BR112012008939A2 - processo para a preparação de compostos úteis como inibidores de sglt2 - Google Patents

processo para a preparação de compostos úteis como inibidores de sglt2

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Publication number
BR112012008939A2
BR112012008939A2 BR112012008939A BR112012008939A BR112012008939A2 BR 112012008939 A2 BR112012008939 A2 BR 112012008939A2 BR 112012008939 A BR112012008939 A BR 112012008939A BR 112012008939 A BR112012008939 A BR 112012008939A BR 112012008939 A2 BR112012008939 A2 BR 112012008939A2
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BR
Brazil
Prior art keywords
formula
compound
preparation
compounds useful
sglt2 inhibitors
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Application number
BR112012008939A
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English (en)
Other versions
BR112012008939B1 (pt
Inventor
N Houpis Ioannis
Francois Emmanuel Lemaire Sebastien
Farina Vittorio
Original Assignee
Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112012008939A2 publication Critical patent/BR112012008939A2/pt
Publication of BR112012008939B1 publication Critical patent/BR112012008939B1/pt

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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 System
    • 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

Abstract

processo para a preparação de compostos úteis como inibidores de sglt2. a presente invenção é encaminhada a um processo inovador de preparação de compostos da fórmula (i): ou um sal farmaceuticamente aceitável ou solvato do mesmo; que compreende: fórmula (vii) (viii) (ix) reagir um composto da fórmula (vii), sendo que m^ 2^ é uma espécie de zinco, com um composto de fórmula (viii), em que cada z é um grupo protetor de oxigênio selecionado independentemente e sendo que lg^ 2^ é um grupo de saída; em uma mistura de um solvente éter e um solvente hidrocarboneto; para produzir o composto correspondente de fórmula (ix); desproteger o composto de f´romula (ix); para produzir o composto correspondente de fórmula formula (i).
BR112012008939-0A 2009-10-14 2010-10-14 Processo para a preparação de compostos úteis como inibidores de sglt2 BR112012008939B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25137809P 2009-10-14 2009-10-14
US61/251,378 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 (2)

Publication Number Publication Date
BR112012008939A2 true BR112012008939A2 (pt) 2017-06-27
BR112012008939B1 BR112012008939B1 (pt) 2021-06-22

Family

ID=43127364

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012008939-0A BR112012008939B1 (pt) 2009-10-14 2010-10-14 Processo para a preparação de compostos úteis como inibidores de sglt2

Country Status (29)

Country Link
US (1) US9174971B2 (pt)
EP (1) EP2488515B1 (pt)
JP (1) JP5833011B2 (pt)
KR (1) KR101730920B1 (pt)
CN (1) CN102648196B (pt)
AU (1) AU2010306797B2 (pt)
BR (1) BR112012008939B1 (pt)
CA (1) CA2777528C (pt)
CL (1) CL2012000929A1 (pt)
CY (1) CY1118777T1 (pt)
DK (1) DK2488515T3 (pt)
EA (1) EA024368B1 (pt)
ES (1) ES2620469T3 (pt)
HK (1) HK1170241A1 (pt)
HR (1) HRP20170446T1 (pt)
HU (1) HUE031375T2 (pt)
IL (1) IL219094A (pt)
IN (1) IN2012DN03299A (pt)
LT (1) LT2488515T (pt)
ME (1) ME02634B (pt)
MX (1) MX340214B (pt)
NZ (1) NZ599306A (pt)
PL (1) PL2488515T3 (pt)
PT (1) PT2488515T (pt)
RS (1) RS55909B1 (pt)
SG (1) SG10201500258WA (pt)
SI (1) SI2488515T1 (pt)
UA (1) UA109883C2 (pt)
WO (1) WO2011047113A1 (pt)

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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
CN104530023A (zh) * 2014-12-25 2015-04-22 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
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