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11 条记录 (耗时 0.015 秒)

    Thienylalanine derivatives as inhibitors of cell adhesion
    1.
    发明授权
    Thienylalanine derivatives as inhibitors of cell adhesion 有权
    噻吩丙氨酸衍生物作为细胞粘附的抑制剂

    公开(公告)号：US06762190B2

    公开(公告)日：2004-07-13

    申请号：US10169612

    申请日：2002-09-23

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

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

    IPC分类号： C07D40912

    CPC分类号： C07D409/12

    摘要： The present invention relates to compounds of formula (I), in which A, B, X, Y, R1, R2, R3 and n have the meanings indicated in the claims. The compounds of formula (I) 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 (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中A，B，X，Y，R 1，R 2，R 3和n具有权利要求中所示的含义。 式（I）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（I）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。

    Guanidine derivatives as inhibitors of cell adhesion
    4.
    发明授权
    Guanidine derivatives as inhibitors of cell adhesion 有权
    胍衍生物作为细胞粘附抑制剂

    公开(公告)号：US06340679B1

    公开(公告)日：2002-01-22

    申请号：US09502577

    申请日：2000-02-11

    申请人： Anuschirwan Peyman ,  Jochen Knolle ,  Karl-Heinz Scheunemann ,  David William Will ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas R. Gadek ,  Sarah Catherine Bodary

    发明人： Anuschirwan Peyman ,  Jochen Knolle ,  Karl-Heinz Scheunemann ,  David William Will ,  Denis Carniato ,  Jean-Francois Gourvest ,  Thomas R. Gadek ,  Sarah Catherine Bodary

    IPC分类号： C07D23916

    CPC分类号： C07D409/12 ,  C07D239/16

    摘要： The present invention relates to acylguanidine derivatives of the formula I in which R1, R2, R4, Ar, X and n have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion. They inhibit, for example, bone resorption by osteoclasts and are suitable for the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example osteoporosis. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceutical preparations, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式Iin的酰基胍衍生物，其中R 1，R 2，R 4，Ar，X和n具有权利要求中所示的含义，其生理上可耐受的盐及其前药。 式I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。 它们抑制例如破骨细胞的骨吸收，并且适用于治疗和预防至少部分由不期望的骨吸收程度引起的疾病，例如骨质疏松症。 本发明还涉及制备式I化合物的方法，其用途，特别是作为药物制剂中的活性成分，以及包含它们的药物制剂。

    Naphthyridine derivatives, processes for their preparation, their use and pharmaceutical compositions comprising them
    10.
    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。