JP2018512041A5 - - Google Patents
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- JP2018512041A5 JP2018512041A5 JP2017534279A JP2017534279A JP2018512041A5 JP 2018512041 A5 JP2018512041 A5 JP 2018512041A5 JP 2017534279 A JP2017534279 A JP 2017534279A JP 2017534279 A JP2017534279 A JP 2017534279A JP 2018512041 A5 JP2018512041 A5 JP 2018512041A5
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- 230000000692 anti-sense Effects 0.000 claims 9
- 125000003729 nucleotide group Chemical group 0.000 claims 9
- 150000007523 nucleic acids Chemical class 0.000 claims 8
- 108020004707 nucleic acids Proteins 0.000 claims 8
- 239000002773 nucleotide Substances 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 4
- 229920001850 Nucleic acid sequence Polymers 0.000 claims 3
- 229920000972 Sense strand Polymers 0.000 claims 3
- 230000004048 modification Effects 0.000 claims 3
- 238000006011 modification reaction Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- IQFYYKKMVGJFEH-XLPZGREQSA-N DEOXYTHYMIDINE Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 IQFYYKKMVGJFEH-XLPZGREQSA-N 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 101710033922 KRAS Proteins 0.000 claims 1
- 102100009279 KRAS Human genes 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 201000009030 carcinoma Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 239000002502 liposome Substances 0.000 claims 1
- 125000001921 locked nucleotide group Chemical group 0.000 claims 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical class [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 1
Claims (9)
- センス鎖及びアンチセンス鎖を含むp21の発現を阻害する核酸分子であって、前記鎖が二重鎖領域を形成し、前記アンチセンス鎖はUUAAAAUGUCUGACUCCUUNN（配列番号７１）のヌクレオチド配列又は修飾を有する当該ヌクレオチド鎖を含み、前記センス鎖はAAGGAGUCAGACAUUUUAANN（配列番号５７）のヌクレオチド配列又は修飾を有する当該ヌクレオチド鎖を含む（これらヌクレオチド配列において、A、G、C及びUはそれぞれリボA、リボG、リボC及びリボUであり、NはA、C、G、U、2'-OMe置換U、a、c、g、u、t、修飾ヌクレオチド、逆方向（inverted）ヌクレオチド又は化学修飾ヌクレオチドである（a、c、g、u及びtはそれぞれ2'-デオキシ-A、2'-デオキシ-C、2'-デオキシ-G、2'-デオキシ-U及び2'-デオキシ-T））、核酸分子。
- 前記修飾が、2’-デオキシヌクレオチド、2’-O-アルキル置換ヌクレオチド、2’-デオキシ-2’-フルオロ置換ヌクレオチド、ホスホロチオエートヌクレオチド、ロックドヌクレオチド又はそれらの任意の組み合わせである、請求項１記載の核酸分子。
- 前記アンチセンス鎖が複数の位置にデオキシヌクレオチドを有し、前記複数の位置が以下のうちの1つである、請求項１記載の核酸分子。
アンチセンス鎖の5’末端からの位置4、6及び8のそれぞれ;
アンチセンス鎖の5’末端からの位置3、5及び7のそれぞれ;
アンチセンス鎖の5’末端からの位置1、3、5及び7のそれぞれ;
アンチセンス鎖の5’末端からの位置3〜8のそれぞれ;又は
アンチセンス鎖の5’末端からの位置5〜8のそれぞれ - 前記二重鎖領域内に1つ以上の2'-デオキシ-2'-フルオロ置換ヌクレオチドを有する、請求項１記載の核酸分子。
- 前記アンチセンス鎖及び前記センス鎖は、下記表のIDで示される組み合わせであることを特徴とする請求項１記載の核酸分子。
ここで、表中の大文字のA、G、C及びUはそれぞれリボA、リボG、リボC及びリボUを意味し、小文字a、u、g、c及びtはそれぞれ2'-デオキシ-A、2'-デオキシ-U、2'-デオキシ-G、2'-デオキシ-C及びデオキシチミジンを意味し、下線は2'-OMe置換体を意味し、小文字のfは2'-デオキシ-2'-フルオロ置換を意味する。
- 請求項１〜５いずれか１項記載の核酸分子及び薬学的に許容される担体を含む医薬組成物。
- 前記担体が脂質分子又はリポソームを含む、請求項６記載の医薬組成物。
- 悪性腫瘍、癌、突然変異KRASを発現する細胞に起因する癌、肉腫及び癌腫から選ばれる少なくとも一種に対する治療のための請求項６記載の医薬組成物。
- 請求項１〜５いずれか１項記載の核酸分子を含むベクター又は細胞。
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014266198 | 2014-12-26 | ||
| JP2014266198 | 2014-12-26 | ||
| US201562184209P | 2015-06-24 | 2015-06-24 | |
| US62/184,209 | 2015-06-24 | ||
| US201562266668P | 2015-12-13 | 2015-12-13 | |
| US62/266,668 | 2015-12-13 | ||
| PCT/US2015/067557 WO2016106402A1 (en) | 2014-12-26 | 2015-12-28 | Rna interference agents for p21 gene modulation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018512041A JP2018512041A (ja) | 2018-05-10 |
| JP2018512041A5 true JP2018512041A5 (ja) | 2019-02-14 |
| JP6865169B2 JP6865169B2 (ja) | 2021-04-28 |
Family
ID=56151549
Family Applications (9)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017534274A Pending JP2018513104A (ja) | 2014-12-26 | 2015-12-28 | Ｈｓｐ４７及びｐ２１を標的とするｒｎａｉ分子による悪性腫瘍の治療用組成物及び方法 |
| JP2017534297A Active JP6457645B2 (ja) | 2014-12-26 | 2015-12-28 | ＧＳＴ−π遺伝子を調節するためのＲＮＡ干渉剤 |
| JP2017534275A Pending JP2018512373A (ja) | 2014-12-26 | 2015-12-28 | Ｋｒａｓ突然変異に関連する悪性腫瘍に対する治療のための方法及び組成物 |
| JP2017534286A Active JP6793649B2 (ja) | 2014-12-26 | 2015-12-28 | Ｐ２１遺伝子調節のためのｒｎａ剤 |
| JP2017534287A Pending JP2018513669A (ja) | 2014-12-26 | 2015-12-28 | Ｇｓｔ−ｐｉ遺伝子調節のためのｒｎａ剤 |
| JP2017534279A Active JP6865169B2 (ja) | 2014-12-26 | 2015-12-28 | Ｐ２１遺伝子調節のためのｒｎａ干渉剤 |
| JP2017534294A Active JP6730285B2 (ja) | 2014-12-26 | 2015-12-28 | Ｒｎａ干渉組成物及び悪性腫瘍のための方法 |
| JP2021183788A Active JP7307137B2 (ja) | 2014-12-26 | 2021-11-11 | ＧＳＴ－π遺伝子を調節するためのＲＮＡ干渉剤 |
| JP2023106970A Pending JP2023123743A (ja) | 2014-12-26 | 2023-06-29 | ＧＳＴ－π遺伝子を調節するためのＲＮＡ干渉剤 |
Family Applications Before (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017534274A Pending JP2018513104A (ja) | 2014-12-26 | 2015-12-28 | Ｈｓｐ４７及びｐ２１を標的とするｒｎａｉ分子による悪性腫瘍の治療用組成物及び方法 |
| JP2017534297A Active JP6457645B2 (ja) | 2014-12-26 | 2015-12-28 | ＧＳＴ−π遺伝子を調節するためのＲＮＡ干渉剤 |
| JP2017534275A Pending JP2018512373A (ja) | 2014-12-26 | 2015-12-28 | Ｋｒａｓ突然変異に関連する悪性腫瘍に対する治療のための方法及び組成物 |
| JP2017534286A Active JP6793649B2 (ja) | 2014-12-26 | 2015-12-28 | Ｐ２１遺伝子調節のためのｒｎａ剤 |
| JP2017534287A Pending JP2018513669A (ja) | 2014-12-26 | 2015-12-28 | Ｇｓｔ−ｐｉ遺伝子調節のためのｒｎａ剤 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017534294A Active JP6730285B2 (ja) | 2014-12-26 | 2015-12-28 | Ｒｎａ干渉組成物及び悪性腫瘍のための方法 |
| JP2021183788A Active JP7307137B2 (ja) | 2014-12-26 | 2021-11-11 | ＧＳＴ－π遺伝子を調節するためのＲＮＡ干渉剤 |
| JP2023106970A Pending JP2023123743A (ja) | 2014-12-26 | 2023-06-29 | ＧＳＴ－π遺伝子を調節するためのＲＮＡ干渉剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (14) | US10264976B2 (ja) |
| EP (9) | EP3236975A4 (ja) |
| JP (9) | JP2018513104A (ja) |
| KR (4) | KR102527430B1 (ja) |
| CN (7) | CN107108686B (ja) |
| AU (4) | AU2015369595A1 (ja) |
| BR (2) | BR112017013599A2 (ja) |
| CA (4) | CA2972265A1 (ja) |
| RU (4) | RU2017126601A (ja) |
| WO (7) | WO2016106405A1 (ja) |
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