[EN] HETEROARYL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS HÉTÉROARYLE ET UTILISATIONS ASSOCIÉES
申请人:CELGENE AVILOMICS RES INC
公开号:WO2014144737A1
公开(公告)日:2014-09-18
The present invention relates to compounds useful as inhibitors of protein kinases, containing a cysteine residue in the ATP binding site. The invention further provides for pharmaceutically acceptable compositions comprising therapeutically effective amounts of one or more of the protein kinase inhibitor compounds and methods of using said compositions in the treatment of cancers and carcinomas.
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; Z
2
represents CH or the like; Z
1
represents CR
6
or the like; R
6
represents a hydrogen atom or the like; X
1
represents CHR
7
or the like; R
7
represents a hydrogen atom or the like; X
2
represents CH
2
or the like; R
1
and R
2
are the same as or different from each other, and each of R
1
and R
2
represents a hydrogen atom or the like; R
3
, R
4
, and R
5
are the same as or different from each other, and each of R
3
, R
4
, and R
5
represents a hydrogen atom, NR
a
R
b
, or the like; and each of R
a
and R
b
represents a hydrogen atom, a C
1-8
alkyl group which may have a substituent, or the like.)
提供一种由通用式[1A]表示的吗啉衍生物或其盐。
(在该式中,环A代表由通用式[I]表示的环;*代表连接位置;Z
2
代表CH或类似物;Z
1
代表CR
6
或类似物;R
6
代表氢原子或类似物;X
1
代表CHR
7
或类似物;R
7
代表氢原子或类似物;X
2
代表CH
2
或类似物;R
1
和R
2
相同或不同,且R
1
和R
2
中的每一个代表氢原子或类似物;R
3
,R
4
和R
5
相同或不同,且R
3
,R
4
和R
5
中的每一个代表氢原子,NR
a
R
b
或类似物;R
a
和R
b
中的每一个代表氢原子,可能具有取代基的C
1-8
烷基基团,或类似物。)
[EN] MK2 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS MK2 ET UTILISATIONS ASSOCIÉES
申请人:CELGENE AVILOMICS RES INC
公开号:WO2014149164A1
公开(公告)日:2014-09-25
The present invention provides compounds, compositions thereof, and methods of using the same.
本发明提供了化合物、其组合物以及使用方法。
INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR
申请人:Bifulco, Jr. Neil
公开号:US20150119405A1
公开(公告)日:2015-04-30
Described herein are inhibitors of FGFR-4, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
申请人:Abbisko Therapeutics Co., Ltd.
公开号:US20190270742A1
公开(公告)日:2019-09-05
Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs.