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1.发明授权
公开(公告)号：US5080907A
公开(公告)日：1992-01-14
申请号：US607743
申请日：1990-10-29
申请人： Takeo Iijima , Masaki Otagiri , Masao Ueno , Tetsu Miyoshi
发明人： Takeo Iijima , Masaki Otagiri , Masao Ueno , Tetsu Miyoshi
CPC分类号： A61K9/0095 , A61K38/012 , A61K47/42 , A61K9/2063 , A61K9/4866 , Y10S514/801
摘要： Pharmaceutical preparations for oral administration are disclosed which comprise (a) an acidic non-steroidal anti-inflammatory agent having the mean particle size of about 100 .mu.m or less and (b) a protein hydrolyzate or a polypeptide having the mean molecular weight of 4000-12000. The pharmaceutical preparations are in the form of tablets, granules, capsules and dry syrups. They achieve high bioavailability of the anti-inflammatory agent, e.g., ibuprofen.
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公开(公告)号：US5474989A
公开(公告)日：1995-12-12
申请号：US203863
申请日：1994-03-01
申请人： Masanori Hashimoto , Masaki Otagiri , Teruko Imai
发明人： Masanori Hashimoto , Masaki Otagiri , Teruko Imai
摘要： The present invention relates to a drug composition in which the solubility and the dissolution rate of a drug having low water solubility are improved by incoroprating therein a low molecular weight chitosan in an amount of from 0.2 to 10 parts by weight per one part by weight of the poorly water-soluble drug. As the low molecular weight chitosan, those having a weight average molecular weight in the range from 500 to 50,000 and soluble in water were employed. This drug composition is prepared by mixing the components intimately so as to obtain a homogeneous dispersion of the low molecular weight chitosan with the mass of the composition.The drug composition according to the invention can be worked up into various preparation forms, such as, granules etc., as medicaments for administration to living organisms in which the bioabsorptivity and biouptake are improved.
摘要翻译： 本发明涉及药物组合物，其中水溶性低的药物的溶解度和溶解速度通过其中低分子量壳聚糖的加入量得到改善，所述低分子量壳聚糖的量为每10重量份 水溶性差的药物。 作为低分子量壳聚糖，使用重均分子量为500〜50000且可溶于水的那些。 通过紧密混合各组分制备该药物组合物，以获得低分子量壳聚糖与组合物质量的均匀分散体。 根据本发明的药物组合物可以被加工成各种制剂形式，例如颗粒等，作为用于生物吸收和生物吸收改善的生物体的给药的药物。
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公开(公告)号：US5317026A
公开(公告)日：1994-05-31
申请号：US25167
申请日：1993-03-02
申请人： Masaki Otagiri , Teruko Imai
发明人： Masaki Otagiri , Teruko Imai
IPC分类号： A61K31/445 , A61P1/04 , C07D295/08 , C07D295/096 , C07D211/32
CPC分类号： C07D295/096
摘要： 2-Substituted-N-{3-[3-(1-piperidinomethyl)phenoxy]propyl}acetamide, derivatives thereof, and pharmaceutically acceptable salts thereof. The substitution group may be aminomethylcyclohexane carbonyl group or N-carbobenzoxy-p-aminomethylhexane carbonyl group. The compounds having the first-mentioned group can be an effective component of an antiulcer drug composition, and the compounds of the last-mentioned group are intermediates for producing the compounds having the first-mentioned group. Disclosed also is an antiulcer drug composition comprising the above compound as an effective component. The antiulcer drug composition exhibits both the gastric acid secretion inhibitive activity and the gastric mucosa protective activity, and is effective as suppression and cure of ulcers.
摘要翻译： 2-取代的N- {3- [3-（1-哌啶基甲基）苯氧基]丙基}乙酰胺及其衍生物及其药学上可接受的盐。 取代基可以是氨甲基环己烷羰基或N-苄氧羰基对氨基甲基己烷羰基。 具有前述基团的化合物可以是抗溃疡药物组合物的有效成分，并且最后提到的基团的化合物是用于制备具有前述基团的化合物的中间体。 还公开了包含上述化合物作为有效成分的抗溃疡药物组合物。 抗溃疡药物组合物既显示胃酸分泌抑制活性又具有胃粘膜保护作用，并且作为溃疡的抑制和治愈是有效的。
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公开(公告)号：US5302399A
公开(公告)日：1994-04-12
申请号：US852624
申请日：1992-03-12
申请人： Masaki Otagiri , Teruko Imai
发明人： Masaki Otagiri , Teruko Imai
CPC分类号： A61K9/1652
摘要： A slow-releasing pharmaceutical easily prepared with alginic acid gel beads as a slow releasing carrier, and a basic medicament such as a beta-blocking agent or a calcium antagonistic agent therein, whereby the basic medicament can be relesed at a desired rate by means of oral administration, etc.
摘要翻译： 用海藻酸凝胶珠作为缓释载体容易制备的缓释药物和碱性药物如β-封闭剂或其中的拮抗剂，其中碱性药物可通过 口服等
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5.发明授权S-nitroso group-containing albumin, method for production, and anticancer agent 有权含有亚硝基的白蛋白，生产方法和抗癌剂公开(公告)号：US07893212B2
公开(公告)日：2011-02-22
申请号：US12201825
申请日：2008-08-29
申请人： Masaki Otagiri , Keisuke Nakajo , Naohisa Katayama , Toshiya Kai
发明人： Masaki Otagiri , Keisuke Nakajo , Naohisa Katayama , Toshiya Kai
IPC分类号： C07K16/00
CPC分类号： C07K14/76
摘要： The present invention provides an S-nitroso group-containing albumin, comprising an S-nitroso group introduced to at least one lysine in the amino acid sequence for albumin. The S-nitro group has been introduced into a lysine in the S-nitroso group-containing albumin of the invention to allow more S-nitroso groups to be included in the albumin, thus ensuring more potent inhibition of cancer cells in NO groups.
摘要翻译： 本发明提供含有S-亚硝基的白蛋白，其包含引入白蛋白氨基酸序列中的至少一个赖氨酸的S-亚硝基。 已将S-硝基引入本发明的含S-亚硝基基团的白蛋白中的赖氨酸中，以允许更多的S-亚硝基被包括在白蛋白中，从而确保NO组中对癌细胞的更有效的抑制。
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公开(公告)号：US20080051320A1
公开(公告)日：2008-02-28
申请号：US11890542
申请日：2007-08-07
申请人： Yu Ishima , Takaaki Akaike , Masaki Otagiri
发明人： Yu Ishima , Takaaki Akaike , Masaki Otagiri
CPC分类号： C07K1/1077 , A61K38/00 , C07K14/76
摘要： A protein is efficiently nitrosylated with nitrogen monoxide by merely mixing S-nitrosoglutathione as a nitrogen monoxide donor with a protein solution containing a stabilizing agent comprising at least one compound or a combination of plural compounds selected from an N-acetylamino acid, a fatty acid, and a fatty acid salt. The method that enables efficient NO addition to a cysteine residue in un-nitrosylated protein without changing the structure of protein and hence provides NO to a living organism.
摘要翻译： 通过仅将含有至少一种化合物或多种化合物的组合的蛋白质溶液与N-亚乙基氨基酸，脂肪酸， 和脂肪酸盐。 能够在不改变蛋白质结构的情况下对非亚硝基化蛋白质中的半胱氨酸残基进行高效NO添加，从而为活体提供NO的方法。
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公开(公告)号：US07253259B2
公开(公告)日：2007-08-07
申请号：US11044265
申请日：2005-01-28
申请人： Masaki Otagiri , Yoshinori Kida , Naohisa Katayama , Toshiya Kai
发明人： Masaki Otagiri , Yoshinori Kida , Naohisa Katayama , Toshiya Kai
IPC分类号： C07K1/00
CPC分类号： C07K14/765
摘要： A protein produced by gene recombinant technology, including at least one domain selected from domains I, II, and III of serum albumin but having a different structure from that of native albumin; and a method of producing the protein. The protein has an enhanced functional activity or activities selected from among various functional activities or serum albumin including antibacterial activity, antioxidative effect, inflammation inhibitory effect, in vivo substance transporting action, and enzymatic activity.
摘要翻译： 由基因重组技术产生的蛋白质，其包括至少一个选自血清白蛋白结构域I，II和III的结构域，但与天然白蛋白结构不同的结构域; 和蛋白质的制造方法。 蛋白质具有增强的功能活性或选自各种功能活性或血清白蛋白的活性，包括抗菌活性，抗氧化作用，炎症抑制作用，体内物质运输作用和酶活性。
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8.发明授权公开(公告)号：US07943570B2
公开(公告)日：2011-05-17
申请号：US11873393
申请日：2007-10-16
申请人： Keisuke Nakajou , Naohisa Katayama , Toshiya Kai , Masaki Otagiri
发明人： Keisuke Nakajou , Naohisa Katayama , Toshiya Kai , Masaki Otagiri
IPC分类号： C07K14/00
CPC分类号： C07K14/765 , A61K38/00 , C07K14/76 , C12P21/005
摘要： Glycosylated albumin as a drug carrier for a DDS targeting the liver (particularly kupffer's cell) can be provided by mutating a DNA encoding albumin to encode a mutant albumin containing a partial amino acid sequence permitting glycosylation modification by eukaryotic cell, preferably a consensus sequence of N-linked sugar chain, introducing an expression vector containing the mutant DNA into a host eukaryotic cell, preferably a host cell permitting addition of a high-mannose type sugar chain, culturing the obtained transformant, and recovering a glycosylated albumin protein from the obtained culture.
摘要翻译： 作为靶向肝脏（特别是枯否氏细胞）的DDS的药物载体的糖基化白蛋白可以通过使编码白蛋白的DNA突变来编码含有允许真核细胞进行糖基化修饰的部分氨基酸序列的突变白蛋白，优选N 连接的糖链，将含有突变型DNA的表达载体导入宿主真核细胞，优选宿主细胞，允许加入高甘露糖型糖链，培养获得的转化体，并从获得的培养物中回收糖基化白蛋白。
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9.发明申请公开(公告)号：US20090099337A1
公开(公告)日：2009-04-16
申请号：US12201825
申请日：2008-08-29
申请人： Masaki Otagiri , Keisuke Nakajo , Naohisa Katayama , Toshiya Kai
发明人： Masaki Otagiri , Keisuke Nakajo , Naohisa Katayama , Toshiya Kai
IPC分类号： C07K14/76
CPC分类号： C07K14/76
摘要： The present invention provides an S-nitroso group-containing albumin, comprising an S-nitroso group introduced to at least one lysine in the amino acid sequence for albumin. The S-nitro group has been introduced into a lysine in the S-nitroso group-containing albumin of the invention to allow more S-nitroso groups to be included in the albumin, thus ensuring more potent inhibition of cancer cells in NO groups.
摘要翻译： 本发明提供含有S-亚硝基的白蛋白，其包含引入白蛋白氨基酸序列中的至少一个赖氨酸的S-亚硝基。 已将S-硝基引入本发明的含S-亚硝基基团的白蛋白中的赖氨酸中，以允许更多的S-亚硝基被包括在白蛋白中，从而确保NO组中对癌细胞的更有效的抑制。
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公开(公告)号：US20050222026A1
公开(公告)日：2005-10-06
申请号：US10976708
申请日：2004-10-29
申请人： Masaki Otagiri , Takaaki Akaike
发明人： Masaki Otagiri , Takaaki Akaike
IPC分类号： A61K38/38 , C07K14/76 , C07K14/765
CPC分类号： C07K14/765 , A61K38/38 , C07K14/76 , Y02A50/481
摘要： The present invention provides a nitrosylated albumin variant wherein one or more amino acid residues of constituent amino acid sequences are substituted, or a different amino acid residue is inserted into a part of the constituent amino acid sequences. The albumin variant has sufficient antimicrobial property and permits application as various useful pharmaceutical compositions.
摘要翻译： 本发明提供一种亚硝酰化白蛋白变体，其中构成氨基酸序列的一个或多个氨基酸残基被取代，或者不同的氨基酸残基被插入到构成氨基酸序列的一部分中。 白蛋白变体具有足够的抗微生物特性，可用作各种有用的药物组合物。
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