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2004
Fused pyrimidine derivatives
R 0515
Spiroquinazolinones as Novel, Potent, and Selective PDE7 Inhibitors. Part 1. —
biphenyl subseries of spiroquinazolinone-based derivatives of a PDE7 inhibitor
52- 137 The
screening hit is discovered as new class of PDE7 inhibitors. Furthermore, druglike
characteristics such as solubility are explored by introducing ionizable functions onto
the aromatic ring. Functionalities reaching from carboxylic acid to basic amines have
little influence on PDE7 inhibitory activity. Introduction of an alkylamine group leads
to the identification of soluble and highly potent PDE7 inhibitors, cf. (VI) and (VII).
— (LORTHIOIS*, E.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 18, 4623-4626;
Novartis Pharma AG, CH-4002 Basel, Switz.; Eng.) — H. Hoennerscheid
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