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    • 9. 发明授权
    • Naphthyridine derivatives
    • 萘啶衍生物
    • US4341784A
    • 1982-07-27
    • US187081
    • 1980-09-15
    • Jun-ichi MatsumotoYoshiyuki TakaseYoshiro Nishimura
    • Jun-ichi MatsumotoYoshiyuki TakaseYoshiro Nishimura
    • C07D487/02A61K31/435A61P31/04C07D471/04A61K31/44
    • C07D471/04Y02P20/55
    • The present invention provides a 1,8-naphthyridine compound of the formula ##STR1## wherein R is hydrogen, methyl, ethyl or propyl, and a nontoxic pharmaceutically acceptable salt thereof, and a process for preparing a 1,8-naphthyridine compound of the above formula which comprises(A) reacting a compound of the formula ##STR2## wherein Y is halogen, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower alkylsulfonyloxy or arylsulfonyloxy, and R.sub.1 is hydrogen or lower alkyl,with a compound of the formula ##STR3## wherein R.sub.2 is hydrogen or a protective group for the amino group, and R is as defined above,and when a reaction product in which R.sub.1 is lower alkyl and/or R.sub.2 is the amino protective group is obtained, treating it with an acid or base, and/or reductively cleaving it,(B) decomposing a compound of the formula ##STR4## wherein A .crclbar. is a fluorine-containing anion, and R.sub.1 and R.sub.2 are as defined above,and when a reaction product in which R.sub.1 is lower alkyl and/or R.sub.2 is the amino protective group is obtained, treating it with an acid or base, and/or reductively cleaving it,(C) treating a compound of the formula ##STR5## wherein R'.sub.1 is hydrogen or lower alkyl, R'.sub.2 is hydrogen or a protective group for the amino group, provided that R'.sub.1 and R'.sub.2 are not hydrogen atoms at the same time, and R is as defined above,with an acid or base, and/or reductively cleaving it, and optionally converting the resulting compound to a nontoxic pharmaceutically acceptable salt thereof.The 1,8-naphthyridine compound is useful as an antibacterial agent.
    • 本发明提供式IMA图示的1,8-萘啶化合物,其中R是氢,甲基,乙基或丙基,及其无毒的药学上可接受的盐,以及制备1,8-萘啶化合物的方法 其包含(A)使式(I)的化合物其中Y为卤素,低级烷氧基,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,低级烷基磺酰氧基或芳基磺酰氧基,R 1为氢或低级烷基, 其中R2是氢或氨基保护基的式“IMAGE”,R的定义同上,当R1是低级烷基和/或R2是氨基保护基的反应产物得到时,将其处理 (B)分解其中A( - )为含氟阴离子的式“IMAGE”的化合物,并且R 1和R 2如上所定义,当反应 其中R1是低级烷基和/或 r R2是得到的氨基保护基团,用酸或碱处理,和/或还原性地裂解它;(C)处理下式化合物其中R'1是氢或低级烷基,R'2 是氢或氨基的保护基团,条件是R 1和R 2不同时为氢原子,R为如上所定义,与酸或碱反应,和/或还原性地裂解,和 任选地将所得化合物转化为无毒的药学上可接受的盐。 1,8-萘啶化合物可用作抗菌剂。
    • 10. 发明授权
    • 2-[4-(P-Aminobenzyl)-1-piperazinyl]-8-ethyl-5,8-dihydro-5-oxopyrido[2,3-d]p
y
    • 2- {8 4-(对氨基苄基)-1-哌嗪基{9-8乙基-5,8-二氢-5-氧代吡啶并[8,2,3- d {9嘧啶-6-羧酸,其药学上可接受的 盐,其生产和使用的过程
    • US4125615A
    • 1978-11-14
    • US817539
    • 1977-07-20
    • Jun-ichi Matsumoto
    • Jun-ichi Matsumoto
    • A61K31/505A61P31/04C07D471/04C07D401/14
    • C07D471/04
    • 2-[4-(P-Aminobenzyl)-1-piperazinyl]-8-ethyl-5,8-dihydro-5-oxopyrido-[2,3-d]pyrimidine-6-carboxylic acid, and its pharmaceutically acceptable salt. This novel compound can be prepared by reacting a compound of the formula ##STR1## wherein R is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, with a compound of the formula ##STR2## wherein R.sub.1 is an amino group or a group convertible to the amino group, and X is a reactive moiety capable of splitting off together with the hydrogen atom at the 4-position of the 1-piperazinyl group of the compound of the formula (II). Pharmaceutical compositions containing aforesaid compounds as active ingredients are useful for treating a bacterial infection of man and other warm-blooded animals.
    • 2- [4-(对氨基苄基)-1-哌嗪基] -8-乙基-5,8-二氢-5-氧代吡啶并[2,3-d]嘧啶-6-羧酸及其药学上可接受的盐。 这种新化合物可以通过其中R为氢原子或具有1至6个碳原子的烷基的式(II)化合物与下式化合物(III)反应制备:其中R 1 是氨基或可转换成氨基的基团,X是能够与式(II)化合物的1-哌嗪基的4-位上的氢原子一起分解的反应性部分。 含有上述化合物作为活性成分的药物组合物可用于治疗人和其他温血动物的细菌感染。