Insulin derivatives, process for their preparation, their use and a
pharmaceutical preparation containing them
    1.
    发明授权
    Insulin derivatives, process for their preparation, their use and a pharmaceutical preparation containing them 失效
    胰岛素衍生物,其制备方法,其使用和含有它们的药物制剂

    公开(公告)号:US5149716A

    公开(公告)日:1992-09-22

    申请号:US603835

    申请日:1990-10-26

    CPC分类号: C07K14/62

    摘要: The invention relates to insulin derivatives of the formula III ##STR1## in which R.sup.30 and R.sup.31 together are OH, or R.sup.30 is a radical of a neutral, genetically encodable L-amino acid and R.sup.31 is OH or a physiologically acceptable organic group of basic character having up to 50 carbon atoms, whose synthesis involves 0 to 3 .alpha.-amino acids and whose optional terminal carboxyl function can be present free, as an ester function, as an amide function, as a lactone or reduced to CH.sub.2 OH, and R.sup.A-1 is a radical of a genetically encodable L-amino acid, and physiologically acceptable salts of said insulin derivative of the formula III.

    摘要翻译: 本发明涉及式III(III)的胰岛素衍生物,其中R30和R31一起是OH,或R30是中性的,可遗传编码的L-氨基酸的基团,R31是OH或生理上可接受的有机基团 具有多至50个碳原子的基本特征,其合成涉及0至3个α-氨基酸,并且其任选的末端羧基官能团可作为酯官能团作为酰胺官能团作为内酯,作为内酯或还原成CH2OH,以及 RA-1是基因编码的L-氨基酸的基团,以及所述式III的胰岛素衍生物的生理上可接受的盐。

    Polycyclic thiazol-2-ylidene amines, processes for their preparation and their use as medicaments
    5.
    发明授权
    Polycyclic thiazol-2-ylidene amines, processes for their preparation and their use as medicaments 有权
    多环噻唑-2-亚基胺,其制备方法及其用作药物

    公开(公告)号:US06288093B1

    公开(公告)日:2001-09-11

    申请号:US09697151

    申请日:2000-10-27

    IPC分类号: A61K31429

    CPC分类号: C07D277/60 C07D513/04

    摘要: The invention relates to polycyclic thiazolidin-2-ylidene amines and their physiologically tolerated salts and physiologically functional derivatives. Polycyclic thiazolidin-2-ylidene amines of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example as anorectics and in the treatment or prophylaxis of type II diabetes.

    摘要翻译: 本发明涉及多环噻唑烷-2-亚基胺及其生理上耐受的盐和生理功能衍生物。式I的多环噻唑烷-2-亚基胺,其中基团具有所述含义,以及它们的生理学耐受的盐和方法 描述了它们的准备。 这些化合物是适合的,例如作为抗精神病药和治疗或预防II型糖尿病。

    Use of pyrimidine derivatives for the prevention of cancer, on their own
or in combination with other therapeutic measures
    6.
    发明授权
    Use of pyrimidine derivatives for the prevention of cancer, on their own or in combination with other therapeutic measures 失效
    使用嘧啶衍生物自身或与其他治疗措施相结合预防癌症

    公开(公告)号:US6156755A

    公开(公告)日:2000-12-05

    申请号:US038156

    申请日:1998-03-11

    申请人: Karl Geisen

    发明人: Karl Geisen

    CPC分类号: A61K31/506

    摘要: Use of pyrimidine derivatives for the prevention of cancer, on their own or in combination with other therapeutic measures.The present invention is concerned with the use of pyrimidine derivatives as agents for the prevention of carcinomatous disorders.The pyrimidine derivatives used are active compounds of the formula I ##STR1## in which R.sup.1 to R.sup.7 have the meaning indicated, and their physiologically tolerable salts.

    摘要翻译: 使用嘧啶衍生物自身或与其他治疗措施相结合预防癌症。 本发明涉及嘧啶衍生物作为预防癌症的药物的用途。 所用的嘧啶衍生物是其中R 1至R 7具有所述含义的式I的活性化合物及其生理上可耐受的盐。

    Certain nicotinamido-n-benzoic acid derivatives
    8.
    发明授权
    Certain nicotinamido-n-benzoic acid derivatives 失效
    某些烟酰氨基 - 正苯甲酸衍生物

    公开(公告)号:US4181658A

    公开(公告)日:1980-01-01

    申请号:US878602

    申请日:1978-02-16

    摘要: Benzoic acid derivatives of the formula ##STR1## wherein T is hydrogen or halogen, W is a carboxyl group, an ester or salt thereof; X is ##STR2## wherein R.sub.1 is alkyl having from 2 to 8 carbon atoms, aralkyl or phenyl, cycloalkyl, cycloalkylalkyl or alkylcycloalkyl; R.sub.2 is hydrogen or halogen, R.sub.3 is alkyl having from 5 to 8 carbon atoms, aralkyl or phenyl, or cycloalkyl having from 5 to 8 carbon atoms; R.sub.4 is hydrogen or alkyl; Y is a single chemical bond or a hydrocarbon chain having from 1 to 3 carbon atoms; and Z is hydrogen, halogen, alkyl, alkoxy, alkoxyalkoxy or alkenyloxy, have a blood sugar lowering effect and can be used for the treatment of Diabetes mellitus.

    摘要翻译: 其中T为氢或卤素,W为羧基,其酯或其盐的式IMAMA的苯甲酸衍生物; X是其中R1是具有2至8个碳原子的烷基,芳烷基或苯基,环烷基,环烷基烷基或烷基环烷基; R2是氢或卤素,R3是具有5-8个碳原子的烷基,芳烷基或苯基,或具有5-8个碳原子的环烷基; R4是氢或烷基; Y是单个化学键或具有1至3个碳原子的烃链; Z为氢,卤素,烷基,烷氧基,烷氧基烷氧基或烯氧基,具有降血糖作用,可用于治疗糖尿病。

    Insulin analogs with enhanced zinc binding
    9.
    发明授权
    Insulin analogs with enhanced zinc binding 有权
    胰岛素类似物具有增强的锌结合

    公开(公告)号:US06686177B1

    公开(公告)日:2004-02-03

    申请号:US09701968

    申请日:2001-05-14

    IPC分类号: A61K3828

    摘要: The invention relates to insulin analogs exhibiting enhanced zinc binding capacity and to stable zinc complexes thereof having a retarded activity in comparison with human insulin. The invention further relates to a method for the production of said insulin analogs and to their use, particularly in pharmaceutical preparations for therapy of type I and type II diabetes mellitus.

    摘要翻译: 本发明涉及具有增强的锌结合能力的胰岛素类似物和与人胰岛素相比具有延迟活性的稳定的锌络合物。 本发明还涉及生产所述胰岛素类似物的方法及其用途,特别是用于治疗I型和II型糖尿病的药物制剂。