公开(公告)号：US09051310B2

公开(公告)日：2015-06-09

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

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。

公开(公告)号：US09586951B2

公开(公告)日：2017-03-07

申请号：US15052252

申请日：2016-02-24

Applicant: FUJIFILM Corporation

Inventor： Yohei Kubo ,  Makoto Ando ,  Hidehiko Tanaka ,  Shuhei Osaka ,  Takuya Matsumoto ,  Hiyoku Nakata ,  Daisuke Terada ,  Tatsuya Nitabaru

IPC: C07D413/14 ,  C07D401/14 ,  C07D405/14 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D411/04 ,  C07D411/14 ,  C07D417/14 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08

CPC classification number: C07D413/14 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D411/04 ,  C07D411/14 ,  C07D417/14 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08

Abstract: There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like).

Abstract translation: （式中，环A表示通式[I]表示的环; *表示键合位置，Z 2表示CH等，Z1表示CR 6等，R 6表示氢原子等; X 1表示 CHR 7等; R 7表示氢原子等; X 2表示CH 2等; R 1和R 2相同或不同，R 1和R 2各自表示氢原子等; R 3， R 4和R 5彼此相同或不同，R 3，R 4和R 5各自表示氢原子，NR a R b等; R a和R b分别表示氢原子，C 1-8烷基 可以具有取代基的基团等）。