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US 2003/0125327 A1Published application
Prodrugs of imidazopyridine derivatives
OwnerJ?ouml;rg Senn-Bilfinger, Wilm Buhrinventors
Life of this patent
Estimating the term…
Abstract
Compounds of formula (1), in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases. 1
Claims10
A compound of the formula 1
- 7
- in which
- R1 is hydrogen, 1-4C-alkyl or hydroxy-1-4C-alkyl,
- R2 is hydrogen, 1-4C-alkyl, hydroxy-1-4C-alkyl, halogen, 2-4C-alkenyl or 2-4C-alkynyl,
- R3 is hydrogen, halogen, trifluoromethyl, 1-4C-alkyl, 2-4C-alkenyl, 2-4C-alkynyl, carboxyl, —CO-1-4C-alkoxy, hydroxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, fluoro-1-4C-alkoxy-1-4C-alkyl or the radical —CO—NR3aR3b,
- one of the substitutents R4a and R4b is hydrogen and the other is hydroxyl, 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkoxy, 1-4C-alkylcarbonyloxy or the radical R4′, or in which R4a and R4b together are O (oxygen),
- where R4′ is a radical from which a hydroxyl group is formed under physiological conditions,
- one of the substitutents R5a and R5b is hydrogen and the other is hydrogen, hydroxyl, 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkoxy, 1-4C-alkylcarbonyloxy or the radical R5′, or in which R5a and R5b together are O (oxygen),
- where R5′ is a radical from which a hydroxyl group is formed under physiological conditions,
- where
- one of the substituents R4a and R4b must have the meaning R4′ and/or one of the substituents R5a and R5b must have the meaning R5′,
- R6 is hydrogen, halogen, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonylamino, 1-4C-alkoxy-1-4C-alkoxycarbonylamino or trifluoromethyl,
- R7 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy and
- X is O (oxygen) or NH,
- where
- R3a is hydrogen, 1-7C-alkyl, hydroxy-1-4C-alkyl or 1-4C-alkoxy-1-4C-alkyl and
- R3b is hydrogen, 1-7C-alkyl, hydroxy-1-4C-alkyl or 1-4C-alkoxy-1-4C-alkyl,
- or where
- R3a and R3b together, including the nitrogen atom to which both are bonded, are a pyrrolidino, piperidino or morpholino radical,
- or its salts.
17 more elements
Dependencies are inferred from the claim text.