JP6891183B2 - ラパフシン・ライブラリの合成と組成物 - Google Patents
ラパフシン・ライブラリの合成と組成物 Download PDFInfo
- Publication number
- JP6891183B2 JP6891183B2 JP2018540102A JP2018540102A JP6891183B2 JP 6891183 B2 JP6891183 B2 JP 6891183B2 JP 2018540102 A JP2018540102 A JP 2018540102A JP 2018540102 A JP2018540102 A JP 2018540102A JP 6891183 B2 JP6891183 B2 JP 6891183B2
- Authority
- JP
- Japan
- Prior art keywords
- rapafcin
- library
- synthesis
- composition
- viii
- 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
Links
- FPGXOHHWOLBEGI-HXUWFJFHSA-N CC(C)(C)C(COc1cccc([C@@H](CCc2ccc(C)c(OC)c2)O)c1)=O Chemical compound CC(C)(C)C(COc1cccc([C@@H](CCc2ccc(C)c(OC)c2)O)c1)=O FPGXOHHWOLBEGI-HXUWFJFHSA-N 0.000 description 1
- BNWCETAHAJSBFG-UHFFFAOYSA-N CC(C)(C)OC(CBr)=O Chemical compound CC(C)(C)OC(CBr)=O BNWCETAHAJSBFG-UHFFFAOYSA-N 0.000 description 1
- ALZNWMXUAQSCSA-UHFFFAOYSA-N CC(C)(C)OC(COc1cc(C(CCc(cc2OC)ccc2OC)=O)ccc1)=O Chemical compound CC(C)(C)OC(COc1cc(C(CCc(cc2OC)ccc2OC)=O)ccc1)=O ALZNWMXUAQSCSA-UHFFFAOYSA-N 0.000 description 1
- FMQIDODVYIXOCY-DPRQTADFSA-N CC(C)(C)OC(COc1cc([C@@H](CCc2ccc(C)c(OC)c2)OC([C@H](CCCC2)N2C(C(C(C)(C)COC(C=C)=O)=O)=O)=O)ccc1)O Chemical compound CC(C)(C)OC(COc1cc([C@@H](CCc2ccc(C)c(OC)c2)OC([C@H](CCCC2)N2C(C(C(C)(C)COC(C=C)=O)=O)=O)=O)ccc1)O FMQIDODVYIXOCY-DPRQTADFSA-N 0.000 description 1
- MJAVVYWNSTURBG-JTQLQIEISA-N CC(C)(COC(C=C)=O)C(C(N(CCCC1)[C@@H]1C(O)=O)=O)=O Chemical compound CC(C)(COC(C=C)=O)C(C(N(CCCC1)[C@@H]1C(O)=O)=O)=O MJAVVYWNSTURBG-JTQLQIEISA-N 0.000 description 1
- AYPUVXGSXSKEGZ-IZZNHLLZSA-N CC(C)(COC(C=C)=O)C(C(N(CCCC1)[C@@H]1C(O[C@H](CCc(cc1OC)ccc1OC)c1cccc(OCC(O)=O)c1)=O)=O)=O Chemical compound CC(C)(COC(C=C)=O)C(C(N(CCCC1)[C@@H]1C(O[C@H](CCc(cc1OC)ccc1OC)c1cccc(OCC(O)=O)c1)=O)=O)=O AYPUVXGSXSKEGZ-IZZNHLLZSA-N 0.000 description 1
- LUJMEECXHPYQOF-UHFFFAOYSA-N CC(c1cccc(O)c1)=O Chemical compound CC(c1cccc(O)c1)=O LUJMEECXHPYQOF-UHFFFAOYSA-N 0.000 description 1
- SUALBXZCVIZQQY-CMDGGOBGSA-N Cc(ccc(/C=C/C(c1cccc(O)c1)=O)c1)c1OC Chemical compound Cc(ccc(/C=C/C(c1cccc(O)c1)=O)c1)c1OC SUALBXZCVIZQQY-CMDGGOBGSA-N 0.000 description 1
- TVDHPUFLDYYBPO-UHFFFAOYSA-N Cc1ccc(C=O)cc1OC Chemical compound Cc1ccc(C=O)cc1OC TVDHPUFLDYYBPO-UHFFFAOYSA-N 0.000 description 1
- KVHOEZPZFZYAQX-UHFFFAOYSA-N Cc1ccc(CCC(c2cccc(O)c2)=O)cc1OC Chemical compound Cc1ccc(CCC(c2cccc(O)c2)=O)cc1OC KVHOEZPZFZYAQX-UHFFFAOYSA-N 0.000 description 1
Images
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
- G01N33/574—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)
- Immunology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Urology & Nephrology (AREA)
- Biophysics (AREA)
- Analytical Chemistry (AREA)
- Genetics & Genomics (AREA)
- Physics & Mathematics (AREA)
- Food Science & Technology (AREA)
- Biotechnology (AREA)
- Pathology (AREA)
- General Physics & Mathematics (AREA)
- Microbiology (AREA)
- Cell Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (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)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021088242A JP7158532B2 (ja) | 2016-02-04 | 2021-05-26 | ラパフシン・ライブラリの合成と組成物 |
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021088242A Division JP7158532B2 (ja) | 2016-02-04 | 2021-05-26 | ラパフシン・ライブラリの合成と組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019510738A JP2019510738A (ja) | 2019-04-18 |
| JP2019510738A5 JP2019510738A5 (enExample) | 2020-02-06 |
| JP6891183B2 true JP6891183B2 (ja) | 2021-06-18 |
Family
ID=59501078
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018540102A Active JP6891183B2 (ja) | 2016-02-04 | 2017-02-03 | ラパフシン・ライブラリの合成と組成物 |
| JP2021088242A Active JP7158532B2 (ja) | 2016-02-04 | 2021-05-26 | ラパフシン・ライブラリの合成と組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021088242A Active JP7158532B2 (ja) | 2016-02-04 | 2021-05-26 | ラパフシン・ライブラリの合成と組成物 |
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) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021138726A (ja) * | 2016-02-04 | 2021-09-16 | ザ・ジョンズ・ホプキンス・ユニバーシティ | ラパフシン・ライブラリの合成と組成物 |
| US11555054B2 (en) | 2016-02-04 | 2023-01-17 | The Johns Hopkins University | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
| US11708391B2 (en) | 2016-02-04 | 2023-07-25 | The Johns Hopkins University | Rapaglutins, novel inhibitors of GLUT and use thereof |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2813512B1 (en) | 2011-12-28 | 2021-03-31 | Chugai Seiyaku Kabushiki Kaisha | Peptide-compound cyclization method |
| DK3269809T3 (da) | 2015-03-13 | 2022-09-12 | Chugai Pharmaceutical Co Ltd | MODIFICERET AMINOACYL-tRNA-SYNTETASE OG ANVENDELSE DERAF |
| US11066416B2 (en) | 2016-02-04 | 2021-07-20 | The Johns Hopkins University | Rapafucin derivative compounds and methods of use thereof |
| US12391971B2 (en) | 2017-01-31 | 2025-08-19 | Chugai Seiyaku Kabushiki Kaisha | Method for synthesizing peptides in cell-free translation system |
| JP7232758B2 (ja) * | 2017-06-09 | 2023-03-06 | 中外製薬株式会社 | 膜透過性の高い環状ペプチド化合物、及びこれを含むライブラリ |
| 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 |
| US20220372014A1 (en) * | 2019-10-01 | 2022-11-24 | The Johns Hopkins University | Neuroprotective compounds and methods of use thereof |
| 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 |
Family Cites Families (14)
| 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 |
| 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 |
| US5696135A (en) | 1995-06-07 | 1997-12-09 | Gpi Nil Holdings, Inc. | Inhibitors of rotamase enzyme activity effective at stimulating neuronal growth |
| 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 |
| US6984635B1 (en) | 1998-02-13 | 2006-01-10 | Board Of Trustees Of The Leland Stanford Jr. University | Dimerizing agents, their production and use |
| AU766513B2 (en) * | 1998-02-13 | 2003-10-16 | Board Of Trustees Of The Leland Stanford Junior University | Novel 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 |
| AU2011336727B2 (en) * | 2010-11-30 | 2016-11-03 | The Johns Hopkins University | Hybrid cyclic libraries and screens thereof |
| EP2607352A1 (en) * | 2011-12-22 | 2013-06-26 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Pipecolate-diketoamides for treatment of psychiatric disorders |
| EP3007696B1 (en) * | 2013-06-14 | 2019-10-16 | The Board of Regents of The University of Texas System | Novel allosteric inhibitors of proteasome and methods of use thereof |
| CN108713028B (zh) | 2016-02-04 | 2021-12-28 | 约翰霍普金斯大学 | rapafucin文库的合成和组合物 |
-
2017
- 2017-02-03 CN CN201780010182.2A patent/CN108713028B/zh active Active
- 2017-02-03 WO PCT/US2017/016481 patent/WO2017136708A1/en not_active Ceased
- 2017-02-03 US US16/074,017 patent/US10662220B2/en active Active
- 2017-02-03 CA CA3013589A patent/CA3013589A1/en not_active Abandoned
- 2017-02-03 MX MX2018009405A patent/MX2018009405A/es unknown
- 2017-02-03 AU AU2017214550A patent/AU2017214550B2/en active Active
- 2017-02-03 JP JP2018540102A patent/JP6891183B2/ja active Active
- 2017-02-03 EP EP17748264.3A patent/EP3411413A4/en active Pending
-
2021
- 2021-05-26 JP JP2021088242A patent/JP7158532B2/ja active Active
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021138726A (ja) * | 2016-02-04 | 2021-09-16 | ザ・ジョンズ・ホプキンス・ユニバーシティ | ラパフシン・ライブラリの合成と組成物 |
| JP7158532B2 (ja) | 2016-02-04 | 2022-10-21 | ザ・ジョンズ・ホプキンス・ユニバーシティ | ラパフシン・ライブラリの合成と組成物 |
| US11555054B2 (en) | 2016-02-04 | 2023-01-17 | The Johns Hopkins University | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
| US11708391B2 (en) | 2016-02-04 | 2023-07-25 | The Johns Hopkins University | Rapaglutins, novel inhibitors of GLUT and use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2017214550A1 (en) | 2018-08-16 |
| US10662220B2 (en) | 2020-05-26 |
| CN108713028B (zh) | 2021-12-28 |
| JP7158532B2 (ja) | 2022-10-21 |
| JP2019510738A (ja) | 2019-04-18 |
| WO2017136708A1 (en) | 2017-08-10 |
| MX2018009405A (es) | 2018-11-09 |
| US20190092808A1 (en) | 2019-03-28 |
| EP3411413A1 (en) | 2018-12-12 |
| CA3013589A1 (en) | 2017-08-10 |
| EP3411413A4 (en) | 2019-09-18 |
| JP2021138726A (ja) | 2021-09-16 |
| CN108713028A (zh) | 2018-10-26 |
| AU2017214550B2 (en) | 2024-03-07 |
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