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35 条记录 (耗时 0.029 秒)

    Thienylalanine derivatives as inhibitors of cell adhesion
    6.
    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。

    Substituted purine derivatives as inhibitors of cell adhesion
    7.
    发明授权
    Substituted purine derivatives as inhibitors of cell adhesion 失效
    取代嘌呤衍生物作为细胞粘附的抑制剂

    公开(公告)号：US06747016B1

    公开(公告)日：2004-06-08

    申请号：US10030290

    申请日：2002-03-06

    申请人： Anuschirwan Peyman ,  Jochen Knolle ,  Thomas R Gadek ,  Jean-Francois Gourvest ,  Jean-Marie Ruxer

    发明人： Anuschirwan Peyman ,  Jochen Knolle ,  Thomas R Gadek ,  Jean-Francois Gourvest ,  Jean-Marie Ruxer

    IPC分类号： C07D47334

    CPC分类号： C07D473/34

    摘要： The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist 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 prolifertion 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B，D，E，G，X，Y，Z，R 1，R 2和s具有权利要求书中所示的含义， 盐及其前药。 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。

    HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof
    10.
    发明授权
    HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof 有权
    HSP90抑制性咔唑衍生物，含有该组合物的组合物及其应用

    公开(公告)号：US08309721B2

    公开(公告)日：2012-11-13

    申请号：US12881414

    申请日：2010-09-14

    申请人： Jean-Marie Ruxer ,  Victor Certal ,  Marcel Alasia ,  Luc Bertin ,  Herve Minoux ,  Patrick Mailliet ,  Frank Halley ,  Maria Mendez-Perez

    发明人： Jean-Marie Ruxer ,  Victor Certal ,  Marcel Alasia ,  Luc Bertin ,  Herve Minoux ,  Patrick Mailliet ,  Frank Halley ,  Maria Mendez-Perez

    IPC分类号： C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/14 ,  C07D471/04

    CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D451/04 ,  C07D453/00 ,  C07D471/04 ,  C07D493/08

    摘要： The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R′1; R is selected from the group comprising Formula (A′), (B), (C), (D), or (E), with R1 and/or R′1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.

    摘要翻译： 本发明涉及式（I）中的新物质：其中Het是任选被一个或多个基团R 1或R 11取代的杂环; R选自式（A'），（B），（C），（D）或（E）中的R 1和/或R 1选自H，卤素，CF 3，硝基，氰基， 烷基，羟基，巯基，氨基，烷基氨基，二烷基氨基，烷氧基，苯基氧基，烷基或羧基，它们被烷基，甲酰胺，CO-NH（烷基），CON（烷基）2，NH-CO-烷基， 磺酰胺，NH-SO 2 - 烷基，S（O）2 -NH烷基或S（O 2）-N（烷基）2基团; 所有这些基团任选被取代; W1，W2和W3独立地为CH或N; X为0，S，NR2，C（O），S（O）或S（0）2; Z是任选取代的H，Hal，-O-R 2或-NH-R 2，其中R 2是H，烷基，环烷基或杂环烷基; 并且这些物质都是用作药物的异构形式及其盐。