MX380313B - Rapadocinas, inhibidores de transportador 1 de nucleósido equilibrador y usos de los mismos. - Google Patents
Rapadocinas, inhibidores de transportador 1 de nucleósido equilibrador y usos de los mismos.Info
- Publication number
- MX380313B MX380313B MX2018009407A MX2018009407A MX380313B MX 380313 B MX380313 B MX 380313B MX 2018009407 A MX2018009407 A MX 2018009407A MX 2018009407 A MX2018009407 A MX 2018009407A MX 380313 B MX380313 B MX 380313B
- Authority
- MX
- Mexico
- Prior art keywords
- increasing
- nucleoside transporter
- rapadocines
- inhibitors
- formula
- Prior art date
Links
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- 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
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
- C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
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- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
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- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Endocrinology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Vascular Medicine (AREA)
Abstract
Se proporcionan un compuesto de la fórmula I, (ver fórmula) y sus análogos. Se pueden utilizar las composiciones que incluyen la Fórmula I para inhibir al transportador de nucleósido equilibrador 1 humano, incrementar la señalización de adenosina y producir efectos que incluyen el incremento de la actividad antiviral, incremento de la actividad antiparasitaria, incremento de la tolerancia a alcohol, disminución del dolor, protección de isquemia, así como muchas otras condiciones.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662291428P | 2016-02-04 | 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 (2)
| Publication Number | Publication Date |
|---|---|
| MX2018009407A MX2018009407A (es) | 2018-11-09 |
| MX380313B true MX380313B (es) | 2025-03-12 |
Family
ID=59500022
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2018009407A MX380313B (es) | 2016-02-04 | 2017-02-03 | Rapadocinas, inhibidores de transportador 1 de nucleósido equilibrador y usos de los mismos. |
| MX2021002588A MX2021002588A (es) | 2016-02-04 | 2018-08-02 | Rapadocinas, inhibidores de transportador 1 de nucleosido equilibrador y usos de los mismos. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2021002588A MX2021002588A (es) | 2016-02-04 | 2018-08-02 | Rapadocinas, inhibidores de transportador 1 de nucleosido equilibrador y usos de los mismos. |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US10774110B2 (es) |
| EP (2) | EP3411032B1 (es) |
| JP (1) | JP7022069B2 (es) |
| CN (2) | CN108697701B (es) |
| AU (1) | AU2017214557B2 (es) |
| CA (1) | CA3013650A1 (es) |
| ES (1) | ES2837484T3 (es) |
| MX (2) | MX380313B (es) |
| WO (1) | WO2017136717A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11066416B2 (en) | 2016-02-04 | 2021-07-20 | The Johns Hopkins University | Rapafucin derivative compounds and methods of use thereof |
| CN108697701B (zh) * | 2016-02-04 | 2021-10-26 | 约翰霍普金斯大学 | 平衡型核苷转运蛋白1的抑制剂Rapadocin及其用途 |
| MX2018009408A (es) * | 2016-02-04 | 2018-11-09 | Univ Johns Hopkins | Rapaglutinas, nuevos inhibidores de transportadores de glucosa (glut) y uso de los mismos. |
| 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 |
| CA3179526A1 (en) * | 2020-04-07 | 2021-10-14 | Michael Deligny | Macrocyclic diamine derivatives as ent inhibitors for the treatment of cancers, and combination thereof with adenosine receptor antagonists |
| EP4413003A1 (en) * | 2021-10-06 | 2024-08-14 | iTeos Belgium SA | Processes for preparing a macrocyclic compound having ent1 inhibiting activity |
| EP4413004A1 (en) * | 2021-10-06 | 2024-08-14 | iTeos Belgium SA | Macrocyclic compounds 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 |
| DE602004023924D1 (en) | 2003-04-18 | 2009-12-17 | Enanta Pharm Inc | Ease-hemmer |
| WO2005117562A2 (en) * | 2004-06-04 | 2005-12-15 | 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 |
| US7989395B2 (en) | 2005-10-28 | 2011-08-02 | Glaxosmithkline Llc | 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 |
| LT2481409T (lt) | 2007-03-07 | 2018-10-25 | Abraxis Bioscience, Llc | Nanodalelės, apimančios rapamiciną ir albuminą, kaip priešvėžinį agentą |
| EP2164875A4 (en) * | 2007-05-24 | 2011-11-30 | Us Dept Veterans Affairs | INTRANUCLEAR PROTEIN TRANSDUCTION THROUGH A NUCLEOSIDE SALVAGE PATHWAY |
| EP2313419A1 (en) | 2008-06-17 | 2011-04-27 | Biotica Technology Limited | Novel compounds and methods for their production |
| CN106084002A (zh) | 2010-11-30 | 2016-11-09 | 约翰·霍普金斯大学 | 杂交环状文库和其筛选 |
| US20140206624A1 (en) | 2011-02-04 | 2014-07-24 | The Brigham And Women's Hospital, Inc. | 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 |
| EP3247378B8 (en) | 2015-01-09 | 2023-08-23 | Revolution Medicines, Inc. | Macrocyclic compounds that participate in cooperative binding and medical uses thereof |
| WO2017059207A1 (en) | 2015-10-01 | 2017-04-06 | Warp Drive Bio, Inc. | Methods and reagents for analyzing protein-protein interfaces |
| MX2018009408A (es) * | 2016-02-04 | 2018-11-09 | Univ Johns Hopkins | Rapaglutinas, nuevos inhibidores de transportadores de glucosa (glut) y uso de los mismos. |
| CN108697701B (zh) | 2016-02-04 | 2021-10-26 | 约翰霍普金斯大学 | 平衡型核苷转运蛋白1的抑制剂Rapadocin及其用途 |
| US11066416B2 (en) | 2016-02-04 | 2021-07-20 | The Johns Hopkins University | Rapafucin derivative compounds and methods of use thereof |
| US10662220B2 (en) * | 2016-02-04 | 2020-05-26 | The Johns Hopkins University | Synthesis and composition of rapafucin libraries |
| CN109071566B (zh) | 2016-04-22 | 2021-08-31 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的大环mcl-1抑制剂 |
| JP2019532038A (ja) | 2016-09-02 | 2019-11-07 | ザ・ジョンズ・ホプキンス・ユニバーシティ | Mif阻害剤及びそれらの使用方法 |
| UY37900A (es) | 2017-09-26 | 2019-04-30 | Novartis Ag | Nuevos derivados de rapamicina |
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2017
- 2017-02-03 CN CN201780010178.6A patent/CN108697701B/zh active Active
- 2017-02-03 WO PCT/US2017/016494 patent/WO2017136717A1/en not_active Ceased
- 2017-02-03 CN CN202111210158.8A patent/CN113999281A/zh active Pending
- 2017-02-03 AU AU2017214557A patent/AU2017214557B2/en active Active
- 2017-02-03 JP JP2018540114A patent/JP7022069B2/ja active Active
- 2017-02-03 ES ES17748270T patent/ES2837484T3/es active Active
- 2017-02-03 EP EP17748270.0A patent/EP3411032B1/en active Active
- 2017-02-03 MX MX2018009407A patent/MX380313B/es unknown
- 2017-02-03 EP EP20198397.0A patent/EP3782636B1/en active Active
- 2017-02-03 CA CA3013650A patent/CA3013650A1/en not_active Abandoned
- 2017-02-03 US US16/073,746 patent/US10774110B2/en 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
Also Published As
| Publication number | Publication date |
|---|---|
| EP3782636A1 (en) | 2021-02-24 |
| CN113999281A (zh) | 2022-02-01 |
| US20200392182A1 (en) | 2020-12-17 |
| EP3411032A1 (en) | 2018-12-12 |
| MX2018009407A (es) | 2018-11-09 |
| EP3411032A4 (en) | 2019-08-14 |
| CA3013650A1 (en) | 2017-08-10 |
| ES2837484T3 (es) | 2021-06-30 |
| EP3411032B1 (en) | 2020-09-30 |
| US10774110B2 (en) | 2020-09-15 |
| CN108697701B (zh) | 2021-10-26 |
| US11555054B2 (en) | 2023-01-17 |
| US20190031716A1 (en) | 2019-01-31 |
| WO2017136717A1 (en) | 2017-08-10 |
| AU2017214557A1 (en) | 2018-08-16 |
| CN108697701A (zh) | 2018-10-23 |
| MX2021002588A (es) | 2021-04-19 |
| EP3782636B1 (en) | 2024-05-15 |
| JP7022069B2 (ja) | 2022-02-17 |
| JP2019508397A (ja) | 2019-03-28 |
| AU2017214557B2 (en) | 2022-05-19 |
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