| 摘要 |
Novel compounds are disclosed having formula (I) as well as pharmaceutically acc eptable salts, esters and amides thereof, wherein R1 is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralky l), (d) loweralkoxy, (e) cycloalkyl of from 3 to 8 carbons (f) phenyl, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyl, (k) lowe ralkynyl, (l) alkoxycarbonyl, (m) nitrogen-containing aromatic heterocycle and (n) a group of the formula -NR7R8; R2 is selected from the group containing of halogen, loweralkoxy, carbocyclic aryloxy or carbocyclic aryl(loweralkyl)oxy, loweralkyl, loweralkenyl, cycloalkyl of from 3 to 8 carbons, cycloalkenyl of from 4 to 8 carbons, carbocyclic aryl(loweralkyl), cycl oalkyl(loweralkyl), phenyl, amino, (loweralkyl)amino, carbocyclic aryl(loweralkyl)amino, hydroxy-substituted (loweralkyl)amino, nitrog en-containing aromatic heterocycle, bicyclic nitrogen-containing heterocycle and nitrogen-containing heterocycle hav ing formula (II), wherein x is 0 to 3; R9 is selected from (a)-(CH2)m-, wherein m is 1, 2 or 3, and (b) -(CH2)n R10(CH, )p-, wherein R10 is selected from S, O and N, n is 1 or 2, and p is 1 or 2: and Y is a non-hydrogen substituent independently selected from loweralkyl, halo(loweralkyl), loweralkoxy, hydroxy-substituted loweralkyl, hydroxy, amino(loweralkyl), halogen and a group having the formula -NR11R12; R3 is hydrogen, halogen or loweralkoxy; R4 is selected from the group consisting of hydrogen loweralkyl, a pharmaceutically acceptable cation and a prodrug ester group: R5 is selected fro m the group consisting of hydrogen halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formul a -NR13R14; and A is N or CR6, wherein R6 is selected from hydrogen, halogen, loweralkyl. halo(loweralkyl), hyd roxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy and amino(loweralkyl) or, alternatively, R 1 and R6, taken together with the atoms to which they are attached form a 6-membered saturated ring which may contain an oxygen o r a sulfur atom and which may be substituted with loweralkyl; with the proviso that when R5 is hydrogen and A is CH then either (a) R1 is NR7R8, or (b) R2 is a group having formula (III), wherein x is 1-3 and R9 and Y are as defined above.
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