JP6940477B2 - ＧａｌＮＡｃ酸誘導体の調製法 - Google Patents

ＧａｌＮＡｃ酸誘導体の調製法 Download PDF

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Publication number
JP6940477B2
JP6940477B2 JP2018502203A JP2018502203A JP6940477B2 JP 6940477 B2 JP6940477 B2 JP 6940477B2 JP 2018502203 A JP2018502203 A JP 2018502203A JP 2018502203 A JP2018502203 A JP 2018502203A JP 6940477 B2 JP6940477 B2 JP 6940477B2
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formula
acid
ester
galnac
protecting group
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JP2018523643A (ja
JP2018523643A5 (OSRAM
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ヨルグ リル
ヨルグ リル
ルネ トラサルディ
ルネ トラサルディ
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C07H15/08—Polyoxyalkylene derivatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C245/00—Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
    • C07C245/20—Diazonium compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/125—Saturated compounds having only one carboxyl group and containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/10—Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with ester groups or with a carbon-halogen bond
    • C07C67/11—Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with ester groups or with a carbon-halogen bond being mineral ester groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
    • C07C69/67—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of saturated acids
    • C07C69/708—Ethers
    • 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
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes
    • 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)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2018502203A 2015-08-06 2016-08-02 ＧａｌＮＡｃ酸誘導体の調製法 Active JP6940477B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15180058 2015-08-06
EP15180058.8 2015-08-06
PCT/EP2016/068361 WO2017021385A1 (en) 2015-08-06 2016-08-02 Processes for the preparation of galnac acid derivatives

Publications (3)

Publication Number Publication Date
JP2018523643A JP2018523643A (ja) 2018-08-23
JP2018523643A5 JP2018523643A5 (OSRAM) 2019-09-19
JP6940477B2 true JP6940477B2 (ja) 2021-09-29

Family

ID=54056068

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JP2018502203A Active JP6940477B2 (ja) 2015-08-06 2016-08-02 ＧａｌＮＡｃ酸誘導体の調製法

Country Status (14)

Country Link
US (1) US10597417B2 (OSRAM)
EP (1) EP3331892B1 (OSRAM)
JP (1) JP6940477B2 (OSRAM)
KR (1) KR102579520B1 (OSRAM)
CN (1) CN107709342B (OSRAM)
AU (1) AU2016302697B2 (OSRAM)
CA (1) CA2982825C (OSRAM)
ES (1) ES2744437T3 (OSRAM)
HR (1) HRP20191589T1 (OSRAM)
IL (1) IL256528B (OSRAM)
MX (1) MX369556B (OSRAM)
PL (1) PL3331892T3 (OSRAM)
SI (1) SI3331892T1 (OSRAM)
WO (1) WO2017021385A1 (OSRAM)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018215049A1 (en) * 2017-05-23 2018-11-29 F. Hoffmann-La Roche Ag Process for galnac oligonucleotide conjugates
BR112020010436A2 (pt) * 2018-01-26 2020-11-24 F. Hoffmann-La Roche Ag oligonucleotídeo radiomarcado, processos para a preparação de um oligonucleotídeo radiomarcado, uso do oligonucleotídeo radiomarcado, método para determinar a biodistribuição e farmacocinética e oligonucleotídeo
SG11202007218YA (en) 2018-01-29 2020-08-28 Hoffmann La Roche Process for the preparation of galnac oligonucleotide conjugates
US11510939B1 (en) 2019-04-19 2022-11-29 Apellis Pharmaceuticals, Inc. RNAs for complement inhibition
AU2020278797B2 (en) * 2019-05-20 2025-06-05 F. Hoffmann-La Roche Ag Process for the preparation of GalNAc phosphoramidite epimers
US20230087946A1 (en) 2019-06-20 2023-03-23 Hoffmann-La Roche Inc. Radiolabeled moem type oligonucleotides and process for their preparation
CN110734372B (zh) * 2019-09-30 2024-09-24 兰州交通大学 一种合成烯丙基脂肪醇聚氧乙烯醚羧酸（apea-9）的方法

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US156917A (en) * 1874-11-17 Improvement in car-couplings
US133170A (en) * 1872-11-19 Improvement in wheelbarrows
US1185198A (en) * 1912-11-25 1916-05-30 Elliott Co Tube-cleaning apparatus.
JP5004234B2 (ja) * 2006-11-10 2012-08-22 独立行政法人産業技術総合研究所 膜マイクロドメイン又はコレステロール認識タンパク質検出用高感度分子プローブ
WO2010071878A1 (en) * 2008-12-19 2010-06-24 Pinnacle Pharmaceuticals, Inc. Phenazopyridine compounds
CA3257131A1 (en) * 2009-03-19 2025-04-15 The Johns Hopkins University PSMA-TARGETING COMPOUNDS AND RELATED USES
WO2011053614A1 (en) * 2009-10-30 2011-05-05 Merck Sharp & Dohme Corp. Crystalline cdm-nag and methods for producing same
NZ601737A (en) 2010-02-24 2013-06-28 Arrowhead Res Corp Compositions for targeted delivery of sirna
KR101852215B1 (ko) * 2010-08-10 2018-04-25 다케다 야쿠힌 고교 가부시키가이샤 헤테로시클릭 화합물 및 이의 용도
EP3192800A1 (en) * 2010-12-17 2017-07-19 Arrowhead Pharmaceuticals, Inc. Galactose cluster-pharmacokinetic modulator targeting moiety for sirna
US8501930B2 (en) 2010-12-17 2013-08-06 Arrowhead Madison Inc. Peptide-based in vivo siRNA delivery system
PL2992098T3 (pl) 2013-05-01 2019-09-30 Ionis Pharmaceuticals, Inc. Kompozycje i sposoby modulowania ekspresji hbv i ttr
SG10201908122XA (en) 2013-06-27 2019-10-30 Roche Innovation Ct Copenhagen As Antisense oligomers and conjugates targeting pcsk9
KR20160083876A (ko) * 2013-11-14 2016-07-12 로슈 이노베이션 센터 코펜하겐 에이/에스 ApoB 안티센스 접합체 화합물
EP3137605B1 (en) 2014-05-01 2020-10-28 Ionis Pharmaceuticals, Inc. Compositions and methods for modulating angiopoietin-like 3 expression

Also Published As

Publication number Publication date
US20180162894A1 (en) 2018-06-14
KR20180030783A (ko) 2018-03-26
EP3331892B1 (en) 2019-07-03
CA2982825C (en) 2023-10-17
MX2017015662A (es) 2018-04-18
SI3331892T1 (sl) 2019-10-30
US10597417B2 (en) 2020-03-24
HRP20191589T1 (hr) 2019-12-13
ES2744437T3 (es) 2020-02-25
KR102579520B1 (ko) 2023-09-15
CN107709342A (zh) 2018-02-16
MX369556B (es) 2019-11-12
WO2017021385A1 (en) 2017-02-09
BR112017021926A2 (pt) 2018-07-03
AU2016302697B2 (en) 2020-10-29
PL3331892T3 (pl) 2019-11-29
EP3331892A1 (en) 2018-06-13
HK1250717A1 (zh) 2019-01-11
CN107709342B (zh) 2021-09-03
IL256528B (en) 2020-01-30
AU2016302697A1 (en) 2017-10-26
JP2018523643A (ja) 2018-08-23
CA2982825A1 (en) 2017-02-09
IL256528A (en) 2018-02-28

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