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1. 发明授权

US5023239A Sialosyl cholesterol, process for producing the same, and neuropathy remedy comprising the same 失效
标题翻译：唾液酸胆固醇，其制备方法和包含其的神经病学治疗药物
公开(公告)号：US5023239A
公开(公告)日：1991-06-11
申请号：US150647
申请日：1988-01-07
申请人： Haruo Ogura , Kimio Furuhata , Shingo Sato , Masayoshi Ito , Yoshiyasu Shitori , Yoshitaka Nagai
发明人： Haruo Ogura , Kimio Furuhata , Shingo Sato , Masayoshi Ito , Yoshiyasu Shitori , Yoshitaka Nagai
IPC分类号： C07J41/00 , C07J51/00
CPC分类号： C07J41/0055 , C07J51/00
摘要： The present invention relates to a sodium salt of sialosyl cholesterol. The present compound has an excellent high water solubility, and therefore the compound is very useful as a medicine to be used for curing various diseases derived from lesions of peripheral or central nerves.

2. 发明授权

US4447600A N-Acetylneuraminic acid derivatives and the preparation thereof 失效
标题翻译： N-乙酰神经氨酸衍生物及其制备方法
公开(公告)号：US4447600A
公开(公告)日：1984-05-08
申请号：US380401
申请日：1982-05-20
申请人： Haruo Ogura , Kimio Furuhata , Toshiaki Osawa , Satoshi Toyoshima , Yoshiyasu Shitori , Masayoshi Ito
发明人： Haruo Ogura , Kimio Furuhata , Toshiaki Osawa , Satoshi Toyoshima , Yoshiyasu Shitori , Masayoshi Ito
IPC分类号： C07H13/06 , A61K31/70 , A61K31/7024 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P37/00 , C07H13/04 , C07H19/06 , C07H19/067 , C07H19/16 , C07H19/167 , C07H17/00
CPC分类号： C07H13/04 , C07H19/06 , C07H19/16
摘要： Nucleoside or glucose derivatives of N-acetylneuraminic acids are provided, which have immunological activity, are clinically useful, as an immuno suppressive, in particular to treat autoimmune disease such as collagenosis disease without causing any serious side-effects and may be prepared by subjecting a halide of N-acetylneuraminate derivative together with a nucleoside or a glucose to Koenigs-Knorr reaction.
摘要翻译：提供具有免疫学活性的N-乙酰神经氨酸的核苷或葡萄糖衍生物在临床上可用作免疫抑制剂，特别是治疗自身免疫性疾病如胶原病，而不引起任何严重的副作用，并且可以通过使 N-乙酰神经氨酸衍生物的卤化物与核苷或葡萄糖一起转化为Koenigs-Knorr反应。

3. 发明授权

US5126330A Sialosyl cholesterol and neuropathy remedy comprising the same 失效
标题翻译：唾液酸胆固醇和包含其的神经病变药物
公开(公告)号：US5126330A
公开(公告)日：1992-06-30
申请号：US649531
申请日：1991-02-01
申请人： Haruo Ogura , Kimio Furuhata , Shingo Sato , Masayoshi Ito , Yoshiyasu Shitori , Yoshitaka Nagai
发明人： Haruo Ogura , Kimio Furuhata , Shingo Sato , Masayoshi Ito , Yoshiyasu Shitori , Yoshitaka Nagai
IPC分类号： C07J41/00 , C07J51/00
CPC分类号： C07J41/0055 , C07J51/00
摘要： The present invention relates to a sodium salt of sialosyl cholesterol. The present compound has an excellent high water solubility, and therefore the compound is very useful as a medicine to be used for treating various diseases derived from lesions of peripheral or central nerves.

4. 发明授权

US4691012A Sialic acid derivative and process for preparing the same 失效
标题翻译：唾液酸衍生物及其制备方法
公开(公告)号：US4691012A
公开(公告)日：1987-09-01
申请号：US708638
申请日：1985-03-06
申请人： Haruo Ogura , Kimio Furuhata , Toshiaki Osawa , Satoshi Toyoshima , Yoshiyasu Shitori , Masayoshi Ito , Shoji Yoshimura
发明人： Haruo Ogura , Kimio Furuhata , Toshiaki Osawa , Satoshi Toyoshima , Yoshiyasu Shitori , Masayoshi Ito , Shoji Yoshimura
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P35/00 , C07H19/04 , C07H19/06 , C07H19/067 , C07H19/16 , C07H19/167 , C07H17/00
CPC分类号： C07H19/06 , C07H19/04
摘要： A novel N-acetylneuraminic acid derivative, represented by the general formula: ##STR1## wherein the R.sup.1 groups are, independently, hydrogen or acetyl; R.sup.2 is a nucleoside residue; and R.sup.3 is carboxyl or methoxycarbonyl.The N-acetylneuraminic acid derivative is useful in inhibiting metastasis of cancer cells. Also provided is a process for the preparation of the derivatives.
摘要翻译：一种新的N-乙酰神经氨酸衍生物，由以下通式表示：其中R1基团独立地为氢或乙酰基; R2是核苷残基; R3为羧基或甲氧基羰基。 N-乙酰神经氨酸衍生物可用于抑制癌细胞的转移。还提供了制备衍生物的方法。

5. 发明授权

US4914195A Process for preparing N-acetylneuraminic acid derivatives 失效
标题翻译： N-乙酰神经氨酸衍生物的制备方法
公开(公告)号：US4914195A
公开(公告)日：1990-04-03
申请号：US664686
申请日：1984-11-26
申请人： Haruo Ogura , Kimio Furuhata , Yoshiyasu Shitori , Masayoshi Ito
发明人： Haruo Ogura , Kimio Furuhata , Yoshiyasu Shitori , Masayoshi Ito
IPC分类号： C07H13/06 , C07H13/04 , C07H13/08 , C07H19/06 , C07H19/16
CPC分类号： C07H13/04 , C07H19/06 , C07H19/16
摘要： A new process for preparing halides of N-acetylneuraminic acids useful as an intermediate in preparing new N-acetylneuraminic acid derivatives having an excellent immunological activity is provided, which process comprises simultaneously acetylating and halogenating an esterified N-acetylneuraminic acid with the aid of an acetyl halide, and according to the process, the halides may be obtained in high yield of about 90%.
摘要翻译：提供了用于制备具有优异免疫活性的新的N-乙酰神经氨酸衍生物的中间体的N-乙酰神经氨酸卤化物的新方法，该方法同时借助乙酰基乙酰化和卤化酯化的N-乙酰神经氨酸卤化物，根据该方法，可以以约90％的高产率获得卤化物。

6. 发明授权

US4774327A N-glycolylneuraminic acid derivative 失效
标题翻译： N-羟乙酰神经氨酸衍生物
公开(公告)号：US4774327A
公开(公告)日：1988-09-27
申请号：US917559
申请日：1986-10-10
申请人： Haruo Ogura , Kimio Furuhata , Masayoshi Ito , Yoshiyasu Shitori
发明人： Haruo Ogura , Kimio Furuhata , Masayoshi Ito , Yoshiyasu Shitori
IPC分类号： C07H13/04 , C07H13/06 , C07H13/08 , C07H15/04 , C07B59/00
CPC分类号： C07H13/04 , C07H15/04
摘要： This invention provides a novel compound having the following formula: ##STR1## This compound is a useful intermediate for the preparation of N-glycolylneuraminic acid: ##STR2##
摘要翻译：本发明提供了具有下式的新化合物：该化合物是制备N-羟乙酰神经氨酸的有用中间体：

7. 发明授权

US4025622A Novel sugar ureide and thioureide derivatives 失效
标题翻译：新型糖苷和硫脲衍生物
公开(公告)号：US4025622A
公开(公告)日：1977-05-24
申请号：US553121
申请日：1975-02-26
申请人： Haruo Ogura , Hiroshi Takahashi
发明人： Haruo Ogura , Hiroshi Takahashi
IPC分类号： C07C265/04 , C07C265/12 , C07C327/54 , C07C335/26 , C07D213/75 , C07D213/86 , C07D231/40 , C07D239/69 , C07D261/16 , C07D277/52 , C07D277/82 , C07D499/68 , C07D501/20 , C07H13/00 , C07H13/12 , C07H15/18 , A61K31/13 , C07H5/04
CPC分类号： C07D213/75 , C07C265/00 , C07C327/54 , C07C335/26 , C07D213/86 , C07D231/40 , C07D239/69 , C07D261/16 , C07D277/52 , C07D277/82 , C07H13/00 , C07H13/12 , C07H15/18
摘要： Novel sugar ureide and thioureide derivatives are provided by this invention, which exhibit certain antibacterial activity against a variety of gram-positive and gram-negative bacteria and useful in therapeutic treatment of bacterial infections. The compounds have the formula ##STR1## wherein R.sub.1 is a monovalent residue of aldose, aldonic acid and their 2-amino derivatives, R.sub.2 is an aralkyl, heterocyclic, sulfamoylaryl, R.sub.3 CONH or R.sub.4 NH-- where R.sub.3 is a heterocyclic and R.sub.4 is an aryl group and Y is oxygen or sulfur atom, which are prepared by reacting an isocyanate or isothiocyanate of the formula R.sub.1 NC=Y with an amino compound of the formula R.sub.2 NH.sub.2.
摘要翻译：本发明提供了新型糖苷和硫脲衍生物，其对各种革兰氏阳性和革兰氏阴性细菌具有一定的抗菌活性，可用于治疗细菌感染。该化合物具有下式：其中R1是醛糖，醛糖酸及其2-氨基衍生物的单价残基，R2是芳烷基，杂环基，氨磺酰基芳基，R3CONH或R4NH-，其中R3是杂环，R4是芳基 Y是氧或硫原子，其通过使式R 1 NC = Y的异氰酸酯或异硫氰酸酯与式R 2 NH 2的氨基化合物反应制备。

8. 发明授权

US4939156A New tetramethyl-cis-diaza-bicyclo{4.2.0}octane-3,5-dione derivatives having differentiation-inducing activity and antiviral activity 失效
标题翻译：具有分化诱导活性和抗病毒活性的新的四甲基 - 顺 - 二氮杂双环{4.2.0}辛烷-3,5-二酮衍生物
公开(公告)号：US4939156A
公开(公告)日：1990-07-03
申请号：US219200
申请日：1988-07-08
申请人： Motoo Hozumi , Tsuneo Itoh , Yoshio Honma , Norio Kawahara , Ichiro Ishikawa , Haruo Ogura
发明人： Motoo Hozumi , Tsuneo Itoh , Yoshio Honma , Norio Kawahara , Ichiro Ishikawa , Haruo Ogura
IPC分类号： C07D239/70 , C07H19/06
CPC分类号： C07H19/06 , C07D239/70
摘要： As new compounds are now provided 7,7,8,8,-tetramethyl-cis-diaza-bicyclo{4.2.0}octane-3,5,-dione derivatives which have an activity to induce the differentiation of tumor cells and are useful as antitumor agent, and which also have an antiviral activity against various viruses and are useful as antiviral agent. These new derivatives may be produced by a photo-addition reaction of a uracil compound with 2,3-dimethyl-2-butene.

9. 发明授权

US4427768A Method of hardening gelatin 失效
标题翻译：硬化明胶的方法
公开(公告)号：US4427768A
公开(公告)日：1984-01-24
申请号：US394988
申请日：1982-07-02
申请人： Katuji Kitatani , Hidefumi Sera , Atsuaki Arai , Masasi Ogawa , Kunio Ishigaki , Haruo Ogura
发明人： Katuji Kitatani , Hidefumi Sera , Atsuaki Arai , Masasi Ogawa , Kunio Ishigaki , Haruo Ogura
IPC分类号： C07D249/18 , C07D207/46 , C07D209/44 , C07D209/48 , C07D209/52 , C07D211/94 , C08K5/32 , C08K5/41 , C08L89/00 , G03C1/30
CPC分类号： C07D209/48 , C07D207/46 , C07D209/52 , G03C1/30
摘要： A method of hardening gelatin is described comprising treating gelatin with a compound of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 can each represent a monovalent group including a carbon atom or a nitrogen atom forming a bond together with the nitrogen atom N forming an acid ester in the formula (I); or R.sup.1 and R.sup.2 together can form a heterocyclic ring together with said nitrogen atom N, andn is 1 or 2; andwhen n is 1, X is ##STR2## and Y is an alkyl group, an aryl group or an aralkyl group; and when n is 2, X is ##STR3##
摘要翻译：描述了一种硬化明胶的方法，其包括用式（I）化合物（I）处理明胶，其中R 1和R 2各自表示与氮原子或氮原子一起形成一个氮原子的一价基团在式（I）中形成酸酯的原子N; 或者R 1和R 2一起可与所述氮原子N一起形成杂环，n为1或2; 当n为1时，X为“IMA”，Y为烷基，芳基或芳烷基; 当n为2时，X为

10. 发明授权

US4341707A Imido carbonate compound, production thereof and uses thereof as reagent for forming active ester of amino acids 失效
标题翻译：酰亚胺碳酸酯化合物，其制备方法和用作形成氨基酸活性酯的试剂
公开(公告)号：US4341707A
公开(公告)日：1982-07-27
申请号：US141365
申请日：1980-04-18
申请人： Haruo Ogura , Kazuyoshi Takeda
发明人： Haruo Ogura , Kazuyoshi Takeda
IPC分类号： C07D207/14 , C07D207/46 , C07D209/48 , C07D209/72 , C07D209/76 , C07D235/26 , C07K1/08 , C07K1/10 , C07D403/12 , C07D498/04 , C07F9/09
CPC分类号： C07D209/48 , C07D207/14 , C07D207/46 , C07D209/76 , C07D235/26 , C07K1/10
摘要： A new carbonate compound which is N,N'-di-succinimidyl carbonate, N,N'-diphthalimidyl carbonate or N,N'-bis(5-norbornene-2,3-dicarboxyimidyl) carbonate is produced by reacting an N-hydroxy compound of the formulaR-OHwherein R is succinimido, phthalimido or 5-norbornene-2,3-dicarboximido group, with a silylating agent, followed by reacting the resultant silylated product with phosgene, or alternatively by reacting said N-hydroxy compound with trichloromethyl chloroformate either in the molten state or in the presence of a non-polar organic solvent such as xylene. This new carbonate compound is useful not only as a reagent for forming active esters from amino acid but also as a reagent for introducing a carbonyl group between a pair of amino groups, a pair of amino and hydroxyl groups or a pair of amino and mercapto groups, for producing an isothiocyanate from a dithicarbamic acid by removal of hydrogen sulfide from the latter, and for producing acrylic acid derivatives from N-protected serine by dehydration of the latter.
摘要翻译：碳酸N，N'-二琥珀酰亚胺酯，碳酸N，N'-二邻苯二甲酰亚胺酯或N，N'-双（5-降冰片烯-2,3-二羧基亚氨基）碳酸酯的碳酸酯化合物是通过使N-羟基式R-OH的化合物，其中R是琥珀酰亚胺基，苯二甲酰亚氨基或5-降冰片烯-2,3-二羧酰亚胺基，与甲硅烷基化试剂反应，然后使所得的甲硅烷基化产物与光气反应，或者通过使所述N-羟基化合物与或者在非极性有机溶剂如二甲苯的存在下，氯甲酸三氯甲酯。这种新的碳酸酯化合物不仅可用作从氨基酸形成活性酯的试剂，而且可用作在一对氨基，一对氨基和羟基之间引入羰基的试剂或一对氨基和巯基用于通过从后者中除去硫化氢从二硫氨酸生产异硫氰酸酯，并通过后者的脱水由N-保护的丝氨酸制备丙烯酸衍生物。

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