DK2016045T3 - Krystalform af tigecyclin og fremgangsmåder til fremstilling heraf - Google Patents
Krystalform af tigecyclin og fremgangsmåder til fremstilling heraf Download PDFInfo
- Publication number
- DK2016045T3 DK2016045T3 DK07776245.8T DK07776245T DK2016045T3 DK 2016045 T3 DK2016045 T3 DK 2016045T3 DK 07776245 T DK07776245 T DK 07776245T DK 2016045 T3 DK2016045 T3 DK 2016045T3
- Authority
- DK
- Denmark
- Prior art keywords
- tigecycline
- crystalline
- present
- solution
- preparing
- Prior art date
Links
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
-
- 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
-
- 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
Claims (20)
1. Krystalform af tigecyclin, der er kendetegnet ved et pulver-røntgendiffraktionsmønster med toppe ved 6,8, 9,5, 9,8, 12,1, 12, 6, 18,1, 20,2, 21, 6, 23, 3 og 26,8 ± 0,2 grader 2-theta.
2. Krystallinsk tigecyclin ifølge krav 1, der yderligere er kendetegnet ved et pulver-røntgendiffraktionsmønster som vist i figur 3.
3. Krystallinsk tigecyclin ifølge et hvilket som helst af kravene 1-2, hvor det krystallinske tigecyclin er til stede i en sammensætning, der har mindre end 20 % af nogen anden form af tigecyclin.
4. Krystallinsk tigecyclin ifølge krav 3, hvor det krystallinske tigecyclin er til stede i en sammensætning, der har mindre end 10 % af nogen anden form af tigecyclin.
5. Krystallinsk tigecyclin ifølge krav 4, hvor det krystallinske tigecyclin er til stede i en sammensætning, der har mindre end 5 % af nogen anden form af tigecyclin.
6. Krystallinsk tigecyclin ifølge et hvilket som helst af kravene 1-5, hvor det krystallinske tigecyclin har en maksimal partikelstørrelse på 300 ym.
7. Krystallinsk tigecyclin ifølge krav 6, hvor det krystallinske tigecyclin har en maksimal partikelstørrelse på 200 ym.
8. Krystallinsk tigecyclin ifølge krav 7, hvor det krystallinske tigecyclin har en maksimal partikelstørrelse på 100 ym.
9. Krystallinsk tigecyclin ifølge krav 8, hvor det krystallinske tigecyclin har en maksimal partikelstørrelse på 50 pm.
10. Fremgangsmåde til fremstilling af den krystallinske form af tigecyclin ifølge et hvilket som helst af ovennævnte krav, der omfatter krystallisering af tigecyclin fra et opløsningsmiddel, der omfatter en mættet Ci-5-nitril.
11. Fremgangsmåde ifølge krav 10, hvor opløsningsmidlet er acetonitril.
12. Fremgangsmåde ifølge krav 10 eller krav 11, hvor krystalliseringen omfatter trinene: a) fremstilling af en opløsning af tigecyclin i opløsningsmidlet; og b) inddampning af opløsningsmidlet til opnåelse af krystalformen.
13. Fremgangsmåde ifølge krav 12, hvor opløsningen opretholdes ved en temperatur på -10 °C til 30 °C.
14. Fremgangsmåde ifølge krav 13, hvor opløsningen opretholdes ved en temperatur på 0 °C til 25 °C.
15. Fremgangsmåde ifølge et hvilket som helst af kravene 12 til 14, hvor opløsningen opretholdes i en time.
16. Fremgangsmåde til fremstilling af krystalformen af tigecyclin ifølge et hvilket som helst af kravenes 1-9, der omfatter krystallisering af tigecyclin fra en blanding af dimethoxyethan og n-heptan.
17. Fremgangsmåde ifølge krav 16, hvor krystalliseringen omfatter trinene: a) fremstilling af en opløsning af tigecyclin i dimethoxyethan; b) iblanding af n-heptan i opløsningen til opnåelse af en suspension; og c) indvinding af det krystallinske tigecyclin fra suspensionen.
18. Farmaceutisk formulering, der omfatter formen af krystallinsk tigecyclin ifølge et hvilket som helst af kravene 1-9 og et farmaceutisk acceptabelt excipiens.
19. Farmaceutisk formulering ifølge krav 18, hvor excipienset er udvalgt fra gruppen, der består af fortyndingsmidler, bindemidler, opløsningsmidler, flyderegulerende midler, smøremidler, smagsstoffer og farvestoffer.
20. Forbindelse ifølge et hvilket som helst af kravene 1-9 til behandling af et pattedyr, der lider af infektioner.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79476306P | 2006-04-24 | 2006-04-24 | |
| US79680006P | 2006-05-01 | 2006-05-01 | |
| PCT/US2007/010108 WO2007127292A2 (en) | 2006-04-24 | 2007-04-24 | Tigeycline crystalline forms and processes for preparation thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2016045T3 true DK2016045T3 (da) | 2015-02-02 |
Family
ID=38521791
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK07776245.8T DK2016045T3 (da) | 2006-04-24 | 2007-04-24 | Krystalform af tigecyclin og fremgangsmåder til fremstilling heraf |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US7871993B2 (da) |
| EP (3) | EP2016045B1 (da) |
| CN (1) | CN101479235B (da) |
| BR (1) | BRPI0702875A2 (da) |
| CA (1) | CA2649075A1 (da) |
| CY (1) | CY1116048T1 (da) |
| DE (1) | DE202007019460U1 (da) |
| DK (1) | DK2016045T3 (da) |
| ES (2) | ES2528202T3 (da) |
| IL (1) | IL194329A (da) |
| PL (1) | PL2016045T3 (da) |
| PT (1) | PT2016045E (da) |
| SI (1) | SI2016045T1 (da) |
| TW (1) | TW200812943A (da) |
| WO (1) | WO2007127292A2 (da) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2649075A1 (en) * | 2006-04-24 | 2007-11-08 | Teva Pharmaceutical Industries Ltd. | Tigeycline crystalline forms and processes for preparation thereof |
| EP2236491A3 (en) | 2006-11-29 | 2010-11-03 | Teva Pharmaceutical Industries, Ltd. | Crystalline form of tigecycline and processes for preparation thereof |
| US20100160264A1 (en) * | 2007-06-21 | 2010-06-24 | Josef Wieser | Crystalline solid forms |
| US20100256402A1 (en) * | 2007-11-14 | 2010-10-07 | Sandoz Ag | Novel solvate |
| JP5574967B2 (ja) * | 2007-11-14 | 2014-08-20 | サンド・アクチエンゲゼルシヤフト | チゲサイクリン塩酸塩の結晶型 |
| WO2009070799A1 (en) * | 2007-11-29 | 2009-06-04 | Teva Pharmaceutical Industries Ltd. | Processes for preparation of crystalline tigecycline form ii |
| US20110124893A1 (en) * | 2008-01-23 | 2011-05-26 | Sandoz Ag | Antibiotic compounds |
| TW202216656A (zh) * | 2008-05-23 | 2022-05-01 | 美商Ｐｒｔｋ Ｓｐｖ２公司 | 四環素化合物之甲苯磺酸鹽及同素異形體 |
| ES2528490T3 (es) | 2008-12-18 | 2015-02-10 | Sandoz Ag | Forma cristalina C de dihidrocloruro de tigeciclina y métodos para su preparación |
| PT104350A (pt) | 2009-01-23 | 2010-07-23 | Hovione Farmaci Ncia S A | Processo de isolamento de tigeciclina |
| CN102295576A (zh) * | 2011-06-29 | 2011-12-28 | 赵军旭 | 替加环素的晶型及其制备方法 |
| CN102898325B (zh) * | 2011-07-29 | 2015-07-08 | 江苏奥赛康药业股份有限公司 | 替加环素晶体及其制备方法 |
| CN102952035A (zh) * | 2011-09-15 | 2013-03-06 | 北京海步国际医药科技发展有限公司 | 替加环素新晶型及其制备方法 |
| CN102924322B (zh) * | 2012-11-05 | 2014-09-17 | 赵军旭 | 一种替加环素的新晶型及其制备方法 |
| CN106431963B (zh) * | 2015-08-13 | 2019-03-05 | 江苏豪森药业集团有限公司 | 替加环素的新晶型及其制备方法 |
| CN112577917A (zh) * | 2020-12-28 | 2021-03-30 | 瀚晖制药有限公司 | 注射用替加环素中有色杂质的检测方法 |
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| US2990331A (en) | 1956-11-23 | 1961-06-27 | Pfizer & Co C | Stable solutions of salts of tetracyclines for parenteral administration |
| US2980584A (en) | 1957-10-29 | 1961-04-18 | Pfizer & Co C | Parenteral magnesium oxytetracycline acetic or lactic acid carboxamide vehicle preparation |
| GB876500A (en) | 1958-04-25 | 1961-09-06 | American Cyanamid Co | Substituted 6-deoxytetracyclines |
| US2997471A (en) | 1958-08-18 | 1961-08-22 | Bristol Myers Co | Tetracycline derivatives |
| US3062717A (en) | 1958-12-11 | 1962-11-06 | Pfizer & Co C | Intramuscular calcium tetracycline acetic or lactic acid carboxamide vehicle preparation |
| US3165531A (en) | 1962-03-08 | 1965-01-12 | Pfizer & Co C | 13-substituted-6-deoxytetracyclines and process utilizing the same |
| US3454697A (en) | 1965-06-08 | 1969-07-08 | American Cyanamid Co | Tetracycline antibiotic compositions for oral use |
| NL6607516A (da) | 1966-05-31 | 1967-12-01 | ||
| DE1767891C3 (de) | 1968-06-28 | 1980-10-30 | Pfizer | Verfahren zur Herstellung von wäßrigen arzneilichen Lösungen für die parenterale, perorale und lokale Anwendung mit einem Gehalt an einem Tetracyclinderivat |
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| DE2442829A1 (de) | 1974-09-06 | 1976-03-18 | Merck Patent Gmbh | Tetracyclische verbindungen und verfahren zu ihrer herstellung |
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| GB9105943D0 (en) | 1991-03-20 | 1991-05-08 | Philips Nv | A method of manufacturing a semiconductor device |
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| AR057649A1 (es) * | 2005-05-27 | 2007-12-12 | Wyeth Corp | Formas solidas cristalinas de tigeciclina y metodos para preparar las mismas |
| PE20070072A1 (es) | 2005-06-16 | 2007-02-25 | Wyeth Corp | Proceso de manufactura para tigeciclina como polvo reconstituible |
| CA2649075A1 (en) * | 2006-04-24 | 2007-11-08 | Teva Pharmaceutical Industries Ltd. | Tigeycline crystalline forms and processes for preparation thereof |
| EP2236491A3 (en) | 2006-11-29 | 2010-11-03 | Teva Pharmaceutical Industries, Ltd. | Crystalline form of tigecycline and processes for preparation thereof |
| US20100160264A1 (en) | 2007-06-21 | 2010-06-24 | Josef Wieser | Crystalline solid forms |
-
2007
- 2007-04-24 CA CA002649075A patent/CA2649075A1/en not_active Abandoned
- 2007-04-24 TW TW096114448A patent/TW200812943A/zh unknown
- 2007-04-24 EP EP07776245.8A patent/EP2016045B1/en active Active
- 2007-04-24 SI SI200731593T patent/SI2016045T1/sl unknown
- 2007-04-24 DK DK07776245.8T patent/DK2016045T3/da active
- 2007-04-24 US US11/789,432 patent/US7871993B2/en active Active
- 2007-04-24 ES ES07776245.8T patent/ES2528202T3/es active Active
- 2007-04-24 BR BRPI0702875-0A patent/BRPI0702875A2/pt not_active IP Right Cessation
- 2007-04-24 WO PCT/US2007/010108 patent/WO2007127292A2/en active Application Filing
- 2007-04-24 EP EP11180957A patent/EP2426104A1/en not_active Withdrawn
- 2007-04-24 PT PT77762458T patent/PT2016045E/pt unknown
- 2007-04-24 ES ES14185362.2T patent/ES2622356T3/es active Active
- 2007-04-24 CN CN2007800145992A patent/CN101479235B/zh active Active
- 2007-04-24 PL PL07776245T patent/PL2016045T3/pl unknown
- 2007-04-24 EP EP14185362.2A patent/EP2857386B1/en active Active
- 2007-04-24 DE DE202007019460U patent/DE202007019460U1/de not_active Expired - Lifetime
-
2008
- 2008-09-24 IL IL194329A patent/IL194329A/en active IP Right Grant
-
2011
- 2011-01-14 US US13/006,719 patent/US8207361B2/en not_active Expired - Fee Related
-
2015
- 2015-01-27 CY CY20151100084T patent/CY1116048T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0702875A2 (pt) | 2011-03-15 |
| EP2016045A2 (en) | 2009-01-21 |
| EP2426104A1 (en) | 2012-03-07 |
| WO2007127292A2 (en) | 2007-11-08 |
| CA2649075A1 (en) | 2007-11-08 |
| US8207361B2 (en) | 2012-06-26 |
| CY1116048T1 (el) | 2017-01-25 |
| DE202007019460U1 (de) | 2012-10-24 |
| ES2528202T3 (es) | 2015-02-05 |
| US7871993B2 (en) | 2011-01-18 |
| EP2016045B1 (en) | 2014-10-29 |
| PT2016045E (pt) | 2015-02-05 |
| IL194329A (en) | 2013-12-31 |
| US20110112316A1 (en) | 2011-05-12 |
| TW200812943A (en) | 2008-03-16 |
| CN101479235A (zh) | 2009-07-08 |
| PL2016045T3 (pl) | 2015-04-30 |
| WO2007127292A3 (en) | 2008-03-20 |
| CN101479235B (zh) | 2013-09-18 |
| US20080090789A1 (en) | 2008-04-17 |
| SI2016045T1 (sl) | 2015-03-31 |
| EP2857386A1 (en) | 2015-04-08 |
| EP2857386B1 (en) | 2017-02-22 |
| ES2622356T3 (es) | 2017-07-06 |
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