公开(公告)号：US20110045028A1

公开(公告)日：2011-02-24

申请号：US12516536

申请日：2007-11-29

申请人： Satoshi Iinuma ,  Yoshie Iinuma ,  Tomohiro Yoshinari ,  Tsuneaki Tottori

发明人： Satoshi Iinuma ,  Yoshie Iinuma ,  Tomohiro Yoshinari ,  Tsuneaki Tottori

IPC分类号： A61K31/513 ,  A61K9/00 ,  A61P7/02 ,  A61P9/10

CPC分类号： A61K31/506 ,  A61K9/2018 ,  A61K9/2054

摘要： Disclosed is a sustained-release preparation which is prepared by shaping a granule comprising a blood coagulation factor Xa inhibitor and a mixture of at least two hydrophilic polymers. Also disclosed is a pharmaceutical composition comprising a combination of the sustained-release preparation and an immediate release preparation comprising a blood coagulation factor Xa inhibitor. It becomes possible to provide a controlled release preparation comprising a blood coagulation factor Xa inhibitor for the prevention or treatment of thrombosis, which can control the activity of blood coagulation factor Xa for a long term and is excellent in convenience and compliance. It is also becomes possible to provide a method for producing the controlled release preparation.

摘要翻译： 公开了一种缓释制剂，其通过使包含凝血因子Xa抑制剂和至少两种亲水性聚合物的混合物的颗粒成形而制备。 还公开了包含缓释制剂和包含凝血因子Xa抑制剂的速释制剂的组合的药物组合物。 可以提供一种控制释放制剂，其包含凝血因子Xa抑制剂，用于预防或治疗血栓形成，其可以长期控制凝血因子Xa的活性，并且方便性和顺应性优异。 也可以提供一种制备控释制剂的方法。

公开(公告)号：US20090011003A1

公开(公告)日：2009-01-08

申请号：US11883168

申请日：2005-10-24

申请人： Masahiro Yamauchi ,  Tsuneaki Tottori ,  Atsushi Ishihara ,  Nobuhiro Yagi ,  Yasuki Kato

发明人： Masahiro Yamauchi ,  Tsuneaki Tottori ,  Atsushi Ishihara ,  Nobuhiro Yagi ,  Yasuki Kato

IPC分类号： A61K9/127 ,  A61K31/7105 ,  A61K48/00

CPC分类号： C12N15/1135 ,  A61K9/127 ,  A61K31/7105 ,  C12N2310/14

摘要： The present invention has its object to provide a composition for suppressing the expression of a target gene and the like, and provides a composition, comprising an RNA-encapsulated liposome which comprises complex particles comprising as constituent components a lead particle and an RNA comprising a sequence consisting of 15 to 30 contiguous nucleotides of a target gene mRNA and a sequence complementary to the sequence, and a lipid membrane for coating the complex particles, wherein constituent components of the lipid membrane can be solved in a polar organic solvent, and wherein the polar organic solvent can be contained in a liquid at such a concentration that the constituent components of the lipid membrane are dispersible and the complex particles are dispersible, and the like.

摘要翻译： 本发明的目的是提供抑制靶基因表达等的组合物，提供包含RNA包封的脂质体的组合物，其包含作为铅粒子的构成成分的复合粒子和包含序列的RNA 由靶基因mRNA的15〜30个连续核苷酸和与该序列互补的序列构成，以及用于涂布复合粒子的脂质膜，其中脂质膜的构成成分可以在极性有机溶剂中溶解，其中极性 有机溶剂可以以使得脂质膜的组成成分可分散并且复合颗粒可分散的浓度包含在液体中。

公开(公告)号：US20070275917A1

公开(公告)日：2007-11-29

申请号：US10565997

申请日：2004-07-29

申请人： Ryozo Nagai ,  Ichiro Manabe ,  Atsushi Ishihara ,  Tsuneaki Tottori

发明人： Ryozo Nagai ,  Ichiro Manabe ,  Atsushi Ishihara ,  Tsuneaki Tottori

IPC分类号： A61K48/00 ,  C07H21/02

CPC分类号： C12N15/113 ,  A61K38/00 ,  A61K48/00 ,  C12N2310/111 ,  C12N2310/14

摘要： An RNA capable of suppressing the expression of KLF5 gene, which comprises a sequence consisting of 15 to 30 contiguous nucleotides of KLF5 mRNA and a sequence complementary to the sequence, and which has been designed from the nucleotide sequence of Kruppel-like factor 5 (KLF5) cDNA. Specifically, a double-stranded RNA having a strand of a sequence shown in any one of SEQ ID NOS: 2 to 16 and a strand of a sequence complementary to the sequence, in which 2 uridylic acids are added to the 3′-terminus of each of the strands. By transfecting the RNA or a vector for expression of the RNA into cells, the expression of KLF5 gene in the cells can be suppressed. The RNA or a vector for expression of the RNA can be used as a therapeutic agent for cardiovascular disease or cancer.

摘要翻译： 能够抑制KLF5基因表达的RNA，其包含由KLF5 mRNA的15〜30个连续核苷酸和与该序列互补的序列组成的序列，并且由Kruppel样因子5（KLF5）的核苷酸序列设计 ）cDNA。 具体地说，具有SEQ ID NO：2〜16中任一项所示的序列的链的双链RNA和与该序列互补的序列的链，其中2个尿苷酸加入到 每个股。 通过将RNA或用于将RNA表达的载体转染到细胞中，可以抑制细胞中KLF5基因的表达。 用于表达RNA的RNA或载体可用作心血管疾病或癌症的治疗剂。

公开(公告)号：US20060029663A1

公开(公告)日：2006-02-09

申请号：US10515204

申请日：2004-07-16

申请人： Akihiro Uchida ,  Yasuhiro Ishikawa ,  Yasuhiko Ueno ,  Kiichiro Kaji ,  Tsuneaki Tottori

发明人： Akihiro Uchida ,  Yasuhiro Ishikawa ,  Yasuhiko Ueno ,  Kiichiro Kaji ,  Tsuneaki Tottori

IPC分类号： A61K31/522 ,  A61K9/20

CPC分类号： A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2866 ,  A61K31/522 ,  C07D473/04

摘要： (wherein R1, R2 and R3 may be the same or different and each represents a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; and R4 represents cycloalkyl, —(CH2)n—R5 or the above formula (II)) The present invention provides a solid formulation comprising a xanthine derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof, and microcrystalline cellulose, which possesses excellent pharmaceutical properties, for example, in hardness, disintegration property, dissolution property, stability or the like.

摘要翻译： （其中R 1，R 2和R 3）可以相同或不同，并且各自表示氢原子，低级烷基，低级烯基或 低级炔基; R 4表示环烷基， - （CH 2）n - R 5 - 或上式 （II））本发明提供包含由上述式（I）表示的黄嘌呤衍生物或其药学上可接受的盐和微晶纤维素的固体制剂，其具有优异的药物性质，例如硬度，崩解性，溶解性 财产，稳定性等。