N3 alkylated benzimidazole derivatives as MEK inhibitors
申请人:——
公开号:US20040116710A1
公开(公告)日:2004-06-17
Disclosed are compounds of the formula I
1
and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R
1
, R
2
, R
7
, R
8
, R
9
and R
10
are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
[EN] COMPOUNDS AND METHODS FOR TREATING NEOPLASIA<br/>[FR] COMPOSÉS ET PROCÉDÉS POUR LE TRAITEMENT DE LA NÉOPLASIE
申请人:MEDEXIS S A
公开号:WO2012013816A1
公开(公告)日:2012-02-02
The invention features compounds, pharmaceutical compositions and methods useful for the treatment of neoplasia. In particular embodiments, the compounds of the invention are useful for the treatment of multidrug resistant neoplasia.
The invention relates to novel compounds of the formula (I)
in which Z, Y, A
1
, A
2
, A
3
, A
4
, X, R
7
, R
8
and R
9
have the meanings mentioned above,
and processes and intermediates for the preparation thereof, and their use for controlling animal pests, in particular insects.
作者:Michael S. Malamas、Jimit Girish Raghav、Xiaoyu Ma、Chandrashekhar Honrao、JodiAnne T. Wood、Othman Benchama、Han Zhou、Srikrishnan Mallipeddi、Alexandros Makriyannis
DOI:10.1016/j.bmc.2018.08.003
日期:2018.10
conformation was coincided with that of the AM11542 CB1 agonist-bound structure, stabilizing the CB1 receptor at the active-state (agonistic functional effect). We have selected oxime trans-8a based on its potency for CB1, and favorable pharmacodynamic profile, such as fast onset and predictable duration of pharmacological action, for evaluation in pre-clinical models of anorexia nervosa.