JP2011504362A5 - - Google Patents
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- JP2011504362A5 JP2011504362A5 JP2010534367A JP2010534367A JP2011504362A5 JP 2011504362 A5 JP2011504362 A5 JP 2011504362A5 JP 2010534367 A JP2010534367 A JP 2010534367A JP 2010534367 A JP2010534367 A JP 2010534367A JP 2011504362 A5 JP2011504362 A5 JP 2011504362A5
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- 125000003729 nucleotide group Chemical group 0.000 claims 9
- 229920001850 Nucleic acid sequence Polymers 0.000 claims 8
- 102000001307 androgen receptors Human genes 0.000 claims 6
- 108010080146 androgen receptors Proteins 0.000 claims 6
- 229920003013 deoxyribonucleic acid Polymers 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 239000002773 nucleotide Substances 0.000 claims 4
- 108020004999 Messenger RNA Proteins 0.000 claims 3
- 230000000875 corresponding Effects 0.000 claims 3
- 230000003463 hyperproliferative Effects 0.000 claims 3
- 229920002106 messenger RNA Polymers 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229920000160 (ribonucleotides)n+m Polymers 0.000 claims 2
- LRSASMSXMSNRBT-UHFFFAOYSA-N 5-Methylcytosine Chemical compound CC1=CNC(=O)N=C1N LRSASMSXMSNRBT-UHFFFAOYSA-N 0.000 claims 2
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 claims 2
- 230000000295 complement Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000000178 monomer Substances 0.000 claims 2
- 150000007523 nucleic acids Chemical class 0.000 claims 2
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000240 adjuvant Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 108020004707 nucleic acids Proteins 0.000 claims 1
- 229920000023 polynucleotide Polymers 0.000 claims 1
- 239000002157 polynucleotide Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
Claims (18)
- 合計10〜30個のヌクレオチドの連続するヌクレオチド配列を含む長さ10〜30個のヌクレオチドのオリゴマーであって、前記連続するヌクレオチド配列が、哺乳動物アンドロゲン受容体遺伝子に対応する領域または配列番号1のmRNAの逆相補体もしくはその天然変異体と少なくとも80％相同であり、少なくとも1個のLNA単位を含む、前記オリゴマー。
- 前記連続するヌクレオチド配列が、i)配列番号94もしくは配列番号58、ii)配列番号105もしくは配列番号77またはiii)配列番号2〜22および86〜106からなる群より選択される配列に対応する領域と少なくとも80％相同である、請求項１に記載のオリゴマー。
- 前記連続するヌクレオチド配列が、請求項１に記載の対応する領域の逆相補体について不一致を含まないか、または1もしくは2個以下の不一致を含む、請求項１または２に記載のオリゴマー。
- 前記オリゴマーのヌクレオチド配列が、前記連続するヌクレオチド配列からなる、請求項１〜３のいずれか１項に記載のオリゴマー。
- 前記連続するヌクレオチド配列が、長さ10〜18個のヌクレオチドである、請求項１〜４のいずれか１項に記載のオリゴマー。
- 前記連続するヌクレオチド配列が、ヌクレオチド類似体を含む、請求項１〜５のいずれか１項に記載のオリゴマー。
- 前記ヌクレオチド類似体が、固定核酸(LNA)単位；2'-O-アルキル-RNA単位、2'-OMe-RNA単位、2'-アミノ-DNA単位、および2'-フルオロ-DNA単位からなる群より選択される糖修飾ヌクレオチドなどの糖修飾ヌクレオチドである、請求項６に記載のオリゴマー。
- 前記ヌクレオチド類似体がLNAである、請求項６に記載のオリゴマー。
- ギャップマーである、請求項６〜８のいずれか１項に記載のオリゴマー。
- アンドロゲン受容体遺伝子またはmRNAを発現する細胞中のアンドロゲン受容体遺伝子またはmRNAの発現を阻害する、請求項１〜９のいずれか１項に記載のオリゴマー。
- 前記オリゴマーが、
5'-As MeCs MeCsasasgstststscststscsAsGs MeC-3'(配列番号58)および、
5'-MeCs MeCs MeCsasasgsgscsascstsgscsAsGsA-3'(配列番号77)
(式中、大文字はβ-D-オキシ-LNAモノマーを表し、小文字はDNAモノマーを表し、下付文字「s」はホスホロチオエート結合を表し、およびMeCは5-メチルシトシン塩基を含むβ-D-オキシ-LNAモノマーを表す)
から選択される連続するヌクレオチド配列からなるか、またはそれを含む、請求項１〜１０のいずれか１項に記載のオリゴマー。 - 請求項１〜１１のいずれか１項に記載のオリゴマーと、該オリゴマーに共有結合した少なくとも1個の非ヌクレオチドまたは非ポリヌクレオチド部分とを含むコンジュゲート。
- 請求項１〜１１のいずれか１項に記載のオリゴマー、または請求項１２に記載のコンジュゲートと、製薬上許容し得る希釈剤、担体、塩もしくはアジュバントとを含む医薬組成物。
- 本明細書に開示される疾患または医学的障害の治療のための医薬の製造のための、請求項１〜１１のいずれか１項に記載のオリゴマー、または請求項１２に定義されるコンジュゲートを含む組成物。
- 過増殖性障害の治療のための医薬組成物であって、該治療が、請求項１〜１１のいずれか１項に記載のオリゴマー、または請求項１２に記載のコンジュゲートの有効量を、過増殖性障害に罹患している患者、またはかかる過増殖性障害に罹患しやすい患者に投与することを含む、前記医薬組成物。
- アンドロゲン受容体を発現している細胞中のアンドロゲン受容体を阻害する方法であって、請求項１〜１１のいずれか１項に記載のオリゴマー、または請求項１２に記載のコンジュゲートを、該細胞に投与して、該細胞中のアンドロゲン受容体を阻害することを含む、前記方法。
- 癌の治療のための医薬の製造のための、請求項１〜１１のいずれか１項に記載のオリゴマー、または請求項１２に定義されるコンジュゲートを含む組成物。
- 以下の式：
5'-A s Me C s Me C s a s a s g s t s t s t s c s t s t s c s A s G s Me C-3'(配列番号58)または
5'- Me C s Me C s Me C s a s a s g s g s c s a s c s t s g s c s A s G s A-3'(配列番号77)
(式中、大文字はβ-D-オキシ-LNAモノマーを表し、小文字はDNAモノマーを表し、下付文字「s」はホスホロチオエート結合を表し、および Me Cは5-メチルシトシン塩基を含むβ-D-オキシ-LNAモノマーを表す)
からなるオリゴマーを含み、1個以上の官能基が5'末端、3'末端、リボース糖の2'-OH、および塩基から独立に選択される1個以上の位置で該オリゴマーに共有結合している、活性化オリゴマー。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99012507P | 2007-11-26 | 2007-11-26 | |
| US60/990,125 | 2007-11-26 | ||
| PCT/DK2008/000417 WO2009068033A2 (en) | 2007-11-26 | 2008-11-26 | Lna antagonists targeting the androgen receptor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015208689A Division JP2016105703A (ja) | 2007-11-26 | 2015-10-23 | アンドロゲン受容体を標的化するｌｎａアンタゴニスト |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011504362A JP2011504362A (ja) | 2011-02-10 |
| JP2011504362A5 true JP2011504362A5 (ja) | 2011-12-08 |
| JP5872162B2 JP5872162B2 (ja) | 2016-03-01 |
Family
ID=40379703
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010534367A Expired - Fee Related JP5872162B2 (ja) | 2007-11-26 | 2008-11-26 | アンドロゲン受容体を標的化するｌｎａアンタゴニスト |
| JP2015208689A Pending JP2016105703A (ja) | 2007-11-26 | 2015-10-23 | アンドロゲン受容体を標的化するｌｎａアンタゴニスト |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015208689A Pending JP2016105703A (ja) | 2007-11-26 | 2015-10-23 | アンドロゲン受容体を標的化するｌｎａアンタゴニスト |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US7737125B2 (ja) |
| EP (1) | EP2225377B1 (ja) |
| JP (2) | JP5872162B2 (ja) |
| KR (1) | KR20100110298A (ja) |
| CN (1) | CN101932709B (ja) |
| AU (1) | AU2008329327B2 (ja) |
| BR (1) | BRPI0820508A2 (ja) |
| CA (1) | CA2705714A1 (ja) |
| DK (1) | DK2225377T3 (ja) |
| EA (1) | EA020026B1 (ja) |
| ES (1) | ES2456990T3 (ja) |
| IL (2) | IL205944A (ja) |
| MX (1) | MX2010005703A (ja) |
| NZ (1) | NZ585327A (ja) |
| TW (1) | TW200930382A (ja) |
| UA (1) | UA100253C2 (ja) |
| WO (1) | WO2009068033A2 (ja) |
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| JP2010503414A (ja) | 2006-09-15 | 2010-02-04 | エンゾン ファーマスーティカルズ インコーポレイテッド | 正に荷電した部分を含有するポリマー複合体 |
| US9398493B2 (en) | 2006-10-30 | 2016-07-19 | Nokia Technologies Oy | Method, apparatus, and system providing operator controlled mobility for user equipment |
| JP5168944B2 (ja) | 2007-02-28 | 2013-03-27 | 三浦工業株式会社 | 羽根車式流量計 |
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2008
- 2008-11-26 UA UAA201007942A patent/UA100253C2/uk unknown
- 2008-11-26 CN CN200880125544.3A patent/CN101932709B/zh not_active Expired - Fee Related
- 2008-11-26 JP JP2010534367A patent/JP5872162B2/ja not_active Expired - Fee Related
- 2008-11-26 BR BRPI0820508A patent/BRPI0820508A2/pt not_active IP Right Cessation
- 2008-11-26 US US12/324,033 patent/US7737125B2/en not_active Expired - Fee Related
- 2008-11-26 ES ES08855697.2T patent/ES2456990T3/es active Active
- 2008-11-26 MX MX2010005703A patent/MX2010005703A/es active IP Right Grant
- 2008-11-26 AU AU2008329327A patent/AU2008329327B2/en not_active Ceased
- 2008-11-26 DK DK08855697.2T patent/DK2225377T3/da active
- 2008-11-26 EA EA201070660A patent/EA020026B1/ru not_active IP Right Cessation
- 2008-11-26 NZ NZ585327A patent/NZ585327A/xx not_active IP Right Cessation
- 2008-11-26 KR KR1020107012993A patent/KR20100110298A/ko not_active Application Discontinuation
- 2008-11-26 TW TW097145706A patent/TW200930382A/zh unknown
- 2008-11-26 CA CA2705714A patent/CA2705714A1/en not_active Abandoned
- 2008-11-26 EP EP08855697.2A patent/EP2225377B1/en active Active
- 2008-11-26 WO PCT/DK2008/000417 patent/WO2009068033A2/en active Application Filing
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2010
- 2010-03-18 US US12/726,554 patent/US7989429B2/en not_active Expired - Fee Related
- 2010-05-25 IL IL205944A patent/IL205944A/en not_active IP Right Cessation
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2011
- 2011-05-31 US US13/149,155 patent/US20110319471A1/en not_active Abandoned
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2012
- 2012-10-11 IL IL222397A patent/IL222397A/en not_active IP Right Cessation
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2015
- 2015-10-23 JP JP2015208689A patent/JP2016105703A/ja active Pending
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