The present invention is a compound of formula
1
wherein
R
1
is halogen or lower alkyl;
R
2
is hydrogen, lower alkyl, cycloalkyl, —(CH
2
)
m
-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH
2
)
m
-indolyl;
R
3
is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl;
n is 0, 1 or 2;
m is 0, 1 or 2;
or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A &agr;5 receptor binding sites.
本发明是一种化合物,其化学式为
1
其中
R
1
是卤素或较低的烷基;
R
2
是氢、较低的烷基、环烷基、—(CH
2
)
m
-苯基,其中苯环可能被较低的烷氧基取代,或者是—(CH
2
)
m
-吲哚基;
R
3
是—C(O)O-较低的烷基、—C(O)OH,或者是一个五元杂环芳基,这些环可能被较低的烷基或环烷基取代;
n为0、1或2;
m为0、1或2;
或其药学上可接受的酸盐。化合物I显示出对GALA A &agr;5受体结合位点的高亲和力和选择性。
Lactam compounds useful as protein kinase inhibitors
申请人:Blackburn Christopher
公开号:US20060100194A1
公开(公告)日:2006-05-11
The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
申请人:Blackburn Christopher
公开号:US20120178739A1
公开(公告)日:2012-07-12
The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
[EN] FUSED AZEPINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS D'AZÉPINE FUSIONNÉS ET LEUR UTILISATION EN CANCÉROTHÉRAPIE
申请人:CHENGDU ANTICANCER BIOSCIENCE LTD
公开号:WO2022152097A1
公开(公告)日:2022-07-21
The present disclose includes, among other things, compounds that treat or lessen the severity of cancer, pharmaceutical compositions and methods of making and using the same.