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1. 发明授权

US06204394B1 Method for preparing oxy-diphthalic anhydrides 有权
标题翻译：氧代邻苯二甲酸酐的制备方法
公开(公告)号：US06204394B1
公开(公告)日：2001-03-20
申请号：US09341860
申请日：1999-07-14
申请人： Junichi Sakata , Shinsuke Inoue , Shinichi Kadono
发明人： Junichi Sakata , Shinsuke Inoue , Shinichi Kadono
IPC分类号： C07D30789
CPC分类号： C07C51/567 , C07C65/24
摘要： Disclosed is a method for preparing oxy-diphthalic anhydrides, which comprises reacting a halo-phthalic anhydride represented by the formula (1): where Hal represents F, Cl, Br or I, with a carbonate salt selected from the group consisting of lithium carbonate, sodium carbonate, magnesium carbonate and calcium carbonate in a solvent to prepare oxy-diphthalic anhydrides represented by the formula (2):
摘要翻译：公开了一种制备氧代二邻苯二甲酸酐的方法，其包括使式（1）表示的卤代邻苯二甲酸酐与Hal，其中Hal代表F，Cl，Br或I的碳酸盐与选自碳酸锂，碳酸钠，碳酸镁和碳酸钙在溶剂中制备由式（2）表示的氧代二邻苯二甲酸酐：

2. 发明授权

US09540301B2 Method for manufacturing phosphonocrotonic acid derivative 有权
标题翻译：膦酸巴豆酸衍生物的制备方法
公开(公告)号：US09540301B2
公开(公告)日：2017-01-10
申请号：US14113498
申请日：2012-04-26
申请人： Shinji Ina , Takahiro Yamazaki , Junichi Sakata , Koji Ezaki , Katsuhiro Sakamoto
发明人： Shinji Ina , Takahiro Yamazaki , Junichi Sakata , Koji Ezaki , Katsuhiro Sakamoto
IPC分类号： C07C51/09 , C07F9/40 , C07C57/03 , A61K31/167 , A61K31/202 , A61K33/16 , A61K35/742 , A61K35/744 , A61K45/06 , C07C67/343 , C07C51/353 , A61K9/48
CPC分类号： C07C51/09 , A61K9/4858 , A61K9/4866 , A61K9/4875 , A61K31/167 , A61K31/202 , A61K33/16 , A61K35/742 , A61K35/744 , A61K45/06 , C07C51/353 , C07C57/03 , C07C67/343 , C07F9/4015 , A61K2300/00 , C07C69/587
摘要： Provided is a method of manufacturing a high quality phosphonocrotonic acid derivative.The present invention is a method of manufacturing a compound represented by the following Formula (3) by reacting a compound represented by the following Formula (1) with a compound represented by the following Formula (2), which comprises a treatment process using an acid or base.[in the formula, R1 represents a C1-6 linear or branched alkyl group that may be substituted by a C6-10 aryl group, a C2-6 linear or branched alkenyl group that may be substituted by a C6-10 aryl group, a C2-6 linear or branched alkynyl group that may be substituted by a C6-10 aryl group, or a C6-10 aryl group, R2 represents a hydrogen atom, or a C1-6 linear or branched alkyl group that may be substituted by a C6-10 aryl group, R3 represents a C1-6 linear or branched alkyl group, a C6-10 aryl group, or a halogen atom, and X represents a halogen atom, and multiple R1s may be the same or different].
摘要翻译：提供制造高品质膦酸巴豆酸衍生物的方法。本发明是通过使由下式（1）表示的化合物与下式（2）表示的化合物反应来制备由下式（3）表示的化合物的方法，该方法包括使用酸或基地。 [式中，R 1表示可以被C 6-10芳基取代的C 1-6直链或支链烷基，可以被C 6-10芳基取代的C 2-6直链或支链烯基， 10芳基，可以被C 6-10芳基取代的C 2-6直链或支链炔基或C 6-10芳基，R 2表示氢原子或C 1-6直链或可被C 6-10芳基取代的支链烷基，R 3表示C 1-6直链或支链烷基，C 6-10芳基或卤素原子，X表示卤素原子，多个R 1可以相同或不同]。

3. 发明授权

US08722094B2 Solid dispersion and pharmaceutical composition of the same, and production processes thereof 有权
标题翻译：固体分散体及其药物组合物及其制备方法
公开(公告)号：US08722094B2
公开(公告)日：2014-05-13
申请号：US12922029
申请日：2009-03-10
申请人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
发明人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
IPC分类号： A61K9/14
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K9/2077
摘要： A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950° C. for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100 g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier. This invention provides a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) which allows improvement in a solubility and a bioavailability of an active ingredient hardly soluble in water (e.g., a fibrate compound).
摘要翻译：包含多孔含硅载体的粉状多孔载体用含有有机溶剂和难溶于水的活性成分的溶液浸渍，除去有机溶剂，得到固体分散体，其中活性成分负载在多孔载体上，没有用超临界流体处理。多孔含硅载体在950℃的温度下具有不超过4重量％的加热损失2小时（例如球形含硅载体，例如球形多孔二氧化硅）。多孔含硅载体可以是平均孔径为10〜40nm，吸油量为175〜500ml / 100g的球状二氧化硅。可以从固体分散体和药学上可接受的载体制备药物组合物（例如片剂，颗粒剂或胶囊剂）。本发明提供一种固体分散体和药物组合物（或药物制剂），其允许改善难溶于水的活性成分（例如贝特类化合物）的溶解度和生物利用度。

4. 发明授权

US5859048A Pharmaceutics for mucosal administration 失效
标题翻译：粘膜给药制剂
公开(公告)号：US5859048A
公开(公告)日：1999-01-12
申请号：US860459
申请日：1997-06-25
申请人： Masami Oohashi , Noriaki Uchida , Junichi Sakata , Masaru Sunamoto
发明人： Masami Oohashi , Noriaki Uchida , Junichi Sakata , Masaru Sunamoto
IPC分类号： A61K9/00 , A61K9/02 , A61K38/11 , A61K38/23 , A61K38/28 , A61K47/22 , A61K47/32 , A01N43/36
CPC分类号： A61K9/02 , A61K38/11 , A61K38/23 , A61K38/28 , A61K47/22 , A61K47/32 , A61K9/0031
摘要： In pharmaceutics for mucosal administration containing pharmacologically active peptides or proteins and tolmetin or salts thereof exhibited very excellent effect as mucosal absorption enhancers.Furthermore, when the pharmaceutics for mucosal administration are for rectal administration, the suppository in which at least either the active ingredient, peptide or protein, or the mucosal absorption enhancer is converted to a complex with a high molecular compound dissolving in water at pH 5 or higher and together uniformly dispersed in a fatty suppository base exhibited markedly improved rectal absorbability compared with that of conventional pharmaceutics for rectal administration and at the same time increased stability of the peptide or protein which is the active ingredient.
摘要翻译： PCT No.PCT / JP95 / 02633 Sec。 371日期：1997年6月25日 102（e）1997年6月25日PCT 1997年12月22日PCT PCT。 WO96 / 20001 PCT出版物日期1996年7月4日在含有药理活性肽或蛋白质和甲苯胺或其盐的粘膜给药药物中，作为粘膜吸收促进剂表现出非常优异的作用。此外，当用于粘膜给药的药物用于直肠给药时，其中活性成分，肽或蛋白质或粘膜吸收增强剂中的至少一种的栓剂与溶于pH5的水中的高分子化合物转化为复合物，或与用于直肠给药的常规药物相比，更高和一起均匀分散在脂肪栓剂基质中的直肠吸收能力显着提高，同时提高作为活性成分的肽或蛋白质的稳定性。

5. 发明申请

US20140051876A1 METHOD FOR MANUFACTURING PHOSPHONOCROTONIC ACID DERIVATIVE 有权
标题翻译：制备磷酸酯衍生物的方法
公开(公告)号：US20140051876A1
公开(公告)日：2014-02-20
申请号：US14113498
申请日：2012-04-26
申请人： Shinji Ina , Takahiro Yamazaki , Junichi Sakata , Koji Ezaki , Katsuhiro Sakamoto
发明人： Shinji Ina , Takahiro Yamazaki , Junichi Sakata , Koji Ezaki , Katsuhiro Sakamoto
IPC分类号： C07C51/09 , C07C57/03 , C07F9/40
CPC分类号： C07C51/09 , A61K9/4858 , A61K9/4866 , A61K9/4875 , A61K31/167 , A61K31/202 , A61K33/16 , A61K35/742 , A61K35/744 , A61K45/06 , C07C51/353 , C07C57/03 , C07C67/343 , C07F9/4015 , A61K2300/00 , C07C69/587
摘要： Provided is a method of manufacturing a high quality phosphonocrotonic acid derivative.The present invention is a method of manufacturing a compound represented by the following Formula (3) by reacting a compound represented by the following Formula (1) with a compound represented by the following Formula (2), which comprises a treatment process using an acid or base.[in the formula, R1 represents a C1-6 linear or branched alkyl group that may be substituted by a C6-10 aryl group, a C2-6 linear or branched alkenyl group that may be substituted by a C6-10 aryl group, a C2-6 linear or branched alkynyl group that may be substituted by a C6-10 aryl group, or a C6-10 aryl group, R2 represents a hydrogen atom, or a C1-6 linear or branched alkyl group that may be substituted by a C6-10 aryl group, R3 represents a C1-6 linear or branched alkyl group, a C6-10 aryl group, or a halogen atom, and X represents a halogen atom, and multiple R1s may be the same or different].
摘要翻译：提供制造高品质膦酸巴豆酸衍生物的方法。本发明是通过使由下式（1）表示的化合物与下式（2）表示的化合物反应来制备由下式（3）表示的化合物的方法，该方法包括使用酸或基地。 [式中，R 1表示可被C 6-10芳基取代的C 1-6直链或支链烷基，可被C 6-10芳基取代的C 2-6直链或支链烯基，可被C 6-10芳基或C 6-10芳基取代的C 2-6直链或支链炔基，R 2表示氢原子，或可被C 1-6烷基取代的C 1-6直链或支链烷基 C6-10芳基，R3表示C1-6直链或支链烷基，C6-10芳基或卤素原子，X表示卤素原子，多个R1可以相同或不同]。

6. 发明申请

US20110020455A1 SOLID DISPERSION AND PHARMACEUTICAL COMPOSITION OF THE SAME, AND PRODUCTION PROCESSES THEREOF 有权
标题翻译：其固体分散体及其药物组合物及其生产工艺
公开(公告)号：US20110020455A1
公开(公告)日：2011-01-27
申请号：US12922029
申请日：2009-03-10
申请人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
发明人： Kazushi Yoshida , Norimichi Okubo , Junichi Sakata , Hashime Kanazawa
IPC分类号： A61K9/14 , A61K31/216 , A61K31/47 , A61K31/505 , A61K31/40 , A61K31/351 , A61P9/12 , A61P3/04 , A61P3/00 , A61P7/10 , A61P7/02 , A61P3/10
CPC分类号： A61K9/2009 , A61K9/1611 , A61K9/1652 , A61K9/2054 , A61K9/2077
摘要： A powdery porous carrier comprising a porous silicon-containing carrier is impregnated with a solution containing an organic solvent and an active ingredient hardly soluble in water, and the organic solvent is removed to give a solid dispersion having the active ingredient supported to the porous carrier without a treatment with a supercritical fluid. The porous silicon-containing carrier has a heating loss of not more than 4% by weight at a temperature of 950° C. for 2 hours (e.g., a spherical silicon-containing carrier such as a spherical porous silica). The porous silicon-containing carrier may be a spherical silica having a mean pore size of 10 to 40 nm and an oil absorption of 175 to 500 ml/100 g. A pharmaceutical composition (e.g., tablets, granules, or capsules) may be prepared from the solid dispersion and a pharmaceutically acceptable carrier. This invention provides a solid dispersion and a pharmaceutical composition (or a pharmaceutical preparation) which allows improvement in a solubility and a bioavailability of an active ingredient hardly soluble in water (e.g., a fibrate compound).
摘要翻译：包含多孔含硅载体的粉状多孔载体用含有有机溶剂和难溶于水的活性成分的溶液浸渍，除去有机溶剂，得到固体分散体，其中活性成分负载在多孔载体上，没有用超临界流体处理。多孔含硅载体在950℃的温度下具有不超过4重量％的加热损失2小时（例如球形含硅载体，例如球形多孔二氧化硅）。多孔含硅载体可以是平均孔径为10〜40nm，吸油量为175〜500ml / 100g的球状二氧化硅。可以从固体分散体和药学上可接受的载体制备药物组合物（例如片剂，颗粒剂或胶囊剂）。本发明提供一种固体分散体和药物组合物（或药物制剂），其允许改善难溶于水的活性成分（例如贝特类化合物）的溶解度和生物利用度。

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