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21. 发明授权

EP2510948B1 T CELL ACTIVATION INHIBITOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND SCREENING METHOD FOR T CELL ACTIVATION INHIBITING SUBSTANCE 有权
标题翻译： T细胞活化抑制剂，T细胞活化炎性物质药物组合物适当的筛选方法
公开(公告)号：EP2510948B1
公开(公告)日：2015-09-09
申请号：EP10835979.5
申请日：2010-12-08
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： YAMASHITA, Toshihide , KUBO, Takekazu
IPC分类号： A61K45/00 , A61K31/7088 , A61K39/395 , A61P37/06 , A61P43/00 , A61K31/07 , A61K31/122 , A61K31/355 , A61K31/375 , A61K33/00 , A61K33/04 , A61K33/06 , A61K33/26 , C07K16/18 , C07K16/28 , A61K33/30
CPC分类号： C07K16/22 , A61K31/07 , A61K31/122 , A61K31/355 , A61K31/375 , A61K33/00 , A61K33/04 , A61K33/06 , A61K33/26 , A61K33/30 , A61K2039/505 , C07K16/18 , C07K16/28 , C07K2317/76 , C12N15/1136 , C12N2310/14 , C12N2320/30 , A61K2300/00
摘要： Provided is a T cell activation inhibitor containing an RGM inhibiting substance such as an anti-RGM neutralizing antibody and the like as an active ingredient. The T cell activation inhibitor is useful as a pharmaceutical composition for the prophylaxis or treatment of autoimmune diseases such as multiple sclerosis and the like, and other diseases caused by T cell activation. In addition, a T cell activation inhibiting substance can be screened for by contacting a test substance with RGM and selecting a test substance that lowers the activity level of RGM.

22. 发明公开

EP2896613A1 SULFONAMIDE COMPOUND 有权转让
标题翻译： SULFONAMIDVERBINDUNG
公开(公告)号：EP2896613A1
公开(公告)日：2015-07-22
申请号：EP13837919.3
申请日：2013-09-13
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： KATO, Taku , SAKAMOTO, Toshiaki , KUBO, Akira , SAWAMOTO, Daisuke
IPC分类号： C07D217/22 , A61K31/472 , A61K31/4725 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/00 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
CPC分类号： C07D217/22 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
摘要： The present invention provides novel sulfonamide compounds having TRPM8 antagonistic activity which are useful as medicaments. Specifically, the present invention provides a sulfonamide compound of the formula (I):

wherein Ring A is the following formula (i), (ii), or (ix):

R 4 is optionally substituted alkyl,
X 1 and X 2 are each independently tetrazolyl, tetrazolinonyl, optionally substituted triazolyl, triazolinonyl, oxadiazolonyl, optionally substituted alkanoylaminomethyl, or optionally substituted alkylsulfonylaminomethyl, or
R 4 and X 2 combine with each other at their terminals together with the adjacent benzene to form indazolinonyl or benzoisoxazolonyl, and
the other symbols are the same as described in the specification,
or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了可用作药物的具有TRPM8拮抗活性的新型磺酰胺化合物。具体而言，本发明提供式（I）的磺酰胺化合物：其中环A为下式（ⅰ），（ⅱ）或ix）：R 4为任选取代的烷基，X 1和X 2为独立的四唑基，四唑啉酮基，任选取代的三唑基，三唑啉酮基，恶二唑啉酮，任选取代的烷酰基氨基甲基或任选取代的烷基磺酰基氨基甲基，或R 4和X 2在其末端与相邻的苯相互结合形成吲唑啉酮基或苯并异恶唑啉，与说明书中描述的相同或其药学上可接受的盐。

23. 发明公开

EP2883870A1 METHOD FOR PRODUCING 1,4-BENZOXAZINE COMPOUND 有权转让
标题翻译： VERFAHREN ZUR HERSTELLUNG EINER 1,4-BENZOXAZIN-VERBINDUNG
公开(公告)号：EP2883870A1
公开(公告)日：2015-06-17
申请号：EP13828067.2
申请日：2013-08-08
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： OKABE, Tomoyuki , HAMADA, Takeshi , TOMIKAWA, Kaori , OKAMOTO, Yukie , IIJIMA, Toru , AKATSUKA, Hidenori , TOYAMA, Kenichi , MORODA, Atsushi , SUGIURA, Yoshihiro
IPC分类号： C07D265/36 , A61K31/538 , A61P5/40 , A61P5/42 , A61P9/00 , A61P9/12 , A61P13/12 , A61P43/00 , C07B61/00
CPC分类号： C07D265/36 , C07B2200/13
摘要： The present invention provides an industrially advantageous method for producing a 1,4-benzoxazine compound useful as a medicine while avoiding safety and health risks. Specifically, the present invention provides a method for producing a 1,4-benzoxazine compound [A], which comprises the three steps in the following scheme, namely, a step of converting the amino group at 7-position in a compound [a] into a dimesylamino group, a step of coupling a compound [b] with a boronic acid compound, and a step of converting the 7-position in a compound [c] into a monomesylamino group.

In the above scheme, Ms is a methanesulfonyl group, and each of R' and R" is a hydrogen atom etc.
摘要翻译：本发明提供了一种工业上有利的方法，用于生产用作药物的1,4-苯并恶嗪化合物，同时避免了安全和健康的风险。具体地说，本发明提供了1,4-苯并恶嗪化合物[A]的制造方法，其包括以下方案中的三个步骤，即将化合物[a]中的7-位的氨基转化的步骤，将化合物[b]与硼酸化合物偶联的步骤和将化合物[c]中的7-位转化为单甲硅烷基氨基的步骤。在上述方案中，Ms是甲磺酰基，R'和R“各自为氢原子等。

24. 发明公开

EP2808013A1 Orally rapidly disintegrating tablet and process for producing same 审中-公开
标题翻译：口腔ell ell e e e e。。。。。。。。。。
公开(公告)号：EP2808013A1
公开(公告)日：2014-12-03
申请号：EP14178298.7
申请日：2009-11-25
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： Sugimoto, Masaaki , Kitaoka, Kenichi , Saito, Yasunori , Uemura, Katsuji
IPC分类号： A61K9/20 , A61K31/138 , A61K31/4166 , A61K31/444 , A61K31/513 , A61K31/519 , A61K47/10 , A61K47/32 , A61K47/38 , A61K9/00
CPC分类号： A61K31/138 , A61K9/0056 , A61K9/2027 , A61K9/2054 , A61K31/4166 , A61K31/444 , A61K31/513 , A61K31/519
摘要： Disclosed is an orally rapidly disintegrating tablet characterized in that the tablet can be produced in a conventional tablet manufacturing facility and has a satisfactory level of hardness for practical applications, and the change in properties of the tablet (i.e., decreased in hardness of the tablet, and delay of the disintegration time of the tablet in the oral cavity) are rarely caused by factors such as humidity. The orally rapidly disintegrating tablet has hardness of 40N or more, can be disintegrated in the oral cavity within 60 seconds, and is produced by compressing of a mixture of (a) an active ingredient, (b) an excipient having good water wettability, (c) a water-insoluble polymer that is well compactible and does not substantially cause a decrease in the water wettability of the excipient and (d) a disintegrating agent.
摘要翻译：公开了一种口服快速崩解片剂，其特征在于片剂可以在常规的片剂制造设备中制备，并且在实际应用中具有令人满意的硬度水平，并且片剂的性能变化（即，片剂的硬度降低，并且片剂在口腔中的崩解时间的延迟）很少由湿度等因素引起。口服快速崩解片剂的硬度为40N以上，可以在60秒内在口腔内分解，通过压缩（a）活性成分，（b）具有良好的水润湿性的赋形剂（ c）非常可压缩并且基本上不引起赋形剂的水润湿性降低的水不溶性聚合物和（d）崩解剂。

25. 发明授权

EP2184282B1 NOVEL SALT OF ISOQUINOLINE COMPOUND AND CRYSTAL THEREOF 有权
标题翻译：异喹啉和晶体的新盐
公开(公告)号：EP2184282B1
公开(公告)日：2014-10-08
申请号：EP08792346.2
申请日：2008-08-08
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： FUJIO, Masakazu , TANAKA, Toshihiko , TAKAYANAGI, Hisao , SATOH, Hiroyuki , ITO, Takanori
IPC分类号： C07D403/06 , A61K31/4725 , A61P9/10 , A61P43/00
CPC分类号： C07D403/06 , C07D401/06

27. 发明公开

EP2602259A3 Salt of proline derivative, solvate thereof, and production method thereof 审中-公开
标题翻译：脯氨酸衍生物的盐，溶剂化物，以及它们的制造方法
公开(公告)号：EP2602259A3
公开(公告)日：2014-09-10
申请号：EP13157384.2
申请日：2006-02-17
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： Yoshida, Tomohiro , Sakashita, Hiroshi , Ueda, Naoko , Kirihara, Shinji , Uemori, Satoru , Tsutsumiuchi, Reiko , Akahoshi, Fumihiko
IPC分类号： C07D417/14 , A61K31/496 , A61P3/10 , A61P43/00
CPC分类号： C07D417/14
摘要： A crystal of 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl) piperazin-1-yl] pyrrolidin-2-ylcarbonyl}thiazolidine with 2.0 hydrobromic acid, 2.5 hydrobromic acid, 2 maleic acid, 2 tosyl acid, 2 besyl acid, 2 hydrochloric acid, 2.5 hydrochloric acid, 2 naphthalene-1-sulfonic acid, 2 naphthalene-2-sulfonic acid, 2 camphorsulfonic acid, fumaric acid, sulfuric acid, succinic acid, L-tartaric acid or citric acid, or a hydrate thereof.

28. 发明授权

EP2017257B1 2-AMINOBUTANOL COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES 有权转让
标题翻译： 2 AMINOBUTANOLVERBINDUNG及其用途为医疗目的
公开(公告)号：EP2017257B1
公开(公告)日：2014-08-06
申请号：EP07742585.8
申请日：2007-04-27
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： KIUCHI, Masatoshi , NAKAMURA, Mitsuharu , HAMADA, Maiko , SUGAHARA, Kunio
IPC分类号： C07C217/64 , C07C225/16 , C07C309/65 , C07C323/32 , C07C323/38 , C07C323/41 , C07D333/22 , C07D333/34 , C07F9/653 , A61K31/135 , A61K31/145 , A61K31/381 , A61K31/661 , A61P37/06 , C07F9/09
CPC分类号： C07F9/653 , C07C217/64 , C07C225/16 , C07C309/65 , C07C323/32 , C07C323/38 , C07C323/41 , C07D333/22 , C07D333/34 , C07F9/091

29. 发明公开

EP2749558A1 METHOD FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE COMPOUND 审中-公开
标题翻译：生产光学活性萘系化合物的方法
公开(公告)号：EP2749558A1
公开(公告)日：2014-07-02
申请号：EP12826351.4
申请日：2012-08-24
申请人： Mitsubishi Tanabe Pharma Corporation
发明人： MATSUYAMA, Koji , HATSUDA, Masanori , YOSHINAGA, Masahiko , YADA, Mitsuhiro , TANIMOTO, Koichi
IPC分类号： C07D401/04 , A61K31/4709 , A61P17/00 , A61P17/02 , A61P17/04 , A61P29/00 , A61P43/00 , C07B61/00
CPC分类号： C07D401/04 , C07B53/00 , C07C25/06 , C07C255/03
摘要： The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, R a and R b represent the same or different lower alkyl groups; and X 1 represents a halogen atom.)
摘要翻译：本发明提供了一种工业上有利的制备可用作皮炎等治疗剂的光学活性萘化合物的方法。具体而言，本发明提供一种光学活性萘化合物[I]的制造方法，其包括：使化合物[a-1]与化合物[b-1]在碱存在下反应的工序和由Pd化合物和叔膦配体组成的催化剂（步骤a）; 在氢供体和由钌化合物和手性配体制备的络合物存在下，或者在光学活性恶唑硼烷化合物（CBS催化剂）存在下，对化合物[c-1]进行不对称氢化的步骤，和氢化硼化合物（步骤b）; 和用还原剂处理化合物[d-1]的步骤（步骤c）。（在上式中，Ra和Rb表示相同或不同的低级烷基;并且X1表示卤素原子。）

30. 发明授权

EP2160387B1 HETEROARYLAMIDE PYRIMIDONE COMPOUNDS 有权
标题翻译：杂芳酰胺嘧啶酮化合物
公开(公告)号：EP2160387B1
公开(公告)日：2014-05-14
申请号：EP08807115.4
申请日：2008-05-14
申请人： SANOFI , Mitsubishi Tanabe Pharma Corporation
发明人： LOCHEAD, Alistair , SAADY, Mourad , VERONIQUE, Corinne , YAICHE, Philippe
IPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/513 , A61P25/00 , A61P3/00 , C07D239/36
CPC分类号： C07D403/12 , C07D239/36 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04

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