JP2015503608A5 - - Google Patents
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- JP2015503608A5 JP2015503608A5 JP2014551706A JP2014551706A JP2015503608A5 JP 2015503608 A5 JP2015503608 A5 JP 2015503608A5 JP 2014551706 A JP2014551706 A JP 2014551706A JP 2014551706 A JP2014551706 A JP 2014551706A JP 2015503608 A5 JP2015503608 A5 JP 2015503608A5
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- cancer
- rnai agent
- beta
- composition
- catenin
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- 239000003795 chemical substances by application Substances 0.000 claims 19
- 239000000203 mixture Substances 0.000 claims 19
- 230000025458 RNA interference Effects 0.000 claims 18
- 125000003729 nucleotide group Chemical group 0.000 claims 14
- 230000000692 anti-sense Effects 0.000 claims 12
- 102000015735 beta Catenin Human genes 0.000 claims 11
- 108060000903 beta Catenin Proteins 0.000 claims 11
- 239000002773 nucleotide Substances 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 206010038389 Renal cancer Diseases 0.000 claims 6
- 201000010982 kidney cancer Diseases 0.000 claims 6
- 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 Chemical compound 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
- 229920000972 Sense strand Polymers 0.000 claims 4
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- 102000004196 processed proteins & peptides Human genes 0.000 claims 4
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- 206010006187 Breast cancer Diseases 0.000 claims 3
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- 206010025650 Malignant melanoma Diseases 0.000 claims 3
- 208000000172 Medulloblastoma Diseases 0.000 claims 3
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 3
- 208000001132 Osteoporosis Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 3
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- 201000005290 uterine carcinosarcoma Diseases 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
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- 229920002307 Dextran Polymers 0.000 claims 2
- -1 Epi-Freedelanol Natural products 0.000 claims 2
- 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 2
- 101710015954 HVA1 Proteins 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
- 101700065814 LEA2 Proteins 0.000 claims 2
- 101700021338 LEC Proteins 0.000 claims 2
- 101700077545 LECC Proteins 0.000 claims 2
- 101700028499 LECG Proteins 0.000 claims 2
- 101700063913 LECT Proteins 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
- 101710034340 Os04g0173800 Proteins 0.000 claims 2
- 229920001218 Pullulan Polymers 0.000 claims 2
- 239000004373 Pullulan Substances 0.000 claims 2
- 102000004338 Transferrin Human genes 0.000 claims 2
- 108090000901 Transferrin Proteins 0.000 claims 2
- 229940088594 Vitamin Drugs 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 239000002253 acid Substances 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
- 239000003431 cross linking reagent Substances 0.000 claims 2
- 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 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
- 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 2
- 101700036391 lecA 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
- 101700001016 mbhA Proteins 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
- 239000012581 transferrin Substances 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
- 150000003722 vitamin derivatives Chemical class 0.000 claims 2
- 229930003231 vitamins Natural products 0.000 claims 2
- 230000029663 wound healing Effects 0.000 claims 2
- 238000009472 formulation Methods 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 1
Claims (20)
- センス鎖とアンチセンス鎖とを含むRNAi剤を含む組成物であって、アンチセンス鎖が、表1に示すベータ−カテニンに特異的なRNAi剤のアンチセンス鎖と0、1、2または3ヌクレオチド異なる少なくとも15の連続したヌクレオチドを含む、組成物。
- ベータ−カテニンに対する第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つの改変骨格および/または少なくとも1つの2’−改変ヌクレオチドを含む、請求項1に記載の組成物。
- RNAi剤が、診断用化合物、レポーター基、架橋剤、ヌクレアーゼ耐性付与部分、天然または異常核酸塩基、親脂性分子、コレステロール、脂質、レクチン、ステロイド、ウバオール、ヘシゲニン、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由来リトコール酸、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、オリゴ乳酸15マー、天然ポリマー、低分子量または中分子量ポリマー、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、インテグリンターゲティング分子、ポリカチオン、ペプチド、ポリアミン、模倣ペプチドおよび/またはトランスフェリンから選択される1または複数の作用剤にライゲーションされる、請求項1に記載の組成物。
- 第1鎖と第2鎖とを含むRNAi剤を含む組成物であって、第1鎖および第2鎖が、表1に示すベータ−カテニンに特異的なRNAi剤の第1鎖および第2鎖とそれぞれ0、1、2または3ヌクレオチド異なる少なくとも15の連続したヌクレオチドを含む、組成物。
- ベータ−カテニンに対する第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’−改変ヌクレオチドを含む、請求項1に記載の組成物。
- RNAi剤が、診断用化合物、レポーター基、架橋剤、ヌクレアーゼ耐性付与部分、天然または異常核酸塩基、親脂性分子、コレステロール、脂質、レクチン、ステロイド、ウバオール、ヘシゲニン、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由来リトコール酸、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、オリゴ乳酸15マー、天然ポリマー、低分子量または中分子量ポリマー、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、インテグリンターゲティング分子、ポリカチオン、ペプチド、ポリアミン、模倣ペプチドおよび/またはトランスフェリンから選択される1または複数の作用剤にライゲーションされる、請求項1に記載の組成物。
- 個体においてベータ−カテニン関連疾患を処置するための医薬組成物であって、センス鎖とアンチセンス鎖とを含むRNAi剤を含む治療有効量の組成物を含み、アンチセンス鎖が、表1に示すベータ−カテニンに特異的なRNAi剤のアンチセンス鎖と0、1、2または3ヌクレオチド異なる少なくとも15の連続したヌクレオチドを含む、医薬組成物。
- ベータ−カテニン関連疾患が、大腸腺腫症、結腸直腸癌、基底細胞癌腫、乳癌、腎癌、ウイルムス腫瘍、髄芽腫、卵巣癌、副腎皮質腫瘍、胃癌、肝癌、黒色腫、膵癌、前立腺癌、腎癌、異所性歯牙および味覚乳頭、皮膚癌、石灰化上皮腫、組織非形成性甲状腺癌腫および子宮癌肉腫、部分的無歯症、骨粗鬆症、老化、変性疾患、褥瘡、ならびに慢性創傷および創傷治癒障害から選択される、請求項9に記載の医薬組成物。
- 大腸腺腫症、結腸直腸癌、基底細胞癌腫、乳癌、腎癌、ウイルムス腫瘍、髄芽腫、卵巣癌、副腎皮質腫瘍、胃癌、肝癌、黒色腫、膵癌、前立腺癌、腎癌、異所性歯牙および味覚乳頭、皮膚癌、石灰化上皮腫、組織非形成性甲状腺癌腫および子宮癌肉腫、部分的無歯症、骨粗鬆症、老化、変性疾患、褥瘡および/または慢性創傷および創傷治癒障害のためのさらなる処置と共に用いるための、請求項9に記載の医薬組成物。
- ベータ−カテニンに対するさらなるRNAi剤を含む、請求項11に記載の医薬組成物。
- 個体においてベータ−カテニン遺伝子の発現を阻害するための医薬組成物であって、センス鎖とアンチセンス鎖とを含むRNAi剤を含む治療有効量の組成物を含み、アンチセンス鎖が、表1に示すベータ−カテニンに特異的なRNAi剤のアンチセンス鎖と0、1、2または3ヌクレオチド異なる少なくとも15の連続したヌクレオチドを含む、医薬組成物。
- ベータ−カテニン関連疾患が、大腸腺腫症、結腸直腸癌、基底細胞癌腫、乳癌、腎癌、ウイルムス腫瘍、髄芽腫、卵巣癌、副腎皮質腫瘍、胃癌、肝癌、黒色腫、膵癌、前立腺癌、腎癌、異所性歯牙および味覚乳頭、皮膚癌、石灰化上皮腫、組織非形成性甲状腺癌腫および子宮癌肉腫、部分的無歯症、骨粗鬆症、老化、変性疾患、褥瘡ならびに慢性創傷および/または創傷治癒障害である、請求項13に記載の医薬組成物。
- センス鎖とアンチセンス鎖とを含むRNAi剤を含むRNAi製剤において用いるための医薬であって、アンチセンス鎖が、表1に示すベータ−カテニンに特異的なRNAi剤のアンチセンス鎖と0、1、2または3ヌクレオチド異なる少なくとも15の連続したヌクレオチドを含む医薬。
- 薬学的に有効な製剤中の上記の任意の組成物。
- 治療有効量の請求項1に記載の組成物を個体に投与するステップを含む、個体においてベータ−カテニン関連疾患を処置する方法において用いるための、請求項1に記載の組成物。
- ベータ−カテニン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−改変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−改変ヌクレオチドである、請求項5に記載の組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261584530P | 2012-01-09 | 2012-01-09 | |
US61/584,530 | 2012-01-09 | ||
US201261598530P | 2012-02-14 | 2012-02-14 | |
US61/598,530 | 2012-02-14 | ||
PCT/IB2013/050159 WO2013105022A2 (en) | 2012-01-09 | 2013-01-08 | Organic compositions to treat beta-catenin-related diseases |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015503608A JP2015503608A (ja) | 2015-02-02 |
JP2015503608A5 true JP2015503608A5 (ja) | 2016-03-03 |
JP6158833B2 JP6158833B2 (ja) | 2017-07-05 |
Family
ID=47720548
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2014551706A Active JP6158833B2 (ja) | 2012-01-09 | 2013-01-08 | ベータ−カテニン関連疾患を処置するための有機組成物 |
Country Status (9)
Country | Link |
---|---|
US (2) | US10023862B2 (ja) |
EP (1) | EP2802658A2 (ja) |
JP (1) | JP6158833B2 (ja) |
CN (1) | CN104302768A (ja) |
AU (1) | AU2013208720A1 (ja) |
BR (1) | BR112014016870A2 (ja) |
CA (1) | CA2860676A1 (ja) |
HK (1) | HK1205758A1 (ja) |
WO (1) | WO2013105022A2 (ja) |
Families Citing this family (9)
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2013
- 2013-01-08 AU AU2013208720A patent/AU2013208720A1/en not_active Abandoned
- 2013-01-08 EP EP13704633.0A patent/EP2802658A2/en active Pending
- 2013-01-08 BR BR112014016870A patent/BR112014016870A2/pt not_active IP Right Cessation
- 2013-01-08 CA CA2860676A patent/CA2860676A1/en not_active Abandoned
- 2013-01-08 US US14/371,131 patent/US10023862B2/en active Active
- 2013-01-08 JP JP2014551706A patent/JP6158833B2/ja active Active
- 2013-01-08 CN CN201380013297.9A patent/CN104302768A/zh active Pending
- 2013-01-08 WO PCT/IB2013/050159 patent/WO2013105022A2/en active Application Filing
-
2015
- 2015-07-06 HK HK15106407.7A patent/HK1205758A1/xx unknown
-
2018
- 2018-06-13 US US16/007,517 patent/US20180282728A1/en not_active Abandoned
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