HRP20140254T4 - CRYSTALLINE FORM OF 1- (ß-D-GLUCOPYRANOSYL) -4 -METHYL- 3- [5- (4 -FLUOROPHENYL) -2-THIENYLMETHYL]BENZENE HEMIHYDRATE - Google Patents

CRYSTALLINE FORM OF 1- (ß-D-GLUCOPYRANOSYL) -4 -METHYL- 3- [5- (4 -FLUOROPHENYL) -2-THIENYLMETHYL]BENZENE HEMIHYDRATE Download PDF

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Publication number
HRP20140254T4
HRP20140254T4 HRP20140254TT HRP20140254T HRP20140254T4 HR P20140254 T4 HRP20140254 T4 HR P20140254T4 HR P20140254T T HRP20140254T T HR P20140254TT HR P20140254 T HRP20140254 T HR P20140254T HR P20140254 T4 HRP20140254 T4 HR P20140254T4
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Croatia
Prior art keywords
thienylmethyl
glucopyranosyl
fluorophenyl
methyl
crystalline form
Prior art date
Application number
HRP20140254TT
Other languages
Croatian (hr)
Inventor
Sumihiro Nomura
Eiji Kawanishi
Original Assignee
Mitsubishi Tanabe Pharma Corporation
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Filing date
Publication date
Priority claimed from PCT/JP2007/073729 external-priority patent/WO2008069327A1/en
Application filed by Mitsubishi Tanabe Pharma Corporation filed Critical Mitsubishi Tanabe Pharma Corporation
Publication of HRP20140254T1 publication Critical patent/HRP20140254T1/en
Publication of HRP20140254T4 publication Critical patent/HRP20140254T4/en

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    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04—Carbocyclic radicals

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (6)

1. Kristalni oblik hemihidrata 1-(β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2-tienilmetil]benzena, naznačen time što ima uglavnom isti uzorak difrakcije rendgenskih zraka kao što je prikazano na SL. 1.1. A crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, characterized as having substantially the same X-ray diffraction pattern as shown on FIG. 1. 2. Kristalni oblik hemihidrata 1-(β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2-tienilmetil]benzena, naznačen time što ima uglavnom isti IR spektar kao što je prikazano na SL. 2.2. A crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate, characterized by having essentially the same IR spectrum as shown in FIG. . 2. 3. Kristalni oblik hemihidrata 1-(β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2-tienilmetil]benzena u skladu s patentnim zahtjevom 2, naznačen time što IR spektar kristalnog oblika u mineralnom ulju sadrži sljedeće glavne signale u: 1626, 1600, 1549, te 1507 cm-1.3. The crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate in accordance with claim 2, characterized in that the IR spectrum of the crystalline form in mineral oil contains the following main signals at: 1626, 1600, 1549, and 1507 cm-1. 4. Postupak dobivanja kristalnog oblika hemihidrata 1-(β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2- tienilmetil]benzena u skladu s patentnim zahtjevom 1, 2 ili 3, naznačen time što se sastoji u pripravi otopine 1-β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2-tienilmetil]benzena u otapalu koje sadrži vodu i kristaliziranju navedenog hemihidrata iz otopine taloženjem ili prekristaliziranjem.4. Process for obtaining the crystalline form of hemihydrate 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene in accordance with patent claim 1, 2 or 3, indicated by which consists in preparing a solution of 1-β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene in a solvent containing water and crystallizing the said hemihydrate from the solution by precipitation or recrystallization. 5. Farmaceutski pripravak, naznačen time što sadrži djelotvornu količinu kristalnog oblika hemihidrata 1-(β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2-tienilmetil]benzena u skladu s patentnim zahtjevom 1, 2 ili 3, kao i farmaceutski prihvatljivu podlogu.5. Pharmaceutical preparation, characterized in that it contains an effective amount of the crystalline form of hemihydrate 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene in accordance with claim 1 , 2 or 3, as well as a pharmaceutically acceptable base. 6. Kristalni oblik hemihidrata 1-(β-D-glukopiranozil)-4-metil-3-[5-(4-fluorfenil)-2-tienilmetil]benzena u skladu s patentnim zahtjevom 1, 2 ili 3, naznačen time što je namijenjen upotrebi u liječenju ili odgađanju napredovanja ili početka dijabetesa melitusa, dijabetične retinopatije, dijabetične neuropatije, dijabetične nefropatije, usporenog zacjeljivanja rana, otpornosti na inzulin, hiperglikemije, hiperinzulinemije, povišenih razina masnih kiselina u krvi, povišenih razina glicerola u krvi, hiperlipidemije, pretilosti, hipertrigliceridemije, sindroma X, dijabetičnih komplikacija, ateroskleroze ili hipertenzije.6. The crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate according to claim 1, 2 or 3, characterized in that intended for use in treating or delaying the progression or onset of diabetes mellitus, diabetic retinopathy, diabetic neuropathy, diabetic nephropathy, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood fatty acid levels, elevated blood glycerol levels, hyperlipidemia, obesity, hypertriglyceridemia, syndrome X, diabetic complications, atherosclerosis or hypertension.
HRP20140254TT 2006-12-04 2014-03-18 CRYSTALLINE FORM OF 1- (ß-D-GLUCOPYRANOSYL) -4 -METHYL- 3- [5- (4 -FLUOROPHENYL) -2-THIENYLMETHYL]BENZENE HEMIHYDRATE HRP20140254T4 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US86842606P 2006-12-04 2006-12-04
JP2006327019 2006-12-04
PCT/JP2007/073729 WO2008069327A1 (en) 2006-12-04 2007-12-03 CRYSTALLINE FORM OF 1- (β-D-GLUCOPYRANOSYL) -4 -METHYL- 3- [5- (4 -FLUOROPHENYL) -2-THIENYLMETHYL] BENZENE HEMIHYDRATE
EP07850306.7A EP2102224B2 (en) 2006-12-04 2007-12-03 CRYSTALLINE FORM OF 1- (ß-D-GLUCOPYRANOSYL) -4 -METHYL- 3- [5- (4 -FLUOROPHENYL) -2-THIENYLMETHYL]BENZENE HEMIHYDRATE

Publications (2)

Publication Number Publication Date
HRP20140254T1 HRP20140254T1 (en) 2014-04-25
HRP20140254T4 true HRP20140254T4 (en) 2021-10-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20140254TT HRP20140254T4 (en) 2006-12-04 2014-03-18 CRYSTALLINE FORM OF 1- (ß-D-GLUCOPYRANOSYL) -4 -METHYL- 3- [5- (4 -FLUOROPHENYL) -2-THIENYLMETHYL]BENZENE HEMIHYDRATE

Country Status (3)

Country Link
HR (1) HRP20140254T4 (en)
NI (1) NI200900113A (en)
UA (1) UA93135C2 (en)

Also Published As

Publication number Publication date
NI200900113A (en) 2010-11-29
HRP20140254T1 (en) 2014-04-25
UA93135C2 (en) 2011-01-10

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