JP2020516296A5 - - Google Patents
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- JP2020516296A5 JP2020516296A5 JP2019555936A JP2019555936A JP2020516296A5 JP 2020516296 A5 JP2020516296 A5 JP 2020516296A5 JP 2019555936 A JP2019555936 A JP 2019555936A JP 2019555936 A JP2019555936 A JP 2019555936A JP 2020516296 A5 JP2020516296 A5 JP 2020516296A5
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- 150000003839 salts Chemical class 0.000 claims description 246
- 150000001875 compounds Chemical class 0.000 claims description 236
- 108020004459 Small interfering RNA Proteins 0.000 claims description 76
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 45
- 125000000217 alkyl group Chemical group 0.000 claims description 40
- 125000005647 linker group Chemical group 0.000 claims description 38
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- 125000001475 halogen functional group Chemical group 0.000 claims description 35
- 125000003545 alkoxy group Chemical group 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 25
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 25
- 125000001072 heteroaryl group Chemical group 0.000 claims description 23
- 239000007787 solid Substances 0.000 claims description 23
- 125000000304 alkynyl group Chemical group 0.000 claims description 18
- 230000008685 targeting Effects 0.000 claims description 15
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims description 14
- 239000003446 ligand Substances 0.000 claims description 14
- 150000007523 nucleic acids Chemical group 0.000 claims description 13
- 125000004429 atom Chemical group 0.000 claims description 12
- 241001465754 Metazoa Species 0.000 claims description 11
- 125000003342 alkenyl group Chemical group 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 11
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 10
- 150000001720 carbohydrates Chemical class 0.000 claims description 10
- 108020004707 nucleic acids Proteins 0.000 claims description 10
- 102000039446 nucleic acids Human genes 0.000 claims description 10
- 125000006239 protecting group Chemical group 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 7
- 239000003937 drug carrier Substances 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- -1 salts compound Chemical class 0.000 claims description 5
- 210000004185 liver Anatomy 0.000 claims description 4
- 238000011282 treatment Methods 0.000 claims description 3
- 208000002672 hepatitis B Diseases 0.000 claims description 2
- 238000013160 medical therapy Methods 0.000 claims description 2
- 230000000069 prophylactic effect Effects 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 230000008878 coupling Effects 0.000 claims 4
- 238000010168 coupling process Methods 0.000 claims 4
- 238000005859 coupling reaction Methods 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 239000004055 small Interfering RNA Substances 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 description 37
- 125000004432 carbon atom Chemical group C* 0.000 description 26
- 0 CC(C)(C)N(CCC1)C1C(CO*=C)O Chemical compound CC(C)(C)N(CCC1)C1C(CO*=C)O 0.000 description 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 16
- 150000002431 hydrogen Chemical class 0.000 description 16
- 239000012071 phase Substances 0.000 description 16
- 229920006395 saturated elastomer Polymers 0.000 description 15
- 229930195734 saturated hydrocarbon Natural products 0.000 description 15
- 229930195735 unsaturated hydrocarbon Natural products 0.000 description 15
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 14
- 125000004043 oxo group Chemical group O=* 0.000 description 14
- 125000001424 substituent group Chemical group 0.000 description 14
- 150000001345 alkine derivatives Chemical class 0.000 description 12
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 11
- 125000004104 aryloxy group Chemical group 0.000 description 11
- 150000001540 azides Chemical class 0.000 description 11
- 125000004093 cyano group Chemical group *C#N 0.000 description 11
- 125000005553 heteroaryloxy group Chemical group 0.000 description 11
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 11
- 238000000034 method Methods 0.000 description 9
- 235000000346 sugar Nutrition 0.000 description 9
- 125000001188 haloalkyl group Chemical group 0.000 description 8
- 125000004414 alkyl thio group Chemical group 0.000 description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 7
- 229910052799 carbon Inorganic materials 0.000 description 6
- 125000004438 haloalkoxy group Chemical group 0.000 description 5
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 description 4
- 125000004423 acyloxy group Chemical group 0.000 description 4
- 125000001589 carboacyl group Chemical group 0.000 description 4
- 150000001721 carbon Chemical group 0.000 description 4
- 125000000623 heterocyclic group Chemical group 0.000 description 4
- 150000008163 sugars Chemical class 0.000 description 4
- 150000008574 D-amino acids Chemical class 0.000 description 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Natural products NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 3
- 150000008575 L-amino acids Chemical class 0.000 description 3
- 230000003213 activating effect Effects 0.000 description 3
- 125000002947 alkylene group Chemical group 0.000 description 3
- ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphonic acid group Chemical group P(O)(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 description 3
- 208000009594 Animal Hepatitis Diseases 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 239000004471 Glycine Substances 0.000 description 2
- 241000700721 Hepatitis B virus Species 0.000 description 2
- 208000029433 Herpesviridae infectious disease Diseases 0.000 description 2
- OVRNDRQMDRJTHS-KEWYIRBNSA-N N-acetyl-D-galactosamine Chemical compound CC(=O)N[C@H]1C(O)O[C@H](CO)[C@H](O)[C@@H]1O OVRNDRQMDRJTHS-KEWYIRBNSA-N 0.000 description 2
- MBLBDJOUHNCFQT-UHFFFAOYSA-N N-acetyl-D-galactosamine Natural products CC(=O)NC(C=O)C(O)C(O)C(O)CO MBLBDJOUHNCFQT-UHFFFAOYSA-N 0.000 description 2
- 150000002016 disaccharides Chemical class 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 208000006454 hepatitis Diseases 0.000 description 2
- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 2
- 150000002772 monosaccharides Chemical class 0.000 description 2
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 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 description 1
- ADYGKTWSELPLSQ-UHFFFAOYSA-N CC(C)(CCO)OC(C(C1O)NC(C)=O)OC(CO)C1O Chemical compound CC(C)(CCO)OC(C(C1O)NC(C)=O)OC(CO)C1O ADYGKTWSELPLSQ-UHFFFAOYSA-N 0.000 description 1
- QQGNLKJAIVSNCO-UHFFFAOYSA-N CCCCNC=O Chemical compound CCCCNC=O QQGNLKJAIVSNCO-UHFFFAOYSA-N 0.000 description 1
- NZHMROSYTLLOCR-GFMAATOTSA-N CCCOC([C@@H]([C@H]1O)NC(C)=O)OC[C@@H]1O Chemical compound CCCOC([C@@H]([C@H]1O)NC(C)=O)OC[C@@H]1O NZHMROSYTLLOCR-GFMAATOTSA-N 0.000 description 1
- UJUOHBCTKYTJEZ-UHFFFAOYSA-N CCN(C)NC(CC[O](C)C)(CC1)CC1O Chemical compound CCN(C)NC(CC[O](C)C)(CC1)CC1O UJUOHBCTKYTJEZ-UHFFFAOYSA-N 0.000 description 1
- 108091034117 Oligonucleotide Proteins 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical group OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 1
- 125000005103 alkyl silyl group Chemical group 0.000 description 1
- 239000000427 antigen Substances 0.000 description 1
- 102000036639 antigens Human genes 0.000 description 1
- 108091007433 antigens Proteins 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 description 1
- 238000001668 nucleic acid synthesis Methods 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000007790 solid phase Substances 0.000 description 1
- 238000011421 subcutaneous treatment Methods 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 150000004043 trisaccharides Chemical class 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022176285A JP7564173B2 (ja) | 2017-04-11 | 2022-11-02 | 標的化組成物 |
| JP2024166900A JP2024174053A (ja) | 2017-04-11 | 2024-09-26 | 標的化組成物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762484247P | 2017-04-11 | 2017-04-11 | |
| US62/484,247 | 2017-04-11 | ||
| US201762525071P | 2017-06-26 | 2017-06-26 | |
| US62/525,071 | 2017-06-26 | ||
| PCT/US2018/026918 WO2018191278A2 (en) | 2017-04-11 | 2018-04-10 | Targeted compositions |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022176285A Division JP7564173B2 (ja) | 2017-04-11 | 2022-11-02 | 標的化組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020516296A JP2020516296A (ja) | 2020-06-11 |
| JP2020516296A5 true JP2020516296A5 (cg-RX-API-DMAC7.html) | 2021-05-27 |
Family
ID=62063656
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019555936A Pending JP2020516296A (ja) | 2017-04-11 | 2018-04-10 | 標的化組成物 |
| JP2022176285A Active JP7564173B2 (ja) | 2017-04-11 | 2022-11-02 | 標的化組成物 |
| JP2024166900A Pending JP2024174053A (ja) | 2017-04-11 | 2024-09-26 | 標的化組成物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022176285A Active JP7564173B2 (ja) | 2017-04-11 | 2022-11-02 | 標的化組成物 |
| JP2024166900A Pending JP2024174053A (ja) | 2017-04-11 | 2024-09-26 | 標的化組成物 |
Country Status (15)
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MA45478A (fr) * | 2016-04-11 | 2019-02-20 | Arbutus Biopharma Corp | Compositions de conjugués d'acides nucléiques ciblés |
| EP3950004A1 (en) | 2017-04-11 | 2022-02-09 | Arbutus Biopharma Corporation | Targeted compositions |
| CN110997917B (zh) | 2017-12-01 | 2024-04-09 | 苏州瑞博生物技术股份有限公司 | 一种核酸、含有该核酸的组合物与缀合物及制备方法和用途 |
| EP4455285A3 (en) | 2017-12-01 | 2025-02-26 | Suzhou Ribo Life Science Co., Ltd. | Nucleic acid, composition and conjugate comprising the same, and preparation method and use thereof |
| EP3718572B1 (en) | 2017-12-01 | 2024-07-31 | Suzhou Ribo Life Science Co., Ltd. | Nucleic acid, composition and conjugate containing nucleic acid, preparation method and use |
| CN118291457A (zh) | 2017-12-01 | 2024-07-05 | 苏州瑞博生物技术股份有限公司 | 一种核酸、含有该核酸的组合物与缀合物及制备方法和用途 |
| AU2018374219C1 (en) | 2017-12-01 | 2023-05-11 | Suzhou Ribo Life Science Co., Ltd. | Double-stranded oligonucleotide, composition and conjugate comprising double-stranded oligonucleotide, preparation method therefor and use thereof |
| KR102617947B1 (ko) | 2017-12-29 | 2023-12-27 | 쑤저우 리보 라이프 사이언스 컴퍼니, 리미티드 | 접합체와 제조 및 그 용도 |
| WO2020038377A1 (zh) | 2018-08-21 | 2020-02-27 | 苏州瑞博生物技术有限公司 | 一种核酸、含有该核酸的药物组合物和缀合物及其用途 |
| CN111655297A (zh) | 2018-09-30 | 2020-09-11 | 苏州瑞博生物技术有限公司 | 一种siRNA缀合物及其制备方法和用途 |
| JP7588855B2 (ja) * | 2018-11-02 | 2024-11-25 | ジェネヴァント サイエンシズ ゲーエムベーハー | 治療方法 |
| CN113226332B (zh) * | 2018-11-02 | 2025-05-09 | 阿布特斯生物制药公司 | 二价靶向缀合物 |
| EP3903830A4 (en) | 2018-12-28 | 2023-04-26 | Suzhou Ribo Life Science Co., Ltd. | NUCLEIC ACID, COMPOSITION AND CONJUGATE WITH NUCLEIC ACID, PROCESS FOR THEIR PREPARATION AND ITS USE |
| EP3941921A4 (en) * | 2019-03-20 | 2023-05-03 | Arbutus Biopharma Corporation | Therapeutic methods for treating hepatitis b |
| CN113227376B (zh) | 2019-05-22 | 2024-04-09 | 苏州瑞博生物技术股份有限公司 | 核酸、药物组合物与缀合物及制备方法和用途 |
| JP7610268B2 (ja) * | 2019-05-22 | 2025-01-08 | スーチョウ リボ ライフ サイエンス カンパニー、リミテッド | 核酸、薬物組成物及び複合体ならびに調製方法と使用 |
| US20220305107A1 (en) | 2019-06-18 | 2022-09-29 | Janssen Sciences Ireland Unlimited Company | COMBINATION OF HEPATITIS B VIRUS (HBV) VACCINES AND HBV-TARGETING RNAi |
| CN115884984A (zh) * | 2019-12-06 | 2023-03-31 | 盖纳万科学有限公司 | 用于治疗肝纤维化的结合物和方法 |
| AU2020408039A1 (en) | 2019-12-20 | 2022-08-18 | Arbutus Biopharma Corporation | Synthetic processes and intermediates |
| MX2023005138A (es) * | 2020-11-06 | 2023-06-23 | Arbutus Biopharma Corp | Conjugados dirigidos que comprenden arnpi modificado. |
| CN114853829A (zh) * | 2021-02-05 | 2022-08-05 | 上海拓界生物医药科技有限公司 | 一种核酸配体、其缀合物、制备方法及用途 |
| WO2022199685A1 (zh) * | 2021-03-25 | 2022-09-29 | 安沛治疗有限公司 | 具有延长的体内半衰期的核酸分子缀合物 |
| TW202340466A (zh) * | 2021-12-16 | 2023-10-16 | 大陸商上海拓界生物醫藥科技有限公司 | 一種ｄｓｒｎａ、其製備方法及應用 |
| KR20240136985A (ko) * | 2022-01-20 | 2024-09-19 | 청두 신정허 파마슈티컬 테크놀로지 컴퍼니 리미티드 | 표적화 리간드 및 이의 용도 |
| CN117756866A (zh) * | 2022-01-30 | 2024-03-26 | 大睿生物医药科技(上海)有限公司 | 含有n-乙酰半乳糖胺的靶向配体 |
| CN119213005A (zh) | 2022-03-16 | 2024-12-27 | 艾姆皮瑞克公司 | 用于提高siRNA生物利用度的GALNAC组合物 |
| WO2024255761A1 (zh) * | 2023-06-12 | 2024-12-19 | 大睿生物 | 包含糖的寡核苷酸递送配体 |
| WO2025007274A1 (zh) * | 2023-07-04 | 2025-01-09 | 成都先导药物开发股份有限公司 | 一种缀合物及其中间体化合物和用途 |
| WO2025007907A1 (zh) * | 2023-07-04 | 2025-01-09 | 大睿生物 | 包含肽的寡核苷酸递送配体 |
| WO2025242321A1 (en) | 2024-05-24 | 2025-11-27 | Glaxosmithkline Intellectual Property (No.3) Limited | Novel use |
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| MA45478A (fr) | 2016-04-11 | 2019-02-20 | Arbutus Biopharma Corp | Compositions de conjugués d'acides nucléiques ciblés |
| EP3950004A1 (en) | 2017-04-11 | 2022-02-09 | Arbutus Biopharma Corporation | Targeted compositions |
| CN118384268A (zh) * | 2017-04-18 | 2024-07-26 | 阿尔尼拉姆医药品有限公司 | 具有乙肝病毒（hbv）感染的受试者的治疗方法 |
| EP3941921A4 (en) | 2019-03-20 | 2023-05-03 | Arbutus Biopharma Corporation | Therapeutic methods for treating hepatitis b |
| US20220305107A1 (en) * | 2019-06-18 | 2022-09-29 | Janssen Sciences Ireland Unlimited Company | COMBINATION OF HEPATITIS B VIRUS (HBV) VACCINES AND HBV-TARGETING RNAi |
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2018
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