JP2012509366A5 - - Google Patents
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- JP2012509366A5 JP2012509366A5 JP2011536581A JP2011536581A JP2012509366A5 JP 2012509366 A5 JP2012509366 A5 JP 2012509366A5 JP 2011536581 A JP2011536581 A JP 2011536581A JP 2011536581 A JP2011536581 A JP 2011536581A JP 2012509366 A5 JP2012509366 A5 JP 2012509366A5
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- JP
- Japan
- Prior art keywords
- substituted
- nhc
- alkyl
- compound
- group
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 28
- 125000000217 alkyl group Chemical group 0.000 claims 27
- 239000002105 nanoparticle Substances 0.000 claims 23
- 239000000203 mixture Substances 0.000 claims 17
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 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 14
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- -1 aryl mercapto Chemical class 0.000 claims 11
- 125000000547 substituted alkyl group Chemical group 0.000 claims 11
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 11
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000004405 heteroalkoxy group Chemical group 0.000 claims 8
- 125000001072 heteroaryl 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
- 125000003107 substituted aryl group Chemical group 0.000 claims 8
- 235000012000 cholesterol Nutrition 0.000 claims 7
- 150000001412 amines 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
- 108091034117 Oligonucleotide Proteins 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000002887 hydroxy group Chemical class [H]O* 0.000 claims 5
- 150000002632 lipids Chemical class 0.000 claims 5
- 125000004423 acyloxy group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 4
- 125000005199 aryl carbonyloxy group Chemical group 0.000 claims 4
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 4
- 125000001589 carboacyl group Chemical group 0.000 claims 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims 4
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 4
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 230000000799 fusogenic effect Effects 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 108091023037 Aptamer Proteins 0.000 claims 2
- 108700011259 MicroRNAs Proteins 0.000 claims 2
- 108091093037 Peptide nucleic acid Proteins 0.000 claims 2
- 108020004459 Small interfering RNA Proteins 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 230000000890 antigenic effect Effects 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 230000001588 bifunctional effect Effects 0.000 claims 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 229920001427 mPEG Polymers 0.000 claims 2
- 239000002679 microRNA Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 239000004055 small Interfering RNA Substances 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 claims 1
- 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
- YDNKGFDKKRUKPY-JHOUSYSJSA-N C16 ceramide Natural products CCCCCCCCCCCCCCCC(=O)N[C@@H](CO)[C@H](O)C=CCCCCCCCCCCCCC YDNKGFDKKRUKPY-JHOUSYSJSA-N 0.000 claims 1
- 102000053642 Catalytic RNA Human genes 0.000 claims 1
- 108090000994 Catalytic RNA Proteins 0.000 claims 1
- CRJGESKKUOMBCT-VQTJNVASSA-N N-acetylsphinganine Chemical compound CCCCCCCCCCCCCCC[C@@H](O)[C@H](CO)NC(C)=O CRJGESKKUOMBCT-VQTJNVASSA-N 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
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 1
- 125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 125000003178 carboxy group Chemical class [H]OC(*)=O 0.000 claims 1
- 229940106189 ceramide Drugs 0.000 claims 1
- ZVEQCJWYRWKARO-UHFFFAOYSA-N ceramide Natural products CCCCCCCCCCCCCCC(O)C(=O)NC(CO)C(O)C=CCCC=C(C)CCCCCCCCC ZVEQCJWYRWKARO-UHFFFAOYSA-N 0.000 claims 1
- 125000004093 cyano group Chemical class *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 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
- 230000009368 gene silencing by RNA Effects 0.000 claims 1
- 125000005843 halogen group Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000002466 imines Chemical class 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- VVGIYYKRAMHVLU-UHFFFAOYSA-N newbouldiamide Natural products CCCCCCCCCCCCCCCCCCCC(O)C(O)C(O)C(CO)NC(=O)CCCCCCCCCCCCCCCCC VVGIYYKRAMHVLU-UHFFFAOYSA-N 0.000 claims 1
- KITHNHJPIHPBQH-UHFFFAOYSA-N nitro(nitrosilyloxy)silane Chemical class [N+](=O)([O-])[SiH2]O[SiH2][N+](=O)[O-] KITHNHJPIHPBQH-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
- 125000003729 nucleotide group Chemical group 0.000 claims 1
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 238000006116 polymerization reaction Methods 0.000 claims 1
- 230000035755 proliferation Effects 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
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims 1
- 125000000472 sulfonyl group Chemical class *S(*)(=O)=O 0.000 claims 1
- 230000008685 targeting Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11537908P | 2008-11-17 | 2008-11-17 | |
| US11537108P | 2008-11-17 | 2008-11-17 | |
| US61/115,371 | 2008-11-17 | ||
| US61/115,379 | 2008-11-17 | ||
| PCT/US2009/064701 WO2010057150A1 (en) | 2008-11-17 | 2009-11-17 | Releasable polymeric lipids for nucleic acids delivery systems |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012509366A JP2012509366A (ja) | 2012-04-19 |
| JP2012509366A5 true JP2012509366A5 (enExample) | 2013-01-10 |
Family
ID=42170403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011536581A Withdrawn JP2012509366A (ja) | 2008-11-17 | 2009-11-17 | 核酸送達系のための放出可能ポリマー脂質 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20110305770A1 (enExample) |
| EP (1) | EP2362728A1 (enExample) |
| JP (1) | JP2012509366A (enExample) |
| CN (1) | CN102231950A (enExample) |
| CA (1) | CA2742838A1 (enExample) |
| TW (1) | TW201023914A (enExample) |
| WO (1) | WO2010057150A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8450290B2 (en) * | 2007-11-26 | 2013-05-28 | Enzon Pharmaceuticals, Inc. | Methods for treating androgen receptor dependent disorders including cancers |
| JP2012509258A (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分岐カチオン性脂質 |
| CA2843503C (en) * | 2011-08-12 | 2020-12-22 | Ulrich Hersel | Polymeric hyperbranched carrier-linked prodrugs |
| EP2581448B1 (en) * | 2011-10-13 | 2015-01-28 | Association Institut de Myologie | Tricyclo-phosphorothioate DNA |
| US9061063B2 (en) | 2011-12-07 | 2015-06-23 | Alnylam Pharmaceuticals, Inc. | Biodegradable lipids for the delivery of active agents |
| HUE060907T2 (hu) * | 2014-06-25 | 2023-04-28 | Acuitas Therapeutics Inc | Új lipidek és lipid nanorészecske formulációk nukleinsavak bevitelére |
| CA2984125A1 (en) | 2015-04-27 | 2016-11-03 | The Trustees Of The University Of Pennsylvania | Nucleoside-modified rna for inducing an adaptive immune response |
| US10221127B2 (en) | 2015-06-29 | 2019-03-05 | Acuitas Therapeutics, Inc. | Lipids and lipid nanoparticle formulations for delivery of nucleic acids |
| US10940201B2 (en) | 2015-09-30 | 2021-03-09 | Shionogi & Co., Ltd. | Nucleic acid derivative having immunostimulatory activity |
| MX374553B (es) * | 2015-09-30 | 2025-03-06 | Shionogi & Co | Derivado de ácido nucleico que tiene actividad inmunoestimuladora. |
| EP3357514B1 (en) | 2015-09-30 | 2021-04-14 | NOF Corporation | Lipid derivative in which hydrophilic polymer is bound via cyclic benzylidene acetal linkers |
| IL307179A (en) | 2015-10-28 | 2023-11-01 | Acuitas Therapeutics Inc | Novel lipids and lipid nanoparticle formulations for delivery of nucleic acids |
| US12491261B2 (en) | 2016-10-26 | 2025-12-09 | Acuitas Therapeutics, Inc. | Lipid nanoparticle formulations |
| JP7317715B2 (ja) | 2017-01-11 | 2023-07-31 | ザ・トラステイーズ・オブ・ザ・ユニバーシテイ・オブ・ペンシルベニア | ジカウイルスに対する免疫応答を誘導するためのヌクレオシド改変ｒｎａ |
| US11357856B2 (en) | 2017-04-13 | 2022-06-14 | Acuitas Therapeutics, Inc. | Lipids for delivery of active agents |
| CN116693411A (zh) | 2017-04-28 | 2023-09-05 | 爱康泰生治疗公司 | 用于递送核酸的新型羰基脂质和脂质纳米颗粒制剂 |
| US11639329B2 (en) | 2017-08-16 | 2023-05-02 | Acuitas Therapeutics, Inc. | Lipids for use in lipid nanoparticle formulations |
| US11524932B2 (en) | 2017-08-17 | 2022-12-13 | Acuitas Therapeutics, Inc. | Lipids for use in lipid nanoparticle formulations |
| WO2019036028A1 (en) | 2017-08-17 | 2019-02-21 | Acuitas Therapeutics, Inc. | LIPIDS FOR USE IN LIPID NANOPARTICULAR FORMULATIONS |
| US12065396B2 (en) | 2017-08-17 | 2024-08-20 | Acuitas Therapeutics, Inc. | Lipids for use in lipid nanoparticle formulations |
| US12329857B2 (en) | 2018-09-21 | 2025-06-17 | Acuitas Therapeutics, Inc. | Systems and methods for manufacturing lipid nanoparticles and liposomes |
| US11141491B2 (en) * | 2018-10-15 | 2021-10-12 | National Yang Ming Chiao Tung University | PH-sensitive lipid nanoparticles for encapsulation of anticancer drugs and microRNA and use thereof |
| CN109251150B (zh) * | 2018-11-02 | 2021-07-30 | 宁夏医科大学 | 一种2，3-二氨基丙酸甲酯的制备方法 |
| AU2020205717B2 (en) | 2019-01-11 | 2025-09-11 | Acuitas Therapeutics, Inc. | Lipids for lipid nanoparticle delivery of active agents |
| AU2021308681A1 (en) | 2020-07-16 | 2023-03-09 | Acuitas Therapeutics, Inc. | Cationic lipids for use in lipid nanoparticles |
| KR102433981B1 (ko) * | 2020-12-15 | 2022-08-19 | 대구가톨릭대학교산학협력단 | HIF-1α 및 STAT5 전사인자를 억제하는 합성 디코이 올리고핵산 및 이를 유효성분으로 함유하는 아토피 피부염의 예방 또는 치료용 약학적 조성물 |
| CN114904003B (zh) * | 2021-02-09 | 2023-09-29 | 广州立得生物医药科技有限公司 | 可电离的阳离子脂质类似物材料在作为核酸药物递送载体或转染试剂中的应用 |
| AU2022281746B2 (en) | 2021-05-24 | 2025-01-16 | Suzhou Abogen Biosciences Co., Ltd. | Lipid compounds and lipid nanoparticle compositions |
| WO2023056282A1 (en) * | 2021-09-28 | 2023-04-06 | The Trustees Of The University Of Pennsylvania | Compositions and methods for t cell targeted delivery of therapeutic agents |
| WO2023056418A1 (en) * | 2021-10-01 | 2023-04-06 | The Trustees Of The University Of Pennsylvania | Lipid nanoparticle (lnp) compositions and methods of use thereof |
| US20250127719A1 (en) * | 2021-12-07 | 2025-04-24 | The Trustees Of The University Of Pennsylvania | Anisamide-containing lipids and compositions and methods of use thereof |
| KR20240123832A (ko) | 2021-12-16 | 2024-08-14 | 아퀴타스 테라퓨틱스 인크. | 지질 나노입자 제형에 사용하기 위한 지질 |
| CN116549659B (zh) * | 2022-01-27 | 2025-11-21 | 中山大学 | 阳离子脂质类似物在基因编辑核糖核蛋白复合物胞内递送中的应用 |
| CN114699997B (zh) * | 2022-03-28 | 2022-11-25 | 山东大学 | 一种具有高抗盐性的碱基@囊泡复合体及其制备方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010503708A (ja) * | 2006-09-15 | 2010-02-04 | エンゾン ファーマスーティカルズ インコーポレイテッド | 多官能性リンカーを含む標的化ポリマープロドラッグ |
| NZ580707A (en) * | 2007-05-04 | 2011-11-25 | Marina Biotech Inc | Acylated cationic amino acids and uses thereof |
-
2009
- 2009-11-17 JP JP2011536581A patent/JP2012509366A/ja not_active Withdrawn
- 2009-11-17 CN CN2009801458902A patent/CN102231950A/zh active Pending
- 2009-11-17 TW TW098138947A patent/TW201023914A/zh unknown
- 2009-11-17 CA CA2742838A patent/CA2742838A1/en not_active Abandoned
- 2009-11-17 US US13/129,628 patent/US20110305770A1/en not_active Abandoned
- 2009-11-17 WO PCT/US2009/064701 patent/WO2010057150A1/en not_active Ceased
- 2009-11-17 EP EP09826946A patent/EP2362728A1/en not_active Withdrawn
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