JP2019510738A5 - - Google Patents
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- Publication number
- JP2019510738A5 JP2019510738A5 JP2018540102A JP2018540102A JP2019510738A5 JP 2019510738 A5 JP2019510738 A5 JP 2019510738A5 JP 2018540102 A JP2018540102 A JP 2018540102A JP 2018540102 A JP2018540102 A JP 2018540102A JP 2019510738 A5 JP2019510738 A5 JP 2019510738A5
- Authority
- JP
- Japan
- 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.)
- Granted
Links
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 49
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 46
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 45
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000003342 alkenyl group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000000304 alkynyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000003282 alkyl amino group Chemical group 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000004404 heteroalkyl group Chemical group 0.000 claims 11
- 125000004414 alkyl thio group Chemical group 0.000 claims 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 10
- 125000002877 alkyl aryl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 239000012636 effector Substances 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000005010 perfluoroalkyl group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 150000001413 amino acids Chemical class 0.000 claims 4
- -1 amino, hydroxyl Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 3
- 125000006239 protecting group Chemical group 0.000 claims 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 2
- 150000008574 D-amino acids Chemical class 0.000 claims 2
- 102000000521 Immunophilins Human genes 0.000 claims 2
- 108010016648 Immunophilins Proteins 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 229930014626 natural product Natural products 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 2
- 239000011347 resin Substances 0.000 claims 2
- 229920005989 resin Polymers 0.000 claims 2
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 2
- 229960002930 sirolimus Drugs 0.000 claims 2
- 238000003786 synthesis reaction Methods 0.000 claims 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
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 true JP2019510738A5 (enExample) | 2020-02-06 |
| JP6891183B2 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) |
Families Citing this family (11)
| 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 |
| EP3411046B1 (en) | 2016-02-04 | 2025-07-16 | The Johns Hopkins University | Rapaglutins, novel inhibitors of glut and 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 |
| AU2017214557B2 (en) * | 2016-02-04 | 2022-05-19 | The Johns Hopkins University | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
| 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
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