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31. 发明专利

JP2013006804A Method for producing benzophenone derivative 审中-公开
标题翻译：生产苯并噻吩衍生物的方法
公开(公告)号：JP2013006804A
公开(公告)日：2013-01-10
申请号：JP2011141366
申请日：2011-06-27
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： SAITO TOSHIICHI , HAGIWARA KOJI , KATSUHIRA KEN , NAKAJO IWAO
IPC分类号： C07D295/08 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a synthetic intermediate etc. of a benzophenone derivative with antitumor activity etc.SOLUTION: The method for producing a benzophenone derivative represented by formula (III) (wherein Rrepresents a lower alkyl optionally having a substituent, and Rrepresents a lower alkoxy carbonyl optionally having a substituent, Rrepresents a lower alkyl optionally having a substituent, and Rrepresents an aliphatic heterocyclic alkyl optionally having a substituent) or a salt thereof is disclosed.
摘要翻译：要解决的问题：提供具有抗肿瘤活性的二苯甲酮衍生物的合成中间体等的制造方法。解决方案：由式（III）表示的二苯甲酮衍生物的制备方法（其中R < SP POS =“POST”> 1 表示任选具有取代基的低级烷基，R 3 表示任选具有取代基的低级烷基，R 4表示任选具有取代基的脂族杂环烷基或其盐。版权所有（C）2013，JPO＆INPIT

32. 发明专利

JP2012184267A Solid pharmaceutical preparation with improved stability and method for producing the same 审中-公开
标题翻译：具有改进的稳定性的固体药物制备及其生产方法
公开(公告)号：JP2012184267A
公开(公告)日：2012-09-27
申请号：JP2012149388
申请日：2012-07-03
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： NANABE SHOZO , ISHIKAWA YASUHIRO , KATO YASUKI
IPC分类号： A61K31/335 , A61K9/14 , A61K9/16 , A61K9/28 , A61K47/02 , A61K47/26 , A61K47/36 , A61K47/38 , A61P29/00 , A61P37/08
CPC分类号： A61K9/5078 , A61K9/1676
摘要： PROBLEM TO BE SOLVED: To provide a solid pharmaceutical preparation with excellent preservation stability such as light stability, and to provide a method, etc., for producing the same.SOLUTION: There is provided the solid pharmaceutical preparation including a raw pharmaceutical preparation comprising a core part containing an active ingredient and a core-coating layer containing dusting powder coating the core part; and a film containing a compound assuming photocatalyst activity or a property of a semiconductor coating the raw pharmaceutical preparation. Furthermore, there is provided a method for producing the solid pharmaceutical preparation including a step of coating the core part containing the active ingredient with constituent components of the core-coating layer containing the dusting powder by a powder-coating method.
摘要翻译：要解决的问题：提供具有优异的保存稳定性如光稳定性的固体药物制剂，并提供其制备方法等。解决方案：提供固体药物制剂，包括含有含有活性成分的核心部分的原料药物制剂和含有涂覆核心部分的除尘粉末的芯涂层; 以及含有假定光催化活性的化合物或半导体涂覆该原料药制剂的性质的膜。此外，提供了一种固体药物制剂的制造方法，其包括通过粉末涂布法将含有活性成分的核心部分与含有除尘粉末的芯涂层的构成成分进行涂布的工序。版权所有（C）2012，JPO＆INPIT

33. 发明专利

JP2012087131A Antibody composition 有权
标题翻译：抗体组合物
公开(公告)号：JP2012087131A
公开(公告)日：2012-05-10
申请号：JP2011253200
申请日：2011-11-18
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： KANDA YUTAKA , SATO MITSUO , NAKAMURA KAZUYASU , UCHIDA KAZUHISA , SHINKAWA TOYOHIDE , YAMANE NAOKO , HOSAKA EMI , YAMANO KAZUYA , YAMAZAKI MOTOO , HANAI NOBUO
IPC分类号： C07K16/00 , A61K39/395 , A61P35/00 , C07K16/06 , C07K16/18 , C07K16/28 , C07K16/32 , C12N5/10 , C12N9/04 , C12N9/10 , C12N9/12 , C12N9/88 , C12N9/90 , C12P21/00 , C12P21/08 , G01N33/531 , G01N33/574
CPC分类号： C07K16/3084 , A61K2039/505 , C07K16/00 , C07K16/065 , C07K16/18 , C07K16/2866 , C07K16/32 , C07K2317/24 , C07K2317/41 , C07K2317/732 , C07K2319/30 , C12N9/0006 , C12N9/1051 , C12N9/1241 , C12N9/90 , C12P21/005
摘要： PROBLEM TO BE SOLVED: To provide a host cell which produces an antibody composition and can control a sugar chain structure bound to an antibody molecule, a cell which can produce an antibody composition having high ADCC activity, a production method of an antibody composition using the cell, and the antibody composition produced by the production method.SOLUTION: The antibody composition contains an antibody to which complex N-glycoside-linked sugar chains are bound and which recognizes GM2, wherein all antibodies have complex N-glycoside-linked sugar chains in which fucose is not bound to N-acetylglucosamine in the reducing end.
摘要翻译：待解决的问题：提供产生抗体组合物并能够控制与抗体分子结合的糖链结构的宿主细胞，能够产生具有高ADCC活性的抗体组合物的细胞，抗体的制备方法使用细胞的组合物，以及通过制造方法制备的抗体组合物。解决方案：抗体组合物含有与复合N-糖苷连接的糖链结合并识别GM2的抗体，其中所有抗体具有复合N-糖苷连接的糖链，其中岩藻糖不与N-乙酰葡糖胺结合在减量端。版权所有（C）2012，JPO＆INPIT

34. 发明专利

JP2012085655A Method for producing animal cell for producing antibody composition 有权
标题翻译：生产抗体组合物的动物细胞生产方法
公开(公告)号：JP2012085655A
公开(公告)日：2012-05-10
申请号：JP2012005621
申请日：2012-01-13
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： KANDA YUTAKA , SATO MITSUO , NAKAMURA KAZUYASU , UCHIDA KAZUHISA , SHINKAWA TOYOHIDE , YAMANE NAOKO , HOSAKA EMI , YAMANO KAZUYA , YAMAZAKI MOTOO , HANAI NOBUO
IPC分类号： C12N5/07 , A61K39/395 , C07K16/00 , C07K16/06 , C07K16/18 , C07K16/28 , C07K16/32 , C12N5/10 , C12N9/04 , C12N9/10 , C12N9/12 , C12N9/88 , C12N9/90 , C12N15/09 , C12P21/00 , C12P21/08
CPC分类号： C07K16/3084 , A61K2039/505 , C07K16/00 , C07K16/065 , C07K16/18 , C07K16/2866 , C07K16/32 , C07K2317/24 , C07K2317/41 , C07K2317/732 , C07K2319/30 , C12N9/0006 , C12N9/1051 , C12N9/1241 , C12N9/90 , C12P21/005
摘要： PROBLEM TO BE SOLVED: To provide a method for producing animal cells for producing antibody compositions.SOLUTION: There is disclosed a method for producing animal cells for producing antibody compositions wherein antibodies bound to N-glycoside linkage complex sugar chain are contained and all the antibodies have N-glycoside linkage complex sugar chains which are free from fucose bound to N-acetylglucosamine at the reducing end. The method comprises either a process of inducing a mutation in a gene encoding an enzyme relating to synthesis of intracellular sugar nucleotide GDP-fucose in the animal cells or an enzyme relating to sugar chain modification wherein the 1-position of fucose binds to the 6-position of N-acetylglucosamine at the sugar chain reducing end of N-glycoside linkage through α-bond or a process of deleting the gene, and a process of introducing a gene encoding an antibody molecule.
摘要翻译：待解决的问题：提供生产抗体组合物的动物细胞的制备方法。解决方案：公开了一种生产用于产生抗体组合物的动物细胞的方法，其中包含与N-糖苷键合复合物糖链结合的抗体，并且所有抗体均具有N-糖苷键复合物糖链，其不含岩藻糖结合还原末端的N-乙酰氨基葡萄糖。该方法包括在编码与动物细胞中细胞内糖核苷酸GDP-岩藻糖合成相关的酶的基因中诱导突变的过程或与糖链修饰相关的酶，其中岩藻糖的1-位与6- 通过α-键的N-糖苷键的糖链还原末端的N-乙酰葡糖胺的位置或缺失该基因的方法，以及引入编码抗体分子的基因的方法。版权所有（C）2012，JPO＆INPIT

35. 发明专利

JP2012075441A Method for promoting adcc activity of antibody composition 有权
标题翻译：用于促进抗体组成的ADCC活性的方法
公开(公告)号：JP2012075441A
公开(公告)日：2012-04-19
申请号：JP2012005620
申请日：2012-01-13
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： KANDA YUTAKA , SATO MITSUO , NAKAMURA KAZUYASU , UCHIDA KAZUHISA , SHINKAWA TOYOHIDE , YAMANE NAOKO , HOSAKA EMI , YAMANO KAZUYA , YAMAZAKI MOTOO , HANAI NOBUO
IPC分类号： C12P21/08 , A61K39/395 , C07K16/00 , C07K16/06 , C07K16/18 , C07K16/28 , C07K16/32 , C12N5/10 , C12N9/04 , C12N9/10 , C12N9/12 , C12N9/88 , C12N9/90 , C12N15/09 , C12P21/00
CPC分类号： C07K16/3084 , A61K2039/505 , C07K16/00 , C07K16/065 , C07K16/18 , C07K16/2866 , C07K16/32 , C07K2317/24 , C07K2317/41 , C07K2317/732 , C07K2319/30 , C12N9/0006 , C12N9/1051 , C12N9/1241 , C12N9/90 , C12P21/005
摘要： PROBLEM TO BE SOLVED: To provide a method for promoting ADCC activity of an antibody composition.SOLUTION: There is provided the method for promoting ADCC activity of an antibody composition such as a fused protein having the Fc region of an antibody having high antibody-dependent cellular cytotoxic activity useful for various diseases.
摘要翻译：待解决的问题：提供一种促进抗体组合物的ADCC活性的方法。解决方案：提供了用于促进抗体组合物的ADCC活性的方法，所述抗体组合物如具有抗体依赖性细胞毒活性的抗体的Fc区的融合蛋白可用于各种疾病。版权所有（C）2012，JPO＆INPIT

36. 发明专利

JP2012075408A Physiologically active peptide and application thereof 审中-公开
标题翻译：生理活性肽及其应用
公开(公告)号：JP2012075408A
公开(公告)日：2012-04-19
申请号：JP2010225276
申请日：2010-10-04
申请人： Kyowa Hakko Kirin Co Ltd , National Cerebral & Cardiovascular Center , 協和発酵キリン株式会社 , 独立行政法人国立循環器病研究センター
发明人： YAMAZAKI MOTOO , TAKAHASHI NORIYUKI , MINAMINO NAOTO , SASAKI KAZUKI
IPC分类号： C12N15/09 , A61K38/00 , A61P1/14 , A61P3/00 , A61P3/14 , A61P25/00 , A61P25/20 , A61P43/00 , C07K14/47 , C07K16/18 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12P21/02 , C12Q1/02 , G01N33/15 , G01N33/50
摘要： PROBLEM TO BE SOLVED: To provide a new peptide which has energy metabolism modulating activity or circulation modulating activity.SOLUTION: There are provided a peptide composed of specific amino acid sequence or pharmacologically permissible salt thereof, and energy metabolism regulator or circulation regulator which contains the peptides and the salts as active ingredients. Also a method for screening substances which promote or inhibit activity of the peptide or agonist or antagonist to a receptor of the peptide utilizing the peptide or salts thereof is provided.
摘要翻译：待解决的问题：提供具有能量代谢调节活性或循环调节活性的新肽。提供由特定氨基酸序列或其药理学上允许的盐组成的肽，以及含有肽和盐作为活性成分的能量代谢调节剂或循环调节剂。还提供了利用肽或其盐筛选促进或抑制肽或激动剂或拮抗剂对肽受体的活性的物质的方法。版权所有（C）2012，JPO＆INPIT

37. 发明专利

JP2012072181A Composition for inhibiting expression of target gene 审中-公开
标题翻译：用于抑制目标基因表达的组合物
公开(公告)号：JP2012072181A
公开(公告)日：2012-04-12
申请号：JP2011278409
申请日：2011-12-20
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： YAMAUCHI MASAHIRO , TOTTORI TSUNEAKI , ISHIHARA ATSUSHI , YAGI NOBUHIRO , KATO YASUKI
IPC分类号： A61K48/00 , A61K9/127 , A61K31/7105 , A61K31/713 , A61K47/18 , A61K47/24 , A61K47/34 , A61P9/00 , A61P9/10 , A61P29/00 , A61P35/00
CPC分类号： C12N15/1135 , A61K9/127 , A61K31/7105 , C12N2310/14
摘要： PROBLEM TO BE SOLVED: To provide a composition, or the like, for inhibiting the expression of a target gene.SOLUTION: The composition, or the like, comprises an RNA-enclosing liposome composed of a composite particle, the composite particle composed of as constituent components a lead particle and RNA containing a sequence of continuous 15 to 30 bases of mRNA of target gene and a sequence complementary to the sequence, and a lipid membrane covering the composite particle, which liposome is filled with a liquid containing a polar organic solvent in which constituents of the lipid membrane are soluble wherein the polar organic solvent is contained in such a concentration that the lipid membrane constituents are dispersible and that also the composite particle is dispersible.
摘要翻译：待解决的问题：提供抑制靶基因表达的组合物等。组合物等包含由复合颗粒构成的包封RNA的脂质体，复合颗粒由作为构成成分的铅颗粒组成，含有目标mRNA连续15〜30个碱基序列的RNA 基因和与该序列互补的序列，以及覆盖复合粒子的脂质膜，该脂质体填充有含有极性有机溶剂的液体，其中脂质膜的成分可溶，其中极性有机溶剂的浓度为脂质膜组分是可分散的，并且复合颗粒也是可分散的。版权所有（C）2012，JPO＆INPIT

38. 发明专利

JP2010260851A SOLID PREPARATION CONTAINING DIBENZ[b, e]OXEPINE DERIVATIVE 有权
标题翻译：含有二苯并[b，e]氧化衍生物的固体制剂
公开(公告)号：JP2010260851A
公开(公告)日：2010-11-18
申请号：JP2010084827
申请日：2010-04-01
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： SUGISHITA JUN , OUCHI KAZUE , ISHIKAWA YASUHIRO
IPC分类号： A61K47/02 , A61K9/16 , A61K9/20 , A61K31/335 , A61K47/10 , A61K47/26 , A61K47/36 , A61K47/38 , A61P11/06 , A61P29/00 , A61P37/08
CPC分类号： A61K31/335 , A61K9/1611 , A61K9/1652
摘要： PROBLEM TO BE SOLVED: To provide a solid preparation which contains a specific dibenz[b, e]oxepine derivative (compound (I)) or a pharmaceutically acceptable salt thereof, and has excellent storage stability such as light stability.
SOLUTION: The solid preparation includes drug-containing granules that contain (i) the specific dibenz[b, e]oxepine derivative (compound (I)) or a pharmaceutically acceptable salt thereof, (ii) iron oxide and (iii) one or more substances selected from among sugars, starches, starch derivatives, celluloses, cellulose derivatives and sugar alcohols. In the drug-containing granules, the components (i)-(iii) are blended with one another.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供含有特定的二苯并[b，e]氧杂七环衍生物（化合物（I））或其药学上可接受的盐的固体制剂，并且具有优异的储存稳定性如光稳定性。固体制剂包括含有（i）特定二苯并[b，e]氧杂七环衍生物（化合物（I））或其药学上可接受的盐，（ii）氧化铁和（iii）一种或多种选自糖，淀粉，淀粉衍生物，纤维素，纤维素衍生物和糖醇的物质。在含药颗粒中，组分（i） - （iii）彼此混合。版权所有（C）2011，JPO＆INPIT

39. 发明专利

JP2010241718A Stable aqueous solution preparation of antibody 审中-公开
标题翻译：稳定的水溶液制备抗体
公开(公告)号：JP2010241718A
公开(公告)日：2010-10-28
申请号：JP2009091598
申请日：2009-04-03
申请人： Kyowa Hakko Kirin Co Ltd , 協和発酵キリン株式会社
发明人： ISHIKAWA TOMOYOSHI , NAKAGAWA KAORUKO , OSAWA CHIE
IPC分类号： A61K39/395 , A61K9/08 , A61K47/10 , A61K47/20 , A61K47/26 , A61K47/34
摘要： PROBLEM TO BE SOLVED: To provide an aqueous solution preparation comprising an antibody and having a pH of 6.00-7.00, particularly an aqueous solution preparation keeping the antibody stable even after long-term preservation.
SOLUTION: The aqueous solution preparation comprises a buffering agent, a surfactant, an antioxidant, an isotonic agent and an antibody and has a pH of 6.00-7.00. The surfactant is preferably a polysorbate, more preferably polysorbate 80. The antioxidant is preferably methionine. The isotonic agent is preferably sugar or sorbitol. The concentration of the buffering agent is preferably 10-20 mM. The surfactant is preferably polysorbate 80 in a concentration of 0.5-1.0 mg/mL. The concentration of methionine as the antioxidant is preferably 10-15 mM.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供包含抗体并具有6.00-7.00的pH的水溶液制剂，特别是即使在长期保存后仍保持抗体稳定的水溶液制剂。水溶液制剂包含缓冲剂，表面活性剂，抗氧化剂，等渗剂和抗体，pH为6.00-7.00。表面活性剂优选为聚山梨酯，更优选为聚山梨醇酯80.抗氧化剂优选为甲硫氨酸。等渗剂优选为糖或山梨糖醇。缓冲剂的浓度优选为10〜20mM。表面活性剂优选浓度为0.5-1.0mg / mL的聚山梨醇酯80。作为抗氧化剂的甲硫氨酸的浓度优选为10〜15mM。版权所有（C）2011，JPO＆INPIT

40. 发明专利

JP2010229136A Chemokine receptor antagonist and method of use thereof 审中-公开
标题翻译：化合物受体拮抗剂及其使用方法
公开(公告)号：JP2010229136A
公开(公告)日：2010-10-14
申请号：JP2010106678
申请日：2010-05-06
申请人： Kyowa Hakko Kirin Co Ltd , Millennium Pharmaceuticals Inc , ミレニアム・ファーマシューティカルズ・インコーポレイテッドMillennium Pharmaceuticals, Inc. , 協和発酵キリン株式会社
发明人： LULY JAY R , NAKASATO YOSHISUKE , OSHIMA ETSUO , HARRIMAN GERALDINE C B , CARSON KENNETH G , GHOSH SHOMIR , ELDER AMY M , MATTIA KAREN M
IPC分类号： C07D211/52 , C07D491/044 , A61K20060101 , A61K31/4353 , A61K31/438 , A61K31/4427 , A61K31/451 , A61K31/4523 , A61K31/4525 , A61K31/4535 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/527 , A61K31/537 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P20060101 , A61P1/00 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/06 , A61P13/12 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/18 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D221/00 , C07D223/00 , C07D223/20 , C07D313/00 , C07D313/12 , C07D337/00 , C07D337/12 , C07D401/06 , C07D401/14 , C07D405/00 , C07D405/06 , C07D409/06 , C07D451/00 , C07D471/04 , C07D491/00 , C07D491/04 , C07D493/04 , C07D495/04 , C07D497/04 , C07D513/04 , C07D519/00
CPC分类号： C07D491/04 , C07D211/46
摘要： PROBLEM TO BE SOLVED: To provide a modulator of a chemokine receptor mechanism. SOLUTION: The compound is expressed by formula (1), provided that, Z is expressed by formula (2). COPYRIGHT: (C)2011,JPO&INPIT

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