EA007120B8 - Псевдополиморфные формы ингибитора вич-протеазы - Google Patents
Псевдополиморфные формы ингибитора вич-протеазыInfo
- 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
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
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.
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 (26)
Country | Link |
---|---|
US (8) | US7700645B2 (ru) |
EP (4) | EP2314591B2 (ru) |
JP (1) | JP4864320B2 (ru) |
KR (2) | KR101128370B1 (ru) |
CN (1) | CN100475819C (ru) |
AP (1) | AP2052A (ru) |
AU (2) | AU2003271740B2 (ru) |
BR (1) | BRPI0311176B8 (ru) |
CA (1) | CA2485834C (ru) |
CY (3) | CY1117928T1 (ru) |
DK (3) | DK1567529T4 (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) | PT1567529E (ru) |
SI (3) | SI1567529T2 (ru) |
WO (1) | WO2003106461A2 (ru) |
ZA (1) | ZA200410154B (ru) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT1088098E (pt) | 1998-06-23 | 2011-05-25 | Univ Illinois | Medicamento para tratar mam?feros infectados com hiv |
EA007120B8 (ru) | 2002-05-16 | 2012-03-30 | Тиботек Фармасьютикалз Лтд. | Псевдополиморфные формы ингибитора вич-протеазы |
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 |
KR101333627B1 (ko) | 2005-02-25 | 2013-11-27 | 얀센 알 앤드 디 아일랜드 | 프로테아제 저해제 전구체 합성 |
WO2008055970A2 (en) * | 2006-11-09 | 2008-05-15 | Tibotec Pharmaceuticals Ltd. | 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. |
US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
MX2011007790A (es) * | 2009-01-29 | 2011-11-18 | Mapi Pharma Ltd | Polimorfos de darunavir. |
US8703980B2 (en) * | 2009-09-17 | 2014-04-22 | Siva Rama Prasad Vellanki | 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. |
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 |
WO2011145099A1 (en) * | 2010-05-20 | 2011-11-24 | 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 |
JP6122427B2 (ja) | 2011-07-07 | 2017-04-26 | ヤンセン・サイエンシズ・アイルランド・ユーシー | ダルナビル複合製剤 |
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 |
US9475821B2 (en) * | 2012-07-24 | 2016-10-25 | Laurus Labs Private Limited | Process for preparation of Darunavir |
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 |
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 |
EP3496719B1 (en) | 2016-08-08 | 2023-06-14 | Hetero Labs Limited | A multi-class anti-retroviral composition |
BR112019002132A2 (pt) | 2016-08-08 | 2019-05-14 | Hetero Labs Limited | composições anti-retrovirais |
US10407438B2 (en) | 2016-10-27 | 2019-09-10 | Gilead Sciences, Inc. | Crystalline forms of 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)
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)
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 |
ES2150105T3 (es) | 1995-02-22 | 2000-11-16 | Aventis Pharma Ltd | Piretanida amorfa, polimorfos de piretanida, proceso para su preparacion y su uso. |
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 |
EP1131303A1 (en) | 1998-11-19 | 2001-09-12 | Du Pont Pharmaceuticals Company | Crystalline (-)-6- chloro-4- cyclopropylethynyl- 4-trifluoromethyl- 3,4-dihydro- 2(1h)-quinazolinone |
EP1159278B1 (en) | 1999-02-12 | 2005-11-30 | Vertex Pharmaceuticals Incorporated | Inhibitors of aspartyl protease |
EA007120B8 (ru) | 2002-05-16 | 2012-03-30 | Тиботек Фармасьютикалз Лтд. | Псевдополиморфные формы ингибитора вич-протеазы |
WO2011083287A2 (en) * | 2010-01-05 | 2011-07-14 | Cipla Limited | Darunavir polymorph and process for preparation thereof |
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2003
- 2003-05-16 EA EA200401503A patent/EA007120B8/ru unknown
- 2003-05-16 PT PT37535713T patent/PT1567529E/pt unknown
- 2003-05-16 AP AP2004003191A patent/AP2052A/xx active
- 2003-05-16 CN CNB038164590A patent/CN100475819C/zh not_active Expired - Lifetime
- 2003-05-16 SI SI200332389T patent/SI1567529T2/sl unknown
- 2003-05-16 PT PT141686865T patent/PT2767539T/pt unknown
- 2003-05-16 PT PT101808319T patent/PT2314591E/pt unknown
- 2003-05-16 EP EP10180831.9A patent/EP2314591B2/en not_active Expired - Lifetime
- 2003-05-16 EP EP03753571.3A patent/EP1567529B2/en not_active Expired - Lifetime
- 2003-05-16 ES ES03753571T patent/ES2498370T5/es not_active Expired - Lifetime
- 2003-05-16 EP EP16158480.0A patent/EP3045460B1/en not_active Expired - Lifetime
- 2003-05-16 KR KR1020047018426A patent/KR101128370B1/ko active IP Right Grant
- 2003-05-16 KR KR1020107024106A patent/KR20100119906A/ko not_active Application Discontinuation
- 2003-05-16 AU AU2003271740A patent/AU2003271740B2/en not_active Revoked
- 2003-05-16 SI SI200332383T patent/SI2314591T2/sl unknown
- 2003-05-16 JP JP2004513292A patent/JP4864320B2/ja not_active Expired - Lifetime
- 2003-05-16 NZ NZ536497A patent/NZ536497A/en not_active IP Right Cessation
- 2003-05-16 ES ES14168686.5T patent/ES2638412T3/es not_active Expired - Lifetime
- 2003-05-16 ES ES10180831T patent/ES2503551T5/es not_active Expired - Lifetime
- 2003-05-16 DK DK03753571.3T patent/DK1567529T4/da active
- 2003-05-16 MX MXPA04011427A patent/MXPA04011427A/es active IP Right Grant
- 2003-05-16 DK DK10180831.9T patent/DK2314591T4/da active
- 2003-05-16 US US10/514,352 patent/US7700645B2/en active Active
- 2003-05-16 HU HUE14168686A patent/HUE034389T2/en unknown
- 2003-05-16 LT LTEP14168686.5T patent/LT2767539T/lt unknown
- 2003-05-16 CA CA002485834A patent/CA2485834C/en not_active Expired - Lifetime
- 2003-05-16 SI SI200332545T patent/SI2767539T1/sl unknown
- 2003-05-16 ES ES16158480T patent/ES2728735T3/es not_active Expired - Lifetime
- 2003-05-16 EP EP14168686.5A patent/EP2767539B1/en not_active Expired - Lifetime
- 2003-05-16 PL PL374321A patent/PL215151B1/pl unknown
- 2003-05-16 DK DK14168686.5T patent/DK2767539T3/en active
- 2003-05-16 BR BRPI0311176A patent/BRPI0311176B8/pt active IP Right Grant
- 2003-05-16 WO PCT/EP2003/050176 patent/WO2003106461A2/en active Application Filing
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2004
- 2004-11-10 IL IL16514004A patent/IL165140A0/xx unknown
- 2004-11-12 HR HRP20041061AA patent/HRP20041061B1/hr not_active IP Right Cessation
- 2004-12-10 NO NO20045409A patent/NO331477B1/no not_active IP Right Cessation
- 2004-12-15 ZA ZA2004/10154A patent/ZA200410154B/en unknown
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2006
- 2006-02-23 HK HK06102443.3A patent/HK1081969A1/xx not_active IP Right Cessation
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2009
- 2009-08-06 US US12/536,807 patent/US8518987B2/en not_active Expired - Lifetime
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2012
- 2012-07-03 AU AU2012205289A patent/AU2012205289A1/en active Pending
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2013
- 2013-07-11 US US13/939,494 patent/US20130303790A1/en not_active Abandoned
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2014
- 2014-02-19 US US14/183,712 patent/US20140171499A1/en not_active Abandoned
- 2014-09-17 CY CY20141100756T patent/CY1117928T1/el unknown
- 2014-09-17 CY CY20141100755T patent/CY1115665T1/el unknown
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2015
- 2015-08-04 US US14/817,827 patent/US20150336980A1/en not_active Abandoned
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2017
- 2017-05-22 US US15/600,932 patent/US10000504B2/en not_active Expired - Lifetime
- 2017-08-23 CY CY20171100896T patent/CY1119311T1/el unknown
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2018
- 2018-05-16 US US15/980,993 patent/US10858369B2/en not_active Expired - Lifetime
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2020
- 2020-10-30 US US17/085,096 patent/US20210179631A1/en not_active Abandoned
Patent Citations (2)
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)
Title |
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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 * |
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PD4A | Registration of transfer of a eurasian patent in accordance with the succession in title | ||
PC4A | Registration of transfer of a eurasian patent by assignment |