Process for preparing 1-deoxynojirimycin and N-derivatives thereof
    3.
    发明授权
    Process for preparing 1-deoxynojirimycin and N-derivatives thereof 失效
    1-脱氧野尻霉素及其N-衍生物的制备方法

    公开(公告)号:US4806650A

    公开(公告)日:1989-02-21

    申请号:US34466

    申请日:1987-04-02

    CPC分类号: C07D211/46 Y02P20/55

    摘要: A process for preparing a 1-deoxynojirimycin of the formula ##STR1## in which R is hydrogen, optionally substituted alkyl or aralkyl, which comprises converting D-glucose to an aminosorbitol ##STR2## protecting the amino group of the aminosorbitol with an alkalinically detachable group to form the protected compound of the formula ##STR3## in which X is an alkalinically detachable protective group, microbiologically oxidizing the protected compound to an oxidation product of the formula ##STR4## alkalinically splitting off the protective group X to form an aminosorbose of the formula ##STR5## and reducing the aminosorbose.

    摘要翻译: 制备式“IMAGE”的1-脱氧野尻霉素的方法,其中R是氢,任选取代的烷基或芳烷基,其包括将D-葡萄糖转化成用碱性可分离基保护氨基山梨糖醇的氨基的氨基异山梨醇 形成受保护的式“IMAGE”化合物,其中X是可碱性取代的保护基团,将保护的化合物微生物氧化成式VIII的氧化产物,碱性分解保护基团X以形成式 并且减少氨基吗啡。

    N-Substituted amino glycoside compounds, their production, and their use
as medicaments
    5.
    发明授权
    N-Substituted amino glycoside compounds, their production, and their use as medicaments 失效
    N-取代氨基糖苷化合物,其生产及其作为药物的用途

    公开(公告)号:US4199572A

    公开(公告)日:1980-04-22

    申请号:US881263

    申请日:1978-02-24

    CPC分类号: C07H15/234

    摘要: The invention relates to new derivatives, substituted on one or more nitrogen atoms, of 4,6-di-(amino-glycosyl)-1,3-diamino-cyclitols, which include the gentamycins, sisomicin, verdamycin, tobramycin, the kanamycins, the antibiotics G-418, 66-40 B, 66-40 D, JI-20 B, JI-20 B and G-52, and the 5-epi-, 5-epi-amino-5-deoxy and 5-epi-azido-5-deoxy derivatives of these antibiotics and the metamycins, and furthermore to processes for the preparation of these derivatives and to pharmaceutical compositions which contain the derivatives of the above mentioned 4,6-di-(amino-glycosyl)-1,3-diamino-cyclitols or their pharmaceutically acceptable acid addition salts, and to their use as antibacterial agents.

    摘要翻译: 本发明涉及由一个或多个氮原子取代的4,6-二 - (氨基 - 糖基)-1,3-二氨基 - 环醇的新衍生物,其包括:万古霉素,西索米星,维尔霉素,妥布霉素,卡那霉素, 抗生素G-418,66-40B,66-40D,JI-20B,JI-20B和G-52,以及5表位,5-表氨基-5-脱氧和5-epi - 氨基-5-脱氧衍生物,以及这些衍生物的制备方法,以及含有上述4,6-二(氨基 - 糖基)-1的衍生物的药物组合物, 3-二氨基 - 环状醇或其药学上可接受的酸加成盐,以及它们作为抗菌剂的用途。

    3-Amino-4,5-dihydroxypiperidines, process for their preparation and
their use
    6.
    发明授权
    3-Amino-4,5-dihydroxypiperidines, process for their preparation and their use 失效
    3-氨基-4,5-二羟基哌啶,其制备及其用途

    公开(公告)号:US4871747A

    公开(公告)日:1989-10-03

    申请号:US937645

    申请日:1986-12-03

    摘要: A 3-amino-4,5-dihydroxy-piperidine compound of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, alkyl having up to 8 carbon atoms, aralkyl having 7 to 14 carbon atoms, or represents a group of the formula ##STR2## R.sup.4 denotes straight-chain or branched alkyl having up to 8 carbon atoms, straight-chain or branched alkoxy having up to 8 carbon atoms, or aralkoxy having up to 10 carbon atoms, andR.sup.2 and R.sup.3 represent hydrogen or represent the group NHR.sup.5,R.sup.5 having the same meaning as R.sup.1 and being identical to or different from the latter,with the proviso that, in every case, one substituent of R.sup.2 or R.sup.3 represents hydrogen and the other substituent of R.sup.2 or R.sup.3 represents NHR.sup.5, and physiologically acceptable salts thereof. Such compound is useful to treat prediabetes, gastritis, constipation, caries, atherosclerosis, obesity, diabetes and hyperlipoproteinaemia.

    摘要翻译: 式(I)的3-氨基-4,5-二羟基 - 哌啶化合物其中R 1表示氢,具有至多8个碳原子的烷基,具有7-14个碳原子的芳烷基,或表示 式的基团R4表示具有至多8个碳原子的直链或支链烷基,具有至多8个碳原子的直链或支链烷氧基或具有至多10个碳原子的芳烷氧基,R2和R3表示氢 或代表NHR5基团,R 5具有与R 1相同的含义并且与后者相同或不同,条件是在每种情况下,R 2或R 3的一个取代基表示氢,R 2或R 3的其它取代基表示NHR 5 ,及其生理上可接受的盐。 这种化合物可用于治疗糖尿病前期,胃炎,便秘,龋齿,动脉粥样硬化,肥胖,糖尿病和高脂蛋白血症。