利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

39 条记录 (耗时 0.027 秒)

    Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them
    24.
    发明授权
    Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them 失效
    萘啶衍生物，其制备方法，用途和包含它们的药物组合物

    公开(公告)号：US06743800B1

    公开(公告)日：2004-06-01

    申请号：US10030301

    申请日：2002-03-20

    申请人： Anuschirvan Peyman ,  Karl-Heinz Scheunemann ,  Thomas R Gadek ,  Jean-Francois Gourvest ,  Jean-Marie Ruxer

    发明人： Anuschirvan Peyman ,  Karl-Heinz Scheunemann ,  Thomas R Gadek ,  Jean-Francois Gourvest ,  Jean-Marie Ruxer

    IPC分类号： A61K3152

    CPC分类号： C07D473/34

    摘要： The present invention relates to compounds of formula (1), in which H, G, Z, X, Y, r, s and t have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (1) are valuable, pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (1), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（1）化合物，其中H，G，Z，X，Y，r，s和t具有权利要求书中所示的含义，其生理上可耐受的盐及其前药。 式（1）的化合物是有价值的药理活性化合物。 它们是玻连蛋白受体拮抗剂和细胞粘附抑制剂，并且适用于治疗和预防基于玻连蛋白受体及其配体在细胞 - 细胞或细胞 - 基质相互作用过程中的相互作用的疾病，或可被预防，缓解或 通过影响这种相互作用来治愈。 例如，它们可以用于抑制破骨细胞的骨吸收，从而用于治疗和预防骨质疏松症，或用于抑制血管平滑肌肉细胞的不期望的血管生成或增殖。 本发明还涉及制备式（1）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

    Steroids
    27.
    发明授权
    Steroids 失效
    STEROIDS

    公开(公告)号：US5081114A

    公开(公告)日：1992-01-14

    申请号：US633288

    申请日：1990-12-24

    申请人： Jean-Francois Gourvest ,  Dominique Lesuisse

    发明人： Jean-Francois Gourvest ,  Dominique Lesuisse

    IPC分类号： A61K31/565 ,  A61P35/00 ,  A61P43/00 ,  C07J1/00 ,  C07J41/00

    CPC分类号： C07J1/0011 ,  C07J41/0038

    摘要： A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, ##STR2## alkyl and alkoxy of 1 to 12 carbon atoms, aryl and aryloxy of 6 to 12 carbon atoms and aralkyl and aralkoxy of 7 to 12 carbon atoms, R.sub.1 and R.sub.2 are individually alkyl of 1 to 6 carbon atoms or taken together with the nitrogen atom to which they are attached form a 5 or 6 membered heterocycle optionally containing a second heteroatom of --S--, --O-- or --N--, R.sub.A is selected from the group consisting of hydrogen, halogen, --OH, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, --NH.sub.2, mono- and dialkylamino of 1 to 6 alkyl carbon atoms, carbamoyl and alkoxy carbamoyl of up to 7 carbon atoms, X is --O-- or ##STR3## R.sub.17 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of 1 to 12 carbon atoms and the dotted lines at 1(2) and 6(7) indicates an optional double bond, with the proviso that R.sub.A is not hydrogen when R is alkoxy, aryloxy or aralkoxy having aromatic specific activity useful in treating cancers.

    摘要翻译： 式I的化合物，其中R选自氢，1〜12个碳原子的烷基和烷氧基，6-12个碳原子的芳基和芳氧基以及7-12个碳原子的芳烷基和芳烷氧基 碳原子，R 1和R 2分别是1至6个碳原子的烷基或与它们所连接的氮原子一起形成5或6元杂环，任选地含有-S + 13，-O-或 - N-，RA选自氢，卤素，-OH，烷基，烷硫基和1至6个碳原子的烷氧基，-NH 2，1至6个烷基碳原子的一烷基氨基和二烷基氨基，氨基甲酰基和烷氧基氨基甲酰基 最多7个碳原子，X是-O-或者R 17选自氢，1至12个碳原子的烷基和1至12个碳原子的有机羧酸的酰基，虚线在 1（2）和6（7）表示任选的双键，条件是当R是烷氧基时，RA不是氢，芳基 具有芳族比活性的氧或芳烷氧基可用于治疗癌症。