CO2021004427A2 - Derivados de azitromicina y roxitromicina como fármacos senolíticos - Google Patents
Derivados de azitromicina y roxitromicina como fármacos senolíticosInfo
- Publication number
- CO2021004427A2 CO2021004427A2 CONC2021/0004427A CO2021004427A CO2021004427A2 CO 2021004427 A2 CO2021004427 A2 CO 2021004427A2 CO 2021004427 A CO2021004427 A CO 2021004427A CO 2021004427 A2 CO2021004427 A2 CO 2021004427A2
- Authority
- CO
- Colombia
- Prior art keywords
- azithromycin
- senolytic
- roxithromycin
- activity
- drugs
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/65—Tetracyclines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Toxicology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Abstract
Esta descripción expone el uso de azitromicina, roxitromicina y telitromicina, inclusive derivados de los mismos, como fármacos senolíticos. La BrdU se usó para inducir la senescencia en un modelo de líneas de células fibroblastos humanas. También se dan a conocer métodos para seleccionar compuestos por la actividad senolítica. El ensayo de SRB se usó para medir la viabilidad celular a través del contenido de proteínas. Se descubrió que la azitromicina, la roxitromicina y la telitromicina, productos farmacéuticos aprobados clínicamente, son fármacos senolíticos. Sin embargo, el compuesto precursor relacionado estrechamente, eritromicina, no mostró actividad senolítica. La azitromicina indujo considerablemente tanto glicólisis aeróbica como autofagia en fibroblastos humanos, pero mostró efectos bifásicos que incluían sobre las tasas de consumo de oxígeno mitocondrial con actividad inhibitoria a 50 M y actividad estimuladora a 100 M. El sistema de ensayo en tiempo real xCELLigenceMR mostró que la azitromicina focaliza preferentemente las células senescentes, eliminando aproximadamente 97% (casi una reducción de 25 veces en las células senescentes).
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862740137P | 2018-10-02 | 2018-10-02 | |
| US201862750559P | 2018-10-25 | 2018-10-25 | |
| US201962788187P | 2019-01-04 | 2019-01-04 | |
| PCT/US2019/054231 WO2020072598A1 (en) | 2018-10-02 | 2019-10-02 | Azithromycin and roxithromycin derivatives as senolytic drugs |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2021004427A2 true CO2021004427A2 (es) | 2021-04-30 |
Family
ID=70054763
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2021/0004427A CO2021004427A2 (es) | 2018-10-02 | 2021-04-09 | Derivados de azitromicina y roxitromicina como fármacos senolíticos |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US11957700B2 (es) |
| EP (1) | EP3860616A4 (es) |
| JP (1) | JP2022504204A (es) |
| KR (1) | KR20210072026A (es) |
| CN (1) | CN113164504A (es) |
| AU (1) | AU2019353002A1 (es) |
| BR (1) | BR112021006423A2 (es) |
| CA (1) | CA3114888A1 (es) |
| CL (1) | CL2021000825A1 (es) |
| CO (1) | CO2021004427A2 (es) |
| CR (1) | CR20210221A (es) |
| CU (1) | CU20210024A7 (es) |
| DO (1) | DOP2021000056A (es) |
| EC (1) | ECSP21029576A (es) |
| IL (1) | IL281879A (es) |
| MX (1) | MX2021003808A (es) |
| PE (1) | PE20211006A1 (es) |
| PH (1) | PH12021550719A1 (es) |
| SG (1) | SG11202103293UA (es) |
| WO (1) | WO2020072598A1 (es) |
| ZA (1) | ZA202102157B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019104115A1 (en) * | 2017-11-24 | 2019-05-31 | Lunella Biotech, Inc. | Triphenylphosphonium-derivative compounds for eradicating cancer stem cells |
| KR20230073984A (ko) * | 2021-11-10 | 2023-05-26 | (주)라이프신약 | 노화세포 제거용 조성물 및 이의 용도 |
| WO2023090901A1 (ko) * | 2021-11-18 | 2023-05-25 | 의료법인 성광의료재단 | 기계 학습을 이용한 세포 노화의 마커를 선별하는 방법, 세포 노화 바이오 마커, 및 이를 이용한 세놀리틱 제제를 스크리닝 하는 방법 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20022292A1 (it) * | 2002-10-29 | 2004-04-30 | Zambon Spa | 9a-azalidi ad attivita' antiinfiammatoria. |
| US8202843B2 (en) | 2004-02-27 | 2012-06-19 | Rib-X Pharmaceuticals, Inc. | Macrocyclic compounds and methods of making and using the same |
| DK2102226T3 (da) * | 2006-12-12 | 2012-12-10 | Zambon Spa | Makrolidforbindelser med inflammationshæmmende virkning |
| GB0912584D0 (en) * | 2009-07-20 | 2009-08-26 | Ucl Business Plc | Cyclosporin conjugates |
| US9180134B2 (en) * | 2011-08-18 | 2015-11-10 | Ecole Polytechnique Federale De Lausanne (Epel) | Mitochondrial ribosomal proteins as aging regulators |
| WO2013040206A1 (en) * | 2011-09-14 | 2013-03-21 | Lewis Thomas J | Novel formulations comprising macrolide and tetracycline and their uses |
| KR101435717B1 (ko) * | 2012-09-06 | 2014-09-01 | 영남대학교 산학협력단 | 퀘세틴-3-Ｏ-β-Ｄ-글루쿠로니드를 유효성분으로 함유하는 세포 노화 억제용 조성물 |
| US20180021323A1 (en) * | 2015-01-22 | 2018-01-25 | Bioventures, Llc | Flip - a selective molecular target of senescent cells |
| JP2020511951A (ja) | 2017-01-03 | 2020-04-23 | バイオアトラ、エルエルシー | 老化細胞の処置のためのタンパク質療法 |
| IL305316B1 (en) | 2017-03-15 | 2024-05-01 | Lunella Biotech Inc | Mitoriboscines: Mitochondrial-Based Therapies Targeting Cancer Cells, Bacteria, and Pathogenic Yeasts |
| WO2018193125A1 (en) * | 2017-04-20 | 2018-10-25 | Novintum Biotechnology Gmbh | Azithromycin derivatives containing a phosphonium ion as anticancer agents |
| CA3060510A1 (en) | 2017-04-21 | 2018-10-25 | Lunella Biotech, Inc. | Vitamin c and doxycycline: a synthetic lethal combination therapy for eradicating cancer stem cells (cscs) |
| EP3624840A4 (en) | 2017-05-19 | 2021-03-10 | Lunella Biotech, Inc. | ANTIMITOSCINE: TARGETED INHIBITORS OF MITOCHONDRIAL BIOGENESIS TO DESCRIBE CANCER STEM CELLS |
| EP3624897A4 (en) | 2017-05-19 | 2021-07-14 | Lunella Biotech, Inc. | COMPANION DIAGNOSIS FOR MITOCHONDRIAL INHIBITORS |
| MX2019014806A (es) | 2017-06-26 | 2020-02-10 | Lunella Biotech Inc | Mitocetoscinas: agentes terapeuticos basados en mitocondrias que fijan como objetivo el metabolismo de cetonas en celulas cancerosas. |
| WO2019083997A1 (en) | 2017-10-24 | 2019-05-02 | Lunella Biotech, Inc. | MITOFLAVOSCINS: TARGETING FLAVIN-CONTAINING ENZYMES THAT REMOVE CANCER STEM CELLS (CSC) BY INHIBITING MITOCHONDRIAL BREATHING |
| WO2019104115A1 (en) | 2017-11-24 | 2019-05-31 | Lunella Biotech, Inc. | Triphenylphosphonium-derivative compounds for eradicating cancer stem cells |
| WO2019108729A1 (en) | 2017-12-01 | 2019-06-06 | Lunella Biotech, Inc. | Repurposcins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
| WO2019126179A1 (en) | 2017-12-20 | 2019-06-27 | Lunella Biotech, Inc. | Targeting mitochondrial fission through mdivi-1 derivatives |
| PE20220499A1 (es) | 2018-12-17 | 2022-04-07 | Lunella Biotech Inc | Terapias de combinacion triple para anti-envejecimiento |
-
2019
- 2019-10-02 BR BR112021006423A patent/BR112021006423A2/pt unknown
- 2019-10-02 KR KR1020217012994A patent/KR20210072026A/ko unknown
- 2019-10-02 JP JP2021518508A patent/JP2022504204A/ja active Pending
- 2019-10-02 PE PE2021000425A patent/PE20211006A1/es unknown
- 2019-10-02 EP EP19869744.3A patent/EP3860616A4/en active Pending
- 2019-10-02 MX MX2021003808A patent/MX2021003808A/es unknown
- 2019-10-02 CA CA3114888A patent/CA3114888A1/en active Pending
- 2019-10-02 CR CR20210221A patent/CR20210221A/es unknown
- 2019-10-02 CU CU2021000024A patent/CU20210024A7/es unknown
- 2019-10-02 CN CN201980079188.4A patent/CN113164504A/zh active Pending
- 2019-10-02 WO PCT/US2019/054231 patent/WO2020072598A1/en active Application Filing
- 2019-10-02 SG SG11202103293UA patent/SG11202103293UA/en unknown
- 2019-10-02 US US17/282,212 patent/US11957700B2/en active Active
- 2019-10-02 AU AU2019353002A patent/AU2019353002A1/en active Pending
-
2021
- 2021-03-29 IL IL281879A patent/IL281879A/en unknown
- 2021-03-30 ZA ZA2021/02157A patent/ZA202102157B/en unknown
- 2021-03-31 DO DO2021000056A patent/DOP2021000056A/es unknown
- 2021-03-31 PH PH12021550719A patent/PH12021550719A1/en unknown
- 2021-03-31 CL CL2021000825A patent/CL2021000825A1/es unknown
- 2021-04-09 CO CONC2021/0004427A patent/CO2021004427A2/es unknown
- 2021-04-26 EC ECSENADI202129576A patent/ECSP21029576A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA202102157B (en) | 2022-09-28 |
| CL2021000825A1 (es) | 2021-10-22 |
| IL281879A (en) | 2021-05-31 |
| SG11202103293UA (en) | 2021-04-29 |
| EP3860616A1 (en) | 2021-08-11 |
| US11957700B2 (en) | 2024-04-16 |
| CN113164504A (zh) | 2021-07-23 |
| MX2021003808A (es) | 2021-05-27 |
| EP3860616A4 (en) | 2022-07-06 |
| KR20210072026A (ko) | 2021-06-16 |
| CU20210024A7 (es) | 2021-11-04 |
| PE20211006A1 (es) | 2021-06-01 |
| JP2022504204A (ja) | 2022-01-13 |
| US20210275560A1 (en) | 2021-09-09 |
| PH12021550719A1 (en) | 2021-12-06 |
| WO2020072598A1 (en) | 2020-04-09 |
| CA3114888A1 (en) | 2020-04-09 |
| AU2019353002A1 (en) | 2021-05-06 |
| CR20210221A (es) | 2021-06-24 |
| DOP2021000056A (es) | 2021-06-30 |
| BR112021006423A2 (pt) | 2021-07-06 |
| ECSP21029576A (es) | 2021-05-31 |
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