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WO2010137032A3 - Novel polymorphic forms of elvitegravir and its pharmaceutically acceptable salts - Google Patents

Novel polymorphic forms of elvitegravir and its pharmaceutically acceptable salts Download PDF

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Publication number
WO2010137032A3
WO2010137032A3 PCT/IN2010/000301 IN2010000301W WO2010137032A3 WO 2010137032 A3 WO2010137032 A3 WO 2010137032A3 IN 2010000301 W IN2010000301 W IN 2010000301W WO 2010137032 A3 WO2010137032 A3 WO 2010137032A3
Authority
WO
WIPO (PCT)
Prior art keywords
elvitegravir
polymorphic forms
pharmaceutically acceptable
acceptable salts
novel polymorphic
Prior art date
Application number
PCT/IN2010/000301
Other languages
French (fr)
Other versions
WO2010137032A2 (en
Inventor
Siva Rama Prasad Vellanki
Vilas Nathu Dhake
Satyanarayana Ravi
Ravi Nuchu
Ravindra Puliyala
Original Assignee
Matrix Laboratories 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 Matrix Laboratories Ltd. filed Critical Matrix Laboratories Ltd.
Publication of WO2010137032A2 publication Critical patent/WO2010137032A2/en
Publication of WO2010137032A3 publication Critical patent/WO2010137032A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV

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  • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to amorphous Elvitegravir, amorphous Elvitegravir sodium, crystalline Elvitegravir sodium and processes for the preparation thereof. The present invention also relates to novel processes for the preparation of Elvitegravir polymorphic forms Il & III.
PCT/IN2010/000301 2009-05-14 2010-05-11 Novel polymorphic forms of elvitegravir and its pharmaceutically acceptable salts WO2010137032A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1114CH2009 2009-05-14
IN1114/CHE/2009 2009-05-14

Publications (2)

Publication Number Publication Date
WO2010137032A2 WO2010137032A2 (en) 2010-12-02
WO2010137032A3 true WO2010137032A3 (en) 2011-09-15

Family

ID=43014237

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2010/000301 WO2010137032A2 (en) 2009-05-14 2010-05-11 Novel polymorphic forms of elvitegravir and its pharmaceutically acceptable salts

Country Status (1)

Country Link
WO (1) WO2010137032A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102212032B (en) * 2011-04-20 2013-07-31 复旦大学 5-hyroxyquinolone derivatives, and preparation method and application thereof
US20150141457A1 (en) * 2012-05-21 2015-05-21 Hetero Research Foundation Elvitegravir solid dispersion

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1564210A1 (en) * 2002-11-20 2005-08-17 Japan Tobacco Inc. 4-oxoquinoline compounds and utilization thereof as hiv integrase inhibitors
WO2005113508A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1564210A1 (en) * 2002-11-20 2005-08-17 Japan Tobacco Inc. 4-oxoquinoline compounds and utilization thereof as hiv integrase inhibitors
WO2005113508A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BYRN ET AL.: "PHARMACEUTICAL SOLIDS: A STRATEGIC APPROACH TO REGULATORY CONSIDERATIONS", PHARMACEUTICAL RESEARCH, vol. 12, no. 7, 1 July 1995 (1995-07-01), pages 945 - 954, XP000996386, ISSN: 0724-8741, DOI: 10.1023/A:1016241927429 *
HANCOCK ET AL.: "CHARACTERISTICS AND SIGNIFICANCE OF THE AMORPHOUS STATE IN PHARMACEUTICAL SYSTEMS", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 86, no. 1, 1 January 1997 (1997-01-01), pages 1 - 12, XP000929450, ISSN: 0022-3549, DOI: 10.1021/JS9601896 *
YU: "AMORPHOUS PHARMACEUTICAL SOLIDS: PREPARATION, CHARACTERIZATION AND STABILIZATION", ADVANCED DRUG DELIVERY REVIEWS, vol. 48, no. 1, 16 May 2001 (2001-05-16), pages 27 - 42, XP009065056, ISSN: 0169-409X, DOI: 10.1016/S0169-409X(01)00098-9 *

Also Published As

Publication number Publication date
WO2010137032A2 (en) 2010-12-02

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