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

    • 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (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)
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 (25)

Country Link
US (8) US7700645B2 (es)
EP (4) EP2767539B1 (es)
JP (1) JP4864320B2 (es)
KR (2) KR20100119906A (es)
CN (1) CN100475819C (es)
AP (1) AP2052A (es)
AU (2) AU2003271740B2 (es)
BR (1) BRPI0311176B8 (es)
CA (1) CA2485834C (es)
CY (3) CY1117928T1 (es)
DK (3) DK1567529T4 (es)
EA (1) EA007120B8 (es)
ES (4) ES2498370T5 (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) SI2314591T2 (es)
WO (1) WO2003106461A2 (es)
ZA (1) ZA200410154B (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US7700645B2 (en) 2002-05-16 2010-04-20 Tibotec Pharmaceuticals Ltd. 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
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
ES2331257T3 (es) 2005-02-25 2009-12-28 Tibotec Pharmaceuticals Sintesis de precursores de inhibidores de proteasas.
RS51675B (sr) * 2006-11-09 2011-10-31 Tibotec Pharmaceuticals Metode za dobivanje heksahidrofuro[2,3-b]furan-3-ola
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.
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
WO2010086844A1 (en) * 2009-01-29 2010-08-05 Mapi Pharma Hk Limited Polymorphs of darunavir
CA2776807C (en) * 2009-09-17 2018-10-16 Mylan 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.
WO2011073993A1 (en) 2009-12-16 2011-06-23 Hetero Research Foundation Polymorphs of darunavir
WO2011083287A2 (en) * 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof
PL2528923T3 (pl) 2010-01-28 2015-01-30 Mapi Pharma Ltd Sposób wytwarzania darunawiru i pochodnych darunawiru
PT2571355T (pt) 2010-05-20 2016-10-17 Hetero Research Foundation Sal de cloridrato cristalino de darunavir
WO2012107889A1 (en) 2011-02-10 2012-08-16 Ranbaxy Laboratories Limited Process for the preparation of amorphous darunavir
PL2729130T3 (pl) 2011-07-07 2018-02-28 Janssen Sciences Ireland Uc Preparaty kombinowane darunawiru
US9216990B2 (en) 2011-12-05 2015-12-22 Mylan Labs Limited Crystalline Darunavir
WO2013108105A2 (en) * 2012-01-18 2013-07-25 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
US9227990B2 (en) 2012-10-29 2016-01-05 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
WO2016092527A1 (en) * 2014-12-12 2016-06-16 Sun Pharmaceutical Industries Limited A process for the preparation of dolutegravir
WO2016092525A1 (en) * 2014-12-12 2016-06-16 Lupin Limited Darunavir n-propanol solvate and process for preparation thereof
CN107428724B (zh) 2015-03-19 2021-07-02 迈科维亚医药公司 抗真菌化合物及制备方法
WO2018029565A1 (en) 2016-08-08 2018-02-15 Hetero Labs Limited A multi-class anti-retroviral composition
US11045423B2 (en) 2016-08-08 2021-06-29 Hetero Labs Limited Anti-retroviral compositions
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

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
CN1072215C (zh) 1995-02-22 2001-10-03 赫彻斯特药品和化学品公司 无定形吡咯他尼、吡咯他尼多晶型物,其制备方法和用途
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
BR9916750A (pt) 1998-11-19 2001-11-06 Du Pont Pharm Co Compostos inibidores de transcriptase reversa, composições farmacêuticas, métodos de tratamento de infecções por vìrus da imunodeficiência humana, processos de preparação do composto e forma cristalina do mesmo
EP1159278B1 (en) 1999-02-12 2005-11-30 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
US7700645B2 (en) 2002-05-16 2010-04-20 Tibotec Pharmaceuticals Ltd. Pseudopolymorphic forms of a 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)

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

Similar Documents

Publication Publication Date Title
AP2004003191A0 (en) Pseudopolymorphic forms of HIV protease inhibitor.
PL375486A1 (en) Potent inhibitor of hcv serine protease
GB0125445D0 (en) Protease Inhibitors
EP1549316A4 (en) HAMMER OF TFGbeta
AU2003213776A1 (en) Carbamates as hiv protease inhibitors
EP1483254A4 (en) INHIBITORS OF ANTI-RESISTANCE RETROVIRAL PROTEASE
IL165475A0 (en) Nitrooxyderivatives of eyclooxygenase-2 inhibitors
AU2003277891A1 (en) Hcv ns-3 serine protease inhibitors
AU2003269984A8 (en) Protease inhibitors
EP1401453A4 (en) PROTEASE INHIBITORS
AU2003287325A8 (en) N-cycloalkylglycines as hiv protease inhibitors
AU2003263738A8 (en) Protease inhibitors
AU2001280634A1 (en) Salt forms of an hiv protease inhibitor
GB0123467D0 (en) Carbocyclic HIV Protease inhibitors
AU2003304496A8 (en) Protease inhibitors
GB0200479D0 (en) Fluorogenic protease substrates
AU2003233642A8 (en) Protease inhibitors
IL160626A0 (en) Antiviral protease inhibitors
AU2003252417A1 (en) Protease inhibitor
ZA200500560B (en) Potent inhibitor of HCV serine protease
AU2003269878A8 (en) Protease inhibitors
AU2003265240A8 (en) Protease inhibitors
AU2002255485A8 (en) Hiv/fiv protease inhibitors
GB0104691D0 (en) Enzyme inhibitor
TW578899U (en) Switch of tool