BRPI0212341B8 - compostos intermediários de inibidores de protease de hiv e processo para preparação dos mesmos - Google Patents

compostos intermediários de inibidores de protease de hiv e processo para preparação dos mesmos

Info

Publication number
BRPI0212341B8
BRPI0212341B8 BRPI0212341A BR0212341A BRPI0212341B8 BR PI0212341 B8 BRPI0212341 B8 BR PI0212341B8 BR PI0212341 A BRPI0212341 A BR PI0212341A BR 0212341 A BR0212341 A BR 0212341A BR PI0212341 B8 BRPI0212341 B8 BR PI0212341B8
Authority
BR
Brazil
Prior art keywords
preparing
intermediate compounds
hiv protease
same
protease inhibitors
Prior art date
Application number
BRPI0212341A
Other languages
English (en)
Other versions
BR0212341A (pt
BRPI0212341B1 (pt
Inventor
Rudolf Romanie Kesteleyn Bart
Louis Nestor Ghislain Surleraux Dominique
Jan Leonard Mario Quaedflieg Peter
Original Assignee
Janssen R&D Ireland
Janssen Sciences Ireland Uc
Tibotec Pharm Ltd
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=8180908&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0212341(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen R&D Ireland, Janssen Sciences Ireland Uc, Tibotec Pharm Ltd filed Critical Janssen R&D Ireland
Publication of BR0212341A publication Critical patent/BR0212341A/pt
Publication of BRPI0212341B1 publication Critical patent/BRPI0212341B1/pt
Publication of BRPI0212341B8 publication Critical patent/BRPI0212341B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/20—Oxygen atoms
    • 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Furan Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

inibidor de protease de hiv, compostos intermediários e processo para preparação dos mesmos. a presente invenção refere-se a um método para preparação de hexaidro-furo[2,3-b]furan-3-ol, bem como novos intermediários para uso no método. mais especificamente, a invenção refere-se a um método estereosseletivo para a preparação de hexaidro-furo[2,3-b]furan-3-ol e a um método receptível em escala industrial.
BRPI0212341A 2001-09-10 2002-09-06 compostos intermediários de inibidores de protease de hiv e processo para preparação dos mesmos BRPI0212341B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP01203416.1 2001-09-10
EP01203416 2001-09-10
PCT/EP2002/010062 WO2003022853A1 (en) 2001-09-10 2002-09-06 Method for the preparation of hexahydro-furo[2,3-b]furan-3-ol

Publications (3)

Publication Number Publication Date
BR0212341A BR0212341A (pt) 2004-07-27
BRPI0212341B1 BRPI0212341B1 (pt) 2019-04-02
BRPI0212341B8 true BRPI0212341B8 (pt) 2021-05-25

Family

ID=8180908

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0212341A BRPI0212341B8 (pt) 2001-09-10 2002-09-06 compostos intermediários de inibidores de protease de hiv e processo para preparação dos mesmos

Country Status (27)

Country Link
US (1) US7126015B2 (pt)
EP (1) EP1448567B1 (pt)
JP (1) JP4521185B2 (pt)
KR (1) KR100894673B1 (pt)
CN (2) CN100519561C (pt)
AP (1) AP1758A (pt)
AR (1) AR036501A1 (pt)
AT (1) ATE453648T1 (pt)
AU (1) AU2002333809C1 (pt)
BR (1) BRPI0212341B8 (pt)
CA (1) CA2459168C (pt)
CY (1) CY1109974T1 (pt)
DE (1) DE60234952D1 (pt)
DK (1) DK1448567T3 (pt)
EA (1) EA010883B1 (pt)
ES (1) ES2338538T3 (pt)
HR (1) HRP20040320B1 (pt)
HU (1) HU229505B1 (pt)
IL (2) IL160166A0 (pt)
MX (1) MXPA04002247A (pt)
NO (1) NO328934B1 (pt)
NZ (1) NZ531641A (pt)
PL (1) PL224030B1 (pt)
PT (1) PT1448567E (pt)
SI (1) SI21463B (pt)
WO (1) WO2003022853A1 (pt)
ZA (1) ZA200401501B (pt)

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ES2268427T3 (es) * 2002-06-27 2007-03-16 Smithkline Beecham Corporation Preparacion de estereoisomeros de (3alfa, 3alfa/beta, 6alfa/beta) hexahidrofuro(2,3-b)furan-3-ol.
EP1589018A4 (en) * 2002-12-27 2007-03-14 Sumitomo Chemical Co METHOD OF PREPARING HEXAHYDROFUROFURANOL DERIVATIVES, INTERMEDIATE PRODUCTS AND MANUFACTURING METHOD THEREFOR
JP4818124B2 (ja) 2003-12-23 2011-11-16 テイボテク・フアーマシユーチカルズ・リミテツド (3R,3aS,6aR)−ヘキサヒドロフロ〔2,3−b〕フラン−3−イル(1S,1R)−3−〔〔(4−アミノフェニル)スルホニル〕(イソブチル)アミノ〕−1−ベンジル−2−ヒドロキシプロピルカルバマートの製造方法
TWI383975B (zh) * 2004-03-31 2013-02-01 悌柏泰克醫藥有限公司 製備(3R,3aS,6aR)六氫-呋喃并〔2,3-b〕呋喃-3-醇之方法
JP5549898B2 (ja) * 2006-03-31 2014-07-16 独立行政法人産業技術総合研究所 5−ヒドロキシメチル−2−フルフラールの製造法
RS51675B (sr) * 2006-11-09 2011-10-31 Tibotec Pharmaceuticals Metode za dobivanje heksahidrofuro[2,3-b]furan-3-ola
CN101024646B (zh) * 2007-02-06 2010-07-14 启东东岳药业有限公司 4-甲氧基呋喃并呋喃-2-酮的纯化方法
WO2008132154A1 (en) 2007-04-27 2008-11-06 Tibotec Pharmaceuticals Ltd. Methods for the preparation of n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
AR073248A1 (es) 2008-09-01 2010-10-20 Tibotec Pharm Ltd Proceso para la preparacion de (1s, 2r)-3- ((4-aminofenil) sulfonil) ( isobutil) amino)-1- bencil-2- hidroxipropilcarbamato de (3r, 3as,6ar)- hexahidrofuro-(2,3-b) furan-3- ilo (darunavir) y compuestos intermediarios utiles en dicho proceso.
EP2358198A4 (en) * 2008-10-24 2012-11-14 Concert Pharmaceuticals Inc HYDROXYETHYLAMINO SULFONAMIDE DERIVATIVES
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
BR112012009956A2 (pt) 2009-10-30 2015-09-29 Lupin Ltd um novo processo para a preparação de darunavir e etanolato darunavir de tamanho de partícula.
PL2528923T3 (pl) 2010-01-28 2015-01-30 Mapi Pharma Ltd Sposób wytwarzania darunawiru i pochodnych darunawiru
US8841467B2 (en) 2010-11-23 2014-09-23 Mylan Laboratories Limited Process for the preparation of (3R, 3aS, 6aR)-hexahydrofuro [2, 3-b] furan-3-ol
WO2012075122A2 (en) * 2010-11-30 2012-06-07 Purdue Research Foundation Processes and intermediates for preparing substituted hexahydrofuro [2,3-b] furans
EP3795572B1 (en) 2012-07-24 2023-11-15 Laurus Labs Limited Darunavir propionate solvate
EP2883858B1 (en) * 2012-08-09 2017-12-27 Sumitomo Chemical Company Limited Method for producing hexahydrofurofuranol derivative
CN103864813B (zh) * 2012-12-18 2017-02-22 上海迪赛诺化学制药有限公司 一种合成六氢呋喃并[2,3‑b]呋喃‑3‑醇及其对映体的方法
WO2016207907A1 (en) * 2015-06-25 2016-12-29 Msn Laboratories Private Limited Process for the preparation of [(1 s,2r)-3-[[(4-aminophenyl)sulfonyl] (2-methylpropyl)amino]-2-hydroxy-1 -(phenylmethyl)propyl]-carbamic acid (3r,3as,6ar)hexahydro furo[2,3-b]furan-3-yl ester and its amorphous form
WO2017041228A1 (zh) * 2015-09-08 2017-03-16 浙江九洲药业股份有限公司 六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法
CN107043385B (zh) * 2016-02-05 2019-07-09 成都博腾药业有限公司 一种制备地瑞那韦中间体的方法
EP3532478B1 (en) 2016-10-27 2021-05-26 Gilead Sciences, Inc. Crystalline form of darunavir free base
CN106928248B (zh) * 2017-02-04 2019-01-04 青岛科技大学 一种制备(3R,3aS,6aR)六氢呋喃并[2,3-b]呋喃-3-醇的方法
CN110272398B (zh) 2018-03-16 2022-11-29 江苏瑞科医药科技有限公司 六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法
WO2022035499A1 (en) * 2020-08-11 2022-02-17 Ghosh Arun K Methods for making darunavir p2-ligand precursors
CN114853774A (zh) * 2022-06-24 2022-08-05 盐城迪赛诺制药有限公司 一种达卢那韦关键中间体的制备方法
CN115557964A (zh) * 2022-10-18 2023-01-03 启东东岳药业有限公司 一种药物化合物的制备方法
CN117186053A (zh) * 2023-09-08 2023-12-08 上海凌凯医药科技有限公司 一种莱克酮中间体的制备方法

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PT2336134T (pt) * 1998-06-23 2016-10-19 The Board Of Trustees Of The Univ Of Illionis Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia
AU4828199A (en) * 1998-06-23 2000-01-10 Board Of Trustees Of The University Of Illinois, The Multi-drug resistant retroviral protease inhibitors and associated methods
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Also Published As

Publication number Publication date
PL224030B1 (pl) 2016-11-30
IL160166A0 (en) 2004-07-25
MXPA04002247A (es) 2005-09-07
EA010883B1 (ru) 2008-12-30
HRP20040320A2 (en) 2005-04-30
BR0212341A (pt) 2004-07-27
US20040249175A1 (en) 2004-12-09
CN101172980B (zh) 2011-11-16
HUP0402140A2 (hu) 2005-02-28
ES2338538T3 (es) 2010-05-10
WO2003022853A1 (en) 2003-03-20
BRPI0212341B1 (pt) 2019-04-02
EP1448567B1 (en) 2009-12-30
CN1553915A (zh) 2004-12-08
AP1758A (en) 2007-07-30
SI21463B (sl) 2011-08-31
EP1448567A1 (en) 2004-08-25
NZ531641A (en) 2005-08-26
HUP0402140A3 (en) 2007-05-29
NO328934B1 (no) 2010-06-21
CY1109974T1 (el) 2014-09-10
ZA200401501B (en) 2005-07-27
HRP20040320B1 (hr) 2012-11-30
US7126015B2 (en) 2006-10-24
ATE453648T1 (de) 2010-01-15
AU2002333809B8 (en) 2008-07-03
IL160166A (en) 2012-05-31
AU2002333809B9 (en) 2008-06-26
AU2002333809B2 (en) 2008-02-28
PL367817A1 (en) 2005-03-07
DE60234952D1 (de) 2010-02-11
HK1068887A1 (en) 2005-05-06
AR036501A1 (es) 2004-09-15
EA200400430A1 (ru) 2004-08-26
CN100519561C (zh) 2009-07-29
NO20041434L (no) 2004-06-10
DK1448567T3 (da) 2010-04-26
PT1448567E (pt) 2010-03-12
KR20040029425A (ko) 2004-04-06
JP2005502707A (ja) 2005-01-27
CN101172980A (zh) 2008-05-07
AU2002333809C1 (en) 2009-02-05
KR100894673B1 (ko) 2009-04-24
CA2459168C (en) 2014-01-28
AP2004002981A0 (en) 2004-03-31
SI21463A (sl) 2004-10-31
CA2459168A1 (en) 2003-03-20
HU229505B1 (hu) 2014-01-28
JP4521185B2 (ja) 2010-08-11

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