AR057034A1 - Metodos para purificar tigeciclina - Google Patents
Metodos para purificar tigeciclinaInfo
- Publication number
- AR057034A1 AR057034A1 ARP060102156A ARP060102156A AR057034A1 AR 057034 A1 AR057034 A1 AR 057034A1 AR P060102156 A ARP060102156 A AR P060102156A AR P060102156 A ARP060102156 A AR P060102156A AR 057034 A1 AR057034 A1 AR 057034A1
- Authority
- AR
- Argentina
- Prior art keywords
- methods
- compound
- formula
- branched
- alkyl
- Prior art date
Links
- 239000000203 mixture Substances 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- SOVUOXKZCCAWOJ-HJYUBDRYSA-N (4s,4as,5ar,12ar)-9-[[2-(tert-butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=C(NC(=O)CNC(C)(C)C)C(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O SOVUOXKZCCAWOJ-HJYUBDRYSA-N 0.000 abstract 2
- 239000004098 Tetracycline Substances 0.000 abstract 2
- 235000019364 tetracycline Nutrition 0.000 abstract 2
- 150000003522 tetracyclines Chemical class 0.000 abstract 2
- 229960004089 tigecycline Drugs 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003880 polar aprotic solvent Substances 0.000 abstract 1
- 239000003586 protic polar solvent Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229960002180 tetracycline Drugs 0.000 abstract 1
- 229930101283 tetracycline Natural products 0.000 abstract 1
- 229940040944 tetracyclines Drugs 0.000 abstract 1
- -1 tigecycline Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/22—Separation; Purification; Stabilisation; Use of additives
- C07C231/24—Separation; Purification
-
- 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
-
- 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
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Communicable Diseases (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Se revelan métodos para preparar y purificar tetraciclinas, tales como tigeciclina. También se revelan composiciones de tetraciclina, tales como composiciones de tigeciclina, preparadas por estos métodos. Reivindicacion 1: Un método para purificar al menos un compuesto de formula (1) o una sal aceptable para uso farmacéutico del mismo, donde R1 y R2 se selecciona cada uno en forma independiente de H, alquilo C1-6 de cadena recta y ramificada, y cicloalquilo, o R1 y R2, junto con N, forman un heterociclo; R es -NR3R4, donde R3 y R4 se selecciona cada uno en forma independiente de H, y alquilo C1-4 recto y ramificado; y n oscila de 1-4, que comprende: A combinar el al menos un compuesto de formula (1) con al menos un solvente aprotico polar y al menos un solvente polar protico; B) mezclar durante al menos un período de tiempo que oscila entre 15 minutos y 2 horas a una temperatura que oscila entre 0°C y 40°C para dar una primera mezcla; y C) obtener el al menos un compuesto de formula (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68562605P | 2005-05-27 | 2005-05-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057034A1 true AR057034A1 (es) | 2007-11-14 |
Family
ID=36997702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060102156A AR057034A1 (es) | 2005-05-27 | 2006-05-24 | Metodos para purificar tigeciclina |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US20070049561A1 (es) |
| EP (1) | EP1890997A1 (es) |
| JP (1) | JP2008545702A (es) |
| KR (1) | KR20080016892A (es) |
| CN (1) | CN101228114A (es) |
| AR (1) | AR057034A1 (es) |
| AU (1) | AU2006252796A1 (es) |
| BR (1) | BRPI0610057A2 (es) |
| CA (1) | CA2609307A1 (es) |
| CR (1) | CR9542A (es) |
| EC (1) | ECSP078050A (es) |
| GT (1) | GT200600224A (es) |
| IL (1) | IL187361A0 (es) |
| MX (1) | MX2007014717A (es) |
| NI (1) | NI200700302A (es) |
| NO (1) | NO20075997L (es) |
| PA (1) | PA8676401A1 (es) |
| PE (1) | PE20070318A1 (es) |
| RU (1) | RU2007143158A (es) |
| TW (1) | TW200716516A (es) |
| WO (1) | WO2006130431A1 (es) |
| ZA (1) | ZA200710174B (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102512429A (zh) | 2005-03-14 | 2012-06-27 | 惠氏公司 | 替加环素组合物及制备方法 |
| AR057649A1 (es) * | 2005-05-27 | 2007-12-12 | Wyeth Corp | Formas solidas cristalinas de tigeciclina y metodos para preparar las mismas |
| AR055336A1 (es) | 2005-06-16 | 2007-08-22 | Wyeth Corp | Proeso de elaboracion para la produccion de tigeciclina como un polvo reconstituible, polvo de tigeciclina liofilizado y producto hecho mediante el proceso |
| US20070244335A1 (en) * | 2006-04-17 | 2007-10-18 | Teva Pharmaceutical Industries Ltd. | Isolation of tetracycline derivatives |
| US8198470B2 (en) | 2006-04-24 | 2012-06-12 | Teva Pharmaceutical Industries Ltd. | Crystalline form II of tigecycline and processes for preparation thereof |
| DE202007019460U1 (de) * | 2006-04-24 | 2012-10-24 | Teva Pharmaceutical Industries Ltd. | Kristalline Tigecyclin-Formen |
| US8198469B2 (en) | 2006-11-29 | 2012-06-12 | Teva Pharmaceutical Industries Ltd. | Crystalline forms of tigecycline and processes for preparation thereof |
| BRPI0706517A2 (pt) * | 2006-11-30 | 2011-03-29 | Teva Pharma | processos para preparação de f 9-haloacetamidominociclinas |
| WO2008106234A1 (en) * | 2007-03-01 | 2008-09-04 | Teva Pharmaceutical Industries Ltd. | Processes for purification of tigecycline |
| AU2008246119A1 (en) * | 2007-04-27 | 2008-11-06 | Paratek Pharmaceuticals, Inc. | Methods for synthesizing and purifying aminoalkyl tetracycline compounds |
| EP2178827A1 (en) * | 2007-06-21 | 2010-04-28 | Sandoz AG | Crystalline solid forms |
| US20090099376A1 (en) * | 2007-10-16 | 2009-04-16 | Wyeth | Tigecycline and methods of preparing intermediates |
| ES2532880T3 (es) | 2007-11-14 | 2015-04-01 | Sandoz Ag | Formas cristalinas del Clorhidrato de Tigeciclina |
| CN101450916B (zh) * | 2007-11-30 | 2012-11-21 | 上海来益生物药物研究开发中心有限责任公司 | 替加环素的合成方法 |
| US20110124893A1 (en) * | 2008-01-23 | 2011-05-26 | Sandoz Ag | Antibiotic compounds |
| CA2746585C (en) | 2008-12-18 | 2017-08-29 | Sandoz Ag | Crystalline form c of tigecycline dihydrochloride and methods for its preparation |
| CA2751238A1 (en) | 2009-03-12 | 2010-10-07 | Wyeth Llc | Nitration of tetracyclines |
| ES2469829T3 (es) * | 2009-11-26 | 2014-06-20 | Sandoz Ag | Reacción de compuestos orgánicos con bajas cantidades de hidrógeno |
| 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 |
| CN103091424B (zh) * | 2013-01-31 | 2014-11-19 | 成都百裕科技制药有限公司 | 替加环素中杂质的检测方法 |
| CN104515820B (zh) * | 2013-10-06 | 2018-08-14 | 山东新时代药业有限公司 | 一种替加环素中间体的分析检测方法 |
| EP3068370A2 (en) | 2013-11-12 | 2016-09-21 | Galenicum Health S.L. | Stable pharmaceutical compositions |
| PT108223B (pt) * | 2015-02-13 | 2018-05-08 | Hovione Farm S A | Novas formas polimórficas de minociclina base e processos para a sua preparação |
| CN105085311A (zh) * | 2015-08-13 | 2015-11-25 | 江苏豪森药业股份有限公司 | 替加环素或其盐的高效纯化方法 |
| CN107304173A (zh) * | 2016-04-25 | 2017-10-31 | 浙江医药股份有限公司新昌制药厂 | 一种替加环素的晶型及其制备方法 |
| CN111978196A (zh) * | 2020-08-03 | 2020-11-24 | 河北圣雪大成制药有限责任公司 | 一种替加环素的纯化方法 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| USRE26271E (en) * | 1967-09-26 | Reductive alkylation process | ||
| US3502696A (en) * | 1961-08-18 | 1970-03-24 | Pfizer & Co C | Antibacterial agents |
| USRE26253E (en) * | 1963-05-17 | 1967-08-15 | And z-alkylamino-g-deoxytetracycline | |
| US3433834A (en) * | 1966-03-14 | 1969-03-18 | American Cyanamid Co | Nitration of 11a-chloro tetracyclines |
| US3849493A (en) * | 1966-08-01 | 1974-11-19 | Pfizer | D-ring substituted 6-deoxytetracyclines |
| US3518306A (en) * | 1968-02-19 | 1970-06-30 | American Cyanamid Co | 7- and/or 9-(n-nitrosoalkylamino)-6-demethyl-6-deoxytetracyclines |
| US3579579A (en) * | 1968-04-18 | 1971-05-18 | American Cyanamid Co | Substituted 7- and/or 9-amino-6-demethyl-6-deoxytetracyclines |
| US4038315A (en) * | 1972-05-11 | 1977-07-26 | American Cyanamid Company | Isolation and recovery of calcium chloride complex of 7-dimethylamino-6-dimethyl l-6-deoxytetracycline hydrochloride |
| US5202449A (en) * | 1987-07-28 | 1993-04-13 | Nippon Kayaku Kabushiki Kaisha | Process for purifying 7-dimethylamino-6-demethyl-6-deoxytetracycline |
| US5141960A (en) * | 1991-06-25 | 1992-08-25 | G. D. Searle & Co. | Tricyclic glycinamide derivatives as anti-convulsants |
| US5494903A (en) * | 1991-10-04 | 1996-02-27 | American Cyanamid Company | 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines |
| US5281628A (en) * | 1991-10-04 | 1994-01-25 | American Cyanamid Company | 9-amino-7-(substituted)-6-demethyl-6-deoxytetracyclines |
| US5420272A (en) * | 1992-08-13 | 1995-05-30 | American Cyanamid Company | 7-(substituted)-8-(substituted)-9-](substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines |
| US5284963A (en) * | 1992-08-13 | 1994-02-08 | American Cyanamid Company | Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines |
| US5442059A (en) * | 1992-08-13 | 1995-08-15 | American Cyanamid Company | 9-[(substituted glycyl)amido)]-6-demethyl-6-deoxytetracyclines |
| US5248797A (en) * | 1992-08-13 | 1993-09-28 | American Cyanamid Company | Method for the production of 9-amino-6-demethyl-6-deoxytetracycline |
| US5328902A (en) * | 1992-08-13 | 1994-07-12 | American Cyanamid Co. | 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines |
| SG47520A1 (en) * | 1992-08-13 | 1998-04-17 | American Cyanamid Co | New method for the production of 9-amino-6-demethyl-6-deoxytetracycline |
| US5371076A (en) * | 1993-04-02 | 1994-12-06 | American Cyanamid Company | 9-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines |
| WO1995022529A1 (en) * | 1994-02-17 | 1995-08-24 | Pfizer Inc. | 9-(substituted amino)-alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics |
| US5675030A (en) * | 1994-11-16 | 1997-10-07 | American Cyanamid Company | Method for selective extracting a 7-(hydrogen or substituted amino)-9- (substituted glycyl) amido!-6-demethyl-6-deoxytetracycline compound |
| US5843925A (en) * | 1994-12-13 | 1998-12-01 | American Cyanamid Company | Methods for inhibiting angiogenesis, proliferation of endothelial or tumor cells and tumor growth |
| US6506740B1 (en) * | 1998-11-18 | 2003-01-14 | Robert A. Ashley | 4-dedimethylaminotetracycline derivatives |
| CZ2003343A3 (cs) * | 2000-07-07 | 2003-05-14 | Trustees Of Tufts College | 7-Substituované tetracyklinové sloučeniny |
-
2006
- 2006-05-24 AR ARP060102156A patent/AR057034A1/es unknown
- 2006-05-25 GT GT200600224A patent/GT200600224A/es unknown
- 2006-05-25 CA CA002609307A patent/CA2609307A1/en not_active Abandoned
- 2006-05-25 RU RU2007143158/04A patent/RU2007143158A/ru not_active Application Discontinuation
- 2006-05-25 BR BRPI0610057-0A patent/BRPI0610057A2/pt not_active IP Right Cessation
- 2006-05-25 MX MX2007014717A patent/MX2007014717A/es not_active Application Discontinuation
- 2006-05-25 WO PCT/US2006/020270 patent/WO2006130431A1/en not_active Ceased
- 2006-05-25 JP JP2008513713A patent/JP2008545702A/ja not_active Withdrawn
- 2006-05-25 TW TW095118594A patent/TW200716516A/zh unknown
- 2006-05-25 PE PE2006000555A patent/PE20070318A1/es not_active Application Discontinuation
- 2006-05-25 KR KR1020077030569A patent/KR20080016892A/ko not_active Withdrawn
- 2006-05-25 AU AU2006252796A patent/AU2006252796A1/en not_active Abandoned
- 2006-05-25 EP EP06771191A patent/EP1890997A1/en not_active Withdrawn
- 2006-05-25 US US11/440,034 patent/US20070049561A1/en not_active Abandoned
- 2006-05-25 PA PA20068676401A patent/PA8676401A1/es unknown
- 2006-05-25 CN CNA2006800267923A patent/CN101228114A/zh active Pending
-
2007
- 2007-11-14 IL IL187361A patent/IL187361A0/en unknown
- 2007-11-22 NI NI200700302A patent/NI200700302A/es unknown
- 2007-11-22 CR CR9542A patent/CR9542A/es not_active Application Discontinuation
- 2007-11-23 NO NO20075997A patent/NO20075997L/no not_active Application Discontinuation
- 2007-11-26 ZA ZA200710174A patent/ZA200710174B/xx unknown
- 2007-12-22 EC EC2007008050A patent/ECSP078050A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| GT200600224A (es) | 2007-01-12 |
| NO20075997L (no) | 2008-02-19 |
| RU2007143158A (ru) | 2009-07-10 |
| ZA200710174B (en) | 2009-08-26 |
| EP1890997A1 (en) | 2008-02-27 |
| TW200716516A (en) | 2007-05-01 |
| KR20080016892A (ko) | 2008-02-22 |
| AU2006252796A1 (en) | 2006-12-07 |
| CA2609307A1 (en) | 2006-12-07 |
| PA8676401A1 (es) | 2009-03-31 |
| WO2006130431A1 (en) | 2006-12-07 |
| JP2008545702A (ja) | 2008-12-18 |
| PE20070318A1 (es) | 2007-04-11 |
| BRPI0610057A2 (pt) | 2010-05-25 |
| MX2007014717A (es) | 2008-02-15 |
| CN101228114A (zh) | 2008-07-23 |
| ECSP078050A (es) | 2008-01-23 |
| IL187361A0 (en) | 2008-04-13 |
| US20070049561A1 (en) | 2007-03-01 |
| CR9542A (es) | 2008-02-20 |
| NI200700302A (es) | 2008-07-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |