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1. 发明公开

EP3546463A1 SULFONAMIDE DERIVATIVE HAVING COUMARIN SKELETON 有权
公开(公告)号：EP3546463A1
公开(公告)日：2019-10-02
申请号：EP17874264.9
申请日：2017-11-22
申请人： Daiichi Sankyo Co., Ltd.
发明人： OTA, Masahiro , INOUE, Hidekazu , KAWAI, Junya , OHKI, Hitoshi , TOKI, Tadashi
IPC分类号： C07D491/052 , A61K31/496 , A61P35/00 , A61P43/00
摘要： Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2.
[Solution]
Provided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents:

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are the same as defined in the specification,
and a salt thereof.

2. 发明授权

EP3130608B1 (ANTI-HER2 ANTIBODY)-DRUG CONJUGATE 有权
公开(公告)号：EP3130608B1
公开(公告)日：2019-09-04
申请号：EP15776810.2
申请日：2015-04-06
申请人： Daiichi Sankyo Co., Ltd.
发明人： NAITO, Hiroyuki , MASUDA, Takeshi , NAKADA, Takashi , YOSHIDA, Masao , ASHIDA, Shinji , MIYAZAKI, Hideki , KASUYA, Yuji , MORITA, Koji , OGITANI, Yusuke , ABE, Yuki
IPC分类号： C07K16/32 , A61K31/4745 , A61K39/395 , A61P35/00 , C07K5/072 , C07K5/083 , C07K5/103 , C07K7/06

3. 发明公开

EP3272346A4 SOLID PREPARATION CONTAINING COLORANT 审中-公开
公开(公告)号：EP3272346A4
公开(公告)日：2018-08-01
申请号：EP16765093
申请日：2016-03-17
申请人： DAIICHI SANKYO CO LTD
发明人： TAJIRI SHINICHIRO , YOSHINAGA SHINJI , OZAKI YURIKA
IPC分类号： A61K31/195 , A61K9/20 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/22 , A61K47/24 , A61K47/26 , A61K47/36 , A61K47/38 , A61K47/40 , A61P25/00 , A61P25/04 , A61P29/00
CPC分类号： A61K9/28 , A61K31/195 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/36 , A61K47/38
摘要： An object of the present invention is to provide [(1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate as a stabilized pharmaceutical solid preparation, and also to provide a method for preparing the stabilized pharmaceutical solid preparation. The object can be attained by a pharmaceutical solid preparation comprising [(1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl]acetic acid monobenzenesulfonate which is compound represented by the following formula (I) in combination with (i) one or two or more components selected from the group consisting of D-mannitol, lactose, corn starch, and crystalline cellulose, (ii) carmellose calcium, and (iii) colorants.

4. 发明公开

EP3323808A1 NOVEL METHOD FOR PRODUCING 1-(ACYLOXY)ALKYL CARBAMATE DERIVATIVE 审中-公开
公开(公告)号：EP3323808A1
公开(公告)日：2018-05-23
申请号：EP16814478.0
申请日：2016-06-24
申请人： Daiichi Sankyo Co., Ltd.
发明人： UEDA, Tsuyoshi , ABE, Yuzo
IPC分类号： C07D233/64 , C07C68/06 , C07C69/96 , C12P41/00 , C07B61/00
CPC分类号： C07D233/64 , C07B43/06 , C07B61/00 , C07B2200/13 , C07C68/06 , C07C69/96 , C12P17/14 , C12P41/00 , C12Y301/01003
摘要： A method for producing a 1-(acyloxy)alkyl carbamate derivative (III), using a fluorous alkyl carbonate derivative (I), and a fluorous alkyl carbonate derivative (I) and a method for producing the same. In the formula, R 1 represents C 1 -C 4 alkyl group or a C 3 -C 6 cycloalkyl group, R 2 represents a C 1 -C 4 alkyl group or a hydrogen atom, and A represents a fluorous alkyl group (wherein the fluorous alkyl group represents a C 2 -C 11 alkyl group in which 40% or more of the hydrogen atoms are replaced by fluorine atoms).

5. 发明公开

EP3196193A4 METHOD FOR PRODUCING OPTICALLY ACTIVE VALERIC ACID DERIVATIVE 失效
公开(公告)号：EP3196193A4
公开(公告)日：2018-02-21
申请号：EP15841682
申请日：2015-09-17
申请人： DAIICHI SANKYO CO LTD
发明人： UEDA TSUYOSHI , UKAI KAZUTOSHI
IPC分类号： C07D233/64 , A61K31/417 , A61P43/00 , C07B61/00
CPC分类号： C07D233/64 , A61K31/417 , C07B53/00 , C07B61/00 , C07B2200/07
摘要： A method for producing a compound (3), which comprises allowing a compound (1) to react with hydrogen gas in an inert solvent, in the presence of a specific chiral ligand and a ruthenium catalyst, or in the presence of an asymmetric transition metal complex catalyst previously generated from the chiral ligand and the ruthenium catalyst.

6. 发明公开

EP3204514A1 ALGORITHMS FOR GENE SIGNATURE-BASED PREDICTOR OF SENSITIVITY TO MDM2 INHIBITORS 审中-公开
标题翻译：基于基因特征的MDM2抑制剂灵敏度预测算法
公开(公告)号：EP3204514A1
公开(公告)日：2017-08-16
申请号：EP15790296.6
申请日：2015-10-09
申请人： Daiichi Sankyo Co., Ltd.
发明人： TSE, Ngai-chiu Archie , NAKAMARU, Kenji , TAZAKI, Koichi , WATANABE, Kenji , SEKI, Takahiko
IPC分类号： C12Q1/68 , A61K31/499
CPC分类号： C12Q1/6886 , A61K31/4439 , A61K31/499 , C12Q2600/106 , C12Q2600/156 , C12Q2600/158 , G01N33/574
摘要： Provided are gene signatures that are predictive of the sensitivity of a cancer or tumor to an MDM2i or an antagonist of the MDM2-p53 interaction. Differentially expressed genes in the provided gene signatures serve as biomarkers for determining and assessing the sensitivity of cancer and tumor samples to treatment or therapy with an MDM2i. Also provided are methods of determining MDM2i sensitivity of a test sample such as different cancer and tumor types and subtypes, based on the expression of genes in the MDM2i sensitive gene signatures in reference samples and the test sample even if all of the MDM2i sensitivities of the reference samples are unknown, and treating individuals with an MDM2i if their cancers are determined to be MDM2i-sensitive, based on the practice of the described methods. TP53 gene and p53 protein status can also be determined for the samples undergoing analysis for MDM2i sensitivity.
摘要翻译：提供可预测癌症或肿瘤对MDM2i或MDM2-p53相互作用拮抗剂敏感性的基因标记。所提供的基因标记中的差异表达基因充当用于确定和评估癌症和肿瘤样品对用MDM2i治疗或治疗的敏感性的生物标志物。还提供了基于参考样品和测试样品中MDM2i敏感性基因标签中的基因表达来确定测试样品（例如不同癌症和肿瘤类型和亚型）的MDM2i敏感性的方法，即使所有MDM2i敏感性参考样本是未知的，并且基于所描述的方法的实践，如果MDM2i的癌症被确定为MDM2i敏感的，则用MDM2i治疗个体。对于MDM2i敏感性分析的样品，也可以确定TP53基因和p53蛋白的状态。本发明的方法，平台，试剂盒，试剂和组合物提供了用于个体化或个体化治疗其癌症对MDM2抑制剂显示敏感性的有利方法和工具，如通过基因标记中的基因相对于对照到所描述的方法。

7. 发明公开

EP3121175A4 1,3-BENZODIOXOLE DERIVATIVE 有权
标题翻译： 1,3-苯并二氧戊衍生金融
公开(公告)号：EP3121175A4
公开(公告)日：2017-08-02
申请号：EP15765525
申请日：2015-03-16
申请人： DAIICHI SANKYO CO LTD
发明人： KANNO OSAMU , WATANABE JUN , HORIUCHI TAKAO , NAKAO AKIRA , SUZUKI KEISUKE , YAMASAKI TOMONORI , ADACHI NOBUAKI , HONMA DAISUKE , HAMADA YOSHITO
IPC分类号： C07D405/12 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P43/00 , C07D405/14 , C07D417/14
CPC分类号： C07D405/12 , C07D405/14 , C07D417/14
摘要： The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1,3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and V in the formula (I) are each as defined in the present specification).
摘要翻译：本发明提供具有特定化学结构的化合物或其药理学上可接受的盐，其对EZH1和/或EZH2活性具有优异的抑制效果。本发明提供具有由通式（I）表示的1,3-苯并间二氧杂环戊烯结构的化合物或其药理学上可接受的盐，或含有该化合物（其中R 1，R 2，R 3，R 4，式（I）中的R 5，R 6和V各自如本说明书中所定义）。

8. 发明公开

EP3192875A1 SUSTAINED-RELEASE PHARMACEUTICAL COMPOSITION FOR TREATING AND PREVENTING OPHTHALMIC DISEASES 无效转让
标题翻译：持续释放药物组合物，用于治疗和预防眼部疾病
公开(公告)号：EP3192875A1
公开(公告)日：2017-07-19
申请号：EP15840177.8
申请日：2015-09-09
申请人： Daiichi Sankyo Co., Ltd.
发明人： KASUYA, Yuji , NAKAGAMI, Yasuhiro , HATANO, Emiko , INOUE, Tatsuya , YOSHIDA, Kazuhiro , KOMORIYA, Satoshi , MURAKAMI, Yoko , IWASAKI, Masaru , SAKAMOTO, Atsunobu , MASUDA, Kayoko , MINAMI, Masako , IIZUKA, Mayumi , ONO, Yasunori , OHNUKI, Takashi
IPC分类号： C12P33/06 , A61K9/52 , A61K31/277 , A61K31/336 , A61K47/34 , A61P1/16
摘要： The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body
摘要翻译：本发明涉及具有激活Keap1 / Nrf2 / ARE信号传导途径的能力并且具有优异的抗炎作用和细胞保护作用的萜类衍生物，以及对于治疗和预防后部结构有效的缓释药物组合物包含萜类衍生物作为活性成分的氧化应激引起的眼病。本发明提供含有本发明的萜类衍生物作为有效成分的用于治疗或预防后眼病的局部给药型缓释药物组合物，其中所述缓释药物组合物保持其药理作用通过在生理条件下持续释放萜类衍生物1周或更长时间，并且具有可给予玻璃体的基质材料和玻璃体可施用的形式

9. 发明授权

EP2853505B1 CONTROLLED PILL DISPENSING CONTAINER 有权
标题翻译： GESTEUERTERTABLETTENAUSGABEBEHÄLTER
公开(公告)号：EP2853505B1
公开(公告)日：2017-05-03
申请号：EP13793387
申请日：2013-05-22
申请人： DAIICHI SANKYO CO LTD
发明人： DODO MASAAKI , KUBOTA KIYOSHI , IKEMOTO KENJI , MIWATA TORU
IPC分类号： B65D83/04 , A61J1/03 , A61J7/00 , A61J7/02 , A61J7/04
CPC分类号： B65D83/04 , A61J7/0076 , A61J7/0418 , A61J7/0436 , A61J7/0481 , A61J2200/30 , B65D83/0409 , B65D2583/0454 , B65D2583/0486 , B65D2585/56
摘要： An upper case is provided with a stopper projection that extends downward between an outlet and a dispensing standby space, in a situation where a container body is closed. A lower case is provided with a pusher member that is positioned on a side opposed to the stopper projection with respect to the dispensing standby space, in a situation where the container body is closed, the pusher member being configured to, during an operation for opening the upper case, push a tablet located in the dispensing standby space toward the outlet. During the operation for opening the upper case, the stopper projection is configured to get over a side surface of the tablet located in the dispensing standby space, and is configured to stop an outlet-side surface of a tablet succeeding to the tablet having been located in the dispensing standby space. A sensor unit is configured to detect passage of one tablet moving from the dispensing standby space to the outlet so as to detect occurrence of dispensing of the tablet. The detection result is recorded in a data recording unit.
摘要翻译：在上壳体设置有在容器本体关闭的情况下在出口和分配待机空间之间向下延伸的止动突起。下壳体设置有推动构件，该推动构件在关闭容器主体的情况下位于与止动突起相对的一侧上，推动构件构造成在打开操作期间上壳体将位于分配待机空间内的药片推向出口。在打开上壳体的操作期间，止动器突起被构造成越过位于分配待机空间中的药片的侧表面，并且被配置为停止药片的位于已定位的药片的出口侧表面在分配待机空间中。传感器单元被构造成检测一个片剂从分配待机空间移动到出口的通过，以检测片剂分配的发生。检测结果被记录在数据记录单元中。

10. 发明公开

EP3040330A4 METHOD FOR PRODUCING PYRROLE DERIVATIVE, AND INTERMEDIATE THEREOF 有权
标题翻译：用于生产吡咯及其中间体
公开(公告)号：EP3040330A4
公开(公告)日：2017-04-19
申请号：EP14839943
申请日：2014-08-26
申请人： DAIICHI SANKYO CO LTD
发明人： WATANABE MASASHI , NAGASAWA HIROSHI , SATO NORITADA
IPC分类号： C07D207/456 , C07B57/00 , C12P41/00
CPC分类号： C07D207/34 , C07B57/00 , C07D207/456 , C12P17/10 , C12P41/005
摘要： The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R 1 represents a C1-C4 alkyl group, and R 2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.

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