Electrochemical oxidation of 1-trimethylsilyl-1,3-dienes
作者:Jun-ichi Yoshida、Toshiki Murata、Sachihiko Isoe
DOI:10.1016/s0040-4039(00)95688-0
日期:1987.1
BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:US20190047990A1
公开(公告)日:2019-02-14
The invention provides a compound of formula (0):
or a pharmaceutically acceptable salt, N-oxide or tautomer thereof; wherein:
n is 1 or 2;
X is CH or N;
Y is selected from CH and C—F;
Z is selected from C—R
z
and N;
R
1
is selected from:
-(Alk
1
)
t
-Cyc
1
; wherein t is 0 or 1;
Optionally substituted C
1-6
acyclic hydrocarbon groups
R
2
is selected from hydrogen; halogen; and C
1-3
hydrocarbon groups optionally substituted with one or more fluorine atoms;
R
3
is hydrogen or a group L
1
-R
7
;
R
4
is selected from hydrogen; methoxy; and optionally substituted C
1-3
alkyl; and
R
4a
is selected from hydrogen and a C
1-3
alkyl group;
wherein R
z
, Alk
1
, Cyc
1
, L
1
and R
7
are defined herein;
provided that the compound is other than 6-benzyl-3-2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and 3-2-[(2-methylpyrimidin-4-yl)amino]pyridin-4-yl}-7,8-dihydro-1,6-naphthyridin-5(6H)-one and salts and tautomers thereof.
The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
Very high 1,2- and 1,3-asymmetric induction in the reactions of allylic boron compounds with chiral imines
作者:Yoshinori. Yamamoto、Kazuhiro. Maruyama、Toshiaki. Komatsu、Wataru. Ito