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305 条记录 (耗时 0.023 秒)

    6- and 6,6-Disubstituted-2-substituted-oxapen-2-em-3-carboxylic acids
    43.
    发明授权
    6- and 6,6-Disubstituted-2-substituted-oxapen-2-em-3-carboxylic acids 失效
    6-和6,6-二取代-2-取代 - 氧杂-2-烯-3-羧酸

    公开(公告)号：US4293555A

    公开(公告)日：1981-10-06

    申请号：US83721

    申请日：1979-10-10

    申请人： Burton G. Christensen ,  Frank P. DiNinno

    发明人： Burton G. Christensen ,  Frank P. DiNinno

    IPC分类号： C07D205/08 ,  C07D213/70 ,  C07D249/02 ,  C07D257/04 ,  C07D307/64 ,  C07D333/34 ,  C07D409/06 ,  C07D498/04 ,  C07D499/00 ,  C07D503/00 ,  A61K31/42

    CPC分类号： C07D213/70 ,  C07C327/00 ,  C07D205/08 ,  C07D249/02 ,  C07D257/04 ,  C07D307/64 ,  C07D333/34 ,  C07D499/00 ,  C07D503/00

    摘要： Disclosed are 6- and 6,6-disubstituted-2-substituted-oxapen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, alkoxyl, aralkyl, aryl, heterocyclyl and heterocyclylalkyl; R is selected from hydrogen, --OR, --SR, --NR.sub.2, alkyl, aryl, aralkyl, heterocyclyl, or heterocyclylalkyl. Such compounds and their pharmaceutically acceptable salt, and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

    摘要翻译： 公开了以下结构的6-和6,6-二取代-2-取代 - 氧杂-2-烯-3-羧酸：其中：R 1和R 2独立地选自氢，烷基，烷氧基，芳烷基， 芳基，杂环基和杂环基烷基; R选自氢，-OR，-SR，-NR 2，烷基，芳基，芳烷基，杂环基或杂环基烷基。 这些化合物及其药学上可接受的盐和酯衍生物可用作抗生素。 还公开了制备这些化合物的方法，包含这些化合物的药物组合物和治疗方法，包括当指出抗生素作用时施用这些化合物和组合物。

    Process for preparing 2-acyl-5-substituted thiatetrahydrofuran-4-ones
    44.
    发明授权
    Process for preparing 2-acyl-5-substituted thiatetrahydrofuran-4-ones 失效
    2-酰基-5-取代的四氢呋喃-4-酮的制备方法

    公开(公告)号：US4138413A

    公开(公告)日：1979-02-06

    申请号：US887631

    申请日：1978-03-17

    申请人： Braja D. Mookherjee ,  William J. Evers ,  Alfred E. Goossens

    发明人： Braja D. Mookherjee ,  William J. Evers ,  Alfred E. Goossens

    IPC分类号： A24B15/40 ,  C07D307/32 ,  C07D307/64 ,  C11B9/00

    CPC分类号： C07D307/32 ,  A24B15/406 ,  C07D307/64 ,  C11B9/0076

    摘要： Described are 2-acyl-5-substituted thiatetrahydrofuran-4-ones having the generic structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.1 ' and R.sub.2 ' are the same or different and each represents hydrogen or methyl and wherein R.sub.3 represents one of C.sub.1 -C.sub.9 alkyl, benzyl, phenyl, substituted or unsubstituted allyl having the structure: ##STR2## substituted or unsubstituted 3-furyl having the structure: ##STR3## (wherein R.sub.4 and R.sub.8 are the same or different and each represents hydrogen or methyl) hydroxy alkyl, oxoalkyl, hydroxycycloalkyl or oxocycloalkyl having the structure: ##STR4## (wherein R.sub.5 and R.sub.6, taken separately, represent hydrogen or C.sub.1 -C.sub.3 alkyl or R.sub.5 and R.sub.6, taken together, complete a cycloalkyl group and wherein Q is one of the moieties: ##STR5## prepared according to the process of dimerizing one or more alpha, beta-alkane dione(s) to form one or more alpha, beta-alkane dione dimer(s) having the structure: ##STR6## and reacting the said alkane dione dimer(s) in acidic medium and in the presence of a solvent with a mercaptan, having the structure:R.sub.3 SHthe 2-acyl-5-substituted thiatetrahydrofuran-4-ones of our invention have organoleptic properties which make them useful for augmenting or enhancing the aroma or flavor of foodstuffs, tobaccos and the aroma of perfumes and perfumed articles.

    摘要翻译： 描述了具有以下通用结构的2-酰基-5-取代的硫代四氢呋喃-4-酮：其中R 1，R 2，R 1'和R 2'相同或不同，各自表示氢或甲基，并且其中R 3表示C1 -C9烷基，苄基，苯基，具有以下结构的取代或未取代的烯丙基：具有以下结构的取代或未取代的3-呋喃基：其中R 4和R 8相同或不同，各自表示氢或甲基）羟基 烷基，氧代烷基，羟基环烷基或氧代环烷基，其结构为：其中R 5和R 6分别代表氢或C 1 -C 3烷基或R 5和R 6一起形成环烷基，其中Q是部分之一 ：根据使一种或多种α，β-烷烃二酮二聚形成一种或多种具有以下结构的α，β-烷烃二酮二聚体的方法制备：＆lt; IMAGE＆gt;并使所述烷烃 二酸二聚体在酸性介质中并在溶剂存在下进行 具有硫醇，具有以下结构：

    Aminoalkyl furan derivatives
    45.
    发明授权
    Aminoalkyl furan derivatives 失效
    氨基烷基呋喃衍生物

    公开(公告)号：US4128658A

    公开(公告)日：1978-12-05

    申请号：US818762

    申请日：1977-07-25

    申请人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    发明人： Barry J. Price ,  John W. Clitherow ,  John Bradshaw

    IPC分类号： C07C323/25 ,  A61K31/34 ,  A61K31/341 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07D207/08 ,  C07D233/64 ,  C07D275/02 ,  C07D275/03 ,  C07D307/38 ,  C07D307/52 ,  C07D307/54 ,  C07D307/64 ,  C07D405/06 ,  C07D405/12 ,  C07D413/14 ,  A01N9/12 ,  A01N9/20

    CPC分类号： C07D275/03 ,  A61K31/34 ,  C07D207/08 ,  C07D307/38 ,  C07D307/52 ,  C07D307/64

    摘要： Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O or S;Y represents .dbd. S, .dbd. O, .dbd. NR.sub.5 or .dbd. CHR.sub.6 ;Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms;R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl;R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl;M is an integer from 2 to 4; andN is 1 or 2; or when X .dbd. S, or --CH.sub.2 --, n is zero, 1 or 2.These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.

    摘要翻译： 通式I的化合物及其生理上可接受的盐和N-氧化物和水合物，其中可以相同或不同的R 1和R 2表示氢，低级烷基，环烷基，低级烯基，芳烷基或 被氧原子间隔的低级烷基或其中R 4表示氢或低级烷基或R 1和R 2的基团可以与它们所连接的氮原子一起形成杂环，该杂环可以含有选自O 且R 3为氢，低级烷基，低级烯基或烷氧基烷基; X是-CH 2 - ，O或S; Y表示= S，= O，= NR5或= CHR6; Alk表示1〜6个碳原子的直链或支链亚烷基链; R5是H，硝基，氰基，低级烷基，芳基，烷基磺酰基或芳基磺酰基; R6表示硝基，芳基磺酰基或烷基磺酰基; M是从2到4的整数; 和N是1或2; 或当X = S或-CH 2 - 时，n为0,1或2。