JP2010532786A5 - - Google Patents
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- JP2010532786A5 JP2010532786A5 JP2010516035A JP2010516035A JP2010532786A5 JP 2010532786 A5 JP2010532786 A5 JP 2010532786A5 JP 2010516035 A JP2010516035 A JP 2010516035A JP 2010516035 A JP2010516035 A JP 2010516035A JP 2010532786 A5 JP2010532786 A5 JP 2010532786A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical formulation
- here
- hydrophilic
- acid
- irna
- 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.)
- Pending
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- 239000008194 pharmaceutical composition Substances 0.000 claims 19
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 230000002209 hydrophobic effect Effects 0.000 claims 5
- 239000000693 micelle Substances 0.000 claims 4
- WWZKQHOCKIZLMA-UHFFFAOYSA-N Caprylic acid Natural products CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims 3
- 229930186217 Glycolipid Natural products 0.000 claims 3
- 230000015556 catabolic process Effects 0.000 claims 3
- 238000006731 degradation reaction Methods 0.000 claims 3
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 150000003904 phospholipids Chemical class 0.000 claims 3
- PORPENFLTBBHSG-MGBGTMOVSA-N 1,2-dihexadecanoyl-sn-glycerol-3-phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=O)OC(=O)CCCCCCCCCCCCCCC PORPENFLTBBHSG-MGBGTMOVSA-N 0.000 claims 2
- TZCPCKNHXULUIY-RGULYWFUSA-N 1,2-distearoyl-sn-glycero-3-phosphoserine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCCCCCCCCCCCC TZCPCKNHXULUIY-RGULYWFUSA-N 0.000 claims 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 2
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 claims 2
- ZWZWYGMENQVNFU-UHFFFAOYSA-N Glycerophosphorylserin Natural products OC(=O)C(N)COP(O)(=O)OCC(O)CO ZWZWYGMENQVNFU-UHFFFAOYSA-N 0.000 claims 2
- 101710163270 Nuclease Proteins 0.000 claims 2
- ATBOMIWRCZXYSZ-XZBBILGWSA-N [1-[2,3-dihydroxypropoxy(hydroxy)phosphoryl]oxy-3-hexadecanoyloxypropan-2-yl] (9e,12e)-octadeca-9,12-dienoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCC(O)CO)OC(=O)CCCCCCC\C=C\C\C=C\CCCCC ATBOMIWRCZXYSZ-XZBBILGWSA-N 0.000 claims 2
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- UKMSUNONTOPOIO-UHFFFAOYSA-N docosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCC(O)=O UKMSUNONTOPOIO-UHFFFAOYSA-N 0.000 claims 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims 2
- VKOBVWXKNCXXDE-UHFFFAOYSA-N icosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCC(O)=O VKOBVWXKNCXXDE-UHFFFAOYSA-N 0.000 claims 2
- 230000003834 intracellular effect Effects 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 150000004668 long chain fatty acids Chemical class 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 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 2
- 150000008104 phosphatidylethanolamines Chemical class 0.000 claims 2
- 150000003905 phosphatidylinositols Chemical class 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- JSPNNZKWADNWHI-PNANGNLXSA-N (2r)-2-hydroxy-n-[(2s,3r,4e,8e)-3-hydroxy-9-methyl-1-[(2r,3r,4s,5s,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoctadeca-4,8-dien-2-yl]heptadecanamide Chemical compound CCCCCCCCCCCCCCC[C@@H](O)C(=O)N[C@H]([C@H](O)\C=C\CC\C=C(/C)CCCCCCCCC)CO[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O JSPNNZKWADNWHI-PNANGNLXSA-N 0.000 claims 1
- GYSCBCSGKXNZRH-UHFFFAOYSA-N 1-benzothiophene-2-carboxamide Chemical compound C1=CC=C2SC(C(=O)N)=CC2=C1 GYSCBCSGKXNZRH-UHFFFAOYSA-N 0.000 claims 1
- HVCOBJNICQPDBP-UHFFFAOYSA-N 3-[3-[3,5-dihydroxy-6-methyl-4-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-2-yl]oxydecanoyloxy]decanoic acid;hydrate Chemical compound O.OC1C(OC(CC(=O)OC(CCCCCCC)CC(O)=O)CCCCCCC)OC(C)C(O)C1OC1C(O)C(O)C(O)C(C)O1 HVCOBJNICQPDBP-UHFFFAOYSA-N 0.000 claims 1
- 235000021357 Behenic acid Nutrition 0.000 claims 1
- 229920001661 Chitosan Polymers 0.000 claims 1
- GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Natural products CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims 1
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims 1
- 235000021353 Lignoceric acid Nutrition 0.000 claims 1
- CQXMAMUUWHYSIY-UHFFFAOYSA-N Lignoceric acid Natural products CCCCCCCCCCCCCCCCCCCCCCCC(=O)OCCC1=CC=C(O)C=C1 CQXMAMUUWHYSIY-UHFFFAOYSA-N 0.000 claims 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N Myristic acid Natural products CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 claims 1
- 235000021314 Palmitic acid Nutrition 0.000 claims 1
- 229920002873 Polyethylenimine Polymers 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- OBETXYAYXDNJHR-UHFFFAOYSA-N alpha-ethylcaproic acid Natural products CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 claims 1
- 229940116226 behenic acid Drugs 0.000 claims 1
- GONOPSZTUGRENK-UHFFFAOYSA-N benzyl(trichloro)silane Chemical compound Cl[Si](Cl)(Cl)CC1=CC=CC=C1 GONOPSZTUGRENK-UHFFFAOYSA-N 0.000 claims 1
- 229930183167 cerebroside Natural products 0.000 claims 1
- RIZIAUKTHDLMQX-UHFFFAOYSA-N cerebroside D Natural products CCCCCCCCCCCCCCCCC(O)C(=O)NC(C(O)C=CCCC=C(C)CCCCCCCCC)COC1OC(CO)C(O)C(O)C1O RIZIAUKTHDLMQX-UHFFFAOYSA-N 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- KFEVDPWXEVUUMW-UHFFFAOYSA-N docosanoic acid Natural products CCCCCCCCCCCCCCCCCCCCCC(=O)OCCC1=CC=C(O)C=C1 KFEVDPWXEVUUMW-UHFFFAOYSA-N 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 150000002270 gangliosides Chemical class 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N n-hexanoic acid Natural products CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229920000765 poly(2-oxazolines) Polymers 0.000 claims 1
- 229920002401 polyacrylamide Polymers 0.000 claims 1
- 229920001601 polyetherimide Polymers 0.000 claims 1
- -1 polymorpholine Polymers 0.000 claims 1
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 150000005843 sulfated lipids Chemical class 0.000 claims 1
- QZZGJDVWLFXDLK-UHFFFAOYSA-N tetracosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCCCCCC(O)=O QZZGJDVWLFXDLK-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94843307P | 2007-07-06 | 2007-07-06 | |
| PCT/US2008/008326 WO2009009025A1 (en) | 2007-07-06 | 2008-07-07 | Mixed micelles including amphipathic conjugates of rna agents, and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010532786A JP2010532786A (ja) | 2010-10-14 |
| JP2010532786A5 true JP2010532786A5 (enExample) | 2011-08-25 |
Family
ID=40228904
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010516035A Pending JP2010532786A (ja) | 2007-07-06 | 2008-07-07 | Ｒｎａ薬剤の両親媒性接合を含む混合ミセルおよびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20110008395A1 (enExample) |
| EP (1) | EP2171095A4 (enExample) |
| JP (1) | JP2010532786A (enExample) |
| KR (1) | KR20100037120A (enExample) |
| CA (1) | CA2692748A1 (enExample) |
| WO (1) | WO2009009025A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3065577C (en) | 2008-05-13 | 2022-05-31 | Phaserx, Inc. | Diblock copolymers and polynucleotide complexes thereof for delivery into cells |
| US9006193B2 (en) | 2008-05-13 | 2015-04-14 | University Of Washington | Polymeric carrier |
| BRPI0911989A2 (pt) | 2008-05-13 | 2015-10-20 | Phaserx Inc | uniões micélicas |
| JP2012500793A (ja) | 2008-08-22 | 2012-01-12 | ユニヴァーシティ オブ ワシントン | 細胞内デリバリーのための異種性ポリマーミセル |
| JP2012507581A (ja) | 2008-11-06 | 2012-03-29 | ユニヴァーシティ オブ ワシントン | 二重特異性細胞内送達媒体 |
| BRPI0921357A2 (pt) | 2008-11-06 | 2016-06-21 | Phaserx Inc | copolímeros em multibloco |
| EP2373715A4 (en) | 2008-12-08 | 2014-12-03 | Univ Washington | OMEGA FUNCTIONALIZED POLYMERS, TRANSITIONALIZED BLOCK COPOLYMERS, POLYMER BIOKON JUGATES, AND RADICAL CHAIN EXTENSION POLICY RESPONSE |
| GB0910723D0 (en) * | 2009-06-22 | 2009-08-05 | Sylentis Sau | Novel drugs for inhibition of gene expression |
| US9238811B2 (en) * | 2009-07-14 | 2016-01-19 | Northeastern University | siRNA phospholipid conjugate |
| WO2011062965A2 (en) | 2009-11-18 | 2011-05-26 | University Of Washington Through Its Center For Commercialization | Targeting monomers and polymers having targeting blocks |
| DK2591792T3 (en) * | 2010-07-09 | 2017-04-03 | Univ Tokyo | COMPOSITION FOR NUCLEIC ACID RELEASE, CARRIER COMPOSITION, PHARMACEUTICAL COMPOSITION WITH COMPOSITION FOR NUCLEIC ACID RELEASE OR CARRIER COMPOSITION AND PROCEDURE FOR NUCLEAR PROCESS |
| JP6190132B2 (ja) * | 2013-03-21 | 2017-08-30 | 学校法人近畿大学 | 遺伝子試料導入用基板及び遺伝子試料導入方法 |
| CA3160394C (en) | 2013-07-30 | 2023-11-07 | Genevant Sciences Gmbh | Block copolymers and their conjugates or complexes with oligonucleotides |
| CN114642735A (zh) | 2015-01-21 | 2022-06-21 | 菲泽尔克斯公司 | 用于将治疗剂和诊断剂递送到细胞中的方法、组合物和系统 |
| EP3503730B1 (en) | 2016-08-23 | 2023-09-27 | Dicerna Pharmaceuticals, Inc. | Compositions comprising reversibly modified oligonucleotides and uses thereof |
| WO2018126084A1 (en) | 2016-12-30 | 2018-07-05 | Phaserx, Inc. | Branched peg molecules and related compositions and methods |
| TW202016301A (zh) | 2018-05-07 | 2020-05-01 | 美商阿里拉姆製藥股份有限公司 | 肝外遞送技術 |
| WO2021054927A2 (en) * | 2018-08-10 | 2021-03-25 | South Dakota Board Of Regents | Glutathione-cholesterol derivatives as brain targeting agents |
| US11753591B2 (en) | 2021-03-08 | 2023-09-12 | Extiel AP, LLC | Device for pyrolysis of carbonaceous materials and method |
| CN113633613B (zh) * | 2021-07-20 | 2023-04-25 | 河南大学 | 一种siRNA胶束、制备方法、组合物及其应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH11504926A (ja) * | 1995-05-04 | 1999-05-11 | ネクスター ファーマスーティカルズ，インコーポレイテッド | 核酸リガンド複合体 |
| WO2001041738A2 (en) * | 1999-12-10 | 2001-06-14 | Celator Technologies Inc. | Lipid carrier compositions with protected surface reactive functions |
| US8202979B2 (en) * | 2002-02-20 | 2012-06-19 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid |
| WO2005041859A2 (en) * | 2003-04-30 | 2005-05-12 | Sirna Therapeutics, Inc. | Conjugates and compositions for cellular delivery. |
| WO2004090108A2 (en) * | 2003-04-03 | 2004-10-21 | Alnylam Pharmaceuticals | Irna conjugates |
| DK1620544T3 (en) * | 2003-04-17 | 2019-01-14 | Alnylam Pharmaceuticals Inc | MODIFIED iRNA AGENTS |
-
2008
- 2008-07-07 WO PCT/US2008/008326 patent/WO2009009025A1/en not_active Ceased
- 2008-07-07 JP JP2010516035A patent/JP2010532786A/ja active Pending
- 2008-07-07 EP EP08826166A patent/EP2171095A4/en not_active Withdrawn
- 2008-07-07 KR KR1020107001933A patent/KR20100037120A/ko not_active Withdrawn
- 2008-07-07 CA CA 2692748 patent/CA2692748A1/en not_active Abandoned
- 2008-07-07 US US12/667,713 patent/US20110008395A1/en not_active Abandoned
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