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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (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 (27)

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)
HK (1) HK1085482A1 (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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ATE427948T1 (de) * 2001-04-24 2009-04-15 Purdue Research Foundation Folat-mimetika und deren folatrezeptorbindende konjugate
CA2484640C (en) * 2002-05-15 2012-01-17 Endocyte, Inc. Vitamin-mitomycin conjugates
CA2493878C (en) 2002-07-30 2013-07-23 Wyeth Parenteral formulations containing a rapamycin hydroxyester
WO2004069159A2 (en) 2003-01-27 2004-08-19 Endocyte, Inc. Vitamin receptor binding drug delivery conjugates
JP2007504226A (ja) * 2003-09-03 2007-03-01 ワイス 非晶質状のラパマイシンの３−ヒドロキシ−２−（ヒドロキシメチル）−２−メチルプロピオン酸との４２−エステル、およびそれを含むその医薬組成物
MXPA06007829A (es) * 2004-01-08 2006-09-01 Wyeth Corp Composicion farmaceutica directamente comprimible para la administracion oral de 42-ester de rapamicina con acido 3-hidroxi-2-(hidroximetil)-2-metilpropionico.
SG152234A1 (en) 2004-04-14 2009-05-29 Wyeth Corp Regiospecific synthesis of rapamycin 42-ester derivatives
ATE410431T1 (de) * 2004-04-14 2008-10-15 Wyeth Corp Verfahren zur herstellung von rapamycin-42-estern und fk-506-32-estern mit dicarbonsäure, vorstufen für rapamycinkonjugate und antikörper
US7202256B2 (en) 2004-04-14 2007-04-10 Wyeth Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779
BRPI0510277A (pt) * 2004-04-27 2007-10-30 Wyeth Corp método para marcar especificamente uma rapamicina, rapamicina especificamente marcada, composição, e, kit
WO2006012527A1 (en) 2004-07-23 2006-02-02 Endocyte, Inc. Bivalent linkers and conjugates thereof
AU2005292647A1 (en) * 2004-08-10 2006-04-13 Wyeth CCI-779 derivatives and methods of making same
RU2007112787A (ru) 2004-10-28 2008-12-10 Вайет (Us) ПРИМЕНЕНИЕ ИНГИБИТОРА mTOR ПРИ ЛЕЧЕНИИ ЛЕЙОМИОМЫ МАТКИ
KR20070107030A (ko) * 2005-02-09 2007-11-06 와이어쓰 Ｃｃｉ-７７９ 다형체 및 그의 용도
CA2599582A1 (en) 2005-03-02 2006-09-08 Wyeth Purification of rapamycin
AU2006218916A1 (en) * 2005-03-02 2006-09-08 Wyeth Recovery of CCI-779 from mother liquors
JP5289935B2 (ja) 2005-03-16 2013-09-11 エンドサイト，インコーポレイテッド プテロイン酸およびその結合体の合成と精製
US20080280937A1 (en) * 2005-08-19 2008-11-13 Christopher Paul Leamon Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives
ES2468240T3 (es) 2005-08-19 2014-06-16 Endocyte, Inc. Conjugados de ligando de múltiples fármacos
WO2007056118A1 (en) 2005-11-04 2007-05-18 Wyeth Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272
WO2007056175A2 (en) * 2005-11-04 2007-05-18 Wyeth 41-methoxy isotope labeled rapamycin 42-ester
CA2630645A1 (en) * 2005-12-07 2007-06-14 Wyeth Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate
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
RU2008121240A (ru) 2005-12-07 2010-01-20 Вайет (Us) Способ получения очищенного кристаллического cci-779
KR20080077989A (ko) * 2005-12-20 2008-08-26 와이어쓰 약물의 불순물 조절을 통한 ｃｃｉ-779 제형의 안정성 조절
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
US9700704B2 (en) 2006-11-20 2017-07-11 Lutonix, Inc. Drug releasing coatings for balloon catheters
US9737640B2 (en) 2006-11-20 2017-08-22 Lutonix, Inc. Drug releasing coatings for medical devices
US8414526B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids
US8430055B2 (en) 2008-08-29 2013-04-30 Lutonix, Inc. Methods and apparatuses for coating balloon catheters
US8425459B2 (en) 2006-11-20 2013-04-23 Lutonix, Inc. Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent
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
US8414910B2 (en) 2006-11-20 2013-04-09 Lutonix, Inc. Drug releasing coatings for medical devices
US8414909B2 (en) 2006-11-20 2013-04-09 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
WO2008101231A2 (en) 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
CN101678124A (zh) * 2007-03-14 2010-03-24 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
EP3569251A1 (en) 2007-06-25 2019-11-20 Endocyte, Inc. Conjugates containing hydrophilic spacer linkers
CA2703491C (en) 2007-10-25 2017-06-13 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
EP2528906A2 (en) * 2010-01-28 2012-12-05 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
CA2828829A1 (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
AU2013331440A1 (en) 2012-10-16 2015-04-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
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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US5362718A (en) * 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
DE19857765A1 (de) * 1998-12-15 2000-06-21 Clariant Gmbh Verfahren zur Herstellung von para-Oxadiazolyl-phenyl-boronsäuren
US6277983B1 (en) * 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives

Also Published As

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

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