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。

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。

公开(公告)号：US07259159B2

公开(公告)日：2007-08-21

申请号：US10343173

申请日：2001-07-23

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

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

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D473/16 ,  C07D473/24 ,  C07D473/28 ,  C07D473/32 ,  C07D473/34 ,  C07D473/36 ,  C07D473/40 ,  A61K31/437 ,  A61K31/519

CPC分类号： C07D473/00 ,  C07D487/04

摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R1, R2, R3, A, B, X, Y and n have the meanings indicated in claim 1, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness 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 treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them

摘要翻译： 本发明涉及式（I）的酰基胍基衍生物，其中R 1，R 2，R 3，A，B，X ，Y和n具有权利要求1所述的含义，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物活性化合物。 它们是玻连蛋白受体拮抗剂和破骨细胞的细胞粘附和骨吸收的抑制剂。 这使得它们适合于例如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的治疗和预防，或通过影响这些相互作用可以预防，缓解或治愈 。 例如，它们可以用于治疗和预防骨质疏松症，或用于抑制血管平滑肌细胞的不期望的血管生成或增殖。 本发明还涉及制备式（I）化合物的方法，其用途，特别是作为药物活性成分，以及包含它们的药物组合物