HUP0202609A2 - Rapamicinszármazékok regioszelektív előállítása - Google Patents

Rapamicinszármazékok regioszelektív előállítása

Info

Publication number
HUP0202609A2
HUP0202609A2 HU0202609A HUP0202609A HUP0202609A2 HU P0202609 A2 HUP0202609 A2 HU P0202609A2 HU 0202609 A HU0202609 A HU 0202609A HU P0202609 A HUP0202609 A HU P0202609A HU P0202609 A2 HUP0202609 A2 HU P0202609A2
Authority
HU
Hungary
Prior art keywords
rapamycin
silyl ether
rapamycin derivatives
regioselective synthesis
bis
Prior art date
Application number
HU0202609A
Other languages
English (en)
Inventor
Gloria Karen Cheal
Genevieve Fortier
Razzak Noureldin
John Hamilton Sellstedt
Chia-Cheng Shaw
Original Assignee
Wyeth
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 filed Critical Wyeth
Publication of HUP0202609A2 publication Critical patent/HUP0202609A2/hu
Publication of HUP0202609A3 publication Critical patent/HUP0202609A3/hu

Links

Classifications

    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A találmány tárgya eljárás rapamicin 31-szilil-éter előállítására olymódon, hogy (a) rapamicint egy szililezőszerrel reagáltatják, ígynyerik a rapamicin 31,42-bisz-szilil-éter, és (b) a kapott 31,42-bisz-szilil-étert hideg, híg savval hidrolizálják, így nyerik a rapamicin31-szilil-étert. A találmány vonatkozik továbbá a rapamicin 42-észtervagy -éterszármazékainak regioszelektív előállítási eljárásaira is. Ó
HU0202609A 1999-09-29 2000-09-27 Regioselective synthesis of rapamycin derivatives HUP0202609A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40883099A 1999-09-29 1999-09-29
PCT/US2000/026445 WO2001023395A2 (en) 1999-09-29 2000-09-27 Regioselective synthesis of rapamycin derivatives

Publications (2)

Publication Number Publication Date
HUP0202609A2 true HUP0202609A2 (hu) 2002-12-28
HUP0202609A3 HUP0202609A3 (en) 2004-11-29

Family

ID=23617953

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0202609A HUP0202609A3 (en) 1999-09-29 2000-09-27 Regioselective synthesis of rapamycin derivatives

Country Status (24)

Country Link
EP (1) EP1216251B1 (hu)
JP (1) JP4289813B2 (hu)
KR (1) KR100754236B1 (hu)
CN (1) CN1176925C (hu)
AR (1) AR029181A1 (hu)
AT (1) ATE233269T1 (hu)
AU (1) AU782234B2 (hu)
BR (1) BR0014433A (hu)
CA (1) CA2385461C (hu)
CZ (1) CZ300368B6 (hu)
DE (1) DE60001510T2 (hu)
DK (1) DK1216251T3 (hu)
EA (1) EA004331B1 (hu)
ES (1) ES2189768T3 (hu)
HK (1) HK1044774B (hu)
HU (1) HUP0202609A3 (hu)
IL (2) IL148542A0 (hu)
MX (1) MXPA02003243A (hu)
NO (1) NO20021360L (hu)
NZ (1) NZ517644A (hu)
PL (1) PL200899B1 (hu)
TW (1) TWI256395B (hu)
WO (1) WO2001023395A2 (hu)
ZA (1) ZA200201918B (hu)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
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
AR046194A1 (es) 2003-11-04 2005-11-30 Mayo Foundation Metodo de tratamiento del linfoma de celulas del manto
BRPI0509854A (pt) 2004-04-14 2007-10-23 Wyeth Corp composto, métodos para a preparação regio-especìfica de um 42-éster de rapamicina ou 42-éster de prolina-rapamicina e para a preparação de um 42-éster de prolina-rapamicina, composição, e, produto
SG152234A1 (en) * 2004-04-14 2009-05-29 Wyeth Corp Regiospecific synthesis of rapamycin 42-ester derivatives
JP2008517874A (ja) 2004-08-10 2008-05-29 ワイス Ｃｃｉ−７７９誘導体及びそれらの作製法
CN102886045A (zh) 2005-02-03 2013-01-23 综合医院公司 治疗吉非替尼耐药性癌症的方法
CA2595766A1 (en) 2005-02-09 2006-08-17 Wyeth Cci-779 polymorph and use thereof
AR057854A1 (es) 2005-11-04 2007-12-19 Wyeth Corp Combinaciones antineoplasicas con inhibidor de mtor, herceptina y/o hki-272 (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi) anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida
US8022216B2 (en) 2007-10-17 2011-09-20 Wyeth Llc Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
EP2915532B1 (en) 2008-06-17 2016-10-19 Wyeth LLC Antineoplastic combinations containing hki-272 and vinorelbine
CN101676291B (zh) 2008-09-18 2012-05-09 上海海和药物研究开发有限公司 一类雷帕霉素碳酸酯类似物、其药物组合物及其制备方法和用途
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
WO2012131019A1 (en) * 2011-04-01 2012-10-04 Sandoz Ag Regioselective acylation of rapamycin at the c-42 position
CN103421023B (zh) * 2013-07-30 2015-09-23 福建省微生物研究所 一种替西罗莫司的合成工艺
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
CN106146536B (zh) * 2015-04-25 2019-07-26 山东新时代药业有限公司 一种依维莫司的制备方法
JP6942141B2 (ja) * 2016-03-14 2021-09-29 ウイスコンシン アラムニ リサーチ ファンデーション 抗がん効能を高めたオリゴ乳酸複合体及びミセル
CN107561170B (zh) * 2016-07-02 2021-07-30 山东新时代药业有限公司 一种坦西莫司中间体的分析检测方法
CN108948046B (zh) * 2017-05-20 2020-11-10 鲁南制药集团股份有限公司 一种替西罗莫司的中间体及其制备方法
CN108948045A (zh) * 2017-05-20 2018-12-07 鲁南制药集团股份有限公司 一种替西罗莫司的制备方法
CN109206441B (zh) * 2017-06-30 2022-05-20 正大天晴药业集团股份有限公司 一种依维莫司的纯化方法
CN109776570A (zh) * 2017-11-14 2019-05-21 上海医药工业研究院 一种依维莫司中间体、其制备方法及其应用
SG11202012447YA (en) 2018-06-15 2021-01-28 Navitor Pharm Inc Rapamycin analogs and uses thereof
CN109369679A (zh) * 2018-12-24 2019-02-22 江苏卓和药业有限公司 一种雷帕霉素的精制方法
CN109851626B (zh) * 2019-01-08 2021-11-02 扬子江药业集团四川海蓉药业有限公司 一种替西罗莫司的分离纯化方法
IL293549A (en) 2019-12-05 2022-08-01 Anakuria Therapeutics Inc Rapamycin analogs and their uses
CN113372359A (zh) * 2020-03-10 2021-09-10 鲁南制药集团股份有限公司 一种坦西莫司的制备方法
CN114106014B (zh) * 2020-08-27 2024-03-15 鲁南制药集团股份有限公司 一种依维莫司的制备方法
CN115028658A (zh) * 2022-07-06 2022-09-09 国药集团川抗制药有限公司 雷帕霉素硅醇酯及其制备方法和应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5120842A (en) * 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5387680A (en) * 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5362718A (en) * 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5563145A (en) * 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines

Also Published As

Publication number Publication date
JP4289813B2 (ja) 2009-07-01
HUP0202609A3 (en) 2004-11-29
CN1402731A (zh) 2003-03-12
EA004331B1 (ru) 2004-04-29
KR100754236B1 (ko) 2007-09-03
AU7718200A (en) 2001-04-30
IL148542A0 (en) 2002-09-12
CN1176925C (zh) 2004-11-24
EA200200412A1 (ru) 2002-10-31
HK1044774B (zh) 2003-05-30
NO20021360D0 (no) 2002-03-19
IL148542A (en) 2006-08-20
DK1216251T3 (da) 2003-06-16
WO2001023395A2 (en) 2001-04-05
MXPA02003243A (es) 2002-09-30
AU782234B2 (en) 2005-07-14
EP1216251B1 (en) 2003-02-26
JP2003510329A (ja) 2003-03-18
DE60001510D1 (de) 2003-04-03
CA2385461C (en) 2009-03-17
TWI256395B (en) 2006-06-11
NZ517644A (en) 2003-09-26
BR0014433A (pt) 2002-06-11
CA2385461A1 (en) 2001-04-05
CZ20021136A3 (cs) 2002-06-12
WO2001023395A3 (en) 2001-10-25
ATE233269T1 (de) 2003-03-15
DE60001510T2 (de) 2003-10-02
ES2189768T3 (es) 2003-07-16
PL354461A1 (en) 2004-01-12
HK1044774A1 (en) 2002-11-01
AR029181A1 (es) 2003-06-18
EP1216251A2 (en) 2002-06-26
KR20020029796A (ko) 2002-04-19
PL200899B1 (pl) 2009-02-27
NO20021360L (no) 2002-03-19
CZ300368B6 (cs) 2009-05-06
ZA200201918B (en) 2003-08-27

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Legal Events

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FD9A Lapse of provisional protection due to non-payment of fees