WO2010131118A3 - Polymorphs of etravirine and processes for preparation thereof - Google Patents

Polymorphs of etravirine and processes for preparation thereof Download PDF

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Publication number
WO2010131118A3
WO2010131118A3 PCT/IB2010/001331 IB2010001331W WO2010131118A3 WO 2010131118 A3 WO2010131118 A3 WO 2010131118A3 IB 2010001331 W IB2010001331 W IB 2010001331W WO 2010131118 A3 WO2010131118 A3 WO 2010131118A3
Authority
WO
WIPO (PCT)
Prior art keywords
etravirine
polymorphs
processes
preparation
crystalline forms
Prior art date
Application number
PCT/IB2010/001331
Other languages
French (fr)
Other versions
WO2010131118A2 (en
Inventor
Maja Sepelj
Edislav Leksic
Marina Marinkovic
Irena Krizamanic
Original Assignee
Pliva Hrvatska D.O.O.
Teva Pharmaceuticals Usa , Inc.
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 Pliva Hrvatska D.O.O., Teva Pharmaceuticals Usa , Inc. filed Critical Pliva Hrvatska D.O.O.
Publication of WO2010131118A2 publication Critical patent/WO2010131118A2/en
Publication of WO2010131118A3 publication Critical patent/WO2010131118A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicinal Chemistry (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention provides novel crystalline forms of etravirine such as forms A, B, D, E, H, J, K, L and M, pharmaceutical compositions comprising the crystalline forms and method of using at least one of the crystalline forms or pharmaceutical compositions to treat HIV. Formula (I)
PCT/IB2010/001331 2009-05-12 2010-05-12 Polymorphs of etravirine and processes for preparation thereof WO2010131118A2 (en)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US17749609P 2009-05-12 2009-05-12
US61/177,496 2009-05-12
US22005609P 2009-06-24 2009-06-24
US61/220,056 2009-06-24
US22726009P 2009-07-21 2009-07-21
US61/227,260 2009-07-21
US23837509P 2009-08-31 2009-08-31
US61/238,375 2009-08-31
US26515709P 2009-11-30 2009-11-30
US61/265,157 2009-11-30

Publications (2)

Publication Number Publication Date
WO2010131118A2 WO2010131118A2 (en) 2010-11-18
WO2010131118A3 true WO2010131118A3 (en) 2011-01-06

Family

ID=42651498

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2010/001331 WO2010131118A2 (en) 2009-05-12 2010-05-12 Polymorphs of etravirine and processes for preparation thereof

Country Status (1)

Country Link
WO (1) WO2010131118A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA106972C2 (en) * 2009-06-22 2014-11-10 Емк'Юр Фармас'Ютікалз Лімітед A method for synthesis of diarylpyrimidine non-nucleoside reverse transcriptase inhibitor
CN102675220B (en) * 2012-05-28 2014-03-19 南京药石药物研发有限公司 Etravirine preparing method and intermediate of etravirine

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000027825A1 (en) * 1998-11-10 2000-05-18 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines
WO2008068299A2 (en) * 2006-12-06 2008-06-12 Tibotec Pharmaceuticals Ltd. Hydrobromide salt of an anti-hiv compound

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000027825A1 (en) * 1998-11-10 2000-05-18 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines
WO2008068299A2 (en) * 2006-12-06 2008-06-12 Tibotec Pharmaceuticals Ltd. Hydrobromide salt of an anti-hiv compound

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ANONYMOUS: "Polymorphs of ETV and processes for preparation thereof", IP.COM JOURNAL, 4 January 2010 (2010-01-04), XP002599010 *
QI S. ET AL: "An investigation into the crystallisation behaviour of an amorphous cryomilled pharmaceutical material above and below the glass transition temperature", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 99, no. 1, 2 June 2009 (2009-06-02), pages 196 - 208, XP002599009 *

Also Published As

Publication number Publication date
WO2010131118A2 (en) 2010-11-18

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