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

    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D498/22—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 four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; 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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KR20040106547A (ko) * 2002-05-15 2004-12-17 엔도사이트, 인코포레이티드 비타민-마이토마이신 공액체
RU2344821C2 (ru) * 2002-07-30 2009-01-27 Уайт Парентеральные композиции, содержащие гидроксиэфиры рапамицина
US7601332B2 (en) 2003-01-27 2009-10-13 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
EP1660081A1 (en) * 2003-09-03 2006-05-31 Wyeth Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and pharmaceutical compositions containing the same
DE602004011398T2 (de) * 2004-01-08 2009-01-15 Wyeth Direkt komprimierbare pharmazeutische zusammensetzung für die orale verabreichung von cci-779
KR20070015544A (ko) 2004-04-14 2007-02-05 와이어쓰 라파마이신 42-에스테르 유도체의 위치특이성 합성
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
EP1751168A1 (en) 2004-04-14 2007-02-14 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
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
TW200616633A (en) * 2004-08-10 2006-06-01 Wyeth Corp CCI-779 derivatives and methods of making same
EP1804779A1 (en) 2004-10-28 2007-07-11 Wyeth Use of an mtor inhibitor in treatment of uterine leiomyoma
JP2008530090A (ja) * 2005-02-09 2008-08-07 ワイス Ｃｃｉ−７７９多形及びその使用
BRPI0607390A2 (pt) 2005-03-02 2017-08-22 Wyeth Corp Processo para recuperar cci-779 de licores mâe
AU2006218918A1 (en) * 2005-03-02 2006-09-08 Wyeth Purification of rapamycin
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
RU2470668C2 (ru) 2005-08-19 2012-12-27 Эндосайт, Инк. Конъюгаты лиганда с несколькими лекарственными средствами
JP2009504783A (ja) * 2005-08-19 2009-02-05 エンドサイト，インコーポレイテッド ビンカアルカロイド、類似体および誘導体のリガンド結合体
US7538119B2 (en) * 2005-11-04 2009-05-26 Wyeth 41-Methoxy isotope labeled rapamycin 42-ester
EP3488866A1 (en) 2005-11-04 2019-05-29 Wyeth LLC Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272
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.
PE20070748A1 (es) 2005-12-07 2007-08-08 Wyeth Corp Proceso ajustable a escala para la preparacion de un 42-ester de rapamicina a partir de un boronato de 42-ester de rapamicina
JP2009518648A (ja) * 2005-12-07 2009-05-07 ワイス 結晶性ラパマイシンを調製するための方法およびを示差走査熱量測定使用してラパマイシン化合物の結晶化度を測定するための方法
JP2009520818A (ja) * 2005-12-20 2009-05-28 ワイス 薬物物質不純物の制御によるｃｃｉ−７７９製剤安定性の制御
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
US8414909B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8414910B2 (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
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
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US8430055B2 (en) 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
US8998846B2 (en) 2006-11-20 2015-04-07 Lutonix, Inc. Drug releasing coatings for balloon catheters
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
US8414525B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US20100104626A1 (en) * 2007-02-16 2010-04-29 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
CN104127878A (zh) * 2007-03-14 2014-11-05 恩多塞特公司 结合配体连接的微管溶素递药缀合物
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
BRPI0812970A2 (pt) * 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
EP2209374B1 (en) 2007-10-25 2014-12-03 Endocyte, Inc. Tubulysins and processes for preparing
US8754207B2 (en) 2009-09-25 2014-06-17 Cadila Healthcare Limited Process for the preparation of rapamycin derivatives
AU2011210227A1 (en) * 2010-01-28 2012-08-30 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
RU2603261C2 (ru) * 2011-04-01 2016-11-27 Сандоз Аг Региоселективное ацилирование рапамицина в положении с-42
WO2013126797A1 (en) 2012-02-24 2013-08-29 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
EA201590622A1 (ru) 2012-10-16 2015-10-30 Эндосайт, Инк. Конъюгаты для доставки лекарственного средства, содержащие не встречающиеся в природе аминокислоты, и способы применения
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
DE602004007145T2 (de) 2008-02-28
NO20060494L (no) 2006-03-06
BRPI0412667A (pt) 2006-09-26
HK1085482A1 (en) 2006-08-25
DK1658295T3 (da) 2007-09-24
JP2007501783A (ja) 2007-02-01
DE602004007145D1 (de) 2007-08-02
CN1829722A (zh) 2006-09-06
EP1658295B1 (en) 2007-06-20
WO2005016935A3 (en) 2005-04-07
TW200508241A (en) 2005-03-01
CR8189A (es) 2006-10-04
AR045217A1 (es) 2005-10-19
ES2287772T3 (es) 2007-12-16
ATE365169T1 (de) 2007-07-15
WO2005016935A2 (en) 2005-02-24
KR20060057605A (ko) 2006-05-26
AU2004265267A1 (en) 2005-02-24
PT1658295E (pt) 2007-09-25
RU2339639C2 (ru) 2008-11-27
US20050033046A1 (en) 2005-02-10
CA2532988A1 (en) 2005-02-24
MXPA06000951A (es) 2006-03-30
JP4227649B2 (ja) 2009-02-18
EP1658295A2 (en) 2006-05-24
CN1829722B (zh) 2010-10-27
CO5650251A2 (es) 2006-06-30
PL1658295T3 (pl) 2007-11-30
IL173134A0 (en) 2006-06-11
ZA200601055B (en) 2008-07-30
UA83245C2 (en) 2008-06-25
US7153957B2 (en) 2006-12-26
RU2006106910A (ru) 2007-09-20

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