAMPED PEPTIDES AND METHOD OF COMPOSITION
EP2242503A4 (en) * 2008-02-08 2012-04-25 Aileron Therapeutics Inc THERAPEUTIC PEPTIDOMIMETIC MACROCYCLES
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
JP2012515709A (ja) * 2009-01-23 2012-07-12 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
WO2013071039A1 (en) * 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
US8859723B2 (en) * 2010-08-13 2014-10-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US8927500B2 (en) 2012-02-15 2015-01-06 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8987414B2 (en) 2012-02-15 2015-03-24 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
US9074009B2 (en) 2006-11-15 2015-07-07 Dana-Farber Cancer Institute, Inc. Stabilized MAML peptides and uses thereof
US9096684B2 (en) 2011-10-18 2015-08-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9169295B2 (en) 2010-10-13 2015-10-27 Bristol-Myers Squibb Company Macrocycles and macrocycle stabilized peptides
US9175056B2 (en) 2006-12-14 2015-11-03 Alleron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US9278984B2 (en) 2012-08-08 2016-03-08 Pacific Scientific Energetic Materials Company Method for preparation of a lead-free primary explosive
US9284283B2 (en) 2012-02-02 2016-03-15 Ensemble Therapeutics Corporation Macrocyclic compounds for modulating IL-17
AU2014201269B2 (en) * 2008-02-08 2016-09-15 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles
US9458202B2 (en) 2008-11-24 2016-10-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles with improved properties
US9493509B2 (en) 2007-02-23 2016-11-15 Aileron Therapeutics, Inc. Triazole macrocycle systems
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US10023613B2 (en) 2015-09-10 2018-07-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles as modulators of MCL-1
US10059741B2 (en) 2015-07-01 2018-08-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10246491B2 (en) 2013-03-06 2019-04-02 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating HIF1alpha
US10253067B2 (en) 2015-03-20 2019-04-09 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10301351B2 (en) 2007-03-28 2019-05-28 President And Fellows Of Harvard College Stitched polypeptides
US10300109B2 (en) 2009-09-22 2019-05-28 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10471120B2 (en) 2014-09-24 2019-11-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
EP3521300A4 (en) * 2016-09-30 2019-12-25 FUJIFILM Corporation CYCLIC PEPTIDE, AFFINITY CHROMATOGRAPHY CARRIER, MARKED ANTIBODY, ANTIBODY-ACTIVE SUBSTANCE CONJUGATE AND PHARMACEUTICAL PREPARATION
US10905739B2 (en) 2014-09-24 2021-02-02 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
US11091522B2 (en) 2018-07-23 2021-08-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US11198715B2 (en) 2016-07-22 2021-12-14 Massachusetts Institute Of Technology Selective Bfl-1 peptides
US11229708B2 (en) 2015-12-04 2022-01-25 Seagen Inc. Conjugates of quaternized tubulysin compounds
US11286299B2 (en) * 2018-09-17 2022-03-29 Massachusetts Institute Of Technology Peptides selective for Bcl-2 family proteins
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds

Families Citing this family (34)

* 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
US7981998B2 (en) * 2006-12-14 2011-07-19 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
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
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
EP2356139A4 (en) 2008-07-23 2013-01-09 Harvard College LIGURE COMBINED POLYPEPTIDES
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
AU2010273220B2 (en) 2009-07-13 2015-10-15 President And Fellows Of Harvard College Bifunctional stapled polypeptides and uses thereof
US20110223149A1 (en) * 2009-10-14 2011-09-15 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9227995B2 (en) * 2010-04-23 2016-01-05 Øyvind Jacobsen Peptides
WO2012040459A2 (en) 2010-09-22 2012-03-29 President And Fellows Of Harvard College Beta-catenin targeting peptides and uses thereof
FR2967072B1 (fr) 2010-11-05 2013-03-29 Univ Dundee Procede pour ameliorer la production de virus et semences vaccinales influenza
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
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
US8987274B2 (en) 2011-10-28 2015-03-24 Merck Sharp & Dohme Corp Macrocycles that increase p53 activity and the uses thereof
WO2014052647A2 (en) 2012-09-26 2014-04-03 President And Fellows Of Harvard College Proline-locked stapled peptides and uses thereof
KR102196882B1 (ko) 2012-12-20 2020-12-30 머크 샤프 앤드 돔 코포레이션 Hdm2 억제제로서의 치환된 이미다조피리딘
EP3391898A3 (en) 2013-03-13 2019-02-13 President and Fellows of Harvard College Stapled and stitched polypeptides and uses thereof
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
CA2949535C (en) 2014-05-21 2023-09-12 President And Fellows Of Harvard College Ras inhibitory peptides and uses thereof
FI3900742T3 (fi) * 2014-09-11 2024-08-16 Seagen Inc Tertiääristä amiinia sisältävien lääkeaineiden kohdennettu antaminen
US20170360881A1 (en) * 2016-06-17 2017-12-21 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
KR20200051733A (ko) 2017-09-08 2020-05-13 시애틀 지네틱스, 인크. 튜불리신 및 그 중간물의 제조 공정
EP3724216A1 (en) 2017-12-15 2020-10-21 Dana Farber Cancer Institute, Inc. Stabilized peptide-mediated targeted protein degradation
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

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
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
WO1998046631A1 (en) 1997-04-11 1998-10-22 Eli Lilly And Company Combinatorial libraries of peptidomimetic macrocycles and processes therefor
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
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
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
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
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
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
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
BRPI0920889A2 (pt) 2008-09-22 2017-10-10 Aileron Therapeutics Inc macrociclos peptidomiméticos.
CA2737922A1 (en) 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
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
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
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
TW201806968A (zh) 2011-10-18 2018-03-01 艾利倫治療公司 擬肽巨環化合物
WO2013059530A2 (en) 2011-10-18 2013-04-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
EP2819688A4 (en) 2012-02-15 2015-10-28 Aileron Therapeutics Inc TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES
BR112014020103A2 (pt) 2012-02-15 2018-10-09 Aileron Therapeutics, Inc. macrociclos peptidomiméticos
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
AU2015320545C1 (en) 2014-09-24 2020-05-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
EP3197478A4 (en) 2014-09-24 2018-05-30 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses 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

Cited By (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9074009B2 (en) 2006-11-15 2015-07-07 Dana-Farber Cancer Institute, Inc. Stabilized MAML peptides and uses thereof
US9175056B2 (en) 2006-12-14 2015-11-03 Alleron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US9675661B2 (en) 2006-12-14 2017-06-13 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US10328117B2 (en) 2006-12-14 2019-06-25 Aileron Therapeutics, Inc. Bis-sulfhydryl macrocyclization systems
US10202431B2 (en) 2007-01-31 2019-02-12 Aileron Therapeutics, Inc. Stabilized P53 peptides and uses thereof
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US9527896B2 (en) 2007-01-31 2016-12-27 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US9957296B2 (en) 2007-02-23 2018-05-01 Aileron Therapeutics, Inc. Triazole macrocycle systems
US10030049B2 (en) 2007-02-23 2018-07-24 Aileron Therapeutics, Inc. Triazole macrocycle systems
US9493509B2 (en) 2007-02-23 2016-11-15 Aileron Therapeutics, Inc. Triazole macrocycle systems
US10301351B2 (en) 2007-03-28 2019-05-28 President And Fellows Of Harvard College Stitched polypeptides
EP2242503A4 (en) * 2008-02-08 2012-04-25 Aileron Therapeutics Inc THERAPEUTIC PEPTIDOMIMETIC MACROCYCLES
AU2014201269B2 (en) * 2008-02-08 2016-09-15 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles
EP2926827A3 (en) * 2008-02-08 2015-11-04 Aileron Therapeutics, Inc. Therapeutic Peptidomimetic Macrocycles
US8808694B2 (en) 2008-02-08 2014-08-19 Aileron Therapeutics, Inc. Therapeutic peptidomimetic macrocycles
EP2285970A4 (en) * 2008-06-03 2011-10-12 Aileron Therapeutics Inc COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES
US8586707B2 (en) 2008-09-16 2013-11-19 The Research Foundation Of State University Of New York Stapled peptides and method of synthesis
EP2334317A4 (en) * 2008-09-16 2012-03-14 Univ New York State Res Found CLAMPED PEPTIDES AND METHOD OF COMPOSITION
AU2009294877C1 (en) * 2008-09-22 2015-05-07 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
CN102482336A (zh) * 2008-09-22 2012-05-30 爱勒让治疗公司 拟肽大环化合物
JP2016190882A (ja) * 2008-09-22 2016-11-10 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
US8399405B2 (en) 2008-09-22 2013-03-19 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034034A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
AU2009294877B2 (en) * 2008-09-22 2014-11-13 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034031A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP2014221801A (ja) * 2008-09-22 2014-11-27 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． ペプチド模倣大環状分子
WO2010034028A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic marcrocycles
US9175045B2 (en) 2008-09-22 2015-11-03 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034026A1 (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
WO2010034029A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8524653B2 (en) 2008-09-22 2013-09-03 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP2012503026A (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
US9458202B2 (en) 2008-11-24 2016-10-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles with improved properties
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
US10022422B2 (en) 2009-01-14 2018-07-17 Alleron Therapeutics, Inc. Peptidomimetic macrocycles
US9175047B2 (en) 2009-01-14 2015-11-03 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
JP2012515709A (ja) * 2009-01-23 2012-07-12 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
WO2010099436A1 (en) * 2009-02-27 2010-09-02 Mimetogen Pharmaceuticals, Inc. Methods of treating retinitis pigmentosa
AU2010217889B2 (en) * 2009-02-27 2014-12-18 Mimetogen Pharmaceuticals Inc. Peptidomimetic cyclic compounds for treating retinitis pigmentosa
JP2012519180A (ja) * 2009-02-27 2012-08-23 ミメトゲン ファーマシュウティカルズ インコーポレイテッド 網膜色素変性症を処置するためのペプチド模倣環状化合物
US8653036B2 (en) 2009-02-27 2014-02-18 Mimetogen Pharmaceuticals Inc. Methods of treating retinitis pigmentosa
US10300109B2 (en) 2009-09-22 2019-05-28 Aileron Therapeutics, Inc. 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
CN102666565A (zh) * 2009-11-16 2012-09-12 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
WO2011058188A1 (en) * 2009-11-16 2011-05-19 Centre National De La Recherche Scientifique - Cnrs - Compounds and methods for purifying peptides produced by solid phase peptide synthesis
US9073969B2 (en) 2009-11-16 2015-07-07 Centre National de la Recherche Scientifique—CNRS Compounds and methods for purifying peptides produced by solid phase peptide synthesis
US11008366B2 (en) 2010-08-13 2021-05-18 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10703780B2 (en) 2010-08-13 2020-07-07 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8859723B2 (en) * 2010-08-13 2014-10-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9957299B2 (en) 2010-08-13 2018-05-01 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9169295B2 (en) 2010-10-13 2015-10-27 Bristol-Myers Squibb Company Macrocycles and macrocycle stabilized peptides
US10308699B2 (en) 2011-10-18 2019-06-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9096684B2 (en) 2011-10-18 2015-08-04 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9522947B2 (en) 2011-10-18 2016-12-20 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2013071039A1 (en) * 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
US9284283B2 (en) 2012-02-02 2016-03-15 Ensemble Therapeutics Corporation Macrocyclic compounds for modulating IL-17
US10227380B2 (en) 2012-02-15 2019-03-12 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
US8927500B2 (en) 2012-02-15 2015-01-06 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US8987414B2 (en) 2012-02-15 2015-03-24 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
US10213477B2 (en) 2012-02-15 2019-02-26 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US10967042B2 (en) 2012-02-15 2021-04-06 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
EP2819688A4 (en) * 2012-02-15 2015-10-28 Aileron Therapeutics Inc TRIAZOL AND THIOETHER-COUPLED PEPTIDOMIMETIC MACROCYCLES
AU2013221433B2 (en) * 2012-02-15 2018-01-18 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
US9505804B2 (en) 2012-02-15 2016-11-29 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
US9278984B2 (en) 2012-08-08 2016-03-08 Pacific Scientific Energetic Materials Company Method for preparation of a lead-free primary explosive
US10669230B2 (en) 2012-11-01 2020-06-02 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US9845287B2 (en) 2012-11-01 2017-12-19 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
US10246491B2 (en) 2013-03-06 2019-04-02 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and use thereof in regulating HIF1alpha
US10471120B2 (en) 2014-09-24 2019-11-12 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US10905739B2 (en) 2014-09-24 2021-02-02 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
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
US11229708B2 (en) 2015-12-04 2022-01-25 Seagen Inc. Conjugates of quaternized tubulysin compounds
US11198715B2 (en) 2016-07-22 2021-12-14 Massachusetts Institute Of Technology Selective Bfl-1 peptides
EP3521300A4 (en) * 2016-09-30 2019-12-25 FUJIFILM Corporation CYCLIC PEPTIDE, AFFINITY CHROMATOGRAPHY CARRIER, MARKED ANTIBODY, ANTIBODY-ACTIVE SUBSTANCE CONJUGATE AND PHARMACEUTICAL PREPARATION
EP4043479A1 (en) * 2016-09-30 2022-08-17 FUJIFILM Corporation Cyclic peptide, affinity chromatography support, labeled antibody, antibody-drug conjugate, and pharmaceutical preparation
US11066446B2 (en) 2016-09-30 2021-07-20 Fujifilm Corporation Cyclic peptide, affinity chromatography support, labeled antibody, antibody drug conjugate, and pharmaceutical preparation
US11091522B2 (en) 2018-07-23 2021-08-17 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and uses thereof
US11286299B2 (en) * 2018-09-17 2022-03-29 Massachusetts Institute Of Technology Peptides selective for Bcl-2 family proteins

Also Published As

Publication number Publication date
JP5657594B2 (ja) 2015-01-21
JP2010519318A (ja) 2010-06-03
US20080262200A1 (en) 2008-10-23
US20110263815A1 (en) 2011-10-27
US20160304564A1 (en) 2016-10-20
IL200532A (en) 2015-10-29
US20160031936A1 (en) 2016-02-04
EP2564863A2 (en) 2013-03-06
ES2648687T3 (es) 2018-01-05
JP6046686B2 (ja) 2016-12-21
EP2564863B1 (en) 2017-08-23
JP2012144555A (ja) 2012-08-02
EP2564862A2 (en) 2013-03-06
IL200532A0 (en) 2010-04-29
WO2008104000A3 (en) 2008-11-27
US9493509B2 (en) 2016-11-15
US9023988B2 (en) 2015-05-05
CN104086641A (zh) 2014-10-08
JP4997293B2 (ja) 2012-08-08
CN109627287A (zh) 2019-04-16
CN101663044A (zh) 2010-03-03
JP2015107966A (ja) 2015-06-11
US9957296B2 (en) 2018-05-01
IL241729A0 (en) 2015-11-30
CA2678941A1 (en) 2008-08-28
AU2008218116B2 (en) 2012-04-05
BRPI0807578A2 (pt) 2021-06-15
EP2564862A3 (en) 2013-07-10
EP2564862B1 (en) 2017-08-02
US8637686B2 (en) 2014-01-28
EP2114428B1 (en) 2012-10-31
IL241729A (en) 2017-09-28
US10030049B2 (en) 2018-07-24
CA2678941C (en) 2018-11-27
US20160289274A1 (en) 2016-10-06
US7981999B2 (en) 2011-07-19
EP3301108A1 (en) 2018-04-04
US20120190818A1 (en) 2012-07-26
AU2008218116A1 (en) 2008-08-28
CN101663044B (zh) 2014-07-23
ES2398310T3 (es) 2013-03-15
EP2114428A4 (en) 2010-03-31
EP2114428A2 (en) 2009-11-11
ES2649941T3 (es) 2018-01-16
EP2564863A3 (en) 2013-07-03

Similar Documents

Publication Publication Date Title
EP2564862B1 (en) Substituted amino acids for preparing triazole linked macrocyclic peptides
EP2342222B1 (en) Peptidomimetic macrocycles
EP2094721B1 (en) Bis-sulfhydryl macrocyclization systems
US20170298099A1 (en) Biologically active peptidomimetic macrocycles
AU2016216698A1 (en) Peptidomimetic macrocycles with improved properties
AU2012203906A1 (en) Triazole macrocycle systems

Legal Events

Date Code Title Description
WWE Wipo information: entry into national phase

Ref document number: 200880009510.8

Country of ref document: CN

121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08730678

Country of ref document: EP

Kind code of ref document: A2

WWE Wipo information: entry into national phase

Ref document number: 2678941

Country of ref document: CA

Ref document number: 200532

Country of ref document: IL

WWE Wipo information: entry into national phase

Ref document number: 2009551061

Country of ref document: JP

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2008218116

Country of ref document: AU

Ref document number: 5458/DELNP/2009

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 2008730678

Country of ref document: EP

ENP Entry into the national phase

Ref document number: 2008218116

Country of ref document: AU

Date of ref document: 20080225

Kind code of ref document: A

WWE Wipo information: entry into national phase

Ref document number: 241729

Country of ref document: IL

ENP Entry into the national phase

Ref document number: PI0807578

Country of ref document: BR

Kind code of ref document: A2

Effective date: 20090824