ATE541854T1 - Pyrazolderivat, arzneimittelzusammensetzung, die dieses enthält, und zwischenprodukt für dessen herstellung - Google Patents

Pyrazolderivat, arzneimittelzusammensetzung, die dieses enthält, und zwischenprodukt für dessen herstellung

Info

Publication number
ATE541854T1
ATE541854T1 AT04746165T AT04746165T ATE541854T1 AT E541854 T1 ATE541854 T1 AT E541854T1 AT 04746165 T AT04746165 T AT 04746165T AT 04746165 T AT04746165 T AT 04746165T AT E541854 T1 ATE541854 T1 AT E541854T1
Authority
AT
Austria
Prior art keywords
optionally substituted
production
aryl
composition containing
glucose
Prior art date
Application number
AT04746165T
Other languages
English (en)
Inventor
N Kikuchi
H Fujikura
S Tazawa
T Yamato
M Isaji
Original Assignee
Kissei Pharmaceutical
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 Kissei Pharmaceutical filed Critical Kissei Pharmaceutical
Application granted granted Critical
Publication of ATE541854T1 publication Critical patent/ATE541854T1/de

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/28—Two oxygen or sulfur atoms
    • C07D231/30—Two oxygen or sulfur atoms attached in positions 3 and 5
    • C07D231/32—Oxygen atoms
    • 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
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • C07D231/52—Oxygen atom in position 3 and nitrogen atom in position 5, or vice versa

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
AT04746165T 2003-06-20 2004-06-15 Pyrazolderivat, arzneimittelzusammensetzung, die dieses enthält, und zwischenprodukt für dessen herstellung ATE541854T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2003175663 2003-06-20
PCT/JP2004/008695 WO2004113359A1 (ja) 2003-06-20 2004-06-15 ピラゾール誘導体、それを含有する医薬組成物及びその製造中間体

Publications (1)

Publication Number Publication Date
ATE541854T1 true ATE541854T1 (de) 2012-02-15

Family

ID=33534874

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04746165T ATE541854T1 (de) 2003-06-20 2004-06-15 Pyrazolderivat, arzneimittelzusammensetzung, die dieses enthält, und zwischenprodukt für dessen herstellung

Country Status (7)

Country Link
US (1) US7576064B2 (de)
EP (1) EP1637539B1 (de)
JP (1) JP4708187B2 (de)
AT (1) ATE541854T1 (de)
CA (1) CA2529878C (de)
ES (1) ES2377741T3 (de)
WO (1) WO2004113359A1 (de)

Families Citing this family (30)

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JP2004137245A (ja) * 2002-08-23 2004-05-13 Kissei Pharmaceut Co Ltd ピラゾール誘導体、それを含有する医薬組成物、その医薬用途及びその製造中間体
US8785403B2 (en) 2003-08-01 2014-07-22 Mitsubishi Tanabe Pharma Corporation Glucopyranoside compound
ME00411B (me) 2003-08-01 2011-10-10 Tanabe Seiyaku Co Nova jedinjenja koja imaju inhibitorno dejstvo na transporter glukoze zavistan od natrijuma
US7375090B2 (en) 2003-08-26 2008-05-20 Boehringer Ingelheim International Gmbh Glucopyranosyloxy-pyrazoles, pharmaceutical compositions containing these compounds, the use thereof and processed for the preparation thereof
WO2005085267A1 (ja) 2004-03-04 2005-09-15 Kissei Pharmaceutical Co., Ltd. 含窒素縮合環誘導体、それを含有する医薬組成物およびその医薬用途
US7838552B2 (en) 2004-06-04 2010-11-23 Forest Laboratories Holdings Limited Compositions comprising nebivolol
US7803838B2 (en) 2004-06-04 2010-09-28 Forest Laboratories Holdings Limited Compositions comprising nebivolol
DE102004028241B4 (de) * 2004-06-11 2007-09-13 Sanofi-Aventis Deutschland Gmbh Neue Fluorglykosidderivate von Pyrazolen, diese Verbindungen enthaltende Arzneimittel und Herstellung dieser Arzneimittel
TW200637869A (en) 2005-01-28 2006-11-01 Chugai Pharmaceutical Co Ltd The spiroketal derivatives and the use as therapeutical agent for diabetes of the same
AR054852A1 (es) * 2005-07-22 2007-07-18 Boehringer Ingelheim Int Procesos para preparar derivados de pirazol 0- glucosido y nuevos intermediarios de dichos procesos
UY30082A1 (es) 2006-01-11 2007-08-31 Boehringer Ingelheim Int Forma cristalina de 1-(1-metiletil)-4`-((2-fluoro-4-metoxifenil)metil)-5`- metil-1h-pirazol-3`-o-b-d-glucopiranosido, un metodo para su preparacion y el uso de la misma para preparar medicamentos
PE20110235A1 (es) 2006-05-04 2011-04-14 Boehringer Ingelheim Int Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
UY30730A1 (es) 2006-12-04 2008-07-03 Mitsubishi Tanabe Pharma Corp Forma cristalina del hemihidrato de 1-(b (beta)-d-glucopiranosil) -4-metil-3-[5-(4-fluorofenil) -2-tienilmetil]benceno
CN101801371B (zh) 2007-09-10 2012-11-28 詹森药业有限公司 可用作sglt抑制剂的化合物的制备方法
CL2008003653A1 (es) 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
WO2010018438A2 (en) * 2008-08-11 2010-02-18 Hetero Research Foundation Tetrazole glycosides
ES2380408T3 (es) * 2008-08-28 2012-05-11 Pfizer Inc. Derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol
US9056850B2 (en) * 2008-10-17 2015-06-16 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of SGLT
CN101445528B (zh) * 2008-12-25 2011-06-15 天津药物研究院 硫代葡萄糖衍生物、其制备方法和用途
US20110009347A1 (en) * 2009-07-08 2011-01-13 Yin Liang Combination therapy for the treatment of diabetes
SI2451797T1 (sl) 2009-07-10 2013-07-31 Janssen Pharmaceutica, N.V. Postopek kristalizacije 1-(beta-d-glukopiranosil)-4-metil-3-(5-(4-fluorofenil)-2-tienilmetil) benzena
BR112012008939B1 (pt) * 2009-10-14 2021-06-22 Janssen Pharmaceutica Nv Processo para a preparação de compostos úteis como inibidores de sglt2
ME02016B (me) 2009-11-02 2015-05-20 Pfizer Derivati dioksabiciklo[3.2.1]oktan-2,3,4-triola
EA022365B1 (ru) 2010-05-11 2015-12-30 Янссен Фармацевтика Нв Фармацевтические композиции, содержащие производные 1-(бета-d-глюкопиранозил)-2-тиенилметилбензола как ингибиторы нзпг
CA2832938C (en) 2011-04-13 2019-09-03 Janssen Pharmaceutica Nv Process for the preparation of compounds useful as inhibitors of sglt2
US9035044B2 (en) 2011-05-09 2015-05-19 Janssen Pharmaceutica Nv L-proline and citric acid co-crystals of (2S, 3R, 4R, 5S,6R)-2-(3-((5-(4-fluorophenyl)thiopen-2-yl)methyl)4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
EP2937096B1 (de) 2014-04-23 2019-08-21 Julius-Maximilians-Universität Würzburg Aus RS1 abgeleitete Peptide, die Glukoseabsorption nach einer glukosereichen Mahlzeit herunterregulieren und die Insulinsensitivität steigern
US20170071970A1 (en) 2015-09-15 2017-03-16 Janssen Pharmaceutica Nv Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders
CN108456182A (zh) * 2018-01-25 2018-08-28 于磊 Sglt2蛋白的抑制剂以及应用
CA3089092A1 (en) * 2018-04-04 2019-10-10 Japan Tobacco Inc. Pyrazole compounds substituted with heteroaryl and pharmaceutical use thereof

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FR2529786A1 (fr) * 1982-07-12 1984-01-13 Nativelle Sa Ets Compositions pharmaceutiques a base de derives de la pyrazolone-5, nouveaux produits et procede de preparation
FR2529891A1 (fr) 1982-07-12 1984-01-13 Nativelle Sa Ets Derives du pyridyl-3 alcoxy-5 pyrazole, procede de preparation et application en therapeutique
CA2382480C (en) * 1999-08-31 2008-09-30 Kissei Pharmaceutical Co., Ltd. Glucopyranosyloxypyrazole derivatives, medicinal compositions containing the same and intermediates in the production thereof
US6555519B2 (en) * 2000-03-30 2003-04-29 Bristol-Myers Squibb Company O-glucosylated benzamide SGLT2 inhibitors and method
AU2002210990A1 (en) * 2000-11-02 2002-05-15 Ajinomoto Co. Inc. Novel pyrazole derivatives and diabetes remedies containing the same
US7084123B2 (en) 2000-12-28 2006-08-01 Kissei Pharmaceutical Co., Ltd. Glucopyranosyloxypyrazole derivatives and use thereof in medicines
ES2319263T3 (es) * 2001-02-26 2009-05-06 Kissei Pharmaceutical Co., Ltd. Derivados de glucopiranosilooxipirazol y su utilizacion como medicamentos.
CA2438595C (en) 2001-02-27 2011-08-09 Kissei Pharmaceutical Co., Ltd. Glucopyranosyloxypyrazole derivatives and medicinal use thereof
JP4292570B2 (ja) 2001-04-27 2009-07-08 味の素株式会社 Ｎ−置換ピラゾール−ｏ−グリコシド誘導体及びそれらを含有する糖尿病治療薬
WO2002098893A1 (en) 2001-05-30 2002-12-12 Kissei Pharmaceutical Co., Ltd. Glucopyranosyloxypyrazole derivative, medicinal composition containing the same, medicinal use thereof, and intermediate therefor
JP4115105B2 (ja) * 2001-07-02 2008-07-09 協和醗酵工業株式会社 ピラゾール誘導体
JP4284091B2 (ja) * 2002-03-27 2009-06-24 キッセイ薬品工業株式会社 単糖類共輸送担体
EP1568380A4 (de) * 2002-12-04 2009-10-21 Kissei Pharmaceutical Vorbeugende massnahme oder heilmittel für krankheiten aufgrund von blutzuckererhöhung

Also Published As

Publication number Publication date
EP1637539A4 (de) 2009-06-17
CA2529878A1 (en) 2004-12-29
JPWO2004113359A1 (ja) 2006-07-27
US20070060531A1 (en) 2007-03-15
ES2377741T3 (es) 2012-03-30
EP1637539A1 (de) 2006-03-22
CA2529878C (en) 2012-11-20
EP1637539B1 (de) 2012-01-18
US7576064B2 (en) 2009-08-18
WO2004113359A1 (ja) 2004-12-29
JP4708187B2 (ja) 2011-06-22

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