EA200401503A1 - Псевдополиморфные формы ингибитора вич-протеазы - Google Patents

Псевдополиморфные формы ингибитора вич-протеазы

Info

Publication number
EA200401503A1
EA200401503A1 EA200401503A EA200401503A EA200401503A1 EA 200401503 A1 EA200401503 A1 EA 200401503A1 EA 200401503 A EA200401503 A EA 200401503A EA 200401503 A EA200401503 A EA 200401503A EA 200401503 A1 EA200401503 A1 EA 200401503A1
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
EA007120B8 (ru
Inventor
Ханс Вим Питер Вермеерш
Даниел Джосеф Кристиан Тоне
Люк Донне Мари-Луиз Янссенс
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=EA200401503(A1) "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

  • 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)

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.Отчет о международном поиске был опубликован 2004.05.13.
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 true EA200401503A1 (ru) 2005-06-30
EA007120B1 EA007120B1 (ru) 2006-06-30
EA007120B8 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 (26)

Country Link
US (8) US7700645B2 (ru)
EP (4) EP1567529B2 (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) DK2767539T3 (ru)
EA (1) EA007120B8 (ru)
ES (4) ES2498370T5 (ru)
HK (1) HK1081969A1 (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) PT2767539T (ru)
SI (3) SI2314591T2 (ru)
WO (1) WO2003106461A2 (ru)
ZA (1) ZA200410154B (ru)

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CA2336160C (en) 1998-06-23 2015-02-17 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Use of compounds for treating hiv
AU2003271740B2 (en) 2002-05-16 2010-05-13 Janssen R&D Ireland Pseudopolymorphic forms of a 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.
PL2089371T3 (pl) * 2006-11-09 2011-06-30 Janssen Sciences Ireland Uc Sposoby wytwarzania heksahydrofuro[2,3-b]furan-3-olu
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
WO2011048604A2 (en) * 2009-09-17 2011-04-28 Matrix Laboratories Limited An improved process for the preparation 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.
CN102686594A (zh) * 2009-12-16 2012-09-19 熙德隆研究基金会 地瑞那韦的多晶型物
WO2011083287A2 (en) * 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof
WO2011092687A1 (en) 2010-01-28 2011-08-04 Mapi Pharma Hk Limited Process for the preparation of darunavir and darunavir intermediates
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
DK2729130T3 (en) 2011-07-07 2017-12-11 Janssen Sciences Ireland Uc Darunavir-COMBINATION FORMULATIONS
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
ES2969589T3 (es) * 2012-07-24 2024-05-21 Laurus Labs Ltd Solvato de Propionato de Darunavir
WO2014068265A1 (en) 2012-10-29 2014-05-08 Cipla Limited Antiviral phosphonate analogues and process for preparation thereof
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
AU2016233113B2 (en) 2015-03-19 2020-05-07 Mycovia Pharmaceuticals, Inc. Antifungal compounds and processes for making
BR112019002132A2 (pt) 2016-08-08 2019-05-14 Hetero Labs Limited composições anti-retrovirais
BR112019002120A2 (pt) 2016-08-08 2019-05-14 Hetero Labs Limited composição anti-retroviral de várias classes
EP3532478B1 (en) 2016-10-27 2021-05-26 Gilead Sciences, Inc. Crystalline form of darunavir free base
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

Family Cites Families (16)

* 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
ATE174587T1 (de) 1993-08-24 1999-01-15 Searle & Co Hydroxyaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
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
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
CA2336160C (en) * 1998-06-23 2015-02-17 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Use of compounds for treating hiv
US6225317B1 (en) 1998-11-19 2001-05-01 Dupont Pharmaceuticals Company Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone
SI1159278T1 (sl) 1999-02-12 2006-06-30 Vertex Pharma Inhibitorji aspartil proteaze
AU2003271740B2 (en) 2002-05-16 2010-05-13 Janssen R&D Ireland Pseudopolymorphic forms of a HIV protease inhibitor
WO2011083287A2 (en) * 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof

Also Published As

Publication number Publication date
HK1081969A1 (en) 2006-05-26
CY1115665T1 (el) 2017-01-25
US7700645B2 (en) 2010-04-20
EP2767539B1 (en) 2017-07-12
ZA200410154B (en) 2005-12-28
SI2767539T1 (sl) 2017-10-30
KR101128370B1 (ko) 2012-04-23
AP2004003191A0 (en) 2004-12-31
WO2003106461A3 (en) 2004-05-13
PT2767539T (pt) 2017-08-28
SI2314591T1 (sl) 2014-11-28
CY1117928T1 (el) 2017-05-17
CY1119311T1 (el) 2018-02-14
EP2314591A1 (en) 2011-04-27
US10000504B2 (en) 2018-06-19
US20210179631A1 (en) 2021-06-17
AU2012205289A1 (en) 2012-08-09
PL215151B1 (pl) 2013-10-31
BRPI0311176B1 (pt) 2019-08-20
CN100475819C (zh) 2009-04-08
EP1567529A2 (en) 2005-08-31
ES2498370T5 (es) 2021-11-24
NO20045409L (no) 2004-12-10
CA2485834A1 (en) 2003-12-24
US20150336980A1 (en) 2015-11-26
AP2052A (en) 2009-10-05
KR20050008715A (ko) 2005-01-21
DK2767539T3 (en) 2017-09-11
ES2503551T3 (es) 2014-10-07
DK1567529T4 (da) 2021-05-10
NO331477B1 (no) 2012-01-16
EP2314591B2 (en) 2021-02-24
EP3045460B1 (en) 2019-04-17
US20130303790A1 (en) 2013-11-14
BR0311176A (pt) 2005-03-15
US20050250845A1 (en) 2005-11-10
JP4864320B2 (ja) 2012-02-01
ES2728735T3 (es) 2019-10-28
BRPI0311176B8 (pt) 2021-05-25
SI1567529T2 (sl) 2021-08-31
ES2638412T3 (es) 2017-10-20
KR20100119906A (ko) 2010-11-11
NZ536497A (en) 2006-08-31
EP1567529B1 (en) 2014-06-18
JP2005533068A (ja) 2005-11-04
US20170260196A1 (en) 2017-09-14
EP3045460A1 (en) 2016-07-20
DK2314591T3 (da) 2014-09-22
US20180312517A1 (en) 2018-11-01
CA2485834C (en) 2007-07-17
CN1668623A (zh) 2005-09-14
DK1567529T3 (da) 2014-09-15
EP2314591B1 (en) 2014-06-18
EA007120B1 (ru) 2006-06-30
PT1567529E (pt) 2014-09-09
EP2767539A1 (en) 2014-08-20
US10858369B2 (en) 2020-12-08
AU2003271740A1 (en) 2003-12-31
AU2003271740B2 (en) 2010-05-13
LT2767539T (lt) 2017-09-25
DK2314591T4 (da) 2021-05-10
EA007120B8 (ru) 2012-03-30
US20140171499A1 (en) 2014-06-19
EP1567529B2 (en) 2021-02-24
IL165140A0 (en) 2005-12-18
HRP20041061B1 (hr) 2015-02-27
ES2503551T5 (es) 2021-10-28
PL374321A1 (en) 2005-10-17
PT2314591E (pt) 2014-09-19
HUE034389T2 (en) 2018-02-28
WO2003106461A2 (en) 2003-12-24
US20100204316A1 (en) 2010-08-12
ES2498370T3 (es) 2014-09-24
SI1567529T1 (sl) 2014-11-28
US8518987B2 (en) 2013-08-27
SI2314591T2 (sl) 2021-08-31
HRP20041061A2 (en) 2006-07-31
MXPA04011427A (es) 2005-02-17

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