PE20070748A1 - 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
- PE20070748A1 PE20070748A1 PE2006001557A PE2006001557A PE20070748A1 PE 20070748 A1 PE20070748 A1 PE 20070748A1 PE 2006001557 A PE2006001557 A PE 2006001557A PE 2006001557 A PE2006001557 A PE 2006001557A PE 20070748 A1 PE20070748 A1 PE 20070748A1
- Authority
- PE
- Peru
- Prior art keywords
- rapamycin
- ester
- crude
- boronate
- preparation
- Prior art date
Links
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
SE REFIERE A UN PROCEDIMIENTO DE PREPARACION DE UN 42-ESTER DE RAPAMICINA QUE COMPRENDE: A) HACER REACCIONAR UN BORONATO DE 42-ESTER DE RAPAMICINA QUE SE ENCUENTRA EN UNA CANTIDAD DE 10% A 30% EN PESO CON UN DIOL TAL COMO 2-METIL-2,4-PENTANDIOL EN UNA MEZCLA DE SOLVENTES TAL COMO ETER DIETILICO Y HEPTANO QUE SE ENCUENTRAN EN UNA PROPORCION DE 1:1 A 2:1, PARA PRODUCIR 42-ESTER DE RAPAMICINA CRUDO; EN DONDE LA RELACION MOLAR DEL DIOL Y EL BORONATO DE 42-ESTER DE RAPAMICINA ES DE 5:1 A 10:1 Y LA TEMPERATURA DE REACCION ES DE 30ºC A 40ºC; Y B) PURIFICAR EL 42-ESTER DE RAPAMICINA CRUDO MEDIANTE RECRISTALIZACION QUE COMPRENDE i) DISOLVER EL 42-ESTER DE RAPAMICINA CRUDO EN UN SOLVENTE POLAR TAL COMO ACETONA; ii) FILTRAR LA SUSPENSION Y CONCENTRAR EL FILTRADO DEL 42-ESTER DE RAPAMICINA CRUDO PARA DAR UNA ESPUMA QUE SERA DISUELTA EN ETER DIETILICO; Y iii) REACCIONAR EL 42-ESTER DE RAPAMICINA CRUDO CON DIOL A UNA TEMPERATURA DE 20ºC A 25ºC. DICHO PROCEDIMIENTO EVITA LA UTILIZACION DEL TETRAHIDROFURANO COMO SOLVENTE, EL CUAL DIFICULTA EL AISLAMIENTO DEL 42-ESTER DE RAPAMICINA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74814305P | 2005-12-07 | 2005-12-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20070748A1 true PE20070748A1 (es) | 2007-08-08 |
Family
ID=37813522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006001557A PE20070748A1 (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 |
|---|---|---|---|---|
| RU2344821C2 (ru) | 2002-07-30 | 2009-01-27 | Уайт | Парентеральные композиции, содержащие гидроксиэфиры рапамицина |
| EP1962819A1 (en) * | 2005-12-20 | 2008-09-03 | 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 |
| US5385909A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Heterocyclic esters of rapamycin |
| US5385908A (en) | 1993-11-22 | 1995-01-31 | American Home Products Corporation | Hindered 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 |
| WO2002024706A2 (en) * | 2000-09-19 | 2002-03-28 | Wyeth | Water soluble rapamycin esters |
| ES2287772T3 (es) * | 2003-08-07 | 2007-12-16 | Wyeth | Sintesis regioselectiva de cci-779. |
| KR20060090803A (ko) * | 2003-09-03 | 2006-08-16 | 와이어쓰 | 3-하이드록시-2-(하이드록시메틸)-2-메틸프로피온산을 갖는무정형 라파마이신 42-에스테르 및 이를 함유하는약제학적 조성물 |
| WO2005100366A1 (en) | 2004-04-14 | 2005-10-27 | Wyeth | Proline cci-779 (proline-rapamycin 42-ester with 2,2-bis (hydroxymethyl) propionic acid) and two-step enzymatic synthesis of proline cci-779 and cci-779 using microbial lipase |
| US7268144B2 (en) * | 2004-04-14 | 2007-09-11 | Wyeth | Regiospecific synthesis of rapamycin 42-ester derivatives |
| DK1735321T3 (da) * | 2004-04-14 | 2009-01-12 | Wyeth Corp | Fremgangsmåde til fremstilling af rapamycin 42-estere og FK-506 32-estere med dicarboxylsyre, precursors for rapamycinkonjugater og antistoffer |
| GT200500216A (es) * | 2004-08-10 | 2006-03-02 | Derivados de cci-779 y metodos para su preparacion | |
| CN101084227B (zh) * | 2004-12-20 | 2011-11-16 | 惠氏公司 | 雷帕霉素类似物及其治疗神经紊乱、增殖性和炎性疾病的用途 |
| CN101084226A (zh) * | 2004-12-20 | 2007-12-05 | 惠氏公司 | 雷帕霉素衍生物及其治疗神经紊乱的用途 |
| KR20070107030A (ko) * | 2005-02-09 | 2007-11-06 | 와이어쓰 | Ｃｃｉ-７７９ 다형체 및 그의 용도 |
| MX2007010715A (es) * | 2005-03-02 | 2007-10-12 | Wyeth Corp | Recuperacion de cc-779 a partir de soluciones madre. |
| MX2007010892A (es) * | 2005-03-07 | 2007-12-05 | Wyeth Corp | Isomero de oxepano de 42-o-(2-hidroxi)etil-rapamicina. |
-
2006
- 2006-12-06 BR BRPI0619578-4A patent/BRPI0619578A2/pt not_active IP Right Cessation
- 2006-12-06 EP EP06839035A patent/EP1957501A2/en not_active Withdrawn
- 2006-12-06 TW TW095145391A patent/TW200804399A/zh unknown
- 2006-12-06 AR ARP060105390A patent/AR058284A1/es unknown
- 2006-12-06 RU RU2008120670/04A patent/RU2008120670A/ru not_active Application Discontinuation
- 2006-12-06 WO PCT/US2006/046434 patent/WO2007067560A2/en active Application Filing
- 2006-12-06 JP JP2008544446A patent/JP2009518412A/ja not_active Withdrawn
- 2006-12-06 KR KR1020087013750A patent/KR20080077619A/ko not_active Application Discontinuation
- 2006-12-06 CA CA002630645A patent/CA2630645A1/en not_active Abandoned
- 2006-12-06 CN CNA2006800457190A patent/CN101321770A/zh active Pending
- 2006-12-06 PE PE2006001557A patent/PE20070748A1/es not_active Application Discontinuation
- 2006-12-06 US US11/634,707 patent/US7622578B2/en not_active Expired - Fee Related
- 2006-12-06 AU AU2006322024A patent/AU2006322024A1/en not_active Abandoned
-
2008
- 2008-05-19 CR CR9986A patent/CR9986A/es not_active Application Discontinuation
- 2008-05-19 IL IL191550A patent/IL191550A0/en unknown
- 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 |
|---|---|
| WO2007067560A3 (en) | 2007-08-02 |
| AU2006322024A1 (en) | 2007-06-14 |
| ECSP088516A (es) | 2008-07-30 |
| JP2009518412A (ja) | 2009-05-07 |
| NO20082375L (no) | 2008-09-04 |
| WO2007067560A2 (en) | 2007-06-14 |
| CA2630645A1 (en) | 2007-06-14 |
| EP1957501A2 (en) | 2008-08-20 |
| CR9986A (es) | 2008-08-21 |
| RU2008120670A (ru) | 2010-01-20 |
| TW200804399A (en) | 2008-01-16 |
| BRPI0619578A2 (pt) | 2011-10-04 |
| KR20080077619A (ko) | 2008-08-25 |
| US7622578B2 (en) | 2009-11-24 |
| AR058284A1 (es) | 2008-01-30 |
| GT200800087A (es) | 2008-10-06 |
| CN101321770A (zh) | 2008-12-10 |
| RU2008142554A (ru) | 2010-05-10 |
| US20070129541A1 (en) | 2007-06-07 |
| IL191550A0 (en) | 2008-12-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FX | Voluntary withdrawal |