| 摘要 |
<p>There are disclosed N<6>-Bicycloadenosines of the formula (I) <CHEM> its individual diastereomers or mixtures thereof, or a pharmaceutically acceptable acid addition salt thereof; wherein R1 is of formula <CHEM> in which NH- is either endo or exo; @@@@ is a double or single bond; n is zero, one, or two; A and B are either both hydrogen or both methyl; D and E are also either both hydrogen or both methyl; C is hydrogen or methyl; with the proviso that when D and E are methyl then A and B are both hydrogen and C is methyl, but when D and E are hydrogen then A, B, and C are all hydrogen or all methyl; X is -C(CH3)2-, -CH2-, -CH2CH2-, or -CH=CH-; R2 is hydrogen, halogen, SR where R is hydrogen or lower alkyl, NR<i>R<ii> where R<i> and R<ii> are independently hydrogen, lower alkyl, phenyl and phenyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl; R2 min and R3 min are independently hydrogen, lower alkanoyl, benzoyl, or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl, or, when taken together, R2 min and R3 min may be lower alkylidene; and R6 min is halogen, hydrogen or R min 5O where R5 min is hydrogen, lower alkanoyl, benzoyl, or benzoyl substituted by lower alkyl, lower alkoxy, halogen, or trifluoromethyl; and the NH- is attached to either one or the other of the adjacent carbons in the radical IIB. Process for producing the compounds, pharmaceutical compositions containing the compositions and methods for using the compounds are also described. The compounds have highly desirable antiflammatory and analgesic activity.</p> |
