The present invention provides compounds of formula (I*):
their use as H
3
inhibitors, processes for their preparation, and pharmaceutical compositions thereof.
本发明提供了式(I*)的化合物:它们作为H3抑制剂的用途,其制备方法以及药物组合物。
COMPOUNDS AS NEURONAL HISTAMINE RECEPTOR-3 ANTAGONISTS AND USES THEREOF
申请人:XW LABORATORIES INC.
公开号:US20200102289A1
公开(公告)日:2020-04-02
The present invention relates compounds of Formula (A) as H3R antagonists, as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses as modulators of Histamine 3 Receptor (H3R) functions. The present invention also relates to the uses of the compounds or pharmaceutical compositions in treating or preventing certain disorders and diseases which relate to H3R functions in humans.
Drug design: Oxazoles and thiazoles were designed and synthesised based on previously reported ligands of the 3rd histamine receptor (H3R). The aminopropoxy‐phenyl‐oxazole chemotype was identified as a promising H3R inverseagonist with superior drug‐like properties, good efficacy in vivo and good safety margin.
Compounds Comprising a Lactam or a Lactam Derivative Moiety, Processes for Making Them, and Their Uses
申请人:Celanire Sylvain
公开号:US20090023708A1
公开(公告)日:2009-01-22
The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
Compounds of a formula (I)
[wherein, A represents formula (III-1)
R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et al; p is 0 to 4; X is a carbon atom or nitrogen atom; and X1 to X4 is a lower alkyl et al], or pharmaceutical acceptable salts thereof. These have a potency antagonistic to binding to histamine H3 receptor, or have a potency inhibiting the constant activity of histamine H3 receptor, and are useful in the therapy of obesity, diabetes et al.