A series of phenothiazine carboxylic acid derivatives, having 6-amino-pyrimidine-2,4(1H,3H)-dione moiety via a appropriate linker, were synthesized and evaluated for their affinity toward human histamine H1 receptor and Caco-2 cell permeability. Selected compounds were further evaluated for their oral anti-histaminic activity in mice and bioavailability in rats. Finally, promising compounds were examined
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof
in which m, n, W, X, Y, Z, R, R
1
, R
2
, R
3
and R
4
are as defined in the specification, for use in therapy.
[EN] SULFONYL PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATING PROKINETICIN MEDIATED DISEASES<br/>[FR] DÉRIVÉS DE SULFONYLPIPÉRIDINE ET LEUR UTILISATION POUR LE TRAITEMENT DE MALADIES MÉDIÉES PAR UNE PROKINÉTICINE
申请人:TAKEDA PHARMACEUTICAL
公开号:WO2013179024A1
公开(公告)日:2013-12-05
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof : (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conitions.
Novel aza-ring derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
申请人:Peters Dan
公开号:US20070021404A1
公开(公告)日:2007-01-25
This invention relates to novel aza-ring derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.