AU2017214550B2 - Synthesis and composition of Rapafucin libraries - Google Patents

Synthesis and composition of Rapafucin libraries Download PDF

Info

Publication number
AU2017214550B2
AU2017214550B2 AU2017214550A AU2017214550A AU2017214550B2 AU 2017214550 B2 AU2017214550 B2 AU 2017214550B2 AU 2017214550 A AU2017214550 A AU 2017214550A AU 2017214550 A AU2017214550 A AU 2017214550A AU 2017214550 B2 AU2017214550 B2 AU 2017214550B2
Authority
AU
Australia
Prior art keywords
substituted
unsubstituted
alkyl
alkenyl
alkynyl
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.)
Active
Application number
AU2017214550A
Other languages
English (en)
Other versions
AU2017214550A1 (en
Inventor
Manisha Das
Zufeng Guo
Sam Hong
Jun Liu
Wukun LIU
Hanjing Peng
Jingxin Wang
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.)
Johns Hopkins University
Original Assignee
Johns Hopkins University
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 Johns Hopkins University filed Critical Johns Hopkins University
Publication of AU2017214550A1 publication Critical patent/AU2017214550A1/en
Application granted granted Critical
Publication of AU2017214550B2 publication Critical patent/AU2017214550B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
    • C07K1/047—Simultaneous synthesis of different peptide species; Peptide libraries
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K17/00—Carrier-bound or immobilised peptides; Preparation thereof
    • C07K17/02—Peptides being immobilised on, or in, an organic carrier
    • C07K17/08—Peptides being immobilised on, or in, an organic carrier the carrier being a synthetic polymer
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6803—General methods of protein analysis not limited to specific proteins or families of proteins
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2570/00—Omics, e.g. proteomics, glycomics or lipidomics; Methods of analysis focusing on the entire complement of classes of biological molecules or subsets thereof, i.e. focusing on proteomes, glycomes or lipidomes
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/24—Immunology or allergic disorders

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biotechnology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
AU2017214550A 2016-02-04 2017-02-03 Synthesis and composition of Rapafucin libraries Active AU2017214550B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662291437P 2016-02-04 2016-02-04
US62/291,437 2016-02-04
PCT/US2017/016481 WO2017136708A1 (en) 2016-02-04 2017-02-03 Synthesis and composition of rapafucin libraries

Publications (2)

Publication Number Publication Date
AU2017214550A1 AU2017214550A1 (en) 2018-08-16
AU2017214550B2 true AU2017214550B2 (en) 2024-03-07

Family

ID=59501078

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017214550A Active AU2017214550B2 (en) 2016-02-04 2017-02-03 Synthesis and composition of Rapafucin libraries

Country Status (8)

Country Link
US (1) US10662220B2 (enExample)
EP (1) EP3411413A4 (enExample)
JP (2) JP6891183B2 (enExample)
CN (1) CN108713028B (enExample)
AU (1) AU2017214550B2 (enExample)
CA (1) CA3013589A1 (enExample)
MX (1) MX2018009405A (enExample)
WO (1) WO2017136708A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI852183B (zh) 2011-12-28 2024-08-11 日商中外製藥股份有限公司 胜肽化合物之環化方法
US10815489B2 (en) 2015-03-13 2020-10-27 Chugai Seiyaku Kabushiki Kaisha Modified aminoacyl-tRNA synthetase and use thereof
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
CN108697729B (zh) 2016-02-04 2023-05-09 约翰霍普金斯大学 新型GLUT抑制剂rapaglutin及其用途
WO2017136708A1 (en) * 2016-02-04 2017-08-10 The Johns Hopkins University Synthesis and composition of rapafucin libraries
AU2017214557B2 (en) * 2016-02-04 2022-05-19 The Johns Hopkins University Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof
US12391971B2 (en) 2017-01-31 2025-08-19 Chugai Seiyaku Kabushiki Kaisha Method for synthesizing peptides in cell-free translation system
EP3636807A4 (en) * 2017-06-09 2021-07-28 Chugai Seiyaku Kabushiki Kaisha CYCLIC PEPTIDE COMPOUND WITH HIGH MEMBRANE PERMEABILITY AND LIBRARY WITH IT
US12594275B2 (en) 2019-02-07 2026-04-07 The Regents Of The University Of California Immunophilin binding agents and uses thereof
KR102994657B1 (ko) * 2019-03-15 2026-07-22 추가이 세이야쿠 가부시키가이샤 방향족 아미노산 유도체의 제조 방법
WO2021067405A1 (en) * 2019-10-01 2021-04-08 The Johns Hopkins University Neuroprotective compounds and methods of use thereof
TW202126323A (zh) * 2019-10-01 2021-07-16 約翰斯赫普金斯大學 雷帕弗辛（Ｒａｐａｆｕｃｉｎ）衍生化合物及其使用方法
WO2021071931A1 (en) 2019-10-07 2021-04-15 The Johns Hopkins University Three-dimentional surface for protein and small molecule microarrays
CN120271673A (zh) * 2024-01-08 2025-07-08 重庆医科大学 一种化合物、包含其的药物组合物及其用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
WO2012075048A2 (en) * 2010-11-30 2012-06-07 The Johns Hopkins University Hybrid cyclic libraries and screens thereof
WO2014201405A1 (en) * 2013-06-14 2014-12-18 The Board Of Regents Of The University Of Texas System Novel allosteric inhibitors of proteasome and methods of use thereof

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US7056935B2 (en) 1995-06-07 2006-06-06 Gpi Nil Holdings, Inc. Rotamase enzyme activity inhibitors
CN1187127A (zh) * 1995-06-07 1998-07-08 吉尔福特药品有限公司 旋转异构酶活性抑制剂
US5696135A (en) 1995-06-07 1997-12-09 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth
JP2002503667A (ja) * 1998-02-13 2002-02-05 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 新規な二量体化剤、その製造および使用
US6984635B1 (en) 1998-02-13 2006-01-10 Board Of Trustees Of The Leland Stanford Jr. University Dimerizing agents, their production and use
GB0417852D0 (en) * 2004-08-11 2004-09-15 Biotica Tech Ltd Production of polyketides and other natural products
US20080306098A1 (en) * 2006-11-06 2008-12-11 Mutz Mitchell W Pharmacokinetics of protease inhibitors and other drugs
WO2010004304A1 (en) * 2008-06-17 2010-01-14 Biotica Technology Limited Novel compounds and methods for their production
EP2607352A1 (en) 2011-12-22 2013-06-26 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Pipecolate-diketoamides for treatment of psychiatric disorders
WO2017136708A1 (en) * 2016-02-04 2017-08-10 The Johns Hopkins University Synthesis and composition of rapafucin libraries

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5798355A (en) * 1995-06-07 1998-08-25 Gpi Nil Holdings, Inc. Inhibitors of rotamase enzyme activity
WO2012075048A2 (en) * 2010-11-30 2012-06-07 The Johns Hopkins University Hybrid cyclic libraries and screens thereof
WO2014201405A1 (en) * 2013-06-14 2014-12-18 The Board Of Regents Of The University Of Texas System Novel allosteric inhibitors of proteasome and methods of use thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
PUNIT UPADHYAYA ET AL: "Inhibition of Ras Signaling by Blocking Ras-Effector Interactions with Cyclic Peptides", ANGEWANDTE CHEMIE, INTERNATIONAL EDITION, vol. 54, no. 26, 2015, pages 7602 - 7606 *
XIANGHONG WU ET AL: "Creating Diverse Target-Binding Surfaces on FKBP12: Synthesis and Evaluation of a Rapamycin Analogue Library", ACS COMBINATORIAL SCIENCE, vol. 13, no. 5, 2011, pages 486 - 495 *
XIANGHONG WU ET AL: "Inhibition of Ras-effector interactions by cyclic peptides", MEDCHEMCOMM, vol. 4, no. 2, 2013, pages 378 - 382 *

Also Published As

Publication number Publication date
EP3411413A1 (en) 2018-12-12
JP2019510738A (ja) 2019-04-18
JP7158532B2 (ja) 2022-10-21
JP6891183B2 (ja) 2021-06-18
CN108713028A (zh) 2018-10-26
US20190092808A1 (en) 2019-03-28
WO2017136708A1 (en) 2017-08-10
JP2021138726A (ja) 2021-09-16
EP3411413A4 (en) 2019-09-18
US10662220B2 (en) 2020-05-26
MX2018009405A (es) 2018-11-09
CN108713028B (zh) 2021-12-28
CA3013589A1 (en) 2017-08-10
AU2017214550A1 (en) 2018-08-16

Similar Documents

Publication Publication Date Title
US12565518B2 (en) Hybrid cyclic libraries and screens thereof
WO2017136708A1 (en) Synthesis and composition of rapafucin libraries
Fouché et al. Design and development of a cyclic decapeptide scaffold with suitable properties for bioavailability and oral exposure
Chakraborty et al. Design and Synthesis of a rapamycin-based high affinity binding FKBP12 ligand
Vasilenko et al. Tick-borne flavivirus reproduction inhibitors based on isoxazole core linked with adamantane
Serpell et al. Chloride anion triggered motion in a bis-imidazolium rotaxane
Atkinson et al. Development of small cyclic peptides targeting the CK2α/β interface
US20040063716A1 (en) Cholesterol biosynthesis inhibitors containing as the active ingredient tricyclic spiro compounds
WO2001002397A9 (en) Tricyclic compounds having spiro union
Petros et al. NMR studies of an FK-506 analog,[U-carbon-13] ascomycin, bound to FK-506-binding protein
Tuin et al. Synthesis and Biological Evaluation of Novel Gramicidin S Analogues
US20030045520A1 (en) Tricyclic compound having spiro union
Ross Peptidomimetic foldamers of β-secondary structural elements
Bogdan et al. New [4.4] Cyclophane diketals, monoketones, and diketones: Design, synthesis, and structural analysis
Swaby Design and Synthesis of 4-Hydroxy Proline Based Library for Pharmaceutical Uses
Lfzal Supramolecular Host Molecules for Anion Binding
HK1231081A (en) Hybrid cyclic libraries and screens thereof
HK1231081A1 (zh) 雜交環狀文庫和其篩選
Brownlow Building block approach to the synthesis of a cucurbit [7] uril derivative bearing sulfonate functional groups