Amine compounds, their production and use
    55.
    发明申请
    Amine compounds, their production and use 有权
    胺化合物,其生产和使用

    公开(公告)号:US20020032189A1

    公开(公告)日:2002-03-14

    申请号:US09931140

    申请日:2001-08-16

    摘要: A compound of the formula: 1 wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) nullSnull, nullSOnull or nullSO2null, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc., (iv) nullCOnullOnull or (v) null(CH2)p-X1-, null(CH2)p-X1-(CH2)q-, null(CH2)r-CO-X1-, nullSO2nullNR8- or null(CH2)r-SO2nullNR8- wherein X1 is O or NR8, R8 is H, a hydrocarbon group which may be substituted or an acyl, p is 0 to 5, q is 1 to 5, pnullq is 1 to 5, and r is 1 to 4; Y is a divalent C1-6 aliphatic hydrocarbon group optionally containing O or S, which may be substituted; R1 and R2 each is H or a lower alkyl which may be substituted, or R1 and R2 form a N-containing heterocyclic ring which may be substituted; Ring A is a benzene ring which may be further substituted; and Ring B is a 4- to 8-membered ring which may be further substituted, or a salt thereof has the effect of inhibiting amyloid-null protein production and/or secretion and is useful as a pharmaceutical composition for preventing and/or treating the neurodegenerative disease, etc.

    摘要翻译: 下式的化合物:其中Ar是可被取代的芳环组合基团或可被取代的稠合芳基; X是(i)键,(ii)-S-,-SO-或-SO 2 - ,(iii)C 1-6亚烷基,C 2-6亚烯基或C 2-6亚炔基等,(iv)-CO- O-或(V) - (CH 2)p -X 1 - , - (CH 2)p -X 1 - (CH 2)q - , - (CH 2)r -CO-X 1 - ,-SO 2 -NR 8 - 或 - (CH 2) r-SO 2 -NR 8 - ,其中X 1为O或NR 8,R 8为H,可被取代的烃基或酰基,p为0至5,q为1至5,p + q为1至5,r 是1到4; Y是任选地含有O或S的二价C 1-6脂族烃基,其可被取代; R 1和R 2各自为H或可被取代的低级烷基,或R 1和R 2形成可被取代的含氮杂环; 环A是可以被进一步取代的苯环; 环B为可进一步取代的4-至8-元环,或其盐具有抑制淀粉样蛋白β蛋白产生和/或分泌的作用,并且可用作预防和/或治疗 神经变性疾病等

    1-Amino (or substituted
amino)-1,4-dihydro-4-oxo-6-fluoro-7-heterylquinoline-3-carboxylic acids
and their use as antibacterial agents
    57.
    发明授权
    1-Amino (or substituted amino)-1,4-dihydro-4-oxo-6-fluoro-7-heterylquinoline-3-carboxylic acids and their use as antibacterial agents 失效
    1-氨基(或取代的氨基)-1,4-二氢-4-氧代-6-氟-7-杂环喹啉-3-羧酸及其作为抗菌剂的用途

    公开(公告)号:US4499091A

    公开(公告)日:1985-02-12

    申请号:US466095

    申请日:1983-02-14

    CPC分类号: C07D401/04 C07D215/58

    摘要: Novel 1-R-1,4-dihydro-4-oxo-6-fluoro-7-(Z.dbd.N--)-quinolinecarboxylic acids and esters thereof, where R is amino, lower-alkylamino, 2-propenylamino or di-lower-alkylamino, R" is hydrogen or lower-alkyl, and Z.dbd.N is a heterocyclic group, useful as antibacterial agents, are prepared by reacting the corresponding 7-chloroquinoline derivatives with the appropriate heterocyclic compound, Z.dbd.NH. A preferred group of compounds are those where Z.dbd.N is 1-piperazinyl or 4-lower-alkyl-1-piperazinyl.

    摘要翻译: 新的1-R-1,4-二氢-4-氧代-6-氟-7-(Z = N - ) - 喹啉羧酸及其酯,其中R是氨基,低级烷基氨基,2-丙烯基氨基或二低级 - 烷基氨基,R“是氢或低级烷基,Z = N是可用作抗菌剂的杂环基团,通过使相应的7-氯喹啉衍生物与适当的杂环化合物Z = NH反应来制备。 一组优选的化合物是其中Z = N是1-哌嗪基或4-低级 - 烷基-1-哌嗪基的化合物。