公开(公告)号：US06562954B1

公开(公告)日：2003-05-13

申请号：US09478025

申请日：2000-01-05

申请人： Yuji Matsuzaki ,  Yousuke Yasuda ,  Satoshi Miyauchi ,  Junichi Onaya ,  Yusuke Hori ,  Akira Tawada ,  Hideo Mochizuki ,  Masami Iida

发明人： Yuji Matsuzaki ,  Yousuke Yasuda ,  Satoshi Miyauchi ,  Junichi Onaya ,  Yusuke Hori ,  Akira Tawada ,  Hideo Mochizuki ,  Masami Iida

IPC分类号： C07H1702

CPC分类号： C07H11/00 ,  Y02P20/55

摘要： Oligosaccharides including those usable as anti-inflammatory agent or anti-allergy agent, represented by the following general formula (3): wherein R10 and R11 each independently represent a hydrogen atom or —SO3M where M represents a proton or a monovalent cation, Ac represents an acetyl group, R12 represents a hydrogen atom or an anomeric substituent (a 6-O-sulfated N-acetylglucosamine residue, an alkyl group, a glycerol residue, an O-alkylglycerol residue, a cholesterol residue, a cholestanyl group, a ceramide residue, a phospholipid residue, a biotin residue, or a peptide residue), and Z represents an oxygen atom or —NHCO—.

摘要翻译： 包括可用作抗炎剂或抗过敏剂的寡糖，由以下通式（3）表示：其中R10和R11各自独立地表示氢原子或-SO3M，其中M表示质子或一价阳离子，Ac表示 乙酰基，R 12表示氢原子或端基异构取代基（6-O-硫酸化N-乙酰葡糖胺残基，烷基，甘油残基，O-烷基甘油残基，胆固醇残基，胆甾烷基，神经酰胺残基 ，磷脂残基，生物素残基或肽残基），Z表示氧原子或-NHCO-。

公开(公告)号：US07601488B2

公开(公告)日：2009-10-13

申请号：US11622673

申请日：2007-01-12

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： A01N1/02 ,  A61K31/702

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： A method for promoting expression of a heat shock protein, or for inhibiting cell injury or cell death, or for treating a disease for which cell or tissue protection is desired, or for promoting production of IL-10, or for inhibiting production of IL-8, by administering an effective amount of a fraction containing a hyaluronic acid tetrasaccharide comprising four saccharide residues and having certain physicochemical properties or by administering an effective amount of an isolated and substantially pure tetrasaccharide of formula (1) described in the application. Methods for preserving an organ.

摘要翻译： 用于促进热休克蛋白的表达或用于抑制细胞损伤或细胞死亡或用于治疗需要细胞或组织保护的疾病或用于促进IL-10的产生或用于抑制IL- 如图8所示，通过施用有效量的含有包含四个糖残基并具有一定物理化学性质的透明质酸四糖的级分，或通过施用有效量的分离和基本上纯的本申请中描述的式（1）四糖。 保存器官的方法

公开(公告)号：US20070134646A1

公开(公告)日：2007-06-14

申请号：US11622673

申请日：2007-01-12

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： A01N1/02 ,  A61K31/728

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： A method for promoting expression of a heat shock protein, or for inhibiting cell injury or cell death, or for treating a disease for which cell or tissue protection is desired, or for promoting production of IL-10, or for inhibiting production of IL-8, by administering an effective amount of a fraction containing a hyaluronic acid tetrasaccharide comprising four saccharide residues and having certain physicochemical properties or by administering an effective amount of an isolated and substantially pure tetrasaccharide of formula (1) described in the application. Methods for preserving an organ.

摘要翻译： 用于促进热休克蛋白的表达或用于抑制细胞损伤或细胞死亡或用于治疗需要细胞或组织保护的疾病或用于促进IL-10的产生或用于抑制IL- 如图8所示，通过施用有效量的含有包含四个糖残基并具有一定物理化学性质的透明质酸四糖的级分，或通过施用有效量的分离和基本上纯的本申请中描述的式（1）四糖。 保存器官的方法

公开(公告)号：US08314079B2

公开(公告)日：2012-11-20

申请号：US13115435

申请日：2011-05-25

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： A61K31/702

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： A method for promoting expression of a heat shock protein, or for inhibiting cell injury or cell death, or for treating a disease for which cell or tissue protection is desired, or for promoting production of IL-10, or for inhibiting production of IL-8, by administering an effective amount of a fraction containing a hyaluronic acid tetrasaccharide comprising four saccharide residues and having certain physicochemical properties or by administering an effective amount of an isolated and substantially pure tetrasaccharide of formula (1) described in the application. Methods for preserving an organ.

摘要翻译： 用于促进热休克蛋白的表达或用于抑制细胞损伤或细胞死亡或用于治疗需要细胞或组织保护的疾病或用于促进IL-10的产生或用于抑制IL- 如图8所示，通过施用有效量的含有包含四个糖残基并具有一定物理化学性质的透明质酸四糖的级分，或通过施用有效量的分离和基本上纯的本申请中描述的式（1）四糖。 保存器官的方法

公开(公告)号：US20110224169A1

公开(公告)日：2011-09-15

申请号：US13115435

申请日：2011-05-25

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： A61K31/702 ,  A61P1/16 ,  A61P1/04

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： A method for promoting expression of a heat shock protein, or for inhibiting cell injury or cell death, or for treating a disease for which cell or tissue protection is desired, or for promoting production of IL-10, or for inhibiting production of IL-8, by administering an effective amount of a fraction containing a hyaluronic acid tetrasaccharide comprising four saccharide residues and having certain physicochemical properties or by administering an effective amount of an isolated and substantially pure tetrasaccharide of formula (1) described in the application. Methods for preserving an organ.

摘要翻译： 用于促进热休克蛋白的表达或用于抑制细胞损伤或细胞死亡或用于治疗需要细胞或组织保护的疾病或用于促进IL-10的产生或用于抑制IL- 如图8所示，通过施用有效量的含有包含四个糖残基并具有一定物理化学性质的透明质酸四糖的级分，或通过施用有效量的分离和基本上纯的本申请中描述的式（1）四糖。 保存器官的方法

公开(公告)号：US20080182983A1

公开(公告)日：2008-07-31

申请号：US11928833

申请日：2007-10-30

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： C08B37/00 ,  C07H1/00

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： Hyaluronic acid oligosaccharides having a size selected from sizes of 4 to 60 saccharides, fractions containing the hyaluronic acid oligosaccharides and having particular physicochemical properties, and drugs containing the same. The hyaluronic acid oligosaccharides of the present invention are extremely useful, because they exert superior pharmaceutical effects as active ingredients of a heat shock protein expression promoter, cell death inhibitor, cell injury inhibitor and cell and tissue protecting agent (e.g., organ preservation agent, antiulcer agent, antihepatopathic agent, IL-10 production promoter or IL-8 production inhibitor) and exhibit high safety.

摘要翻译： 具有选自尺寸为4至60个糖的大小的透明质酸寡糖，含有透明质酸寡糖的部分并且具有特定的理化性质，以及含有该物质的药物。 本发明的透明质酸寡糖是非常有用的，因为它们作为热休克蛋白表达启动子，细胞死亡抑制剂，细胞损伤抑制剂和细胞和组织保护剂（例如器官保存剂，抗溃疡剂）的活性成分发挥优异的药物作用 药物，抗肝病，IL-10生产促进剂或IL-8产生抑制剂），并表现出高安全性。

公开(公告)号：US20050090661A1

公开(公告)日：2005-04-28

申请号：US10312879

申请日：2001-07-06

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： A61K31/702 ,  A61K31/728 ,  A61P1/04 ,  A61P1/16 ,  A61P43/00 ,  C07H7/033 ,  C08B37/08 ,  C08B37/00

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： Hyaluronic acid oligosaccharides having a size selected from sizes of 4 to 60 saccharides, fractions containing the hyaluronic acid oligosaccharides and having particular physicochemical properties, and drugs containing the same. The hyaluronic acid oligosaccharides of the present invention are extremely useful, because they exert superior pharmaceutical effects as active ingredients of a heat shock protein expression promoter, cell death inhibitor, cell injury inhibitor and cell and tissue protecting agent (e.g., organ preservation agent, antiulcer agent, antihepatopathic agent, IL-10 production promoter or IL-8 production inhibitor) and exhibit high safety.

摘要翻译： 具有选自尺寸为4至60个糖的大小的透明质酸寡糖，含有透明质酸寡糖的部分并且具有特定的理化性质，以及含有该物质的药物。 本发明的透明质酸寡糖是非常有用的，因为它们作为热休克蛋白表达启动子，细胞死亡抑制剂，细胞损伤抑制剂和细胞和组织保护剂（例如器官保存剂，抗溃疡剂）的活性成分发挥优异的药物作用 药物，抗肝病，IL-10生产促进剂或IL-8产生抑制剂），并表现出高安全性。

公开(公告)号：US07507723B2

公开(公告)日：2009-03-24

申请号：US10312879

申请日：2001-07-06

申请人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

发明人： Akira Asari ,  Hitoshi Kurihara ,  Tomomi Shibata ,  Yuka Miyazaki ,  Hiroko Yamanokuchi ,  Akira Tawada ,  Takahiro Masa ,  Yuji Matsuzaki

IPC分类号： A61K31/702 ,  A61K31/728

CPC分类号： C08B37/0072 ,  A61K31/702 ,  A61K31/728 ,  C07H7/033

摘要： Hyaluronic acid oligosaccharides having a size selected from sizes of 4 to 60 saccharides, fractions containing the hyaluronic acid oligosaccharides and having particular physicochemical properties, and drugs containing the same. The hyaluronic acid oligosaccharides of the present invention are extremely useful, because they exert superior pharmaceutical effects as active ingredients of a heat shock protein expression promoter, cell death inhibitor, cell injury inhibitor and cell and tissue protecting agent (e.g., organ preservation agent, antiulcer agent, antihepatopathic agent, IL-10 production promoter or IL-8 production inhibitor) and exhibit high safety.

摘要翻译： 具有选自尺寸为4至60个糖的大小的透明质酸寡糖，含有透明质酸寡糖的部分并且具有特定的理化性质，以及含有该物质的药物。 本发明的透明质酸寡糖是非常有用的，因为它们作为热休克蛋白表达启动子，细胞死亡抑制剂，细胞损伤抑制剂和细胞和组织保护剂（例如器官保存剂，抗溃疡剂）的活性成分发挥优异的药物作用 药物，抗肝病，IL-10生产促进剂或IL-8产生抑制剂），并表现出高安全性。

公开(公告)号：US07531554B2

公开(公告)日：2009-05-12

申请号：US11133470

申请日：2005-05-20

申请人： Motohide Satoh ,  Takashi Matsuda ,  Satoshi Okuda ,  Hiroshi Kawakami ,  Hisateru Aramaki ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki ,  Mitsuru Takahashi ,  Naohito Yamada ,  Akemi Nagao

发明人： Motohide Satoh ,  Takashi Matsuda ,  Satoshi Okuda ,  Hiroshi Kawakami ,  Hisateru Aramaki ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Wataru Watanabe ,  Kazunobu Yamataka ,  Shinichi Kiyonari ,  Shuichi Wamaki ,  Mitsuru Takahashi ,  Naohito Yamada ,  Akemi Nagao

IPC分类号： C07D215/04 ,  A61K31/44

CPC分类号： C07D215/56 ,  C07D401/04 ,  C07D401/06 ,  C07D405/06 ,  C07D491/04

摘要： Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity.A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification. The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent, and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.

摘要翻译： 提供具有抗HIV活性的化合物，特别是整合酶抑制活性。 由下式[I]表示的4-氧代喹啉化合物或其药学上可接受的盐：其中每个符号如说明书中所定义。 本发明还涉及含有4-氧代喹啉化合物或其药学上可接受的盐和药学上可接受的载体的药物组合物; 含有4-氧代喹啉化合物或其药学上可接受的盐作为活性成分的整合酶抑制剂，抗病毒剂，抗HIV剂等; 含有4-氧代喹啉化合物或其药学上可接受的盐的抗HIV组合物和一种或多种其它类型的抗HIV活性物质作为活性成分; 含有4-氧代喹啉化合物或其药学上可接受的盐作为活性成分的抗HIV剂，其用于与其它抗HIV剂的多重药物治疗等。

公开(公告)号：US20080207618A1

公开(公告)日：2008-08-28

申请号：US11767021

申请日：2007-06-22

申请人： Motohide SATOH ,  Hisateru Aramaki ,  Masaki Yamashita ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Hiroshi Nakamura ,  Yuji Matsuzaki ,  Shuichi Wamaki

发明人： Motohide SATOH ,  Hisateru Aramaki ,  Masaki Yamashita ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Hiroshi Nakamura ,  Yuji Matsuzaki ,  Shuichi Wamaki

IPC分类号： A61K31/5377 ,  C07D413/08 ,  C07D403/08 ,  A61K31/4709 ,  A61P31/18

CPC分类号： C07D215/56 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10

摘要： The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

摘要翻译： 本发明涉及由下式[I]表示的化合物，其中每个符号如说明书中所定义，或其药学上可接受的盐，或其溶剂合物，药物组合物，抗HIV剂和HIV 含有该化合物的整合酶抑制剂。 本发明的化合物具有HIV整合酶抑制活性，可用作抗HIV剂，或用作预防或治疗AIDS的药剂。 此外，通过与其它抗HIV剂如蛋白酶抑制剂，逆转录酶抑制剂等的组合使用，它可以是更有效的抗HIV剂。 因为它显示出整合酶特异性的高抑制活性，所以化合物可以是对人体安全的药剂，其副作用较小。