PE20180687A1 - Reactivos quirales para la preparacion de oligomeros homogeneos - Google Patents

Reactivos quirales para la preparacion de oligomeros homogeneos

Info

Publication number
PE20180687A1
PE20180687A1 PE2018000192A PE2018000192A PE20180687A1 PE 20180687 A1 PE20180687 A1 PE 20180687A1 PE 2018000192 A PE2018000192 A PE 2018000192A PE 2018000192 A PE2018000192 A PE 2018000192A PE 20180687 A1 PE20180687 A1 PE 20180687A1
Authority
PE
Peru
Prior art keywords
preparation
chiral reagents
diastereomerically pure
benzyl
alkyl
Prior art date
Application number
PE2018000192A
Other languages
English (en)
Inventor
Atsushi Endo
Robert T Yu
Francis Fang
Hyeong Wook Choi
Mingde Shan
Original Assignee
Eisai Randd Man 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 Eisai Randd Man Co Ltd filed Critical Eisai Randd Man Co Ltd
Publication of PE20180687A1 publication Critical patent/PE20180687A1/es

Links

Classifications

    • 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 System
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/7125Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/713Double-stranded nucleic acids or oligonucleotides
    • 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 System
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

SE REFIERE A COMPUESTOS FOSFORAMIDOCLORIDATO MORFONILO NUCLEOSIDOS ACTIVADOS DIASTEREOMERICAMENTE PUROS DE FORMULA (20), (22), (25), ENTRE OTROS, DONDE R1 Y R2 SON CADA UNO H, ALQUILO C1-C3, FENILO, ENTRE OTROS; R3 ES TRITILO OPCIONALMENTE SUSTITUIDO, BENCILO, DIFENILMETILO, ENTRE OTROS; R4 Y R5 SON CADA UNO -H, -C(O)R7 O C(O)OR7, EN DONDE R7 ES ALQUILO C1-C6, BENCILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN METODO DE PREPARACION Y UNA COMPOSICION QUE COMPRENDE UN OLIGOMERO DIASTEREOMERICAMENTE PURO
PE2018000192A 2015-08-05 2016-08-05 Reactivos quirales para la preparacion de oligomeros homogeneos PE20180687A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562201510P 2015-08-05 2015-08-05

Publications (1)

Publication Number Publication Date
PE20180687A1 true PE20180687A1 (es) 2018-04-23

Family

ID=56943909

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000192A PE20180687A1 (es) 2015-08-05 2016-08-05 Reactivos quirales para la preparacion de oligomeros homogeneos

Country Status (30)

Country Link
US (3) US10457698B2 (es)
EP (2) EP4039690A1 (es)
JP (3) JP6978406B2 (es)
KR (1) KR20180044303A (es)
CN (3) CN108350005B (es)
AU (3) AU2016302009B2 (es)
BR (2) BR112018002430A2 (es)
CA (1) CA2994842A1 (es)
CL (1) CL2018000322A1 (es)
CO (1) CO2018001615A2 (es)
DK (1) DK3331891T3 (es)
ES (1) ES2907629T3 (es)
HK (1) HK1248708A1 (es)
HR (1) HRP20220129T1 (es)
HU (1) HUE057593T2 (es)
IL (3) IL293066A (es)
LT (1) LT3331891T (es)
MA (1) MA44209B1 (es)
MD (1) MD3331891T2 (es)
MX (2) MX2018001557A (es)
MY (1) MY196627A (es)
PE (1) PE20180687A1 (es)
PH (1) PH12018500265A1 (es)
PL (1) PL3331891T3 (es)
PT (1) PT3331891T (es)
RS (1) RS62930B1 (es)
SI (1) SI3331891T1 (es)
UA (1) UA123995C2 (es)
WO (1) WO2017024264A2 (es)
ZA (2) ZA201801518B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108350005B (zh) * 2015-08-05 2024-02-06 卫材R&D管理有限公司 用于制备均一低聚物的手性试剂
WO2018057430A1 (en) 2016-09-20 2018-03-29 The Regents Of The University Of Colorado, A Body Corporate Synthesis of backbone modified morpholino oligonucleotides and chimeras using phosphoramidite chemistry
IL294271A (en) 2019-12-26 2022-08-01 Nippon Shinyaku Co Ltd Antisense nucleic acids that cause splicing on exon 50
JPWO2021172498A1 (es) 2020-02-28 2021-09-02
US20240060068A1 (en) 2020-12-11 2024-02-22 Eisai R&D Management Co., Ltd. Poly-morpholino oligonucleotide gapmers
AR124302A1 (es) 2020-12-11 2023-03-15 Eisai R&D Man Co Ltd Gápmeros de oligonucleótidos de objetivo tau
IL307787A (en) 2021-04-28 2023-12-01 Eisai R&D Man Co Ltd ANTISENSE OLIGONUCLEOTIDES and their use for the treatment of neurodegenerative disorders
WO2024010870A2 (en) * 2022-07-07 2024-01-11 Eisai R&D Management Co., Ltd. Crystalline monomers for preparing antisense oligonucleotides and methods of their preparation and use
WO2024092256A2 (en) 2022-10-27 2024-05-02 Eisai R&D Management Co., Ltd. Peptide-antisense oligonucleotides and their use for treatment of neurodegenerative disorders

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5185444A (en) 1985-03-15 1993-02-09 Anti-Gene Deveopment Group Uncharged morpolino-based polymers having phosphorous containing chiral intersubunit linkages
US6117993A (en) * 1995-05-23 2000-09-12 Hybridon, Inc. Synthons for oligonucleotide synthesis
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
US5874554A (en) 1996-12-13 1999-02-23 Incyte Pharmaceuticals, Inc. Methods and solvent vehicles for reagent delivery in oligonucleotide synthesis using automated pulse jetting devices
US6306599B1 (en) * 1999-07-16 2001-10-23 Agilent Technologies Inc. Biopolymer arrays and their fabrication
EP1176151B1 (en) * 2000-07-28 2014-08-20 Agilent Technologies, Inc. Synthesis of polynucleotides using combined oxidation/deprotection chemistry
AR036122A1 (es) 2001-07-03 2004-08-11 Avecia Biotechnology Inc Un complejo de sal que comprende un n-alquilimidazol y una 1,1-dioxo-1,2-dihidro-1l6-benzo [d]-isotiazol-3-ona y un metodo para sintetizar oligonucleotidos utilizando la quimica de fosforamidita
CA2884340C (en) * 2007-11-15 2017-07-25 Sarepta Therapeutics, Inc. Method of synthesis of morpholino oligomers
US8076476B2 (en) 2007-11-15 2011-12-13 Avi Biopharma, Inc. Synthesis of morpholino oligomers using doubly protected guanine morpholino subunits
WO2011018798A2 (en) 2009-08-14 2011-02-17 Indian Association For The Cultivation Of Science Morpholino-based antisense agent
CA2799501C (en) * 2010-05-28 2022-02-15 Sarepta Therapeutics, Inc. Oligonucleotide analogues having modified intersubunit linkages and/or terminal groups
RS55610B1 (sr) * 2010-09-30 2017-06-30 Nippon Shinyaku Co Ltd Derivat morfolino nukleinske kiseline
US9161948B2 (en) 2011-05-05 2015-10-20 Sarepta Therapeutics, Inc. Peptide oligonucleotide conjugates
KR102183273B1 (ko) * 2011-05-05 2020-11-27 사렙타 쎄러퓨틱스, 인코퍼레이티드 펩타이드 올리고뉴클레오타이드 접합체
TWI689513B (zh) 2011-10-07 2020-04-01 美商基利科學股份有限公司 抗病毒核苷酸類似物的製備方法
EA035030B1 (ru) 2011-11-18 2020-04-20 Сарепта Терапьютикс, Инк. Модифицированные морфолиновые аналоги олигонуклеотидов
ES2832531T3 (es) 2011-11-30 2021-06-10 Sarepta Therapeutics Inc Oligonucleótidos para el tratamiento de enfermedades por expansión de repeticiones
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
DE102015214943A1 (de) 2015-08-05 2017-02-09 Siemens Aktiengesellschaft Verfahren und Anlage für eine chemische Synthese
MY188405A (en) 2015-08-05 2021-12-08 Janssen Biotech Inc Anti-cd154 antibodies and methods of using them
GB201513921D0 (en) 2015-08-05 2015-09-23 Immatics Biotechnologies Gmbh Novel peptides and combination of peptides for use in immunotherapy against prostate cancer and other cancers
CN108350005B (zh) * 2015-08-05 2024-02-06 卫材R&D管理有限公司 用于制备均一低聚物的手性试剂

Also Published As

Publication number Publication date
UA123995C2 (uk) 2021-07-07
JP6978406B2 (ja) 2021-12-08
JP2022003067A (ja) 2022-01-11
RU2018107663A3 (es) 2020-05-21
MY196627A (en) 2023-04-23
AU2023226763A1 (en) 2023-09-28
IL284611B1 (en) 2023-07-01
RS62930B1 (sr) 2022-03-31
BR122023025447A2 (pt) 2024-01-16
HUE057593T2 (hu) 2022-05-28
JP7254869B2 (ja) 2023-04-10
RU2018107663A (ru) 2019-09-05
LT3331891T (lt) 2022-02-25
EP3331891A2 (en) 2018-06-13
MD3331891T2 (ro) 2022-04-30
AU2016302009B2 (en) 2021-09-30
CN113461733A (zh) 2021-10-01
IL257353A (en) 2018-04-30
PL3331891T3 (pl) 2022-03-28
EP3331891B1 (en) 2021-12-15
MX2022000124A (es) 2022-02-16
ZA201801518B (en) 2020-10-28
US20210171555A1 (en) 2021-06-10
US10457698B2 (en) 2019-10-29
IL293066A (en) 2022-07-01
ZA201905394B (en) 2022-07-27
DK3331891T3 (da) 2022-02-28
BR112018002430A2 (pt) 2018-09-18
CA2994842A1 (en) 2017-02-09
IL257353B2 (en) 2023-02-01
WO2017024264A2 (en) 2017-02-09
PT3331891T (pt) 2022-02-28
MA44209A (fr) 2021-04-28
AU2016302009A1 (en) 2018-03-29
MA44209B1 (fr) 2022-03-31
WO2017024264A8 (en) 2018-04-12
IL284611B2 (en) 2023-11-01
EP4039690A1 (en) 2022-08-10
HK1248708A1 (zh) 2018-10-19
US20200115405A1 (en) 2020-04-16
WO2017024264A3 (en) 2017-03-30
ES2907629T3 (es) 2022-04-25
IL257353B (en) 2022-10-01
HRP20220129T1 (hr) 2022-04-15
JP2018525380A (ja) 2018-09-06
CN108350005B (zh) 2024-02-06
AU2021290235A1 (en) 2022-01-20
CN108350005A (zh) 2018-07-31
JP2023085402A (ja) 2023-06-20
MX2018001557A (es) 2018-05-02
CO2018001615A2 (es) 2018-07-19
US20180222932A1 (en) 2018-08-09
KR20180044303A (ko) 2018-05-02
IL284611A (en) 2021-08-31
PH12018500265A1 (en) 2018-08-13
SI3331891T1 (sl) 2022-04-29
US10836784B2 (en) 2020-11-17
CN117924364A (zh) 2024-04-26
CL2018000322A1 (es) 2018-05-18
AU2021290235B2 (en) 2023-06-08

Similar Documents

Publication Publication Date Title
PE20180687A1 (es) Reactivos quirales para la preparacion de oligomeros homogeneos
CO2017008403A2 (es) Derivados de nucleósidos sustituidos útiles como agentes antineoplásicos
AR125320A2 (es) Compuesto cristalino, método de preparación y composición que lo comprende
CL2018003504A1 (es) Derivados de carbonucleósidos sustituidos útiles como agentes antineoplasicos.
ES2770058T3 (es) Compuestos y composiciones destinados a modular las actividades de quinasa de EGFR mutante
UY36838A (es) Compuestos heterocíclicos moduladores de la señalización de tnf alfa y composiciones farmacéuticas que los contienen
CL2017002813A1 (es) Proceso para preparar 4-amino-piridazinas
ES2723355T3 (es) Métodos útiles en la síntesis de análogos de halicondrina B
ECSP16012693A (es) Polipéptido para la escisión hidrolítica de la zearalenona y/o derivados de la zearalenona, polinucleótido aislado de la misma y polipéptido que contiene aditivo, uso y procedimiento de los mismos
EA201792503A1 (ru) Соль (s)-kck s-кетамина, соль (r)-kck s-кетамина и способы получения s-кетамина
EA201890648A2 (ru) Диоксолановые аналоги уридина для лечения рака
CO2017001178A2 (es) Derivado de piridona que tiene un grupo tetrahidropiranil metilo
PE20170946A1 (es) 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1
CO2017002253A2 (es) Compuesto dirigido a il-23a y tnf-alfa
DOP2017000120A (es) 4-oxo-3,4-dihidro-1,2,3-benzotriazinas como moduladores de gpr139
EA201790570A1 (ru) Модуляторы р2х7
CR20170438A (es) Desacetoxitubulisina h y análogos de esta
PE20180252A1 (es) Moduladores alostericos positivos del receptor muscarinico m2
PE20190979A1 (es) Compuestos de heteroarilcarboxamida como inhibidores de ripk2
PE20181352A1 (es) Compuestos heterociclicos que contienen bencilamina y composiciones utiles contra infeccion por micobacterias
AR104731A1 (es) Benzamidas sustituidas y métodos para utilizarlas
CL2019000662A1 (es) Inhibidores de dopamina–b–hidroxilasa.
CR20170005A (es) Derivados de insoindolina
PE20211780A1 (es) Compuestos de pirimidinodiona biciclicos sustituidos con tetrahidropirano (thp)
BR112017004925A2 (pt) composição e método