PE20080138A1 - Procesos para preparar conjugados de polietilen glicol solubles en agua de inmunosupresores macrolidos - Google Patents
Procesos para preparar conjugados de polietilen glicol solubles en agua de inmunosupresores macrolidosInfo
- Publication number
- PE20080138A1 PE20080138A1 PE2007000234A PE2007000234A PE20080138A1 PE 20080138 A1 PE20080138 A1 PE 20080138A1 PE 2007000234 A PE2007000234 A PE 2007000234A PE 2007000234 A PE2007000234 A PE 2007000234A PE 20080138 A1 PE20080138 A1 PE 20080138A1
- Authority
- PE
- Peru
- Prior art keywords
- macrolide
- polyethylene glycol
- macrolid
- immunosuppressors
- processes
- Prior art date
Links
- 229920001223 polyethylene glycol Polymers 0.000 title abstract 3
- 239000002202 Polyethylene glycol Substances 0.000 title abstract 2
- 239000003120 macrolide antibiotic agent Substances 0.000 abstract 5
- 239000003018 immunosuppressive agent Substances 0.000 abstract 3
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[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 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 abstract 2
- 229960003444 immunosuppressant agent Drugs 0.000 abstract 2
- 229960000235 temsirolimus Drugs 0.000 abstract 2
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[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 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 abstract 1
- 102000004882 Lipase Human genes 0.000 abstract 1
- 108090001060 Lipase Proteins 0.000 abstract 1
- 239000004367 Lipase Substances 0.000 abstract 1
- 210000001744 T-lymphocyte Anatomy 0.000 abstract 1
- QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical group 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
- 230000000845 anti-microbial effect Effects 0.000 abstract 1
- ZDQSOHOQTUFQEM-PKUCKEGBSA-N ascomycin Chemical group 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 Chemical group 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
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229960005167 everolimus Drugs 0.000 abstract 1
- 230000001861 immunosuppressant effect Effects 0.000 abstract 1
- 235000019421 lipase Nutrition 0.000 abstract 1
- 229920001427 mPEG Polymers 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- JXOHGGNKMLTUBP-HSUXUTPPSA-N shikimic acid Chemical compound O[C@@H]1CC(C(O)=O)=C[C@@H](O)[C@H]1O JXOHGGNKMLTUBP-HSUXUTPPSA-N 0.000 abstract 1
- JXOHGGNKMLTUBP-JKUQZMGJSA-N shikimic acid Natural products O[C@@H]1CC(C(O)=O)=C[C@H](O)[C@@H]1O JXOHGGNKMLTUBP-JKUQZMGJSA-N 0.000 abstract 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical group 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 1
- QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 abstract 1
- 150000003573 thiols Chemical class 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
-
- 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
-
- 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 REFIERE A UN PROCESO PARA PREPARAR CONJUGADOS DE POLIETILEN GLICOL SOLUBLES EN AGUA DE MACROLIDOS INMUNOSUPRESORES, QUE COMPRENDEN: a) HACER REACCIONAR UN AGENTE ACILADOR CON UN MACROLIDO INMUNOSUPRESOR QUE TIENE UNA REGION CICLOHEXILO DERIVADA DEL ACIDO SHIKIMICO EN PRESENCIA DE UNA LIPASA PARA FORMAR UN MACROLIDO ACILADO; b) HACER REACCIONAR EL MACROLIDO ACILADO CON UN DERIVADO DE METOXI POLI(ETILEN GLICOL) O UN DERIVADO DE POLI(ETILEN GLICOL) TIOL TERMINAL, EN PRESENCIA DE UNA BASE. DONDE DICHO MACROLIDO INMUNOSUPRESOR ES RAPAMICINA (SIROLIMUS) O DERIVADOS TAL COMO EVEROLIMUS, TEMSIROLIMUS (CCI-779) REGIOESPECIFICAMENTE ACILADA EN LA POSICION 42, O TACROLIMUS (FK506) Y ASCOMICINA (FK520) REGIOESPECIFICAMENTE ACILADAS EN LA POSICION 32, ENTRE OTROS. ESTOS COMPUESTOS SUPRIMEN LA ACTIVIDAD DE LAS CELULAS T Y PRESENTAN ACTIVIDAD ANTIMICROBIANA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US77993906P | 2006-03-07 | 2006-03-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20080138A1 true PE20080138A1 (es) | 2008-03-05 |
Family
ID=38420553
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000234A PE20080138A1 (es) | 2006-03-07 | 2007-03-05 | Procesos para preparar conjugados de polietilen glicol solubles en agua de inmunosupresores 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 (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20060642A1 (es) * | 2004-08-10 | 2006-08-01 | Wyeth Corp | Derivados de 42-ester de rapamicina con acido 2,2-bis(hidoximetil)propionico (cci-779) y metodos para su preparacion |
| 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 |
| CN104203959B (zh) * | 2012-06-08 | 2017-09-15 | 百多力股份公司 | 雷帕霉素40‑o‑环状烃酯、组合物和方法 |
| ES2700824T3 (es) | 2012-08-16 | 2019-02-19 | Pfizer | Procedimientos y composiciones de glucoconjugación |
| 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 |
| US20210023232A1 (en) * | 2018-03-29 | 2021-01-28 | Jenkem Technology Co., Ltd. (Tianjin) | Combination of polyethylene glycol and rapamycin and use thereof |
| US20230226016A1 (en) * | 2020-05-29 | 2023-07-20 | The Regents Of University Of California | Agents and methods for treating tauopathies |
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 |
| DE60136200D1 (de) * | 2000-09-19 | 2008-11-27 | Wyeth Corp | Wasserlösliche rapamycin-ester |
| SG152234A1 (en) * | 2004-04-14 | 2009-05-29 | Wyeth Corp | Regiospecific synthesis of rapamycin 42-ester derivatives |
| CN1942478A (zh) | 2004-04-14 | 2007-04-04 | 惠氏公司 | 用于制备与二羧酸的纳巴霉素42－酯和fk－506 32－酯的方法，用于纳巴霉素配合物的前体和抗体 |
-
2007
- 2007-03-05 KR KR1020087021729A patent/KR20080106225A/ko not_active Application Discontinuation
- 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 TW TW096107516A patent/TW200812622A/zh unknown
- 2007-03-05 CN CNA2007800079204A patent/CN101394867A/zh not_active Withdrawn
- 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 JP JP2008558347A patent/JP2009529050A/ja active Pending
- 2007-03-05 BR BRPI0708562-1A patent/BRPI0708562A2/pt not_active Application Discontinuation
- 2007-03-05 AU AU2007223963A patent/AU2007223963A1/en not_active Abandoned
- 2007-03-05 CA CA002644156A patent/CA2644156A1/en not_active Abandoned
- 2007-03-05 RU RU2008134369/15A patent/RU2008134369A/ru not_active Application Discontinuation
- 2007-03-05 AR ARP070100901A patent/AR059740A1/es unknown
- 2007-03-05 WO PCT/US2007/005646 patent/WO2007103348A2/en active Application Filing
-
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 |
|---|---|
| NO20083716L (no) | 2008-10-06 |
| TW200812622A (en) | 2008-03-16 |
| AU2007223963A1 (en) | 2007-09-13 |
| SV2009003017A (es) | 2009-03-04 |
| US20070212371A1 (en) | 2007-09-13 |
| BRPI0708562A2 (pt) | 2011-06-07 |
| ECSP088719A (es) | 2008-10-31 |
| CA2644156A1 (en) | 2007-09-13 |
| WO2007103348A2 (en) | 2007-09-13 |
| CN101394867A (zh) | 2009-03-25 |
| US7605257B2 (en) | 2009-10-20 |
| RU2008134369A (ru) | 2010-04-20 |
| IL193636A0 (en) | 2009-05-04 |
| JP2009529050A (ja) | 2009-08-13 |
| KR20080106225A (ko) | 2008-12-04 |
| EP1993610A2 (en) | 2008-11-26 |
| WO2007103348A3 (en) | 2008-05-08 |
| CR10234A (es) | 2008-10-29 |
| MX2008011458A (es) | 2008-09-24 |
| AR059740A1 (es) | 2008-04-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FX | Voluntary withdrawal |