3-ammoniopropenyl cephalosporin compounds as antibacterial agents and
process for preparing the same
    3.
    发明授权
    3-ammoniopropenyl cephalosporin compounds as antibacterial agents and process for preparing the same 失效
    3-氨基丙烯基头孢菌素化合物作为抗菌剂及其制备方法

    公开(公告)号:US5872249A

    公开(公告)日:1999-02-16

    申请号:US941772

    申请日:1997-09-30

    CPC分类号: C07D501/00

    摘要: A 3-ammoniopropenyl cephalosporin of the following formula (I): ##STR1## wherein P is hydroxylated alicyclic or aliphatic amines such as meso-3,4-dihydroxy-1-methylpyrrolidine, (3S,4S)-3,4-dihydroxy-1-methylpyrrolidine, (3R,4R)-3,4-dihydroxy-1-methylpyrrolidine, rac-3,4-trans-dihydroxy-1-methylpyrrlidine, (2S,4R)-4-hydroxy-1-methyl-2-pyrrolidinemethanol, N-methyl-bis(2-hydroxyethyl)amine, 3,4-cis-dihydroxy-1-methylpiperidine, 3,4-trans-dihydroxypiperidine, 4-hydroxy-1-methylpiperidine, 2-hydroxymethyl-1-methylpiperidine, or tropine, or a pharmaceutically acceptable salt thereof, exhibits good anti-bacterial activities against a wide variety of Gram-positive and Gram-negative bacteria; and a process for the preparation thereof.

    摘要翻译: 下式(I)的3-氨基丙烯基头孢菌素:其中P是羟基化脂环族或脂肪族胺如内消旋-3,4-二羟基-1-甲基吡咯烷,(3S,4S)-3,4 - 二羟基-1-甲基吡咯烷,(3R,4R)-3,4-二羟基-1-甲基吡咯烷,外消旋-3,4-反式 - 二羟基-1-甲基吡咯烷,(2S,4R)-4-羟基-1-甲基 -2-吡咯烷甲醇,N-甲基 - 双(2-羟乙基)胺,3,4-顺式 - 二羟基-1-甲基哌啶,3,4-反式二羟基哌啶,4-羟基-1-甲基哌啶,2-羟甲基-1 - 甲基哌啶或托品妥或其药学上可接受的盐对各种革兰氏阳性和革兰氏阴性细菌表现出良好的抗菌活性; 及其制备方法。

    Cephalosporin compounds and processes for preparing thereof
    4.
    发明授权
    Cephalosporin compounds and processes for preparing thereof 失效
    头孢菌素化合物及其制备方法

    公开(公告)号:US5571909A

    公开(公告)日:1996-11-05

    申请号:US255266

    申请日:1994-06-07

    CPC分类号: C07D501/00

    摘要: Quaternary ammoniocephalosporins of formula(I) wherein Q.dbd.CH or N, P.dbd.hydroxylated amine or hydroxylated heterocyclylamines including N-methyl-bis(2-hydroxyethyl)amine, rac-3,4-trans-dihydroxy-1-methylpyrrolidine, (3S, 4S)-3,4-dihydroxy-1-methylpyrrolidine, (3R,4R)-3,4-dihydroxy-1-methylpyrrolidine, meso-3,4-dihydorcy-1-methylpyrrolidine, (2S, 4R)-4-hydroxy-1-methyl-2-pyrrolidinemethanol 3,4-cis-dihydroxy-1-methylpiperidine, 3,4-trans-dihydroxy-1-methylpiperidine, or tropine, and preparation methods are disclosed. ##STR1##

    摘要翻译: 式(I)的季铵氨孢子,其中Q = CH或N,P =羟基化胺或羟基化杂环基胺,包括N-甲基 - 双(2-羟乙基)胺,外消旋-3,4-反式 - 二羟基-1-甲基吡咯烷,(3S ,4S)-3,4-二羟基-1-甲基吡咯烷,(3R,4R)-3,4-二羟基-1-甲基吡咯烷,内消旋-3,4-二水合-1-甲基吡咯烷,(2S,4R)-4- 羟基-1-甲基-2-吡咯烷甲醇3,4-顺式 - 二羟基-1-甲基哌啶,3,4-反式 - 二羟基-1-甲基哌啶或托品,公开了制备方法。 (一)

    3-ammoniopropenyl cephalosporin compounds as antibacterial agents
    6.
    发明授权
    3-ammoniopropenyl cephalosporin compounds as antibacterial agents 失效
    3-氨基丙烯基头孢菌素化合物作为抗菌剂

    公开(公告)号:US5675003A

    公开(公告)日:1997-10-07

    申请号:US522792

    申请日:1995-09-01

    CPC分类号: C07D501/00

    摘要: A 3-ammoniopropenyl cephalosporin of the following formula (I): ##STR1## wherein P is hydroxylated alicyclic or aliphatic amines such as meso-3,4-dihydroxy-1-methylpyrrolidine, (3S,4S)-3,4-dihydroxy-1-methylpyrrolidine, (3R,4R)-3,4-dihydroxy-1-methylpyrrolidine, rac-3,4-trans-dihydroxy-1-methylpyrrlidine, (2S,4R)-4-hydroxy-1-methyl-2-pyrrolidinemethanol, N-methyl-bis(2-hydroxyethyl)amine, 3,4-cis-dihydroxy-1-methylpiperidine, 3,4-trans-dihydroxypiperidine, 4-hydroxy-1-methylpiperidine, 2-hydroxymethyl-1-methylpiperidine, or tropine, or a pharmaceutically acceptable salt thereof, exhibits good anti-bacterial activities against a wide variety of Gram-positive and Gram-negative bacteria; and a process for the preparation thereof.

    摘要翻译: 下式(I)的3-氨基丙烯基头孢菌素:其中P是羟基化脂环族或脂肪族胺如内消旋-3,4-二羟基-1-甲基吡咯烷,(3S,4S)-3,4 - 二羟基-1-甲基吡咯烷,(3R,4R)-3,4-二羟基-1-甲基吡咯烷,外消旋-3,4-反式 - 二羟基-1-甲基吡咯烷,(2S,4R)-4-羟基-1-甲基 -2-吡咯烷甲醇,N-甲基 - 双(2-羟乙基)胺,3,4-顺式 - 二羟基-1-甲基哌啶,3,4-反式二羟基哌啶,4-羟基-1-甲基哌啶,2-羟甲基-1 - 甲基哌啶或托品妥或其药学上可接受的盐对各种革兰氏阳性和革兰氏阴性细菌表现出良好的抗菌活性; 及其制备方法。

    3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same
    7.
    发明授权
    3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same 失效
    3,4-二氢喹唑啉衍生物作为T型钙通道阻滞剂及其制备方法

    公开(公告)号:US07271260B2

    公开(公告)日:2007-09-18

    申请号:US11018786

    申请日:2004-12-20

    CPC分类号: C07D239/74 C07D239/84

    摘要: The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihydroquinazoline derivatives of the present invention can be effectively used for preventing and treating angina pectoris, high blood pressure, myocardial disease, pain and epilepsy by blocking the T-type calcium channel.

    摘要翻译: 本发明涉及作为T型钙通道阻断剂的3,4-二氢喹唑啉衍生物及其制备方法。 本发明还涉及包含该组合物的组合物。 包含本发明的3,4-二氢喹唑啉衍生物的组合物可以有效地用于通过阻断T型钙通道来预防和治疗心绞痛,高血压,心肌病,疼痛和癫痫。