BR112013025085A2 - processo para a acilação de rapamicina e processo para sintetizar tensirolimo - Google Patents

processo para a acilação de rapamicina e processo para sintetizar tensirolimo

Info

Publication number
BR112013025085A2
BR112013025085A2 BR112013025085A BR112013025085A BR112013025085A2 BR 112013025085 A2 BR112013025085 A2 BR 112013025085A2 BR 112013025085 A BR112013025085 A BR 112013025085A BR 112013025085 A BR112013025085 A BR 112013025085A BR 112013025085 A2 BR112013025085 A2 BR 112013025085A2
Authority
BR
Brazil
Prior art keywords
rapamycin
acylation
tensirolimus
synthesizing
remainder
Prior art date
Application number
BR112013025085A
Other languages
English (en)
Inventor
Niklas Schöne
Wolfgang Felzmann
Original Assignee
Sandoz Ag
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 Sandoz Ag filed Critical Sandoz Ag
Publication of BR112013025085A2 publication Critical patent/BR112013025085A2/pt

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
    • C07D498/12—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
    • C07D498/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B41/00—Formation or introduction of functional groups containing oxygen
    • C07B41/06—Formation or introduction of functional groups containing oxygen of carbonyl groups
    • 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

Landscapes

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

Abstract

resumo acilação regiosseletiva da rapamicina na posição c-42 a invenção refere-se à acilação seletiva de rapamicina na posição 42 (i) com um agente de acilação de fórmula (ii), em que r4 e r5 são iguais ou diferentes, individualmente o restante de um acetal, especialmente de tetra-hidropirano, ou de um carbonato ou o restante de um éter silílico ou, tomados em conjunto, são o restante de um boronato, um acetal ou cetal.
BR112013025085A 2011-04-01 2012-03-30 processo para a acilação de rapamicina e processo para sintetizar tensirolimo BR112013025085A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11160858 2011-04-01
PCT/EP2012/055757 WO2012131019A1 (en) 2011-04-01 2012-03-30 Regioselective acylation of rapamycin at the c-42 position

Publications (1)

Publication Number Publication Date
BR112013025085A2 true BR112013025085A2 (pt) 2016-07-19

Family

ID=43920672

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013025085A BR112013025085A2 (pt) 2011-04-01 2012-03-30 processo para a acilação de rapamicina e processo para sintetizar tensirolimo

Country Status (11)

Country Link
US (1) US9051336B2 (pt)
EP (1) EP2694520A1 (pt)
JP (1) JP5998198B2 (pt)
KR (1) KR20140013000A (pt)
CN (1) CN103517911B (pt)
AU (1) AU2012233667C1 (pt)
BR (1) BR112013025085A2 (pt)
CA (1) CA2828829A1 (pt)
MX (1) MX2013011412A (pt)
RU (1) RU2603261C2 (pt)
WO (1) WO2012131019A1 (pt)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117088931A (zh) 2014-08-12 2023-11-21 莫纳什大学 定向淋巴的前药
CN104592253B (zh) * 2014-12-29 2020-01-17 广东莱佛士制药技术有限公司 一种替西罗莫司的新合成方法
WO2017041139A1 (en) 2015-09-08 2017-03-16 Monash University Lymph directing prodrugs
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
CN108948047A (zh) * 2017-05-20 2018-12-07 鲁南制药集团股份有限公司 一种替西罗莫司的纯化方法
CN109020995A (zh) * 2017-06-12 2018-12-18 鲁南制药集团股份有限公司 一种替西罗莫司的晶型物
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
WO2019126374A1 (en) * 2017-12-19 2019-06-27 Ariya Therapeutics, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
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
CA3166908A1 (en) 2020-02-05 2021-08-12 Daniel Kenneth BONNER Lipid prodrugs of neurosteroids

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4316885A (en) * 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US5120727A (en) 1991-05-29 1992-06-09 American Home Products Corporation Rapamycin dimers
US5489680A (en) * 1992-10-13 1996-02-06 American Home Products Corporation Carbamates of rapamycin
US5480989A (en) * 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5527907A (en) * 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
TWI256395B (en) * 1999-09-29 2006-06-11 Wyeth Corp Regioselective synthesis of rapamycin derivatives
US6277983B1 (en) * 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives
US7160867B2 (en) * 2003-05-16 2007-01-09 Isotechnika, Inc. Rapamycin carbohydrate derivatives
KR20060057605A (ko) * 2003-08-07 2006-05-26 와이어쓰 Ｃｃｉ-779의 위치선택적 합성 방법
US7659244B2 (en) * 2003-11-03 2010-02-09 Quest Pharmatech, Inc. Rapamycin peptides conjugates: synthesis and uses thereof
CN1942477A (zh) * 2004-04-14 2007-04-04 惠氏公司 脯氨酸cci－779(与2,2－二(羟基甲基)丙酸的脯氨酸-纳巴霉素42-酯)和使用微生物脂肪酶进行的脯氨酸cci－779和cci－779的两步酶合成
SG152234A1 (en) * 2004-04-14 2009-05-29 Wyeth Corp Regiospecific synthesis of rapamycin 42-ester derivatives
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
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
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
TW201035104A (en) * 2009-03-27 2010-10-01 Chunghwa Chemical Synthesis & Biotech Co Ltd Improved synthesis method for Temsirolimus and its similar compounds

Also Published As

Publication number Publication date
AU2012233667A1 (en) 2013-09-19
US20140081016A1 (en) 2014-03-20
CA2828829A1 (en) 2012-10-04
AU2012233667C1 (en) 2017-03-02
AU2012233667B2 (en) 2016-11-24
CN103517911B (zh) 2016-08-17
EP2694520A1 (en) 2014-02-12
WO2012131019A1 (en) 2012-10-04
US9051336B2 (en) 2015-06-09
MX2013011412A (es) 2014-04-30
RU2603261C2 (ru) 2016-11-27
JP2014509629A (ja) 2014-04-21
CN103517911A (zh) 2014-01-15
JP5998198B2 (ja) 2016-09-28
RU2013148626A (ru) 2015-05-10
KR20140013000A (ko) 2014-02-04

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2508 DE 29-01-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.