JP2016537027A5 - - Google Patents
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- JP2016537027A5 JP2016537027A5 JP2016553242A JP2016553242A JP2016537027A5 JP 2016537027 A5 JP2016537027 A5 JP 2016537027A5 JP 2016553242 A JP2016553242 A JP 2016553242A JP 2016553242 A JP2016553242 A JP 2016553242A JP 2016537027 A5 JP2016537027 A5 JP 2016537027A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- group
- alkylene
- alkyl
- heteroatoms selected
- 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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- 229910052717 sulfur Inorganic materials 0.000 claims 56
- 125000005842 heteroatom Chemical group 0.000 claims 51
- 229910052760 oxygen Inorganic materials 0.000 claims 48
- 239000002157 polynucleotide Substances 0.000 claims 45
- 102000040430 polynucleotide Human genes 0.000 claims 45
- 108091033319 polynucleotide Proteins 0.000 claims 45
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 21
- 125000002993 cycloalkylene group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 19
- 125000000732 arylene group Chemical group 0.000 claims 17
- 125000005724 cycloalkenylene group Chemical group 0.000 claims 17
- 125000005549 heteroarylene group Chemical group 0.000 claims 17
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 17
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 229920000642 polymer Polymers 0.000 claims 12
- 229920001184 polypeptide Polymers 0.000 claims 12
- 102000004196 processed proteins & peptides Human genes 0.000 claims 12
- 108090000765 processed proteins & peptides Proteins 0.000 claims 12
- 235000014633 carbohydrates Nutrition 0.000 claims 11
- 150000001720 carbohydrates Chemical class 0.000 claims 11
- 239000003814 drug Substances 0.000 claims 11
- 230000007935 neutral effect Effects 0.000 claims 11
- 230000008685 targeting Effects 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 229920000620 organic polymer Polymers 0.000 claims 10
- 229940124597 therapeutic agent Drugs 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 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 8
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 7
- 210000001163 endosome Anatomy 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 6
- 229960002685 biotin Drugs 0.000 claims 6
- 235000020958 biotin Nutrition 0.000 claims 6
- 239000011616 biotin Substances 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 239000001177 diphosphate Substances 0.000 claims 6
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims 6
- 235000011180 diphosphates Nutrition 0.000 claims 6
- 150000004712 monophosphates Chemical class 0.000 claims 6
- 125000003729 nucleotide group Chemical group 0.000 claims 6
- 125000004434 sulfur atom Chemical group 0.000 claims 6
- 239000001226 triphosphate Substances 0.000 claims 6
- 235000011178 triphosphate Nutrition 0.000 claims 6
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 claims 6
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 239000002773 nucleotide Substances 0.000 claims 5
- SHIBSTMRCDJXLN-UHFFFAOYSA-N Digoxigenin Natural products C1CC(C2C(C3(C)CCC(O)CC3CC2)CC2O)(O)C2(C)C1C1=CC(=O)OC1 SHIBSTMRCDJXLN-UHFFFAOYSA-N 0.000 claims 4
- RYYWUUFWQRZTIU-UHFFFAOYSA-N Thiophosphoric acid Chemical compound OP(O)(S)=O RYYWUUFWQRZTIU-UHFFFAOYSA-N 0.000 claims 4
- YDHWWBZFRZWVHO-UHFFFAOYSA-H [oxido-[oxido(phosphonatooxy)phosphoryl]oxyphosphoryl] phosphate Chemical compound [O-]P([O-])(=O)OP([O-])(=O)OP([O-])(=O)OP([O-])([O-])=O YDHWWBZFRZWVHO-UHFFFAOYSA-H 0.000 claims 4
- QTPILKSJIOLICA-UHFFFAOYSA-N bis[hydroxy(phosphonooxy)phosphoryl] hydrogen phosphate Chemical compound OP(O)(=O)OP(O)(=O)OP(O)(=O)OP(O)(=O)OP(O)(O)=O QTPILKSJIOLICA-UHFFFAOYSA-N 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 235000012000 cholesterol Nutrition 0.000 claims 4
- 230000000295 complement effect Effects 0.000 claims 4
- QONQRTHLHBTMGP-UHFFFAOYSA-N digitoxigenin Natural products CC12CCC(C3(CCC(O)CC3CC3)C)C3C11OC1CC2C1=CC(=O)OC1 QONQRTHLHBTMGP-UHFFFAOYSA-N 0.000 claims 4
- SHIBSTMRCDJXLN-KCZCNTNESA-N digoxigenin Chemical compound C1([C@@H]2[C@@]3([C@@](CC2)(O)[C@H]2[C@@H]([C@@]4(C)CC[C@H](O)C[C@H]4CC2)C[C@H]3O)C)=CC(=O)OC1 SHIBSTMRCDJXLN-KCZCNTNESA-N 0.000 claims 4
- 125000002228 disulfide group Chemical group 0.000 claims 4
- 125000000524 functional group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims 3
- 125000004450 alkenylene group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 150000003384 small molecules Chemical class 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 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
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 2
- 239000000178 monomer Substances 0.000 claims 2
- MWWATHDPGQKSAR-UHFFFAOYSA-N propyne Chemical group CC#C MWWATHDPGQKSAR-UHFFFAOYSA-N 0.000 claims 2
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 2
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 1
- -1 5 ′ Cap Chemical compound 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 238000009396 hybridization Methods 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 1
- 235000021317 phosphate Nutrition 0.000 claims 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 1
- 125000004437 phosphorous atom Chemical group 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000005309 thioalkoxy group Chemical group 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361900685P | 2013-11-06 | 2013-11-06 | |
| US61/900,685 | 2013-11-06 | ||
| US201461975686P | 2014-04-04 | 2014-04-04 | |
| US61/975,686 | 2014-04-04 | ||
| US201462008906P | 2014-06-06 | 2014-06-06 | |
| US62/008,906 | 2014-06-06 | ||
| PCT/US2014/064401 WO2015069932A1 (en) | 2013-11-06 | 2014-11-06 | Polynucleotide constructs having disulfide groups |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016537027A JP2016537027A (ja) | 2016-12-01 |
| JP2016537027A5 true JP2016537027A5 (https=) | 2017-12-14 |
Family
ID=53042090
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016553242A Pending JP2016537027A (ja) | 2013-11-06 | 2014-11-06 | ジスルフィド基を有するポリヌクレオチド構築物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20160257961A1 (https=) |
| EP (1) | EP3066105A4 (https=) |
| JP (1) | JP2016537027A (https=) |
| CN (1) | CN106061981A (https=) |
| AU (1) | AU2014346658A1 (https=) |
| CA (1) | CA2929651A1 (https=) |
| WO (1) | WO2015069932A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3079668A1 (en) | 2013-12-09 | 2016-10-19 | Durect Corporation | Pharmaceutically active agent complexes, polymer complexes, and compositions and methods involving the same |
| CA2950960A1 (en) * | 2014-06-06 | 2015-12-10 | Solstice Biologics, Ltd. | Polynucleotide constructs having bioreversible and non-bioreversible groups |
| US20180133327A1 (en) * | 2015-03-16 | 2018-05-17 | Amal Therapeutics Sa | Cell Penetrating Peptides and Complexes Comprising the Same |
| CN105175546A (zh) * | 2015-05-27 | 2015-12-23 | 连祺周 | 人血管内皮生长因子与表皮生长因子样结构域7的融合蛋白 |
| JPWO2016208773A1 (ja) * | 2015-06-26 | 2018-04-12 | 協和発酵キリン株式会社 | オリゴヌクレオチド誘導体 |
| CN105037739B (zh) * | 2015-07-28 | 2017-10-27 | 四川大学 | 具有精氨酸穿膜作用的还原敏感型聚合物及其制备方法与应用 |
| TWI639614B (zh) * | 2015-11-06 | 2018-11-01 | 美商齊亞雋科學公司 | 核苷酸類似物 |
| WO2017100461A1 (en) * | 2015-12-08 | 2017-06-15 | Solstice Biologics, Ltd. | Polynucleotide constructs having an auxiliary moiety non-bioreversibly linked to an internucleoside phosphate or phosphorothioate |
| PL3429618T3 (pl) | 2016-03-16 | 2024-07-01 | Amal Therapeutics Sa | Kombinacja modulatora immunologicznego punktu kontrolnego i kompleks zawierający peptyd penetrujący komórkę, cargo i agonistę peptydu tlr do zastosowania w medycynie |
| TWI746590B (zh) * | 2016-06-30 | 2021-11-21 | 日商協和麒麟股份有限公司 | 核酸複合體 |
| AU2017311510B2 (en) | 2016-08-10 | 2021-11-18 | Cancer Targeted Technology Llc | Chelated PSMA inhibitors |
| CA3033867A1 (en) * | 2016-08-17 | 2018-02-22 | Solstice Biologics, Ltd. | Polynucleotide constructs |
| JP7249080B2 (ja) * | 2016-08-23 | 2023-03-30 | ディセルナ ファーマシューティカルズ インコーポレイテッド | 可逆的に修飾されたオリゴヌクレオチドを含む組成物及びその使用 |
| HUE067838T2 (hu) | 2016-09-21 | 2024-11-28 | Amal Therapeutics Sa | Egy sejtpenetráló peptidet, egy multiepitópot és egy TLR peptidagonistát tartalmazó fúzió rák kezelésére |
| MX2019005742A (es) | 2016-11-23 | 2019-09-13 | Cancer Targeted Tech Llc | Inhibidores de antigeno de membrana especifico de la prostata (psma) de union a albumina. |
| MX2019012295A (es) * | 2017-04-14 | 2020-02-07 | Tollnine Inc | Polinucleotidos inmunomoduladores, conjugados de anticuerpos de los mismos y metodos para su uso. |
| US11597744B2 (en) | 2017-06-30 | 2023-03-07 | Sirius Therapeutics, Inc. | Chiral phosphoramidite auxiliaries and methods of their use |
| PH12020551219A1 (en) | 2018-02-14 | 2021-04-19 | Deep Genomics Incorporated | Oligonucleotide therapy for wilson disease |
| JP7536025B2 (ja) * | 2018-10-17 | 2024-08-19 | タラック セラピューティクス，インク． | 免疫調節性ポリヌクレオチドコンジュゲートと使用方法 |
| CN109384715B (zh) * | 2018-11-19 | 2021-09-03 | 复旦大学附属肿瘤医院 | 前列腺特异性膜抗原的小分子抑制剂的制备方法 |
| WO2020139788A2 (en) * | 2018-12-28 | 2020-07-02 | Sirnaomics, Inc. | Targeted delivery of therapeutic molecules |
| CA3164050A1 (en) | 2019-12-09 | 2021-06-17 | Empirico Inc. | Oligonucleotides for treatment of angiopoietin like 4 (angptl4) related diseases |
| CA3169523A1 (en) | 2020-02-28 | 2021-09-02 | Jaume Pons | Transglutaminase-mediated conjugation |
| CN112402620A (zh) * | 2020-12-07 | 2021-02-26 | 南开大学 | 肿瘤微环境还原响应性的纳米药物及其制备方法 |
| EP4271696A2 (en) * | 2020-12-31 | 2023-11-08 | Alnylam Pharmaceuticals, Inc. | Cyclic-disulfide modified phosphate based oligonucleotide prodrugs |
| CN112679583B (zh) * | 2021-01-07 | 2022-02-22 | 杭州医学院 | 一种靶向癌蛋白boris的特异性多肽及其应用和基因 |
| CA3198230A1 (en) * | 2021-01-28 | 2022-08-04 | Jian Chen | Conjugate and use thereof |
| CN112898206A (zh) * | 2021-02-05 | 2021-06-04 | 河北凡博医药科技有限公司 | 一种5,6-二甲基苯并咪唑的制备方法 |
| CN113024854B (zh) * | 2021-03-24 | 2022-06-03 | 西南石油大学 | 一种结构可控且规整的凝胶材料的制备方法 |
| US11879125B2 (en) | 2022-03-16 | 2024-01-23 | Empirico Inc. | GalNAc compositions for improving siRNA bioavailability |
| WO2024093947A1 (zh) * | 2022-10-31 | 2024-05-10 | 大睿生物医药科技(上海)有限公司 | 向细胞内递送siRNA的前药 |
| CN115925586A (zh) * | 2022-11-01 | 2023-04-07 | 青岛蓝谷多肽生物医药科技有限公司 | 一种靶向psma的母体及其衍生物的制备方法 |
| CN116715624B (zh) * | 2023-06-14 | 2025-11-28 | 信阳师范学院 | 一种n-烷基化吡啶硫酮类化合物的合成方法 |
| WO2025160446A1 (en) * | 2024-01-25 | 2025-07-31 | Ai Proteins, Inc. | Methods and systems for characterizing structural features of a protein |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU7759291A (en) * | 1990-03-29 | 1991-10-21 | Gilead Sciences, Inc. | Oligonucleotide-transport agent disulfide conjugates |
| US6610841B1 (en) * | 1997-12-18 | 2003-08-26 | Gilead Sciences, Inc. | Nucleotide-based prodrugs |
| US20070142267A1 (en) * | 1998-11-23 | 2007-06-21 | Novelos Therapeutics, Inc. | Methods for production of the oxidized glutathione composite with CIS-diamminedichloroplatinum and pharmaceutical compositions based thereof regulating metabolism, proliferation, differentiation and apoptotic mechanisms for normal and transformed cells |
| CN100406065C (zh) * | 2000-12-01 | 2008-07-30 | 细胞工厂治疗公司 | 糖基化/半乳糖基化肽、双官能接头和核苷酸单体/多聚体的缀合物以及相关的组合物和使用方法 |
| US20030073618A1 (en) * | 2001-02-08 | 2003-04-17 | Kozhemyakin Leonid A. | Compounds comprising disulfide-containing peptides and nitrogenous bases, and medical uses thereof |
| US7785610B2 (en) * | 2001-06-21 | 2010-08-31 | Dynavax Technologies Corporation | Chimeric immunomodulatory compounds and methods of using the same—III |
| EP2423335B1 (en) * | 2001-06-21 | 2014-05-14 | Dynavax Technologies Corporation | Chimeric immunomodulatory compounds and methods of using the same |
| WO2007011722A2 (en) * | 2005-07-15 | 2007-01-25 | President And Fellows Of Harvard College | Reaction discovery system |
| CA2679393A1 (en) * | 2007-03-05 | 2008-09-12 | Newsouth Innovations Pty Limited | Methods for detecting and modulating the sensitivity of tumour cells to anti-mitotic agents |
| US20120142763A1 (en) * | 2009-06-01 | 2012-06-07 | The Regents Of The University Of California | Nucleic acid delivery compositions and methods of use thereof |
| CN103796657B (zh) * | 2011-07-19 | 2017-07-11 | 波涛生命科学有限公司 | 合成官能化核酸的方法 |
| US20150018579A1 (en) * | 2012-02-22 | 2015-01-15 | Suresh C. Srivastava | Synthesis of high purity dmt-c3-disulfide phosphoramidite |
| CN104781271B (zh) * | 2012-08-20 | 2018-07-06 | 加利福尼亚大学董事会 | 具有生物可逆的基团的多核苷酸 |
-
2014
- 2014-11-06 EP EP14860025.7A patent/EP3066105A4/en not_active Withdrawn
- 2014-11-06 US US15/034,973 patent/US20160257961A1/en not_active Abandoned
- 2014-11-06 AU AU2014346658A patent/AU2014346658A1/en not_active Abandoned
- 2014-11-06 WO PCT/US2014/064401 patent/WO2015069932A1/en not_active Ceased
- 2014-11-06 CN CN201480072173.2A patent/CN106061981A/zh active Pending
- 2014-11-06 CA CA2929651A patent/CA2929651A1/en not_active Abandoned
- 2014-11-06 JP JP2016553242A patent/JP2016537027A/ja active Pending
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