AP2052A - Pseudopolymorphic forms of HIV protease inhibitor - Google Patents

Pseudopolymorphic forms of HIV protease inhibitor

Info

Publication number
AP2052A
AP2052A AP2004003191A AP2004003191A AP2052A AP 2052 A AP2052 A AP 2052A AP 2004003191 A AP2004003191 A AP 2004003191A AP 2004003191 A AP2004003191 A AP 2004003191A AP 2052 A AP2052 A AP 2052A
Authority
AP
ARIPO
Prior art keywords
protease inhibitor
hiv protease
pseudopolymorphic forms
pseudopolymorphic
forms
Prior art date
Application number
AP2004003191A
Other languages
English (en)
Other versions
AP2004003191A0 (en
Inventor
Hans Wim Pieter Vermeersch
Daniel Joseph Christiaan Thone
Luc Donne Marie-Louise Janssens
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=29724454&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AP2052(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 AP2004003191A0 publication Critical patent/AP2004003191A0/xx
Application granted granted Critical
Publication of AP2052A publication Critical patent/AP2052A/xx

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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AP2004003191A 2002-05-16 2003-05-16 Pseudopolymorphic forms of HIV protease inhibitor AP2052A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02076929 2002-05-16
PCT/EP2003/050176 WO2003106461A2 (en) 2002-05-16 2003-05-16 Pseudopolymorphic forms of a hiv protease inhibitor

Publications (2)

Publication Number Publication Date
AP2004003191A0 AP2004003191A0 (en) 2004-12-31
AP2052A true AP2052A (en) 2009-10-05

Family

ID=29724454

Family Applications (1)

Application Number Title Priority Date Filing Date
AP2004003191A AP2052A (en) 2002-05-16 2003-05-16 Pseudopolymorphic forms of HIV protease inhibitor

Country Status (26)

Country Link
US (8) US7700645B2 (es)
EP (4) EP2314591B2 (es)
JP (1) JP4864320B2 (es)
KR (2) KR101128370B1 (es)
CN (1) CN100475819C (es)
AP (1) AP2052A (es)
AU (2) AU2003271740B2 (es)
BR (1) BRPI0311176B8 (es)
CA (1) CA2485834C (es)
CY (3) CY1115665T1 (es)
DK (3) DK2767539T3 (es)
EA (1) EA007120B8 (es)
ES (4) ES2728735T3 (es)
HK (1) HK1081969A1 (es)
HR (1) HRP20041061B1 (es)
HU (1) HUE034389T2 (es)
IL (1) IL165140A0 (es)
LT (1) LT2767539T (es)
MX (1) MXPA04011427A (es)
NO (1) NO331477B1 (es)
NZ (1) NZ536497A (es)
PL (1) PL215151B1 (es)
PT (3) PT1567529E (es)
SI (3) SI2767539T1 (es)
WO (1) WO2003106461A2 (es)
ZA (1) ZA200410154B (es)

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EP1088098B2 (en) 1998-06-23 2015-07-01 THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES Fitness assay and methods for reducing resistance of hiv to therapy
JP4864320B2 (ja) * 2002-05-16 2012-02-01 テイボテク・フアーマシユーチカルズ・リミテツド Hivプロテアーゼ阻害剤の疑似多形相
HRP20020614A2 (en) * 2002-07-22 2004-06-30 PLIVA-ISTRAŽIVAČKI INSTITUT d.o.o. Rhombic pseudopolymorph of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin a
UA85567C2 (en) 2003-12-23 2009-02-10 Тиботек Фармасьютикелз Лтд. 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
DK1856125T3 (da) 2005-02-25 2009-12-07 Tibotec Pharm Ltd Syntese af proteasehæmmerforstadie
EP2089371B1 (en) * 2006-11-09 2011-02-02 Tibotec Pharmaceuticals Methods for the preparation of hexahydrofuro[2,3-b]furan-3-ol
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.
PL2381786T3 (pl) * 2009-01-29 2015-06-30 Mapi Pharma Ltd Dimetylosulfotlenkowy solwat darunawiru
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
PT2477992T (pt) 2009-09-17 2017-03-20 Mylan Laboratories Ltd Processos para a preparação de darunavir e a forma amorfa do mesmo
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.
PT2513116E (pt) 2009-12-16 2015-10-14 Hetero Research Foundation Polimorfos de darunavir
WO2011083287A2 (en) 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof
JP2013518096A (ja) 2010-01-28 2013-05-20 マピ ファーマ リミテッド ダルナビル及びダルナビル中間体の調製方法
ES2595235T3 (es) 2010-05-20 2016-12-28 Hetero Research Foundation Sal clorhidrato cristalina de darunavir
WO2012107889A1 (en) 2011-02-10 2012-08-16 Ranbaxy Laboratories Limited Process for the preparation of amorphous darunavir
RS56667B1 (sr) 2011-07-07 2018-03-30 Janssen Sciences Ireland Uc Kombinovane formulacije darunavira
WO2013114382A1 (en) 2011-12-05 2013-08-08 Mylan Laboratories Ltd Crystalline darunavir
EP2804869B1 (en) * 2012-01-18 2019-06-12 Aurobindo Pharma Limited Novel solvates of darunavir
CN103509031B (zh) * 2012-06-20 2016-04-27 上海迪赛诺药业有限公司 制备达芦那韦无定形物的方法
EP3795572B1 (en) 2012-07-24 2023-11-15 Laurus Labs Limited Darunavir propionate solvate
JP2015536940A (ja) 2012-10-29 2015-12-24 シプラ・リミテッド 抗ウイルス性ホスホネート類似体及びその製造方法
US9346820B2 (en) * 2013-09-11 2016-05-24 Purdue Research Foundation HIV-1 protease inhibitors having gem-di-fluoro bicyclic P2-ligands
WO2016092525A1 (en) 2014-12-12 2016-06-16 Lupin Limited Darunavir n-propanol solvate and process for preparation thereof
WO2016092527A1 (en) * 2014-12-12 2016-06-16 Sun Pharmaceutical Industries Limited A process for the preparation of dolutegravir
WO2016149486A1 (en) 2015-03-19 2016-09-22 Viamet Pharmaceuticals, Inc. Antifungal compounds and processes for making
EP3496718A4 (en) 2016-08-08 2020-01-22 Hetero Labs Limited ANTIRETROVIRAL COMPOSITIONS
US20190175511A1 (en) 2016-08-08 2019-06-13 Hetero Labs Limited A Multi-Class Anti-Retroviral Composition
ES2881949T3 (es) 2016-10-27 2021-11-30 Gilead Sciences Inc Forma cristalina de base libre de darunavir
CN108727401A (zh) * 2017-04-20 2018-11-02 盐城迪赛诺制药有限公司 达鲁那韦新晶型及其制备方法和应用
CN109053753A (zh) * 2018-08-05 2018-12-21 浙江大学 一种制备达卢那韦二水合物晶型的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995006030A1 (en) * 1993-08-24 1995-03-02 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1999067417A2 (en) * 1998-06-23 1999-12-29 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Fitness assay and associated methods

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
JPH05230044A (ja) 1992-02-21 1993-09-07 Hoechst Japan Ltd ピレタニドの新規な結晶多形
US5968942A (en) 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
PT812320E (pt) 1995-02-22 2000-12-29 Aventis Pharma Ltd Firetanido amorfo piretanido polimorfo processo para a sua preparacao e sua utilizacao
ZA984514B (en) 1997-05-29 1998-11-30 Merck & Co Inc Hiv protease inhibitor
GB9712253D0 (en) 1997-06-13 1997-08-13 Glaxo Group Ltd Antiviral compound
US6287693B1 (en) 1998-02-25 2001-09-11 John Claude Savoir Stable shaped particles of crystalline organic compounds
GB9805898D0 (en) 1998-03-20 1998-05-13 Glaxo Group Ltd Process for the sythesis of hiv protease inhibitors
GB9807354D0 (en) 1998-04-07 1998-06-03 Glaxo Group Ltd Antiviral compound
WO1999067254A2 (en) * 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Multi-drug resistant retroviral protease inhibitors and use thereof
HRP990358A2 (en) 1998-11-19 2000-08-31 Du Pont Pharm Co Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1h)-quinazolinone
PE20010560A1 (es) 1999-02-12 2001-05-04 Vertex Pharma Sulfonamidas y amidas como inhibidores de aspartil proteasa
JP4864320B2 (ja) 2002-05-16 2012-02-01 テイボテク・フアーマシユーチカルズ・リミテツド Hivプロテアーゼ阻害剤の疑似多形相
WO2011083287A2 (en) * 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995006030A1 (en) * 1993-08-24 1995-03-02 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
WO1999067417A2 (en) * 1998-06-23 1999-12-29 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Fitness assay and associated methods

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Borka L et al *
Ghosh A K et al *
Giron et al *
Grunenberg A et al *

Also Published As

Publication number Publication date
CY1119311T1 (el) 2018-02-14
CA2485834C (en) 2007-07-17
ES2498370T5 (es) 2021-11-24
HRP20041061B1 (hr) 2015-02-27
ZA200410154B (en) 2005-12-28
HUE034389T2 (en) 2018-02-28
PL215151B1 (pl) 2013-10-31
US10858369B2 (en) 2020-12-08
CN100475819C (zh) 2009-04-08
NO331477B1 (no) 2012-01-16
EA200401503A1 (ru) 2005-06-30
CN1668623A (zh) 2005-09-14
EP2767539A1 (en) 2014-08-20
US20130303790A1 (en) 2013-11-14
EP3045460A1 (en) 2016-07-20
NO20045409L (no) 2004-12-10
KR101128370B1 (ko) 2012-04-23
US20100204316A1 (en) 2010-08-12
EP3045460B1 (en) 2019-04-17
EP2767539B1 (en) 2017-07-12
DK2314591T4 (da) 2021-05-10
DK2767539T3 (en) 2017-09-11
JP4864320B2 (ja) 2012-02-01
BR0311176A (pt) 2005-03-15
DK2314591T3 (da) 2014-09-22
US20150336980A1 (en) 2015-11-26
ES2503551T3 (es) 2014-10-07
US7700645B2 (en) 2010-04-20
CA2485834A1 (en) 2003-12-24
US8518987B2 (en) 2013-08-27
CY1117928T1 (el) 2017-05-17
NZ536497A (en) 2006-08-31
SI2314591T2 (sl) 2021-08-31
PT1567529E (pt) 2014-09-09
ES2503551T5 (es) 2021-10-28
EP1567529B1 (en) 2014-06-18
ES2638412T3 (es) 2017-10-20
BRPI0311176B8 (pt) 2021-05-25
LT2767539T (lt) 2017-09-25
HRP20041061A2 (en) 2006-07-31
US20180312517A1 (en) 2018-11-01
ES2728735T3 (es) 2019-10-28
KR20100119906A (ko) 2010-11-11
EP2314591B2 (en) 2021-02-24
PT2767539T (pt) 2017-08-28
US10000504B2 (en) 2018-06-19
SI1567529T1 (sl) 2014-11-28
PT2314591E (pt) 2014-09-19
WO2003106461A2 (en) 2003-12-24
EP2314591A1 (en) 2011-04-27
HK1081969A1 (en) 2006-05-26
SI2767539T1 (sl) 2017-10-30
SI1567529T2 (sl) 2021-08-31
AU2012205289A1 (en) 2012-08-09
EA007120B1 (ru) 2006-06-30
CY1115665T1 (el) 2017-01-25
AU2003271740B2 (en) 2010-05-13
SI2314591T1 (sl) 2014-11-28
DK1567529T4 (da) 2021-05-10
US20140171499A1 (en) 2014-06-19
AP2004003191A0 (en) 2004-12-31
EA007120B8 (ru) 2012-03-30
KR20050008715A (ko) 2005-01-21
US20050250845A1 (en) 2005-11-10
PL374321A1 (en) 2005-10-17
BRPI0311176B1 (pt) 2019-08-20
AU2003271740A1 (en) 2003-12-31
EP1567529B2 (en) 2021-02-24
DK1567529T3 (da) 2014-09-15
JP2005533068A (ja) 2005-11-04
MXPA04011427A (es) 2005-02-17
US20170260196A1 (en) 2017-09-14
US20210179631A1 (en) 2021-06-17
EP2314591B1 (en) 2014-06-18
WO2003106461A3 (en) 2004-05-13
EP1567529A2 (en) 2005-08-31
ES2498370T3 (es) 2014-09-24
IL165140A0 (en) 2005-12-18

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