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1. 发明专利

JP2005075794A Glucosylation method of sugar acceptor with sialic acid as sugar donor 审中-公开
标题翻译：具有蔗糖糖的蔗糖的糖酵解方法
公开(公告)号：JP2005075794A
公开(公告)日：2005-03-24
申请号：JP2003309716
申请日：2003-09-02
申请人： Chemgenesis Inc , Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 株式会社ケムジェネシス , 孝志高橋
发明人： TAKAHASHI TAKASHI , TANAKA HIROSHI , ADACHI MASAATSU
IPC分类号： C07H5/04
CPC分类号： Y02P20/55
摘要： PROBLEM TO BE SOLVED: To perform an α-selective glucosylation reaction under a mild condition by using a sialic acid as a sugar donor. SOLUTION: The hydroxy group of a sialic acid is protected with a proper protective group, the 5-amino group of the sialic acid is protected with 2,2,2-trichloroethoxycarbonyl group and a phenylthio group is introduced to the anomer site as an eliminable group. An α-glycoside bond is selectively formed by using the obtained sialic acid derivative as a sugar donor and an N-iodosuccinimide-trifluoromethanesulfonic acid as a promoter. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：通过使用唾液酸作为糖供体，在温和条件下进行α-选择性葡糖基化反应。解决方案：用适当的保护基保护唾液酸的羟基，用2,2,2-三氯乙氧基羰基保护唾液酸的5-氨基，并将苯硫基引入到前体位点作为一个可消除的群体。通过使用得到的唾液酸衍生物作为糖供体和N-碘代琥珀酰亚胺 - 三氟甲磺酸作为促进剂，选择性地形成α-糖苷键。版权所有（C）2005，JPO＆NCIPI

2. 发明专利

JP2004136228A Automatic liquid-phase organic synthesis apparatus 有权
公开(公告)号：JP2004136228A
公开(公告)日：2004-05-13
申请号：JP2002304441
申请日：2002-10-18
申请人： Chemgenesis Inc , 株式会社ケムジェネシス
发明人： MACHIDA KAZUHIRO , HIROSE YOICHIRO , SEKIYAMA SHIGETOSHI , TAKAHASHI TAKASHI , FUSE SHINICHIRO
IPC分类号： B01J19/00 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide an automatic synthesis apparatus which can suppress increase in the numbers of pipelines and valves accompanying the increase in the number of reaction units.
SOLUTION: In this automatic synthesis apparatus, the inside of an aluminum-made rack is divided into a fixed area A and a variable area B. In the lower stage of the fixed area A, an enclosure 1 for a waste liquid tank, a trap, a pump, etc., is arranged; in the middle stage, a computer 2 for control is arranged; and in the upper stage, an enclosure 3 for a relay and boards is arranged. Next to the enclosure 3, a cleaning unit 4 is arranged. In the middle stage, a liquid separating unit 5, a drying unit 6, a recovery unit 7, and a transfer unit 8 are arranged next to the computer 2 for control.
COPYRIGHT: (C)2004,JPO

3. 发明专利

JP2013129660A Low-viscosity liquid crystal compound 审中-公开
标题翻译：低粘度液晶化合物
公开(公告)号：JP2013129660A
公开(公告)日：2013-07-04
申请号：JP2013027100
申请日：2013-02-14
申请人： Chemgenesis Inc , 株式会社ケムジェネシス
发明人： IKEDA YUTAKA , YAMASHITA HAYATO , TSUCHIGURO ICHIRO , IMUTA SATOSHI , HIROKI YASUHIRO , TAKAHASHI TAKASHI
IPC分类号： C07C69/533 , A61K9/08 , A61K47/10 , A61K47/26 , C07C43/23 , C07D307/62 , C07H15/10
CPC分类号： A61K47/14 , A61K9/0019 , A61K9/0024 , A61K47/08 , A61K47/10 , A61K47/22 , A61K47/26 , C07H15/10 , C09K19/06
摘要： PROBLEM TO BE SOLVED: To provide a liquid crystal compound that can be used as a base for injection formulations.SOLUTION: An amphipathic compound has the following general formula (I), wherein X and Y each denote a hydrogen atom or together denote an oxygen atom, n denotes an integer of 0, m denotes an integer 1 or 2, and R denotes a hydrophilic group generated by removal of one hydroxyl group from any one selected from the group consisting of glycerol, erythritol, pentaerythritol, diglycerol, triglycerol, xylose, sorbitol, ascorbic acid, glucose, galactose, mannose, dipentaerythritol, maltose, mannitol, and xylitol. In addition, a base for injection formulations and a depot formulation comprising the same are disclosed.
摘要翻译：要解决的问题：提供可用作注射制剂基质的液晶化合物。解决方案：两性化合物具有以下通式（I），其中X和Y各自表示氢原子或一起表示氧原子，n表示0的整数，m表示整数1或2，R表示通过从选自甘油，赤藓糖醇，季戊四醇，双甘油，三甘油，木糖中的任何一种除去一个羟基而产生的亲水基团，山梨糖醇，抗坏血酸，葡萄糖，半乳糖，甘露糖，二季戊四醇，麦芽糖，甘露糖醇和木糖醇。此外，公开了注射用制剂的基质和包含其的药剂制剂。

4. 发明专利

JP2010126454A Beauveriolide having acat2 inhibitory activity 审中-公开
标题翻译：具有ACAT2抑制活性的BEAUVERIOLIDE
公开(公告)号：JP2010126454A
公开(公告)日：2010-06-10
申请号：JP2008300016
申请日：2008-11-25
申请人： Chemgenesis Inc , Kitasato Institute , 学校法人北里研究所 , 株式会社ケムジェネシス
发明人： KODA HIROSHI , OMURA SATOSHI , TAKAHASHI TAKASHI , DOI TAKAYUKI , TSUCHIGURO ICHIRO , IMUTA SATOSHI , MATSUDA DAISUKE , OSHIRO TAICHI
IPC分类号： C07K5/12 , A61K38/55 , A61P3/04 , A61P3/06 , A61P9/10 , A61P9/12 , A61P43/00 , C12N9/99
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/0821
摘要： PROBLEM TO BE SOLVED: To provide a compound having ACAT2 inhibitory activity of action mechanism different from that of statin-based medicine. SOLUTION: The beauveriolide derivative is represented by general formula (I) or (II), (wherein R 1 is methyl or H; R 2 is, for example, butyl; X is an alanine residue; and Y and Z are each an amino acid residue), a salt, a solvate and a hydrate thereof. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供具有与基于他汀类药物不同的作用机制的具有ACAT2抑制活性的化合物。解决方案：通过通式（I）或（II）表示，其中R SB为甲基或H; R SB 2为例如丁基; X是丙氨酸残基; Y和Z各自是氨基酸残基），其盐，溶剂合物和水合物。版权所有（C）2010，JPO＆INPIT

5. 发明专利

JP2003064097A New cyclic depsipeptide and method for producing the same 审中-公开
标题翻译：新的循环抑制剂及其生产方法
公开(公告)号：JP2003064097A
公开(公告)日：2003-03-05
申请号：JP2001295052
申请日：2001-08-23
申请人： Chemgenesis Inc , Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 株式会社ケムジェネシス , 孝志高橋
发明人： TAKAHASHI TAKASHI , DOI TAKAYUKI , EIMIYA HIROYUKI
IPC分类号： A61K38/00 , A61P35/00 , A61P43/00 , C07K1/06 , C07K7/54 , C40B40/02 , C40B50/06
摘要： PROBLEM TO BE SOLVED: To provide a method for simultaneously synthesizing various kinds of cyclic depsipeptide including aurilide analogue expected to exhibit bioactivities because the aurilide isolated from Dolabella auricularia of Aplysiidae exhibits very strong cytotoxicity and attracts the attention.
SOLUTION: This method utilizes a means of combinatorial synthesis. Many kinds of amino acids are simultaneously reacted after immobilizing the amino acid on a resin. Thereafter, the product is reacted with a fatty acid ester, and the product is cut out from the resin and cyclized to provide the many kinds of the cyclic depeptides simultaneously.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：提供一种同时合成预期显示出生物活性的各种类型的含有尿苷类似物的环状缩酚酸肽的方法，因为分离自蚜虫的耳朵的耳垢表现出非常强的细胞毒性并引起注意。解决方案：该方法采用组合合成手段。在将氨基酸固定在树脂上之后，许多种氨基酸同时发生反应。此后，将产物与脂肪酸酯反应，并从树脂中切出产物并环化，同时提供多种环状肽。

6. 发明专利

JP2013181108A Highly-active complete organic dye compound for dye-sensitized photoelectric conversion element, and photoelectric conversion element using the same 审中-公开
标题翻译：用于透明光电转换元件的高活性完全有机染料化合物和使用该光电转换元件的光电转换元件
公开(公告)号：JP2013181108A
公开(公告)日：2013-09-12
申请号：JP2012045914
申请日：2012-03-01
申请人： Kanto Natural Gas Development Co Ltd , 関東天然瓦斯開発株式会社 , Tokyo Institute Of Technology , 国立大学法人東京工業大学 , Kyushu Institute Of Technology , 国立大学法人九州工業大学 , Chemgenesis Inc , 株式会社ケムジェネシス
发明人： KAIHO TATSUO , TAKAHASHI TAKASHI , FUSE SHINICHIRO , WADA YUJI , YONETANI MASATO , HAYASE SHUJI , IMUTA SATOSHI
IPC分类号： C09B23/00 , C07D409/14 , C07D495/04 , H01L31/04 , H01M14/00
CPC分类号： Y02E10/542
摘要： PROBLEM TO BE SOLVED: To provide a complete organic dye compound used for an excellent dye-sensitized photoelectric conversion element, and to provide a photoelectric conversion element using the same.SOLUTION: There is provided an organic dye compound shown by X-U-Z (wherein X, U and Z are a donor site, electronic conjugation site and accepter site, respectively) such as a figure below.
摘要翻译：要解决的问题：提供用于优异的染料敏化光电转换元件的完整的有机染料化合物，并提供使用其的光电转换元件。溶液：提供由XUZ表示的有机染料化合物（其中X， U和Z分别是供体位点，电子缀合位点和受体位点），如下图所示。

7. 发明专利

JP2003064094A New cyclic peptide 审中-公开
标题翻译：新循环肽
公开(公告)号：JP2003064094A
公开(公告)日：2003-03-05
申请号：JP2001295045
申请日：2001-08-23
申请人： Chemgenesis Inc , Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 株式会社ケムジェネシス , 孝志高橋
发明人： TAKAHASHI TAKASHI , DOI TAKAYUKI , SHIMAZU SAYAKA
IPC分类号： A61K38/55 , A61P31/14 , A61P43/00 , C07B61/00 , C07K1/113 , C07K5/02
摘要： PROBLEM TO BE SOLVED: To solve the problem that the conformation of a cyclic peptide is urgently required to be restricted and fixed because the cyclic peptide is known to have various kinds of bioactivities exemplified by that as a protease inhibitor, and has a possibility that the cyclic peptide mimicking the β-turn structure becomes the protease inhibitor, but the conformation of the cyclic peptide has a wide freedom, and looses the three-dimensional structure especially in an aqueous solution, to cause the case in which the expected protease inhibiting ability is not exhibited. SOLUTION: This cyclic peptide is obtained by introducing an aromatic ring and two carbonyl groups to the cyclic peptide to restrict and fix the conformation of the cyclic peptide. Various kinds of the conformations become possible by changing the aromatic ring. As a result, various kinds of the bioactive cyclic peptide can be provided.
摘要翻译：要解决的问题为了解决环状肽的构象迫切需要限制和固定的问题，因为已知环状肽具有例如作为蛋白酶抑制剂的各种生物活性，并且具有以下可能性：模拟β-转角结构的环状肽成为蛋白酶抑制剂，但是环状肽的构象具有宽的自由度，特别是在水溶液中失去三维结构，导致预期的蛋白酶抑制能力为没有展出。解决方案：通过向环状肽引入芳环和两个羰基来限制和固定环肽的构象，获得该环肽。通过改变芳环可以使各种构象变得可能。结果，可以提供各种生物活性环肽。

8. 发明专利

JP2003064086A Method for producing new silicon linker 审中-公开
标题翻译：生产新型硅连接器的方法
公开(公告)号：JP2003064086A
公开(公告)日：2003-03-05
申请号：JP2001295046
申请日：2001-08-23
申请人： Chemgenesis Inc , Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 株式会社ケムジェネシス , 孝志高橋
发明人： TAKAHASHI TAKASHI , DOI TAKAYUKI
IPC分类号： C07F7/08 , C40B80/00
摘要： PROBLEM TO BE SOLVED: To provide a method for easily and economically producing a solid carrier bearing as linker hydrosilyl groups used in combinatorial synthesis, solid phase synthesis and the like.
SOLUTION: This method comprises the steps of reacting a di-Grignard reagent to a chloromethyl group-bearing solid carrier followed by filtration to remove excess of the di-Grignard reagent and then reacting a dialkylsilane having functional group highly reactive with the di-Grignard reagent.
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：提供一种容易且经济地制备作为用于组合合成，固相合成等的连接剂氢甲硅烷基的固体载体的方法。解决方案：该方法包括以下步骤：将二格氏试剂与含氯甲基的固体载体反应，然后过滤除去过量的二格氏试剂，然后使具有高反应性的二格基硅烷与二格氏试剂。

9. 发明专利

JP2003064052A New fatty acid derivative 审中-公开
标题翻译：新脂肪酸衍生物
公开(公告)号：JP2003064052A
公开(公告)日：2003-03-05
申请号：JP2001295051
申请日：2001-08-23
申请人： Chemgenesis Inc , Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 株式会社ケムジェネシス , 孝志高橋
发明人： TAKAHASHI TAKASHI , DOI TAKAYUKI , EIMIYA HIROYUKI
IPC分类号： C07C323/12 , C40B99/00
摘要： PROBLEM TO BE SOLVED: To provide a fatty acid derivative which is a constituent element of a depsipeptide containing aurilide analogues isolated from Dolabella auricularia of the family Aplysiidae, attracting attention to potent cytotoxicity and expected to express a physiological activity and can be utilized for synthesizing the depsipeptide.
SOLUTION: This new fatty acid derivative is represented by the following general formula [wherein, AA is an amino acid residue; R
1 is hydrogen or 2-oxo-2-phenylethyl group; R
2 is hydrogen or methylthiomethyl group; and R
3 is hydrogen, (9H-fluoren-9-ylmethoxy)carbonyl group or tert-butoxycarbonyl group].
COPYRIGHT: (C)2003,JPO
摘要翻译：要解决的问题：为了提供一种脂肪酸衍生物，其是包含从Aplysiidae的耳朵中分离出的含有尿苷类似物的depsipeptide的构成元件，引起注意有效的细胞毒性并预期表达生理活性并且可以用于合成 depsipeptide。解决方案：该新型脂肪酸衍生物由以下通式表示[其中，AA为氨基酸残基; R 1是氢或2-氧代-2-苯基乙基; R 2是氢或甲硫基甲基; 和R 3为氢，（9H-芴-9-基甲氧基）羰基或叔丁氧基羰基]。

10. 发明专利

JP2012017318A Liquid crystal and skin external preparation containing the same 审中-公开
标题翻译：液晶和皮肤外用制剂
公开(公告)号：JP2012017318A
公开(公告)日：2012-01-26
申请号：JP2011120120
申请日：2011-05-30
申请人： Chemgenesis Inc , Cosmos Technical Center:Kk , Cytopathfinder Inc , Nikko Chemical Co Ltd , Nippon Surfactant Kogyo Kk , 日光ケミカルズ株式会社 , 日本サーファクタント工業株式会社 , 株式会社ケムジェネシス , 株式会社コスモステクニカルセンター , 株式会社サイトパスファインダー
发明人： IKEDA YUTAKA , YAMASHITA HAYATO , TSUCHIGURO ICHIRO , IMUTA SATOSHI , HIROKI YASUHIRO , TAKAHASHI TAKASHI
IPC分类号： A61K47/10 , A61K8/03 , A61K8/04 , A61K8/06 , A61K8/34 , A61K8/60 , A61K8/67 , A61K8/92 , A61K9/10 , A61K9/107 , A61K47/22 , A61K47/26 , A61K47/44 , A61P17/00 , A61P17/16 , A61Q19/00
摘要： PROBLEM TO BE SOLVED: To provide a skin external preparation which induces volatilization of a moisture content or a volatile oily ingredient and transition of the preparation into a liquid crystal after applied to skin, and thereby, develops an excellent moisture retaining effect specific to the liquid crystal, an emollient effect and a percutaneous penetration promoting effect on a compounded physiologically active ingredient.SOLUTION: A liquid crystal containing as essential components an amphiphlic compound expressed by general formula (1) and water forms a liquid crystal with excellent temperature stability. The external preparation containing the liquid crystal exhibits, after applied to skin, a reduced sticky touch or oily touch, and transitions into a liquid crystal structure by volatilization of the moisture content or the volatile oily ingredient, and develops a skin care effect and a percutaneous penetration promoting effect on a physiologically active ingredient included in the preparation. In formula (1), X and Y each represents a hydrogen atom or are integrated to represent an oxygen atom; n is an integer of 0 to 2; m is an integer of 1 or 2; and R represents a hydrophilic group such as a glycerol or sugar polyol compound from which one hydroxy group is removed.
摘要翻译：要解决的问题：提供皮肤外用制剂，其在施用于皮肤之后诱发水分含量挥发或挥发性油性成分和制剂转变成液晶，从而产生特别的保湿效果对于液晶，对配合的生理活性成分的润肤效果和经皮渗透促进作用。解决方案：以通式（1）表示的两相化合物和水为主要成分的液晶形成具有优异的温度稳定性的液晶。含有液晶的外用制剂在施用于皮肤后表现出减少的粘性触感或油性触感，并且通过水分含量挥发或挥发性油性成分的挥发而转变为液晶结构，并产生护肤效果和经皮渗透促进作用包括在制剂中的生理活性成分上。在式（1）中，X和Y各自表示氢原子或一体化以代表氧原子; n为0〜2的整数， m为1或2的整数; R表示除去一个羟基的亲水性基团，例如甘油或糖多元醇化合物。版权所有（C）2012，JPO＆INPIT

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