JP2019508397A5 - - Google Patents
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- Publication number
- JP2019508397A5 JP2019508397A5 JP2018540114A JP2018540114A JP2019508397A5 JP 2019508397 A5 JP2019508397 A5 JP 2019508397A5 JP 2018540114 A JP2018540114 A JP 2018540114A JP 2018540114 A JP2018540114 A JP 2018540114A JP 2019508397 A5 JP2019508397 A5 JP 2019508397A5
- Authority
- JP
- Japan
- Prior art keywords
- improved
- compound
- group
- independently selected
- disease
- 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
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- 150000001875 compounds Chemical class 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 102100021469 Equilibrative nucleoside transporter 1 Human genes 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 101000822020 Homo sapiens Equilibrative nucleoside transporter 1 Proteins 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 102000019055 Nucleoside Transport Proteins Human genes 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 229960005305 adenosine Drugs 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 230000002141 anti-parasite Effects 0.000 claims 1
- 230000000840 anti-viral effect Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 238000009792 diffusion process Methods 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000028329 epileptic seizure Diseases 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000003908 liver function Effects 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 108091006527 nucleoside transporters Proteins 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662291428P | 2016-02-04 | 2016-02-04 | |
| US62/291,428 | 2016-02-04 | ||
| PCT/US2017/016494 WO2017136717A1 (en) | 2016-02-04 | 2017-02-03 | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019508397A JP2019508397A (ja) | 2019-03-28 |
| JP2019508397A5 true JP2019508397A5 (https=) | 2020-02-13 |
| JP7022069B2 JP7022069B2 (ja) | 2022-02-17 |
Family
ID=59500022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018540114A Active JP7022069B2 (ja) | 2016-02-04 | 2017-02-03 | ラパドシン（Ｒａｐａｄｏｃｉｎｓ）、受動拡散型ヌクレオシド輸送体１阻害剤及びその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US10774110B2 (https=) |
| EP (2) | EP3411032B1 (https=) |
| JP (1) | JP7022069B2 (https=) |
| CN (2) | CN113999281A (https=) |
| AU (1) | AU2017214557B2 (https=) |
| CA (1) | CA3013650A1 (https=) |
| ES (1) | ES2837484T3 (https=) |
| MX (2) | MX380313B (https=) |
| WO (1) | WO2017136717A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10774110B2 (en) * | 2016-02-04 | 2020-09-15 | The Johns Hopkins University | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
| CA3013783A1 (en) * | 2016-02-04 | 2017-08-10 | The Johns Hopkins University | Rapaglutins, novel inhibitors of glut and use thereof |
| US11066416B2 (en) | 2016-02-04 | 2021-07-20 | The Johns Hopkins University | Rapafucin derivative 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 |
| AR121777A1 (es) * | 2020-04-07 | 2022-07-06 | iTeos Belgium SA | Derivados de diamina macrocíclica como inhibidores de ent para el tratamiento de cánceres, y combinación de estos con antagonistas del receptor de adenosina |
| JP2024537110A (ja) * | 2021-10-06 | 2024-10-10 | アイテオ ベルギウム エスエー | Ｅｎｔ１阻害活性を有する大環状化合物 |
| WO2023056910A1 (en) * | 2021-10-06 | 2023-04-13 | iTeos Belgium SA | Processes for preparing a macrocyclic compound having ent1 inhibiting activity |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5100899A (en) * | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
| US5457194A (en) * | 1993-03-17 | 1995-10-10 | Abbott Laboratories | Substituted aliphatic amine-containing macrocyclic immunomodulators |
| 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 |
| US6984635B1 (en) | 1998-02-13 | 2006-01-10 | Board Of Trustees Of The Leland Stanford Jr. University | Dimerizing agents, their production and use |
| EP1352910A1 (en) | 2002-04-10 | 2003-10-15 | Grünenthal GmbH | New analogs of nitrobenzylthioinosine |
| GB0228723D0 (en) * | 2002-12-09 | 2003-01-15 | Cambridge Biotechnology Ltd | Treatment of pain |
| CN1788006A (zh) | 2003-04-18 | 2006-06-14 | 安南塔制药公司 | 喹喔啉基大环丙型肝炎丝氨酸蛋白酶抑制剂 |
| US20060003362A1 (en) | 2004-06-04 | 2006-01-05 | Xenoport, Inc. | ENT1 transporters expressed in cancer cells |
| GB0417852D0 (en) | 2004-08-11 | 2004-09-15 | Biotica Tech Ltd | Production of polyketides and other natural products |
| EP2368868A1 (en) | 2005-10-28 | 2011-09-28 | Praecis Pharmaceuticals Inc. | Methods for identifying compounds of interest using encoded libraries |
| US20080306098A1 (en) | 2006-11-06 | 2008-12-11 | Mutz Mitchell W | Pharmacokinetics of protease inhibitors and other drugs |
| WO2008109163A1 (en) | 2007-03-07 | 2008-09-12 | Abraxis Bioscience, Llc. | Nanoparticle comprising rapamycin and albumin as anticancer agent |
| EP3486653A1 (en) | 2007-05-24 | 2019-05-22 | The United States Government as represented by The Department of Veterans Affairs | Treatment of skeletal muscle disorder using ent2 |
| WO2010004304A1 (en) | 2008-06-17 | 2010-01-14 | Biotica Technology Limited | Novel compounds and methods for their production |
| EP2646440A4 (en) | 2010-11-30 | 2014-06-18 | Univ Johns Hopkins | CYCLIC HYBRID LIBRARIES AND SCREENS FOR THIS |
| WO2012106702A2 (en) | 2011-02-04 | 2012-08-09 | The General Hospital Corporation | Treatment of leukemia |
| EP2607352A1 (en) | 2011-12-22 | 2013-06-26 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Pipecolate-diketoamides for treatment of psychiatric disorders |
| KR101733736B1 (ko) | 2012-01-06 | 2017-05-10 | 삼성에스디아이 주식회사 | 리튬 이차 전지용 음극 활물질, 그 제조 방법 및 이를 포함하는 리튬 이차 전지 |
| WO2014008636A1 (en) | 2012-07-11 | 2014-01-16 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as hiv integrase inhibitors |
| 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 |
| US10533016B2 (en) | 2015-01-09 | 2020-01-14 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
| WO2017059207A1 (en) | 2015-10-01 | 2017-04-06 | Warp Drive Bio, Inc. | Methods and reagents for analyzing protein-protein interfaces |
| MX2018009405A (es) * | 2016-02-04 | 2018-11-09 | Univ Johns Hopkins | Sintesis y composicion de bibliotecas de rapafucina. |
| US11066416B2 (en) | 2016-02-04 | 2021-07-20 | The Johns Hopkins University | Rapafucin derivative compounds and methods of use thereof |
| CA3013783A1 (en) | 2016-02-04 | 2017-08-10 | The Johns Hopkins University | Rapaglutins, novel inhibitors of glut and use thereof |
| US10774110B2 (en) | 2016-02-04 | 2020-09-15 | The Johns Hopkins University | Rapadocins, inhibitors of equilibrative nucleoside transporter 1 and uses thereof |
| PT3445767T (pt) | 2016-04-22 | 2020-05-13 | Astrazeneca Ab | Inibidores de mcl-1 macrocíclicos para o tratamento de cancro |
| WO2018045250A1 (en) | 2016-09-02 | 2018-03-08 | The Johns Hopkins University | Mif inhibitors and methods of use thereof |
| AR112834A1 (es) | 2017-09-26 | 2019-12-18 | Novartis Ag | Derivados de rapamicina |
-
2017
- 2017-02-03 US US16/073,746 patent/US10774110B2/en active Active
- 2017-02-03 EP EP17748270.0A patent/EP3411032B1/en active Active
- 2017-02-03 ES ES17748270T patent/ES2837484T3/es active Active
- 2017-02-03 MX MX2018009407A patent/MX380313B/es unknown
- 2017-02-03 AU AU2017214557A patent/AU2017214557B2/en active Active
- 2017-02-03 EP EP20198397.0A patent/EP3782636B1/en active Active
- 2017-02-03 CN CN202111210158.8A patent/CN113999281A/zh active Pending
- 2017-02-03 WO PCT/US2017/016494 patent/WO2017136717A1/en not_active Ceased
- 2017-02-03 JP JP2018540114A patent/JP7022069B2/ja active Active
- 2017-02-03 CA CA3013650A patent/CA3013650A1/en not_active Abandoned
- 2017-02-03 CN CN201780010178.6A patent/CN108697701B/zh active Active
-
2018
- 2018-08-02 MX MX2021002588A patent/MX2021002588A/es unknown
-
2020
- 2020-08-26 US US17/003,940 patent/US11555054B2/en active Active
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