201286-26-2Relevant academic research and scientific papers
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I
Hulme, Christopher,Moriarty, Kevin,Miller, Bruce,Mathew, Rose,Ramanjulu, Mercy,Cox, Paul,Souness, John,Page, Ken M.,Uhl, Joanne,Travis, Jeffrey,Huang, Fu-Chih,Labaudiniere, Richard,Djuric, Stevan W.
, p. 1867 - 1872 (1998)
This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds described contain an indole moiety which replaces the 'rolipram- like' 3-methoxy-4-cyclopentoxy motif. Several of the compounds presented possess low nanomolar IC50's for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-α levels in LPS challenged mice (mouse endotoxemia model) are also reported.
Substituted azabicyclic compounds
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, (2008/06/13)
This invention is directed to certain physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.
