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1. 发明专利

JP2009095249A Antibody improved in effector function 有权
标题翻译：改善效果的抗体功能
公开(公告)号：JP2009095249A
公开(公告)日：2009-05-07
申请号：JP2007267207
申请日：2007-10-12
申请人： Igaku Seibutsugaku Kenkyusho:Kk , Otsuka Chemical Co Ltd , 大塚化学株式会社 , 株式会社医学生物学研究所
发明人： TSUJI TAKASHI , KAJIWARA YASUHIRO , TEZUKA KATSUNARI , NANBU YURI , FUKAE KAZUHIRO , ASAI HIROAKI , KITA SHOICHI , SETO MINAE , MURAKAMI AKIHIRO
IPC分类号： C12N15/09 , A61K31/7088 , A61K35/76 , A61K39/395 , A61K48/00 , A61P1/04 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/06 , C07K16/18 , C07K16/46 , C12N5/10
摘要： PROBLEM TO BE SOLVED: To provide an antibody improved in an effector function, a method for simply producing the antibody, a method for improving the effector function of an antibody, and a therapeutic composition which contains the antibody, has a high pharmacological activity, can reduce dosages with less side effects, and can be used for wide-ranging uses. SOLUTION: This antibody whose 295-amino acid in the EU index number of Kabat is replaced with a cysteine residue comprises (1) a mutein antibody whose amino acids at specific positions are replaced by other amino acids, and/or (2) an antibody in which the fucose molecules of sugar chains bound to the antibody are reduced. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：为了提供改善效应子功能的抗体，简单生产抗体的方法，改善抗体的效应子功能的方法和含有该抗体的治疗组合物具有高的药理学活性，可以减少副作用较少的剂量，可用于广泛用途。解决方案：在EU指数Kabat中295个氨基酸被半胱氨酸残基取代的该抗体包含（1）特定位置的氨基酸被其它氨基酸替代的突变蛋白抗体，和/或（2 ）抗体，其中与抗体结合的糖链的岩藻糖分子被还原。版权所有（C）2009，JPO＆INPIT

2. 发明专利

JP2006036649A Method for producing sialic acid derivative and sialic acid derivative 有权
标题翻译：生产酸式衍生物和酸式衍生物的方法
公开(公告)号：JP2006036649A
公开(公告)日：2006-02-09
申请号：JP2004214739
申请日：2004-07-22
申请人： Yasuhiro Kajiwara , Otsuka Chemical Co Ltd , 大塚化学株式会社 , 康宏梶原
发明人： KAJIWARA YASUHIRO , ASAI HIROAKI
IPC分类号： C07H13/00 , C07H19/10
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a sialic acid derivative which can utilize cytidine without protection, can greatly reduce the number of steps, and is more suitable for industrial production, and to obtain a novel sialic acid derivative.
SOLUTION: The method for producing the sialic acid derivative represented by formula (1) comprises reacting a compound represented by formula (2) (wherein R
2 is an acyl group, a silyl group, allyl group, benzyl group, a trityl group or an acetal group; and X
+ and Y
+ are the same or different cations) with cytidine.
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供一种可以无保护地利用胞苷的唾液酸衍生物的制备方法，可以大大减少步骤数，更适合工业化生产，得到新的唾液酸衍生物。解决方案：制备由式（1）表示的唾液酸衍生物的方法包括使由式（2）表示的化合物（其中R 2 SP 2是酰基，甲硅烷基，烯丙基基团，苄基，三苯甲基或缩醛基;并且与Cytidine相比，X + 和Y + 是相同或不同的阳离子）。版权所有（C）2006，JPO＆NCIPI

3. 发明专利

JP2005247734A Method for producing optically active amino acid derivative 有权
标题翻译：生产光学活性氨基酸衍生物的方法
公开(公告)号：JP2005247734A
公开(公告)日：2005-09-15
申请号：JP2004059147
申请日：2004-03-03
申请人： Otsuka Chemical Co Ltd , 大塚化学株式会社
发明人： TANAKA HITOSHI , NIWA MIKI , ASAI HIROAKI
IPC分类号： C07C231/12 , C07B61/00 , C07C233/47
摘要： PROBLEM TO BE SOLVED: To provide a convenient method for producing an optically active amino acid derivative suitable for industrial production.
SOLUTION: The method for producing the optically active amino acid derivative comprises reducing a compound represented by general formula (1) (wherein, R
1 and R
2 are the same or different, and each a hydrogen atom, an alkyl group, a halogen, an amino group, -NHCOR
4 , -OR
4 , or -OCOR
4 ; R
3 is an alkyl group, an amino group, -NHCOR
4 , -OR
4 , or -OCOR
4 ; R
4 is a hydrogen atom, an alkyl group or an aryl group; with the proviso that at least one of R
1 to R
3 is the -NHCOR
4 ) in the presence of a palladium-carbon catalyst with hydrogen to provide the amino acid derivative.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：提供适合于工业生产的光学活性氨基酸衍生物的方便的方法。解决方案：用于制备光学活性氨基酸衍生物的方法包括将通式（1）表示的化合物（其中，R 1和R 2分别是相同或不同，并且各自为氢原子，烷基，卤素，氨基，-NHCOR 4，或-OR SP 3，或-OCOR 4 R 3是烷基，氨基，-NHCOR 4，或-OR SP 3，或-OCOR 4 ; R 4 是氢原子，烷基或芳基;条件是R SP 1至R SP中的至少一个在具有氢气的钯 - 碳催化剂的存在下，将3> 是-NHCOR 4 ）以提供氨基酸衍生物。版权所有（C）2005，JPO＆NCIPI

4. 发明专利

JP2009155353A Method for producing sugar chain compound 审中-公开
标题翻译：生产糖链化合物的方法
公开(公告)号：JP2009155353A
公开(公告)日：2009-07-16
申请号：JP2006092702
申请日：2006-03-30
申请人： Otsuka Chemical Co Ltd , Yokohama City Univ , 公立大学法人横浜市立大学 , 大塚化学株式会社
发明人： KAJIWARA YASUHIRO , NANBU YURI , FUKAE KAZUHIRO , ASAI HIROAKI
IPC分类号： C08B37/08
CPC分类号： C07H1/00 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing an N-bonded type sugar chain compound having a free hydroxy group at its reducing terminal by using safer hydrazine hydrate as compared with that of anhydrous hydrazine. SOLUTION: This sugar chain compound of formula (2) is obtained by effecting the hydrazine hydrate on a sugar chain asparagine compound of formula (1) [wherein, R 1 to R 3 are each H or a sugar residue; R 4 is H or a fucose residue; R 5 is H, a lipid-soluble protecting group or the like; R 6 is carboxy or a group expressed by -CONHR 7 ]. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：与无水肼相比，通过使用更安全的水合肼，提供其还原性末端具有游离羟基的N-键合型糖链化合物的制造方法。解决方案：式（2）的糖链化合物是通过在式（1）的糖链天冬酰胺化合物上进行水合肼而获得的[其中，R 1 至R 3 各自为H或糖残基; R 4 是H或岩藻糖残基; R 5 是H，脂溶性保护基等; R 6是羧基或由-CONHR表示的基团]。版权所有（C）2009，JPO＆INPIT

5. 发明专利

JP2009148720A Immobilized catalyst 有权
标题翻译：固定催化剂
公开(公告)号：JP2009148720A
公开(公告)日：2009-07-09
申请号：JP2007329940
申请日：2007-12-21
申请人： Otsuka Chemical Co Ltd , 大塚化学株式会社
发明人： NISHIZAWA MUGIO , IMAGAWA HIROSHI , YAMAMOTO HIROBUMI , ASAI HIROAKI
IPC分类号： B01J31/02 , C07B61/00 , C07D209/30 , C07D311/04
CPC分类号： Y02P20/52
摘要： PROBLEM TO BE SOLVED: To provide an immobilized catalyst which allows a load on the environment to be decreased, hardly discharges an environmental loading material even when a compound is produced, and has excellent recyclability. SOLUTION: The immobilized catalyst is obtained by immobilizing a mercury triflate catalyst to a solid-phase carrier while interposing a linker between them. A method for producing the compound by using the immobilized catalyst is provided. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：为了提供允许环境负荷降低的固定化催化剂，即使制备化合物也难以排出环境负载材料，并且具有优异的可回收性。解决方案：固定化催化剂是通过将汞三氟甲磺酸酯催化剂固定在固相载体上而在它们之间插入连接体而获得的。提供了使用固定化催化剂制造化合物的方法。版权所有（C）2009，JPO＆INPIT

6. 发明专利

JP2012046511A Pharmaceutical agent containing low molecular weight polysulfated hyaluronic acid derivative 审中-公开
标题翻译：含有低分子量聚对苯二甲酸衍生物的药物代理
公开(公告)号：JP2012046511A
公开(公告)日：2012-03-08
申请号：JP2011167126
申请日：2011-07-29
申请人： Otsuka Chem Co Ltd , Otsuka Pharmaceut Co Ltd , 大塚化学株式会社 , 大塚製薬株式会社
发明人： KAKEHI KAZUAKI , ASAI HIROAKI , HAYASHI NAOHIRO , SHIMIZU SATOSHI , GOTO FUMITAKA , KOGA YASUO , TOMOYASU TAKAHIRO , TAKI TAKAO , KATO YUSUKE , NAKAZATO SATORU , TAKABA JUNJI , AZUMA ATSUSHI , HIRANO CHIKO , IZUMI KAZUNARI , KASHIMOTO NENRYU , SAKAMOTO YOKO , HAYASHI TAKASHI , NISHIDA MASARU
IPC分类号： A61K31/728 , A61K31/7016 , A61K31/702 , A61P11/02 , A61P11/06 , A61P17/04 , A61P27/14 , A61P37/08 , C07H5/06 , C07H7/033 , C07H11/00 , C08B37/00
摘要： PROBLEM TO BE SOLVED: To provide a polysulfated hyaluronic acid derivative useful for preventing and/or treating allergic diseases.SOLUTION: A low molecular weight polysulfated hyaluronic acid derivative expressed by general formula (IA) or (IB) or a pharmaceutically acceptable salt thereof is provided, wherein n represents a number of 0-15; and R each independently represents H, SOH or the like.
摘要翻译：待解决的问题：提供可用于预防和/或治疗过敏性疾病的多硫酸化透明质酸衍生物。解决方案：提供由通式（IA）或（IB）表示的低分子量多硫酸化透明质酸衍生物或其药学上可接受的盐，其中n表示0-15的数; R各自独立地表示H，SO，SB，SO 3等。版权所有（C）2012，JPO＆INPIT

7. 发明专利

JP2011168591A Low-molecular polysulfated hyaluronic acid derivative and medicine containing the same 有权
标题翻译：低分子量聚羟基丙酸衍生物及其含有药物
公开(公告)号：JP2011168591A
公开(公告)日：2011-09-01
申请号：JP2011055681
申请日：2011-03-14
申请人： Otsuka Chem Co Ltd , Otsuka Pharmaceut Co Ltd , 大塚化学株式会社 , 大塚製薬株式会社
发明人： KAKEHI KAZUAKI , ASAI HIROAKI , HAYASHI NAOHIRO , SHIMIZU SATOSHI , GOTO FUMITAKA , KOGA YASUO , TOMOYASU TAKAHIRO , TAKI TAKAO , KATO YUSUKE , NAKAZATO SATORU , TAKABA JUNJI , AZUMA ATSUSHI , HIRANO CHIKO , IZUMI KAZUNARI , KASHIMOTO NENRYU , SAKAMOTO YOKO , HAYASHI TAKASHI , NISHIDA MASARU
IPC分类号： A61K31/728 , A61P11/02 , A61P11/06 , A61P17/00 , A61P27/02 , A61P37/08 , C07H15/04 , C08B37/08
CPC分类号： A61K31/728 , C08B37/0072
摘要： PROBLEM TO BE SOLVED: To provide a low-molecular polysulfated hyaluronic acid derivative useful in the prevention and/or treatment of allergic diseases.
SOLUTION: There is provided a preventive and/or therapeutic agent for an allergic disease selected from pollinosis, allergic rhinitis, allergic conjunctivitis, atopic dermatitis, and asthma, which agent comprises either a low-molecular polysulfated hyaluronic acid derivative represented by formula (IB) or a pharmaceutically acceptable salt thereof as an active ingredient. In the formula, n is a number of 0-15, and R's represent each independently H, SO
3 H or the like.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供可用于预防和/或治疗过敏性疾病的低分子量多硫酸化透明质酸衍生物。提供了选自花粉osis病，过敏性鼻炎，过敏性结膜炎，特应性皮炎和哮喘的过敏性疾病的预防和/或治疗剂，所述药物包含式（I）表示的低分子多硫酸化透明质酸衍生物（IB）或其药学上可接受的盐作为活性成分。在该式中，n为0-15的数，R为H，SO 3 S 3 H等。版权所有（C）2011，JPO＆INPIT

8. 发明专利

JPH0853462A PRODUCTION OF AMINOMETHYLPENAM DERIVATIVE AND TRIAZOLYLMETHYLPENAM DERIVATIVE 失效
公开(公告)号：JPH0853462A
公开(公告)日：1996-02-27
申请号：JP21036394
申请日：1994-08-10
申请人： OTSUKA CHEMICAL CO LTD
发明人： ASAI HIROAKI , KAWAHARA ICHIRO , TOMOTAKI YOSHIHISA
IPC分类号： C07D499/87 , C07D499/86 , C07D499/897
摘要： PURPOSE:To obtain an aminomethylpenam derivative expressed by a specific formula, useful as a starting material for triazolylmethylpenam derivatives to be used as synthetic intermediates for antibiotics, and freed from problems concerning the reaction for obtaining the subject compound, namely, safety, low selectivity and low yield. CONSTITUTION:This compound, an aminomethylpenam derivative, is expressed by formula I (X and X are each H or a halogen; R is H or a carboxylic acid-protecting group; (n) is 0-2), e.g. 2beta-aminomethyl-2alpha-methylpenicillanic diphenylmethyl ester. It is recommended that this derivative of formula I is obtained, for example, by reaction between a compound of formula II and sodium azide to form an azide compound which is, in turn, reduced in the presence of methylene chloride, lead chloride and aluminum powder. The other objective triazolylmethylpenam derivative of formula III is obtained, preferably, by reaction between the compound of formula I and a hydrazone derivative of formula IV (e.g. 2,2'-dichloroacetaldehyde-p-toluenesulfonyl hydrazone) under neutral or basic conditions.

9. 发明专利

JPH0853425A PRODUCTION OF 1,2,3-TRIAZOLE DERIVATIVE 失效
公开(公告)号：JPH0853425A
公开(公告)日：1996-02-27
申请号：JP21036294
申请日：1994-08-10
申请人： OTSUKA CHEMICAL CO LTD
发明人： ASAI HIROAKI , KAWAHARA ICHIRO , TOMOTAKI YOSHIHISA
IPC分类号： C07D249/04 , C07D249/06
摘要： PURPOSE:To provide a method for producing a 1,2,3-triazole derivative useful as a raw material for medicines and an intermediate for printing and image treatment by a simple operation safely and in high yield. CONSTITUTION:An amine compound of the formula, R -NH2 (R is a lower alkyl which may be replaced with a halogen, phenyl, benzyl or phenylamino whose benzene ring may be replaced with a halogen, a lower alkyl or a lower alkoxy, a lower alkylamino whose alkyl may be replaced with a halogen, ammonium having formed a salt with an inorganic acid or carboxyl having formed a salt with ammonia) is reacted with a hydrazone derivative of formula I (X is a halogen; R and R are each H, a lower alkyl which may be replaced with a halogen or phenyl which may be replaced with a halogen, a lower alkyl or a lower alkoxy) under neutral or basic conditions preferably at 0-80 deg.C for 1-8 hours to give a compound of formula II.

10. 发明专利

JPH04164045A PRODUCTION OF ALPHA,ALPHA-DIHALOKETONE DERIVATIVE 失效
公开(公告)号：JPH04164045A
公开(公告)日：1992-06-09
申请号：JP29007090
申请日：1990-10-25
申请人： OTSUKA CHEMICAL CO LTD
发明人： AKATA ATSUO , ASAI HIROAKI
IPC分类号： B01J31/02 , B01J31/04 , C07B61/00 , C07C67/287 , C07C67/29 , C07C69/63
摘要： PURPOSE:To obtain the subject compound with industrial advantage by reacting 2,5-diacetoxy-3-hexyne, etc., with chlorine, etc., in the presence of a catalytic amount of a secondary amine derivative, etc., in an aqueous solution of an alkali metal bromide containing an alkali metal bicarbonate, etc. CONSTITUTION:A compound of formula I (Both of two R are methyl. Or one of them is methyl and the other is ethyl) is reacted with chlorine or sodium hypochlorite in the presence of a catalytic amount of a secondary amine derivative or in the presence of a catalytic amount of a secondary amine (e.g. 2,2,6,6- tetramethylpiperidines or di-t-butylamine) and a catalytic amount of an organic peracid (e.g. lower carboxylic acid such as performic acid or peracetic acid or aromatic carboxylic acid such as perbenzoic acid, perphthalic acid or metachloroperbenzoic acid) in an aqueous solution of an alkali metal bromide containing an alkali metal bicarbonate or an alkali metal phosphate, thus obtaining the objective compound of formula III useful as an intermediate for synthesis of compounds (perfume substance for food) of formula I in a high yield using an readily available catalyst and an economic oxidizing agent ready to handle without requirement of a special reaction apparatus.

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