- FUSED-RING OR TRICYCLIC ARYL PYRIMIDINE COMPOUND USED AS KINASE INHIBITOR
-
Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 0131; 0132
(2018/03/25)
-
- 2-aminopyridine derivatives and combinatorial libraries thereof
-
The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R1to R5have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing 2-aminopyridine derivative compounds.
- -
-
-
- Dibenzo-epines: Effect of the basic side-chain on neuroleptic activity
-
Structure-activity relationships in a series of dibenzo[b,f][1,4]thiazepines and -oxazepines and dibenzo[b,e][1,4]diazepines having different basic substituents in the 11-position were studied with reference to their neuroleptic activity. A high degree of structure-specificity was found for the piperazinyl moiety as well as for the distances between the distal nitrogen atom of this group and the tricyclic ring system, which distances are probably of importance for receptor binding. It was shown that the N-oxides of the neuroleptic agents clotiapine, loxapine and clozapine were inactive in in vitro binding tests involving central dopaminergic receptors, and it is very likely therefore that the in vivo activity of these N-oxides in the rat is due to their enzymatic reduction to the active parent compounds. All derivatives having a basic side-chain other than N-alkylpiperazinyl were inactive neuroleptically, with the exception of the N-methyl-4-piperidyl derivative which showed relatively weak effects.
- Burki,Fischer,Hunziker,et al.
-
p. 479 - 485
(2007/10/05)
-
