HRP20170028T1 - Derivat morfolinonukleinske kiseline - Google Patents

Derivat morfolinonukleinske kiseline Download PDF

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Publication number
HRP20170028T1
HRP20170028T1 HRP20170028TT HRP20170028T HRP20170028T1 HR P20170028 T1 HRP20170028 T1 HR P20170028T1 HR P20170028T T HRP20170028T T HR P20170028TT HR P20170028 T HRP20170028 T HR P20170028T HR P20170028 T1 HRP20170028 T1 HR P20170028T1
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HR
Croatia
Prior art keywords
compound
salt
general formula
image
following general
Prior art date
Application number
HRP20170028TT
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English (en)
Inventor
Toshihiro Ueda
Original Assignee
Nippon Shinyaku Co., Ltd.
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 Nippon Shinyaku Co., Ltd. filed Critical Nippon Shinyaku Co., Ltd.
Publication of HRP20170028T1 publication Critical patent/HRP20170028T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (6)

1. Spoj, naznačen time što ga prikazuje sljedeća opća formula (1), ili njegova sol: [image] , gdje R1 predstavlja vodik ili skupinu koju prikazuje sljedeća opća formula (2): [image] , (gdje * predstavlja mjesto vezanja; R11, R12, R13 su isti ili različiti i svaki predstavlja vodik, alkil ili alkoksi) R2 predstavlja skupinu koju prikazuje sljedeća opća formula (3) ili (4): [image] , (gdje je * definiran kao što je opisano gore; R4 predstavlja alkil, arilmetil ili ariloksimetil; R5, R6 su isti ili različiti i svaki predstavlja alkil) R3 predstavlja hidroksi skupinu, koja može biti zaštićena trialkilsililom ili difenilalkilsililom, ili skupinom koju prikazuje sljedeća opća formula (5): [image] , (gdje je * definiran kao što je opisano gore; X predstavlja O ili S; Y predstavlja dialkilamino ili alkoksi; Z predstavlja halogen).
2. Spoj, ili njegova sol, u skladu s patentnim zahtjevom 1, naznačen time što je X O, Y je dialkilamino, a Z je klor.
3. Spoj, ili njegova sol, u skladu s patentnim zahtjevom 1, naznačen time što R3 je hidroksi skupina, koja može biti zaštićena t-butildimetilsililom ili t-butildifenilsililom.
4. Spoj, ili njegova sol, u skladu s patentnim zahtjevom 1, naznačen time što je R4 fenoksimetil.
5. Spoj, ili njegova sol, u skladu s patentnim zahtjevom 1, naznačen time što R1 je tritil, 4-metoksitritil, 4-metiltritil, 4,4′-dimetiltritil, 4,4′-dimetoksitritil ili 4,4′,4″-trimetiltritil.
6. Spoj, naznačen time što ga se bira između sljedećih (1) do (3), ili njihovih soli: (1) N9-[(2R,6S)-6-{(tert-butildimetilsililoksi)metil}-4-tritilmorfolin-2-il]-N2-(fenoksiacetil)-O6-(2-cijanoetil)gvanina, (2) N9-{(2R,6S)-6-hidroksimetil-4-tritilmorfolin-2-il}-N2-(fenoksiacetil)-O6-(2-cijanoetil)gvanina, (3) [(2S,6R)-6-{N2-(fenoksiacetil)-O6-(2-cijanoetil)guanin-9-il}-4-tritilmorfolin-2-il]metil-dimetilfosforoamidokloridata.
HRP20170028TT 2010-09-30 2017-01-10 Derivat morfolinonukleinske kiseline HRP20170028T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2010220865 2010-09-30
PCT/JP2011/072407 WO2012043730A1 (ja) 2010-09-30 2011-09-29 モルホリノ核酸誘導体
EP11829283.8A EP2623507B1 (en) 2010-09-30 2011-09-29 Morpholino nucleic acid derivative

Publications (1)

Publication Number Publication Date
HRP20170028T1 true HRP20170028T1 (hr) 2017-03-24

Family

ID=45893168

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20170028TT HRP20170028T1 (hr) 2010-09-30 2017-01-10 Derivat morfolinonukleinske kiseline

Country Status (18)

Country Link
US (1) US8969551B2 (hr)
EP (1) EP2623507B1 (hr)
JP (1) JP5831455B2 (hr)
KR (1) KR101764462B1 (hr)
CN (1) CN103154009B (hr)
CA (1) CA2813183C (hr)
CY (1) CY1118435T1 (hr)
DK (1) DK2623507T3 (hr)
ES (1) ES2607603T3 (hr)
HR (1) HRP20170028T1 (hr)
HU (1) HUE030292T2 (hr)
LT (1) LT2623507T (hr)
PL (1) PL2623507T3 (hr)
PT (1) PT2623507T (hr)
RS (1) RS55610B1 (hr)
SI (1) SI2623507T1 (hr)
SM (1) SMT201700038B (hr)
WO (1) WO2012043730A1 (hr)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE47769E1 (en) 2004-06-28 2019-12-17 The University Of Western Australia Antisense oligonucleotides for inducing exon skipping and methods of use thereof
WO2006086667A2 (en) 2005-02-09 2006-08-17 Avi Bio Pharma, Inc. Antisense composition and method for treating muscle atrophy
EP2350281B1 (en) 2008-10-24 2014-05-14 Sarepta Therapeutics, Inc. Multiple exon skipping compositions for dmd
ES2693459T3 (es) 2009-11-12 2018-12-11 The University Of Western Australia Moléculas antisentido y métodos para el tratamiento de patologías
CN107353317A (zh) * 2010-05-28 2017-11-17 萨勒普塔医疗公司 具有修饰的亚基间键和/或端基的寡核苷酸类似物
WO2012031243A2 (en) 2010-09-03 2012-03-08 Avi Biopharma, Inc. dsRNA MOLECULES COMPRISING OLIGONUCLEOTIDE ANALOGS HAVING MODIFIED INTERSUBUNIT LINKAGES AND/OR TERMINAL GROUPS
US20130085139A1 (en) 2011-10-04 2013-04-04 Royal Holloway And Bedford New College Oligomers
WO2013074834A1 (en) 2011-11-18 2013-05-23 Sarepta Therapeutics, Inc. Functionally-modified oligonucleotides and subunits thereof
CN104411831B (zh) 2012-03-20 2020-08-11 萨勒普塔医疗公司 寡核苷酸类似物的硼酸缀合物
CN102702265A (zh) * 2012-05-14 2012-10-03 天津特安化学科技有限公司 一种固相合成磷酰二胺吗啉代寡核苷酸及方法
IL293975A (en) 2013-03-14 2022-08-01 Sarepta Therapeutics Inc Preparations that skip axon for the treatment of muscular dystrophy
CA2906812A1 (en) 2013-03-15 2014-09-18 Sarepta Therapeutics, Inc. Improved compositions for treating muscular dystrophy
JP6477464B2 (ja) 2013-05-24 2019-03-06 味の素株式会社 モルフォリノオリゴヌクレオチドの製造方法
IL300444A (en) 2013-09-05 2023-04-01 Sarepta Therapeutics Inc Inclusion of exon 2 is induced by antisense in acid alpha-glucosidase
JP6901966B2 (ja) 2014-05-16 2021-07-14 オレゴン ステート ユニバーシティ アンチセンス抗菌化合物および方法
EP3569252B1 (en) 2014-05-19 2021-12-15 Oregon State University Antisense antibacterial compounds and methods
JP6673211B2 (ja) * 2014-10-14 2020-03-25 味の素株式会社 モルフォリノオリゴヌクレオチドの製造方法
EP3240794A4 (en) * 2014-12-31 2018-10-31 Oregon State University Antisense antibacterial compounds and methods
MA41795A (fr) 2015-03-18 2018-01-23 Sarepta Therapeutics Inc Exclusion d'un exon induite par des composés antisens dans la myostatine
HRP20231431T1 (hr) 2015-05-19 2024-03-01 Sarepta Therapeutics, Inc. Peptidno oligonukleotidni konjugati
WO2016196670A1 (en) 2015-06-01 2016-12-08 Sarepta Therapeutics, Inc. Antisense-induced exon exclusion in type vii collagen
EP3302489A4 (en) 2015-06-04 2019-02-06 Sarepta Therapeutics, Inc. METHOD AND COMPOUNDS FOR THE TREATMENT OF DISEASES AND SUFFERING IN CONNECTION WITH LYMPHOCYTES
EP4039690B1 (en) * 2015-08-05 2024-07-17 Eisai R&D Management Co., Ltd. A substantially diastereomerically pure phosphoramidochloridate, a method and a pharmaceutical composition
JP2018530560A (ja) 2015-10-09 2018-10-18 サレプタ セラピューティクス, インコーポレイテッド デュシェンヌ型筋ジストロフィーおよび関連障害の処置のための組成物および方法
JP2018538302A (ja) * 2015-12-15 2018-12-27 サレプタ セラピューティクス, インコーポレイテッド ペプチドオリゴヌクレオチド複合体
EP3394262B1 (en) 2015-12-23 2024-08-28 Oregon State University Antisense antibacterial compounds and methods
AU2016379399B2 (en) 2015-12-23 2022-12-08 Board Of Regents, The University Of Texas System Antisense antibacterial compounds and methods
AU2017254106B2 (en) 2016-04-18 2024-07-11 Sarepta Therapeutics, Inc. Antisense oligomers and methods of using the same for treating diseases associated with the acid alpha-glucosidase gene
AU2017258642B2 (en) 2016-04-29 2023-08-31 Sarepta Therapeutics, Inc. Oligonucleotide analogues targeting human LMNA
FI3464305T3 (fi) 2016-05-24 2024-10-30 Sarepta Therapeutics Inc Menetelmiä oligomeerien valmistamiseksi
PT3464306T (pt) 2016-05-24 2024-05-17 Sarepta Therapeutics Inc Processos para preparar oligómeros morfolino de fosforodiamidato
WO2017205880A1 (en) 2016-05-24 2017-11-30 Sarepta Therapeutics, Inc. Processes for preparing phosphorodiamidate morpholino oligomers
US11472824B2 (en) 2016-05-24 2022-10-18 Sarepta Therapeutics, Inc. Processes for preparing phosphorodiamidate morpholino oligomers
SG11201809494VA (en) 2016-05-24 2018-12-28 Sarepta Therapeutics Inc Pharmaceutical composition comprising eteplirsen
MA45362A (fr) 2016-05-24 2019-04-10 Sarepta Therapeutics Inc Procédés de préparation d'oligomères morpholino de phosphorodiamidate
JP7022079B2 (ja) 2016-06-30 2022-02-17 サレプタ セラピューティクス, インコーポレイテッド ホスホロジアミダートモルホリノオリゴマーを調製するためのプロセス
CN109937042B (zh) * 2016-09-20 2023-06-27 科罗拉多州立大学董事会法人团体 使用亚磷酰胺化学法合成主链修饰的吗啉代寡核苷酸和嵌合体
JP2020517638A (ja) 2017-04-20 2020-06-18 エータイアー ファーマ, インコーポレイテッド 肺の炎症を治療するための組成物および方法
US20200362339A1 (en) * 2017-09-25 2020-11-19 Sarepta Therapeutics, Inc. Processes for preparing phosphorodiamidate morpholino oligomers via fast-flow synthesis
JP7394753B2 (ja) 2017-10-18 2023-12-08 サレプタ セラピューティクス, インコーポレイテッド アンチセンスオリゴマー化合物
EP3792269A4 (en) * 2018-05-10 2022-06-22 Nippon Shinyaku Co., Ltd. PROCESS FOR PREPARING AN OLIGONUCLEIC ACID COMPOUND
WO2021025899A1 (en) 2019-08-02 2021-02-11 Sarepta Therapeutics, Inc. Phosphorodiamidate morpholino oligomer pharmaceutical compositions
CN114981280A (zh) 2019-11-13 2022-08-30 日本新药株式会社 寡核苷酸化合物的制造方法
US20230018780A1 (en) * 2019-11-13 2023-01-19 Nippon Shinyaku Co., Ltd. Method for producing oligonucleic acid compound
CN116096724A (zh) * 2020-07-10 2023-05-09 常州合全药业有限公司 用于制备寡核苷酸的方法
JPWO2022230954A1 (hr) * 2021-04-28 2022-11-03
KR20240004609A (ko) 2021-04-30 2024-01-11 사렙타 쎄러퓨틱스 인코퍼레이티드 근이영양증에 대한 치료 방법
US20240318179A1 (en) 2021-10-22 2024-09-26 Murdoch University Morpholino oligomers for treatment of peripheral myelin protein 22 related diseases
EP4458833A1 (en) 2021-12-27 2024-11-06 Nippon Shinyaku Co., Ltd. Method for producing oligonucleic acid compound
WO2023167908A1 (en) * 2022-03-01 2023-09-07 Eisai R&D Management Co., Ltd. Bis-protected, activated guanine monomers
WO2023178230A1 (en) 2022-03-17 2023-09-21 Sarepta Therapeutics, Inc. Phosphorodiamidate morpholino oligomer conjugates
WO2023205451A1 (en) 2022-04-22 2023-10-26 Entrada Therapeutics, Inc. Cyclic peptides for delivering therapeutics
WO2024064237A2 (en) 2022-09-21 2024-03-28 Sarepta Therapeutics, Inc. Dmd antisense oligonucleotide-mediated exon skipping efficiency

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1991009033A1 (en) 1989-12-20 1991-06-27 Anti-Gene Development Group Uncharged morpholino-based polymers having phosphorous-containing chiral intersubunit linkages
JP2005255530A (ja) * 2004-03-09 2005-09-22 Japan Science & Technology Agency 2−チオウリジン誘導体
LT2735568T (lt) * 2006-05-10 2017-11-27 Sarepta Therapeutics, Inc. Oligonukleotido analogai, turintys katijonines jungtis tarp subvienetų
US8076476B2 (en) * 2007-11-15 2011-12-13 Avi Biopharma, Inc. Synthesis of morpholino oligomers using doubly protected guanine morpholino subunits
DK2207779T3 (da) 2007-11-15 2014-07-14 Sarepta Therapeutics Inc Fremgangsmåde til syntese af morpholinooligomerer

Also Published As

Publication number Publication date
EP2623507A4 (en) 2014-03-19
JPWO2012043730A1 (ja) 2014-02-24
CY1118435T1 (el) 2017-06-28
KR101764462B1 (ko) 2017-08-02
US20130197220A1 (en) 2013-08-01
ES2607603T3 (es) 2017-04-03
WO2012043730A1 (ja) 2012-04-05
CA2813183C (en) 2017-09-19
CA2813183A1 (en) 2012-04-05
RS55610B1 (sr) 2017-06-30
LT2623507T (lt) 2017-01-25
CN103154009B (zh) 2015-06-10
PL2623507T3 (pl) 2017-03-31
PT2623507T (pt) 2016-12-23
SMT201700038B (it) 2017-03-08
DK2623507T3 (da) 2017-01-02
CN103154009A (zh) 2013-06-12
HUE030292T2 (en) 2017-04-28
US8969551B2 (en) 2015-03-03
SI2623507T1 (sl) 2017-04-26
EP2623507B1 (en) 2016-11-02
JP5831455B2 (ja) 2015-12-09
KR20130143045A (ko) 2013-12-30
EP2623507A1 (en) 2013-08-07

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