发明名称 DIFLUORO-PENTAPEPTIDE DERIVATIVE ANTI-INFLAMMATORY AGENTS
摘要 <p>The subject invention involves anti-inflammatory compounds having structure (I), wherein: (a) -X is cyclic alkyl, having from 4 to 15 carbon atoms; branched alkyl, having from 6 to 15 carbon atoms; or aryl having from 6 to 15 carbon atoms; (b) n is an integer from 0 to 2; (c) -V- is -OC(O)-, -N(Q)C(O)-, -N(Q)C(S)-, -C(O)-, -SO2- or -P(O)(OH)-; (d) -Q is hydrogen; or straight or branched chain alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to 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 20 carbon atoms; (e) Z is -O- or -NH-; when V is -OC(O)-, -Z- is -NH-; (f) -R1 is a hydrophobic moiety; (g) -R2 is a hydrophobic moiety; (h) -R3 is -(CH2)m-A-NH2 or -(CH2)m-A-B-C(NH2) = NH wherein m is an integer from 1 to about 6, -A- is a covalent bond or p-phenyl or p-cyclohexyl, and -B- is a covalent bond or -NH-; (i) -R4 is a hydrophobic moiety; (j) -R5 is -(CH2)m-A-NH2 or -(CH2)m-A-B-C(NH2) = NH wherein m is an integer from 1 to about 6, -A- is a covalent bond or p-phenyl or p-cyclohexyl, and -B- is a covalent bond or -NH-; and (k) -Y is hydrogen or methyl. The subject invention also involves pharmaceutical compositions comprising the above compounds, and methods for treating inflammation or pain using such compounds and compositions.</p>
申请公布号 WO1994014842(A1) 申请公布日期 1994.07.07
申请号 US1993012349 申请日期 1993.12.16
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