TWI377209B - Novel n-glucoside derivatives having a sglt inhibitory activity - Google Patents

Novel n-glucoside derivatives having a sglt inhibitory activity Download PDF

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Publication number
TWI377209B
TWI377209B TW093122844A TW93122844A TWI377209B TW I377209 B TWI377209 B TW I377209B TW 093122844 A TW093122844 A TW 093122844A TW 93122844 A TW93122844 A TW 93122844A TW I377209 B TWI377209 B TW I377209B
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compound
alkyl
ring
formula
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TW093122844A
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TW200510440A (en
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Sumihiro Nomura
Toshiaki Sakamoto
Kiichiro Ueta
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Mitsubishi Tanabe Pharma Corp
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/203Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H5/00Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
    • C07H5/04Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to nitrogen

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW093122844A 2003-08-01 2004-07-30 Novel n-glucoside derivatives having a sglt inhibitory activity TWI377209B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49152303P 2003-08-01 2003-08-01

Publications (2)

Publication Number Publication Date
TW200510440A TW200510440A (en) 2005-03-16
TWI377209B true TWI377209B (en) 2012-11-21

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Family Applications (1)

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TW093122844A TWI377209B (en) 2003-08-01 2004-07-30 Novel n-glucoside derivatives having a sglt inhibitory activity

Country Status (18)

Country Link
US (1) US7521430B2 (enExample)
EP (1) EP1654269B1 (enExample)
JP (1) JP4717811B2 (enExample)
KR (1) KR101101500B1 (enExample)
CN (2) CN1829728A (enExample)
AU (1) AU2004260760B2 (enExample)
BR (1) BRPI0413233A (enExample)
CA (1) CA2534022C (enExample)
EA (1) EA011025B1 (enExample)
ES (1) ES2527053T3 (enExample)
IL (1) IL173051A (enExample)
MX (1) MXPA06001273A (enExample)
NO (1) NO333679B1 (enExample)
NZ (1) NZ545305A (enExample)
TW (1) TWI377209B (enExample)
UA (5) UA86042C2 (enExample)
WO (1) WO2005012321A1 (enExample)
ZA (2) ZA200601686B (enExample)

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US8785403B2 (en) 2003-08-01 2014-07-22 Mitsubishi Tanabe Pharma Corporation Glucopyranoside compound
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
AR053329A1 (es) * 2005-01-31 2007-05-02 Tanabe Seiyaku Co Derivados de indol utiles como inhibidores de los transportadores de glucosa dependientes del sodio (sglt)
TWI365186B (en) 2005-01-31 2012-06-01 Mitsubishi Tanabe Pharma Corp Indole derivatives
JP5073948B2 (ja) * 2005-01-31 2012-11-14 田辺三菱製薬株式会社 医薬組成物
TWI418556B (zh) * 2006-07-27 2013-12-11 Mitsubishi Tanabe Pharma Corp 吲哚衍生物
TWI499414B (zh) 2006-09-29 2015-09-11 Lexicon Pharmaceuticals Inc 鈉與葡萄糖第2型共同運輸體(co-transporter 2)的抑制物與其應用方法
AU2007329490B2 (en) * 2006-12-04 2012-05-17 Janssen Pharmaceutica N.V. Thienyl-containing glycopyranosyl derivatives as antidiabetics
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
WO2008109591A1 (en) * 2007-03-08 2008-09-12 Lexicon Pharmaceuticals, Inc. Phlorizin analogs as inhibitors of sodium glucose co-transporter 2
WO2009035969A1 (en) 2007-09-10 2009-03-19 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of sglt
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.
EP2668953A1 (en) 2008-05-22 2013-12-04 Bristol-Myers Squibb Company Pharmaceutical compositions comprising an SGLT2 inhibitor with a supply of carbohydrate and/or an inhibitor of uric acid synthesis
CN102149717B (zh) 2008-08-28 2014-05-14 辉瑞大药厂 二氧杂-双环[3.2.1]辛烷-2,3,4-三醇衍生物
WO2010031813A1 (en) * 2008-09-19 2010-03-25 Novartis Ag Glycoside derivatives and uses thereof
US9056850B2 (en) * 2008-10-17 2015-06-16 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of SGLT
US20110009347A1 (en) 2009-07-08 2011-01-13 Yin Liang Combination therapy for the treatment of diabetes
EP2451797B1 (en) 2009-07-10 2013-04-03 Janssen Pharmaceutica, N.V. CRYSTALLISATION PROCESS FOR 1-(ß-D-GLUCOPYRANOSYL)-4-METHYL-3-[5-(4-FLUOROPHENYL)-2-THIENYLMETHYL]BENZENE
WO2011047113A1 (en) * 2009-10-14 2011-04-21 Janssen Pharmaceutica Nv Process for the preparation of compounds useful as inhibitors of sglt2
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MY187718A (en) 2010-05-11 2021-10-14 Janssen Pharmaceutica Nv Pharmaceutical formulations
CN103596944B (zh) 2011-04-13 2017-02-22 詹森药业有限公司 可用作sglt2的抑制剂的化合物的制备方法
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
CN105008379B (zh) * 2013-02-26 2018-06-29 田边三菱制药株式会社 α-卤代四酰基葡萄糖的制造方法
CN103896930B (zh) * 2014-04-02 2016-08-17 安徽联创生物医药股份有限公司 卡格列净半水合物药用晶型的制备方法
US9695159B2 (en) 2014-05-27 2017-07-04 Glenmark Pharmaceuticals Limited Process for preparation of canagliflozin
CN104045673B (zh) * 2014-06-06 2017-01-18 安徽省食品药品检验研究院 双‑三氮唑缀合的假二糖衍生物及其制备方法
CN104478968A (zh) * 2015-01-14 2015-04-01 佛山市赛维斯医药科技有限公司 含噻唑基的o-半乳糖苷衍生物、其制备方法和用途
CN106188022A (zh) * 2015-04-30 2016-12-07 上海医药工业研究院 伊格列净的制备方法
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
MA51203A (fr) 2017-11-30 2020-10-07 Idorsia Pharmaceuticals Ltd Combinaison d'un dérivé de 4-pyrimidinesulfamide avec un inhibiteur de sglt-2 pour le traitement de maladies liées à l'endothéline
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Also Published As

Publication number Publication date
UA86042C2 (en) 2009-03-25
UA85569C2 (ru) 2009-02-10
ZA200601686B (en) 2007-05-30
US20070060545A1 (en) 2007-03-15
KR20060132539A (ko) 2006-12-21
KR101101500B1 (ko) 2012-01-03
EP1654269A1 (en) 2006-05-10
IL173051A (en) 2012-06-28
UA87991C2 (en) 2009-09-10
CA2534022C (en) 2012-10-02
NO20060219L (no) 2006-04-28
ZA200603880B (en) 2010-01-27
EP1654269B1 (en) 2014-10-15
CA2534022A1 (en) 2005-02-10
US7521430B2 (en) 2009-04-21
BRPI0413233A (pt) 2006-10-03
JP4717811B2 (ja) 2011-07-06
IL173051A0 (en) 2006-06-11
NZ545305A (en) 2008-11-28
UA83377C2 (uk) 2008-07-10
WO2005012321A1 (en) 2005-02-10
EA200600348A1 (ru) 2006-08-25
CN102060888A (zh) 2011-05-18
NO333679B1 (no) 2013-08-05
JP2007518682A (ja) 2007-07-12
AU2004260760A1 (en) 2005-02-10
ES2527053T3 (es) 2015-01-20
CN1829728A (zh) 2006-09-06
TW200510440A (en) 2005-03-16
UA86599C2 (en) 2009-05-12
AU2004260760B2 (en) 2009-08-13
EA011025B1 (ru) 2008-12-30
MXPA06001273A (es) 2006-04-11

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