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公开(公告)号：US06746690B2
公开(公告)日：2004-06-08
申请号：US10294865
申请日：2002-11-14
IPC分类号： A61K9127
CPC分类号： A61K31/7088 , A61K9/19 , A61K31/70 , A61K47/541
摘要： A method for producing a composition including a nucleic-acid-containing complex is characterized in that two single strand nucleic acid polymers which can at least partly form double strands are separately mixed, in a single strand form, with a cationic carrier or with source materials for the cationic carrier before the cationic carrier is formed. The resulting mixture is then dispersed in water during the production process of the nucleic-acid-containing complex.
摘要翻译： 制备包含含核酸复合物的组合物的方法的特征在于，可以至少部分形成双链的两条单链核酸聚合物以单链形式与阳离子载体或源材料分开混合 在阳离子载体形成之前为阳离子载体。 然后将所得混合物在含核酸复合物的制备过程中分散在水中。
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公开(公告)号：US06545138B1
公开(公告)日：2003-04-08
申请号：US09701072
申请日：2000-11-20
IPC分类号： C07H2104
CPC分类号： A61K31/7088 , A61K9/19 , A61K31/70 , A61K47/541
摘要： A method for producing a composition including a nucleic-acid-containing complex is characterized in that two single strand nucleic acid polymers which can at least partly form double strands are separately mixed, in a single strand form, with a cationic carrier or with source materials for the cationic carrier before the cationic carrier is formed. The resulting mixture is then dispersed in water during the production process of the nucleic-acid-containing complex.
摘要翻译： 制备包含含核酸复合物的组合物的方法的特征在于，可以至少部分形成双链的两条单链核酸聚合物以单链形式与阳离子载体或源材料分开混合 在阳离子载体形成之前为阳离子载体。 然后将所得混合物在含核酸复合物的制备过程中分散在水中。
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公开(公告)号：US07205282B1
公开(公告)日：2007-04-17
申请号：US09646135
申请日：1999-03-23
申请人： Kazuko Hirabayashi , Junzo Seki
发明人： Kazuko Hirabayashi , Junzo Seki
CPC分类号： A61K9/1272 , A61K9/127 , A61K47/6911
摘要： The object of the present invention is to provide a novel medicinal agent useful in the treatment or the prevention of hepatitis.The present invention is, for example, a therapeutic or preventive agent for hepatitis characterized in that it comprises a complex of a drug carrier consisting essentially of 2-O-(2-diethylaminoethyl)-carbamoyl-1,3-O-dioleoylglycerol and a phospholipid with poly(I).poly(C).
摘要翻译： 本发明的目的是提供一种可用于治疗或预防肝炎的新型药剂。
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4.发明申请Oligo Double-Stranded Rna Inhibiting the Expression of Bcl-2 and Pharmaceutical Composition Containing the Same 审中-公开Oligo双链Rna抑制Bcl-2的表达和含有它的药物组合物公开(公告)号：US20080020990A1
公开(公告)日：2008-01-24
申请号：US10559083
申请日：2004-05-28
IPC分类号： A61K31/7105 , A61K48/00 , A61P35/00 , A61P7/00 , C07H21/02
CPC分类号： C12N15/1135 , A61K31/7105 , C12N2310/14
摘要： The present invention relates to oligo double-stranded RNAs for use in knockdown of the expression of Bcl-2 protein known as a suppressor for apoptosis, and pharmaceutical compositions containing them. It is known that Bcl-2 protein is over-expressed in diseases such as cancer, and by this over-expression, the growth of cancer cells is continued and the drug resistance to anti-cancer agents is caused. The present invention provides highly active oligo double-stranded RNAs cleaving bcl-2 mRNA and further provides pharmaceutical compositions comprising a complex of the oligo double-stranded RNA and a suitable carrier for inhibiting the expression of Bcl-2 protein.
摘要翻译： 本发明涉及用于敲低已知为凋亡抑制剂的Bcl-2蛋白的表达的寡聚双链RNA，以及含有它们的药物组合物。 已知Bcl-2蛋白在诸如癌症的疾病中过度表达，并且由于这种过度表达，癌细胞的生长继续进行，并且导致对抗癌剂的耐药性。 本发明提供了切割bcl-2 mRNA的高活性寡聚双链RNA，并进一步提供了包含寡聚双链RNA和用于抑制Bcl-2蛋白表达的合适载体的复合物的药物组合物。
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5.发明申请Oligonucleic acid-bearing composite and pharmaceutical composition containing the composite 审中-公开含有寡核苷酸的复合材料和含有复合材料的药物组合物公开(公告)号：US20070042979A1
公开(公告)日：2007-02-22
申请号：US10559084
申请日：2004-05-28
CPC分类号： C12N15/1135 , A61K9/1272 , A61K31/7088 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： The present invention provides a complex, which comprises a cationic liposome comprising 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoylglycerol and a phospholipid as main ingredients, and an oligo nucleic acid which is carried on the liposome. Also, the present invention provides a pharmaceutical composition containing the complex to be used for treating or preventing diseases caused by a target molecule of the oligo nucleic acid (target DNA, target RNA, target protein) since it is possible to administer the complex in vivo and to put the complex into practical use as a medicament because the complex can exhibit pharmacological efficacy in vivo.
摘要翻译： 本发明提供了一种复合物，其包含2-O-（2-二乙基氨基乙基）氨基甲酰基-1,3-O-二油酰甘油和磷脂作为主要成分的阳离子脂质体和携带在脂质体上的寡核酸。 此外，本发明提供了含有用于治疗或预防由寡核酸（靶DNA，靶RNA，靶蛋白）的靶分子引起的疾病的复合物的药物组合物，因为可以在体内施用复合物 并将复合物作为药物实际使用，因为该复合物可以在体内具有药理学功效。
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6.发明申请OLIGONUCLEIC ACID-BEARING COMPOSITE AND PHARMACEUTICAL COMPOSITION CONTAINING THE COMPOSITE 审中-公开含有复合材料的聚氨酯酸酯复合材料和药物组合物公开(公告)号：US20090123532A1
公开(公告)日：2009-05-14
申请号：US12277085
申请日：2008-11-24
CPC分类号： C12N15/1135 , A61K9/1272 , A61K31/7088 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： The present invention provides a complex, which comprises a cationic liposome comprising 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoylglycerol and a phospholipid as main ingredients, and an oligo nucleic acid which is carried on the liposome. Also, the present invention provides a pharmaceutical composition containing the complex to be used for treating or preventing diseases caused by a target molecule of the oligo nucleic acid (target DNA, target RNA, target protein) since it is possible to administer the complex in vivo and to put the complex into practical use as a medicament because the complex can exhibit pharmacological efficacy in vivo.
摘要翻译： 本发明提供了一种复合物，其包含2-O-（2-二乙基氨基乙基）氨基甲酰基-1,3-O-二油酰甘油和磷脂作为主要成分的阳离子脂质体和携带在脂质体上的寡核酸。 此外，本发明提供了含有用于治疗或预防由寡核酸（靶DNA，靶RNA，靶蛋白）的靶分子引起的疾病的复合物的药物组合物，因为可以在体内施用复合物 并将复合物作为药物实际使用，因为该复合物可以在体内具有药理学功效。
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公开(公告)号：US20050014942A1
公开(公告)日：2005-01-20
申请号：US10494622
申请日：2002-10-29
IPC分类号： A61K31/404 , A61K31/437 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , C07D209/18 , C07D209/24 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D253/08 , C07D487/02
CPC分类号： C07D401/14 , A61K31/404 , A61K31/437 , A61K31/454 , A61K31/4725 , A61K31/496 , A61K31/497 , C07D209/18 , C07D209/24 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention provides an amide derivative represented by the following formula [1]: wherein n represents 0 or 1; X represents CR4 or N; Y represents CR6 or N; Z represents CR7 or N; R1 and R2 may be the same or different and each represents hydrogen, optionally substituted alkyl, acyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogen, hydroxy, amino, alkyl, haloalkyl, alkoxy, monoalkylamino, dialkylamino, arylalkyl, cyano, or nitro; and R3 represents optionally substituted alkylamino, optionally substituted arylamino, or optionally substituted cyclic amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising them as an active ingredient. The compound of the present invention is useful as a TGF-β inhibitor.
摘要翻译： 本发明提供由下式[1]表示的酰胺衍生物：其中n表示0或1; X表示CR 4或N; Y表示CR 6或N; Z表示CR 7或N; R 1和R 2可以相同或不同，各自表示氢，任选取代的烷基，酰基，任选取代的芳基或任选取代的芳族杂环基; R 4，R 5，R 6和R 7可以相同或不同，各自表示氢，卤素，羟基，氨基，烷基，卤代烷基，烷氧基，单烷基氨基，二烷基氨基，芳基烷基，氰基， 或硝基; 和R 3表示任选取代的烷基氨基，任选取代的芳基氨基或任选取代的环状氨基或其药学上可接受的盐，以及包含它们作为活性成分的药物组合物。 本发明的化合物可用作TGF-β抑制剂。
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公开(公告)号：US5559102A
公开(公告)日：1996-09-24
申请号：US181231
申请日：1994-01-13
IPC分类号： C07H19/20 , A61K31/70 , C07H19/167 , C07H19/173
CPC分类号： C07H19/20
摘要： Cyclic AMP and cyclic GMP derivatives, such as 8-bromoadenosine-3', 5'-cyclic methylphosphonate, are effective in inhibiting phosphodiesterases.
摘要翻译： 环状AMP和环状GMP衍生物，如8-溴腺苷-3'，5'-环状甲基膦酸酯，对抑制磷酸二酯酶有效。
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