AU2016302697B2 - Processes for the preparation of GalNAc acid derivatives - Google Patents
Processes for the preparation of GalNAc acid derivatives Download PDFInfo
- Publication number
- AU2016302697B2 AU2016302697B2 AU2016302697A AU2016302697A AU2016302697B2 AU 2016302697 B2 AU2016302697 B2 AU 2016302697B2 AU 2016302697 A AU2016302697 A AU 2016302697A AU 2016302697 A AU2016302697 A AU 2016302697A AU 2016302697 B2 AU2016302697 B2 AU 2016302697B2
- Authority
- AU
- Australia
- Prior art keywords
- formula
- acid
- ester
- galnac
- protecting group
- Prior art date
- Legal status (The legal status 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 status listed.)
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Classifications
-
- 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
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- 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
Landscapes
- 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15180058.8 | 2015-08-06 | ||
| EP15180058 | 2015-08-06 | ||
| PCT/EP2016/068361 WO2017021385A1 (en) | 2015-08-06 | 2016-08-02 | Processes for the preparation of galnac acid derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2016302697A1 AU2016302697A1 (en) | 2017-10-26 |
| AU2016302697B2 true AU2016302697B2 (en) | 2020-10-29 |
Family
ID=54056068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016302697A Active AU2016302697B2 (en) | 2015-08-06 | 2016-08-02 | Processes for the preparation of GalNAc acid derivatives |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10597417B2 (enExample) |
| EP (1) | EP3331892B1 (enExample) |
| JP (1) | JP6940477B2 (enExample) |
| KR (1) | KR102579520B1 (enExample) |
| CN (1) | CN107709342B (enExample) |
| AU (1) | AU2016302697B2 (enExample) |
| CA (1) | CA2982825C (enExample) |
| ES (1) | ES2744437T3 (enExample) |
| HR (1) | HRP20191589T1 (enExample) |
| IL (1) | IL256528B (enExample) |
| MX (1) | MX369556B (enExample) |
| PL (1) | PL3331892T3 (enExample) |
| SI (1) | SI3331892T1 (enExample) |
| WO (1) | WO2017021385A1 (enExample) |
Families Citing this family (7)
| 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 |
| EP3743116B1 (en) * | 2018-01-26 | 2024-07-10 | F. Hoffmann-La Roche AG | Radiolabelled oligonucleotides and process for their preparation |
| BR112020013431A2 (pt) * | 2018-01-29 | 2020-12-01 | F. Hoffmann-La Roche Ag | processo para a preparação de conjugados de galnac-oligonucleotídeo |
| US11510939B1 (en) | 2019-04-19 | 2022-11-29 | Apellis Pharmaceuticals, Inc. | RNAs for complement inhibition |
| EP3972984A1 (en) * | 2019-05-20 | 2022-03-30 | F. Hoffmann-La Roche AG | Process for the preparation of galnac phosphoramidite epimers |
| CA3140410A1 (en) | 2019-06-20 | 2020-12-24 | Martin Edelmann | 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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010108125A2 (en) * | 2009-03-19 | 2010-09-23 | The Johns Hopkins University | Psma-targeting compounds and uses thereof |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US133170A (en) * | 1872-11-19 | Improvement in wheelbarrows | ||
| US156917A (en) * | 1874-11-17 | Improvement in car-couplings | ||
| 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 |
| KR20110082601A (ko) * | 2008-12-19 | 2011-07-19 | 피너클 파마수티칼스, 인코포레이티드 | 페나조피리딘 화합물 |
| WO2011053614A1 (en) * | 2009-10-30 | 2011-05-05 | Merck Sharp & Dohme Corp. | Crystalline cdm-nag and methods for producing same |
| ES2562817T3 (es) * | 2010-02-24 | 2016-03-08 | Arrowhead Research Corporation | Composiciones para el suministro dirigido de ARNip |
| EA022078B1 (ru) * | 2010-08-10 | 2015-10-30 | Такеда Фармасьютикал Компани Лимитед | Гетероциклическое соединение и его применение |
| US8501930B2 (en) | 2010-12-17 | 2013-08-06 | Arrowhead Madison Inc. | Peptide-based in vivo siRNA delivery system |
| KR20130132475A (ko) * | 2010-12-17 | 2013-12-04 | 애로우헤드 리서치 코오포레이션 | siRNA의 갈락토오스 클러스터-약동학적 조절제 표적 물질 |
| KR102482890B1 (ko) | 2013-05-01 | 2022-12-30 | 아이오니스 파마수티컬즈, 인코포레이티드 | 아포지질단백질 (a) 발현을 조절하는 조성물 및 방법 |
| DK3013959T3 (da) | 2013-06-27 | 2020-02-17 | Roche Innovation Ct Copenhagen As | Antisense-oligomerer og konjugater målrettet pcsk9 |
| JP2017501684A (ja) * | 2013-11-14 | 2017-01-19 | ロシュ・イノベーション・センター・コペンハーゲン・アクティーゼルスカブRoche Innovation Center Copenhagen A/S | Apobアンチセンスコンジュゲート化合物 |
| SI3137605T1 (sl) | 2014-05-01 | 2021-02-26 | Ionis Pharmaceuticals, Inc. | Sestavki in metode za modulacijo ekspresije angiopoetin 3-podobnega |
-
2016
- 2016-08-02 PL PL16745745T patent/PL3331892T3/pl unknown
- 2016-08-02 CN CN201680038736.5A patent/CN107709342B/zh active Active
- 2016-08-02 AU AU2016302697A patent/AU2016302697B2/en active Active
- 2016-08-02 ES ES16745745T patent/ES2744437T3/es active Active
- 2016-08-02 KR KR1020177036266A patent/KR102579520B1/ko active Active
- 2016-08-02 MX MX2017015662A patent/MX369556B/es active IP Right Grant
- 2016-08-02 WO PCT/EP2016/068361 patent/WO2017021385A1/en not_active Ceased
- 2016-08-02 EP EP16745745.6A patent/EP3331892B1/en active Active
- 2016-08-02 SI SI201630375T patent/SI3331892T1/sl unknown
- 2016-08-02 CA CA2982825A patent/CA2982825C/en active Active
- 2016-08-02 HR HRP20191589 patent/HRP20191589T1/hr unknown
- 2016-08-02 JP JP2018502203A patent/JP6940477B2/ja active Active
-
2017
- 2017-12-24 IL IL256528A patent/IL256528B/en active IP Right Grant
-
2018
- 2018-02-06 US US15/890,181 patent/US10597417B2/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010108125A2 (en) * | 2009-03-19 | 2010-09-23 | The Johns Hopkins University | Psma-targeting compounds and uses thereof |
Non-Patent Citations (2)
| Title |
|---|
| CAS Registry No. 1185198-47-3; STN Entry date 16 September 2009; L-Lysine, N6-[(1,1-dimethylethoxy)carbonyl]-, phenylmethyl ester, 4-methylbenzenesulfonate * |
| CAS Registry No. 133170-57-7; STN Entry Date 12 April 1991; L-Lysine, N6-[(1 ,1-dimethylethoxy)carbonyl ]-, phenyl methyl ester, hydrochloride * |
Also Published As
| Publication number | Publication date |
|---|---|
| PL3331892T3 (pl) | 2019-11-29 |
| HRP20191589T1 (hr) | 2019-12-13 |
| BR112017021926A2 (pt) | 2018-07-03 |
| CN107709342B (zh) | 2021-09-03 |
| SI3331892T1 (sl) | 2019-10-30 |
| KR20180030783A (ko) | 2018-03-26 |
| EP3331892B1 (en) | 2019-07-03 |
| JP6940477B2 (ja) | 2021-09-29 |
| IL256528A (en) | 2018-02-28 |
| WO2017021385A1 (en) | 2017-02-09 |
| CA2982825C (en) | 2023-10-17 |
| HK1250717A1 (zh) | 2019-01-11 |
| KR102579520B1 (ko) | 2023-09-15 |
| JP2018523643A (ja) | 2018-08-23 |
| AU2016302697A1 (en) | 2017-10-26 |
| MX369556B (es) | 2019-11-12 |
| EP3331892A1 (en) | 2018-06-13 |
| IL256528B (en) | 2020-01-30 |
| MX2017015662A (es) | 2018-04-18 |
| CN107709342A (zh) | 2018-02-16 |
| US20180162894A1 (en) | 2018-06-14 |
| US10597417B2 (en) | 2020-03-24 |
| ES2744437T3 (es) | 2020-02-25 |
| CA2982825A1 (en) | 2017-02-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |