JP2014525435A5 - - Google Patents
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- JP2014525435A5 JP2014525435A5 JP2014527791A JP2014527791A JP2014525435A5 JP 2014525435 A5 JP2014525435 A5 JP 2014525435A5 JP 2014527791 A JP2014527791 A JP 2014527791A JP 2014527791 A JP2014527791 A JP 2014527791A JP 2014525435 A5 JP2014525435 A5 JP 2014525435A5
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- 239000000203 mixture Substances 0.000 claims 19
- 239000003795 chemical substances by application Substances 0.000 claims 16
- 230000025458 RNA interference Effects 0.000 claims 15
- 125000003729 nucleotide group Chemical group 0.000 claims 12
- 102100003632 HSF1 Human genes 0.000 claims 11
- 108060003800 Hsf Proteins 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 230000000692 anti-sense Effects 0.000 claims 9
- 239000002773 nucleotide Substances 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 5
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol 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 4
- WQLVFSAGQJTQCK-VKROHFNGSA-N Diosgenin Natural products O([C@@H]1[C@@H]([C@]2(CC[C@@H]3[C@@]4(C)CC[C@H](O)CC4=CC[C@H]3[C@@H]2C1)C)[C@@H]1C)[C@]11CC[C@@H](C)CO1 WQLVFSAGQJTQCK-VKROHFNGSA-N 0.000 claims 4
- GMBQZIIUCVWOCD-WWASVFFGSA-N Sarsapogenine Chemical compound O([C@@H]1[C@@H]([C@]2(CC[C@@H]3[C@@]4(C)CC[C@H](O)C[C@H]4CC[C@H]3[C@@H]2C1)C)[C@@H]1C)[C@]11CC[C@H](C)CO1 GMBQZIIUCVWOCD-WWASVFFGSA-N 0.000 claims 4
- 150000001720 carbohydrates Chemical class 0.000 claims 4
- 235000014633 carbohydrates Nutrition 0.000 claims 4
- QOLRLLFJMZLYQJ-GSSCIUJHSA-N Hecogenin Natural products O=C1[C@]2(C)[C@H]3[C@H](C)[C@@]4(O[C@H]3C[C@H]2[C@@H]2[C@@H]([C@]3(C)[C@H](C[C@@H](O)CC3)CC2)C1)OC[C@H](C)CC4 QOLRLLFJMZLYQJ-GSSCIUJHSA-N 0.000 claims 3
- 229920000972 Sense strand Polymers 0.000 claims 3
- 208000001756 Virus Disease Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229920002101 Chitin Polymers 0.000 claims 2
- DJHJJVWPFGHIPH-OODMECLYSA-N Chitin Chemical compound O[C@@H]1C(NC(=O)C)[C@H](O)OC(CO)[C@H]1COC[C@H]1C(NC(C)=O)[C@@H](O)[C@H](COC[C@H]2C([C@@H](O)[C@H](O)C(CO)O2)NC(C)=O)C(CO)O1 DJHJJVWPFGHIPH-OODMECLYSA-N 0.000 claims 2
- 229920001661 Chitosan Polymers 0.000 claims 2
- 229940107161 Cholesterol Drugs 0.000 claims 2
- 229920000858 Cyclodextrin Polymers 0.000 claims 2
- 229920002307 Dextran Polymers 0.000 claims 2
- 229920001202 Inulin Polymers 0.000 claims 2
- JYJIGFIDKWBXDU-MNNPPOADSA-N Inulin Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)OC[C@]1(OC[C@]2(OC[C@]3(OC[C@]4(OC[C@]5(OC[C@]6(OC[C@]7(OC[C@]8(OC[C@]9(OC[C@]%10(OC[C@]%11(OC[C@]%12(OC[C@]%13(OC[C@]%14(OC[C@]%15(OC[C@]%16(OC[C@]%17(OC[C@]%18(OC[C@]%19(OC[C@]%20(OC[C@]%21(OC[C@]%22(OC[C@]%23(OC[C@]%24(OC[C@]%25(OC[C@]%26(OC[C@]%27(OC[C@]%28(OC[C@]%29(OC[C@]%30(OC[C@]%31(OC[C@]%32(OC[C@]%33(OC[C@]%34(OC[C@]%35(OC[C@]%36(O[C@@H]%37[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O%37)O)[C@H]([C@H](O)[C@@H](CO)O%36)O)[C@H]([C@H](O)[C@@H](CO)O%35)O)[C@H]([C@H](O)[C@@H](CO)O%34)O)[C@H]([C@H](O)[C@@H](CO)O%33)O)[C@H]([C@H](O)[C@@H](CO)O%32)O)[C@H]([C@H](O)[C@@H](CO)O%31)O)[C@H]([C@H](O)[C@@H](CO)O%30)O)[C@H]([C@H](O)[C@@H](CO)O%29)O)[C@H]([C@H](O)[C@@H](CO)O%28)O)[C@H]([C@H](O)[C@@H](CO)O%27)O)[C@H]([C@H](O)[C@@H](CO)O%26)O)[C@H]([C@H](O)[C@@H](CO)O%25)O)[C@H]([C@H](O)[C@@H](CO)O%24)O)[C@H]([C@H](O)[C@@H](CO)O%23)O)[C@H]([C@H](O)[C@@H](CO)O%22)O)[C@H]([C@H](O)[C@@H](CO)O%21)O)[C@H]([C@H](O)[C@@H](CO)O%20)O)[C@H]([C@H](O)[C@@H](CO)O%19)O)[C@H]([C@H](O)[C@@H](CO)O%18)O)[C@H]([C@H](O)[C@@H](CO)O%17)O)[C@H]([C@H](O)[C@@H](CO)O%16)O)[C@H]([C@H](O)[C@@H](CO)O%15)O)[C@H]([C@H](O)[C@@H](CO)O%14)O)[C@H]([C@H](O)[C@@H](CO)O%13)O)[C@H]([C@H](O)[C@@H](CO)O%12)O)[C@H]([C@H](O)[C@@H](CO)O%11)O)[C@H]([C@H](O)[C@@H](CO)O%10)O)[C@H]([C@H](O)[C@@H](CO)O9)O)[C@H]([C@H](O)[C@@H](CO)O8)O)[C@H]([C@H](O)[C@@H](CO)O7)O)[C@H]([C@H](O)[C@@H](CO)O6)O)[C@H]([C@H](O)[C@@H](CO)O5)O)[C@H]([C@H](O)[C@@H](CO)O4)O)[C@H]([C@H](O)[C@@H](CO)O3)O)[C@H]([C@H](O)[C@@H](CO)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 JYJIGFIDKWBXDU-MNNPPOADSA-N 0.000 claims 2
- 229940029339 Inulin Drugs 0.000 claims 2
- SMEROWZSTRWXGI-HVATVPOCSA-N Lithocholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 SMEROWZSTRWXGI-HVATVPOCSA-N 0.000 claims 2
- 101700080605 NUC1 Proteins 0.000 claims 2
- 229920001218 Pullulan Polymers 0.000 claims 2
- 239000004373 Pullulan Substances 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 239000011230 binding agent Substances 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims 2
- 229920002674 hyaluronan Polymers 0.000 claims 2
- 229960003160 hyaluronic acid Drugs 0.000 claims 2
- 102000006495 integrins Human genes 0.000 claims 2
- 108010044426 integrins Proteins 0.000 claims 2
- 239000002523 lectin Substances 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 150000002634 lipophilic molecules Chemical class 0.000 claims 2
- 229920005615 natural polymer Polymers 0.000 claims 2
- 101700006494 nucA Proteins 0.000 claims 2
- 229920000768 polyamine Polymers 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 230000036678 protein binding Effects 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 235000019423 pullulan Nutrition 0.000 claims 2
- 150000003230 pyrimidines Chemical class 0.000 claims 2
- MAKUBRYLFHZREJ-JWBQXVCJSA-M sodium;(2S,3S,4R,5R,6R)-3-[(2S,3R,5S,6R)-3-acetamido-5-hydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5,6-trihydroxyoxane-2-carboxylate Chemical compound [Na+].CC(=O)N[C@@H]1C[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](C([O-])=O)O[C@@H](O)[C@H](O)[C@H]1O MAKUBRYLFHZREJ-JWBQXVCJSA-M 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- 150000003505 terpenes Chemical class 0.000 claims 2
- 235000007586 terpenes Nutrition 0.000 claims 2
- 150000003648 triterpenes Chemical class 0.000 claims 2
- 239000011782 vitamin Substances 0.000 claims 2
- 235000013343 vitamin Nutrition 0.000 claims 2
- 229930003231 vitamins Natural products 0.000 claims 2
- SWDZPNJZKUGIIH-QQTULTPQSA-N (5Z)-N-ethyl-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-[4-(morpholin-4-ylmethyl)phenyl]-2H-1,2-oxazole-3-carboxamide Chemical group O1NC(C(=O)NCC)=C(C=2C=CC(CN3CCOCC3)=CC=2)\C1=C1/C=C(C(C)C)C(O)=CC1=O SWDZPNJZKUGIIH-QQTULTPQSA-N 0.000 claims 1
- 239000004971 Cross linker Substances 0.000 claims 1
- OFMXGFHWLZPCFL-ACRUQRPVSA-N Friedelan-3-one Natural products C([C@H]1[C@]2(C)CC[C@@]34C)C(C)(C)CC[C@]1(C)CC[C@]2(C)[C@H]4CC[C@@]1(C)[C@H]3CCC(=O)[C@H]1C OFMXGFHWLZPCFL-ACRUQRPVSA-N 0.000 claims 1
- 101710015954 HVA1 Proteins 0.000 claims 1
- QOLRLLFJMZLYQJ-LOBDNJQFSA-N Hecogenin Chemical compound O([C@@H]1[C@@H]([C@]2(C(=O)C[C@@H]3[C@@]4(C)CC[C@H](O)C[C@@H]4CC[C@H]3[C@@H]2C1)C)[C@@H]1C)[C@]11CC[C@@H](C)CO1 QOLRLLFJMZLYQJ-LOBDNJQFSA-N 0.000 claims 1
- 101700065814 LEA2 Proteins 0.000 claims 1
- 101700021338 LEC Proteins 0.000 claims 1
- 101700077545 LECC Proteins 0.000 claims 1
- 101700028499 LECG Proteins 0.000 claims 1
- 101700063913 LECT Proteins 0.000 claims 1
- 102000004856 Lectins Human genes 0.000 claims 1
- 108090001090 Lectins Proteins 0.000 claims 1
- 101710034340 Os04g0173800 Proteins 0.000 claims 1
- 102000004338 Transferrin Human genes 0.000 claims 1
- 108090000901 Transferrin Proteins 0.000 claims 1
- 229940029983 VITAMINS Drugs 0.000 claims 1
- 229940088594 Vitamin Drugs 0.000 claims 1
- 229940021016 Vitamin IV solution additives Drugs 0.000 claims 1
- 239000003431 cross linking reagent Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- OFMXGFHWLZPCFL-SVRPQWSVSA-N friedelin Chemical compound C([C@H]1[C@]2(C)CC[C@@]34C)C(C)(C)CC[C@]1(C)CC[C@]2(C)[C@H]4CC[C@@]1(C)[C@H]3CCC(=O)[C@@H]1C OFMXGFHWLZPCFL-SVRPQWSVSA-N 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 1
- 101700036391 lecA Proteins 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 101700001016 mbhA Proteins 0.000 claims 1
- 239000000816 peptidomimetic Substances 0.000 claims 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 1
- 239000012581 transferrin Substances 0.000 claims 1
- 150000003722 vitamin derivatives Chemical class 0.000 claims 1
Claims (21)
- センス鎖およびアンチセンス鎖を含むＲＮＡｉ剤を含む組成物であって、該アンチセンス鎖は、表１において提供されるＨＳＦ１に対して特異的なＲＮＡｉ剤のアンチセンス鎖と０、１、２または３個のヌクレオチドにより異なっている少なくとも１５個の連続したヌクレオチドを含む、組成物。
- ＨＳＦ１に対する第２のＲＮＡｉ剤をさらに含む、請求項１に記載の組成物。
- ＲＮＡｉ剤が、少なくとも１つの修飾骨格および／または少なくとも１つの２’−修飾ヌクレオチドを含む、請求項１に記載の組成物。
- ＲＮＡｉ剤が、１つ以上の診断化合物、レポーター基、架橋剤、ヌクレアーゼ耐性付与部分、天然もしくは異常核酸塩基、親油性分子、コレステロール、脂質、レクチン、ステロイド、ウバオール（ｕｖａｏｌ）、ヘコゲニン、ジオスゲニン、テルペン、トリテルペン、サルササポゲニン、フリーデリン（Ｆｒｉｅｄｅｌｉｎ）、エピフリーデラノール誘導体化リトコール酸、ビタミン、炭水化物、デキストラン、プルラン、キチン、キトサン、合成炭水化物、オリゴラクテート（ｏｌｉｇｏ ｌａｃｔａｔｅ）１５−マー（ｍｅｒ）、天然ポリマー、低もしくは中間分子量ポリマー、イヌリン、シクロデキストリン、ヒアルロン酸、タンパク質、タンパク質−結合剤、インテグリン標的分子、ポリカチオン、ペプチド、ポリアミン、ペプチド模倣物および／またはトランスフェリンから選択される１つ以上の薬剤に結合している、請求項１に記載の組成物。
- 第１の鎖および第２の鎖を含むＲＮＡｉ剤を含む組成物であって、該第１の鎖および第２の鎖は、表Ａ１において提供されるＨＳＦ１に対して特異的なＲＮＡｉ剤の第１および第２の鎖のそれぞれと０、１、２または３個のヌクレオチドにより異なっている少なくとも１５個の連続したヌクレオチドを含む、組成物。
- ＨＳＦ１に対する第２のＲＮＡｉ剤を含む、請求項１に記載の組成物。
- ＲＮＡｉ剤がホスホロチオエートおよび／または２’−修飾ヌクレオチドを含む、請求項１に記載の組成物。
- ＲＮＡｉ剤が、１つ以上の薬剤に結合しており、該薬剤が、１つ以上の診断化合物、レポーター基、架橋剤、ヌクレアーゼ耐性付与部分、天然もしくは異常核酸塩基、親油性分子、コレステロール、脂質、レクチン、ステロイド、ウバオール、ヘコゲニン、ジオスゲニン、テルペン、トリテルペン、サルササポゲニン、フリーデリン、エピフリーデラノール誘導体化リトコール酸、ビタミン、炭水化物、デキストラン、プルラン、キチン、キトサン、合成炭水化物、オリゴラクテート １５−マー、天然ポリマー、低もしくは中間分子量ポリマー、イヌリン、シクロデキストリン、ヒアルロン酸、タンパク質、タンパク質−結合剤、インテグリン標的分子、ポリカチオン、ペプチド、ポリアミン、ペプチド模倣物および／またはトランスフェリンから選択される、請求項１に記載の組成物。
- 個体におけるＨＳＦ１−関連疾患を処置するための、センス鎖およびアンチセンス鎖を含む治療有効量のＲＮＡｉ剤を含む医薬組成物であって、
該アンチセンス鎖は、表１において提供されるＨＳＦ１に対して特異的なＲＮＡｉ剤のアンチセンス鎖と０、１、２または３個のヌクレオチドにより異なっている少なくとも１５個の連続したヌクレオチドを含み、
該組成物の治療上有効量は該個体に投与される、医薬組成物。 - ＨＳＦ１−関連疾患が、がん、自己免疫またはウイルス性疾患である、請求項９に医薬組成物。
- がん、自己免疫またはウイルス性疾患に対するさらなる処置を施す工程をさらに含む、請求項９に記載の医薬組成物。
- ＨＳＦ１に対するさらなるＲＮＡｉ剤がさらに投与される、請求項１１に記載の医薬組成物。
- 個体におけるＨＳＦ１遺伝子の発現を阻害するための、センス鎖およびアンチセンス鎖を含む治療有効量のＲＮＡｉ剤を含む組成物であって、
該アンチセンス鎖は、表Ａ１において提供されるＨＳＦ１に対して特異的なＲＮＡｉ剤のアンチセンス鎖と０、１、２または３個のヌクレオチドにより異なっている少なくとも１５個の連続したヌクレオチドを含み、
該組成物の治療上有効量は該個体に投与される、医薬組成物。 - ＨＳＦ１−関連疾患が、がん、自己免疫またはウイルス性疾患である、請求項１３に記載の医薬組成物。
- 薬学的に有効な製剤中の請求項９〜１４のいずれか１項に記載の医薬組成物。
- 個体におけるＨＳＦ１−関連疾患を処置するための請求項１に記載の組成物であって、治療有効量の請求項１に記載の組成物は該個体に投与される、組成物。
- ＨＳＦ１−関連疾患の処置のための医薬の製造における請求項１に記載の組成物の使用。
- 全てのピリミジンが、２’Ｏ−メチル−修飾ヌクレオチドである、請求項１に記載の組成物。
- 全てのピリミジンが、２’Ｏ−メチル−修飾ヌクレオチドである、請求項５に記載の組成物。
- ＨＳＰ９０阻害剤の投与がさらなる処置として使用される、請求項１１に記載の医薬組成物。
- ＨＳＰ９０阻害剤が、ＡＵＹ９２２である、請求項２０に記載の医薬組成物。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161530532P | 2011-09-02 | 2011-09-02 | |
| US61/530,532 | 2011-09-02 | ||
| US201261598453P | 2012-02-14 | 2012-02-14 | |
| US61/598,453 | 2012-02-14 | ||
| PCT/IB2012/054455 WO2013030778A2 (en) | 2011-09-02 | 2012-08-30 | Organic compositions to treat hsf1-related diseases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018168244A Division JP2019001813A (ja) | 2011-09-02 | 2018-09-07 | Ｈｓｆ１関連疾患を処置するための有機組成物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014525435A JP2014525435A (ja) | 2014-09-29 |
| JP2014525435A5 true JP2014525435A5 (ja) | 2015-10-15 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014527791A Pending JP2014525435A (ja) | 2011-09-02 | 2012-08-30 | Ｈｓｆ１関連疾患を処置するための有機組成物 |
| JP2018168244A Pending JP2019001813A (ja) | 2011-09-02 | 2018-09-07 | Ｈｓｆ１関連疾患を処置するための有機組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018168244A Pending JP2019001813A (ja) | 2011-09-02 | 2018-09-07 | Ｈｓｆ１関連疾患を処置するための有機組成物 |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US20160032284A1 (ja) |
| EP (3) | EP3521432A1 (ja) |
| JP (2) | JP2014525435A (ja) |
| KR (1) | KR20140057374A (ja) |
| CN (1) | CN103930547A (ja) |
| AU (1) | AU2016202437B2 (ja) |
| BR (1) | BR112014005103A2 (ja) |
| CA (2) | CA3185394A1 (ja) |
| EA (1) | EA201490553A1 (ja) |
| MX (1) | MX2014002536A (ja) |
| WO (1) | WO2013030778A2 (ja) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
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- 2012-08-30 EA EA201490553A patent/EA201490553A1/ru unknown
- 2012-08-30 CN CN201280053243.0A patent/CN103930547A/zh active Pending
- 2012-08-30 JP JP2014527791A patent/JP2014525435A/ja active Pending
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