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1. 发明公开

EP3305294A1 AQUEOUS DRUG 审中-公开
标题翻译：水性药物
公开(公告)号：EP3305294A1
公开(公告)日：2018-04-11
申请号：EP16803448.6
申请日：2016-06-02
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： GOTO, Takahiro , KOZUKA, Hitoshi , SHIBATA, Mizuho
IPC分类号： A61K31/4709 , A61K9/08 , A61K47/02 , A61K47/12 , A61K47/18 , A61P31/04
CPC分类号： A61K31/4709 , A61K9/08 , A61K47/02 , A61K47/12 , A61K47/18 , A61K47/183
摘要： [Problem] To provide an aqueous drug in which the chemical decomposition of the compound represented by formula (1) or of a salt thereof is inhibited, and to provide a method for producing said aqueous drug.
[Solution] An aqueous drug provided with: a solution (liquid A) that contains the compound represented by formula (1) or a salt thereof and that has a pH of 5.3 or less; and a dilution liquid (liquid B) that is mixed with the liquid A in order to prepare a solution to be administered.
摘要翻译：本发明提供一种抑制式（1）所示的化合物或其盐的化学分解受到抑制的水性药物及其制造方法。 [水溶性药物]具备含有式（1）所示的化合物或其盐并且pH为5.3以下的溶液（液体A）和与液体A混合以制备待施用溶液的稀释液（液体B）。

2. 发明公开

EP3269369A1 RESPIRATORY INFECTION TREATING AGENT 审中-公开
标题翻译：呼吸道感染治疗剂
公开(公告)号：EP3269369A1
公开(公告)日：2018-01-17
申请号：EP16764896.3
申请日：2016-03-11
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： KUME, Kota , YOSHIDA, Hisao , ANDO, Hirotaka , TANAKA, Yuta
IPC分类号： A61K31/4709 , A61P11/00 , A61P11/04 , A61P31/04
CPC分类号： A61K31/4709 , Y02A50/473
摘要： [Problem] The present invention pertains to a safer and more effective respiratory infection treating agent.
[Solution] A respiratory infection treating agent containing, as an active ingredient, 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquin oline-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
摘要翻译： [问题]本发明涉及更安全和更有效的呼吸道感染治疗剂。 [呼吸道感染治疗剂]以7 - [（3S，4S）-3 - {（环丙基氨基）甲基} -4-氟吡咯烷-1-基] -6-氟-1-（2 （3-氟乙基）-8-甲氧基-4-氧代-1,4-二氢喹啉-3-羧酸或其药学上可接受的盐。

3. 发明公开

EP3138560A1 DRUG FOR TREATMENT OF TINNITUS PATIENTS 无效
标题翻译：药物治疗TINNITUS病人
公开(公告)号：EP3138560A1
公开(公告)日：2017-03-08
申请号：EP15786060.2
申请日：2015-04-27
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： DOI, Katsumi , HIRAHARA, Yoshifumi , NAGAI, Shinji , USHIWATA, Ai , NIWAYAMA, Ikuyo , WATANABE, Koichi , TOMINAGA, Madoka , KUROSE, Takafumi , YAMADA, Shinichi , SHINOZAKI, Takehiro , CSIKOS, Janos , GORTELMEYER, Roman
IPC分类号： A61K31/13 , A61P27/16
CPC分类号： A61K31/13
摘要： A drug for treatment of patients having tinnitus associated with age-related hearing loss, comprising neramexane or a pharmaceutically acceptable salt thereof.
摘要翻译：一种用于治疗患有与年龄相关的听力丧失相关的耳鸣的患者的药物，包含奈拉美生或其药学上可接受的盐。

4. 发明公开

EP3138559A1 DRUG FOR TREATMENT OF TINNITUS PATIENTS 无效
标题翻译： ARZNEIMITTEL ZUR BEHANDLUNG VON TINNITUS-PATITENTEN
公开(公告)号：EP3138559A1
公开(公告)日：2017-03-08
申请号：EP15785715.2
申请日：2015-04-27
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： HIRAHARA, Yoshifumi , NAGAI, Shinji , USHIWATA, Ai , NIWAYAMA, Ikuyo , WATANABE, Koichi , TOMINAGA, Madoka , KUROSE, Takafumi , YAMADA, Shinichi , SHINOZAKI, Takehiro , CSIKOS, Janos , GORTELMEYER, Roman , ELLERS-LENZ, Barbara , ALTHAUS, Michael , BANKSTAHL, Ulli
IPC分类号： A61K31/13 , A61P27/16
CPC分类号： A61K31/13 , A61K9/0053
摘要： A drug for treatment of patients having tinnitus associated with sudden hearing loss, comprising neramexane or a pharmaceutically acceptable salt thereof, wherein the morbidity period of the patient having tinnitus associated with sudden hearing loss is 48 months or longer.
摘要翻译：用于治疗与突发性听力损失相关的耳鸣的患者的药物，包括奈拉美生或其药学上可接受的盐，其中与突发性听力损失相关的耳鸣患者的发病期为48个月或更长。

5. 发明公开

EP3112359A1 7-{(3S,4S)-3-[(CYCLOPROPYLAMINO)METHYL]-4-FLUOROPYRROLIDINE-1-YL}-6-FLUORO-1-(2-FLUOROETHYL)-8-METHOXY-4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXYLIC ACID CRYSTAL 审中-公开
标题翻译： 7 - {（3S，4S）-3 - [（环丙基氨基）甲基] -4- FLUORPYRROLIDIN -1-基} -6- FLUOR-1-（2- FLUORETHYL）-8-甲氧基-4-氧代-1,4- -DIHYDROCHINOLIN -3-CARBONSÄUREKRISTALL
公开(公告)号：EP3112359A1
公开(公告)日：2017-01-04
申请号：EP16177827.9
申请日：2012-11-09
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： Araya, Ichiro , Goto, Akinori , Minagawa, Wataru , Funada, Keiko , Nagao, Muneki
IPC分类号： C07D401/04 , A61K31/4709 , A61P31/04
CPC分类号： C07D401/04 , A61K31/4709
摘要： The present application relates to a hydrochloric salt of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid.
摘要翻译：本申请涉及7 - {（3S，4S）-3 - [（环丙基氨基）甲基] -4-氟吡咯烷-1-基} -6-氟-1-（2-氟乙基）-8- 甲氧基-4-氧代-1,4-二氢喹啉-3-羧酸。

6. 发明公开

EP3110819A1 HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：。。。。。。。。
公开(公告)号：EP3110819A1
公开(公告)日：2017-01-04
申请号：EP15754887.6
申请日：2015-02-26
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： HU, Yi , LIN, C. K. Emme , LI, Bei , SIDIQUE, Shyama , ROSENBLUM, S. Jonathan , COCIORVA, M. Oana , SHREDER, R. Kevin , SETO, Shigeki
IPC分类号： C07D487/04 , A61K31/551 , A61P11/00 , A61P17/00 , A61P25/14 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , C07D491/048 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , A61K31/551 , A61K31/5513 , A61K31/554 , A61K31/7068 , A61K45/06 , C07D471/14 , C07D491/14 , C07D491/147 , C07D498/04 , C07D498/14 , C07D513/04 , C07D513/14 , C07D519/00 , A61K2300/00
摘要： Provided herein are compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of ERK5, a BET family protein or both. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of a ERK5 -mediated disease, a BET protein-mediated disease or both.
摘要翻译：本文提供式I化合物和含有该化合物的组合物。化合物和组合物可用于抑制ERK5，BET家族蛋白或两者的作用的方法。在某些实施方案中，化合物和组合物可用于预防，改善或治疗ERK5介导的疾病，BET蛋白质介导的疾病或两者。

7. 发明公开

EP3075726A1 UREA DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF 有权
标题翻译：脲衍生物或其药学上可接受的盐
公开(公告)号：EP3075726A1
公开(公告)日：2016-10-05
申请号：EP14865553.3
申请日：2014-11-27
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： TAKAHASHI, Hiroyasu , SAITO, Yoshifumi , TSUDA, Kosuke , SHIBASAKI, Mitsuhito , OHATA, Kohei
IPC分类号： C07D207/273 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/42 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/497 , A61K31/506 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P29/00 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/08 , A61P43/00
CPC分类号： C07D207/273 , C07D207/22 , C07D209/54 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect.
The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.

8. 发明公开

EP3059226A1 2-AMINO-2-[2-[4-(3-BENZYLOXYPHENYLTHIO)-2-CHLOROPHENYL]-ETHYL]-1,3-PROPANEDIOL HYDROCHLORIDE CRYSTAL 审中-公开
标题翻译： 2-氨基-2- [2- [4-（3-苄氧基苯基）-2-氯苯基] - 乙基] -1,3-丙磺酰氯化物晶体
公开(公告)号：EP3059226A1
公开(公告)日：2016-08-24
申请号：EP16157730.9
申请日：2009-03-18
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： Komatsu, Hidetaka , Satoh, Hiroya
IPC分类号： C07C319/28 , C07C323/32
CPC分类号： C07C319/28 , C07B2200/13 , C07C323/32
摘要： A crystal of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2- chlorophenyl]ethyl]-1,3-propanediol hydrochloride obtainable by a method comprising the steps of:
(1) dissolving 2-amino-2-[2-[4-(3-benzyloxyphenyylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which the compound in the form of the hydrochloride thereof is highly soluble and a solvent in which the compound in its hydrochloride is less soluble, to thus prepare a solution of 2-amino- 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then
(2) adding hydrochloric acid to said solution with stirring, to thus crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]ethyl]-1,3-propanediol, wherein the solvent in which the hydrochloride of the compound is highly soluble is selected from the group consisting of methanol, ethanol, propyl alcohol, isopropyl alcohol, butanol, t-butanol, acetonitrile and propionitrile; and wherein the solvent in which the hydrochloride of the compound is less soluble is selected from the group consisting of water, ethyl formate, ethyl acetate, propyl acetate, ethyl propionate, diethyl ether, diisopropyl ether and ethylene glycol dimethyl ether.
摘要翻译：通过包括以下步骤的方法得到的2-氨基-2- [2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基] -1,3-丙二醇盐酸盐的结晶：（1）将2-氨基 -2- [2- [4-（3-苄氧基苯硫基硫基）-2-氯苯基]乙基] -1,3-丙二醇在包含溶剂的混合溶剂中，其中盐酸盐形式的化合物是高度可溶的，其中盐酸化合物的溶解性较差的溶剂，由此制备2-氨基-2- [2- [4-（3-苄氧基苯硫基）-2-氯苯基]乙基] -1,3-丙二醇的溶液; 然后（2）在搅拌下向所述溶液中加入盐酸，从而使2-氨基-2- [2- [4-（3-苄氧基苯硫基）-2-氯 - 苯基]乙基] -1,3- 丙二醇，其中化合物的盐酸盐高度溶解的溶剂选自甲醇，乙醇，丙醇，异丙醇，丁醇，叔丁醇，乙腈和丙腈; 其中化合物的盐酸盐较少溶解的溶剂选自水，甲酸乙酯，乙酸乙酯，乙酸丙酯，丙酸乙酯，乙醚，二异丙醚和乙二醇二甲醚。

9. 发明公开

EP3050888A1 Compounds for the treatment of bacterial infections 审中-公开
标题翻译： Verbindungen zur Behandlung von bakteriellen Infektionen
公开(公告)号：EP3050888A1
公开(公告)日：2016-08-03
申请号：EP15000223.6
申请日：2015-01-27
申请人： Merck Sharp & Dohme Corp. , Intervet International B.V. , Kyorin Pharmaceutical Co., Ltd.
发明人： Fukuda, Yasumichi , Kawashima, Mikako , Takano, Hisashi , Singh, Sheo B. , Warrass, Ralf , Ullrich, Joachim
IPC分类号： C07D498/04 , A61K31/5383 , A61P31/04
CPC分类号： C07D498/04
摘要： Novel bridged compounds of formula (I) are disclosed herein, along with their pharmaceutically acceptable salts and hydrates. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
摘要翻译：本文公开了式（I）的新型桥连化合物及其药学上可接受的盐和水合物。还公开了包含这些化合物的组合物，制备这些化合物的方法和使用这些化合物作为抗菌剂的方法。所公开的化合物，其药学上可接受的盐，水合物和前药，以及包含这些化合物，盐，水合物和前药的组合物可用于治疗细菌感染和相关疾病和病症。

10. 发明授权

EP1806338B1 PROCESS FOR PRODUCING 2-AMINO-2-[2-[4-(3-BENZYLOXY-PHENYLTHIO)-2-CHLOROPHENYL[ETHYL]-1,3-PROPANEDIOL HYDROCHLORIDE AND HYDRATES THEREOF. AND INTERMEDIATES THE PRODUCTION THEREOF 失效转让
标题翻译：用于生产2-氨基-2- [2- [4-（3-苄氧基苯硫基）-2-氯苯基[乙基] -1,3-丙二醇，以及它们的水合物和中间体的生产
公开(公告)号：EP1806338B1
公开(公告)日：2016-01-20
申请号：EP05790615.8
申请日：2005-10-07
申请人： Kyorin Pharmaceutical Co., Ltd.
发明人： TSUBUKI, Takeshi , KOBAYASHI, Kenichi , KOMATSU, Hidetaka
IPC分类号： C07C319/20 , C07C319/12 , C07C323/07 , C07C323/32 , C07C323/56 , A61K31/137 , A61P1/04 , A61P11/06 , A61P13/12 , A61P17/00 , A61P19/02 , A61P29/00 , A61P37/06 , A61P37/08
CPC分类号： C07C319/20 , C07C323/07 , C07C323/32 , C07C323/56

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