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1.发明申请TREHALOSE COMPOUND, PROCESS FOR PRODUCTION OF THE COMPOUND, AND IMMUNO-STIMULATIVE AGENT COMPRISING THE COMPOUND 审中-公开化合物的制备方法，化合物的生产方法和包含化合物的免疫刺激剂公开(公告)号：US20100093993A1
公开(公告)日：2010-04-15
申请号：US12525184
申请日：2008-01-30
IPC分类号： C08B37/00
摘要： An object of the present invention is to provide a novel trehalose compound that exhibits excellent immunostimulating activity and that can be supplied in a large quantity in an industrial scale, and a method for producing the trehalose compound, wherein the trehalose compound of the present invention exhibits excellent immunostimulating activity, and is represented by general formula (1) below: wherein R1, R2, R3 and R4 may be the same or different, and independently represent a C10-16 alkyl group. The trehalose compound of the present invention is produced by removing a protective group (R5) for a hydroxyl group from a trehalose compound represented by general formula (5) below: wherein R1, R2, R3 and R4 are the same as above. R5 is a protective group for a hydroxyl group.
摘要翻译： 本发明的目的是提供一种显示出优异的免疫刺激活性并且可以以工业规模大量供应的新型海藻糖化合物，以及本发明的海藻糖化合物显示出的海藻糖化合物的制造方法 优异的免疫刺激活性，由以下通式（1）表示：其中R1，R2，R3和R4可以相同或不同，并且独立地表示C10-16烷基。 本发明的海藻糖化合物是通过从下述通式（5）表示的海藻糖化合物中除去羟基的保护基（R5）而制备的：其中R1，R2，R3和R4与上述相同。 R5是羟基的保护基。
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2.发明授权Bis(tetrahydrofuran) compound, method for production of the compund, and use of the compound 失效双（四氢呋喃）化合物，化合物的制备方法和化合物的用途公开(公告)号：US08569524B2
公开(公告)日：2013-10-29
申请号：US12529500
申请日：2008-02-28
IPC分类号： C07D493/00
CPC分类号： C07D493/10
摘要： The present invention provides a new bis(tetrahydrofuran) compound having an excellent neurotrophic factor activity-enhancing effect, and a process for producing the same. The bis(tetrahydrofuran) compound of the present invention is represented by formula (1): wherein R1 and R2 are the same or different, and represent a C1-4 alkyl group, a C1-5 alkoxy group, an aryl C1-5 alkoxy group, a C2-5 alkenyloxy group, or an aryl C2-5 alkenyloxy group, or R1 and R2 together represent ═O or ═CH2; R3 represents a hydrogen atom or a group —CH2—O—R4; R4 represents a C1-4 alkyl group, a C1-5 alkylcarbonyl group, or an aryl C1-4 alkyl group that may have a substituent on an aryl ring; and a carbon-carbon bond between “a” and “b” represents a single bond or a double bond. The bis(tetrahydrofuran) compound has an excellent neurotrophic factor activity-enhancing effect.
摘要翻译： 本发明提供了具有优异的神经营养因子活性增强作用的新的双（四氢呋喃）化合物及其制造方法。 本发明的双（四氢呋喃）化合物由式（1）表示：其中R1和R2相同或不同，表示C1-4烷基，C1-5烷氧基，芳基C1-5烷氧基 基团，C2-5烯氧基或芳基C2-5烯氧基，或R1和R2一起表示= O或= CH 2; R3表示氢原子或基团-CH2-O-R4; R4表示可以在芳基环上具有取代基的C1-4烷基，C1-5烷基羰基或芳基C1-4烷基; “a”和“b”之间的碳 - 碳键表示单键或双键。 双（四氢呋喃）化合物具有优异的神经营养因子活性增强作用。
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3.发明授权Sphingosine compound, method for producing the same, and sphingomyelinase inhibitor 失效鞘氨醇化合物，其制造方法和鞘磷脂酶抑制剂公开(公告)号：US08093395B2
公开(公告)日：2012-01-10
申请号：US12530311
申请日：2008-03-05
申请人： Mugio Nishizawa , Hiroshi Imagawa , Jun Sakurai , Masataka Oda
发明人： Mugio Nishizawa , Hiroshi Imagawa , Jun Sakurai , Masataka Oda
IPC分类号： C07D211/70 , A61K31/44
CPC分类号： C07D213/22
摘要： An object of the invention is to provide a novel sphingosine compound with an inhibitory activity against sphingomyelinase, and a method for producing the sphingosine compound.The novel sphingosine compound or a salt thereof according to the invention is represented by Formula (1): wherein one of R1 and R2 is hydrogen, and the other is a group represented by Formula (G): wherein n is 0 or 1; and R3 is hydrogen, C1-23 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C3-8 cycloalkyloxy, phenyl, or furil.
摘要翻译： 本发明的目的是提供一种对鞘磷脂酶具有抑制活性的新型鞘氨醇化合物及其制备方法。 根据本发明的新型鞘氨醇化合物或其盐由式（1）表示：其中R1和R2之一是氢，另一个是由式（G）表示的基团：其中n是0或1; 和R 3是氢，C 1-3烷基，C 3-8环烷基，C 2-6烯基，C 1-6烷氧基，C 3-8环烷氧基，苯基或杂环。
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4.发明授权Trehalose compound, method for producing same, and pharmaceutical product containing the compound 失效海藻糖化合物，其制造方法以及含有该化合物的药物公开(公告)号：US08741871B2
公开(公告)日：2014-06-03
申请号：US13126842
申请日：2009-10-27
申请人： Mugio Nishizawa , Hiroshi Imagawa , Hirofumi Yamamoto , Jun Sakurai , Masataka Oda , Reiko Nishizawa
IPC分类号： A61K31/7024 , C07H13/06 , C07H13/08
CPC分类号： C07H13/06 , A61K31/7024 , C07H13/04 , C07H13/08 , Y02A50/473
摘要： A trehalose compound having high immunopotentiating activity and low toxicity is represented by formula (1). (In the formula, X and X′ each represents a phenyl, a naphthyl, R1—CHR1— (wherein R1 and R2 each represents a C7-C21 alkyl group or the like) or the like; and n and n′ each independently represents an integer of 0-3). The compound exhibits a high activating effect on macrophages and neutrophils.
摘要翻译： 具有高免疫增强活性和低毒性的海藻糖化合物由式（1）表示。 （式中，X，X'各自表示苯基，萘基，R 1 -CHR 1-（其中，R 1和R 2各自表示C 7〜C 21烷基等）等，n和n'各自独立地表示 0-3的整数）。 该化合物对巨噬细胞和嗜中性粒细胞表现出高活化作用。
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公开(公告)号：US08163713B2
公开(公告)日：2012-04-24
申请号：US12294800
申请日：2007-03-22
摘要： The object of the present invention is to provide a novel trehalose compound having a high affinity for an adenosine A3 receptor. The trehalose compound of the present invention is represented by General Formula (1): wherein X and X′ represent a hydrogen atom, and the like; Y and Y′ independently represent an oxygen atom, and the like; R1 and R2 independently represent a C1-C6 alkyl group; and R3 and R4 independently represent a C3-C6 alkyl group. The trehalose compound of the present invention has a remarkably high affinity for an adenosine A3 receptor.
摘要翻译： 本发明的目的是提供对腺苷A3受体具有高亲和力的新型海藻糖化合物。 本发明的海藻糖化合物由通式（1）表示：其中X和X'表示氢原子等; Y和Y'独立地表示氧原子等; R1和R2独立地表示C1-C6烷基; 并且R 3和R 4独立地表示C 3 -C 6烷基。 本发明的海藻糖化合物对腺苷A3受体具有非常高的亲和力。
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6.发明申请BIS(TETRAHYDROFURAN) COMPOUND, METHOD FOR PRODUCTION OF THE COMPOUND, AND USE OF THE COMPOUND 失效BIS（四氢呋喃）化合物，该化合物的生产方法和化合物的使用公开(公告)号：US20100105931A1
公开(公告)日：2010-04-29
申请号：US12529500
申请日：2008-02-28
IPC分类号： C07D493/04
CPC分类号： C07D493/10
摘要： The present invention provides a new bis(tetrahydrofuran) compound having an excellent neurotrophic factor activity-enhancing effect, and a process for producing the same. The bis(tetrahydrofuran) compound of the present invention is represented by formula (1): wherein R1 and R2 are the same or different, and represent a C1-4 alkyl group, a C1-5 alkoxy group, an aryl C1-5 alkoxy group, a C2-5 alkenyloxy group, or an aryl C2-5 alkenyloxy group, or R1 and R2 together represent ═O or ═CH2; R3 represents a hydrogen atom or a group —CH2—O—R4; R4 represents a C1-4 alkyl group, a C1-5 alkylcarbonyl group, or an aryl C1-4 alkyl group that may have a substituent on an aryl ring; and a carbon-carbon bond between “a” and “b” represents a single bond or a double bond. The bis(tetrahydrofuran) compound has an excellent neurotrophic factor activity-enhancing effect.
摘要翻译： 本发明提供了具有优异的神经营养因子活性增强作用的新的双（四氢呋喃）化合物及其制造方法。 本发明的双（四氢呋喃）化合物由式（1）表示：其中R1和R2相同或不同，表示C1-4烷基，C1-5烷氧基，芳基C1-5烷氧基 基团，C2-5烯氧基或芳基C2-5烯氧基，或R1和R2一起表示= O或= CH2; R3表示氢原子或基团-CH2-O-R4; R4表示可以在芳基环上具有取代基的C1-4烷基，C1-5烷基羰基或芳基C1-4烷基; “a”和“b”之间的碳 - 碳键表示单键或双键。 双（四氢呋喃）化合物具有优异的神经营养因子活性增强作用。
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7.发明申请TREHALOSE COMPOUND, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL PRODUCT CONTAINING THE COMPOUND 失效TREHALOSE化合物，其生产方法和含有该化合物的药物产品公开(公告)号：US20110218171A1
公开(公告)日：2011-09-08
申请号：US13126842
申请日：2009-10-27
申请人： Mugio Nishizawa , Hiroshi Imagawa , Hirofumi Yamamoto , Jun Sakurai , Masataka Oda , Reiko Nishizawa
发明人： Mugio Nishizawa , Hiroshi Imagawa , Hirofumi Yamamoto , Jun Sakurai , Masataka Oda , Reiko Nishizawa
CPC分类号： C07H13/06 , A61K31/7024 , C07H13/04 , C07H13/08 , Y02A50/473
摘要： A trehalose compound having high immunopotentiating activity and low toxicity is represented by formula (1). (In the formula, X and X′ each represents a phenyl, a naphthyl, R1—CHR1— (wherein R1 and R2 each represents a C7-C21 alkyl group or the like) or the like; and n and n′ each independently represents an integer of 0-3). The compound exhibits a high activating effect on macrophages and neutrophils.
摘要翻译： 具有高免疫增强活性和低毒性的海藻糖化合物由式（1）表示。 （式中，X，X'各自表示苯基，萘基，R 1 -CHR 1-（其中，R 1和R 2各自表示C 7〜C 21烷基等）等，n和n'各自独立地表示 0-3的整数）。 该化合物对巨噬细胞和嗜中性粒细胞表现出高活化作用。
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公开(公告)号：US20100249057A1
公开(公告)日：2010-09-30
申请号：US12294800
申请日：2007-03-22
摘要： The object of the present invention is to provide a novel trehalose compound having a high affinity for an adenosine A3 receptor. The trehalose compound of the present invention is represented by General Formula (1): wherein X and X′ represent a hydrogen atom, and the like; Y and Y′ independently represent an oxygen atom, and the like; R1 and R2 independently represent a C1-C6 alkyl group; and R3 and R4 independently represent a C3-C6 alkyl group. The trehalose compound of the present invention has a remarkably high affinity for an adenosine A3 receptor.
摘要翻译： 本发明的目的是提供对腺苷A3受体具有高亲和力的新型海藻糖化合物。 本发明的海藻糖化合物由通式（1）表示：其中X和X'表示氢原子等; Y和Y'独立地表示氧原子等; R1和R2独立地表示C1-C6烷基; 并且R 3和R 4独立地表示C 3 -C 6烷基。 本发明的海藻糖化合物对腺苷A3受体具有非常高的亲和力。
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9.发明申请SPHINGOSINE COMPOUND, METHOD FOR PRODUCING THE SAME, AND SPHINGOMYELINASE INHIBITOR 失效鞘氨醇复合物，其制备方法和丝氨酸激酶抑制剂公开(公告)号：US20100099881A1
公开(公告)日：2010-04-22
申请号：US12530311
申请日：2008-03-05
申请人： Mugio Nishizawa , Hiroshi Imagawa , Jun Sakurai , Masataka Oda
发明人： Mugio Nishizawa , Hiroshi Imagawa , Jun Sakurai , Masataka Oda
IPC分类号： C07D401/06
CPC分类号： C07D213/22
摘要： An object of the invention is to provide a novel sphingosine compound with an inhibitory activity against sphingomyelinase, and a method for producing the sphingosine compound.The novel sphingosine compound or a salt thereof according to the invention is represented by Formula (1): wherein one of R1 and R2 is hydrogen, and the other is a group represented by Formula (G): wherein n is 0 or 1; and R3 is hydrogen, C1-23 alkyl, C3-8 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C3-8 cycloalkyloxy, phenyl, or furil.
摘要翻译： 本发明的目的是提供一种对鞘磷脂酶具有抑制活性的新型鞘氨醇化合物及其制备方法。 根据本发明的新型鞘氨醇化合物或其盐由式（1）表示：其中R1和R2之一是氢，另一个是由式（G）表示的基团：其中n是0或1; 和R 3是氢，C 1-3烷基，C 3-8环烷基，C 2-6烯基，C 1-6烷氧基，C 3-8环烷氧基，苯基或杂环。
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