TRICYCLIC AMINE DERIVATIVES
    86.
    发明公开
    TRICYCLIC AMINE DERIVATIVES 失效
    DREIRINGIGE氨基衍生物

    公开(公告)号:EP0947513A4

    公开(公告)日:2002-10-02

    申请号:EP97909605

    申请日:1997-10-23

    摘要: Compounds represented by general formula (I) carrying a tricylic amine substituent optionally having various substituents, their salts, hydrates thereof or drugs containing these compounds as the active ingredient. Because of having favorable antibacterial activities on gram-negative and gram-positive bacteria and being excellent both in the dynamics in vivo and safety, these compounds are useful in treating infectious diseases. In said formula (I), Q represents a partial structure which is preferably represented by formula (a); or (b) and may have various substituents.

    摘要翻译: 由通式(I)表示的带有任选具有各种取代基的三取代胺取代基的化合物,其盐,其水合物或含有这些化合物的药物作为活性成分。 由于对革兰氏阴性菌和革兰氏阳性菌具有良好的抗菌活性,并且在体内动力学和安全性方面均优异,所以这些化合物可用于治疗感染性疾病。 在所述式(I)中,Q表示优选由式(a)表示的部分结构; 或(b)并可具有各种取代基。

    QUINOLIZINONE TYPE COMPOUNDS
    88.
    发明授权
    QUINOLIZINONE TYPE COMPOUNDS 失效
    喹诺酮类化合物

    公开(公告)号:EP0723545B1

    公开(公告)日:2002-05-08

    申请号:EP94929998.6

    申请日:1994-09-30

    摘要: Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R2is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R3 is halogen; R4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R5 is hydrogen, loweralkyl, halo(loweralkyl), or -NR?13R14; and R6¿ is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

    摘要翻译: 具有式(I)的抗菌化合物及其药学上可接受的盐,酯和酰胺,其优选实例包括其中R 1为3至8个碳原子的环烷基或取代的苯基的化合物; (b)低级烷基,(c)低级链烯基,(d)三至八个碳的环烷基,(e)四至八个碳的环烯基,(f)低级烷氧基,( (低级烷基)氧基,(i)芳基(低级烷基),(j)环烷基(低级烷基),(k)氨基,(l)(低级烷基)氨基,(m) ,(n)羟基取代的(低级烷基)氨基,(o)苯基,(p)取代的苯基,(q)双环含氮杂环,(r)含氮芳香族杂环和(s)含氮杂环, Ia)其中x在0和3之间; R3是卤素; R4是氢,低级烷基,药学上可接受的阳离子或前药酯基团; R5是氢,低级烷基,卤代(低级烷基)或-NR8R14; 和R6是低级烷基,以及含有这些化合物的药物组合物及其在治疗细菌感染中的用途。

    QUINOLIZINONE TYPE COMPOUNDS
    89.
    发明授权
    QUINOLIZINONE TYPE COMPOUNDS 失效
    连接来源于quinolizinone TYPE

    公开(公告)号:EP0527889B1

    公开(公告)日:2000-08-02

    申请号:EP91909628.9

    申请日:1991-05-01

    摘要: Novel compounds are disclosed having formula (I) as well as pharmaceutically acceptable salts, esters and amides thereof, wherein R1 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 -NR7R8; R2 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; R9 is selected from (a)-(CH¿2?)m-, wherein m is 1, 2 or 3, and (b) -(CH2)nR?10(CH¿2)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 -NR?11R12; 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 from the group consisting of hydrogen, halogen, hydroxy, loweralkyl, halo(loweralkyl), loweralkoxy and a group having the formula -NR13R14; and A is N or CR6, wherein R6 is selected from hydrogen, halogen, loweralkyl, halo(loweralkyl), hydroxy-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 or 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) R?1 is NR7R8¿, or (b) R2 is a group having formula (III), wherein x is 1-3 and R9 and Y are as defined above.

    FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES
    90.
    发明公开
    FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES 失效
    VERKNÜPFTE聚合物杂环化合物VERBINDUNGEN

    公开(公告)号:EP0831094A1

    公开(公告)日:1998-03-25

    申请号:EP96920027.8

    申请日:1996-05-31

    申请人: Eisai Co., Ltd.

    摘要: Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same.
    A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof:
    wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula -e-f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl;
       provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded.
    Which has an excellent antitumor activity.

    摘要翻译: 具有优异抗肿瘤效果的新型稠合多环杂环衍生物及其制备方法。 由以下通式(I)表示的化合物或其药理学上可接受的盐:其中环A表示任选取代的单环芳环或二环稠合环,其中至少一个环为芳环; 环B表示吡咯,4H-1,4-恶嗪,4H-1,4-噻嗪或4(1H) - 吡啶酮; 环C表示任选取代的单环或二环稠合芳环; Y表示由式-ef表示的基团(其中e表示低级亚烷基; f表示任选被羟基化或任选低级烷基化的低级烷基取代的脒基,胍基或氨基);条件是环A和B 均为任选取代的单环芳环,其具有优异的抗肿瘤活性。