- LMP7 INHIBITORS
-
The present disclosure provides compounds that are Large Multifunctional Protease 7 (LMP7) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of LMP7. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
- -
-
Page/Page column 82
(2016/04/26)
-
- Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring
-
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine
- Ueno, Hiroshi,Yokota, Katsuyuki,Hoshi, Jun-Ichi,Yasue, Katsutaka,Hayashi, Mikio,Hase, Yasunori,Uchida, Itsuo,Aisaka, Kazuo,Katoh, Susumu,Cho, Hidetsura
-
p. 3586 - 3604
(2007/10/03)
-
- Amidine compounds
-
A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
- -
-
-
- Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors
-
Fluorescent antagonists for human 5-HT4 receptors were synthesized based on ML10302 1, a potent 5-HT4 receptor agonist and on piperazine analogue 2. These molecules were derived with three fluorescent moieties, dansyl, naphthalimide, and NBD (7-nitrobenz-2-oxa-1,3-diazol-4-yl), through alkyl chains. The synthesized molecules were evaluated in binding assays on the recently cloned human 5-HT4(e) receptor isoform stably expressed in C6 glial cells with [3H]GR113808 as the radioligand. The affinity values depended upon the basal structure together with the alkyl chain length. The derivatives based on ML10302 were more potent ligands than the derivatives based on piperazine analogue. For ML10302-based ligands, dansyl and NBD derivatives attached through a chain length of one carbon atom 17a and 32, respectively, led to affinities close to the affinity of ML10302. The most potent compounds 17a, 28, and 32 produced an inhibition of the 5-HT stimulated cyclic AMP synthesis in the same cellular system with nanomolar Kb values. Fluorescent properties of 17a, 28, and 32 were more particularly studied. Interactions of the fluorescent ligand 28 with the h5-HT4(e) receptor were indicated using h5-HT4(e) receptor transfected C6 glial cell membranes and entire cells. Ligand 28 was also used in fluorescence microscopy experiments in order to label h5-HT4(e) receptor transfected C6 glial cells, and subcellular localization of these receptors was more precisely determined using confocal microscopy.
- Berque-Bestel, Isabelle,Soulier, Jean-Louis,Giner, Mireille,Rivail, Lucie,Langlois, Michel,Sicsic, Sames
-
p. 2606 - 2620
(2007/10/03)
-
- Phosphonic acid derivatives
-
A phosphonic acid derivative which is useful for medically treating hyperlipemia, represented by the following general formula (I) or a pharmacologically acceptable salt thereof: STR1 Representative example of the compound according to the present invention is one represented by the following formula: STR2
- -
-
-