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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

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。

3. 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。

4. 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。

5. 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]。

6. 发明专利

JP2004099576A Combinatorial synthesis for chain connected benzene ring compound 审中-公开
标题翻译：链连接苯并环化合物的组合合成
公开(公告)号：JP2004099576A
公开(公告)日：2004-04-02
申请号：JP2002298019
申请日：2002-09-05
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 , 高橋孝志
发明人： TAKAHASHI TAKASHI , DOI TAKAYUKI , INOUE HITOSHI
IPC分类号： C07C231/12 , C07B61/00 , C07C233/65 , C07C235/42 , C07C235/46 , C07C235/84 , C40B50/00
摘要： PROBLEM TO BE SOLVED: To provide a method of producing a chain connected benzene ring compound, particularly to provide a method for synthesizing the core section of a rod-like liquid crystalline molecule required in the fields including liquid crystal display elements.
SOLUTION: In order to solve the above-mentioned subject, the technique of the combinatorial synthesis is utilized. Benzene derivatives bearing reactive sites are supported on a solid carrier and a plurality of benzene derivatives are allowed to react simultaneously and mutually to obtain many kinds of chain-connected benzene ring compounds are obtained that can be used as a core site of rod-like liquid crystalline molecule through one time reaction.
COPYRIGHT: (C)2004,JPO
摘要翻译：要解决的问题：提供一种连接苯环化合物的制备方法，特别是提供一种用于合成包括液晶显示元件在内的领域所需的棒状液晶分子的芯部的方法。解决方案：为了解决上述课题，利用了组合合成技术。带有反应性位点的苯衍生物负载在固体载体上，并使多个苯衍生物同时并相互反应，得到可用作棒状液体的核心部位的多种连接的苯环化合物晶体分子通过一次反应。版权所有（C）2004，JPO

7. 发明专利

JP2004099575A New d-galactosamine derivative and synthetic method for mucin core 2 class by using the same 审中-公开
公开(公告)号：JP2004099575A
公开(公告)日：2004-04-02
申请号：JP2002298018
申请日：2002-09-05
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 , 高橋孝志
发明人： TAKAHASHI TAKASHI , DOI TAKAYUKI , INOUE HITOSHI
IPC分类号： C07H23/00 , C07H3/06
摘要： PROBLEM TO BE SOLVED: To develop a saccharide derivative that functions as a saccharide donor and as a saccharide receptor and to simply synthesize mucin core 2 class by using the developed derivative.
SOLUTION: A D-galactosamine derivative bearing a free hydroxy group at the 3-position is prepared by introducing an arylthio or alkylthio group to the 1-position to allow the product to have the function as a saccharide donor under mild conditions, thereby converting the hydroxy group at the 6 position to trimethylsilyloxoy group. This D-galactosamine derivative has both functions, as a saccharide donor and as a saccharide receptor. In the reaction with a fluorosaccharide, it functions as a saccharide receptor and the regioselective glycosylation reaction can be carried out by selecting an activator. The D-galactosamine functioning as a saccharide donor is obtained by reaction with an N-protected serine ester or with an N-protected threonine ester. This D-galactosamine derivative is employed, when the mucin core 2 class derivative is synthesized through this new process.
COPYRIGHT: (C)2004,JPO

8. 发明专利

JP2005187440A New linker for constituting saccharide chain 审中-公开
标题翻译：用于构成食品链的新连接器
公开(公告)号：JP2005187440A
公开(公告)日：2005-07-14
申请号：JP2003436789
申请日：2003-12-25
申请人： Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 孝志高橋
发明人： TAKAHASHI TAKASHI , TANAKA HIROSHI , MATOBA SENTOKU , ISHIDA KIYOUSUKE
IPC分类号： C07D405/12
摘要： PROBLEM TO BE SOLVED: To provide a linker that carry out the debenzylation reaction on the solid phase, followed by recovering saccharide chains, when saccharide chain library is constituted by using the solid-phase combinatorial synthetic technique.
SOLUTION: The novel linker is prepared by using monoacetyl alkane diol as a starting material, and one end thereof is a tetrahydropyranyl group; an carboxy group of the other end thereof is converted to an active ester by N-hydroxysuccinimide.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：当通过使用固相组合合成技术构成糖链文库时，提供在固相上进行脱苄基化反应的接头，然后回收糖链。解决方案：通过使用单乙酰烷烃二醇作为原料制备新的连接体，其一端为四氢吡喃基; 其另一端的羧基被N-羟基琥珀酰亚胺转化为活性酯。版权所有（C）2005，JPO＆NCIPI

9. 发明专利

JP2005187441A Method for producing n-glycosylamide 审中-公开
标题翻译：生产N-甲酰氨基酰胺的方法
公开(公告)号：JP2005187441A
公开(公告)日：2005-07-14
申请号：JP2003436790
申请日：2003-12-25
申请人： Takashi Takahashi , Tokyo Kasei Kogyo Kk , 東京化成工業株式会社 , 孝志高橋
发明人： TAKAHASHI TAKASHI , TANAKA HIROSHI , TAKAHASHI DAISUKE , IWATA YUKI
IPC分类号： C07H15/18 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for simply producing N-glycosylamide in high yield without via unstable sugar amine.
SOLUTION: In this method for producing N-glycosylamide by direct N-glycosylation of amide, an amide as an sugar acceptor is allowed to react with an imidate sugar as a sugar donor in the presence of a Lewis acid and molecular sieve. In order to obtain N-glycosylamide in good yield, trialkylsilyl triflate and a molecular sieve are used.
COPYRIGHT: (C)2005,JPO&NCIPI

10. 发明专利

JP2008266194A New organic compound useful as raw material for molecular probe 审中-公开
标题翻译：新有机化合物作为原料用于分子探针
公开(公告)号：JP2008266194A
公开(公告)日：2008-11-06
申请号：JP2007110626
申请日：2007-04-19
申请人： Yoshiisa Ando , Nihon Medi Physics Co Ltd , Takashi Takahashi , Hiroshi Tanaka , 吉勇安藤 , 日本メジフィジックス株式会社 , 浩士田中 , 孝志高橋
发明人： TANAKA HIROSHI , TAKAHASHI TAKASHI , ANDO YOSHIISA , KANEZASHI NOBUHIKO
IPC分类号： C07C271/16
CPC分类号： Y02P20/55
摘要： PROBLEM TO BE SOLVED: To obtain a new organic compound useful as a raw material for a molecular probe containing an affinity group and a detective group in the molecule. SOLUTION: The compound represented by formula (wherein n is an integer of 1-5; R 1 is a protective group stable in either a basic environment or an acidic environment in the presence of a palladium catalyst; R 2 , R 3 and R 4 are each a protective group selected from the group consisting of a 9-fluorenylmethyl group, an allyl group and a tert-butyl group; and R 2 , R 3 and R 4 are each selected from mutually different protective groups) is used. Since in the compound, each protective group is deprotected under different conditions, an affinity group or a detective group is selectively introduced into an arbitrary part in the molecule and the polymerization degree of a molecular probe is arbitrarily adjusted. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：获得可用作分子中含有亲和基团和检测基团的分子探针的原料的新的有机化合物。解决方案：由式（其中n是1-5的整数; R 1 ）表示的化合物是在碱存在下在碱性环境或酸性环境中稳定的保护基催化剂; R 2 SP 3，R SP 3，R SP 3，R SP 4，各自为保护基，选自9-芴基甲基，烯丙基基团和叔丁基;并且使用R 2 SP 2，R 3 SP 3和R SP 4各自选自相互不同的保护基）。由于在该化合物中，各保护基在不同的条件下脱保护，所以在分子的任意部分选择性地引入亲和基团或检测基团，并且任意调整分子探针的聚合度。版权所有（C）2009，JPO＆INPIT

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