NO331477B1 - Etanolat pseudopolymorfe former av en HIV-proteaseinhibitor, fremgangsmate ved fremstilling derav samt anvendelse derav - Google Patents

Etanolat pseudopolymorfe former av en HIV-proteaseinhibitor, fremgangsmate ved fremstilling derav samt anvendelse derav Download PDF

Info

Publication number: NO331477B1
Authority: NO; Norway
Prior art keywords: compound; ethanol; formula; pseudopolymorph; ethanolate
Prior art date: 2002-05-16

Application number

NO20045409A

Other languages

English (en)

Norwegian (no)

Other versions

NO20045409L (no

Inventor

Daniel Joseph Christiaan Thone

Hans Wim Pieter Vermeersch

Luc Donne Marie-Louise Janssens

Piet Tom Bert Paul Wigerinck

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.)

2002-05-16

Filing date

2004-12-10

Publication date

2012-01-16

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=NO331477(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2004-12-10 Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd

2004-12-10 Publication of NO20045409L publication Critical patent/NO20045409L/no

2012-01-16 Publication of NO331477B1 publication Critical patent/NO331477B1/no

Links

238000000034 method Methods 0.000 title claims abstract description 41
238000002360 preparation method Methods 0.000 title claims abstract description 17
HHFAWKCIHAUFRX-UHFFFAOYSA-N ethoxide Chemical compound CC[O-] HHFAWKCIHAUFRX-UHFFFAOYSA-N 0.000 title claims description 15
239000004030 hiv protease inhibitor Substances 0.000 title description 2
229940122440 HIV protease inhibitor Drugs 0.000 title 1
CJBJHOAVZSMMDJ-HEXNFIEUSA-N darunavir Chemical compound C([C@@H]([C@H](O)CN(CC(C)C)S(=O)(=O)C=1C=CC(N)=CC=1)NC(=O)O[C@@H]1[C@@H]2CCO[C@@H]2OC1)C1=CC=CC=C1 CJBJHOAVZSMMDJ-HEXNFIEUSA-N 0.000 claims abstract description 10
230000008569 process Effects 0.000 claims abstract description 10
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 105
150000001875 compounds Chemical class 0.000 claims description 66
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 25
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108010010369 HIV Protease Proteins 0.000 claims description 4
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OGHBATFHNDZKSO-UHFFFAOYSA-N propan-2-olate Chemical compound CC(C)[O-] OGHBATFHNDZKSO-UHFFFAOYSA-N 0.000 claims 1
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LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 2
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FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
238000005079 FT-Raman Methods 0.000 description 1
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FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
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239000010775 animal oil Substances 0.000 description 1
XKRFYHLGVUSROY-UHFFFAOYSA-N argon Substances [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 description 1
229910052786 argon Inorganic materials 0.000 description 1
QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
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239000011777 magnesium Substances 0.000 description 1
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ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
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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)

NO20045409A 2002-05-16 2004-12-10 Etanolat pseudopolymorfe former av en HIV-proteaseinhibitor, fremgangsmate ved fremstilling derav samt anvendelse derav NO331477B1 (no)

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
NO20045409L NO20045409L (no)	2004-12-10
NO331477B1 true NO331477B1 (no)	2012-01-16

Family

ID=29724454

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO20045409A NO331477B1 (no)	2002-05-16	2004-12-10	Etanolat pseudopolymorfe former av en HIV-proteaseinhibitor, fremgangsmate ved fremstilling derav samt anvendelse derav

Country Status (25)

Country	Link
US (8)	US7700645B2 (pt)
EP (4)	EP1567529B2 (pt)
JP (1)	JP4864320B2 (pt)
KR (2)	KR101128370B1 (pt)
CN (1)	CN100475819C (pt)
AP (1)	AP2052A (pt)
AU (2)	AU2003271740B2 (pt)
BR (1)	BRPI0311176B8 (pt)
CA (1)	CA2485834C (pt)
CY (3)	CY1115665T1 (pt)
DK (3)	DK2767539T3 (pt)
EA (1)	EA007120B8 (pt)
ES (4)	ES2498370T5 (pt)
HR (1)	HRP20041061B1 (pt)
HU (1)	HUE034389T2 (pt)
IL (1)	IL165140A0 (pt)
LT (1)	LT2767539T (pt)
MX (1)	MXPA04011427A (pt)
NO (1)	NO331477B1 (pt)
NZ (1)	NZ536497A (pt)
PL (1)	PL215151B1 (pt)
PT (3)	PT1567529E (pt)
SI (3)	SI2767539T1 (pt)
WO (1)	WO2003106461A2 (pt)
ZA (1)	ZA200410154B (pt)

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
ES2498370T5 (es) *	2002-05-16	2021-11-24	Janssen Sciences Ireland Unlimited Co	Formas pseudopolimórficas de un inhibidor de la proteasa de VIH
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
ME01059B (me)	2003-12-23	2012-10-20	Janssen Sciences Ireland Uc	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
RU2421459C2 (ru)	2005-02-25	2011-06-20	Тиботек Фармасьютикалз Лтд.	Синтез предшественника ингибитора протеазы
MX2009004957A (es) *	2006-11-09	2009-05-19	Tibotec Pharm Ltd	Metodos para la preparacion de hexahidrofuro[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.
CA2750774A1 (en) *	2009-01-29	2010-08-05	Mapi Pharma Limited	Polymorphs of darunavir
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
WO2011051978A2 (en)	2009-10-30	2011-05-05	Lupin Limited	A novel process for preparation of darunavir and darunavir ethanolate of fine particle size
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Publication number	Publication date
AU2003271740A1 (en)	2003-12-31
HRP20041061B1 (hr)	2015-02-27
DK1567529T4 (da)	2021-05-10
EP2767539B1 (en)	2017-07-12
ES2498370T3 (es)	2014-09-24
ZA200410154B (en)	2005-12-28
KR101128370B1 (ko)	2012-04-23
ES2638412T3 (es)	2017-10-20
US20100204316A1 (en)	2010-08-12
SI2314591T1 (sl)	2014-11-28
EA007120B1 (ru)	2006-06-30
US10000504B2 (en)	2018-06-19
HUE034389T2 (en)	2018-02-28
ES2503551T5 (es)	2021-10-28
PL215151B1 (pl)	2013-10-31
ES2498370T5 (es)	2021-11-24
US20130303790A1 (en)	2013-11-14
US20210179631A1 (en)	2021-06-17
EA007120B8 (ru)	2012-03-30
CY1119311T1 (el)	2018-02-14
EA200401503A1 (ru)	2005-06-30
AP2004003191A0 (en)	2004-12-31
EP1567529B1 (en)	2014-06-18
US20050250845A1 (en)	2005-11-10
US10858369B2 (en)	2020-12-08
CN1668623A (zh)	2005-09-14
BRPI0311176B8 (pt)	2021-05-25
US20150336980A1 (en)	2015-11-26
EP3045460A1 (en)	2016-07-20
JP2005533068A (ja)	2005-11-04
AU2003271740B2 (en)	2010-05-13
BRPI0311176B1 (pt)	2019-08-20
AU2012205289A1 (en)	2012-08-09
ES2503551T3 (es)	2014-10-07
EP2314591B2 (en)	2021-02-24
ES2728735T3 (es)	2019-10-28
EP1567529B2 (en)	2021-02-24
JP4864320B2 (ja)	2012-02-01
MXPA04011427A (es)	2005-02-17
KR20050008715A (ko)	2005-01-21
EP2314591A1 (en)	2011-04-27
US20170260196A1 (en)	2017-09-14
US20140171499A1 (en)	2014-06-19
PT1567529E (pt)	2014-09-09
AP2052A (en)	2009-10-05
CN100475819C (zh)	2009-04-08
CY1115665T1 (el)	2017-01-25
IL165140A0 (en)	2005-12-18
BR0311176A (pt)	2005-03-15
US8518987B2 (en)	2013-08-27
KR20100119906A (ko)	2010-11-11
DK1567529T3 (da)	2014-09-15
CY1117928T1 (el)	2017-05-17
CA2485834C (en)	2007-07-17
EP2767539A1 (en)	2014-08-20
DK2314591T3 (da)	2014-09-22
HK1081969A1 (en)	2006-05-26
WO2003106461A3 (en)	2004-05-13
PL374321A1 (en)	2005-10-17
NZ536497A (en)	2006-08-31
PT2314591E (pt)	2014-09-19
DK2767539T3 (en)	2017-09-11
LT2767539T (lt)	2017-09-25
WO2003106461A2 (en)	2003-12-24
US20180312517A1 (en)	2018-11-01
HRP20041061A2 (en)	2006-07-31
SI2767539T1 (sl)	2017-10-30
DK2314591T4 (da)	2021-05-10
EP3045460B1 (en)	2019-04-17
SI1567529T1 (sl)	2014-11-28
SI2314591T2 (sl)	2021-08-31
NO20045409L (no)	2004-12-10
SI1567529T2 (sl)	2021-08-31
US7700645B2 (en)	2010-04-20
EP2314591B1 (en)	2014-06-18
CA2485834A1 (en)	2003-12-24
PT2767539T (pt)	2017-08-28
EP1567529A2 (en)	2005-08-31

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HK1081969B (en)	2014-09-05	Pseudopolymorphic forms of a hiv protease inhibitor
KR20230117419A (ko)	2023-08-08	화합물의 결정형 및 이의 제조 방법과 적용
HK40074347A (en)	2022-12-30	Salts and crystalline forms of a taar1 agonist