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40 条记录 (耗时 0.018 秒)

    Substituted azabicycloheptanes, the use thereof, pharmaceutical preparations that contain these compounds, and processes for the manufacture of these compounds
    31.
    发明授权
    Substituted azabicycloheptanes, the use thereof, pharmaceutical preparations that contain these compounds, and processes for the manufacture of these compounds 失效
    取代的氮杂双环庚烷，其用途，含有这些化合物的药物制剂，以及这些化合物的制造方法

    公开(公告)号：US4764640A

    公开(公告)日：1988-08-16

    申请号：US32656

    申请日：1987-04-01

    申请人： Alex Alder ,  Jaroslaw Stanek ,  Daniel Bellus

    发明人： Alex Alder ,  Jaroslaw Stanek ,  Daniel Bellus

    IPC分类号： A61K31/435 ,  A61P35/00 ,  A61P43/00 ,  C07D211/88 ,  C07D221/22 ,  C07D311/00 ,  C12N9/99 ,  C07C101/447

    CPC分类号： C07D221/22 ,  C07D311/00

    摘要： 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.

    摘要翻译： 式（Ⅰ）的1-苯基-3-氮杂双环[3.1.1] - 庚烷-2,4-二酮其中R 1表示氢或饱和或不饱和的脂族，脂环族，脂环族 - 脂族，脂族，芳族或 具有至多并包括18个，优选至多且包含12个碳原子的芳族 - 脂族烃基，R 2表示氢，低级烷基，磺基或酰基，R 3表示氢或低级烷基，R 4表示氢，低级烷基，苯基或苯基 被-N（R2）（R3）取代，并且这些化合物的盐具有有价值的药理学性质，作为芳香酶抑制剂是有效的，因此可用于治疗激素依赖性疾病，特别是乳腺癌。

    3,3,5-Trichloroglutaric acid imide
    33.
    发明授权
    3,3,5-Trichloroglutaric acid imide 失效
    3,3,5-三氯戊二酰亚胺

    公开(公告)号：US4360676A

    公开(公告)日：1982-11-23

    申请号：US209576

    申请日：1980-11-24

    申请人： Pierre Martin ,  Daniel Bellus

    发明人： Pierre Martin ,  Daniel Bellus

    IPC分类号： A01N43/40 ,  C07C67/00 ,  C07C253/00 ,  C07C255/27 ,  C07D211/88 ,  C07D213/61 ,  C07D211/38

    CPC分类号： C07C255/00 ,  C07D211/88 ,  C07D213/61

    摘要： 3,3,5-Trichloroglutaric acid imide can be produced either by reacting a trichloroacetic acid alkyl ester, in the presence of a catalyst, with acrylonitrile to the corresponding 2,2,4-trichloro-4-cyanobutyric acid alkyl ester, converting this into the amide, and cyclizing the 2,2,4-trichloro-4-cyano-butanecarboxylic acid amide, in an aqueous acid medium, to the 3,3,5-trichloroglutaric acid imide; or by reacting trichloroacetonitrile, in the presence of a catalyst, to 2,2,4-trichloro-4-cyanobutyronitrile, and cyclizing this, in an aqueous acid medium, to 3,3,5-trichloroglutaric acid imide. The catalyst used for the addition reactions can be for example copper(I) chloride or copper(II) oxide. 3,3,5-Trichloroglutaric acid imide can be converted, by treatment with a dehydrating chlorinating agent, such as POCl.sub.3, into the known 2,3,5,6-tetrachloropyridine, which for its part is used for producing various active substances, particularly insecticides, herbicides and fungicides.

    摘要翻译： 3,3,5-三氯戊二酸酰亚胺可以通过使三氯乙酸烷基酯在催化剂存在下与丙烯腈反应到相应的2,2,4-三氯-4-氰基丁酸烷基酯中，将其转化为 并将2,2,4-三氯-4-氰基 - 丁酰甲酰胺在含水酸性介质中环化为3,3,5-三氯戊二酸酰亚胺; 或在催化剂存在下，使三氯乙腈与2,2,4-三氯-4-氰基异丁腈反应，并将其在含水酸性介质中环化为3,3,5-三氯戊二酸酰亚胺。 用于加成反应的催化剂可以是例如氯化铜（I）或氧化铜（II）。 通过用脱氯氯化剂如POCl 3处理，可以将3,3,5-三氯戊二酸酰亚胺转化成已知的2,3,5,6-四氯吡啶，其用于制备各种活性物质， 特别是杀虫剂，除草剂和杀真菌剂。

    Squaric acid esters
    38.
    发明授权
    Squaric acid esters 失效
    方酸酯

    公开(公告)号：US4159387A

    公开(公告)日：1979-06-26

    申请号：US854287

    申请日：1977-11-23

    申请人： Daniel Bellus

    发明人： Daniel Bellus

    IPC分类号： C07C69/708 ,  C07C43/14 ,  C07C43/18 ,  C07C49/45 ,  C07C69/145

    CPC分类号： C07C49/753 ,  C07C45/45 ,  C07C45/54 ,  C07C45/673 ,  C07C69/708

    摘要： There are described new squaric acid esters, particularly mono-ortho esters, di-ortho esters, ortho ester anhydrides and ortho ester halides of squaric acid; a new process for producing these squaric acid esters; and a process for converting the squaric acid esters into squaric acid. It is possible by the new process to produce, with the use of readily obtainable starting products, the new squaric acid esters according to the invention in an economical manner and with good to very good yields; and the squaric acid esters can be converted under mild reaction conditions into squaric acid.

    摘要翻译： 描述了新的方酸酯，特别是单原酸酯，二原酸酯，原酸酯酸酐和方酸的原酸酯卤化物; 一种生产这些方酸酯的新工艺; 以及将方酸酯转变成方酸的方法。 通过新方法可以以经济的方式生产本发明的新型方酸酯，并且具有良好至非常好的收率; 并且方酸酯可以在温和的反应条件下转化成方酸。

    Process for the production of 2-amino-3-hydroxypyridines
    40.
    发明授权
    Process for the production of 2-amino-3-hydroxypyridines 失效
    2-氨基-3-羟基吡啶的制备方法

    公开(公告)号：US4061644A

    公开(公告)日：1977-12-06

    申请号：US697603

    申请日：1976-06-18

    申请人： Hans Greuter ,  Daniel Bellus

    发明人： Hans Greuter ,  Daniel Bellus

    IPC分类号： C07D213/73 ,  C07D213/74

    CPC分类号： C07D213/73

    摘要： Process for the production of 2-amino-3-hydroxypyridines of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently of one another represent hydrogen or an alkyl group having 1 to 4 carbon atoms, wherein a furan-2-carboxylic acid of formula ##STR2## wherein R.sub.1 and R.sub.2 have the meaning given above, or a derivative thereof, for example a quaternary ammonium salt, an ester, an amide, a halogenide, an amidine salt, an iminoether salt or the nitrile, is reacted at a temperature of between 100.degree. and 300.degree. C in a solvent containing amide groups, in the presence of an acid catalyst, with ammonia.

    摘要翻译： 用于制备式IMAGE的2-氨基-3-羟基吡啶的方法，其中R 1和R 2彼此独立地表示氢或具有1至4个碳原子的烷基，其中式 其中R1和R2具有上面给出的含义，或其衍生物，例如季铵盐，酯，酰胺，卤化物，脒盐，亚氨基醚盐或腈，在 在含有酰胺基的溶剂中，在酸催化剂存在下，与氨反应，在100℃和300℃之间。