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Helmut Haning

Publications and source records attributed to Helmut Haning.

4 recordsLinked to original sources
PubMed2005

Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.

Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3H-imidazo[5,1-f][1,2,4]triazin-4-ones and pyrazolopyrimidinones, isomeric imidazo[1,5-a][1,3,5]triazin-4(3H)-ones were also shown to be potent and selective PDE inhibitor scaffolds with in vivo activity. SAR trends were elucidated for sulfonamide derivatives with generality across different scaffolds.

3',5'-Cyclic-GMP Phosphodiesterases↗
PubMed2005

Novel heterocyclic thyromimetics.

Novel heterocycle-fused thyromimetics are presented carrying indoles or indazoles instead of the phenolic group in T3. Potent agonists were identified in both series. SAR trends are examined and found to be mostly consistent with previously published thyromimetics. Moderate THRbeta selectivity (approx. 10-fold) was observed in the indole series using isoform-selective transient THR transfection assays.

Animals↗
PubMed2002

Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.

2-aryl-substituted imidazo[5,1-f][1,2,4]triazin-4(3H)-ones represent a new class of potent cGMP-PDE 5 inhibitors that prove to be superior to other purine-isosteric inhibitors. Subnanomolar inhibitors of PDE 5 with activity in in vivo models for erectile dysfunction have been identified. BAY 38-9456 (Vardenafil-hydrochloride) has been selected for clinical studies in the indication of erectile dysfunction.

3',5'-Cyclic-GMP Phosphodiesterases↗