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    • 3. 发明申请
    • QUINOLIZINONE TYPE COMPOUNDS
    • 喹诺酮类化合物
    • WO1991016894A1
    • 1991-11-14
    • PCT/US1991002998
    • 1991-05-01
    • ABBOTT LABORATORIESCHU, Daniel, T.LEE, Cheuk, M.LI, QunCOOPER, Curt, S.PLATTNER, Jacob, J.
    • ABBOTT LABORATORIES
    • A61K31/54
    • C07D471/04A61K38/00C07D213/68C07D455/02C07K5/06026
    • Novel compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters and amides thereof, wherein R is selected from (a) loweralkyl, (b) loweralkenyl, (c) halo(loweralkyl), (d) loweralkoxy, (e) cycloalkyl of from 3 to 8 carbons, (f) phenyl, (g) halo, (h) cyano, (i) nitro, (j) bicycloalkyl, (k) loweralkynyl, (l) alkoxycarbonyl, (m) nitrogen-containing aromatic heterocycle and (n) a group of the formula -NR R ; R is selected from the group consisting 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), cycloalkyl(loweralkyl), phenyl, amino, (loweralkyl)amino, carbocyclic aryl(loweralkyl)amino, hydroxy-substituted (loweralkyl)amino, nitrogen-containing aromatic heterocycle, bicyclic nitrogen-containing heterocycle and nitrogen-containing heterocycle having formula (II), wherein x is 0 to 3; R is selected from (a)-(CH2)m-, wherein m is 1, 2 or 3, and (b) -(CH2)nR (CH2)p-, wherein R 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 -NR R ; R is hydrogen, halogen or loweralkoxy; R is selected from the group consisting of hydrogen, loweralkyl, a pharmaceutically acceptable cation and a prodrug ester group; R is selected from the group consisting of hydrogen, halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formula -NR R ; and A is N or CR , wherein R is selected from hydrogen, halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy and amino(loweralkyl) or, alternatively, R and R , taken together with the atoms to which they are attached, form a 6-membered saturated ring which may contain an oxygen or a sulfur atom and which may be substituted with loweralkyl; with the proviso that when R is hydrogen and A is CH then either (a) R is NR R , or (b) R is a group having formula (III), wherein x is 1-3 and R and Y are as defined above.
    • 公开了具有式(I)化合物及其药学上可接受的盐,酯和酰胺的新型化合物,其中R 1选自(a)低级烷基,(b)低级链烯基,(c)卤代(低级烷基),(d) (f)苯基,(g)卤素,(h)氰基,(i)硝基,(j)双环烷基,(k)低级炔基,(I)烷氧基羰基,(m) )含氮芳族杂环和(n)式-NR 7 R 8的基团; R 2选自卤素,低级烷氧基,碳环芳氧基或碳环芳基(低级烷基)氧基,低级烷基,低级烯基,3至8个碳的环烷基,4至8个碳的环烯基,碳环芳基(低级烷基) ,环烷基(低级烷基),苯基,氨基,(低级烷基)氨基,碳环芳基(低级烷基)氨基,羟基取代的(低级烷基)氨基,含氮芳族杂环,双环含氮杂环和含有式 ),其中x为0至3; R 9选自(a) - (CH 2)m - ,其中m为1,2或3,和(b) - (CH 2)n R 10(CH 2)p - ,其中R 10为 选自S,O和N,n为1或2,p为1或2; 并且Y是独立地选自低级烷基,卤代(低级烷基),低级烷氧基,羟基取代的低级烷基,羟基,氨基(低级烷基),卤素和具有式-NR 11 R 12的基团的非氢取代基。 R 3是氢,卤素或低级烷氧基; R 4选自氢,低级烷基,药学上可接受的阳离子和前药酯基; R 5选自氢,卤素,羟基,低级烷基,卤代(低级烷基),低级烷氧基和具有式-NR 13 R 14的基团。 并且A是N或CR 6,其中R 6选自氢,卤素,低级烷基,卤代(低级烷基),羟基取代的低级烷基,低级烷氧基(低级烷基),低级烷氧基和氨基(低级烷基),或者,R 1和R 6与它们所连接的原子一起形成可含有氧或硫原子并且可以被低级烷基取代的6元饱和环; 条件是当R 5为氢且A为CH时,则(a)R 1为NR 7 R 8,或(b)R 2为具有式(III)的基团, ,其中x为1-3且R 9和Y如上所定义。