公开(公告)号：US06664235B1

公开(公告)日：2003-12-16

申请号：US09640776

申请日：2000-08-18

申请人： Osamu Kanie ,  Chi-Huey Wong ,  Yasuo Suzuki

发明人： Osamu Kanie ,  Chi-Huey Wong ,  Yasuo Suzuki

IPC分类号： A61K317028

CPC分类号： A61K31/7012

摘要： A medicament for treatment of a viral infection which comprises as an active ingredient a compound represented by the following formula (I) or its Pharmaceutically acceptable salt, or a hydrate thereof or a solvate thereof. wherein R1 represents hydrogen atom or a C1-6 alkyl group; R2 represents an optionally substituted phenyl group, a C1-20 alkyl group, a C1-20 alkenyl group, or—(CH2)k—[NH—(CH2)m—NH]n—Y or —(CH2)k—[NH—(CH2CH2O)m-1—CH2CH2NH]n—Y in which Y represents phosphatidylethanolamine residue or polyglutamic acid residue, k and m independently represent an integer of from 2 to 10, n represents 0 or 1, provided that when n represents 1, Y represents phosphatidylethyl group; R3 represents hydrogen atom or an optionally substituted hydroxyl group; R4 represents hydrogen atom, a halogen atom, azide group, an optionally substituted amino group, or an optionally substituted hydroxyl group; and R5, R6, R7 and R8 independently represent an optionally substituted hydroxyl group.

摘要翻译： 一种用于治疗病毒感染的药物，其包含作为活性成分的由下式（I）表示的化合物或其药学上可接受的盐或其水合物或其溶剂合物。其中R 1表示氢原子或C1 -6烷基; R 2表示任选取代的苯基，C 1-20烷基，C 1-20链烯基或 - （CH 2）k - [NH-（CH 2）m -NH] n Y或 - （CH 2） [NH-（CH2CH2O）m-1-CH2CH2NH] nY其中Y表示磷脂酰乙醇胺残基或聚谷氨酸残基，k和m独立地表示2至10的整数，n表示0或1，条件是当n表示1时， Y表示磷脂酰乙基; R 3表示氢原子或任选取代的羟基; R 4表示氢原子，卤素原子，叠氮基，任选取代的氨基或任选取代的羟基; R 5，R 6，R 7和R 8独立地表示任选取代的羟基。

公开(公告)号：US06358919B1

公开(公告)日：2002-03-19

申请号：US09109870

申请日：1998-07-06

申请人： Osamu Kanie ,  Chi-Huey Wong ,  Hiroshi Kamitakahara

发明人： Osamu Kanie ,  Chi-Huey Wong ,  Hiroshi Kamitakahara

IPC分类号： A61K3816

CPC分类号： A61K47/645

摘要： A polymer compound or a salt thereof which comprises a biodegradable polymer such as polyglutamic acid acetylated at N-terminal thereof containing a glycosphingolipid such as lysoganglioside GM3, and which exerts antiviral activity against variety of viruses and is useful as an active ingredient of a medicament.

摘要翻译： 一种高分子化合物或其盐，其包含生物降解性聚合物，例如在其N末端乙酰化的聚谷氨酸，其含有鞘糖脂如溶血性神经节苷脂GM3，并且针对各种病毒发挥抗病毒活性，并且可用作药物的活性成分。

公开(公告)号：US07288565B2

公开(公告)日：2007-10-30

申请号：US10726550

申请日：2003-12-04

申请人： Osamu Kanie ,  Chikako Saotome

发明人： Osamu Kanie ,  Chikako Saotome

IPC分类号： A61K31/40 ,  C07D207/04

CPC分类号： C07D207/12 ,  Y02P20/55

摘要： The present invention provides a compound represented by the formula (I) or a salt thereof: wherein R1 represents a hydrogen atom, a C1-10 alkyl group optionally having a substituent, or a protecting group of N; R2 represents a C1-10 alkyl group optionally having a substituent or a C2-10 alkenyl group optionally having a substituent; R3 and R4 independently represent a hydrogen atom or a protecting group of hydroxyl group; X represents —N(R5)R6 or a residue of amino acid or of an amino group of a peptide wherein R5 and R6 independently represent a hydrogen atom, a C1-10 alkyl group optionally having a substituent, or a C3-12 cycloalkyl group optionally having a substituent; and Y represents a hydrogen atom, —CH2NH2, —CONH2, or —COOH. The compound of the present invention is useful as a specific inhibitor of sugar chain related enzymes such as glycosyltransferase and glycosidase, and is useful as, for example, a medicine for treating or preventing diseases associated with sugar chain related enzymes.

摘要翻译： 本发明提供由式（I）表示的化合物或其盐：其中R 1表示氢原子，C 1-10烷基任选具有 取代基或N的保护基; R 2表示任选具有取代基的C 1-10烷基或任选具有取代基的C 2-10链烯基; R 3和R 4独立地表示氢原子或羟基的保护基; X表示-N（R 5）R 6或氨基酸或肽的氨基残基，其中R 5和R 4 独立地表示氢原子，任选具有取代基的C 1-10烷基或任选具有取代基的C 3-12环烷基 取代基; Y表示氢原子，-CH 2 NH 2，-CONH 2 H或-COOH。 本发明的化合物可用作糖链相关酶如糖基转移酶和糖苷酶的特异性抑制剂，并且可用作例如用于治疗或预防与糖链相关的酶相关的疾病的药物。

公开(公告)号：US20130153760A1

公开(公告)日：2013-06-20

申请号：US13818141

申请日：2011-09-07

申请人： Osamu Kanie

发明人： Osamu Kanie

IPC分类号： H01J49/00

CPC分类号： H01J49/0036 ,  G01N30/7233 ,  H01J49/0031 ,  H01J49/005

摘要： A method for analyzing a structure of a substance of interest uses triple-quadrupole mass spectrometry (TQ-MS), and allows for acquisition of MSn information from data resulting from the TQ-MS measurement. The method includes (a) performing a measurement of triple quadrupole mass spectrometry with respect to the substance of interest while varying a value of CID energy; (b) at given values of CID energy, calculating percentages of precursor ion contents to a total ion content, and percentages of product ion contents to the total ion content; (c) extracting values of the percentages of product ion contents to the total ion content, wherein said values are values of the percentages of product ion contents at the respective values of CID energy; and (d) calculating sums of all combinations of the values of the percentages of product ion contents to the total ion content extracted in step (c).

摘要翻译： 用于分析感兴趣物质的结构的方法使用三重四极杆质谱（TQ-MS），并且允许从由TQ-MS测量得到的数据中获取MSn信息。 该方法包括：（a）在改变CID能量的值的同时对感兴趣的物质进行三重四极杆质谱的测量; （b）在给定的CID能量值下，计算前体离子含量与总离子含量的百分比，以及产物离子含量与总离子含量的百分比; （c）将产物离子含量的百分比提取为总离子含量，其中所述值是在各自的CID能量值下的产物离子含量百分比的值; 和（d）计算产物离子含量的百分比与步骤（c）中提取的总离子含量的值的所有组合的和。

公开(公告)号：US20080254996A1

公开(公告)日：2008-10-16

申请号：US11577399

申请日：2005-09-30

申请人： Osamu Kanie ,  Ayako Kurimoto ,  Syusaku Daikoku

发明人： Osamu Kanie ,  Ayako Kurimoto ,  Syusaku Daikoku

IPC分类号： C40B20/08 ,  C40B40/12

CPC分类号： G01N33/6848 ,  G01N2400/00

摘要： It is an objective of the present invention to provide a method of analyzing the structure of a sugar chain by performing CID-MSn measurement of a sugar chain of unknown structure and comparing the obtained data with obtained reference data acquired in advance.

摘要翻译： 本发明的目的是提供一种通过对未知结构的糖链进行CID-MS测定来分析糖链的结构的方法，并将获得的数据与获得的参考数据进行比较 提前获得。

公开(公告)号：US08575543B2

公开(公告)日：2013-11-05

申请号：US13818141

申请日：2011-09-07

申请人： Osamu Kanie

发明人： Osamu Kanie

IPC分类号： B01D59/44 ,  H01J49/26

CPC分类号： H01J49/0036 ,  G01N30/7233 ,  H01J49/0031 ,  H01J49/005

摘要： A method for analyzing a structure of a substance of interest uses triple-quadrupole mass spectrometry (TQ-MS), and allows for acquisition of MSn information from data resulting from the TQ-MS measurement. The method includes (a) performing a measurement of triple quadrupole mass spectrometry with respect to the substance of interest while varying a value of CID energy; (b) at given values of CID energy, calculating percentages of precursor ion contents to a total ion content, and percentages of product ion contents to the total ion content; (c) extracting values of the percentages of product ion contents to the total ion content, wherein said values are values of the percentages of product ion contents at the respective values of CID energy; and (d) calculating sums of all combinations of the values of the percentages of product ion contents to the total ion content extracted in step (c).

摘要翻译： 用于分析感兴趣物质的结构的方法使用三重四极杆质谱（TQ-MS），并且允许从由TQ-MS测量得到的数据中获取MSn信息。 该方法包括：（a）在改变CID能量的值的同时对感兴趣的物质进行三重四极杆质谱的测量; （b）在给定的CID能量值下，计算前体离子含量与总离子含量的百分比，以及产物离子含量与总离子含量的百分比; （c）将产物离子含量的百分比提取为总离子含量，其中所述值是在各自的CID能量值下的产物离子含量百分比的值; 和（d）计算产物离子含量的百分比与步骤（c）中提取的总离子含量的值的所有组合的和。

公开(公告)号：US20060166278A1

公开(公告)日：2006-07-27

申请号：US11319499

申请日：2005-12-29

申请人： Osamu Kanie

发明人： Osamu Kanie

IPC分类号： C08B37/00 ,  C40B40/12

CPC分类号： C07H15/203 ,  C07H1/00 ,  C07H3/06 ,  C07H15/04 ,  C07H15/18

摘要： An object of the present invention is to provide a method for efficiently chemically synthesizing biomolecules including a nucleotide (nucleic acid), a peptide (protein), or a sugar chain, as representative examples. The present invention provides a method of solid-phase synthesis of sugar chain(s) for synthesizing multiple types of sugar chains in at least one sugar chain synthesis reaction system comprising multiple types of monosaccharide units, which is characterized in that it comprises changing the temperature in the sugar chain synthesis reaction system depending on the temperature rising rate that has been determined based on a decrease in side reaction(s) in the reaction system as an indicator.

摘要翻译： 本发明的目的是提供一种用于有效地化学合成包含核苷酸（核酸），肽（蛋白质）或糖链的生物分子的方法作为代表性实例。 本发明提供了一种用于在包含多种单糖单元的至少一种糖链合成反应体系中合成多种类型的糖链的糖链的固相合成方法，其特征在于它包括改变温度 在糖链合成反应体系中，取决于基于作为指示剂的反应体系中副反应降低而确定的升温速率。