WO2003101392A3 - Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods - Google Patents

Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods Download PDF

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Publication number
WO2003101392A3
WO2003101392A3 PCT/US2003/017184 US0317184W WO03101392A3 WO 2003101392 A3 WO2003101392 A3 WO 2003101392A3 US 0317184 W US0317184 W US 0317184W WO 03101392 A3 WO03101392 A3 WO 03101392A3
Authority
WO
WIPO (PCT)
Prior art keywords
conazole
crystalline forms
methods
pharmaceutical compositions
novel
Prior art date
Application number
PCT/US2003/017184
Other languages
French (fr)
Other versions
WO2003101392A2 (en
Inventor
Julius Remenar
Michael Macphee
Matthew Lynn Peterson
Sherry L Morissette
Om Almarsson
Original Assignee
Transform Pharmaceuticals Inc
Julius Remenar
Michael Macphee
Matthew Lynn Peterson
Sherry L Morissette
Om Almarsson
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 Transform Pharmaceuticals Inc, Julius Remenar, Michael Macphee, Matthew Lynn Peterson, Sherry L Morissette, Om Almarsson filed Critical Transform Pharmaceuticals Inc
Priority to AU2003243354A priority Critical patent/AU2003243354A1/en
Priority to EP03756321A priority patent/EP1511490A4/en
Priority to JP2004508750A priority patent/JP2005535602A/en
Publication of WO2003101392A2 publication Critical patent/WO2003101392A2/en
Publication of WO2003101392A3 publication Critical patent/WO2003101392A3/en
Priority to US10/926,842 priority patent/US7446107B2/en
Priority to US12/234,420 priority patent/US20090088443A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Oncology (AREA)
  • Inorganic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The invention provides novel soluble conazole crystalline forms (e.g.itraconazole, posaconazole and saperconazole) that includes salts, co-crystals and related solvates useful as pharmaceuticals. The invention also provides pharmaceutical compositions comprising, and processes for making, these conazole crystalline forms. Methods of using such compositions for the treatment or prevention of systemic and local fungal, yeast, and dermatophyte infections are also provided.
PCT/US2003/017184 2002-02-15 2003-05-30 Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods WO2003101392A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
AU2003243354A AU2003243354A1 (en) 2002-05-31 2003-05-30 Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods
EP03756321A EP1511490A4 (en) 2002-05-31 2003-05-30 Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods
JP2004508750A JP2005535602A (en) 2002-05-31 2003-05-30 Novel conazole crystal forms and related methods, pharmaceutical compositions and methods
US10/926,842 US7446107B2 (en) 2002-02-15 2004-08-26 Crystalline forms of conazoles and methods of making and using the same
US12/234,420 US20090088443A1 (en) 2002-02-15 2008-09-19 Novel crystalline forms of conazoles and methods of making and using the same

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US38415202P 2002-05-31 2002-05-31
US60/384,152 2002-05-31
US43928203P 2003-01-10 2003-01-10
US60/439,282 2003-01-10
US44431503P 2003-01-31 2003-01-31
US60/444,315 2003-01-31
US46396203P 2003-04-18 2003-04-18
US60/463,962 2003-04-18
US10/449,307 US7078526B2 (en) 2002-05-31 2003-05-30 CIS-itraconazole crystalline forms and related processes, pharmaceutical compositions and methods
US10/449,307 2003-05-30

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/027772 Continuation-In-Part WO2004078161A1 (en) 2002-02-15 2003-09-04 Pharmaceutical co-crystal compositions of drugs such as carbamazeptine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US10/449,307 Continuation-In-Part US7078526B2 (en) 2002-02-15 2003-05-30 CIS-itraconazole crystalline forms and related processes, pharmaceutical compositions and methods
US10/926,842 Continuation-In-Part US7446107B2 (en) 2002-02-15 2004-08-26 Crystalline forms of conazoles and methods of making and using the same

Publications (2)

Publication Number Publication Date
WO2003101392A2 WO2003101392A2 (en) 2003-12-11
WO2003101392A3 true WO2003101392A3 (en) 2004-04-08

Family

ID=29716372

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/017184 WO2003101392A2 (en) 2002-02-15 2003-05-30 Novel conazole crystalline forms and related processes, pharmaceutical compositions and methods

Country Status (5)

Country Link
US (1) US7078526B2 (en)
EP (1) EP1511490A4 (en)
JP (1) JP2005535602A (en)
AU (1) AU2003243354A1 (en)
WO (1) WO2003101392A2 (en)

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US7078526B2 (en) * 2002-05-31 2006-07-18 Transform Pharmaceuticals, Inc. CIS-itraconazole crystalline forms and related processes, pharmaceutical compositions and methods
US20100311701A1 (en) * 2002-02-15 2010-12-09 Transform Pharmaceuticals, Inc Pharmaceutical Co-Crystal Compositions
US7790905B2 (en) * 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
US7446107B2 (en) 2002-02-15 2008-11-04 Transform Pharmaceuticals, Inc. Crystalline forms of conazoles and methods of making and using the same
AU2003213719A1 (en) * 2002-03-01 2003-09-16 Regents Of The University Of Michigan Multiple-component solid phases containing at least one active pharmaceutical ingredient
US20070059356A1 (en) * 2002-05-31 2007-03-15 Almarsson Oern Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
AU2003243699B2 (en) 2002-06-21 2009-01-15 Transform Pharmaceuticals, Inc. Pharmaceutical compositions with improved dissolution
US8183290B2 (en) * 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
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Also Published As

Publication number Publication date
US7078526B2 (en) 2006-07-18
EP1511490A4 (en) 2009-03-11
WO2003101392A2 (en) 2003-12-11
AU2003243354A8 (en) 2003-12-19
AU2003243354A1 (en) 2003-12-19
US20040019211A1 (en) 2004-01-29
EP1511490A2 (en) 2005-03-09
JP2005535602A (en) 2005-11-24

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