New 8-aminopiperidinyl-xanthine derivatives, useful for treating e.g. diabetes, arthritis and osteoporosis, are inhibitors of dipeptidylpeptidase-IV

摘要

8-(3-Aminopiperidinyl)-xanthine derivatives (I), their tautomers, enantiomers, diastereomers, or mixtures, and salts are new. 8-(3-aminopiperidinyl)-xanthine derivatives of formula (I), their tautomers, enantiomers, diastereomers, or mixtures, and salts are new. R : benzyl (optionally substituted), (benzo[1,3]dioxol-5-yl)methyl, 2-(3-cyclopropyloxy-, cyclopropylmethoxy- or cyclobutyloxy-phenyl)-2-oxo-ethyl, 2-oxo-2-[2-(pyridin-3 or 4-yl)phenyl]ethyl, naphthalen-1-ylmethyl ring substituted by 3-cyano, 1,4-dicyano or 2,4-dimethoxy, pyridinylmethyl (optionally ring substituted), ([2,2']bipyridinyl-6-yl)methyl, 2-phenylpyrimidin-4-ylmethyl, 4-phenylpyrimidin-2-ylmethyl, ring-substituted quinolin-2-ylmethyl, ring-substituted isoquinolin-3-ylmethyl, optionally ring-substituted quinazolinylmethyl, quinoxalin-5-ylmethyl, 2,3-dimethylquinoxalin-6-ylmethyl or [1,5]naphthyridin-3-ylmethyl. The full definitions are given in the DEFINITIONS - Full Definitions Field. An independent claim is also included for two methods for preparing (I). [Image] ACTIVITY : Antidiabetic; Antiarthritic; Anorectic; Immunosuppressive; Osteopathic; Antilipemic; Antiarteriosclerotic; Cardiant; Hypotensive; Nephrotropic; Antiinfertility; Antiinflammatory. MECHANISM OF ACTION : (I) are inhibitors of dipeptidylpeptidase-IV (DPP-IV). The compound 1-[4(4-phenylaminoquinazolin-2-yl)methyl}-3-methyl-7-(2-butyn-1-yl)-8-(3-aminopiperidin-1-yl)xanthine had in vitro IC50 against human DPP-IV of 6 nM.