CN1176925C - 雷帕霉素衍生物的区域选择性合成方法 - Google Patents

雷帕霉素衍生物的区域选择性合成方法

Info

Publication number
CN1176925C
CN1176925C CNB008163685A CN00816368A CN1176925C CN 1176925 C CN1176925 C CN 1176925C CN B008163685 A CNB008163685 A CN B008163685A CN 00816368 A CN00816368 A CN 00816368A CN 1176925 C CN1176925 C CN 1176925C
Authority
CN
China
Prior art keywords
rapamycin
acid
carbon atoms
ether
alkyl
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 - Fee Related
Application number
CNB008163685A
Other languages
English (en)
Chinese (zh)
Other versions
CN1402731A (zh
Inventor
C-C����
C·－C·邵
J·H·塞尔斯特德特
R·诺雷尔丁
G·K·奇尔
G·福蒂埃
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
Publication of CN1402731A publication Critical patent/CN1402731A/zh
Application granted granted Critical
Publication of CN1176925C publication Critical patent/CN1176925C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related 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 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)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CNB008163685A 1999-09-29 2000-09-27 雷帕霉素衍生物的区域选择性合成方法 Expired - Fee Related CN1176925C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40883099A 1999-09-29 1999-09-29
US09/408,830 1999-09-29

Publications (2)

Publication Number Publication Date
CN1402731A CN1402731A (zh) 2003-03-12
CN1176925C true CN1176925C (zh) 2004-11-24

Family

ID=23617953

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB008163685A Expired - Fee Related CN1176925C (zh) 1999-09-29 2000-09-27 雷帕霉素衍生物的区域选择性合成方法

Country Status (24)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104086564A (zh) * 2014-07-30 2014-10-08 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

Families Citing this family (31)

* 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
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
AU2005233612A1 (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
MX2007001676A (es) 2004-08-10 2007-04-12 Wyeth Corp Derivados de 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionico y metodos para hacer los mismos.
ES2364495T3 (es) 2005-02-03 2011-09-05 The General Hospital Corporation Método para tratar cáncer resistente a gefitinib.
CA2595766A1 (en) 2005-02-09 2006-08-17 Wyeth Cci-779 polymorph and use thereof
JP2009514870A (ja) 2005-11-04 2009-04-09 ワイス ｍＴＯＲインヒビター、ハーセプチン、および／またはＨＫＩ−２７２の抗悪性腫瘍性組み合わせ
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
ES2692769T3 (es) 2008-06-17 2018-12-05 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
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
MX2013011412A (es) * 2011-04-01 2014-04-30 Sandoz Ag Acilacion regioselectiva de rapamicina en la posicion c-42.
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
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
ES2804251T3 (es) * 2016-03-14 2021-02-05 Wisconsin Alumni Res Found Conjugados y micelas de ácido oligoláctico con eficacia anticáncer mejorada
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
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
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
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
IL314362A (en) 2018-06-15 2024-09-01 Janssen Pharmaceutica Nv Rapamycin analogs and their uses
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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104086564A (zh) * 2014-07-30 2014-10-08 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
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

Also Published As

Publication number Publication date
DE60001510D1 (de) 2003-04-03
CZ20021136A3 (cs) 2002-06-12
DE60001510T2 (de) 2003-10-02
EA004331B1 (ru) 2004-04-29
IL148542A (en) 2006-08-20
MXPA02003243A (es) 2002-09-30
HUP0202609A2 (hu) 2002-12-28
KR20020029796A (ko) 2002-04-19
AU7718200A (en) 2001-04-30
NO20021360D0 (no) 2002-03-19
EA200200412A1 (ru) 2002-10-31
JP2003510329A (ja) 2003-03-18
BR0014433A (pt) 2002-06-11
ES2189768T3 (es) 2003-07-16
TWI256395B (en) 2006-06-11
PL200899B1 (pl) 2009-02-27
CN1402731A (zh) 2003-03-12
KR100754236B1 (ko) 2007-09-03
NO20021360L (no) 2002-03-19
IL148542A0 (en) 2002-09-12
NZ517644A (en) 2003-09-26
HK1044774B (en) 2003-05-30
WO2001023395A3 (en) 2001-10-25
PL354461A1 (en) 2004-01-12
WO2001023395A2 (en) 2001-04-05
EP1216251A2 (en) 2002-06-26
CA2385461C (en) 2009-03-17
HUP0202609A3 (en) 2004-11-29
ATE233269T1 (de) 2003-03-15
HK1044774A1 (en) 2002-11-01
DK1216251T3 (da) 2003-06-16
AR029181A1 (es) 2003-06-18
EP1216251B1 (en) 2003-02-26
CA2385461A1 (en) 2001-04-05
AU782234B2 (en) 2005-07-14
JP4289813B2 (ja) 2009-07-01
CZ300368B6 (cs) 2009-05-06
ZA200201918B (en) 2003-08-27

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Legal Events

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C06 Publication
PB01 Publication
C14 Grant of patent or utility model
GR01 Patent grant
C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20041124

Termination date: 20100927