Indole derivatives as histamine 3 receptor inhibitors for the treatment of cognitive and sleep disorders, obesity and other CNS disorders
申请人:Bennani Youssef L.
公开号:US20090036446A1
公开(公告)日:2009-02-05
This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H
3
histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H
3
receptor blockade is beneficial.
INDOLE DERIVATIVES AS HISTAMINE 3 RECEPTOR INHIBITORS FOR THE TREATMENT OF COGNITIVE AND SLEEP DISORDERS, OBESITY AND OTHER CNS DISORDERS
申请人:Bennani Youssef L.
公开号:US20110059966A1
公开(公告)日:2011-03-10
This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H
3
histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H
3
receptor blockade is beneficial.
Sequences in the HSP90 promoter form G-quadruplex structures with selectivity for disubstituted phenyl bis-oxazole derivatives
作者:Stephan A. Ohnmacht、Marialuisa Micco、Vanessa Petrucci、Alan K. Todd、Anthony P. Reszka、Mekala Gunaratnam、Marta A. Carvalho、Mire Zloh、Stephen Neidle
DOI:10.1016/j.bmcl.2012.07.065
日期:2012.9
The HSP90 protein is an important target in cancer. We report here that stable quadruplex DNAs can be formed from a promoter sequence in the HSP90 gene, on the basis of melting, circular and NMR studies, and show that these can be selectively targeted by non-macrocyclic quadruplex-stabilizing phenyl bis-oxazole derivatives. These do not bind significantly to duplex DNA and show low stabilization of the human telomeric quadruplex. These results suggest an approach to targeting HSP90 at the DNA level. (C) 2012 Elsevier Ltd. All rights reserved.
TETRACYCLIC CARBOLINE DERATIVES FOR INHIBITING ANGIOGENESIS