ECSP088719A - Procedimiento para preparar conjugados de polietilenglicol solubles en agua de inmunosupresores de macrolidos - Google Patents
Procedimiento para preparar conjugados de polietilenglicol solubles en agua de inmunosupresores de macrolidosInfo
- Publication number
- ECSP088719A ECSP088719A EC2008008719A ECSP088719A ECSP088719A EC SP088719 A ECSP088719 A EC SP088719A EC 2008008719 A EC2008008719 A EC 2008008719A EC SP088719 A ECSP088719 A EC SP088719A EC SP088719 A ECSP088719 A EC SP088719A
- Authority
- EC
- Ecuador
- Prior art keywords
- macrolidos
- immunosuppressors
- polyethylenglycol
- conjugates
- procedure
- Prior art date
Links
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 title 1
- 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 3
- 102000004882 Lipase Human genes 0.000 abstract 1
- 108090001060 Lipase Proteins 0.000 abstract 1
- 239000004367 Lipase Substances 0.000 abstract 1
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 abstract 1
- ZDQSOHOQTUFQEM-PKUCKEGBSA-N ascomycin Chemical compound C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C\C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](O)[C@H](OC)C1 ZDQSOHOQTUFQEM-PKUCKEGBSA-N 0.000 abstract 1
- ZDQSOHOQTUFQEM-XCXYXIJFSA-N ascomycin Natural products CC[C@H]1C=C(C)C[C@@H](C)C[C@@H](OC)[C@H]2O[C@@](O)([C@@H](C)C[C@H]2OC)C(=O)C(=O)N3CCCC[C@@H]3C(=O)O[C@H]([C@H](C)[C@@H](O)CC1=O)C(=C[C@@H]4CC[C@@H](O)[C@H](C4)OC)C ZDQSOHOQTUFQEM-XCXYXIJFSA-N 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 150000002334 glycols Chemical class 0.000 abstract 1
- 235000019421 lipase Nutrition 0.000 abstract 1
- 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 1
- 229960002930 sirolimus Drugs 0.000 abstract 1
- 229960001967 tacrolimus Drugs 0.000 abstract 1
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Transplantation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicinal Preparation (AREA)
Abstract
Se describen procedimientos para preparar rapamicinas 42-pegiladas incluyendo hacer reaccionar una rapamicina con un agente de acilación en presencia de una lipasa para formar una rapamicina acilada y hacer reaccionar la rapamicina acilada o un derivado de metoxipolietilenglicol en presencia de una base; también se describen procedimientos para preparar tacrolimo y/o ascomicina 32-pegilados utilizando estos pasos
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US77993906P | 2006-03-07 | 2006-03-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP088719A true ECSP088719A (es) | 2008-10-31 |
Family
ID=38420553
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2008008719A ECSP088719A (es) | 2006-03-07 | 2008-09-05 | Procedimiento para preparar conjugados de polietilenglicol solubles en agua de inmunosupresores de macrolidos |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7605257B2 (es) |
| EP (1) | EP1993610A2 (es) |
| JP (1) | JP2009529050A (es) |
| KR (1) | KR20080106225A (es) |
| CN (1) | CN101394867A (es) |
| AR (1) | AR059740A1 (es) |
| AU (1) | AU2007223963A1 (es) |
| BR (1) | BRPI0708562A2 (es) |
| CA (1) | CA2644156A1 (es) |
| CR (1) | CR10234A (es) |
| EC (1) | ECSP088719A (es) |
| IL (1) | IL193636A0 (es) |
| MX (1) | MX2008011458A (es) |
| NO (1) | NO20083716L (es) |
| PE (1) | PE20080138A1 (es) |
| RU (1) | RU2008134369A (es) |
| SV (1) | SV2009003017A (es) |
| TW (1) | TW200812622A (es) |
| WO (1) | WO2007103348A2 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2577011A1 (en) * | 2004-08-10 | 2006-04-13 | Wyeth | Cci-779 derivatives and methods of making same |
| TW200824713A (en) * | 2006-10-18 | 2008-06-16 | Wyeth Corp | Processes for the synthesis of individual isomers of mono-PEG CCI-779 |
| TW200845960A (en) * | 2007-04-05 | 2008-12-01 | Wyeth Corp | Wortmannin-rapalog conjugate and uses thereof |
| IT1394309B1 (it) * | 2009-05-22 | 2012-06-06 | Poli Ind Chimica Spa | Nuovo approccio chimico-enzimatico alla sintesi del pimecrolimus |
| ES2574522T3 (es) * | 2012-06-08 | 2016-06-20 | Biotronik Ag | Ésteres 40-O-hidrocarburo cíclico de rapamicina, composiciones y procedimientos |
| DK2885007T3 (en) * | 2012-08-16 | 2018-12-03 | Pfizer | Methods for glycoconjugation and compositions |
| WO2014145780A1 (en) | 2013-03-15 | 2014-09-18 | Biosensors International Group, Ltd. | Purification of rapamycin derivatives |
| WO2015081821A1 (zh) * | 2013-12-02 | 2015-06-11 | 北京键凯科技有限公司 | 聚乙二醇-多爪寡肽键合的雷帕霉素衍生物 |
| CN109311910B (zh) | 2016-03-24 | 2022-02-01 | 杜兰教育基金委员会 | 他克莫司偶联物、其组合物、及其用途 |
| CN108641075B (zh) * | 2018-03-05 | 2019-12-06 | 江苏千之康生物医药科技有限公司 | 一类雷帕霉素及其衍生物的双短链聚乙二醇前药及其应用 |
| CN110314236A (zh) * | 2018-03-29 | 2019-10-11 | 天津键凯科技有限公司 | 聚乙二醇与雷帕霉素的结合物及其用途 |
| EP4157241A4 (en) * | 2020-05-29 | 2025-01-08 | The Regents of the University of California | AGENTS AND METHODS FOR THE TREATMENT OF TAUOPATHIES |
| CN115160559B (zh) * | 2021-04-02 | 2024-02-02 | 杭州宜生医药科技发展有限公司 | 一种peg化雷帕霉素化合物及其制备方法与应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| US5780462A (en) | 1995-12-27 | 1998-07-14 | American Home Products Corporation | Water soluble rapamycin esters |
| KR100244164B1 (ko) | 1997-07-15 | 2000-03-02 | 김용옥 | 수용성 고분자-타크로리무스 접합체 화합물 및 그의 제조 방법 |
| US6331547B1 (en) | 1999-08-18 | 2001-12-18 | American Home Products Corporation | Water soluble SDZ RAD esters |
| US6277983B1 (en) | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| ATE411321T1 (de) | 2000-09-19 | 2008-10-15 | Wyeth Corp | Wasserlösliche rapamycin-ester |
| JP4224115B2 (ja) | 2004-04-14 | 2009-02-12 | ワイス | ラパマイシン４２−エステル誘導体の位置特異的合成 |
| PL1735321T3 (pl) | 2004-04-14 | 2009-04-30 | Wyeth Corp | Proces wytwarzania 42-estrów rapamycyny i 32-estrów FK-506 z kwasem dikarboksylowym, prekursory koniugatów rapamycyny oraz przeciwciała |
-
2007
- 2007-03-05 CN CNA2007800079204A patent/CN101394867A/zh not_active Withdrawn
- 2007-03-05 AU AU2007223963A patent/AU2007223963A1/en not_active Abandoned
- 2007-03-05 AR ARP070100901A patent/AR059740A1/es unknown
- 2007-03-05 RU RU2008134369/15A patent/RU2008134369A/ru not_active Application Discontinuation
- 2007-03-05 KR KR1020087021729A patent/KR20080106225A/ko not_active Withdrawn
- 2007-03-05 JP JP2008558347A patent/JP2009529050A/ja active Pending
- 2007-03-05 EP EP07752356A patent/EP1993610A2/en not_active Withdrawn
- 2007-03-05 PE PE2007000234A patent/PE20080138A1/es not_active Application Discontinuation
- 2007-03-05 MX MX2008011458A patent/MX2008011458A/es unknown
- 2007-03-05 US US11/713,973 patent/US7605257B2/en not_active Expired - Fee Related
- 2007-03-05 CA CA002644156A patent/CA2644156A1/en not_active Abandoned
- 2007-03-05 TW TW096107516A patent/TW200812622A/zh unknown
- 2007-03-05 WO PCT/US2007/005646 patent/WO2007103348A2/en not_active Ceased
- 2007-03-05 BR BRPI0708562-1A patent/BRPI0708562A2/pt not_active Application Discontinuation
-
2008
- 2008-08-21 CR CR10234A patent/CR10234A/es not_active Application Discontinuation
- 2008-08-21 IL IL193636A patent/IL193636A0/en unknown
- 2008-08-29 NO NO20083716A patent/NO20083716L/no not_active Application Discontinuation
- 2008-09-05 EC EC2008008719A patent/ECSP088719A/es unknown
- 2008-09-05 SV SV2008003017A patent/SV2009003017A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2007223963A1 (en) | 2007-09-13 |
| US7605257B2 (en) | 2009-10-20 |
| NO20083716L (no) | 2008-10-06 |
| KR20080106225A (ko) | 2008-12-04 |
| CN101394867A (zh) | 2009-03-25 |
| PE20080138A1 (es) | 2008-03-05 |
| BRPI0708562A2 (pt) | 2011-06-07 |
| WO2007103348A2 (en) | 2007-09-13 |
| EP1993610A2 (en) | 2008-11-26 |
| WO2007103348A3 (en) | 2008-05-08 |
| CR10234A (es) | 2008-10-29 |
| IL193636A0 (en) | 2009-05-04 |
| TW200812622A (en) | 2008-03-16 |
| RU2008134369A (ru) | 2010-04-20 |
| JP2009529050A (ja) | 2009-08-13 |
| US20070212371A1 (en) | 2007-09-13 |
| AR059740A1 (es) | 2008-04-23 |
| MX2008011458A (es) | 2008-09-24 |
| SV2009003017A (es) | 2009-03-04 |
| CA2644156A1 (en) | 2007-09-13 |
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