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1. 发明授权

US08148505B2 Method of α-selective glycosylation 失效
标题翻译： α-选择性糖基化方法
公开(公告)号：US08148505B2
公开(公告)日：2012-04-03
申请号：US10555565
申请日：2004-05-19
申请人： Hiromune Ando , Akihiro Imamura , Makoto Kiso , Hideharu Ishida
发明人： Hiromune Ando , Akihiro Imamura , Makoto Kiso , Hideharu Ishida
IPC分类号： C07G3/00 , C07H17/00
CPC分类号： C07H1/00 , C07H9/00 , Y02P20/55
摘要： An α-selective glycosylation process of a glycosylation reaction between a sugar structure of hexose or an aldose having a chain with six or more carbon atoms in the molecule, which is a monosaccharide or a reducing end of an oligosaccharide with two or more monosaccharide residues connected by glycosidic linkages (an oligosaccharide with two monosaccharide residues is disaccharide) (also referred to as “a disaccharide to an oligosaccharide”) or a sugar chain and alcoholic hydroxyl group or thiol group, to obtain a sugar structure glycoside containing α-glycoside at a high ratio, under the ring-shaped formation of a protective group in a silyl acetal structure over hydroxyl groups at positions 4 and 6 in the sugar structure.By the process, highly selective α-glycosylation of sugar structure can be progressed in a simple and efficient manner.
摘要翻译：在分子中具有六个或更多个碳原子的链的己糖或醛糖的糖结构之间的糖基化反应的α-选择性糖基化方法，其是连接两个或多个单糖残基的寡糖或还原末端通过糖苷键（具有两个单糖残基的寡糖是二糖）（也称为“寡糖”）或糖链和醇羟基或硫醇基，以获得含有α-糖苷的糖结构糖苷在糖结构中位置4和6的羟基上的甲硅烷基缩醛结构中的环状形成环状形成。通过该过程，糖结构的高选择性α-糖基化可以以简单和有效的方式进行。

2. 发明申请

US20060122379A1 Method of alpha-selective glycosylation 失效
标题翻译： α-选择性糖基化方法
公开(公告)号：US20060122379A1
公开(公告)日：2006-06-08
申请号：US10555565
申请日：2004-05-19
申请人： Hiromune Ando , Akihiro Imamura , Makoto Kiso , Hideharu Ishida
发明人： Hiromune Ando , Akihiro Imamura , Makoto Kiso , Hideharu Ishida
IPC分类号： C07H13/00
CPC分类号： C07H1/00 , C07H9/00 , Y02P20/55
摘要： an α-selective glycosylation process of a glycosylation reaction between a sugar structure of hexose or an aldose having a chain with six or more carbon atoms in the molecuse, which is a monosaccharide or a reducing end of an oligosaccharide with two or more monosaccharide residues connected by glycosidic linkages (an oligosaccharide with two monosaccharide residues is disaccharide) (also referred to as “a disaccharide to an oligosaccharide”) or a sugar chain and alcoholic hydroxyl group of thiol group, to obtain a sugar structure glycoside containing α-glycoside at a high ratio, under the ring-shaped formation of a protective group in a silyl acetal structure over hydroxyl groups at positions 4 and 6 in the sugar structure. By the process, highly selective α-glycosylation of sugar structure can be progressed in a simple and efficient manner.
摘要翻译：在分子中具有六个或更多个碳原子的链的己糖或醛糖的糖结构之间的糖基化反应的α-选择性糖基化方法，其是连接了两个或更多个单糖残基的寡糖的单糖或还原末端通过糖苷键（具有两个单糖残基的寡糖是二糖）（也称为“寡糖的二糖”）或硫醇基的糖链和醇羟基，以获得含有α-糖苷的糖结构糖苷在糖结构中位置4和6的羟基上的甲硅烷基缩醛结构中的环状形成环状形成。通过该过程，糖结构的高选择性α-糖基化可以以简单和有效的方式进行。

3. 发明申请

US20140255317A1 PREPARATION COMPRISING HEXOSE-6-PHOSPHATE-MODIFIED CHOLESTEROL DERIVATIVE 审中-公开
标题翻译：包含十六烷基六磷酸修饰的胆固醇衍生物的制备
公开(公告)号：US20140255317A1
公开(公告)日：2014-09-11
申请号：US14343318
申请日：2012-09-05
申请人： Keita Un , Mitsuru Hashida , Shigeru Kawakami , Makoto Kiso , Akiharu Ueki , Hiromune Ando
发明人： Keita Un , Mitsuru Hashida , Shigeru Kawakami , Makoto Kiso , Akiharu Ueki , Hiromune Ando
IPC分类号： A61K47/28 , C12N15/113 , A61K31/704 , A61K49/00 , C07K14/00 , C07J41/00 , A61K9/127
CPC分类号： C07J41/0055 , A61K9/1272 , A61K9/1278 , A61K31/575 , A61K31/704 , A61K31/7088 , A61K31/7105 , A61K47/28 , A61K47/549 , A61K47/554 , A61K47/6911 , A61K49/0034 , A61K49/0084 , C07J9/00 , C07J51/00 , C12N15/88 , A61K2300/00
摘要： Provided is a compound represented by the general formula (1) (where: G represents a hexose-6-phosphate residue; and L represents a divalent linker group).
摘要翻译：提供由通式（1）表示的化合物（其中：G表示己糖-6-磷酸残基; L表示二价连接基团）。

4. 发明申请

US20110286937A1 SYNTHETIC GLYCOLIPID-CONTAINING LIPOSOME 审中-公开
标题翻译：含有合成的含有甘油的脂质体
公开(公告)号：US20110286937A1
公开(公告)日：2011-11-24
申请号：US12918467
申请日：2009-02-18
申请人： Makoto Kiso , Hideharu Ishida , Taiji Yamashita , Koichi Igarashi , Masahiko Hirai
发明人： Makoto Kiso , Hideharu Ishida , Taiji Yamashita , Koichi Igarashi , Masahiko Hirai
IPC分类号： A61K49/18 , A61K49/00 , A61K39/395 , A61K38/48 , A61K38/47 , A61K38/38 , A61K38/02 , A61K33/24 , A61K31/573 , A61K48/00 , A61K31/7105 , A61K31/225 , A61K31/727 , A61K31/551 , A61K31/663 , A61K31/722 , A61K9/127
CPC分类号： A61K9/1272 , A61K31/22 , A61K31/551 , A61K31/573 , A61K31/663 , A61K31/722 , A61K31/727 , A61K38/38 , A61K38/47 , A61K38/4886 , A61K38/49 , A61K47/549 , A61K47/6911 , C12N15/88 , C12N2810/859
摘要： The present invention provides a glycolipid-containing liposome. In such a glycolipid-containing liposome, the glycolipid includes a plant ceramide portion and a sugar chain portion. The present invention also provides a method of producing a glycolipid-containing liposome. This method includes the following steps of: A) providing a glycolipid in which the glycolipid includes a plant ceramide portion and a sugar chain portion; and B) mixing the provided glycolipid with a liposome raw material and subjecting the mixture to conditions in which a liposome is formed.
摘要翻译：本发明提供了含糖脂的脂质体。在这种含糖脂的脂质体中，糖脂包括植物神经酰胺部分和糖链部分。本发明还提供了含糖脂的脂质体的制造方法。该方法包括以下步骤：A）提供糖脂，其中糖脂包含植物神经酰胺部分和糖链部分; 和B）将所提供的糖脂与脂质体原料混合并使混合物进入其中形成脂质体的条件。

5. 发明授权

US06503885B1 Carboxymethylgalactose derivatives 有权
标题翻译：羧甲基半乳糖衍生物
公开(公告)号：US06503885B1
公开(公告)日：2003-01-07
申请号：US09787610
申请日：2001-03-20
申请人： Makoto Kiso , Hideharu Ishida
发明人： Makoto Kiso , Hideharu Ishida
IPC分类号： A61K3170
CPC分类号： C07H15/10 , C07H15/04
摘要： Carboxymethylgalactose derivatives represented by general formula (1); and salts thereof, which exhibit reactivity to selectins and are useful as inhibitors against selectin-related diseases such as various inflammations and cancerous metastasis; In said formula, R is a group rep resented by formula (1a), (1b) or (1c).
摘要翻译：由通式（1）表示的羧甲基半乳糖衍生物及其盐对选择素具有反应性，可用作抑制选择素相关疾病如各种炎症和癌性转移的药物; 在所述式中，R为式（1a），（1b）或（1c）所代表的基团。

6. 发明授权

US5589465A Glycolipid derivatives acting as ligands for selectins 失效
标题翻译：作为选择素配体的糖脂衍生物
公开(公告)号：US5589465A
公开(公告)日：1996-12-31
申请号：US396793
申请日：1995-03-01
申请人： Hideharu Ishida , Makoto Kiso , Akira Hasegawa
发明人： Hideharu Ishida , Makoto Kiso , Akira Hasegawa
IPC分类号： C07H11/00 , A61K31/70 , A61K31/7028 , A61P29/00 , A61P43/00 , C07H3/06 , C07H15/04
CPC分类号： C07H3/06 , Y02P20/55
摘要： Novel glycolipid derivatives of Formula (I): ##STR1## wherein R is a long chain alkyl, or their salts are disclosed. These compounds act as a ligand for selectin family and exhibit a remarkable inhibitory effect on the binding of selectin family to its native ligand sialyl Lewis.sup.x.
摘要翻译：式（I）的新型糖脂衍生物：其中R是长链烷基或其盐被公开。这些化合物作为选择素家族的配体，并且对选择蛋白家族与其天然配体唾液酸Lewisx的结合表现出显着的抑制作用。

7. 发明授权

US5380829A Thioglycoside analogs of gangliosides 失效
标题翻译：神经节苷脂的硫糖苷类似物
公开(公告)号：US5380829A
公开(公告)日：1995-01-10
申请号：US842532
申请日：1992-02-27
申请人： Akira Hasegawa , Makoto Kiso
发明人： Akira Hasegawa , Makoto Kiso
IPC分类号： A61K31/70 , A61K31/7028 , A61P31/12 , A61P31/16 , C07H15/10 , C07H15/14 , C12N9/99 , C07H5/08
CPC分类号： C07H15/10 , C07H15/14 , Y02P20/55
摘要： Disclosed are thioglycoside analogs of gangliosides represented by the formula ##STR1## in which Y represents a radical of the following formula ##STR2## and X represents a radical of the formula ##STR3## wherein m is an integer of 15 to 25, l is an integer of 0 to 3 and n is an integer of 11 to 15. The thioglycoside analogs are expected to exert specific enzyme-inhibitory effects.
摘要翻译：公开了由式“IMAGE”表示的神经节苷脂的硫代糖苷类似物，其中Y表示下式的基团，其中X表示下式的基团：其中m是 15〜25的整数，l为0〜3的整数，n为11〜15的整数。预期硫代糖苷类似物具有特异性的酶抑制作用。

8. 发明授权

US4746742A Analogs of nonreducing monosaccharide moiety of lipid A 失效
标题翻译：脂质A的非还原性单糖部分的类似物
公开(公告)号：US4746742A
公开(公告)日：1988-05-24
申请号：US930361
申请日：1986-11-12
申请人： Akira Hasegawa , Makoto Kiso , Kazuyuki Morihara
发明人： Akira Hasegawa , Makoto Kiso , Kazuyuki Morihara
IPC分类号： A61K39/00 , C07H13/06 , C07H5/04
CPC分类号： C07H13/06 , A61K39/00 , A61K2039/55572
摘要： Provided herein is a derivative of 2-deoxy-2-amino-4-O-phophono-D-glucopyranose, which is derived from lipid A, of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are a member in a pair selected from the group consisting of those indicated in a following table:______________________________________ Com- pound No. R.sub.1 R.sub.2 ______________________________________ I(R,R) --O--CO--(CH.sub.2).sub.12 --CH.sub.3 --O--CO--(CH.sub.2).sub.12 --CH.sub.3 II --O--CO--(CH.sub.2).sub.12 --CH.sub.3 --OH II(R,R) --O--CO--(CH.sub.2).sub.12 --CH.sub.3 --OH II(S,S) --O--CO--(CH.sub.2).sub.12 --CH.sub.3 --OH III --OH --O--CO--(CH.sub.2).sub.12 --CH.sub.3 III(R,R) --OH --O--CO--(CH.sub.2).sub.12 --CH.sub.3 III(S,S) --OH --O--CO--(CH.sub.2).sub.12 --CH.sub.3 IV(R) --H --O--CO--(CH.sub.2).sub.12 --CH.sub.3 ______________________________________ The compounds of this invention include those of rectus and sinister configurations and act as mitogens for polyclonal B cells.
摘要翻译：本文提供了衍生自脂质A的2-脱氧-2-氨基-4-O-磷酸-D-吡喃葡萄糖的衍生物，其具有下式：其中R 1和R 2是成对选自由下表所示的组组成： - 组合 - 不。 R 1 R 2 -I（R，R）-O-CO-（CH 2）12 -CH 3 -O-CO-（CH 2）12 -CH 3 -II -O-CO-（CH 2）12 -CH 3 -OH -II ，（R）-O-CO-（CH 2）12 -CH 3 -OH -II（S，S）-O-CO-（CH 2）12 -CH 3 -OH -III -OH -O-CO-（CH 2）（CH 2）12 -CH 3 -III（S，S）-OH -O-CO-（CH 2）12 -CH 3 -IV（R）-H -O -CO-（CH 2）12 -CH 3 - 本发明的化合物包括直肠和阴性构型的化合物，并且作为多克隆B细胞的有丝分裂原。

9. 发明授权

US5191072A Lipid A monosaccharide analogues 失效
标题翻译：脂肪单糖类似物
公开(公告)号：US5191072A
公开(公告)日：1993-03-02
申请号：US689770
申请日：1991-07-17
申请人： Akira Hasegawa , Makoto Kiso , Shinichi Uesato , Masanobu Suzuki , Tomio Ishida , Yutaka Saito
发明人： Akira Hasegawa , Makoto Kiso , Shinichi Uesato , Masanobu Suzuki , Tomio Ishida , Yutaka Saito
IPC分类号： A61K31/665 , A61K31/70 , A61K31/7024 , A61P35/00 , A61P37/04 , C07F9/655 , C07H13/06
CPC分类号： C07H13/06 , C07F9/6552 , Y02P20/55
摘要： Lipid A monosaccharide analogues of the following general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a hydroxyl group, 1 is an integer of 8-14, m is an integer of 11-17 integer, and n is 8-14 integer.

10. 发明授权

US5380832A Ganglioside GM3 analogs 失效
标题翻译：神经节苷脂GM3类似物
公开(公告)号：US5380832A
公开(公告)日：1995-01-10
申请号：US243525
申请日：1994-05-16
申请人： Akira Hasegawa , Makoto Kiso
发明人： Akira Hasegawa , Makoto Kiso
IPC分类号： A61K31/70 , A61K31/7028 , A61P31/12 , A61P31/16 , C07H5/06 , C07H15/10 , C12N9/99 , A61K31/72
CPC分类号： C07H15/10
摘要： Disclosed are ganglioside GM.sub.3 analogs represented by the formula ##STR1## in which X represents a radical of the following formula ##STR2## wherein at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the remainder is hydroxyl; ##STR3## wherein at least one of R.sub.5 and R.sub.6 is hydrogen and the remainder is methyl; ##STR4## wherein m is an integer of 15 to 25, l is an integer of 0 to 3, n is an integer of 11 to 15 and Ac represents acetyl. The ganglioside GM.sub.3 analogs are expected to possess an inhibitory activity for influenza virus.
摘要翻译：公开了由式“IMAGE”表示的神经节苷脂GM3类似物，其中X表示下式的基团，其中R 1，R 2，R 3和R 4中的至少一个为氢，其余为羟基; 其中R 5和R 6中的至少一个是氢，其余是甲基; 其中m为15〜25的整数，l为0〜3的整数，n为11〜15的整数，Ac为乙酰基。神经节苷脂GM3类似物预计对流感病毒具有抑制活性。

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