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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 macrolidos

Info

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
Application number
PE2007000234A
Other languages
English (en)
Inventor
Jianxin Gu
Mark Ruppen
Tianmin Zhu
Mahdi Fawzi
Original Assignee
Wyeth Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of PE20080138A1 publication Critical patent/PE20080138A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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
PE2007000234A 2006-03-07 2007-03-05 Procesos para preparar conjugados de polietilen glicol solubles en agua de inmunosupresores macrolidos PE20080138A1 (es)

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 (13)

* Cited by examiner, † Cited by third party
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
PL2859001T3 (pl) * 2012-06-08 2016-08-31 Biotronik Ag 40-o-podstawiona pochodna estrowa rapamycyny i węglowodoru cyklicznego, kompozycje i metody
HUE049531T2 (hu) * 2012-08-16 2020-10-28 Pfizer Glikokonjugációs eljárások és kompozíciók
CN105102967B (zh) 2013-03-15 2018-10-12 生物传感器国际集团有限公司 雷帕霉素衍生物的纯化
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
AU2017238246B2 (en) 2016-03-24 2021-04-01 The Administrators Of The Tulane Educational Fund Conjugates of tacrolimus, their compositions, and their uses
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
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)

* Cited by examiner, † Cited by third party
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
WO2005105811A1 (en) * 2004-04-14 2005-11-10 Wyeth Regiospecific synthesis of rapamycin 42-ester derivatives
EP1735321B1 (en) * 2004-04-14 2008-10-08 Wyeth Process for preparing rapamycin 42-esters and fk-506 32-esters with dicarboxylic acid, precursors for rapamycin conjugates and antibodies

Also Published As

Publication number Publication date
CR10234A (es) 2008-10-29
WO2007103348A3 (en) 2008-05-08
AU2007223963A1 (en) 2007-09-13
NO20083716L (no) 2008-10-06
JP2009529050A (ja) 2009-08-13
SV2009003017A (es) 2009-03-04
US20070212371A1 (en) 2007-09-13
MX2008011458A (es) 2008-09-24
US7605257B2 (en) 2009-10-20
BRPI0708562A2 (pt) 2011-06-07
RU2008134369A (ru) 2010-04-20
KR20080106225A (ko) 2008-12-04
IL193636A0 (en) 2009-05-04
ECSP088719A (es) 2008-10-31
EP1993610A2 (en) 2008-11-26
WO2007103348A2 (en) 2007-09-13
CA2644156A1 (en) 2007-09-13
TW200812622A (en) 2008-03-16
CN101394867A (zh) 2009-03-25
AR059740A1 (es) 2008-04-23

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