| 摘要 |
<p>The subject invention involves anti-inflammatory compounds having structure (1), wherein (a) n is an integer of from 0 to about 2; (b) -R is selected from straight or branched alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to about 6 carbon atoms; and cyclic alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 13 carbon atoms; and the carbon atom to which -R is bonded is in either D or L configuration; (c) -R' is selected from branched alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 6 carbon atoms; cyclic alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 3 to about 13 carbon atoms; and arylalkyl, the alleyl portion being saturated and having from 1 to about 3 carbon atoms; and the carbon atom to which -R' is bonded is in L configuration; (d) -R'' is -(CH2)m-A-NH2 or -(CH2)m-A-B-C(NH2)=NH, wherein m is an integer of from 1 to about 5; -A- is a covalent bond, or p-phenyl or p-cyclohexyl; and -B- is a covalent bond or -NH-; and the carbon atom to which -R'' is bonded is in L configuration; (e) -Y is hydrogen or trifluoromethyl; (f) -Z- is -O- or -NH-; (g) -V- is selected from -OC(O)-, -N(Q)C(O)-, -N(Q)C(S)-, -C(O)-, -SO2- and -P(O)(OH)-; when -V- is -OC(O)-, -Z- is -NH-; (h) -X is selected from the group consisting of cyclic alkyl, branched alkyl having at least two branches, and aryl, each having from 5 to about 20 carbon atoms; and (i) -Q is selected from the group consisting of hydrogen; and straight or branched chain alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to about 6 carbon atoms; or -Q and -X are covalently linked forming a cyclic moiety which includes the nitrogen to which -Q is bonded and from 5 to about 20 carbon atoms. The subject invention also involves pharmaceutical compositions comprising the above compounds, and methods for treating inflammation or pain using such compounds and compositions.</p> |
