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11 条记录 (耗时 0.023 秒)

    Pyridopyridazine compounds and their use
    4.
    发明授权
    Pyridopyridazine compounds and their use 失效
    吡啶并哒嗪化合物及其用途

    公开(公告)号：US5420275A

    公开(公告)日：1995-05-30

    申请号：US144505

    申请日：1993-11-02

    申请人： Hirotomo Masuya ,  Yoshio Aramaki

    发明人： Hirotomo Masuya ,  Yoshio Aramaki

    IPC分类号： C07D471/04 ,  G01N33/58 ,  C07D513/14 ,  C07D487/04 ,  C07D487/14 ,  G01N33/573

    CPC分类号： C07D471/04 ,  G01N33/582 ,  Y10T436/141111 ,  Y10T436/147777

    摘要： An assay method which comprises utilizing chemiluminescence of a pyridopyridazine compound of the formula ##STR1## wherein R.sub.1 is a hydrocarbon group or a heterocyclic group each of which may be substituted and R.sub.2 is hydroxy group, thiol group, amino group or a monosubstituted amino group, and when R.sub.2 is a monosubstituted amino group, R.sub.2 may be taken together with R.sub.1 to form the ring; R.sub.3 is hydrogen atom, a hydroxy group which may be substituted, an amino group which may be substituted, a thiol group which may be substituted, a halogen atom, a heterocyclic group, nitro group, cyano group, carboxyl group which may be esterified or amidated, azido group, sulfo group or an organic sulfonyl group, provided that when R.sub.1 is an aliphalic group, R.sub.3 is not hydrogen atom; and X is oxygen atom or sulfur atom/or a salt thereof; and a novel compound of the formula (I) wherein the symbols are as defined above with proviso that R.sub.3 is hydrogen atom, R.sub.1 is a substituted aryl group or a heterocyclic group which may be substituted, or a salt thereof and the production methods thereof.

    摘要翻译： 一种测定方法，其包括使用式（I）的吡啶并哒嗪化合物的化学发光，其中R 1是各自可以被取代的烃基或杂环基，R 2是羟基，硫醇基，氨基或单取代的 氨基，当R 2为单取代氨基时，R 2可与R 1一起形成环; R 3为氢原子，可被取代的羟基，可被取代的氨基，可被取代的硫醇基，卤素原子，杂环基，硝基，氰基，可被酯化的羧基或 酰胺基，酰胺基，磺基或有机磺酰基，条件是当R 1是脂族基时，R 3不是氢原子; X为氧原子或硫原子，或其盐; 和式（I）的新化合物，其中符号如上所定义，条件是R 3是氢原子，R 1是可被取代的取代的芳基或杂环基，或其盐及其制备方法。

    Antibiotic tan-749, its derivatives, production and use thereof
    5.
    发明授权
    Antibiotic tan-749, its derivatives, production and use thereof 失效
    抗生素tan-749，其衍生物，生产和使用

    公开(公告)号：US4906659A

    公开(公告)日：1990-03-06

    申请号：US129737

    申请日：1987-12-07

    申请人： Setsuo Harada ,  Hideo Ono ,  Hirotomo Masuya ,  Hideaki Natsugari

    发明人： Setsuo Harada ,  Hideo Ono ,  Hirotomo Masuya ,  Hideaki Natsugari

    IPC分类号： C07C237/22 ,  C07C255/29 ,  C07C257/14 ,  C07D295/13 ,  C07C123/00 ,  A61K35/00

    CPC分类号： C07D295/13 ,  C07C237/22 ,  C07C255/29 ,  C07C257/14 ,  C07C2101/02 ,  Y02P20/55

    摘要： A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.

    摘要翻译： 式IMA的化合物，其中R 1和R 4独立地为氨基或通过氮键合的有机残基，R 2为氢或可被取代的烷基，R 3为氢或保护基，R 5为可被取代的羟基或氨基 其可以被取代或其盐; 条件是当R1为氨基，亮氨酰氨基，乙酰氨基或苄氧羰基氨基时，R3为氢，甲基或2-四氢吡喃基，R4为氨基，乙酰氨基或苄氧羰基氨基，R5为可被取代的羟基或可被取代的氨基，R2为烷基 其可以被取代，对耐药细菌具有抗菌活性，因此可用作哺乳动物细菌感染的化学治疗药物。

    Production of 21-phosphate corticords having unprotected hydroxyl radicals at least at the 17.alpha.- and 21-position
    6.
    发明授权
    Production of 21-phosphate corticords having unprotected hydroxyl radicals at least at the 17.alpha.- and 21-position 失效
    至少在17（60和21位）生产具有无保护羟基自由基的21-磷酸皮质激素

    公开(公告)号：US3966778A

    公开(公告)日：1976-06-29

    申请号：US481906

    申请日：1974-06-20

    申请人： Hirotomo Masuya ,  Takuichi Miki

    发明人： Hirotomo Masuya ,  Takuichi Miki

    IPC分类号： A61K31/66 ,  C07F9/09 ,  C07J5/00 ,  C07J75/00

    CPC分类号： A61K31/66 ,  C07F9/09 ,  C07J5/00 ,  C07J75/00

    摘要： There is disclosed a process for preparing 17.alpha.-hydroxy corticoid 21-phosphate which comprises reacting a compound selected from the group consisting of 17.alpha.,21-dihydroxy corticoid and 11, 17.alpha.,21-trihydroxy corticoid with pyrophosphoryl tetrachloride, subjecting the reaction mixture to a hydrolyzing agent and recovering the objective 17.alpha.-hydroxy corticoid 21-phosphate or 11, 17.alpha.-dihydroxy corticoid 21-phosphate from the hydrolysis reaction medium.

    摘要翻译： 公开了一种制备17α-羟基皮质激素21-磷酸的方法，该方法包括使选自17α，21-二羟基皮质激素和11,17α，21-三羟基皮质类固醇与焦磷酰四氯化物的化合物反应， 混合物到水解试剂中并从水解反应介质中回收17α-羟基皮质激素21-磷酸酯或11,17α-二羟基皮质激素21-磷酸酯。

    3-Heterocyclic substituted cephem compounds
    10.
    发明授权
    3-Heterocyclic substituted cephem compounds 失效
    3-杂环取代的头孢烯化合物

    公开(公告)号：US4182866A

    公开(公告)日：1980-01-08

    申请号：US684738

    申请日：1976-05-10

    申请人： Takuichi Miki ,  Taisuke Matsuo ,  Tohru Sugawara ,  Hirotomo Masuya

    发明人： Takuichi Miki ,  Taisuke Matsuo ,  Tohru Sugawara ,  Hirotomo Masuya

    IPC分类号： C07D501/14 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/16 ,  C07D501/18 ,  C07D501/20 ,  C07D501/24 ,  C07D501/48 ,  C07D501/57 ,  C07D501/60

    CPC分类号： C07D501/20

    摘要： Novel cephem compounds having a group of the formula at the 3-position thereof: ##STR1## wherein X represents oxygen, sulfur or imino, which may be substituted; and B represents hydrogen or a hydroxyl, amino, mercapto or hydrocarbon group, which groups may be substituted, can be prepared by reacting a 3-formylcephem compound with a hydrazine compound of the formula: ##STR2## wherein the symbols have the same meanings as above, and subjecting the thus obtained compound to an oxidative ring-closure reaction. The objective compounds are found to have a broad antimicrobial spectrum and, in particular, are effective against gram-negative bacteria including Escherichia Coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus mirabilis, Proteus rettgerii, as well as gram positive ones, and have low-toxity. Thus, these compounds may be used for antimicrobial agents in therapeutical purpose.

    摘要翻译： 在3-位具有下式基团的新型头孢烯化合物：其中X表示可被取代的氧，硫或亚氨基; 并且B表示氢或可以被取代的羟基，氨基，巯基或烃基，可以通过使3-甲酰基头孢烯化合物与下式的肼化合物反应来制备：其中符号具有相同的含义 并将由此得到的化合物进行氧化闭环反应。 发现目标化合物具有广泛的抗菌谱，特别是对革兰氏阴性细菌有效，包括大肠杆菌，肺炎克雷伯菌，普通变形杆菌，奇异变形杆菌，革兰氏阳性菌以及革兰氏阳性细菌， 毒性 因此，这些化合物可以用于治疗目的的抗微生物剂。