BR112017005938A2 - compostos, processo de preparação de composto, processo de preparação de conjugado de galnac e ácido nucleico e usos de composto - Google Patents

compostos, processo de preparação de composto, processo de preparação de conjugado de galnac e ácido nucleico e usos de composto

Info

Publication number
BR112017005938A2
BR112017005938A2 BR112017005938A BR112017005938A BR112017005938A2 BR 112017005938 A2 BR112017005938 A2 BR 112017005938A2 BR 112017005938 A BR112017005938 A BR 112017005938A BR 112017005938 A BR112017005938 A BR 112017005938A BR 112017005938 A2 BR112017005938 A2 BR 112017005938A2
Authority
BR
Brazil
Prior art keywords
preparation process
compound
nucleic acid
galnac
compounds
Prior art date
Application number
BR112017005938A
Other languages
English (en)
Inventor
Rosenbohm Christoph
Ravn Jacob
Albaek Nanna
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112017005938A2 publication Critical patent/BR112017005938A2/pt

Links

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
    • 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
    • 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
    • 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
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

a presente invenção refere-se, de forma geral, ao campo de derivados de fosforamidita. particularmente, a presente invenção refere-se a moléculas de n-acetilgalactosamina fosforamidita e conjugados de moléculas de ácido nucleico com moléculas que contêm n-acetilgalactosamina. também são fornecidos métodos de preparação dessas moléculas e seus possíveis usos, particularmente em medicina.
BR112017005938A 2014-10-10 2015-10-09 compostos, processo de preparação de composto, processo de preparação de conjugado de galnac e ácido nucleico e usos de composto BR112017005938A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14188444 2014-10-10
EP15181807 2015-08-20
PCT/EP2015/073331 WO2016055601A1 (en) 2014-10-10 2015-10-09 Galnac phosphoramidites, nucleic acid conjugates thereof and their use

Publications (1)

Publication Number Publication Date
BR112017005938A2 true BR112017005938A2 (pt) 2017-12-12

Family

ID=54291295

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017005938A BR112017005938A2 (pt) 2014-10-10 2015-10-09 compostos, processo de preparação de composto, processo de preparação de conjugado de galnac e ácido nucleico e usos de composto

Country Status (14)

Country Link
US (2) US20170327524A1 (pt)
EP (1) EP3204397A1 (pt)
JP (1) JP6626101B2 (pt)
KR (1) KR20170068469A (pt)
CN (1) CN106795200B (pt)
AU (1) AU2015329974B2 (pt)
BR (1) BR112017005938A2 (pt)
CA (1) CA2961993A1 (pt)
IL (1) IL251145A0 (pt)
MX (1) MX2017004039A (pt)
RU (1) RU2017114156A (pt)
SG (1) SG11201702877TA (pt)
WO (1) WO2016055601A1 (pt)
ZA (1) ZA201701845B (pt)

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201408623D0 (en) 2014-05-15 2014-07-02 Santaris Pharma As Oligomers and oligomer conjugates
US20170327524A1 (en) 2014-10-10 2017-11-16 Hoffmann-La Roche, Inc. Galnac phosphoramidites, nucleic acid conjugates thereof and their use
US10478503B2 (en) 2016-01-31 2019-11-19 University Of Massachusetts Branched oligonucleotides
UY37146A (es) 2016-03-07 2017-09-29 Arrowhead Pharmaceuticals Inc Ligandos de direccionamiento para compuestos terapéuticos
KR20230136689A (ko) 2016-03-14 2023-09-26 에프. 호프만-라 로슈 아게 Pd-l1 발현의 감소를 위한 올리고뉴클레오티드
EP3228326A1 (en) * 2016-04-05 2017-10-11 Silence Therapeutics GmbH Nucleic acid linked to a trivalent glycoconjugate
MA45478A (fr) * 2016-04-11 2019-02-20 Arbutus Biopharma Corp Compositions de conjugués d'acides nucléiques ciblés
KR102468177B1 (ko) 2016-04-14 2022-11-16 에프. 호프만-라 로슈 아게 트리틸-모노-GalNAc 화합물 및 이의 용도
MA45496A (fr) 2016-06-17 2019-04-24 Hoffmann La Roche Molécules d'acide nucléique pour la réduction de l'arnm de padd5 ou pad7 pour le traitement d'une infection par l'hépatite b
WO2018031933A2 (en) 2016-08-12 2018-02-15 University Of Massachusetts Conjugated oligonucleotides
CN110023321A (zh) 2016-08-17 2019-07-16 索尔斯蒂斯生物有限公司 多核苷酸构建体
KR20230115344A (ko) 2016-09-02 2023-08-02 애로우헤드 파마슈티컬스 인코포레이티드 표적화 리간드
WO2018067900A1 (en) * 2016-10-06 2018-04-12 Ionis Pharmaceuticals, Inc. Method of conjugating oligomeric compounds
EP3594346A4 (en) 2017-03-10 2020-12-16 National Center For Child Health And Development ANTISENSE OLIGONUCLEOTIDE AND COMPOSITION FOR THE PREVENTION OR TREATMENT OF GLYCOGEN STORAGE DISEASE TYPE IA
EP3385272A1 (en) 2017-04-05 2018-10-10 Silence Therapeutics GmbH Further novel oligonucleotide-ligand conjugates
WO2018185252A1 (en) * 2017-04-05 2018-10-11 Silence Therapeutics Gmbh Nucleic acid conjugates
SG11201909433XA (en) 2017-04-11 2019-11-28 Arbutus Biopharma Corp Targeted compositions
CN107674094A (zh) * 2017-09-18 2018-02-09 中国石油大学(华东) 一种亚磷酰胺硫辛醇酯及其合成方法和用途
KR102431353B1 (ko) 2017-10-16 2022-08-10 에프. 호프만-라 로슈 아게 B형 간염 감염을 치료하기 위한 PAPD5 및 PAPD7 mRNA의 감소용 핵산 분자
CN109957566B (zh) * 2017-12-26 2023-08-25 广州市锐博生物科技有限公司 修饰的寡核苷酸和可用于合成修饰的寡核苷酸的化合物
JP7011080B2 (ja) * 2017-12-26 2022-02-10 クワンチョウ リボバイオ カンパニー リミテッド 修飾オリゴヌクレオチドおよび修飾オリゴヌクレオチドの合成に使用可能な化合物
AU2019213004B2 (en) * 2018-01-29 2024-03-07 F. Hoffmann-La Roche Ag Process for the preparation of GalNAc oligonucleotide conjugates
US11958878B2 (en) 2018-03-09 2024-04-16 Daiichi Sankyo Company, Limited Therapeutic agent for glycogen storage disease type IA
MA52661A (fr) 2018-04-05 2021-02-17 Centre Leon Berard Utilisation d'inhibiteurs de fubp1 dans le traitement d'une infection par le virus de l'hépatite b
TW202020151A (zh) 2018-07-03 2020-06-01 瑞士商赫孚孟拉羅股份公司 用於調制 Tau 表現之寡核苷酸
BR112021000538A2 (pt) 2018-07-13 2021-04-06 F. Hoffmann-La Roche Ag Oligonucleotídeos para modular a expressão de rtel1
MX2021001590A (es) 2018-08-10 2021-07-02 Univ Massachusetts Oligonucleótidos modificados dirigidos a snp.
US20220160870A1 (en) 2018-08-28 2022-05-26 Roche Innovation Center Copenhagen A/S Neoantigen engineering using splice modulating compounds
BR112021012713A2 (pt) * 2018-12-28 2021-09-21 Sirnaomics, Inc. Distribuição direcionada de moléculas terapêuticas
US11492619B2 (en) 2019-01-18 2022-11-08 University Of Massachusetts Dynamic pharmacokinetic-modifying anchors
EP3931348B1 (en) 2019-02-26 2023-08-09 Roche Innovation Center Copenhagen A/S Oligonucleotide formulation method
PE20220574A1 (es) 2019-05-31 2022-04-20 Aligos Therapeutics Inc Oligonucleotidos gapmer modificados y metodos de uso
TW202123973A (zh) 2019-09-10 2021-07-01 日商第一三共股份有限公司 用於肝臟遞送之GalNAc-寡核苷酸結合物及製造方法
CN111041025B (zh) 2019-12-17 2021-06-18 深圳市瑞吉生物科技有限公司 基于结合N-乙酰半乳糖胺多肽的mRNA靶向分子及其制备方法
EP4077670A1 (en) 2019-12-19 2022-10-26 F. Hoffmann-La Roche AG Use of cops3 inhibitors for treating hepatitis b virus infection
EP4077668A1 (en) 2019-12-19 2022-10-26 F. Hoffmann-La Roche AG Use of scamp3 inhibitors for treating hepatitis b virus infection
EP4077671A1 (en) 2019-12-19 2022-10-26 F. Hoffmann-La Roche AG Use of saraf inhibitors for treating hepatitis b virus infection
WO2021122735A1 (en) 2019-12-19 2021-06-24 F. Hoffmann-La Roche Ag Use of sept9 inhibitors for treating hepatitis b virus infection
EP4077669A1 (en) 2019-12-19 2022-10-26 F. Hoffmann-La Roche AG Use of sbds inhibitors for treating hepatitis b virus infection
CA3163490A1 (en) 2019-12-24 2021-07-01 F. Hoffman-La Roche Ag Pharmaceutical combination of a therapeutic oligonucleotide targeting hbv and a tlr7 agonist for treatment of hbv
WO2021130270A1 (en) 2019-12-24 2021-07-01 F. Hoffmann-La Roche Ag Pharmaceutical combination of antiviral agents targeting hbv and/or an immune modulator for treatment of hbv
WO2021197371A1 (zh) * 2020-03-31 2021-10-07 南京金斯瑞生物科技有限公司 一种含有刚性连接子的生物偶联物
CN111575279A (zh) * 2020-04-27 2020-08-25 江苏为真生物医药技术股份有限公司 利用asgpr小分子配体特异性捕获肝细胞外囊泡或循环肿瘤细胞的方法
AR122731A1 (es) 2020-06-26 2022-10-05 Hoffmann La Roche Oligonucleótidos mejorados para modular la expresión de fubp1
CN111744019B (zh) 2020-07-01 2023-08-04 深圳瑞吉生物科技有限公司 基于甘露糖的mRNA靶向递送系统及其应用
WO2022038211A2 (en) 2020-08-21 2022-02-24 F. Hoffmann-La Roche Ag Use of a1cf inhibitors for treating hepatitis b virus infection
WO2022140365A1 (en) * 2020-12-22 2022-06-30 Empirico Inc. Galnac compositions for improving sirna bioavailability
TW202246500A (zh) 2021-02-02 2022-12-01 瑞士商赫孚孟拉羅股份公司 用於抑制 ｒｔｅｌ１ 表現之增強型寡核苷酸
WO2022189861A1 (en) 2021-03-08 2022-09-15 Tollys Carbohydrate conjugates of tlr3 ligands and uses thereof
EP4161942B1 (en) 2021-03-19 2023-08-02 Bachem Holding AG Improved oligonucleotide synthesis suppressing depurination
WO2022214692A1 (en) 2021-04-09 2022-10-13 Bachem Holding Ag Pseudo solid phase protecting group and methods for the synthesis of oligonucleotides and oligonucleotide conjugates
WO2022271786A1 (en) 2021-06-23 2022-12-29 University Of Massachusetts Optimized anti-flt1 oligonucleotide compounds for treatment of preeclampsia and other angiogenic disorders
WO2023111210A1 (en) 2021-12-17 2023-06-22 F. Hoffmann-La Roche Ag Combination of oligonucleotides for modulating rtel1 and fubp1
WO2023178144A2 (en) 2022-03-16 2023-09-21 Empirico Inc. Galnac compositions for improving sirna bioavailability
WO2024061842A1 (en) 2022-09-19 2024-03-28 Bachem Holding Ag Improved oligonucleotide synthesis
WO2024083746A1 (en) 2022-10-17 2024-04-25 Bachem Holding Ag Method and composition for oligonucleotide synthesis

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996030386A1 (fr) 1995-03-31 1996-10-03 Drug Delivery System Institute, Ltd. Derives d'amidite et derives d'oligonucleotides
US6617442B1 (en) 1999-09-30 2003-09-09 Isis Pharmaceuticals, Inc. Human Rnase H1 and oligonucleotide compositions thereof
EP2415486B1 (en) 2001-05-18 2017-02-22 Sirna Therapeutics, Inc. Conjugates and compositions for cellular delivery
JP4221921B2 (ja) * 2001-08-23 2009-02-12 ブラザー工業株式会社 印刷装置
DK3222722T3 (da) 2002-11-18 2019-06-17 Roche Innovation Ct Copenhagen As Antisense-design
US20050053981A1 (en) 2003-09-09 2005-03-10 Swayze Eric E. Gapped oligomeric compounds having linked bicyclic sugar moieties at the termini
US20050074801A1 (en) 2003-09-09 2005-04-07 Monia Brett P. Chimeric oligomeric compounds comprising alternating regions of northern and southern conformational geometry
US20120122801A1 (en) 2005-01-05 2012-05-17 Prosensa B.V. Mannose-6-phosphate receptor mediated gene transfer into muscle cells
US20060148740A1 (en) 2005-01-05 2006-07-06 Prosensa B.V. Mannose-6-phosphate receptor mediated gene transfer into muscle cells
WO2007031091A2 (en) 2005-09-15 2007-03-22 Santaris Pharma A/S Rna antagonist compounds for the modulation of p21 ras expression
PL1984381T3 (pl) 2006-01-27 2011-03-31 Isis Pharmaceuticals Inc Zmodyfikowane w pozycji 6 analogi bicykliczne kwasów nukleinowych
EP2019692B1 (en) 2006-05-05 2014-06-04 Isis Pharmaceuticals, Inc. Compounds and methods for modulating expression of gccr
JP5441688B2 (ja) 2006-05-11 2014-03-12 アイシス ファーマシューティカルズ， インコーポレーテッド ５’修飾二環式核酸類似体
US8580756B2 (en) 2007-03-22 2013-11-12 Santaris Pharma A/S Short oligomer antagonist compounds for the modulation of target mRNA
WO2008131419A2 (en) 2007-04-23 2008-10-30 Alnylam Pharmaceuticals, Inc. Glycoconjugates of rna interference agents
WO2008150729A2 (en) 2007-05-30 2008-12-11 Isis Pharmaceuticals, Inc. N-substituted-aminomethylene bridged bicyclic nucleic acid analogs
EP2173760B2 (en) 2007-06-08 2015-11-04 Isis Pharmaceuticals, Inc. Carbocyclic bicyclic nucleic acid analogs
EP2176280B2 (en) 2007-07-05 2015-06-24 Isis Pharmaceuticals, Inc. 6-disubstituted bicyclic nucleic acid analogs
US8546556B2 (en) 2007-11-21 2013-10-01 Isis Pharmaceuticals, Inc Carbocyclic alpha-L-bicyclic nucleic acid analogs
WO2009073809A2 (en) 2007-12-04 2009-06-11 Alnylam Pharmaceuticals, Inc. Carbohydrate conjugates as delivery agents for oligonucleotides
WO2009090182A1 (en) 2008-01-14 2009-07-23 Santaris Pharma A/S C4'-substituted - dna nucleotide gapmer oligonucleotides
WO2009100320A2 (en) 2008-02-07 2009-08-13 Isis Pharmaceuticals, Inc. Bicyclic cyclohexitol nucleic acid analogs
DK2285819T3 (da) 2008-04-04 2013-12-02 Isis Pharmaceuticals Inc Oligomere forbindelser omfattende neutralt bundne, terminale bicykliske nukleosider
EP2274423A2 (en) 2008-04-04 2011-01-19 Isis Pharmaceuticals, Inc. Oligomeric compounds comprising bicyclic nucleosides and having reduced toxicity
WO2010036698A1 (en) 2008-09-24 2010-04-01 Isis Pharmaceuticals, Inc. Substituted alpha-l-bicyclic nucleosides
EP2462153B1 (en) 2009-08-06 2015-07-29 Isis Pharmaceuticals, Inc. Bicyclic cyclohexose nucleic acid analogs
WO2011085102A1 (en) 2010-01-11 2011-07-14 Isis Pharmaceuticals, Inc. Base modified bicyclic nucleosides and oligomeric compounds prepared therefrom
KR101956623B1 (ko) 2010-02-24 2019-03-12 애로우헤드 파마슈티컬스 인코포레이티드 ｓｉＲＮＡ의 표적 전달용 조성물
WO2011115818A1 (en) 2010-03-17 2011-09-22 Isis Pharmaceuticals, Inc. 5'-substituted bicyclic nucleosides and oligomeric compounds prepared therefrom
EP3192800A1 (en) 2010-12-17 2017-07-19 Arrowhead Pharmaceuticals, Inc. Galactose cluster-pharmacokinetic modulator targeting moiety for sirna
RU2599449C1 (ru) 2011-12-15 2016-10-10 Байонир Корпорейшн Новые конъюгаты олигонуклеотидов и их применение
AU2013346767B2 (en) 2012-11-15 2019-04-11 Roche Innovation Center Copenhagen A/S Oligonucleotide conjugates
DK2951305T3 (en) 2013-01-30 2018-10-29 Hoffmann La Roche LNA oligonucleotide KULHYDRATKONJUGATER
AU2014259755B2 (en) * 2013-05-01 2018-08-30 Ionis Pharmaceuticals, Inc. Compositions and methods for modulating apolipoprotein (a) expression
EP3011028B1 (en) * 2013-06-21 2019-06-12 Ionis Pharmaceuticals, Inc. Compositions and methods for modulation of target nucleic acids
EP3974534A1 (en) 2014-05-01 2022-03-30 Ionis Pharmaceuticals, Inc. Compositions and methods for modulating growth hormone receptor expression
SG10201809953QA (en) 2014-05-01 2018-12-28 Ionis Pharmaceuticals Inc Compositions and methods for modulating complement factor b expression
BR122020024443B1 (pt) 2014-05-01 2022-02-22 Ionis Pharmaceuticals, Inc Composto e composição farmacêutica para modulação da expressão de angptl3
EP3137091B1 (en) 2014-05-01 2020-12-02 Ionis Pharmaceuticals, Inc. Conjugates of modified antisense oligonucleotides and their use for modulating pkk expression
US9315241B2 (en) 2014-05-02 2016-04-19 Seahorse Equipment Corp Buoyant turret mooring with porous receptor cage
US20170327524A1 (en) 2014-10-10 2017-11-16 Hoffmann-La Roche, Inc. Galnac phosphoramidites, nucleic acid conjugates thereof and their use

Also Published As

Publication number Publication date
CN106795200B (zh) 2020-06-19
US11505569B2 (en) 2022-11-22
RU2017114156A (ru) 2018-11-15
EP3204397A1 (en) 2017-08-16
SG11201702877TA (en) 2017-05-30
AU2015329974A1 (en) 2017-04-06
JP6626101B2 (ja) 2019-12-25
JP2017533189A (ja) 2017-11-09
US20170327524A1 (en) 2017-11-16
CN106795200A (zh) 2017-05-31
WO2016055601A1 (en) 2016-04-14
AU2015329974A8 (en) 2017-04-13
MX2017004039A (es) 2017-07-24
IL251145A0 (en) 2017-04-30
CA2961993A1 (en) 2016-04-14
AU2015329974B2 (en) 2019-06-20
KR20170068469A (ko) 2017-06-19
ZA201701845B (en) 2018-05-30
RU2017114156A3 (pt) 2019-05-07
US20210017214A1 (en) 2021-01-21

Similar Documents

Publication Publication Date Title
BR112017005938A2 (pt) compostos, processo de preparação de composto, processo de preparação de conjugado de galnac e ácido nucleico e usos de composto
CY1118899T1 (el) Ενωσεις ενεδιυνης, συζευγματα εξ’ αυτων, και χρησεις και μεθοδοι δια τουτων
CY1121225T1 (el) Συμπυκνωμενες iμιδαζολυλιμιδαζολες ως αντιiκες ενωσεις
BR112017027414A2 (pt) Derivados hidroxiéster, processo para prepará- los e composições farmacêuticas os contendo
BR112018013218A2 (pt) derivado de acrilanilida, método de preparação e aplicação do mesmo na farmácia
BR112018075284A2 (pt) derivados de piperidinila substituída por (hetero)arila, processo para sua preparação e composições farmacêuticas contendo-os
BR112015027951A2 (pt) arilquinazolinas
BR112015020772A2 (pt) compostos de pirimidina e piridina e seu uso
BR112017027831A2 (pt) derivados de hidroxiácido, um processo para sua preparação e composições farmacêuticas contendo-os
CU20170172A7 (es) 4,6-diaminoquinolin-3-carbonitrilos sustituidos útiles como agentes analgésicos, antipiréticos o antiinflamatorios y antineoplásicos
CY1123689T1 (el) Κρυσταλλικη μορφη ελευθερης βασης λορλατινιβης
BR112015023752A2 (pt) complexos multiespecificos monovalentes e multivalentes e seus usos
BR112017018832A2 (pt) profármacos de riluzol e seu uso
BR112016024644A2 (pt) vacinas de ácido nucleico
CR20150604A (es) Proceso para la preparación de eritrocitos cargados con una o más sustancias de interés farmacéutico y eritrocitos así obtenidos
BR112014007193A2 (pt) derivados de pirazoloquinolinona, preparação dos mesmos e uso terapêutico dos mesmos
BR112016029333A2 (pt) síntese de compostos de carbamoilpiridona policíclico
BR112016011170A8 (pt) derivados de heteroaril ácido butanoico, seus usos, combinação e composição farmacêutica
CL2017000715A1 (es) Compuestos de 1-alquil-6-oxo-1,6-dihidropiridin-3-ilo
CR20150211A (es) Compuestos diméricos
BR112016001645A2 (pt) derivados de oxoquinazolinil-butanamida
CU20150061A7 (es) PIRIMIDO-[4,5-b]-QUINOLINA-4,5(3H,10H)-DIONAS COMO SUPRESORAS DE MUTACIÓN SIN SENTIDO
BR112016025396A2 (pt) derivados de heterociclil-butanamida
BR112017008481A2 (pt) composto antimicótico
CY1121859T1 (el) Μεθοδος παρασκευης αναστολεων συνθασης γλυκοζυλοκεραμιδης

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07H 15/04 , C07H 15/08 , C07H 21/00

Ipc: C07H 15/04 (2006.01), C07H 15/08 (2006.01), C07H 2

B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements
B350 Update of information on the portal [chapter 15.35 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]