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PE20090987A1 - PHARMACEUTICAL COMPOSITION INCLUDING A DERIVATIVE OF PIRAZOL-O-GLUCOSIDE - Google Patents

PHARMACEUTICAL COMPOSITION INCLUDING A DERIVATIVE OF PIRAZOL-O-GLUCOSIDE

Info

Publication number
PE20090987A1
PE20090987A1 PE2008001380A PE2008001380A PE20090987A1 PE 20090987 A1 PE20090987 A1 PE 20090987A1 PE 2008001380 A PE2008001380 A PE 2008001380A PE 2008001380 A PE2008001380 A PE 2008001380A PE 20090987 A1 PE20090987 A1 PE 20090987A1
Authority
PE
Peru
Prior art keywords
pharmaceutical composition
composition including
glucoside
derivative
carbonitrile
Prior art date
Application number
PE2008001380A
Other languages
Spanish (es)
Inventor
Klaus Dugi
Frank Himmelsbach
Michael Mark
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20090987A1 publication Critical patent/PE20090987A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Biophysics (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE UN DERIVADO DE PIRAZOL-O-GLUCOSIDO DE FORMULA (I), EN COMBINACION CON UN INHIBIDOR DE DPP IV SELECCIONADO DE SITAGLIPTINA, VIDAGLIPTINA, SAXAGLIPTINA, ALOGLIPTINA, DENAGLIPTINA, (2S)-1-{[2-(5-METIL-2-FENILOXAZOL-4-IL)ETILAMINO]ACETIL}PIRROLIDIN-2-CARBONITRILO, (2S)-1-{[1,1-DIMETIL-3-(4-PIRIDIN-3-ILIMIDAZOL-1-IL)PROPILAMINO]ACETIL}PIRROLIDIN-2-CARBONITRILO; (S)-1-((2S, 3S, 11bS)-2-AMINO-9,10-DIMETOXI-1,3,4,7,11b-HEXAHIDRO-2H-PIRIDO[2,1-a]ISOQUINOLIN-3-IL)-4-FLUOROMETILPIRROLIDIN-2-ONA; ENTRE OTROS. DICHO COMPUESTO DE FORMULA (I) TIENE LOS SIGUIENTES SUSTITUYENTES: R1 ES ALCOXI C1-3; L1 Y L2 SON H O F Y R6 ES H, (ALQUIL C1-3)CARBONILO, (ALQUIL C1-6)OXICARBONILO, FENILOXICARBONILO, BENCILOXICARBONILO O BENCILCARBONILO. DICHA COMPOSICION ES ADECUADA PARA EL TRATAMIENTO O PREVENCION DE UNA O MAS AFECCIONES SELECCIONADAS DE DIABETES MELLITUS DE TIPO 1, DIABETES MELLITUS DE TIPO 2, TOLERANCIA ANORMAL A LA GLUCOSA, GLUCOSA SANGUINEA ANORMAL EN AYUNAS E HIPERGLUCEMIAREFERS TO A PHARMACEUTICAL COMPOSITION INCLUDING A PIRAZOLE-O-GLUCOSIDE DERIVATIVE OF FORMULA (I), IN COMBINATION WITH A DPP IV INHIBITOR SELECTED FROM SITAGLIPTINE, VIDAGLIPTIN, SAXAGLIPTIN, [2-DENAGLIPTIN-1, [2-ALOGLIPTIN] 2- (5-METHYL-2-PHENYLOXAZOLE-4-IL) ETHYLAMINE] ACETYL} PYRROLIDIN-2-CARBONITRILE, (2S) -1 - {[1,1-DIMETHYL-3- (4-PYRIDIN-3-ILIMIDAZOLE- 1-IL) PROPYLAMINO] ACETYL} PYRROLIDIN-2-CARBONITRILE; (S) -1 - ((2S, 3S, 11bS) -2-AMINO-9,10-DIMETOXY-1,3,4,7,11b-HEXAHYDRO-2H-PYRIDO [2,1-a] ISOQUINOLIN-3 -IL) -4-FLUOROMETHYLPYRROLIDIN-2-ONA; AMONG OTHERS. SAID COMPOUND OF FORMULA (I) HAS THE FOLLOWING SUBSTITUENTS: R1 IS ALCOXI C1-3; L1 AND L2 ARE H OR F AND R6 IS H, (C1-3 ALKYL) CARBONYL, (C1-6 ALKYL) OXYCARBONYL, PHENYLOXYCARBONYL, BENZYLOXYCARBONYL OR BENZYLCARBONYL. SUCH COMPOSITION IS ADEQUATE FOR THE TREATMENT OR PREVENTION OF ONE OR MORE SELECTED CONDITIONS OF TYPE 1 DIABETES MELLITUS, TYPE 2 DIABETES MELLITUS, ABNORMAL GLUCOSE TOLERANCE, ABNORMAL BLOOD GLUCOSE IN FASTING AND HYPERGLYCEMIA

PE2008001380A 2007-08-16 2008-08-14 PHARMACEUTICAL COMPOSITION INCLUDING A DERIVATIVE OF PIRAZOL-O-GLUCOSIDE PE20090987A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07114461 2007-08-16

Publications (1)

Publication Number Publication Date
PE20090987A1 true PE20090987A1 (en) 2009-08-14

Family

ID=39870441

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001380A PE20090987A1 (en) 2007-08-16 2008-08-14 PHARMACEUTICAL COMPOSITION INCLUDING A DERIVATIVE OF PIRAZOL-O-GLUCOSIDE

Country Status (6)

Country Link
AR (1) AR068102A1 (en)
CL (1) CL2008002424A1 (en)
PE (1) PE20090987A1 (en)
TW (1) TW200918078A (en)
UY (1) UY31290A1 (en)
WO (1) WO2009022009A1 (en)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
DE102004054054A1 (en) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Process for preparing chiral 8- (3-amino-piperidin-1-yl) -xanthines
KR101452915B1 (en) 2006-05-04 2014-10-21 베링거 인겔하임 인터내셔날 게엠베하 Polymorphism
PE20080251A1 (en) 2006-05-04 2008-04-25 Boehringer Ingelheim Int USES OF DPP IV INHIBITORS
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
TW200900094A (en) * 2007-03-13 2009-01-01 Takeda Pharmaceutical Solid preparation
CL2008002427A1 (en) 2007-08-16 2009-09-11 Boehringer Ingelheim Int Pharmaceutical composition comprising 1-chloro-4- (bd-glucopyranos-1-yl) -2- [4 - ((s) -tetrahydrofuran-3-yloxy) benzyl] -benzene combined with 1 - [(4-methylquinazolin- 2-yl) methyl] -3-methyl-7- (2-butyn-1-yl) -8- (3- (r) -aminopiperidin-1-yl) xanthine; and its use to treat type 2 diabetes mellitus.
CL2008003653A1 (en) * 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Use of a glucopyranosyl-derived sglt inhibitor and a selected dppiv inhibitor to treat diabetes; and pharmaceutical composition.
PE20140960A1 (en) 2008-04-03 2014-08-15 Boehringer Ingelheim Int FORMULATIONS INVOLVING A DPP4 INHIBITOR
PE20100156A1 (en) * 2008-06-03 2010-02-23 Boehringer Ingelheim Int NAFLD TREATMENT
KR20190016601A (en) 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 Treatment for diabetes in patients inappropriate for metformin therapy
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
AU2009331471B2 (en) 2008-12-23 2015-09-03 Boehringer Ingelheim International Gmbh Salt forms of organic compound
PT2395983T (en) 2009-02-13 2020-07-03 Boehringer Ingelheim Int Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof
KR20120107080A (en) 2009-11-27 2012-09-28 베링거 인겔하임 인터내셔날 게엠베하 Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
KR101927068B1 (en) 2010-05-05 2018-12-10 베링거 인겔하임 인터내셔날 게엠베하 Sequential Combination Therapy by the Weight Reducing Treatment Followed by the DPP-4 Inhibitor
KR20220025926A (en) 2010-06-24 2022-03-03 베링거 인겔하임 인터내셔날 게엠베하 Diabetes therapy
AR083878A1 (en) 2010-11-15 2013-03-27 Boehringer Ingelheim Int VASOPROTECTORA AND CARDIOPROTECTORA ANTIDIABETIC THERAPY, LINAGLIPTINA, TREATMENT METHOD
UY33937A (en) 2011-03-07 2012-09-28 Boehringer Ingelheim Int PHARMACEUTICAL COMPOSITIONS CONTAINING DPP-4 AND / OR SGLT-2 AND METFORMIN INHIBITORS
CN103781788B (en) 2011-07-15 2016-08-17 勃林格殷格翰国际有限公司 Quinazoline, its preparation and the purposes in pharmaceutical composition thereof being substituted
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
WO2013171166A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis
JP6224084B2 (en) 2012-05-14 2017-11-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Xanthine derivatives as DPP-4 inhibitors for the treatment of glomerular epithelial cell related disorders and / or nephrotic syndrome
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
JP6615109B2 (en) 2014-02-28 2019-12-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Medical use of DPP-4 inhibitors
MX390363B (en) 2016-06-10 2025-03-20 Boehringer Ingelheim Int Combinations of linagliptin and metformin

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JP4424203B2 (en) * 2002-04-26 2010-03-03 味の素株式会社 Diabetes prevention and treatment
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UY29694A1 (en) * 2005-07-28 2007-02-28 Boehringer Ingelheim Int METHODS TO PREVENT AND TREAT METABOLIC AND NEW DISORDERS DERIVED FROM PIRAZOL-O-GLUCOSIDO
ME02005B (en) * 2005-09-14 2012-08-31 Takeda Pharmaceuticals Co Dipeptidyl peptidase inhibitors for treating diabetes
PE20080251A1 (en) * 2006-05-04 2008-04-25 Boehringer Ingelheim Int USES OF DPP IV INHIBITORS
WO2007148185A2 (en) * 2006-06-21 2007-12-27 Pfizer Products Inc. Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors
CL2008000133A1 (en) * 2007-01-19 2008-05-23 Boehringer Ingelheim Int PHARMACEUTICAL COMPOSITION THAT INCLUDES A COMPOUND DERIVED FROM PIRAZOL-O-GLUCOSIDE COMBINED WITH AT LEAST A SECOND THERAPEUTIC AGENT; AND USE OF THE COMPOSITION FOR THE TREATMENT OF MELLITUS DIABETES, CATARATS, NEUROPATHY, MYOCARDIAL INFARTS, AND

Also Published As

Publication number Publication date
WO2009022009A1 (en) 2009-02-19
UY31290A1 (en) 2009-03-31
AR068102A1 (en) 2009-11-04
CL2008002424A1 (en) 2009-09-11
TW200918078A (en) 2009-05-01

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