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1. 发明授权

US07812155B2 Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative 有权
标题翻译：制备邻烷基化雷帕霉素衍生物和邻烷基化雷帕霉素衍生物的方法
公开(公告)号：US07812155B2
公开(公告)日：2010-10-12
申请号：US11984988
申请日：2007-11-26
申请人： Tetsuro Kawanishi , Masashi Isozaki
发明人： Tetsuro Kawanishi , Masashi Isozaki
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , B01D15/322 , B01D15/325
摘要： A process for preparing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying the resulting reaction product with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatography wherein R represents an alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.
摘要翻译：提供了制备由以下通式（1）表示的邻烷基化的雷帕霉素衍生物的方法。该方法包括以下步骤：使雷帕霉素与三氟甲磺酸烷基酯反应，用正相色谱法纯化所得反应产物，并进一步纯化已经用正相色谱法纯化的纯化产物，其中R代表烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰基氨基烷基或芳基。

2. 发明申请

US20080146796A1 Process for preparing an o-alkylated rapamycin derivative and o-alkylated rapamycin derivative 有权
标题翻译：制备邻烷基化雷帕霉素衍生物和邻烷基化雷帕霉素衍生物的方法
公开(公告)号：US20080146796A1
公开(公告)日：2008-06-19
申请号：US11984988
申请日：2007-11-26
申请人： Tetsuro Kawanishi , Masashi Isozaki
发明人： Tetsuro Kawanishi , Masashi Isozaki
IPC分类号： C07D487/14
CPC分类号： C07D498/18 , B01D15/322 , B01D15/325
摘要： A process for preparing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying the resulting reaction product with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatography wherein R represents an alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.
摘要翻译：提供了制备由以下通式（1）表示的邻烷基化的雷帕霉素衍生物的方法。该方法包括以下步骤：使雷帕霉素与三氟甲磺酸烷基酯反应，用正相色谱法纯化所得反应产物，并进一步纯化已经用正相色谱法纯化的纯化产物，其中R代表烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰基氨基烷基或芳基。

3. 发明申请

US20050192311A1 Process for production of O-alkylated rapamycin derivatives 有权
标题翻译： O-烷基化雷帕霉素衍生物的制备方法
公开(公告)号：US20050192311A1
公开(公告)日：2005-09-01
申请号：US11067718
申请日：2005-03-01
申请人： Masashi Isozaki , Tetsuro Kawanishi
发明人： Masashi Isozaki , Tetsuro Kawanishi
IPC分类号： A61F2/82 , A61K31/436 , A61L31/00 , A61M29/02 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/4745 , C07D491/14
CPC分类号： C07D498/18
摘要： Disclosed herein is a process for production of an O-alkylrapamycin derivative represented by the general formula (1) below by reaction between rapamycin and alkyl triflate in an organic solvent, characterized in that the reaction is carried out in the presence of trialkylamine. (where R denotes alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.) This process is capable of producing O-alkylrapamycin derivative efficiently owing to improvement in reaction yields for O-alkylation.
摘要翻译：本文公开了通过在有机溶剂中雷帕霉素和三氟甲磺酸烷基酯之间的反应制备由以下通式（1）表示的O-烷基雷帕霉素衍生物的方法，其特征在于反应在三烷基胺存在下进行。（其中R表示烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰氨基烷基或芳基）。由于O-烷基化的反应产率提高，该方法能够有效地生产O-烷基雷帕霉素衍生物。

4. 发明申请

US20070160646A1 Stent coated by a compound 审中-公开
标题翻译：由化合物涂覆的支架
公开(公告)号：US20070160646A1
公开(公告)日：2007-07-12
申请号：US11723367
申请日：2007-03-19
申请人： Masashi Isozaki , Tetsuro Kawanishi
发明人： Masashi Isozaki , Tetsuro Kawanishi
IPC分类号： A61F2/02
CPC分类号： C07D498/18
摘要： A stent coated by a compound represented by the general formula (1) below which is produced by reaction between rapamycin and alkyl triflate in an organic solvent which is a chlorine-containing organic solvent, wherein said reaction is carried out in the presence of trialkylamine, where R denotes alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.
摘要翻译：一种由下述通式（1）表示的化合物包被的支架，其通过雷帕霉素和三氟甲磺酸烷基酯在有机溶剂（其为含氯有机溶剂）中的反应制备，其中所述反应在三烷基胺存在下进行，其中R表示烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰氨基烷基或芳基。

5. 发明授权

US07193078B2 Process for production of O-alkylated rapamycin derivatives 有权
标题翻译： O-烷基化雷帕霉素衍生物的制备方法
公开(公告)号：US07193078B2
公开(公告)日：2007-03-20
申请号：US11067718
申请日：2005-03-01
申请人： Masashi Isozaki , Tetsuro Kawanishi
发明人： Masashi Isozaki , Tetsuro Kawanishi
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： Disclosed herein is a process for production of an O-alkylrapamycin derivative represented by the general formula (1) below by reaction between rapamycin and alkyl triflate in an organic solvent, characterized in that the reaction is carried out in the presence of trialkylamine. (where R denotes alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.) This process is capable of producing O-alkylrapamycin derivative efficiently owing to improvement in reaction yields for O-alkylation.
摘要翻译：本文公开了通过在有机溶剂中雷帕霉素和三氟甲磺酸烷基酯之间的反应制备由以下通式（1）表示的O-烷基雷帕霉素衍生物的方法，其特征在于反应在三烷基胺存在下进行。（其中R表示烷基，芳基烷基，羟基烷基，烷氧基烷基，酰氧基烷基，氨基烷基，烷基氨基烷基，烷氧基羰基氨基烷基，酰氨基烷基或芳基）。由于O-烷基化的反应产率提高，该方法能够有效地生产O-烷基雷帕霉素衍生物。

6. 发明申请

US20080021236A1 Saccharide-measuring fluorescent monomer, saccharide-measuring fluorescent sensor substance, and implantable, saccharide-measuring sensor 有权
标题翻译：糖测量荧光单体，糖测荧光传感器物质和可植入的糖测量传感器
公开(公告)号：US20080021236A1
公开(公告)日：2008-01-24
申请号：US11890518
申请日：2007-08-07
申请人： Shouji Ochiai , Tetsuro Kawanishi , Atsushi Matsumoto
发明人： Shouji Ochiai , Tetsuro Kawanishi , Atsushi Matsumoto
IPC分类号： C07F5/02 , A61B5/145
CPC分类号： C09K11/06 , C07F5/025 , C09K2211/1007 , C09K2211/1011 , C09K2211/1014
摘要： A fluorescent monomer compound represented by the following formula (1) is provided: wherein Q, Q′ and D3 may be the same or different, may be combined together into a fused ring, and are each a substituent selected from the group consisting of a hydrogen atom, a halogen atom, a hydroxyl group, and substituted or unsubstituted alkyl, acyl, oxyalkyl, carboxyl, carboxylate ester, carboxamido, cyano, nitro, amino and aminoalkyl groups; and D1, D2 and D4 each represent a substituent, wherein at least one of D1, D2 and D4 is a substituent group comprising a vinyl group at an end thereof, and wherein the substituent group comprising a vinyl group at an end thereof enables the fluorescent monomer compound to be soluble in water.
摘要翻译：提供由下式（1）表示的荧光单体化合物：其中Q，Q'和D 3可以相同或不同，可以一起组合成稠环，并且各自为取代基选自氢原子，卤原子，羟基和取代或未取代的烷基，酰基，烷氧基，羧基，羧酸酯，甲酰氨基，氰基，硝基，氨基和氨基烷基; D 1，D 2，D 4和D 4各自表示取代基，其中D 1，S 2， D 2和D 4是末端含有乙烯基的取代基，其末端具有乙烯基的取代基可使荧光单体化合物溶于水。

7. 发明申请

US20060223189A1 Solid-phase saccharide sensing compounds 有权
标题翻译：固相糖感测化合物
公开(公告)号：US20060223189A1
公开(公告)日：2006-10-05
申请号：US10551032
申请日：2003-03-28
申请人： Tetsuro Kawanishi , Mathew Romey , Mark Holody , Peter Zhu , Seiji Shinkai
发明人： Tetsuro Kawanishi , Mathew Romey , Mark Holody , Peter Zhu , Seiji Shinkai
IPC分类号： G01N33/00 , C07F5/02
CPC分类号： C07F5/025
摘要： The present invention provides solid-phase saccharide dyes. The dyes are bisboronic acids covalently bonded to a solid substrate. The dyes selectively conjugate with saccharides, particularly glucose, and register a signal. The signal is proportional to the quantity of saccharide. Thus, the dyes of the present invention are useful for measuring and monitoring saccharide levels, particularly in biological fluids such as blood.
摘要翻译：本发明提供固相糖染料。染料是共价键合到固体基质上的双硼酸。染料选择性地与糖结合，特别是葡萄糖，并记录信号。信号与糖的数量成正比。因此，本发明的染料可用于测量和监测糖水平，特别是在生物液体如血液中。

8. 发明授权

US08101374B2 Oxidative chromogenic compound or salt thereof and production method thereof, and reagent composition and test instrument using the same 有权
标题翻译：氧化显色化合物或其盐及其制备方法，以及使用其的试剂组合物和试验仪器
公开(公告)号：US08101374B2
公开(公告)日：2012-01-24
申请号：US12528112
申请日：2008-03-06
申请人： Tetsuro Kawanishi , Yuzuru Saito , Takako Ariga
发明人： Tetsuro Kawanishi , Yuzuru Saito , Takako Ariga
IPC分类号： C12Q1/54 , C12Q1/28 , C12N9/02 , C07D231/22 , C07D231/24
CPC分类号： C07D231/48 , C07D231/46
摘要： It is an object of the present invention to provide a means for measuring a concentration of various components rapidly with high accuracy and high sensitivity. The present invention is to provide an oxidative chromogenic compound or salt thereof represented by the following chemical formula (1): wherein R1 and R2 are each independently a linear or branched alkyl group having 1 to 5 carbon atoms; R3, R4, R5, R6 and R7 are each independently a hydrogen atom, a carboxyl group or a sulfonic acid group, or salt thereof, provided that at least one of R3 to R7 is a carboxyl group or a sulfonic acid group, or salt thereof, and the others are hydrogen atoms, and the production method thereof, and the reagent composition and test instrument using the same.
摘要翻译：本发明的目的是提供一种用于以高精度和高灵敏度快速测量各种组分的浓度的装置。本发明提供由以下化学式（1）表示的氧化显色化合物或其盐：其中R 1和R 2各自独立地为具有1至5个碳原子的直链或支链烷基; R 3，R 4，R 5，R 6和R 7各自独立地为氢原子，羧基或磺酸基或其盐，条件是R 3至R 7中的至少一个为羧基或磺酸基或盐其他的是氢原子及其制备方法，以及使用其的试剂组合物和试验仪器。

9. 发明授权

US08095196B2 Microsensor needle for pH measurement in tissue 有权
标题翻译：微量传感器针组织中的pH测量
公开(公告)号：US08095196B2
公开(公告)日：2012-01-10
申请号：US11642036
申请日：2006-12-19
申请人： Thomas G. Hacker , Tetsuro Kawanishi
发明人： Thomas G. Hacker , Tetsuro Kawanishi
IPC分类号： A61B5/1459 , A61B5/00 , G02B6/00 , G01N33/50
CPC分类号： A61B5/14542 , A61B5/14539 , A61B5/14556 , A61B5/1459 , A61B5/6848 , Y10T29/49879
摘要： A sensor probe for in-situ measurement of pH in a human tissue (e.g., cardiovascular) environment comprises a hollow needle having a tip and a back end. The tip is insertable into the tissue. An optic cable comprises a light conduit surrounded by a cladding. A first end of the light conduit is inserted from the back end of the needle and extends to within a predetermined distance of the tip to define a cavity within the tip. A porous dye layer is contained within the cavity, wherein the dye layer has a response to excitation light delivered through the light conduit that varies according to the pH of the tissue environment. An overcoat layer is deposited on the dye layer, wherein the overcoat layer is ionically permeable and substantially opaque at a light wavelength corresponding to the variable response of the dye layer.
摘要翻译：用于在人体组织（例如心血管）环境中原位测量pH的传感器探针包括具有尖端和后端的空心针。尖端可插入组织。光缆包括由包层围绕的光导管。光导管的第一端从针的后端插入并延伸到尖端的预定距离内以限定尖端内的空腔。多孔染料层包含在空腔内，其中染料层对根据组织环境的pH变化的通过光导管传递的激发光具有响应。在染料层上沉积外涂层，其中外涂层在对应于染料层的可变响应的光波长处是离子可渗透的并且基本上不透明。

10. 发明授权

US08083715B2 Puncture device 有权
标题翻译：穿刺装置
公开(公告)号：US08083715B2
公开(公告)日：2011-12-27
申请号：US12876005
申请日：2010-09-03
申请人： Yutaro Sonoda , Tetsuro Kawanishi , Atsushi Matsumoto
发明人： Yutaro Sonoda , Tetsuro Kawanishi , Atsushi Matsumoto
IPC分类号： A61M5/00 , A61M5/32 , A61B17/34
CPC分类号： A61M5/425 , A61M5/158 , A61M5/3287 , A61M2005/1585
摘要： The present invention provides a puncture device and an administration device in which a puncture needle can be stuck certainly to a predetermined region of a skin. The puncture device and the administration device of the present invention are provided with a puncture needle moving means for retaining aforesaid puncture needle to be movable and a skin deforming means for deforming the skin, wherein it is constituted such that the puncture needle is moved by aforesaid puncture needle moving means and punctures the skin deformed by aforesaid skin deforming means.
摘要翻译：本发明提供一种穿刺装置和施药装置，其中可以将穿刺针固定地粘附到皮肤的预定区域。本发明的穿刺装置和给药装置设置有用于保持上述穿刺针能够移动的穿刺针移动装置和用于使皮肤变形的皮肤变形装置，其中构成为使穿刺针通过上述移动穿刺针移动装置并刺穿由上述皮肤变形装置变形的皮肤。

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