ES2620469T3 - Procedimiento para la preparación de compuestos útiles como inhibidores de SGLT2 - Google Patents

Procedimiento para la preparación de compuestos útiles como inhibidores de SGLT2 Download PDF

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Publication number
ES2620469T3
ES2620469T3 ES10768162.9T ES10768162T ES2620469T3 ES 2620469 T3 ES2620469 T3 ES 2620469T3 ES 10768162 T ES10768162 T ES 10768162T ES 2620469 T3 ES2620469 T3 ES 2620469T3
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Prior art keywords
group
ring
formula
compound
optionally substituted
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ES10768162.9T
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English (en)
Spanish (es)
Inventor
Vittorio Farina
Sebastien Francois Emmanuel Lemaire
Ioannis N. Houpis
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F3/00—Compounds containing elements of Groups 2 or 12 of the Periodic Table
    • C07F3/06—Zinc compounds
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
ES10768162.9T 2009-10-14 2010-10-14 Procedimiento para la preparación de compuestos útiles como inhibidores de SGLT2 Active ES2620469T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25137809P 2009-10-14 2009-10-14
US251378P 2009-10-14
PCT/US2010/052598 WO2011047113A1 (en) 2009-10-14 2010-10-14 Process for the preparation of compounds useful as inhibitors of sglt2

Publications (1)

Publication Number Publication Date
ES2620469T3 true ES2620469T3 (es) 2017-06-28

Family

ID=43127364

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10768162.9T Active ES2620469T3 (es) 2009-10-14 2010-10-14 Procedimiento para la preparación de compuestos útiles como inhibidores de SGLT2

Country Status (30)

Country Link
US (1) US9174971B2 (OSRAM)
EP (1) EP2488515B1 (OSRAM)
JP (1) JP5833011B2 (OSRAM)
KR (1) KR101730920B1 (OSRAM)
CN (1) CN102648196B (OSRAM)
AU (1) AU2010306797B2 (OSRAM)
BR (1) BR112012008939B1 (OSRAM)
CA (1) CA2777528C (OSRAM)
CL (1) CL2012000929A1 (OSRAM)
CY (1) CY1118777T1 (OSRAM)
DK (1) DK2488515T3 (OSRAM)
EA (1) EA024368B1 (OSRAM)
ES (1) ES2620469T3 (OSRAM)
HR (1) HRP20170446T1 (OSRAM)
HU (1) HUE031375T2 (OSRAM)
IL (1) IL219094A (OSRAM)
IN (1) IN2012DN03299A (OSRAM)
LT (1) LT2488515T (OSRAM)
ME (1) ME02634B (OSRAM)
MX (1) MX340214B (OSRAM)
NZ (1) NZ599306A (OSRAM)
PH (1) PH12012500698A1 (OSRAM)
PL (1) PL2488515T3 (OSRAM)
PT (1) PT2488515T (OSRAM)
RS (1) RS55909B1 (OSRAM)
SG (1) SG10201500258WA (OSRAM)
SI (1) SI2488515T1 (OSRAM)
SM (1) SMT201700162T1 (OSRAM)
UA (1) UA109883C2 (OSRAM)
WO (1) WO2011047113A1 (OSRAM)

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WO2009035969A1 (en) * 2007-09-10 2009-03-19 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of sglt
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
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
WO2013061105A2 (en) * 2011-10-28 2013-05-02 Debreceni Egyetem Glycogen phosphorylase inhibitors
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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
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CN104557894A (zh) * 2013-10-18 2015-04-29 上海信谊药厂有限公司 坎格列汀晶型及其制备方法
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CN103980261B (zh) * 2014-04-01 2016-06-29 天津大学 卡格列净的a晶型及其结晶制备方法
CN103980262B (zh) * 2014-04-01 2016-06-22 天津大学 卡格列净的b晶型及其结晶制备方法
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CN103936726B (zh) * 2014-04-18 2016-06-15 王军 晶体、制备方法及其用途
CN105330706B (zh) * 2014-06-05 2019-04-16 江苏豪森药业集团有限公司 卡格列净中间体的制备方法
US20170247359A1 (en) * 2014-09-05 2017-08-31 Mylan Laboratories Ltd. Process for the preparation of canagliflozin
CN104402946B (zh) * 2014-11-17 2018-01-02 连云港恒运药业有限公司 卡格列净中间体及其无定形的制备方法
CN108003149A (zh) * 2014-12-25 2018-05-08 重庆医药工业研究院有限责任公司 一种卡格列净晶型i及其制备方法
CN104557895B (zh) * 2015-01-27 2017-10-31 江苏嘉逸医药有限公司 1‑(β‑D‑吡喃葡糖基)‑4‑甲基‑3‑[5‑(4‑氟苯基)‑2‑噻吩基甲基]苯的合成工艺
WO2016128995A1 (en) 2015-02-09 2016-08-18 Indoco Remedies Limited Process for the preparation of sglt inhibitor compounds
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
CN105153137A (zh) * 2015-09-17 2015-12-16 上海应用技术学院 一种艾格列净的制备方法
CZ2015729A3 (cs) 2015-10-13 2017-04-26 Zentiva, K.S. Příprava intermediátů pro syntézu Canagliflozinu a Dapagliflozinu
EP3621977A4 (en) 2017-05-09 2021-04-07 Piramal Pharma Limited SGLT2 INHIBITOR PREPARATION PROCESS AND ITS INTERMEDIARIES
CN110054657B (zh) * 2018-01-18 2021-06-29 亚宝药业集团股份有限公司 吡喃葡萄糖取代的吡唑化合物及其制备方法
CN112206216B (zh) * 2020-10-15 2023-03-17 江西华士药业有限公司 一种缓释达格列净的制备方法

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