BRPI0417272A - processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-3il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato - Google Patents

processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-3il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato

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Publication number
BRPI0417272A
BRPI0417272A BRPI0417272-8A BRPI0417272A BRPI0417272A BR PI0417272 A BRPI0417272 A BR PI0417272A BR PI0417272 A BRPI0417272 A BR PI0417272A BR PI0417272 A BRPI0417272 A BR PI0417272A
Authority
BR
Brazil
Prior art keywords
amino
isobutyl
hexahydrofuro
aminophenyl
furan
Prior art date
Application number
BRPI0417272-8A
Other languages
English (en)
Inventor
Nicolaas Martha Feli Goyvaerts
Piet Tom Bert Paul Wigerinck
Hartmut Burghard Zinser
Birgit M Ebert
Original Assignee
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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34740665&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0417272(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of BRPI0417272A publication Critical patent/BRPI0417272A/pt
Publication of BRPI0417272B1 publication Critical patent/BRPI0417272B1/pt
Publication of BRPI0417272B8 publication Critical patent/BRPI0417272B8/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"PROCESSO PARA A PREPARAçãO DE (3R,3AS,6AR)-HEXAHIDROFURO ¢2,3-B! FURAN-3-IL (1S,2R)-3-¢¢(4AMINOFENIL) SULFONIL! (ISOBUTIL) AMINO!-1-BENZIL-2HIDROXIPROPILCARBAMATO". A presente invenção refere-se a um processo para a preparação de (3R,3aS,6aR)hexahidrofuro ¢2,3-b! furan-3-il (1S,2R)-3-¢¢(4-aminofenil) sulfonil! (isobutil) amino!-1-benzil-2-hidroxipropilcarbamato bem como intermediários para uso em ditos processos. Mais em particular, a invenção relaciona-se a processos para a preparação de (3R,3aS,6aR)hexahidrofuro ¢2,3b! furan-3-il (1S,2R)-3-¢¢(4-aminofenil) sulfonil! (isobutil) amino !-1-benzil-2hidroxipropilcarbamato o qual faz uso do intermediário 4-amino-N¢(2R,3S)-3amino-2-hidróxi-4-fenilbutil!-N-isobutil)benzeno sulfonamida, e os quais são processos amenáveis a escala industrial. (3R,3aS,6aR)hexahidrofuro ¢2,3-b! furan-3-il (1S,2R)-3-¢¢(4-aminofenil) sulfonil! (isobutil) amino!-1-benzil-2hidroxipropilcarbamato é particularmente útil como inibidor de HIV-protease.
BRPI0417272A 2003-12-23 2004-12-23 processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato BRPI0417272B8 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP03104949 2003-12-23
EP031049497 2003-12-23
US56818304P 2004-05-04 2004-05-04
US60/568,183 2004-05-04
PCT/EP2004/053692 WO2005063770A1 (en) 2003-12-23 2004-12-23 Process for the preparation of (3r,3as,6ar)-hexahydrofuro [2,3-b] furan-3-yl (1s,2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate

Publications (3)

Publication Number Publication Date
BRPI0417272A true BRPI0417272A (pt) 2007-03-27
BRPI0417272B1 BRPI0417272B1 (pt) 2020-08-18
BRPI0417272B8 BRPI0417272B8 (pt) 2021-05-25

Family

ID=34740665

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0417272A BRPI0417272B8 (pt) 2003-12-23 2004-12-23 processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato

Country Status (21)

Country Link
EP (1) EP1725566B1 (pt)
KR (1) KR101192859B1 (pt)
CN (1) CN1898248B (pt)
AT (1) ATE433982T1 (pt)
AU (1) AU2004309122B2 (pt)
BR (1) BRPI0417272B8 (pt)
CA (1) CA2549460C (pt)
CY (1) CY1109379T1 (pt)
DE (1) DE602004021640D1 (pt)
DK (1) DK1725566T3 (pt)
ES (1) ES2328701T3 (pt)
HR (1) HRP20090488T1 (pt)
IL (1) IL174960A (pt)
MX (1) MXPA06007211A (pt)
NO (1) NO337636B1 (pt)
PL (1) PL1725566T3 (pt)
PT (1) PT1725566E (pt)
RU (1) RU2376308C2 (pt)
SI (1) SI1725566T1 (pt)
WO (1) WO2005063770A1 (pt)
ZA (1) ZA200605163B (pt)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI432438B (zh) * 2005-11-28 2014-04-01 Tibotec Pharm Ltd 作為hiv蛋白酶抑制劑之經取代的胺基苯基磺醯胺化合物及衍生物
AU2007316562B2 (en) * 2006-11-09 2013-02-21 Janssen Sciences Ireland Unlimited Company Methods for the preparation of hexahydrofuro[2,3-b]furan-3-ol
BRPI0810609A2 (pt) 2007-04-27 2014-10-21 Tibotec Pharm Ltd Métodos para a preparação de derivados de n-isobutil-n-(2-hidróxi-a-amino-4-fenilbutil)-p-nitrobe nzenossulfonilamida
CA2703591C (en) * 2007-10-26 2013-05-07 Concert Pharmaceuticals, Inc. Deuterated darunavir
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
TWI482775B (zh) * 2008-09-01 2015-05-01 Tibotec Pharm Ltd 用於製備(3r,3as,6ar)-六氫呋喃并〔2,3-b〕呋喃-3-基(1s,2r)-3-〔〔(4-胺基苯基)磺醯基〕(異丁基)胺基〕-1-苯甲基-2-羥基丙基胺基甲酸酯之方法
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
CN104370932A (zh) * 2009-05-13 2015-02-25 明治制果药业株式会社 生产啶南平衍生物的方法
EP2477992B1 (en) 2009-09-17 2016-12-14 Mylan Laboratories Limited Processes for the preparation of darunavir and the amorphous form thereof
NZ600994A (en) 2010-01-05 2014-04-30 Cipla Ltd Darunavir polymorph and process for preparation thereof
ES2516916T3 (es) 2010-01-28 2014-10-31 Mapi Pharma Limited Procedimiento para la preparación de darunavir e intermedios de darunavir
CN102584844B (zh) * 2011-01-11 2016-04-13 浙江九洲药业股份有限公司 一种达芦那韦晶型及其制备方法
WO2014016660A2 (en) * 2012-07-24 2014-01-30 Laurus Labs Private Limited A process for preparation of darunavir
CN103893178B (zh) * 2014-03-19 2016-06-01 中山大学 苯-磺酰胺类化合物在制备抗hiv-1病毒药物中的应用
US20160075643A1 (en) * 2014-09-16 2016-03-17 Zcl Chemicals Limited Novel process to prepare intermediates of hiv-protease inhibitors thereof
EP3313847A4 (en) * 2015-06-25 2019-04-24 MSN Laboratories Private Limited PROCESS FOR PREPARING (3R, 3AS, 6AR) HEXAHYDROFURO [2,3-B] FURAN-3-YL ESTER OF [(1S, 2R) -3 - [[(4-AMINOPHENYL) SULFONYL] (2-METHYLPROPYL) ACID ) AMINO] -2-HYDROXY-1- (PHENYLMETHYL) PROPYL] -CARBAMIC AND ITS AMORPHOUS FORM
WO2018081292A1 (en) 2016-10-27 2018-05-03 Gilead Sciences, Inc. Crystalline forms of darunavir free base, hydrate, solvates and salts
MX2019005722A (es) 2016-11-17 2019-07-08 Janssen Sciences Ireland Unlimited Co Procedimiento simplificado para la preparacion de darunavir.
CN117142989A (zh) * 2020-12-30 2023-12-01 上海飞腾医药科技有限公司 一种抗hiv类药物中间体晶体a的生长方法和所得晶体
CN113896658A (zh) * 2021-09-24 2022-01-07 上药康丽(常州)药业有限公司 一种利用微通道反应器合成地瑞那韦中间体的方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996022287A1 (en) 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
KR100411856B1 (ko) 1995-02-03 2004-05-20 카네카 코포레이션 α-할로케톤,α-할로히드린및에폭사이드의제조법
US5756533A (en) 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5705500A (en) 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
DE69625183T2 (de) 1995-03-10 2003-10-09 Searle & Co Heterocyclocarbonyl-aminosäure-hydroxyethylamino-sulfonamid inhibitoren retroviraler proteasen
US6344572B1 (en) 1999-01-29 2002-02-05 Kaneka Corporation Processes for the preparation of threo-1,2-epoxy-3-amino-4-phenylbutane derivatives
KR20020046948A (ko) 2000-12-12 2002-06-21 에가시라 구니오 에폭사이드 결정의 제조방법
AR035970A1 (es) 2001-05-11 2004-07-28 Tibotec Pharm Ltd 2-amino-benzoxazol sulfonamidas inhibidoras de amplio espectro de la hiv proteasa, composicion farmaceutica, metodo "in vitro" para inhibir la replicacion retroviral, y utilizacion de estos compuestos en la manufactura de medicamentos
AU2002362189A1 (en) * 2001-12-28 2003-07-24 Ajinomoto Co., Inc. Process for producing crystal of benzenesulfonamide derivative, and novel crystal of intermediate therefor and process for producing the same

Also Published As

Publication number Publication date
EP1725566A1 (en) 2006-11-29
WO2005063770A1 (en) 2005-07-14
CA2549460A1 (en) 2005-07-14
DE602004021640D1 (de) 2009-07-30
AU2004309122A1 (en) 2005-07-14
SI1725566T1 (sl) 2009-12-31
CA2549460C (en) 2014-08-05
ATE433982T1 (de) 2009-07-15
RU2006126670A (ru) 2008-01-27
PL1725566T3 (pl) 2009-11-30
MXPA06007211A (es) 2006-08-18
BRPI0417272B8 (pt) 2021-05-25
CN1898248B (zh) 2011-08-17
PT1725566E (pt) 2009-09-16
ZA200605163B (en) 2007-12-27
CN1898248A (zh) 2007-01-17
BRPI0417272B1 (pt) 2020-08-18
RU2376308C2 (ru) 2009-12-20
NO337636B1 (no) 2016-05-23
IL174960A (en) 2011-06-30
AU2004309122B2 (en) 2011-07-21
IL174960A0 (en) 2006-08-20
ES2328701T3 (es) 2009-11-17
KR101192859B1 (ko) 2012-10-19
HRP20090488T1 (en) 2009-10-31
EP1725566B1 (en) 2009-06-17
CY1109379T1 (el) 2014-07-02
KR20060123740A (ko) 2006-12-04
DK1725566T3 (da) 2009-10-05
NO20063401L (no) 2006-07-21

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Legal Events

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: PARA INT.CL: C07D 493/04, A61P 31/00

Ipc: C07D 493/04 (2011.01)

B25D Requested change of name of applicant approved

Owner name: TIBOTEC PHARMACEUTICALS (IE)

B25D Requested change of name of applicant approved

Owner name: JANSSEN R AND D IRELAND (IE)

B25A Requested transfer of rights approved

Owner name: JANSSEN SCIENCES IRELAND UC (IE)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

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B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06I Publication of requirement cancelled [chapter 6.9 patent gazette]

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B06A Patent application procedure suspended [chapter 6.1 patent gazette]
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