ECSP066413A - Sintesis regioselectiva del cci-779 - Google Patents

Sintesis regioselectiva del cci-779

Info

Publication number
ECSP066413A
ECSP066413A EC2006006413A ECSP066413A ECSP066413A EC SP066413 A ECSP066413 A EC SP066413A EC 2006006413 A EC2006006413 A EC 2006006413A EC SP066413 A ECSP066413 A EC SP066413A EC SP066413 A ECSP066413 A EC SP066413A
Authority
EC
Ecuador
Prior art keywords
cci
element synthesis
regional element
synthesis
regional
Prior art date
Application number
EC2006006413A
Other languages
English (en)
Inventor
Warren Chew
Chia-Cheng Shaw
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 ECSP066413A publication Critical patent/ECSP066413A/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
    • C07D498/02Heterocyclic 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 two hetero rings
    • C07D498/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D498/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Catalysts (AREA)

Abstract

Esta invención provee una síntesis regioselectiva del éster 42 de rapamicina con el ácido 3-hidroxi-2-(hidroximetil)-2-metil propiónico (CCI-779) basada en la química del ácido borónico. Esta invención sobrelleva la complejidad y, a menudo, la purificación laboriosa del monoéster-42 de rapmicina obtenida usando métodos primarios. Otros aspectos y ventajas de la presente invención serán fácilmente aparentes de la descripción detallada siguiente de la invención.
EC2006006413A 2003-08-07 2006-03-07 Sintesis regioselectiva del cci-779 ECSP066413A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49324903P 2003-08-07 2003-08-07

Publications (1)

Publication Number Publication Date
ECSP066413A true ECSP066413A (es) 2006-09-18

Family

ID=34193170

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2006006413A ECSP066413A (es) 2003-08-07 2006-03-07 Sintesis regioselectiva del cci-779

Country Status (26)

Country Link
US (1) US7153957B2 (es)
EP (1) EP1658295B1 (es)
JP (1) JP4227649B2 (es)
KR (1) KR20060057605A (es)
CN (1) CN1829722B (es)
AR (1) AR045217A1 (es)
AT (1) ATE365169T1 (es)
AU (1) AU2004265267A1 (es)
BR (1) BRPI0412667A (es)
CA (1) CA2532988A1 (es)
CO (1) CO5650251A2 (es)
CR (1) CR8189A (es)
DE (1) DE602004007145T2 (es)
DK (1) DK1658295T3 (es)
EC (1) ECSP066413A (es)
ES (1) ES2287772T3 (es)
IL (1) IL173134A0 (es)
MX (1) MXPA06000951A (es)
NO (1) NO20060494L (es)
PL (1) PL1658295T3 (es)
PT (1) PT1658295E (es)
RU (1) RU2339639C2 (es)
TW (1) TW200508241A (es)
UA (1) UA83245C2 (es)
WO (1) WO2005016935A2 (es)
ZA (1) ZA200601055B (es)

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CA2484640C (en) * 2002-05-15 2012-01-17 Endocyte, Inc. Vitamin-mitomycin conjugates
AR040693A1 (es) 2002-07-30 2005-04-13 Wyeth Corp Formulaciones parenterales
WO2004069159A2 (en) 2003-01-27 2004-08-19 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
UA84881C2 (ru) * 2003-09-03 2008-12-10 Уайт Аморфный 42-эфир рапамицина и 3-гидрокси-2-(гидроксиметил)-2-метилпропионовой кислоты и фармацевтическая композиция, содержащая его
EP1701698B1 (en) * 2004-01-08 2008-01-16 Wyeth a Corporation of the State of Delaware Directly compressible pharmaceutical composition for the oral admimistration of cci-779
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
MXPA06011883A (es) 2004-04-14 2006-12-14 Wyeth Corp 42-ester de prolina-rapamicina con acido 2,2-bis(hidroximetil)propionico y sintesis enzimatica de dos etapas de 42-ester de prolina-rapamicina con acido 2,2-bis(hidroximetil)propionico y 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionic
CN1946852A (zh) * 2004-04-27 2007-04-11 惠氏公司 利用雷帕霉素特异性甲基化酶标记雷帕霉素
CN101098854B (zh) * 2004-07-23 2012-12-05 恩多塞特公司 二价连接体及其轭合物
CA2577011A1 (en) 2004-08-10 2006-04-13 Wyeth Cci-779 derivatives and methods of making same
KR20070070184A (ko) 2004-10-28 2007-07-03 와이어쓰 자궁근종의 치료에 있어서 mTOR 억제제의 용도
CA2595766A1 (en) * 2005-02-09 2006-08-17 Wyeth Cci-779 polymorph and use thereof
RU2007130406A (ru) 2005-03-02 2009-04-10 Вайет (Us) Очистка рапамицина
MX2007010715A (es) * 2005-03-02 2007-10-12 Wyeth Corp Recuperacion de cc-779 a partir de soluciones madre.
CN101175757B (zh) 2005-03-16 2012-11-14 恩多塞特公司 蝶酸及其缀合物的合成和纯化
BRPI0615354A2 (pt) 2005-08-19 2011-05-17 Endocyte, Inc. conjugado de liberação de fármaco de ligação de receptor, composição farmacêutica que o compreende, bem como seu uso
EP2382995A3 (en) * 2005-08-19 2013-09-25 Endocyte, Inc. Ligand conjugates of Vinca alkaloids, analogs and derivatives
WO2007056175A2 (en) * 2005-11-04 2007-05-18 Wyeth 41-methoxy isotope labeled rapamycin 42-ester
EP1942937A1 (en) 2005-11-04 2008-07-16 Wyeth Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272
WO2007067566A2 (en) * 2005-12-07 2007-06-14 Wyeth Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry
AR058282A1 (es) 2005-12-07 2008-01-30 Wyeth Corp Forma cristalina purificada de cci-779, un proceso para la preparacion del mismo, un metodo para monitorear la cristalizacion del cci-779, un kit y una composicion farmaceutica que lo comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer.
CN101321770A (zh) * 2005-12-07 2008-12-10 惠氏公司 由雷帕霉素42-酯硼酸酯制备雷帕霉素42-酯的可放大方法
US20070142422A1 (en) * 2005-12-20 2007-06-21 Wyeth Control of CCI-779 dosage form stability through control of drug substance impurities
US20070203169A1 (en) * 2006-02-28 2007-08-30 Zhao Jonathon Z Isomers and 42-epimers of rapamycin ester analogs, methods of making and using the same
TW200824713A (en) * 2006-10-18 2008-06-16 Wyeth Corp Processes for the synthesis of individual isomers of mono-PEG CCI-779
US8414910B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8430055B2 (en) 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8414909B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8414525B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
US8414526B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids
US20080276935A1 (en) 2006-11-20 2008-11-13 Lixiao Wang Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
AU2008224988A1 (en) * 2007-03-14 2008-09-18 Endocyte, Inc. Binding ligand linked drug delivery conjugates of tubulysins
TW200845960A (en) * 2007-04-05 2008-12-01 Wyeth Corp Wortmannin-rapalog conjugate and uses thereof
TW200901989A (en) 2007-04-10 2009-01-16 Wyeth Corp Anti-tumor activity of CCI-779 in papillary renal cell cancer
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
CN101784565B (zh) 2007-06-25 2014-12-10 恩多塞特公司 含有亲水性间隔区接头的共轭物
CN101909441B (zh) 2007-10-25 2015-05-13 恩多塞特公司 微管蛋白抑制剂及其制备方法
US8754207B2 (en) 2009-09-25 2014-06-17 Cadila Healthcare Limited Process for the preparation of rapamycin derivatives
WO2011092564A2 (en) * 2010-01-28 2011-08-04 Fresenius Kabi Oncology Ltd Process for the preparation of temsirolimus and its intermediates
CN102020662B (zh) * 2011-01-07 2013-02-13 天津市炜杰科技有限公司 一种驮瑞塞尔制备方法
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
WO2012131019A1 (en) * 2011-04-01 2012-10-04 Sandoz Ag Regioselective acylation of rapamycin at the c-42 position
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
BR112015008365A2 (pt) 2012-10-16 2017-07-04 Endocyte Inc composto da fórmula b-l(d)x, ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de um composto, composição de forma de dosagem unitária ou dose unitária, composição para tratar um câncer em um paciente, e método para tratar um câncer em um paciente
CN104086564B (zh) * 2014-07-30 2019-02-05 江苏奥赛康药业股份有限公司 一种高纯度坦罗莫司的制备方法

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Also Published As

Publication number Publication date
UA83245C2 (en) 2008-06-25
PL1658295T3 (pl) 2007-11-30
ES2287772T3 (es) 2007-12-16
MXPA06000951A (es) 2006-03-30
NO20060494L (no) 2006-03-06
PT1658295E (pt) 2007-09-25
RU2339639C2 (ru) 2008-11-27
JP4227649B2 (ja) 2009-02-18
RU2006106910A (ru) 2007-09-20
US20050033046A1 (en) 2005-02-10
EP1658295B1 (en) 2007-06-20
EP1658295A2 (en) 2006-05-24
CN1829722B (zh) 2010-10-27
AR045217A1 (es) 2005-10-19
DE602004007145T2 (de) 2008-02-28
CN1829722A (zh) 2006-09-06
ZA200601055B (en) 2008-07-30
US7153957B2 (en) 2006-12-26
DK1658295T3 (da) 2007-09-24
CO5650251A2 (es) 2006-06-30
ATE365169T1 (de) 2007-07-15
WO2005016935A2 (en) 2005-02-24
DE602004007145D1 (de) 2007-08-02
TW200508241A (en) 2005-03-01
WO2005016935A3 (en) 2005-04-07
JP2007501783A (ja) 2007-02-01
IL173134A0 (en) 2006-06-11
AU2004265267A1 (en) 2005-02-24
CR8189A (es) 2006-10-04
CA2532988A1 (en) 2005-02-24
KR20060057605A (ko) 2006-05-26
BRPI0412667A (pt) 2006-09-26
HK1085482A1 (en) 2006-08-25

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