AU2010340799B2 - Darunavir polymorph and process for preparation thereof - Google Patents

Darunavir polymorph and process for preparation thereof Download PDF

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Publication number
AU2010340799B2
AU2010340799B2 AU2010340799A AU2010340799A AU2010340799B2 AU 2010340799 B2 AU2010340799 B2 AU 2010340799B2 AU 2010340799 A AU2010340799 A AU 2010340799A AU 2010340799 A AU2010340799 A AU 2010340799A AU 2010340799 B2 AU2010340799 B2 AU 2010340799B2
Authority
AU
Australia
Prior art keywords
darunavir
crystalline
darunavir hydrate
hydrate
water
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2010340799A
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English (en)
Other versions
AU2010340799A1 (en
Inventor
Rajendra Narayanrao Kankan
Manjinder Singh Phull
Dharmaraj Ramachandra Rao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cipla Ltd
Original Assignee
Cipla 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
Application filed by Cipla Ltd filed Critical Cipla Ltd
Publication of AU2010340799A1 publication Critical patent/AU2010340799A1/en
Application granted granted Critical
Publication of AU2010340799B2 publication Critical patent/AU2010340799B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2010340799A 2010-01-05 2010-10-06 Darunavir polymorph and process for preparation thereof Ceased AU2010340799B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN33MU2010 2010-01-05
IN33/MUM/2010 2010-01-05
PCT/GB2010/001874 WO2011083287A2 (en) 2010-01-05 2010-10-06 Darunavir polymorph and process for preparation thereof

Publications (2)

Publication Number Publication Date
AU2010340799A1 AU2010340799A1 (en) 2012-07-05
AU2010340799B2 true AU2010340799B2 (en) 2015-06-11

Family

ID=43125640

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2010340799A Ceased AU2010340799B2 (en) 2010-01-05 2010-10-06 Darunavir polymorph and process for preparation thereof

Country Status (9)

Country Link
US (2) US20130029945A1 (enExample)
EP (1) EP2521728B1 (enExample)
JP (2) JP2013516397A (enExample)
KR (1) KR20120123077A (enExample)
AU (1) AU2010340799B2 (enExample)
CA (1) CA2785998A1 (enExample)
NZ (1) NZ600994A (enExample)
WO (1) WO2011083287A2 (enExample)
ZA (1) ZA201204365B (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2503551T5 (es) 2002-05-16 2021-10-28 Janssen Sciences Ireland Unlimited Co Formas pseudopolimórficas de un inhibidor de la proteasa de VIH
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
EP2528923B1 (en) 2010-01-28 2014-07-30 Mapi Pharma Limited Process for the preparation of darunavir and darunavir intermediates
WO2013114382A1 (en) 2011-12-05 2013-08-08 Mylan Laboratories Ltd Crystalline 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
ES2848216T3 (es) 2012-07-24 2021-08-05 Laurus Labs Ltd Un proceso para la preparación de Darunavir
WO2016092525A1 (en) 2014-12-12 2016-06-16 Lupin Limited Darunavir n-propanol solvate and process for preparation thereof
CN106854212A (zh) * 2015-12-08 2017-06-16 浙江九洲药业股份有限公司 一种达芦那韦无定型的制备方法
CN106242307A (zh) * 2016-08-11 2016-12-21 京东方科技集团股份有限公司 用于强化制品的边缘的方法、玻璃及显示装置
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
CN108794498A (zh) * 2017-05-03 2018-11-13 江苏瑞科医药科技有限公司 一种达芦那韦无定型的制备方法
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
WO2003106461A2 (en) * 2002-05-16 2003-12-24 Tibotec Pharmaceuticals Ltd Pseudopolymorphic forms of a hiv protease inhibitor
WO2011073993A1 (en) * 2009-12-16 2011-06-23 Hetero Research Foundation Polymorphs of darunavir

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU7669794A (en) 1993-08-24 1995-03-21 G.D. Searle & Co. Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
JP4776775B2 (ja) 1998-06-23 2011-09-21 アメリカ合衆国 Ｈｉｖ感染哺乳動物を治療するための医薬組成物
DE602004021640D1 (de) 2003-12-23 2009-07-30 Tibotec Pharm Ltd Verfahren zur herstellung von (1s,2r)-3-ää(4-aminophenyl)sulfonylü(isobutyl)aminoü-1-benzyl-2-hydroxypropylcarbamidsäure-(3r,3as,6ar)-hexahydrofuroä2,3-büfuran-3-ylester
WO2011048604A2 (en) * 2009-09-17 2011-04-28 Matrix Laboratories Limited An improved process for the preparation of darunavir

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003106461A2 (en) * 2002-05-16 2003-12-24 Tibotec Pharmaceuticals Ltd Pseudopolymorphic forms of a hiv protease inhibitor
WO2011073993A1 (en) * 2009-12-16 2011-06-23 Hetero Research Foundation Polymorphs of darunavir

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GYSEGHEM, E. V. et al., European Journal of Pharmaceutical Sciences, 2009, Vol. 38, pages 489-497 *

Also Published As

Publication number Publication date
US20130029945A1 (en) 2013-01-31
CA2785998A1 (en) 2011-07-14
WO2011083287A2 (en) 2011-07-14
KR20120123077A (ko) 2012-11-07
EP2521728A2 (en) 2012-11-14
JP2016028085A (ja) 2016-02-25
NZ600994A (en) 2014-04-30
WO2011083287A3 (en) 2011-09-15
JP2013516397A (ja) 2013-05-13
EP2521728B1 (en) 2016-09-07
AU2010340799A1 (en) 2012-07-05
ZA201204365B (en) 2013-12-23
US20150141383A1 (en) 2015-05-21

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired