JP2012509273A5 - - Google Patents
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- JP2012509273A5 JP2012509273A5 JP2011536585A JP2011536585A JP2012509273A5 JP 2012509273 A5 JP2012509273 A5 JP 2012509273A5 JP 2011536585 A JP2011536585 A JP 2011536585A JP 2011536585 A JP2011536585 A JP 2011536585A JP 2012509273 A5 JP2012509273 A5 JP 2012509273A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- nhc
- independently
- compound
- 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.)
- Ceased
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- 125000000217 alkyl group Chemical group 0.000 claims 27
- 239000002105 nanoparticle Substances 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 19
- 108091034117 Oligonucleotide Proteins 0.000 claims 17
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
- 230000000692 anti-sense effect Effects 0.000 claims 9
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 108020004707 nucleic acids Proteins 0.000 claims 8
- 102000039446 nucleic acids Human genes 0.000 claims 8
- 150000007523 nucleic acids Chemical class 0.000 claims 8
- 125000000547 substituted alkyl group Chemical group 0.000 claims 8
- 150000001412 amines Chemical class 0.000 claims 6
- 125000004405 heteroalkoxy group Chemical group 0.000 claims 6
- 150000002632 lipids Chemical class 0.000 claims 6
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 5
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- -1 cationic lipid Chemical class 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 108091023037 Aptamer Proteins 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 108700011259 MicroRNAs Proteins 0.000 claims 2
- 108091093037 Peptide nucleic acid Proteins 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- 108020004459 Small interfering RNA Proteins 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 230000001588 bifunctional effect Effects 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 239000002679 microRNA Substances 0.000 claims 2
- 239000002773 nucleotide Substances 0.000 claims 2
- 125000003729 nucleotide group Chemical group 0.000 claims 2
- 239000004055 small Interfering RNA Substances 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 claims 1
- 102100021663 Baculoviral IAP repeat-containing protein 5 Human genes 0.000 claims 1
- 108060000903 Beta-catenin Proteins 0.000 claims 1
- 102000015735 Beta-catenin Human genes 0.000 claims 1
- 125000006539 C12 alkyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 102000053642 Catalytic RNA Human genes 0.000 claims 1
- 108090000994 Catalytic RNA Proteins 0.000 claims 1
- 108020004414 DNA Proteins 0.000 claims 1
- 108010045100 HSP27 Heat-Shock Proteins Proteins 0.000 claims 1
- 102100039165 Heat shock protein beta-1 Human genes 0.000 claims 1
- 101000971171 Homo sapiens Apoptosis regulator Bcl-2 Proteins 0.000 claims 1
- 101001046870 Homo sapiens Hypoxia-inducible factor 1-alpha Proteins 0.000 claims 1
- 101000605639 Homo sapiens Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Proteins 0.000 claims 1
- 102100022875 Hypoxia-inducible factor 1-alpha Human genes 0.000 claims 1
- 102100038332 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Human genes 0.000 claims 1
- 108091030071 RNAI Proteins 0.000 claims 1
- 108091028664 Ribonucleotide Proteins 0.000 claims 1
- 108091027076 Spiegelmer Proteins 0.000 claims 1
- 108010002687 Survivin Proteins 0.000 claims 1
- 108010088665 Zinc Finger Protein Gli2 Proteins 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 102000001307 androgen receptors Human genes 0.000 claims 1
- 108010080146 androgen receptors Proteins 0.000 claims 1
- 239000000074 antisense oligonucleotide Substances 0.000 claims 1
- 238000012230 antisense oligonucleotides Methods 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 150000001735 carboxylic acids Chemical class 0.000 claims 1
- 125000002091 cationic group Chemical group 0.000 claims 1
- 229940106189 ceramide Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000000799 fusogenic effect Effects 0.000 claims 1
- 230000009368 gene silencing by RNA Effects 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002466 imines Chemical class 0.000 claims 1
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001419 myristoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000007935 neutral effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000002811 oleoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000002336 ribonucleotide Substances 0.000 claims 1
- 125000002652 ribonucleotide group Chemical group 0.000 claims 1
- 108091092562 ribozyme Proteins 0.000 claims 1
- 125000006850 spacer group Chemical group 0.000 claims 1
- 125000003696 stearoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 0 *CC(C(*(CC*=C(C1)[*@]1C1C=CC(C(*(CCCCC(*)*)=C)=O)=CC1)=C)=O)=C Chemical compound *CC(C(*(CC*=C(C1)[*@]1C1C=CC(C(*(CCCCC(*)*)=C)=O)=CC1)=C)=O)=C 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11537808P | 2008-11-17 | 2008-11-17 | |
| US61/115,378 | 2008-11-17 | ||
| PCT/US2009/064730 WO2010057160A1 (en) | 2008-11-17 | 2009-11-17 | Releasable fusogenic lipids for nucleic acids delivery systems |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012509273A JP2012509273A (ja) | 2012-04-19 |
| JP2012509273A5 true JP2012509273A5 (enExample) | 2012-12-27 |
Family
ID=42170408
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536585A Ceased JP2012509273A (ja) | 2008-11-17 | 2009-11-17 | 核酸送達系のための放出可能融合性脂質 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20110223257A1 (enExample) |
| EP (1) | EP2355799A4 (enExample) |
| JP (1) | JP2012509273A (enExample) |
| CN (1) | CN102215820A (enExample) |
| CA (1) | CA2742846A1 (enExample) |
| TW (1) | TW201021852A (enExample) |
| WO (1) | WO2010057160A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL282138B2 (en) | 2005-08-24 | 2024-01-01 | Immunogen Inc | Process for preparing purified drug conjugates |
| JP2012509272A (ja) * | 2008-11-17 | 2012-04-19 | エンゾン ファーマシューティカルズ，インコーポレーテッド | 核酸送達系のための放出性カチオン脂質 |
| US20100233270A1 (en) | 2009-01-08 | 2010-09-16 | Northwestern University | Delivery of Oligonucleotide-Functionalized Nanoparticles |
| RS58810B1 (sr) | 2009-06-03 | 2019-07-31 | Immunogen Inc | Metodi konjugacije |
| SG186085A1 (en) * | 2010-06-03 | 2013-01-30 | Alnylam Pharmaceuticals Inc | Biodegradable lipids for the delivery of active agents |
| DK3372248T3 (da) | 2010-06-22 | 2020-04-06 | Onxeo | Optimeret in vivo leveringssystem med endosomolytiske midler til nukleinsyrekonjugater |
| SMT201900114T1 (it) * | 2011-03-29 | 2019-02-28 | Immunogen Inc | Preparazione di coniugati maytansinoide-anticorpo mediante un processo a fase unica |
| EP2527440A1 (en) | 2011-05-27 | 2012-11-28 | Institut Curie | Cancer treatment by combining DNA molecules mimicking double strand breaks with hyperthermia |
| HK1200089A1 (en) | 2011-12-07 | 2015-07-31 | Alnylam Pharmaceuticals, Inc. | Biodegradable lipids for the delivery of active agents |
| SI2791160T1 (sl) | 2011-12-16 | 2022-07-29 | Modernatx, Inc. | Sestave modificirane MRNA |
| US10358680B2 (en) * | 2012-09-11 | 2019-07-23 | Duke University | Nano-plasmonic molecular probes for plasmonics coupling interference |
| NZ707091A (en) | 2012-10-04 | 2018-12-21 | Immunogen Inc | Use of a pvdf membrane to purify cell-binding agent cytotoxic agent conjugates |
| CN105611914B (zh) | 2013-06-19 | 2020-09-08 | 加利福尼亚大学董事会 | 局部递送治疗剂的化学构造物 |
| EP3076918A4 (en) | 2013-12-03 | 2017-06-07 | Northwestern University | Liposomal particles, methods of making same and uses thereof |
| AU2015229014B2 (en) | 2014-03-14 | 2019-07-25 | The Regents Of The University Of California | TCO conjugates and methods for delivery of therapeutic agents |
| TWI665192B (zh) | 2014-05-28 | 2019-07-11 | 德商拜耳作物科學股份有限公司 | 製備二氫異唑衍生物之方法 |
| CA2953216C (en) | 2014-06-04 | 2020-12-22 | Exicure, Inc. | Multivalent delivery of immune modulators by liposomal spherical nucleic acids for prophylactic or therapeutic applications |
| US12264344B2 (en) | 2014-08-19 | 2025-04-01 | Northwestern University | Protein/oligonucleotide core-shell nanoparticle therapeutics |
| EP3220895B1 (en) | 2014-11-21 | 2022-08-31 | Northwestern University | The sequence-specific cellular uptake of spherical nucleic acid nanoparticle conjugates |
| CN117567535A (zh) | 2015-09-10 | 2024-02-20 | 坦伯公司 | 生物正交组合物 |
| US11364304B2 (en) | 2016-08-25 | 2022-06-21 | Northwestern University | Crosslinked micellar spherical nucleic acids |
| CN107951861B (zh) * | 2016-10-17 | 2020-12-01 | 南京绿叶制药有限公司 | 一种脂质纳米粒膜材料组合物 |
| CN107951862B (zh) * | 2016-10-17 | 2021-03-12 | 南京绿叶制药有限公司 | 一种抑制bcl-2的反义寡聚核酸的脂质纳米粒及其制备方法 |
| US10383952B2 (en) | 2016-12-21 | 2019-08-20 | Arcturus Therapeutics, Inc. | Ionizable cationic lipid for RNA delivery |
| WO2018187740A1 (en) | 2017-04-07 | 2018-10-11 | Shasqi, Inc. | Bioorthogonal compositions |
| WO2018209270A1 (en) | 2017-05-11 | 2018-11-15 | Northwestern University | Adoptive cell therapy using spherical nucleic acids (snas) |
| KR20200028997A (ko) | 2017-07-13 | 2020-03-17 | 노오쓰웨스턴 유니버시티 | 올리고뉴클레오타이드-작용화된 금속-유기 프레임워크 나노입자를 제조하는 일반적이고 직접적인 방법 |
| CN111386105B (zh) * | 2017-11-06 | 2023-09-15 | 日东电工株式会社 | 用于递送生物活性分子的膜融合化合物 |
| US12319711B2 (en) | 2019-09-20 | 2025-06-03 | Northwestern University | Spherical nucleic acids with tailored and active protein coronae |
| US12378560B2 (en) | 2019-10-29 | 2025-08-05 | Northwestern University | Sequence multiplicity within spherical nucleic acids |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5945408A (en) * | 1996-03-06 | 1999-08-31 | G.D. Searle & Co. | Hydroxyanidino derivatives useful as nitric oxide synthase inhibitors |
| CA2289702C (en) * | 1997-05-14 | 2008-02-19 | Inex Pharmaceuticals Corp. | High efficiency encapsulation of charged therapeutic agents in lipid vesicles |
| US6794499B2 (en) * | 1997-09-12 | 2004-09-21 | Exiqon A/S | Oligonucleotide analogues |
| US6841537B1 (en) * | 1998-04-22 | 2005-01-11 | Protiva Biotherapeutics Inc. | Combination therapy using nucleic acids and conventional drugs |
| US6169078B1 (en) * | 1998-05-12 | 2001-01-02 | University Of Florida | Materials and methods for the intracellular delivery of substances |
| US20030077829A1 (en) * | 2001-04-30 | 2003-04-24 | Protiva Biotherapeutics Inc.. | Lipid-based formulations |
| US20070042983A1 (en) * | 2001-05-18 | 2007-02-22 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of gene expression using short interfering nucleic acid (siNA) |
| US20050222064A1 (en) * | 2002-02-20 | 2005-10-06 | Sirna Therapeutics, Inc. | Polycationic compositions for cellular delivery of polynucleotides |
| US7015349B2 (en) * | 2003-03-26 | 2006-03-21 | The Gillette Company | Reduction of hair growth |
| AU2004272646B2 (en) * | 2003-09-15 | 2011-11-24 | Arbutus Biopharma Corporation | Polyethyleneglycol-modified lipid compounds and uses thereof |
| EP1692107A4 (en) * | 2003-12-10 | 2008-10-29 | Nitromed Inc | NITROGEN OXIDE-RELATED PYRUVATE COMPOUNDS, COMPOSITIONS AND USE METHOD |
| WO2006007712A1 (en) * | 2004-07-19 | 2006-01-26 | Protiva Biotherapeutics, Inc. | Methods comprising polyethylene glycol-lipid conjugates for delivery of therapeutic agents |
| JP2008530021A (ja) * | 2005-02-08 | 2008-08-07 | アイディー バイオメディカル コーポレイション オブ ケベック シー．オー．ビー． アズ グラクソスミスクライン バイオロジカルズ ノース アメリカ | 医薬組成物 |
| CA2597724A1 (en) * | 2005-02-14 | 2007-08-02 | Sirna Therapeutics, Inc. | Cationic lipids and formulated molecular compositions containing them |
| US7404969B2 (en) * | 2005-02-14 | 2008-07-29 | Sirna Therapeutics, Inc. | Lipid nanoparticle based compositions and methods for the delivery of biologically active molecules |
| CA2600113A1 (en) * | 2005-03-07 | 2006-09-14 | Id Biomedical Corporation Of Quebec C.O.B. As Glaxosmithkline Biological S North America | Pharmaceutical liposomal compositions |
| WO2007090194A2 (en) * | 2006-02-01 | 2007-08-09 | The Burnham Institute For Medical Research | Lymphatic zip codes in tumors and pre-malignant lesions |
| US20070293449A1 (en) * | 2006-06-20 | 2007-12-20 | Nastech Pharmaceutical Company Inc. | Compositions and methods for delivery of double-stranded rna |
| WO2008022309A2 (en) * | 2006-08-18 | 2008-02-21 | F. Hoffmann-La Roche Ag | Polyconjugates for in vivo delivery of polynucleotides |
| US20080255234A1 (en) * | 2007-04-11 | 2008-10-16 | Zinpro Corporation | Rumen protected lysine |
| CA2686735A1 (en) * | 2007-05-04 | 2008-11-13 | Mdrna, Inc. | Amino acid lipids and uses thereof |
-
2009
- 2009-11-17 EP EP09826954A patent/EP2355799A4/en not_active Withdrawn
- 2009-11-17 US US13/129,546 patent/US20110223257A1/en not_active Abandoned
- 2009-11-17 TW TW098138943A patent/TW201021852A/zh unknown
- 2009-11-17 CN CN2009801459159A patent/CN102215820A/zh active Pending
- 2009-11-17 CA CA2742846A patent/CA2742846A1/en not_active Abandoned
- 2009-11-17 WO PCT/US2009/064730 patent/WO2010057160A1/en not_active Ceased
- 2009-11-17 JP JP2011536585A patent/JP2012509273A/ja not_active Ceased
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