ME02469B - Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2 - Google Patents

Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2

Info

Publication number
ME02469B
ME02469B MEP-2016-153A MEP2016153A ME02469B ME 02469 B ME02469 B ME 02469B ME P2016153 A MEP2016153 A ME P2016153A ME 02469 B ME02469 B ME 02469B
Authority
ME
Montenegro
Prior art keywords
ring
formula
compound
optionally substituted
zinc salt
Prior art date
Application number
MEP-2016-153A
Other languages
German (de)
English (en)
French (fr)
Inventor
Ioannis Nicolaos Houpis
Sebastien François Emmanuel Lemaire
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of ME02469B publication Critical patent/ME02469B/me

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Classifications

    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/04—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
    • C07H13/06—Fatty acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biotechnology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (11)

1. Proces za pripremu jedinjenja formule (I)pri čemu su Prsten A, i Prsten B jedan od sledećih:(1) Prsten A je opciono supstituisani nezasićeni monociklični heterociklični prsten, i Prsten B je opciono supstituisani nezasićeni monociklični heterociklični prsten, opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten, ili opciono supstituisani benzenov prsten; ili(2) Prsten A je opciono supstituisani benzenov prsten, i Prsten B je opciono supstituisani nezasićeni monociklični heterociklični prsten, ili opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten pri čemu je Y povezan na heterociklični prsten fuzionisanog heterobicikličnog prstena; ili(3) Prsten A je opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten, pri čemu su šećerni ostatak X- (šećer) i ostatak-Y-(prsten B), oba na istom heterocikličnom prstenu fuzionisanog heterobicikličnog prstena, i Prsten B je opciono supstituisani nezasićeni monociklični heterociklični prsten, opciono supstituisani nezasićeni fuzionisani heterobiciklični prsten, ili opciono supstituisani benzenov prsten;X je atom ugljenika;Y je -(CH2)n-; pri čemu je n 1 ili 2;obezbedjujući da je u Prstenu A, X deo nezasićene veze;ili njegova farmaceutski prihvatljiva so ili solvat; obuhvatajućireagovanje jedinjenja formule (V) pri čemu je LG1 odlazća grupa, sa smešom cinkove soli i organolitijumovog reagensa; u prvom ugljovodoničnom rastvaraču; na temperaturi u rasponu od oko -78°C do oko sobne temperature; da se dobije smeša odgovarajućeg jedinjenja formule (VI), pri čemu je M1 litijum i cinkova so;mešanje u smešu jedinjenja formule (VI) i cinkove soli u prvom etarskom rastvaraču; da se dobije odgovarajuće jedinjenje formule (VII), pri čemu je M2 cink reaktivnih vrsta;reagovanje jedinjenja formule (VII), sa jedinjenjem formule (VIII), pri čemu svaka Z je nezavisno izabrana kiseonik zaštitna grupa i pri čemu je LG2 odlazeća grupa; da se dobije odgovarajuće jedinjenje formule (IX);uklanjanje zaštite jedinjenja formule (IX); da se dobije odgovarajuće jedinjenje formule (I).
2. Proces prema patentnom zahtevu 1 za pripremu jedinjenja formule (IS) ili njegove farmaceutski prihvatljive soli ili solvata; koji sadrži reagovanje jedinjenja formule (V-S) pri čemu je LG1 odlazća grupa, sa smešom cinkove soli i organolitijumovog reagensa; u prvom ugljovodoničnom rastvaraču; na temperaturi u rasponu od oko -78°C do oko sobne temperature; da se dobije smeša odgovarajućeg jedinjenja formule (VI-S), pri čemu je M1 litijum i cinkova so; mešanje u smešu jedinjenja formule (VI-S) i cinkove soli u prvom etarskom rastvaraču; da se dobije odgovarajuće jedinjenje formule (VII-S), pri čemu je M2 cink reaktivnih vrsta; reagovanje jedinjenja formule (VII-S), pri čemu je M2 vrste cinka, sa jedinjenjem formule (VIII-S), pri čemu je svaka Z nezavisno izabrana kiseonik zaštitna grupa i pri čemu je LG2 odlazeća grupa; da se dobije odgovarajuće jedinjenje formule (IX-S); uklanjanje zaštite jedinjenja formule (IX-S); da se dobije odgovarajuće jedinjenje formule (I-S).
3. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je cinkova so ZnBr2 i pri čemu je organo-litijumov reagens n-butil litijum.
4. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu su cinkova so, i organo-litijumov reagens prisutni u molarnom odnosu od oko 1:2.
5. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu su cinkova so, i organo-litijumov reagens prethodno mešani tokom perioda od oko 1 do oko 2 sata.
6. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je prvi ugljovodonični rastvarač toluen.
7. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je LG1 jod, zinkova so je ZnBr2, organolitijumov reagens je n-butil litijum, cinkova so i organo-litijumov reagens su pretrhodno-pomešani, prvi ugljovodonični rastvarač je toluen, i pri čemu je jedinjenje formule (V) reagovalo sa smešom cinkove soli i organolitijumovim reagensom na temperaturi od oko 0°C.
8. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je prvi etarski rastvarač din-butil etar.
9. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je prvi etarski rastvarač prisutan u količini u rasponu od oko 7% do oko 10% po zapremini.
10. Proces prema patentnom zahtevu 1 ili patentnom zahtevu 2, pri čemu je LG1 jod, Z je pivaloil i LG2 je brom.
11. Proces prema patentnom zahtevu 1, pri čemu X je atom ugljenika; Prsten A je izabran iz grupe koja se sastoji od 4-metilfenila i 4-hlorofenila; Y je -CH2- i vezan je na 3-poziciji Prstena A; i Prsten B je izabran iz grupe koja ses sastoji od 2-(5-(4-fluorofenil)-tienila) i 2-(5-(6-fluoro-pirid-3-il)-tienila). Janssen Phamaceutica NV., BE 2
MEP-2016-153A 2011-04-13 2012-04-12 Proces za pripremu jedinjenja koja su korisna kao inhibitori sglt2 ME02469B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161474936P 2011-04-13 2011-04-13
PCT/EP2012/056649 WO2012140120A1 (en) 2011-04-13 2012-04-12 Process for the preparation of compounds useful as inhibitors of sglt2
EP12715362.5A EP2697218B1 (en) 2011-04-13 2012-04-12 Process for the preparation of compounds useful as inhibitors of sglt2

Publications (1)

Publication Number Publication Date
ME02469B true ME02469B (me) 2017-02-20

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Country Status (20)

Country Link
US (1) US10544135B2 (me)
EP (1) EP2697218B1 (me)
JP (1) JP5973551B2 (me)
KR (1) KR101913587B1 (me)
CN (1) CN103596944B (me)
AU (1) AU2012241897C1 (me)
CA (1) CA2832938C (me)
CY (1) CY1117989T1 (me)
DK (1) DK2697218T3 (me)
EA (1) EA028946B1 (me)
ES (1) ES2586846T3 (me)
HR (1) HRP20161062T1 (me)
HU (1) HUE030116T2 (me)
ME (1) ME02469B (me)
PL (1) PL2697218T3 (me)
PT (1) PT2697218T (me)
RS (1) RS55056B1 (me)
SI (1) SI2697218T1 (me)
SM (1) SMT201600274B (me)
WO (1) WO2012140120A1 (me)

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CN104672227A (zh) * 2013-11-28 2015-06-03 镇江新元素医药科技有限公司 一类新型sglt2抑制剂化合物及其药物组合物
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CN103936725B (zh) * 2014-04-01 2016-07-27 天津大学 卡格列净的c晶型及其结晶制备方法
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CN104109157B (zh) * 2014-08-04 2016-05-25 山东康美乐医药科技有限公司 卡格列净的制备方法
CN105440025B (zh) * 2014-09-25 2019-02-12 深圳翰宇药业股份有限公司 一种制备卡格列净及其中间体的方法及所述中间体
CN104817554A (zh) * 2014-11-10 2015-08-05 镇江新元素医药科技有限公司 一类葡萄糖苷衍生物及其药物组合物
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
CN105884755B (zh) * 2015-02-14 2019-05-28 正大天晴药业集团股份有限公司 氘修饰的碳甙衍生物
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
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
CN105503845A (zh) * 2015-12-01 2016-04-20 北京普德康利医药科技发展有限公司 去氟卡格列净化合物及其制备方法和应用
CN109988128B (zh) * 2017-12-29 2022-08-19 江苏扬农化工股份有限公司 一种呋喃醇衍生物的合成方法
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
CN109111490B (zh) * 2018-08-09 2021-02-23 浙江大学 卤代新戊酰基吡喃葡萄糖及其用于sglt2抑制剂的制备方法
CN114591313A (zh) * 2020-12-04 2022-06-07 南京圣鼎医药科技有限公司 一种卡格列净的制备方法
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