AR058284A1 - Proceso ajustable a escala para la preparacion de un 42- ester de rapamicina a partir de un boronato de 42- ester de rapamicina - Google Patents
Proceso ajustable a escala para la preparacion de un 42- ester de rapamicina a partir de un boronato de 42- ester de rapamicinaInfo
- Publication number
- AR058284A1 AR058284A1 ARP060105390A ARP060105390A AR058284A1 AR 058284 A1 AR058284 A1 AR 058284A1 AR P060105390 A ARP060105390 A AR P060105390A AR P060105390 A ARP060105390 A AR P060105390A AR 058284 A1 AR058284 A1 AR 058284A1
- Authority
- AR
- Argentina
- Prior art keywords
- rapamycin ester
- rapamycin
- preparation
- ester
- boronate
- Prior art date
Links
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 abstract 4
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 abstract 4
- 229960002930 sirolimus Drugs 0.000 abstract 4
- 150000002009 diols Chemical class 0.000 abstract 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000001953 recrystallisation Methods 0.000 abstract 1
- 239000011877 solvent mixture Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicacion 1: Un proceso para la preparacion de 42-éster de rapamicina que comprende los siguientes pasos: (a) hacer reaccionar un boronato de 42-éster de rapamicina con un diol en una mezcla de solvente para producir 42-éster de rapamicina crudo y (b) purificar el 42-éster de rapamicina crudo mediante recristalizacion y tratamiento con un diol.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74814305P | 2005-12-07 | 2005-12-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR058284A1 true AR058284A1 (es) | 2008-01-30 |
Family
ID=37813522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105390A AR058284A1 (es) | 2005-12-07 | 2006-12-06 | Proceso ajustable a escala para la preparacion de un 42- ester de rapamicina a partir de un boronato de 42- ester de rapamicina |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7622578B2 (es) |
| EP (1) | EP1957501A2 (es) |
| JP (1) | JP2009518412A (es) |
| KR (1) | KR20080077619A (es) |
| CN (1) | CN101321770A (es) |
| AR (1) | AR058284A1 (es) |
| AU (1) | AU2006322024A1 (es) |
| BR (1) | BRPI0619578A2 (es) |
| CA (1) | CA2630645A1 (es) |
| CR (1) | CR9986A (es) |
| EC (1) | ECSP088516A (es) |
| GT (1) | GT200800087A (es) |
| IL (1) | IL191550A0 (es) |
| NO (1) | NO20082375L (es) |
| PE (1) | PE20070748A1 (es) |
| RU (2) | RU2008120670A (es) |
| TW (1) | TW200804399A (es) |
| WO (1) | WO2007067560A2 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI307277B (en) * | 2002-07-30 | 2009-03-11 | Wyeth Corp | Parenteral formulations |
| WO2007075621A1 (en) * | 2005-12-20 | 2007-07-05 | Wyeth | Control of cci-779 dosage form stability through control of drug substance impurities |
| TW200824713A (en) * | 2006-10-18 | 2008-06-16 | Wyeth Corp | Processes for the synthesis of individual isomers of mono-PEG CCI-779 |
| CN102020661B (zh) * | 2011-01-07 | 2013-02-13 | 天津市炜杰科技有限公司 | 一种驮瑞塞尔合成方法 |
| EP2694520A1 (en) | 2011-04-01 | 2014-02-12 | Sandoz AG | Regioselective acylation of rapamycin at the c-42 position |
| US9446977B2 (en) | 2012-12-10 | 2016-09-20 | Corning Incorporated | Method and system for making a glass article with uniform mold temperature |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5358909A (en) * | 1991-02-27 | 1994-10-25 | Nippon Steel Corporation | Method of manufacturing field-emitter |
| US5358908A (en) * | 1992-02-14 | 1994-10-25 | Micron Technology, Inc. | Method of creating sharp points and other features on the surface of a semiconductor substrate |
| US5385908A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered esters of rapamycin |
| US5385909A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
| US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| US6277983B1 (en) * | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| JP2004509898A (ja) * | 2000-09-19 | 2004-04-02 | ワイス | 水溶性ラパマイシンエステル |
| DK1658295T3 (da) | 2003-08-07 | 2007-09-24 | Wyeth Corp | Regioselektiv syntese af CCI-779 |
| WO2005023254A1 (en) * | 2003-09-03 | 2005-03-17 | Wyeth | Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and its pharmaceutical compositions containing the same |
| US7202256B2 (en) * | 2004-04-14 | 2007-04-10 | Wyeth | Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 |
| DE602005010228D1 (de) * | 2004-04-14 | 2008-11-20 | Wyeth Corp | Verfahren zur herstellung von rapamycin-42-estern und fk-506-32-estern mit dicarbonsäure, vorstufen für rapamycinkonjugate und antikörper |
| BRPI0509852A (pt) * | 2004-04-14 | 2007-10-23 | Wyeth Corp | método para a preparação regioespecìfica dos derivados de 42-éster de rapamicina, preparação regioespecìfica do 42-éster de rapamicina, composição, produto, e, kit farmacêutico |
| GT200500216A (es) * | 2004-08-10 | 2006-03-02 | Derivados de cci-779 y metodos para su preparacion | |
| WO2006068932A2 (en) * | 2004-12-20 | 2006-06-29 | Wyeth | Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders |
| CA2590254A1 (en) * | 2004-12-20 | 2006-06-29 | Wyeth | Rapamycin derivatives and the uses thereof in the treatment of neurological disorders |
| CN101115759A (zh) * | 2005-02-09 | 2008-01-30 | 惠氏公司 | Cci-779多晶形物及其应用 |
| JP2008531685A (ja) * | 2005-03-02 | 2008-08-14 | ワイス | 母液からのcci−779の回収 |
| WO2006096325A1 (en) * | 2005-03-07 | 2006-09-14 | Wyeth | Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin |
-
2006
- 2006-12-06 BR BRPI0619578-4A patent/BRPI0619578A2/pt not_active IP Right Cessation
- 2006-12-06 US US11/634,707 patent/US7622578B2/en not_active Expired - Fee Related
- 2006-12-06 CN CNA2006800457190A patent/CN101321770A/zh active Pending
- 2006-12-06 TW TW095145391A patent/TW200804399A/zh unknown
- 2006-12-06 AU AU2006322024A patent/AU2006322024A1/en not_active Abandoned
- 2006-12-06 CA CA002630645A patent/CA2630645A1/en not_active Abandoned
- 2006-12-06 JP JP2008544446A patent/JP2009518412A/ja not_active Withdrawn
- 2006-12-06 PE PE2006001557A patent/PE20070748A1/es not_active Application Discontinuation
- 2006-12-06 KR KR1020087013750A patent/KR20080077619A/ko not_active Withdrawn
- 2006-12-06 WO PCT/US2006/046434 patent/WO2007067560A2/en not_active Ceased
- 2006-12-06 RU RU2008120670/04A patent/RU2008120670A/ru not_active Application Discontinuation
- 2006-12-06 AR ARP060105390A patent/AR058284A1/es unknown
- 2006-12-06 EP EP06839035A patent/EP1957501A2/en not_active Withdrawn
-
2008
- 2008-05-19 IL IL191550A patent/IL191550A0/en unknown
- 2008-05-19 CR CR9986A patent/CR9986A/es not_active Application Discontinuation
- 2008-05-26 NO NO20082375A patent/NO20082375L/no not_active Application Discontinuation
- 2008-06-05 GT GT200800087A patent/GT200800087A/es unknown
- 2008-06-09 EC EC2008008516A patent/ECSP088516A/es unknown
- 2008-10-27 RU RU2008142554/04A patent/RU2008142554A/ru unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US7622578B2 (en) | 2009-11-24 |
| CN101321770A (zh) | 2008-12-10 |
| TW200804399A (en) | 2008-01-16 |
| IL191550A0 (en) | 2008-12-29 |
| JP2009518412A (ja) | 2009-05-07 |
| AU2006322024A1 (en) | 2007-06-14 |
| RU2008120670A (ru) | 2010-01-20 |
| PE20070748A1 (es) | 2007-08-08 |
| WO2007067560A2 (en) | 2007-06-14 |
| NO20082375L (no) | 2008-09-04 |
| KR20080077619A (ko) | 2008-08-25 |
| EP1957501A2 (en) | 2008-08-20 |
| BRPI0619578A2 (pt) | 2011-10-04 |
| CR9986A (es) | 2008-08-21 |
| US20070129541A1 (en) | 2007-06-07 |
| WO2007067560A3 (en) | 2007-08-02 |
| ECSP088516A (es) | 2008-07-30 |
| CA2630645A1 (en) | 2007-06-14 |
| GT200800087A (es) | 2008-10-06 |
| RU2008142554A (ru) | 2010-05-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |