BR112022022185A2 - Derivados de miristoíla de 9-amino-doxiciclina para alvejar células-tronco cancerígenas e prevenir metástase - Google Patents
Derivados de miristoíla de 9-amino-doxiciclina para alvejar células-tronco cancerígenas e prevenir metástaseInfo
- Publication number
- BR112022022185A2 BR112022022185A2 BR112022022185A BR112022022185A BR112022022185A2 BR 112022022185 A2 BR112022022185 A2 BR 112022022185A2 BR 112022022185 A BR112022022185 A BR 112022022185A BR 112022022185 A BR112022022185 A BR 112022022185A BR 112022022185 A2 BR112022022185 A2 BR 112022022185A2
- Authority
- BR
- Brazil
- Prior art keywords
- doxycycline
- amino
- stem cells
- cancer stem
- doxy
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 5
- 201000011510 cancer Diseases 0.000 title abstract 5
- 206010027476 Metastases Diseases 0.000 title abstract 4
- 230000009401 metastasis Effects 0.000 title abstract 4
- 229960003722 doxycycline Drugs 0.000 title abstract 3
- 210000000130 stem cell Anatomy 0.000 title abstract 3
- 230000003115 biocidal effect Effects 0.000 abstract 2
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 abstract 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 abstract 2
- 241000588724 Escherichia coli Species 0.000 abstract 1
- 239000005639 Lauric acid Substances 0.000 abstract 1
- 235000021314 Palmitic acid Nutrition 0.000 abstract 1
- 241000191967 Staphylococcus aureus Species 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- XQTWDDCIUJNLTR-CVHRZJFOSA-N doxycycline monohydrate Chemical compound O.O=C1C2=C(O)C=CC=C2[C@H](C)[C@@H]2C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]1[C@H]2O XQTWDDCIUJNLTR-CVHRZJFOSA-N 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005313 fatty acid group Chemical group 0.000 abstract 1
- 210000002950 fibroblast Anatomy 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 abstract 1
- 231100000956 nontoxicity Toxicity 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 210000004881 tumor cell Anatomy 0.000 abstract 1
- 230000035899 viability Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
- C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the nitrogen atom of at least one of the carboxamide groups further acylated
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2603/00—Systems containing at least three condensed rings
- C07C2603/02—Ortho- or ortho- and peri-condensed systems
- C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
- C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
- C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
- C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
DERIVADOS DE MIRISTOÍLA DE 9-AMINODOXICICLINA PARA ALVEJAR CÉLULAS-TRONCO CANCERÍGENAS E PREVENIR METÁSTASE. A presente invenção refere-se a derivados de 9-amino-doxiciclina que têm como alvo células-tronco cancerígenas e inibem a metástase do câncer. Esses compostos visam seletivamente as CSCs, inibem potentemente a metástase das células tumorais in vivo, com pouca ou nenhuma toxicidade, e minimizam o risco de levar à resistência aos antibióticos. Em uma modalidade, uma porção de ácido graxo de 14 carbonos está covalentemente ligada ao grupo amino livre de 9-amino-doxiciclina. O conjugado "Doxy-Myr" resultante é mais de 5 vezes mais potente que a doxiciclina para inibir o crescimento independente de ancoragem de CSCs MCF7. Doxy-Myr não afetou a viabilidade da população total de células cancerosas MCF7 ou de fibroblastos normais cultivados como monocamadas 2D, mostrando notável seletividade para CSCs. Doxy-Myr não apresentou atividade antibiótica, contra Escherichia coli e Staphylococcus aureus. Conjugados com comprimentos de cadeia de ácido graxo mais longos (16 carbonos; ácido palmítico) ou mais curtos (12 carbonos; ácido láurico) tiveram atividade semelhante.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063024216P | 2020-05-13 | 2020-05-13 | |
| PCT/IB2021/054111 WO2021229499A1 (en) | 2020-05-13 | 2021-05-13 | Myristoyl derivatives of 9-amino-doxycycline for targeting cancer stem cells and preventing metastasis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112022022185A2 true BR112022022185A2 (pt) | 2022-12-13 |
Family
ID=78525505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022022185A BR112022022185A2 (pt) | 2020-05-13 | 2021-05-13 | Derivados de miristoíla de 9-amino-doxiciclina para alvejar células-tronco cancerígenas e prevenir metástase |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230174464A1 (pt) |
| EP (1) | EP4153563A4 (pt) |
| JP (1) | JP2023526258A (pt) |
| KR (1) | KR20230009454A (pt) |
| CN (1) | CN115551827A (pt) |
| AU (1) | AU2021271315A1 (pt) |
| BR (1) | BR112022022185A2 (pt) |
| CA (1) | CA3181794A1 (pt) |
| IL (1) | IL297661A (pt) |
| MX (1) | MX2022014172A (pt) |
| WO (1) | WO2021229499A1 (pt) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA200201046A1 (ru) * | 2000-03-31 | 2003-04-24 | Трастис Оф Тафтс Коллидж | 7- или 9-замещенные соединения тетрациклина, способ их получения (варианты), фармацевтическая композиция, способ лечения состояния, чувствительного к действию тетрациклина, у млекопитающего и реакционноспособное промежуточное производное |
| EP1807387A2 (en) * | 2004-10-25 | 2007-07-18 | Paratek Pharmaceuticals, Inc. | Substituted tetracycline compounds |
| CR20190524A (es) * | 2017-05-19 | 2020-01-10 | Lunella Biotech Inc | Antimitoscinas: inhibidores específicos de la biogénesis mitocondrial para erradicar células madre cancerosas |
| WO2019108729A1 (en) * | 2017-12-01 | 2019-06-06 | Lunella Biotech, Inc. | Repurposcins: targeted inhibitors of mitochondrial biogenesis for eradicating cancer stem cells |
| JP2022514739A (ja) * | 2018-12-17 | 2022-02-15 | ルネラ・バイオテック・インコーポレーテッド | 抗加齢のための三剤組合せ療法 |
| SG11202106516VA (en) * | 2018-12-17 | 2021-07-29 | Lunella Biotech Inc | Triple combination therapies for targeting mitochondria and killing cancer stem cells |
| US11672810B2 (en) * | 2019-05-24 | 2023-06-13 | Lunella Biotech, Inc. | Therapeutics and methods for predicting and overcoming endocrine resistance in breast cancer |
-
2021
- 2021-05-13 IL IL297661A patent/IL297661A/en unknown
- 2021-05-13 JP JP2022568817A patent/JP2023526258A/ja active Pending
- 2021-05-13 KR KR1020227043082A patent/KR20230009454A/ko active Search and Examination
- 2021-05-13 WO PCT/IB2021/054111 patent/WO2021229499A1/en active Application Filing
- 2021-05-13 AU AU2021271315A patent/AU2021271315A1/en active Pending
- 2021-05-13 EP EP21805219.9A patent/EP4153563A4/en active Pending
- 2021-05-13 CN CN202180034377.7A patent/CN115551827A/zh active Pending
- 2021-05-13 US US17/924,614 patent/US20230174464A1/en active Pending
- 2021-05-13 MX MX2022014172A patent/MX2022014172A/es unknown
- 2021-05-13 CA CA3181794A patent/CA3181794A1/en active Pending
- 2021-05-13 BR BR112022022185A patent/BR112022022185A2/pt unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4153563A4 (en) | 2024-06-19 |
| MX2022014172A (es) | 2022-12-02 |
| IL297661A (en) | 2022-12-01 |
| AU2021271315A1 (en) | 2022-12-01 |
| CA3181794A1 (en) | 2021-11-18 |
| WO2021229499A1 (en) | 2021-11-18 |
| KR20230009454A (ko) | 2023-01-17 |
| EP4153563A1 (en) | 2023-03-29 |
| JP2023526258A (ja) | 2023-06-21 |
| CN115551827A (zh) | 2022-12-30 |
| US20230174464A1 (en) | 2023-06-08 |
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