WO2013153161A3 - Polymorph of rilpivirine hydrochloride - Google Patents

Polymorph of rilpivirine hydrochloride Download PDF

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Publication number
WO2013153161A3
WO2013153161A3 PCT/EP2013/057596 EP2013057596W WO2013153161A3 WO 2013153161 A3 WO2013153161 A3 WO 2013153161A3 EP 2013057596 W EP2013057596 W EP 2013057596W WO 2013153161 A3 WO2013153161 A3 WO 2013153161A3
Authority
WO
WIPO (PCT)
Prior art keywords
polymorph
present
rilpivirine hydrochloride
novel
relates
Prior art date
Application number
PCT/EP2013/057596
Other languages
French (fr)
Other versions
WO2013153161A2 (en
Inventor
Andreas Hotter
Arthur Pichler
Verena Adamer
Ulrich Griesser
Original Assignee
Sandoz Ag
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 Sandoz Ag filed Critical Sandoz Ag
Publication of WO2013153161A2 publication Critical patent/WO2013153161A2/en
Publication of WO2013153161A3 publication Critical patent/WO2013153161A3/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)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to a novel polymorph and to novel solvates of rilpivirine hydrochloride, as well as to their preparation. The novel solvates are valuable intermediates for the preparation of the novel polymorph of rilpivirine hydrochloride of the present invention. Moreover the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and additional therapeutic agents.
PCT/EP2013/057596 2012-04-11 2013-04-11 Novel polymorph of rilpivirine hydrochloride WO2013153161A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12163720 2012-04-11
EP12163720.1 2012-04-11

Publications (2)

Publication Number Publication Date
WO2013153161A2 WO2013153161A2 (en) 2013-10-17
WO2013153161A3 true WO2013153161A3 (en) 2013-12-05

Family

ID=48050762

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2013/057596 WO2013153161A2 (en) 2012-04-11 2013-04-11 Novel polymorph of rilpivirine hydrochloride

Country Status (1)

Country Link
WO (1) WO2013153161A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015136294A1 (en) * 2014-03-13 2015-09-17 Cipla Limited Pharmaceutical composittion comprising rilpivirine
WO2021104487A1 (en) 2019-11-29 2021-06-03 Aptorum Therapeutics Limited Composition including rilpivirine and use thereof for treating tumors or cancer

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1632232A1 (en) * 2004-09-02 2006-03-08 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-Cyanoethenyl)-2,6-dimethylphenyl]amino]-2-Pyrimidinyl]amino]benzonitrile
WO2012125993A1 (en) * 2011-03-17 2012-09-20 Teva Pharmaceutical Industries Ltd. Solid state forms of rilpivirine base, and rilipivirine salts
WO2012143937A2 (en) * 2011-04-15 2012-10-26 Emcure Pharmaceuticals Limited An improved rilpivirine process
WO2012147091A2 (en) * 2011-04-25 2012-11-01 Hetero Research Foundation Process for rilpivirine
WO2013038425A1 (en) * 2011-09-16 2013-03-21 Hetero Research Foundation Rilpivirine hydrochloride

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3429B1 (en) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidines derivatives

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1632232A1 (en) * 2004-09-02 2006-03-08 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-Cyanoethenyl)-2,6-dimethylphenyl]amino]-2-Pyrimidinyl]amino]benzonitrile
WO2012125993A1 (en) * 2011-03-17 2012-09-20 Teva Pharmaceutical Industries Ltd. Solid state forms of rilpivirine base, and rilipivirine salts
WO2012143937A2 (en) * 2011-04-15 2012-10-26 Emcure Pharmaceuticals Limited An improved rilpivirine process
WO2012147091A2 (en) * 2011-04-25 2012-11-01 Hetero Research Foundation Process for rilpivirine
WO2013038425A1 (en) * 2011-09-16 2013-03-21 Hetero Research Foundation Rilpivirine hydrochloride

Also Published As

Publication number Publication date
WO2013153161A2 (en) 2013-10-17

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