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AR067970A1 - Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo - Google Patents

Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo

Info

Publication number
AR067970A1
AR067970A1 ARP080103592A ARP080103592A AR067970A1 AR 067970 A1 AR067970 A1 AR 067970A1 AR P080103592 A ARP080103592 A AR P080103592A AR P080103592 A ARP080103592 A AR P080103592A AR 067970 A1 AR067970 A1 AR 067970A1
Authority
AR
Argentina
Prior art keywords
methyl
beta
glucopyranos
benzyl
benzene
Prior art date
Application number
ARP080103592A
Other languages
English (en)
Inventor
Frank Himmelsbach
Michael Mark
Leo Thomas
Klaus Dugi
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39870130&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR067970(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR067970A1 publication Critical patent/AR067970A1/es

Links

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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
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/141—Intimate 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
    • A61K9/145—Intimate 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
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, 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
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)

Abstract

Método de tratamiento. Uso. Reivindicacion 1: Una composicion farmacéutica que comprende un derivado de benceno sustituido con glucopiranosilo de la formula (1) en la que R1 se refiere a CI, metilo o ciano; R2 se refiere a H, metilo, metoxi o hidroxi y R3 se refiere a etilo, ciclopropilo, etinilo, etoxi, (R)-tetrahidrofurano-3-iloxi o (S)-tetrahidrofurano-3-iloxi o bien, en una primera realizacion (realizacion A), junto con un inhibidor de DPPIV (dipeptidil peptidasa IV) de formula (1), o de formula (2), o de formula (3), o de formula (4) donde R1 se refiere a ([1,5]naftiridin-2-il)metilo, (quinazolin-2-il)metilo, (quinoxalin-6-il)metilo, (4-metil-quinazolin-2-il)metilo, 2-ciano-bencilo, (3-ciano-quinolin-2-il)metilo, (3-ciano-piridin-2-il)metilo, (4-metil-pirimidin-2-il)metilo o (4,6-dimetil-pirimidin-2-il)metilo y R2 se refiere a 3-(R)-amino-piperidin-1-ilo, (2-amino-2-metil-propil)-metilamino o (2-(S)-amino-propil)-metilamino o su sal farmacéuticamente aceptable, o, en una segunda realizacion (realizacion B), junto con un inhibidor de DPP IV seleccionado entre el grupo que consiste en sitagliptina, vildagliptina, saxagliptina, alogliptina, denagliptina, (2S)-1-{[2-(5-Metil-2-fenil-oxazol-4-il)-etilamino]-acetil}-pirrolidina-2-carbonitrilo, (2S)-1-{[1,1,-Dimetil-3-(4-piridin-3-il-imidazol-1-il)-propilamino]acetil}-pirrolidina-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-fluorometil-pirrolidin-2-ona, (3,3-difluoropirrolidin-1-il)-((2S,4S)-4-(4-(pirimidin-2-il)piperazin-1-iI)pirrolidin-2-il)metanona, (1((3S,4S)-4-amino-1-(4-(3,3-difluoropirrolidin-1-il)-1,3,5-triazin-2-il)pirrolidin-3-il)-5,5-difluoropiperidin2-ona, (2S,4S)-1-{2-[(3S,1R)-3-(1H-1,2,4-Triazol-1-ilmetil)ciclopentilamino]-acetil}-4-fluoropirrolidina-2-carbonitrilo y 2-[6-(3-Amino-piperidin-1-il)-3-metil-2,4-dioxo-3,4-dihidro-2H-pirimidin-1-ilmetil]-4-fluoro-benzonitrilo, o su sal farmacéuticamente aceptable. Reivindicacion 2: La composicion farmacéutica de acuerdo con la reivindicacion 1, en la que el derivado de benceno sustituido con glucopiranosilo se selecciona entre e! grupo de compuestos (1) a (11): (1) 6-(4-Etilbencil)-4-(beta-D-glucopiranos-1-il)-2-metoxi-benzonitrilo, (2) 2-4-Etilbencil)-4-(beta-D-glucopiranos-1-il)-5-metoxi-benzonitrilo, (3) 1-Ciano-2-(-etilbencil)-4-(beta-D-glucopiranos-1-il)-5-metil-benceno, (4) 2-(4-Etilbencil)-4-(beta-D-gIucopiranoS-1-il)-5-hidroxi-benzonitrilo, (5) 2-(4-Etil-bencil)-4-(beta-D-glucopiranos-1-il)-benzonitrilo, (6) 2(4-ciclopropil-bencil)-4-(beta-D-glucopiranos-1-iI)-benzonitrilo, (7) 1-cloro-4-(beta-D-gIucopiranos-1-il)-2-(4-etinil-bencil)-benceno, (8) 1-cloro-4-(beta-D-glucopiranos-1-il)-2-[4-(( R)-tetrahidrofurano-3-iloxi)-bencil]-benceno, (9) 1-cloro-4-(beta-D-glucopiranos-1-il)-2-[4-((S)-tetrahidrofurano-3-iloxi)-bencil]-benceno, (10) 1-Metil-2-[4-((R)-tetrahidrofurano-3-iloxi)-bencil]-4-(beta-D-glucopiranos-1-il)-benceno, y (11) 1-Metil-2-(4-((S)-tetrahidrofurano-3-iloxi)-bencil]-4-(beta-D-glucopiranos-1-il)-benceno.
ARP080103592A 2007-08-16 2008-08-15 Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo AR067970A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07114459 2007-08-16

Publications (1)

Publication Number Publication Date
AR067970A1 true AR067970A1 (es) 2009-10-28

Family

ID=39870130

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP080103592A AR067970A1 (es) 2007-08-16 2008-08-15 Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo
ARP120103117A AR087657A2 (es) 2007-08-16 2012-08-23 Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP120103117A AR087657A2 (es) 2007-08-16 2012-08-23 Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo

Country Status (39)

Country Link
US (1) US8551957B2 (es)
EP (4) EP2187879B1 (es)
JP (1) JP5595914B2 (es)
KR (1) KR101491554B1 (es)
CN (3) CN104288166A (es)
AR (2) AR067970A1 (es)
AU (1) AU2008288407B2 (es)
BR (1) BRPI0815331B8 (es)
CA (1) CA2696558C (es)
CL (1) CL2008002427A1 (es)
CO (1) CO6251239A2 (es)
CY (2) CY1118308T1 (es)
DK (1) DK2187879T3 (es)
EA (1) EA018608B1 (es)
EC (1) ECSP109977A (es)
ES (1) ES2602748T3 (es)
HK (2) HK1203351A1 (es)
HR (1) HRP20170022T1 (es)
HU (2) HUE030158T2 (es)
IL (1) IL202886A (es)
LT (2) LT2187879T (es)
MA (1) MA31612B1 (es)
ME (1) ME02573B (es)
MX (1) MX2010001696A (es)
MY (1) MY152037A (es)
NL (1) NL300872I2 (es)
NO (1) NO2017020I2 (es)
NZ (1) NZ583242A (es)
PE (1) PE20090938A1 (es)
PL (1) PL2187879T3 (es)
PT (1) PT2187879T (es)
RS (1) RS55205B1 (es)
SI (1) SI2187879T1 (es)
TN (1) TN2010000073A1 (es)
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