Substituted azabicyclic compounds
This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring, system, of 9 ring members, in which the ring is an oxazole, and the ring is a benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon ato...
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Zusammenfassung: | This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring, system, of 9 ring members, in which the ring is an oxazole, and the ring is a benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, hydroxy, -SO2NR4R5, -NR4SO2R5, -NR4R5, -C(=O)R5, -C(=O)C(=O)R5, -C(=O)NR4R5, -C(=O)OR5, -O(C=O)NR4R5, or -NR4C(=O)R5; R3 represents -C(=Z)-N(R7)R6; A1 represents a straight or branched C1-6alkylene chain optionally substituted by hydroxyl, alkoxy, oxo, cycloalkyl, aryl or heteroaryl; Z1 represents a direct bond, an oxygen or sulphur atom or NH; n is zero; and mis 1; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation. |
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