公开(公告)号：US20150011499A1

公开(公告)日：2015-01-08

申请号：US14498334

申请日：2014-09-26

Applicant: FUJIFILM Corporation

Inventor： Yasutaka BABA ,  Tatsuya MURAKAMI ,  Junko SHINTANI

IPC: C07H19/06 ,  C07C309/66

CPC classification number: C07H19/06 ,  A61K31/7068 ,  C07C309/04 ,  C07C309/66 ,  C07H19/073

Abstract: A superior antitumor agent is provided. A salt of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine shows at least one or more of such characteristics as (1) it has superior antitumor activity, (2) it shows superior crystallinity, (3) it shows high water solubility, (4) it does not show deliquescent property, (5) it shows superior flowability, (6) it shows superior tableting property, (7) it can be manufactured with less environmental load, and (8) it can be manufactured in a large scale, and therefore it is useful as a bulk drug for medicaments.

Abstract translation: 提供了优异的抗肿瘤剂。 1-（2-脱氧-2-氟-4-硫代-β-阿拉伯呋喃糖基）胞嘧啶的盐显示至少一种或多种这样的特性，如（1）它具有优异的抗肿瘤活性，（2）它显示 优异的结晶度，（3）显示出高的水溶性，（4）不显示潮解性，（5）显示出优异的流动性，（6）表现出优异的压片性能，（7） ，（8）可以大规模制造，因此作为药物的大量药物是有用的。

公开(公告)号：US20140309225A1

公开(公告)日：2014-10-16

申请号：US14317001

申请日：2014-06-27

Applicant: FUJIFILM Corporation

Inventor： Hideyasu FUJIWARA ,  Shinsuke MIZUMOTO ,  Yohei KUBO ,  Hiyoku NAKATA ,  Shinji HAGIWARA ,  Yasutaka BABA ,  Takashi TAMURA ,  Hidenobu KUNIYOSHI ,  Tomoyuki MASHIKO ,  Mari YAMAMOTO

IPC: C07D413/12 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14

CPC classification number: C07D413/12 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.

Abstract translation: 本发明的目的是提供具有优异的Syk抑制活性的化合物和药物组合物。 根据本发明，提供由下式（I）表示的烟酰胺衍生物或其盐，其中R 1为下式（II-1），（III-1）或（IV- 1）（其中R3，R4，R5，n和X1具有与说明书中描述的相同的定义），R2是吡啶基，吲唑基，苯基，吡唑并吡啶基，苯并异恶唑基，嘧啶基或喹啉基， 具有至少一个取代基。