JP6433001B2 - 腫瘍細胞へのRNAiトリガーのインビボ送達のためのポリ結合体 - Google Patents
腫瘍細胞へのRNAiトリガーのインビボ送達のためのポリ結合体 Download PDFInfo
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- JP6433001B2 JP6433001B2 JP2016533388A JP2016533388A JP6433001B2 JP 6433001 B2 JP6433001 B2 JP 6433001B2 JP 2016533388 A JP2016533388 A JP 2016533388A JP 2016533388 A JP2016533388 A JP 2016533388A JP 6433001 B2 JP6433001 B2 JP 6433001B2
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- 0 **C(*I)[N+]([N-])N[C@](*)C1OC1*c1ccccc1 Chemical compound **C(*I)[N+]([N-])N[C@](*)C1OC1*c1ccccc1 0.000 description 3
- VZJDCQLFHRYDDV-UHFFFAOYSA-N NC(Nc1cccc(CON(C(CC2)O)C2=O)c1)=N Chemical compound NC(Nc1cccc(CON(C(CC2)O)C2=O)c1)=N VZJDCQLFHRYDDV-UHFFFAOYSA-N 0.000 description 1
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/713—Double-stranded nucleic acids or oligonucleotides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07—ORGANIC CHEMISTRY
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
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- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06043—Leu-amino acid
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
- C07K5/06052—Val-amino acid
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
- C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0815—Tripeptides with the first amino acid being basic
- C07K5/0817—Tripeptides with the first amino acid being basic the first amino acid being Arg
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/322—2'-R Modification
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/351—Conjugate
- C12N2310/3513—Protein; Peptide
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/353—Nature of the modification linked to the nucleic acid via an atom other than carbon
- C12N2310/3535—Nitrogen
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2320/00—Applications; Uses
- C12N2320/30—Special therapeutic applications
- C12N2320/32—Special delivery means, e.g. tissue-specific
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Wood Science & Technology (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- General Engineering & Computer Science (AREA)
- Zoology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Microbiology (AREA)
- Plant Pathology (AREA)
- Physics & Mathematics (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Oil, Petroleum & Natural Gas (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361863056P | 2013-08-07 | 2013-08-07 | |
| US61/863,056 | 2013-08-07 | ||
| US14/452,626 US9487556B2 (en) | 2013-08-07 | 2014-08-06 | Polyconjugates for delivery of RNAi triggers to tumor cells in vivo |
| PCT/US2014/049851 WO2015021092A1 (en) | 2013-08-07 | 2014-08-06 | Polyconjugates for delivery of rnai triggers to tumor cells in vivo |
| US14/452,626 | 2014-08-06 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016535058A JP2016535058A (ja) | 2016-11-10 |
| JP2016535058A5 JP2016535058A5 (enExample) | 2016-12-22 |
| JP6433001B2 true JP6433001B2 (ja) | 2018-12-05 |
Family
ID=52449177
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533388A Active JP6433001B2 (ja) | 2013-08-07 | 2014-08-06 | 腫瘍細胞へのRNAiトリガーのインビボ送達のためのポリ結合体 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US9487556B2 (enExample) |
| EP (1) | EP3030244B1 (enExample) |
| JP (1) | JP6433001B2 (enExample) |
| KR (1) | KR20160035081A (enExample) |
| CN (1) | CN105451743B (enExample) |
| AU (1) | AU2014306021B2 (enExample) |
| CA (1) | CA2919088A1 (enExample) |
| EA (1) | EA201690051A1 (enExample) |
| IL (1) | IL243941B (enExample) |
| MX (1) | MX2016001006A (enExample) |
| SG (1) | SG11201600379TA (enExample) |
| TW (1) | TWI685347B (enExample) |
| WO (1) | WO2015021092A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105451743B (zh) * | 2013-08-07 | 2019-11-19 | 箭头研究公司 | 用于在活体中递送RNAi触发子至肿瘤细胞的聚偶联物 |
| EP3271482A4 (en) * | 2015-03-17 | 2019-02-13 | Arrowhead Pharmaceuticals, Inc. | COMPOSITIONS AND METHODS FOR INHIBITING THE GENE EXPRESSION OF FACTOR XII |
| WO2016149313A1 (en) * | 2015-03-17 | 2016-09-22 | Arrowhead Research Corporation | Improved disulfide-containing alkyne linking agents |
| KR102633963B1 (ko) | 2015-05-29 | 2024-02-05 | 애로우헤드 파마슈티컬스 인코포레이티드 | 생물학적으로 절단가능한 테트라펩티드 연결제 |
| JP7021076B2 (ja) | 2015-05-29 | 2022-02-16 | アローヘッド ファーマシューティカルズ インコーポレイテッド | Hif2αの遺伝子発現を阻害する組成物及び方法 |
| EP3252082A1 (en) * | 2016-05-31 | 2017-12-06 | Galderma S.A. | Method for deacetylation of biopolymers |
| ES2962687T3 (es) * | 2015-12-29 | 2024-03-20 | Galderma Holding SA | Reticulación de carbohidratos |
| PT3623390T (pt) * | 2016-05-31 | 2023-10-27 | Galderma Sa | Reticulador de hidrato de carbono |
| EP3630189A4 (en) | 2017-05-24 | 2021-06-23 | The Board of Regents of The University of Texas System | Linkers for antibody drug conjugates |
| SG11202009734VA (en) | 2018-04-27 | 2020-11-27 | Arrowhead Pharmaceuticals Inc | Integrin targeting ligands and uses thereof |
| KR20210113273A (ko) | 2019-01-09 | 2021-09-15 | 애로우헤드 파마슈티컬스 인코포레이티드 | HIF-2 알파 (EPAS1)의 발현을 억제하기 위한 RNAi 작용제, 그의 조성물, 및 사용 방법 |
| CN110240551B (zh) * | 2019-06-25 | 2022-02-11 | 成都郑源生化科技有限公司 | Fmoc-β-Ala-Gly-OH的制备方法 |
| WO2021111303A1 (en) | 2019-12-02 | 2021-06-10 | Galderma Holding SA | High molecular weight esthetic compositions |
| CN113004515B (zh) * | 2021-03-02 | 2023-02-24 | 厦门大学附属中山医院 | 一种仿透明质酸聚氨基酸衍生物、其制备方法及其应用 |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT850221E (pt) * | 1995-08-30 | 2001-11-30 | Searle & Co | Derivados de meta-guanidina ureia tioureia ou acido aminobenzoico azaciclico como antagonistas de integrina |
| AU2337097A (en) | 1996-03-29 | 1997-10-22 | G.D. Searle & Co. | Meta-substituted phenylene derivatives and their use as alphavbeta3 integrin antagonists or inhibitors |
| EP0927045B1 (en) * | 1996-09-10 | 2005-12-14 | The Burnham Institute | Tumor homing molecules, conjugates derived therefrom, and methods of using same |
| AU6067098A (en) | 1997-04-07 | 1998-10-08 | Cfpi Nufarm | Preparation process for 3,4-disubstituted dinitroanilines |
| CA2464271A1 (en) * | 2001-10-22 | 2003-05-01 | The Scripps Research Institute | Integrin targeting compounds |
| JP2004261024A (ja) * | 2003-02-28 | 2004-09-24 | Japan Science & Technology Agency | ペプチド修飾多糖類を用いる遺伝子治療剤 |
| CA2488224A1 (en) * | 2003-04-03 | 2004-10-21 | Alnylam Pharmaceuticals, Inc. | Irna conjugates |
| EP1742958B1 (en) | 2004-03-15 | 2017-05-17 | City of Hope | Methods and compositions for the specific inhibition of gene expression by double-stranded rna |
| AU2005304816A1 (en) * | 2004-11-04 | 2006-05-18 | Raul Andino | Syntheses of polyamine conjugates of small interfering RNAs (si-RNAs) and conjugates formed thereby |
| JP2008537752A (ja) * | 2005-04-12 | 2008-09-25 | イントラディグム コーポレイション | がんおよび他の新血管形成疾患を処置するためのRNAi治療用の組成物および方法 |
| EP2061443A4 (en) * | 2006-08-18 | 2013-07-24 | Arrowhead Res Corp | POLYCONJUGATE FOR IN VIVO ADMINISTRATION OF POLYNUCLEOTIDES |
| US8017109B2 (en) | 2006-08-18 | 2011-09-13 | Roche Madison Inc. | Endosomolytic poly(acrylate) polymers |
| EP2076257A4 (en) * | 2006-09-15 | 2014-04-16 | Belrose Pharma Inc | POLYMER CONJUGATES WITH POSITIVELY LOADED PARTS |
| WO2008045252A2 (en) | 2006-10-04 | 2008-04-17 | The Board Of Trustees Of The Leland Stanford Junior University | Engineered integrin binding peptides |
| EP2379083B1 (en) | 2008-12-18 | 2017-08-16 | Dicerna Pharmaceuticals, Inc. | Extended dicer substrate agents and methods for the specific inhibition of gene expression |
| US20100249214A1 (en) | 2009-02-11 | 2010-09-30 | Dicerna Pharmaceuticals | Multiplex dicer substrate rna interference molecules having joining sequences |
| ES2562817T3 (es) | 2010-02-24 | 2016-03-08 | Arrowhead Research Corporation | Composiciones para el suministro dirigido de ARNip |
| US8501930B2 (en) * | 2010-12-17 | 2013-08-06 | Arrowhead Madison Inc. | Peptide-based in vivo siRNA delivery system |
| CA2816041C (en) * | 2010-12-29 | 2019-01-08 | Arrowhead Research Corporation | In vivo polynucleotide delivery conjugates having enzyme sensitive linkages |
| KR20130108655A (ko) | 2010-12-29 | 2013-10-04 | 에프. 호프만-라 로슈 아게 | 핵산의 세포내 전달을 위한 소분자 접합체 |
| KR20140051357A (ko) | 2011-08-26 | 2014-04-30 | 애로우헤드 리서치 코오포레이션 | In Vivo 핵산 전달용 폴리(비닐 에스테르) 고분자 |
| EP2806899B1 (en) * | 2012-01-27 | 2016-10-19 | F.Hoffmann-La Roche Ag | Integrin antagonist conjugates for targeted delivery to cells expressing alpha-v-beta-3 |
| US20130197205A1 (en) | 2012-01-27 | 2013-08-01 | Hoffmann-La Roche Inc. | Chitosan covalently linked with small molecule integrin antagonist for targeted delivery |
| JP2015515530A (ja) | 2012-04-18 | 2015-05-28 | アローヘッド リサーチ コーポレイション | インビボ核酸送達のためのポリ(アクリラート)ポリマー |
| CN105451743B (zh) * | 2013-08-07 | 2019-11-19 | 箭头研究公司 | 用于在活体中递送RNAi触发子至肿瘤细胞的聚偶联物 |
-
2014
- 2014-08-06 CN CN201480044362.9A patent/CN105451743B/zh active Active
- 2014-08-06 MX MX2016001006A patent/MX2016001006A/es unknown
- 2014-08-06 US US14/452,626 patent/US9487556B2/en active Active
- 2014-08-06 WO PCT/US2014/049851 patent/WO2015021092A1/en not_active Ceased
- 2014-08-06 AU AU2014306021A patent/AU2014306021B2/en not_active Ceased
- 2014-08-06 EP EP14834389.0A patent/EP3030244B1/en active Active
- 2014-08-06 SG SG11201600379TA patent/SG11201600379TA/en unknown
- 2014-08-06 JP JP2016533388A patent/JP6433001B2/ja active Active
- 2014-08-06 CA CA2919088A patent/CA2919088A1/en not_active Abandoned
- 2014-08-06 EA EA201690051A patent/EA201690051A1/ru unknown
- 2014-08-06 KR KR1020167005887A patent/KR20160035081A/ko not_active Withdrawn
- 2014-08-07 TW TW103127144A patent/TWI685347B/zh not_active IP Right Cessation
-
2016
- 2016-02-03 IL IL243941A patent/IL243941B/en active IP Right Grant
- 2016-09-28 US US15/278,518 patent/US20170022497A1/en not_active Abandoned
-
2018
- 2018-11-13 US US16/189,550 patent/US20190062748A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EA201690051A1 (ru) | 2016-06-30 |
| IL243941A0 (en) | 2016-04-21 |
| CN105451743B (zh) | 2019-11-19 |
| TWI685347B (zh) | 2020-02-21 |
| US20170022497A1 (en) | 2017-01-26 |
| KR20160035081A (ko) | 2016-03-30 |
| US9487556B2 (en) | 2016-11-08 |
| SG11201600379TA (en) | 2016-02-26 |
| AU2014306021A2 (en) | 2016-11-24 |
| JP2016535058A (ja) | 2016-11-10 |
| EP3030244A4 (en) | 2017-06-28 |
| HK1220397A1 (zh) | 2017-05-05 |
| US20150045573A1 (en) | 2015-02-12 |
| EP3030244B1 (en) | 2021-04-21 |
| MX2016001006A (es) | 2016-04-19 |
| AU2014306021A1 (en) | 2016-01-28 |
| CN105451743A (zh) | 2016-03-30 |
| AU2014306021B2 (en) | 2018-12-13 |
| WO2015021092A1 (en) | 2015-02-12 |
| EP3030244A1 (en) | 2016-06-15 |
| US20190062748A1 (en) | 2019-02-28 |
| IL243941B (en) | 2019-06-30 |
| CA2919088A1 (en) | 2015-02-12 |
| TW201601742A (zh) | 2016-01-16 |
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