3-Nitropyrazole compounds and anti-microbial compositions
    11.
    发明授权
    3-Nitropyrazole compounds and anti-microbial compositions 失效
    3-硝基吡唑化合物和抗微生物组合物

    公开(公告)号:US4172136A

    公开(公告)日:1979-10-23

    申请号:US889594

    申请日:1978-03-23

    CPC分类号: C07D231/16

    摘要: New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO-NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.

    摘要翻译: 新的具有下式的3-硝基吡唑化合物:其中R 1是低级烷基; R2是氢或低级烷基; R3是氰基,羧基或低级烷氧基羰基或基团-CO-NR4R5,其中R4是氢或羟基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,硫代氨基甲酰基,脲基,硫脲基,羟基苯基,吡啶甲基或是低级烷基,烯基或环烷基取代 如果需要,通过氰基,羟基,吡咯烷子基,哌啶子基,氨基,低级烷基氨基,低级二烷基氨基或低级酰基氨基取代基,R 5是氢原子或低级烷基,或者R 4和R 5一起代表低级亚烷基桥; 并且其药理学兼容的药物作为抗微生物药剂,特别是在系统性和在尿道感染中是非常有效的。

    Adenosine-5'-carboxylic acid amides
    12.
    发明授权
    Adenosine-5'-carboxylic acid amides 失效
    腺苷-5'-羧酸酰胺

    公开(公告)号:US4224438A

    公开(公告)日:1980-09-23

    申请号:US161338

    申请日:1971-07-09

    IPC分类号: C07H19/16 A61K31/70 C07H19/18

    CPC分类号: C07H19/16

    摘要: Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.

    摘要翻译: 具有以下通式的腺苷-5'-羧酸衍生物:其中Z为两个氢原子或二价低级亚烷基,其中R 1和R 2独立为 氢,羟基,氨基,低级烷基,低级烯基,任选N-烷基化的低级氨基烷基,环烷基,羟基烷基或哌啶基,或者R 1和R 2一起是含有4-7个碳原子的任选被氧或硫中断的二价亚乙基 或亚氨基,亚氨基亚氨基或芳基亚氨基或其药理学上相容的盐。 这些酯令人惊奇地可以通过在硫酸存在下酯化酸而不水解糖基来制备。 虽然酯具有一些活性,但它们可用于制备以标记的冠状动脉为特征的酰胺。

    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
    14.
    发明授权
    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
    (4) - 氧丙醇胺化合物和治疗组合物

    公开(公告)号:US4503067A

    公开(公告)日:1985-03-05

    申请号:US479921

    申请日:1983-04-04

    CPC分类号: C07D209/88 C07D317/64

    摘要: Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

    摘要翻译: 式(I)的羧基 - (4) - 氧丙醇胺化合物,其中R 1是氢,低级烷酰基或芳酰基; R2是氢,低级烷基或芳基烷基; R3是氢或低级烷基; R4是氢或低级烷基,或者当X是氧时,R4与R5一起可以代表-CH2-O-; X是价键,-CH 2 - ,氧或硫; Ar是单环或双环芳基或吡啶基; R5和R6分别选自氢,卤素,羟基,低级烷基,氨基羰基,低级烷氧基,芳烷氧基,低级烷硫基,低级烷基亚磺酰基或低级烷基磺酰基; R5和R6一起可以代表亚甲二氧基; 并且其与生理上可接受的酸的盐在治疗和预防循环和心脏疾病例如高血压和心绞痛方面是显着的。

    Nitropyrazole compounds and anti-microbial compositions
    19.
    发明授权
    Nitropyrazole compounds and anti-microbial compositions 失效
    硝基吡唑化合物和抗微生物组合物

    公开(公告)号:US4069330A

    公开(公告)日:1978-01-17

    申请号:US678588

    申请日:1976-04-20

    CPC分类号: H01B7/368 C07D231/16

    摘要: New nitropyrazole compounds of the formula ##STR1## wherein R.sub.1 is alkyl or hydroxyalkylR.sub.2 and R.sub.3, which may be the same or different, are alkyl orR.sub.2 and R.sub.3 together represent a 4- or 5-membered alkylene bridge which is optionally interrupted by an oxygen atom or by the grouping >N-R, in which R is an alkyl or hydroxyalkyl radical;And the pharmacologically compatible salts thereof, possess excellent anti-microbial action not only in vitro but also in vivo, especially systemically.

    摘要翻译: 其中R 1是烷基或羟基烷基的新的硝基吡唑化合物,其可以相同或不同,R 2和R 3可以是烷基或R 2和R 3一起代表4-或5-元亚烷基桥,其任选地被 氧原子或通过NR> NR,其中R是烷基或羟烷基; 和药物相容性好的药物,不仅仅是体内,而且在体内非常有效地进行非常有效的抗微生物作用。