In the title mol-ecule, C(16)H(15)FN(4)O, the dihedral angle between the fluoro-substituted benzene ring and the pyrimidinone ring is 52.34 (7)°, while the dihedral angle between the fused benzene ring and the pyrimidinone ring is 3.30 (6)°. An intra-molecular N-H⋯N hydrogen bond may, in part, influence the conformation of the mol-ecule. In the crystal structure, inter-molecular N-H⋯N hydrogen ...

In the title complex, [CuCl(2)(C(8)H(6)N(2)O)(2)(H(2)O)(2)], the Cu(II) ion is located on an inversion center and is octahedrally coordinated by two N atoms of the 1H-quinazolin-4-one ligand, two chloride ligands and two aqua ligands. The axial Cu-O distances are significantly longer [2.512 (2) Å], than the Cu-N [2.022 (2) Å] and Cu-Cl [2.3232 (4) Å] distances as a result of Jahn-Teller distort...

The pharmacokinetics and metabolism of linagliptin (BI1356, 8-(3R-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione) were investigated in healthy volunteers. The 10- and 5-mg (14)C-labeled drug was administered orally or intravenously, respectively. Fecal excretion was the dominant excretion pathway with 84.7% (p.o.) and 58.2% (i.v.) of ...

creasing providing a rapidly expanding market for antiallergic drugs. The first generation anti-histamines penetrate the blood brain barrier and also possess anticholinergic properties and this has led to the development of a second generation of H1-antagonists such as terfenadine and astemizole. A common feature of first generation compounds includes two aryl or heteroaryl rings linked to an a...