ES2189768T3 - Sintesis regioselectiva de derivados de rapamicina. - Google Patents

Sintesis regioselectiva de derivados de rapamicina.

Info

Publication number
ES2189768T3
ES2189768T3 ES00966904T ES00966904T ES2189768T3 ES 2189768 T3 ES2189768 T3 ES 2189768T3 ES 00966904 T ES00966904 T ES 00966904T ES 00966904 T ES00966904 T ES 00966904T ES 2189768 T3 ES2189768 T3 ES 2189768T3
Authority
ES
Spain
Prior art keywords
regional
rapamycin
rapamycin derivatives
silyl ether
elementary synthesis
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES00966904T
Other languages
English (en)
Inventor
Chia-Cheng Shaw
John Hamilton Sellstedt
Razzak Noureldin
Gloria Karen Cheal
Genevieve Fortier
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wyeth LLC
Original Assignee
Wyeth LLC
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 LLC filed Critical Wyeth LLC
Application granted granted Critical
Publication of ES2189768T3 publication Critical patent/ES2189768T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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 System
    • 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 System
    • 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

Abstract

Procedimiento para la preparación del éter 31-silílico de rapamicina, que comprende: (a)Tratar la rapamicina con un agente sililante para formar el éter 31,42-bis-silílico de rapamicina; e (b)Hidrolizar el éter 31,42-bis-silílico con ácido diluido frío, para proporcionar el éter 31-silílico de rapamicina.
ES00966904T 1999-09-29 2000-09-27 Sintesis regioselectiva de derivados de rapamicina. Expired - Lifetime ES2189768T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US40883099A 1999-09-29 1999-09-29

Publications (1)

Publication Number Publication Date
ES2189768T3 true ES2189768T3 (es) 2003-07-16

Family

ID=23617953

Family Applications (1)

Application Number Title Priority Date Filing Date
ES00966904T Expired - Lifetime ES2189768T3 (es) 1999-09-29 2000-09-27 Sintesis regioselectiva de derivados de rapamicina.

Country Status (24)

Country Link
EP (1) EP1216251B1 (es)
JP (1) JP4289813B2 (es)
KR (1) KR100754236B1 (es)
CN (1) CN1176925C (es)
AR (1) AR029181A1 (es)
AT (1) ATE233269T1 (es)
AU (1) AU782234B2 (es)
BR (1) BR0014433A (es)
CA (1) CA2385461C (es)
CZ (1) CZ300368B6 (es)
DE (1) DE60001510T2 (es)
DK (1) DK1216251T3 (es)
EA (1) EA004331B1 (es)
ES (1) ES2189768T3 (es)
HK (1) HK1044774B (es)
HU (1) HUP0202609A3 (es)
IL (2) IL148542A0 (es)
MX (1) MXPA02003243A (es)
NO (1) NO20021360D0 (es)
NZ (1) NZ517644A (es)
PL (1) PL200899B1 (es)
TW (1) TWI256395B (es)
WO (1) WO2001023395A2 (es)
ZA (1) ZA200201918B (es)

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
RU2345999C2 (ru) 2003-09-03 2009-02-10 Уайт Аморфный 42-эфир рапамицина и 3-гидрокси-2(гидроксиметил)-2-метилпропионовой кислоты и содержащие его фармацевтические композиции
AR046194A1 (es) 2003-11-04 2005-11-30 Mayo Foundation Metodo de tratamiento del linfoma de celulas del manto
EP1737869A1 (en) * 2004-04-14 2007-01-03 Wyeth a Corporation of the State of Delaware Regiospecific synthesis of rapamycin 42-ester derivatives
CA2564811A1 (en) 2004-04-14 2005-10-27 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
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
ZA200706804B (en) 2005-02-03 2008-10-29 Gen Hospital Corp Method for treating gefitinib resistant cancer
MX2007009590A (es) 2005-02-09 2007-09-12 Wyeth Corp Polimorfo cci-779 y uso del mismo.
PE20070763A1 (es) 2005-11-04 2007-08-08 Wyeth Corp COMBINACIONES ANTINEOPLASICAS DE UN INHIBIDOR DE mTOR, TRASTUZUMAB Y/O HKI-272
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
ES2531322T3 (es) 2008-06-17 2015-03-13 Wyeth Llc Combinaciones antineoplásicas que contienen HKI-272 y vinorelbina
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
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
CA2828829A1 (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
MX2020013630A (es) 2018-06-15 2021-04-28 Anakuria Therapeutics Inc Analogos de rapamicina y usos de los mismos.
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
KR20220128345A (ko) 2019-12-05 2022-09-20 아나쿠리아 테라퓨틱스, 인코포레이티드 라파마이신 유사체 및 이의 용도
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
AR029181A1 (es) 2003-06-18
KR20020029796A (ko) 2002-04-19
DK1216251T3 (da) 2003-06-16
ATE233269T1 (de) 2003-03-15
WO2001023395A2 (en) 2001-04-05
WO2001023395A3 (en) 2001-10-25
KR100754236B1 (ko) 2007-09-03
EA200200412A1 (ru) 2002-10-31
JP2003510329A (ja) 2003-03-18
CZ300368B6 (cs) 2009-05-06
EP1216251B1 (en) 2003-02-26
AU782234B2 (en) 2005-07-14
CN1402731A (zh) 2003-03-12
TWI256395B (en) 2006-06-11
CZ20021136A3 (cs) 2002-06-12
BR0014433A (pt) 2002-06-11
HUP0202609A3 (en) 2004-11-29
DE60001510D1 (de) 2003-04-03
AU7718200A (en) 2001-04-30
ZA200201918B (en) 2003-08-27
HK1044774B (zh) 2003-05-30
PL200899B1 (pl) 2009-02-27
NO20021360L (no) 2002-03-19
NZ517644A (en) 2003-09-26
EP1216251A2 (en) 2002-06-26
IL148542A0 (en) 2002-09-12
EA004331B1 (ru) 2004-04-29
MXPA02003243A (es) 2002-09-30
HUP0202609A2 (hu) 2002-12-28
CA2385461C (en) 2009-03-17
DE60001510T2 (de) 2003-10-02
NO20021360D0 (no) 2002-03-19
PL354461A1 (en) 2004-01-12
HK1044774A1 (en) 2002-11-01
CN1176925C (zh) 2004-11-24
IL148542A (en) 2006-08-20
CA2385461A1 (en) 2001-04-05

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