DK2694531T3 - Fremgangsmåder til fremstilling af et antifungalt middel - Google Patents
Fremgangsmåder til fremstilling af et antifungalt middel Download PDFInfo
- Publication number
- DK2694531T3 DK2694531T3 DK12712244.8T DK12712244T DK2694531T3 DK 2694531 T3 DK2694531 T3 DK 2694531T3 DK 12712244 T DK12712244 T DK 12712244T DK 2694531 T3 DK2694531 T3 DK 2694531T3
- Authority
- DK
- Denmark
- Prior art keywords
- micafungin
- salt
- coupling
- side chain
- compound
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- 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
-
- 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
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (14)
1. One-pot-fremgangsmåde til fremstilling af Micafungin eller et salt deraf, hvilken fremgangsmåde omfatter følgende rækkefølge af trin: a) blanding af en forbindelse med formlen (TTT)
eller et salt deraf, og et koblingsadditiv, der er udvalgt fra gruppen bestående af hydroxybenzotriazoler og ethyl-2-cyan-2-(hydroxyimino)acetat i et opløsningsmiddel; b) tilsætning af et koblingsreagens til blandingen opnået i trin a), hvor koblingsreagenset er et carbodiimid; c) tilsætning af en base og en forbindelse med formlen (II)
eller et salt deraf til blandingen opnået i trin b).
2. Fremgangsmåde ifølge krav 1, hvor koblingsadditivet er 1 -hydroxy-benzotriazol.
3. Fremgangsmåde ifølge krav 1, hvor koblingsadditivet er l-hydroxy-7-azabenzotriazol.
4. Fremgangsmåde ifølge krav 1, hvor koblingsadditivet er ethyl-2- cyan(hydroxyimino)acetat.
5. Fremgangsmåde ifølge et hvilket som helst af kravene 1-4, hvor koblingsreagenset er l-ethyl-3-(3-dimethylaminopropyl)carbodiimid (EDC) eller et salt deraf.
6. Fremgangsmåde ifølge krav 5, hvor koblingsreagenset er hydrochloridsaltet af EDC.
7. Fremgangsmåde ifølge et hvilket som helst af kravene 1-6, hvor solventet anvendt i trin a) er DMF.
8. Fremgangsmåde ifølge et hvilket som helst af kravene 1-7, hvor basen anvendt i trin c) er DIPEA.
9. Fremgangsmåde ifølge et hvilket som helst af kravene 1-8, hvor basen er tilsat til blandingen opnået i b) før tilsætning af forbindelsen med formlen II.
10. Fremgangsmåde ifølge et hvilket som helst af kravene 1-8, hvor basen er tilsat til blandingen opnået i trin b) efter tilsætning af forbindelsen med formlen II.
11. Fremgangsmåde ifølge et hvilket som helst af kravene 1-10, hvor Micafunginsaltet opnået i trin c) er præcipiteret.
12. Fremgangsmåde ifølge krav 11, hvor Micafunginsaltet opnået i trin c) er præcipiteret ved anvendelse af et antisolvent.
13. Fremgangsmåde ifølge krav 12, hvor antisolventet er ethylacetat.
14. Fremgangsmåde ifølge krav 11, hvor Micafunginsaltet opnået i trin c) er præcipiteret efter standsning af reaktionen ved tilsætning af methanol og acetone.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161471218P | 2011-04-04 | 2011-04-04 | |
| PCT/EP2012/055284 WO2012136498A1 (en) | 2011-04-04 | 2012-03-26 | Methods for manufacturing an antifungal agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2694531T3 true DK2694531T3 (da) | 2016-12-12 |
Family
ID=45930661
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK12712244.8T DK2694531T3 (da) | 2011-04-04 | 2012-03-26 | Fremgangsmåder til fremstilling af et antifungalt middel |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8981055B2 (da) |
| EP (1) | EP2694531B1 (da) |
| JP (1) | JP6017534B2 (da) |
| KR (1) | KR101969384B1 (da) |
| CN (1) | CN103492409B (da) |
| AU (1) | AU2012238928B2 (da) |
| BR (1) | BR112013023531A2 (da) |
| CA (1) | CA2829511C (da) |
| DK (1) | DK2694531T3 (da) |
| ES (1) | ES2603582T3 (da) |
| HR (1) | HRP20161519T1 (da) |
| HU (1) | HUE030157T2 (da) |
| IL (1) | IL228623A (da) |
| PL (1) | PL2694531T3 (da) |
| RS (1) | RS55371B1 (da) |
| SI (1) | SI2694531T1 (da) |
| WO (1) | WO2012136498A1 (da) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102775476B (zh) * | 2011-05-12 | 2015-01-07 | 上海天伟生物制药有限公司 | 一种米卡芬净钠盐的制备方法 |
| CN102627689B (zh) * | 2012-03-30 | 2014-08-06 | 上海天伟生物制药有限公司 | 一种环肽类化合物的水合物及其制备方法和用途 |
| WO2014044803A1 (en) * | 2012-09-24 | 2014-03-27 | Dsm Sinochem Pharmaceuticals Netherlands B.V. | Method for producing a cyclic peptide |
| CN103145810B (zh) * | 2012-12-20 | 2016-02-17 | 深圳翰宇药业股份有限公司 | 一种制备米卡芬净的方法 |
| CN107406484A (zh) * | 2014-12-11 | 2017-11-28 | 中化帝斯曼制药有限公司荷兰公司 | 酰化环状肽的方法 |
| CN105777869B (zh) * | 2014-12-24 | 2019-09-27 | 上海天伟生物制药有限公司 | 环肽类化合物的组合物 |
| CN106866650A (zh) * | 2017-01-09 | 2017-06-20 | 博瑞生物医药泰兴市有限公司 | 一种米卡芬净的合成与提纯方法 |
| CN111606901A (zh) * | 2020-06-16 | 2020-09-01 | 大桐制药（中国）有限责任公司 | 一种米卡芬净侧链中间体的合成方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR901379A (fr) | 1943-09-10 | 1945-07-25 | Télégraphie par variations de fréquence | |
| ATE229541T1 (de) * | 1994-10-07 | 2002-12-15 | Fujisawa Pharmaceutical Co | Zyklische hexapeptide mit antibiotischer aktivität |
| JP4784093B2 (ja) * | 2002-08-08 | 2011-09-28 | アステラス製薬株式会社 | イソオキサゾリル安息香酸の製造法 |
-
2012
- 2012-03-16 BR BR112013023531A patent/BR112013023531A2/pt active Search and Examination
- 2012-03-26 HU HUE12712244A patent/HUE030157T2/en unknown
- 2012-03-26 PL PL12712244T patent/PL2694531T3/pl unknown
- 2012-03-26 US US14/009,462 patent/US8981055B2/en active Active
- 2012-03-26 EP EP12712244.8A patent/EP2694531B1/en active Active
- 2012-03-26 DK DK12712244.8T patent/DK2694531T3/da active
- 2012-03-26 CN CN201280016089.XA patent/CN103492409B/zh active Active
- 2012-03-26 ES ES12712244.8T patent/ES2603582T3/es active Active
- 2012-03-26 RS RS20160999A patent/RS55371B1/sr unknown
- 2012-03-26 CA CA2829511A patent/CA2829511C/en active Active
- 2012-03-26 AU AU2012238928A patent/AU2012238928B2/en not_active Ceased
- 2012-03-26 WO PCT/EP2012/055284 patent/WO2012136498A1/en active Application Filing
- 2012-03-26 KR KR1020137029036A patent/KR101969384B1/ko active IP Right Grant
- 2012-03-26 JP JP2014503064A patent/JP6017534B2/ja not_active Expired - Fee Related
- 2012-03-26 SI SI201230767A patent/SI2694531T1/sl unknown
-
2013
- 2013-09-29 IL IL228623A patent/IL228623A/en active IP Right Grant
-
2016
- 2016-11-17 HR HRP20161519TT patent/HRP20161519T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20140371422A1 (en) | 2014-12-18 |
| IL228623A0 (en) | 2013-12-31 |
| US8981055B2 (en) | 2015-03-17 |
| SI2694531T1 (sl) | 2017-01-31 |
| HUE030157T2 (en) | 2017-04-28 |
| HRP20161519T1 (hr) | 2017-01-13 |
| WO2012136498A1 (en) | 2012-10-11 |
| JP6017534B2 (ja) | 2016-11-02 |
| RS55371B1 (sr) | 2017-03-31 |
| CA2829511C (en) | 2019-07-09 |
| PL2694531T3 (pl) | 2017-02-28 |
| AU2012238928A1 (en) | 2013-09-26 |
| CN103492409B (zh) | 2015-09-23 |
| RU2013147309A (ru) | 2015-05-10 |
| ES2603582T3 (es) | 2017-02-28 |
| CN103492409A (zh) | 2014-01-01 |
| IL228623A (en) | 2016-07-31 |
| JP2014510116A (ja) | 2014-04-24 |
| EP2694531A1 (en) | 2014-02-12 |
| BR112013023531A2 (pt) | 2016-12-06 |
| CA2829511A1 (en) | 2012-10-11 |
| KR20140026454A (ko) | 2014-03-05 |
| KR101969384B1 (ko) | 2019-04-16 |
| AU2012238928B2 (en) | 2016-05-26 |
| EP2694531B1 (en) | 2016-09-14 |
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