JP2020526192A5 - - Google Patents
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- JP2020526192A5 JP2020526192A5 JP2019572571A JP2019572571A JP2020526192A5 JP 2020526192 A5 JP2020526192 A5 JP 2020526192A5 JP 2019572571 A JP2019572571 A JP 2019572571A JP 2019572571 A JP2019572571 A JP 2019572571A JP 2020526192 A5 JP2020526192 A5 JP 2020526192A5
- Authority
- JP
- Japan
- Prior art keywords
- rnai agent
- agent according
- nucleotides
- sense strand
- composition
- 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.)
- Withdrawn
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- 108091030071 RNAI Proteins 0.000 claims description 91
- 239000003795 chemical substances by application Substances 0.000 claims description 91
- 230000009368 gene silencing by RNA Effects 0.000 claims description 91
- 125000003729 nucleotide group Chemical group 0.000 claims description 76
- 239000002773 nucleotide Substances 0.000 claims description 64
- 108091081021 Sense strand Proteins 0.000 claims description 42
- 230000000692 anti-sense effect Effects 0.000 claims description 34
- 239000000203 mixture Substances 0.000 claims description 30
- 239000003446 ligand Substances 0.000 claims description 24
- 230000008685 targeting Effects 0.000 claims description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 21
- 101710194189 Amiloride-sensitive sodium channel subunit alpha Proteins 0.000 claims description 16
- 201000010099 disease Diseases 0.000 claims description 15
- 230000014509 gene expression Effects 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- 102100037242 Amiloride-sensitive sodium channel subunit alpha Human genes 0.000 claims description 10
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 8
- NYHBQMYGNKIUIF-UUOKFMHZSA-N Guanosine Chemical compound C1=NC=2C(=O)NC(N)=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O NYHBQMYGNKIUIF-UUOKFMHZSA-N 0.000 claims description 8
- DRTQHJPVMGBUCF-XVFCMESISA-N Uridine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-XVFCMESISA-N 0.000 claims description 8
- 210000004027 cell Anatomy 0.000 claims description 8
- 230000000694 effects Effects 0.000 claims description 8
- 102000006495 integrins Human genes 0.000 claims description 8
- 108010044426 integrins Proteins 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- UHDGCWIWMRVCDJ-UHFFFAOYSA-N 1-beta-D-Xylofuranosyl-NH-Cytosine Natural products O=C1N=C(N)C=CN1C1C(O)C(O)C(CO)O1 UHDGCWIWMRVCDJ-UHFFFAOYSA-N 0.000 claims description 4
- MIKUYHXYGGJMLM-GIMIYPNGSA-N Crotonoside Natural products C1=NC2=C(N)NC(=O)N=C2N1[C@H]1O[C@@H](CO)[C@H](O)[C@@H]1O MIKUYHXYGGJMLM-GIMIYPNGSA-N 0.000 claims description 4
- UHDGCWIWMRVCDJ-PSQAKQOGSA-N Cytidine Natural products O=C1N=C(N)C=CN1[C@@H]1[C@@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-PSQAKQOGSA-N 0.000 claims description 4
- NYHBQMYGNKIUIF-UHFFFAOYSA-N D-guanosine Natural products C1=2NC(N)=NC(=O)C=2N=CN1C1OC(CO)C(O)C1O NYHBQMYGNKIUIF-UHFFFAOYSA-N 0.000 claims description 4
- 108091028043 Nucleic acid sequence Proteins 0.000 claims description 4
- DRTQHJPVMGBUCF-PSQAKQOGSA-N beta-L-uridine Natural products O[C@H]1[C@@H](O)[C@H](CO)O[C@@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-PSQAKQOGSA-N 0.000 claims description 4
- 230000037396 body weight Effects 0.000 claims description 4
- FPUGCISOLXNPPC-IOSLPCCCSA-N cordysinin B Chemical compound CO[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C2=NC=NC(N)=C2N=C1 FPUGCISOLXNPPC-IOSLPCCCSA-N 0.000 claims description 4
- UHDGCWIWMRVCDJ-ZAKLUEHWSA-N cytidine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O1 UHDGCWIWMRVCDJ-ZAKLUEHWSA-N 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229940029575 guanosine Drugs 0.000 claims description 4
- 239000006199 nebulizer Substances 0.000 claims description 4
- 208000023504 respiratory system disease Diseases 0.000 claims description 4
- DRTQHJPVMGBUCF-UHFFFAOYSA-N uracil arabinoside Natural products OC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-UHFFFAOYSA-N 0.000 claims description 4
- 229940045145 uridine Drugs 0.000 claims description 4
- 208000024891 symptom Diseases 0.000 claims description 3
- UUDVSZSQPFXQQM-GIWSHQQXSA-N (2r,3s,4r,5r)-2-(6-aminopurin-9-yl)-3-fluoro-5-(hydroxymethyl)oxolane-3,4-diol Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@]1(O)F UUDVSZSQPFXQQM-GIWSHQQXSA-N 0.000 claims description 2
- FPUGCISOLXNPPC-UHFFFAOYSA-N 2'-O-Methyladenosine Natural products COC1C(O)C(CO)OC1N1C2=NC=NC(N)=C2N=C1 FPUGCISOLXNPPC-UHFFFAOYSA-N 0.000 claims 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 claims description 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 208000025678 Ciliary Motility disease Diseases 0.000 claims description 2
- 206010011732 Cyst Diseases 0.000 claims description 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 2
- 206010013774 Dry eye Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- JVWLUVNSQYXYBE-UHFFFAOYSA-N Ribitol Natural products OCC(C)C(O)C(O)CO JVWLUVNSQYXYBE-UHFFFAOYSA-N 0.000 claims description 2
- 239000002214 arabinonucleotide Substances 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 201000009267 bronchiectasis Diseases 0.000 claims description 2
- 206010006451 bronchitis Diseases 0.000 claims description 2
- 208000007451 chronic bronchitis Diseases 0.000 claims description 2
- 230000000295 complement effect Effects 0.000 claims description 2
- 208000031513 cyst Diseases 0.000 claims description 2
- 239000005547 deoxyribonucleotide Substances 0.000 claims description 2
- 125000002637 deoxyribonucleotide group Chemical group 0.000 claims description 2
- 210000002919 epithelial cell Anatomy 0.000 claims description 2
- ZTWTYVWXUKTLCP-UHFFFAOYSA-L ethenyl-dioxido-oxo-$l^{5}-phosphane Chemical compound [O-]P([O-])(=O)C=C ZTWTYVWXUKTLCP-UHFFFAOYSA-L 0.000 claims description 2
- 208000030533 eye disease Diseases 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 125000001921 locked nucleotide group Chemical group 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
- 229940071648 metered dose inhaler Drugs 0.000 claims description 2
- 125000003835 nucleoside group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000009266 primary ciliary dyskinesia Diseases 0.000 claims description 2
- 108020003175 receptors Proteins 0.000 claims description 2
- 102000005962 receptors Human genes 0.000 claims description 2
- HEBKCHPVOIAQTA-ZXFHETKHSA-N ribitol Chemical compound OC[C@H](O)[C@H](O)[C@H](O)CO HEBKCHPVOIAQTA-ZXFHETKHSA-N 0.000 claims description 2
- 229940124818 soft mist inhaler Drugs 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims description 2
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023146393A JP2023158192A (ja) | 2017-07-06 | 2023-09-08 | アルファ－ＥＮａＣの発現を阻害するためのＲＮＡｉ剤、および使用方法 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762529132P | 2017-07-06 | 2017-07-06 | |
| US62/529,132 | 2017-07-06 | ||
| US201862631683P | 2018-02-17 | 2018-02-17 | |
| US62/631,683 | 2018-02-17 | ||
| US201862679549P | 2018-06-01 | 2018-06-01 | |
| US62/679,549 | 2018-06-01 | ||
| PCT/US2018/040874 WO2019010274A1 (en) | 2017-07-06 | 2018-07-05 | RNAI AGENTS OF INHIBITION OF ALPHA-ENAC GENE EXPRESSION AND METHODS OF USE |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023146393A Division JP2023158192A (ja) | 2017-07-06 | 2023-09-08 | アルファ－ＥＮａＣの発現を阻害するためのＲＮＡｉ剤、および使用方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020526192A JP2020526192A (ja) | 2020-08-31 |
| JP2020526192A5 true JP2020526192A5 (enExample) | 2021-08-12 |
Family
ID=64904123
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019572571A Withdrawn JP2020526192A (ja) | 2017-07-06 | 2018-07-05 | アルファ−ＥＮａＣの発現を阻害するためのＲＮＡｉ剤、および使用方法 |
| JP2023146393A Pending JP2023158192A (ja) | 2017-07-06 | 2023-09-08 | アルファ－ＥＮａＣの発現を阻害するためのＲＮＡｉ剤、および使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023146393A Pending JP2023158192A (ja) | 2017-07-06 | 2023-09-08 | アルファ－ＥＮａＣの発現を阻害するためのＲＮＡｉ剤、および使用方法 |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10590416B2 (enExample) |
| EP (1) | EP3649240A4 (enExample) |
| JP (2) | JP2020526192A (enExample) |
| KR (1) | KR20200024793A (enExample) |
| CN (2) | CN119662650A (enExample) |
| AU (1) | AU2018297262A1 (enExample) |
| BR (1) | BR112019023650A2 (enExample) |
| CA (1) | CA3061752A1 (enExample) |
| CL (1) | CL2020000019A1 (enExample) |
| CO (1) | CO2019014671A2 (enExample) |
| CR (1) | CR20190572A (enExample) |
| EC (1) | ECSP20000655A (enExample) |
| IL (1) | IL271843A (enExample) |
| JO (1) | JOP20190263A1 (enExample) |
| MX (1) | MX2019014800A (enExample) |
| PE (1) | PE20200746A1 (enExample) |
| PH (1) | PH12019502660A1 (enExample) |
| TN (1) | TN2019000308A1 (enExample) |
| TW (1) | TW201919654A (enExample) |
| UY (1) | UY37800A (enExample) |
| WO (1) | WO2019010274A1 (enExample) |
| ZA (1) | ZA202100643B (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20190572A (es) * | 2017-07-06 | 2020-05-23 | Arrowhead Pharmaceuticals Inc | AGENTES DE iARN PARA LA INHIBICIÓN DE LA EXPRESIÓN DE ALFA-ENaC Y MÉTODOS DE USO |
| US12065458B2 (en) | 2018-02-17 | 2024-08-20 | Arrowhead Pharmaceuticals, Inc. | Trialkyne linking agents and methods of use |
| CA3089276A1 (en) * | 2018-02-17 | 2019-08-22 | Arrowhead Pharmaceuticals, Inc. | Trialkyne linking agents and methods of use |
| TW202130809A (zh) * | 2019-10-29 | 2021-08-16 | 美商愛羅海德製藥公司 | 用於抑制β-ENaC表現之RNAi藥劑、其組合物及使用方法 |
| KR20240117104A (ko) | 2021-12-21 | 2024-07-31 | 쑤저우 리보 라이프 사이언스 컴퍼니, 리미티드 | 핵산, 핵산을 포함하는 조성물 및 접합체, 이들의 제조 방법 및 용도 |
| WO2024023254A1 (en) * | 2022-07-27 | 2024-02-01 | E-Therapeutics Plc | Nucleic acid compounds |
| US20250368992A1 (en) * | 2022-07-27 | 2025-12-04 | E-Therapeutics Plc | Nucleic acid compounds |
| WO2024255759A1 (zh) * | 2023-06-13 | 2024-12-19 | 上海拓界生物医药科技有限公司 | 靶向MMP7的siRNA、siRNA缀合物及其医药用途 |
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| CR20190572A (es) * | 2017-07-06 | 2020-05-23 | Arrowhead Pharmaceuticals Inc | AGENTES DE iARN PARA LA INHIBICIÓN DE LA EXPRESIÓN DE ALFA-ENaC Y MÉTODOS DE USO |
| JP7445594B2 (ja) * | 2017-11-01 | 2024-03-07 | アローヘッド ファーマシューティカルズ インコーポレイテッド | インテグリンリガンドおよびその使用 |
| CA3089276A1 (en) * | 2018-02-17 | 2019-08-22 | Arrowhead Pharmaceuticals, Inc. | Trialkyne linking agents and methods of use |
-
2018
- 2018-07-05 CR CR20190572A patent/CR20190572A/es unknown
- 2018-07-05 WO PCT/US2018/040874 patent/WO2019010274A1/en not_active Ceased
- 2018-07-05 PE PE2019002542A patent/PE20200746A1/es unknown
- 2018-07-05 AU AU2018297262A patent/AU2018297262A1/en not_active Abandoned
- 2018-07-05 MX MX2019014800A patent/MX2019014800A/es unknown
- 2018-07-05 US US16/028,006 patent/US10590416B2/en active Active
- 2018-07-05 EP EP18828259.4A patent/EP3649240A4/en active Pending
- 2018-07-05 BR BR112019023650-3A patent/BR112019023650A2/pt not_active Application Discontinuation
- 2018-07-05 KR KR1020197038728A patent/KR20200024793A/ko not_active Ceased
- 2018-07-05 CN CN202411877733.3A patent/CN119662650A/zh active Pending
- 2018-07-05 JP JP2019572571A patent/JP2020526192A/ja not_active Withdrawn
- 2018-07-05 CA CA3061752A patent/CA3061752A1/en active Pending
- 2018-07-05 CN CN201880045293.1A patent/CN110832077B/zh active Active
- 2018-07-05 TN TNP/2019/000308A patent/TN2019000308A1/en unknown
- 2018-07-06 TW TW107123550A patent/TW201919654A/zh unknown
- 2018-07-06 UY UY0001037800A patent/UY37800A/es not_active Application Discontinuation
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2019
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- 2019-11-25 PH PH12019502660A patent/PH12019502660A1/en unknown
- 2019-12-24 CO CONC2019/0014671A patent/CO2019014671A2/es unknown
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2020
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- 2020-01-06 EC ECSENADI2020655A patent/ECSP20000655A/es unknown
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- 2020-01-31 US US16/778,582 patent/US11214802B2/en active Active
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2021
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- 2021-11-29 US US17/536,754 patent/US20220090077A1/en not_active Abandoned
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2023
- 2023-09-08 JP JP2023146393A patent/JP2023158192A/ja active Pending
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