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EA007120B8 - Псевдополиморфные формы ингибитора вич-протеазы - Google Patents

Псевдополиморфные формы ингибитора вич-протеазы

Info

Publication number
EA007120B8
EA007120B8 EA200401503A EA200401503A EA007120B8 EA 007120 B8 EA007120 B8 EA 007120B8 EA 200401503 A EA200401503 A EA 200401503A EA 200401503 A EA200401503 A EA 200401503A EA 007120 B8 EA007120 B8 EA 007120B8
Authority
EA
Eurasian Patent Office
Prior art keywords
protease inhibitor
hiv protease
pseudopolymorphic forms
forms
pseudopolymorphic
Prior art date
Application number
EA200401503A
Other languages
English (en)
Other versions
EA007120B1 (ru
EA200401503A1 (ru
Inventor
Ханс Вим Питер Вермеерш
Даниел Джосеф Кристиан Тоне
Люк Донне Мари-Луиз Янссенс
Пиет Том Берт Пауль Вигеринк
Original Assignee
Тиботек Фармасьютикалз Лтд.
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=EA007120(B8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Тиботек Фармасьютикалз Лтд. filed Critical Тиботек Фармасьютикалз Лтд.
Publication of EA200401503A1 publication Critical patent/EA200401503A1/ru
Publication of EA007120B1 publication Critical patent/EA007120B1/ru
Publication of EA007120B8 publication Critical patent/EA007120B8/ru

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
    • A61P31/12—Antivirals
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)

Abstract

Раскрываются новые псевдополиморфные формы (3R,3aS,6aR)-гексагидрофуро[2,3-b]фуран-3-ил(1S,2R)-3-[[(4-аминофенил)сульфонил](изобутил)амино]-1-бензил-2-гидроксипропилкарбамата и способы их получения.
EA200401503A 2002-05-16 2003-05-16 Псевдополиморфные формы ингибитора вич-протеазы EA007120B8 (ru)

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 (3)

Publication Number Publication Date
EA200401503A1 EA200401503A1 (ru) 2005-06-30
EA007120B1 EA007120B1 (ru) 2006-06-30
EA007120B8 true EA007120B8 (ru) 2012-03-30

Family

ID=29724454

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200401503A EA007120B8 (ru) 2002-05-16 2003-05-16 Псевдополиморфные формы ингибитора вич-протеазы

Country Status (25)

Country Link
US (8) US7700645B2 (ru)
EP (4) EP2314591B2 (ru)
JP (1) JP4864320B2 (ru)
KR (2) KR20100119906A (ru)
CN (1) CN100475819C (ru)
AP (1) AP2052A (ru)
AU (2) AU2003271740B2 (ru)
BR (1) BRPI0311176B8 (ru)
CA (1) CA2485834C (ru)
CY (3) CY1115665T1 (ru)
DK (3) DK1567529T4 (ru)
EA (1) EA007120B8 (ru)
ES (4) ES2503551T5 (ru)
HR (1) HRP20041061B1 (ru)
HU (1) HUE034389T2 (ru)
IL (1) IL165140A0 (ru)
LT (1) LT2767539T (ru)
MX (1) MXPA04011427A (ru)
NO (1) NO331477B1 (ru)
NZ (1) NZ536497A (ru)
PL (1) PL215151B1 (ru)
PT (3) PT2314591E (ru)
SI (3) SI2767539T1 (ru)
WO (1) WO2003106461A2 (ru)
ZA (1) ZA200410154B (ru)

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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
HUE034389T2 (en) 2002-05-16 2018-02-28 Janssen Sciences Ireland Uc Pseudopolymorphic forms of an HIV protease inhibitor
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
RS51073B (sr) 2003-12-23 2010-10-31 Tibotec Pharmaceuticals Ltd. Proces za pripremanje (3r,3as,6ar)-heksahidrofuro│2,3-b│ furan-3-il (1s,2r)-3-││(4-aminofenil) sulfonil│(izobutil) amino │-1-benzil-2-hidroksipropilkarbamata
MX2007010378A (es) 2005-02-25 2007-09-25 Tibotec Pharm Ltd Sintesis del precursor inhibidor de la proteasa.
US8153829B2 (en) * 2006-11-09 2012-04-10 Janssen Pharmaceutica N.V. Methods for the preparation of hexahydrofuro[2,3-B]furan-3-ol
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
US20120035142A1 (en) * 2009-01-29 2012-02-09 Mapi Pharma Limited Polymorphs of darunavir
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
HRP20170392T1 (hr) 2009-09-17 2017-06-02 Mylan Laboratories Limited Postupak za pripremu darunavira i njegovog amorfnog oblika
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.
EP2513116B1 (en) 2009-12-16 2015-08-19 Hetero Research Foundation Polymorphs of darunavir
WO2011083287A2 (en) 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof
CN102725295A (zh) 2010-01-28 2012-10-10 Mapi医药公司 制备达芦那韦和达芦那韦中间体的方法
US8853430B2 (en) * 2010-05-20 2014-10-07 Hetero Research Foundation Crystalline hydrochloride salt of darunavir
WO2012107889A1 (en) 2011-02-10 2012-08-16 Ranbaxy Laboratories Limited Process for the preparation of amorphous darunavir
SI2729130T1 (en) 2011-07-07 2018-03-30 Janssen Sciences Ireland Uc Combined formulations of darunavir
US9216990B2 (en) 2011-12-05 2015-12-22 Mylan Labs Limited Crystalline Darunavir
US9643976B2 (en) * 2012-01-18 2017-05-09 Aurobindo Pharma Ltd. 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
ES2969589T3 (es) * 2012-07-24 2024-05-21 Laurus Labs Ltd Solvato de Propionato de Darunavir
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
KR102603277B1 (ko) 2015-03-19 2023-11-17 마이코비아 파마슈티컬즈, 인코포레이티드 항진균성 화합물 및 이의 제조 방법
BR112019002120A2 (pt) 2016-08-08 2019-05-14 Hetero Labs Limited composição anti-retroviral de várias classes
US11045423B2 (en) 2016-08-08 2021-06-29 Hetero Labs Limited Anti-retroviral compositions
WO2018081292A1 (en) 2016-10-27 2018-05-03 Gilead Sciences, Inc. Crystalline forms of darunavir free base, hydrate, solvates and salts
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

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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
CA2213693C (en) 1995-02-22 2008-04-15 Hoechst Pharmaceuticals & Chemicals K.K. Amorphous piretanide, piretanide polymorphs, process for their preparation and their use
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
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
AU1735000A (en) 1998-11-19 2000-06-05 Du Pont Pharmaceuticals Company Crystalline (-)-6- chloro-4- cyclopropylethynyl- 4-trifluoromethyl- 3,4-dihydro-2(1h)-quinazolinone
EP1637518A3 (en) 1999-02-12 2013-04-10 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
HUE034389T2 (en) 2002-05-16 2018-02-28 Janssen Sciences Ireland Uc Pseudopolymorphic forms of an HIV protease inhibitor
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)

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Title
BORKA L. ET AL.: "Crystal polymorphism of pharmaceuticals", ACTA PHARMACEUTICA JUGOSLAVICA, SAVEZ FARMACEUTSKIH DRUSTAVA JUGOSLAVIJA, ZAGREB, YU, vol. 40, 1990, pages 71-94, XP002195530, ISSN: 0001-6667, see page 81, introduction, the whole document *
GHOSH A. K. ET AL.: "Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 8, no. 6, 17 March 1998 (1998-03-17), pages 687-690, XP004136945, ISSN: 0960-894X, cited in the application, see page 689, cpd. 13, the whole document *
GIRON ET AL.: "Thermal analysis and calorimetric methods in the characterisation of polymorphs and solvates", THERMOCHIMICA ACTA, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 248, 1995, pages 1-59, XP002101808, ISSN: 0040-6031, see pages 3-11, chapter 2, the whole document *
GRUNENBERG A. ET AL.: "THEORETICAL DERIVATION AND PRACTICAL APPLICATION OF ENERGY/TEMPERATURE DIAGRAMS AS AN INSTRUMENT IN PREFORMULATION STUDIES OF POLYMORPHIC DRUG SUBSTANCES", INTERNATIONAL JOURNAL OF PHARMACEUTICS, AMSTERDAM, NL, vol. 129, 1996, pages 147-158, XP000909867, ISSN: 0378-5173, see page 147, introduction, the whole document *

Also Published As

Publication number Publication date
WO2003106461A3 (en) 2004-05-13
DK2314591T3 (da) 2014-09-22
HK1081969A1 (en) 2006-05-26
JP2005533068A (ja) 2005-11-04
ES2638412T3 (es) 2017-10-20
EP1567529A2 (en) 2005-08-31
US20210179631A1 (en) 2021-06-17
ES2503551T5 (es) 2021-10-28
WO2003106461A2 (en) 2003-12-24
SI2767539T1 (sl) 2017-10-30
US20140171499A1 (en) 2014-06-19
ES2498370T3 (es) 2014-09-24
LT2767539T (lt) 2017-09-25
JP4864320B2 (ja) 2012-02-01
SI2314591T1 (sl) 2014-11-28
EP2314591B1 (en) 2014-06-18
DK1567529T4 (da) 2021-05-10
AU2003271740A1 (en) 2003-12-31
HRP20041061B1 (hr) 2015-02-27
US20050250845A1 (en) 2005-11-10
PT2314591E (pt) 2014-09-19
SI1567529T1 (sl) 2014-11-28
AU2003271740B2 (en) 2010-05-13
DK2314591T4 (da) 2021-05-10
HRP20041061A2 (en) 2006-07-31
CA2485834C (en) 2007-07-17
US7700645B2 (en) 2010-04-20
BRPI0311176B8 (pt) 2021-05-25
PT2767539T (pt) 2017-08-28
KR20100119906A (ko) 2010-11-11
HUE034389T2 (en) 2018-02-28
AP2052A (en) 2009-10-05
US20130303790A1 (en) 2013-11-14
SI2314591T2 (sl) 2021-08-31
SI1567529T2 (sl) 2021-08-31
EP2314591B2 (en) 2021-02-24
DK1567529T3 (da) 2014-09-15
EP3045460A1 (en) 2016-07-20
CA2485834A1 (en) 2003-12-24
US20170260196A1 (en) 2017-09-14
BR0311176A (pt) 2005-03-15
US10858369B2 (en) 2020-12-08
CY1119311T1 (el) 2018-02-14
EP2314591A1 (en) 2011-04-27
US20150336980A1 (en) 2015-11-26
KR20050008715A (ko) 2005-01-21
CN100475819C (zh) 2009-04-08
DK2767539T3 (en) 2017-09-11
ES2728735T3 (es) 2019-10-28
EP1567529B1 (en) 2014-06-18
PT1567529E (pt) 2014-09-09
NO331477B1 (no) 2012-01-16
AP2004003191A0 (en) 2004-12-31
NO20045409L (no) 2004-12-10
EP2767539B1 (en) 2017-07-12
PL374321A1 (en) 2005-10-17
EP3045460B1 (en) 2019-04-17
US10000504B2 (en) 2018-06-19
US20180312517A1 (en) 2018-11-01
US20100204316A1 (en) 2010-08-12
NZ536497A (en) 2006-08-31
IL165140A0 (en) 2005-12-18
US8518987B2 (en) 2013-08-27
CN1668623A (zh) 2005-09-14
BRPI0311176B1 (pt) 2019-08-20
CY1117928T1 (el) 2017-05-17
EP2767539A1 (en) 2014-08-20
EP1567529B2 (en) 2021-02-24
PL215151B1 (pl) 2013-10-31
CY1115665T1 (el) 2017-01-25
MXPA04011427A (es) 2005-02-17
EA007120B1 (ru) 2006-06-30
EA200401503A1 (ru) 2005-06-30
ES2503551T3 (es) 2014-10-07
AU2012205289A1 (en) 2012-08-09
ES2498370T5 (es) 2021-11-24
ZA200410154B (en) 2005-12-28
KR101128370B1 (ko) 2012-04-23

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