公开(公告)号：EP1065208A1

公开(公告)日：2001-01-03

申请号：EP99112637.6

申请日：1999-07-02

申请人： Aventis Pharma Deutschland GmbH ,  Genentech, Inc.

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

IPC分类号： C07D473/34 ,  A61K31/52

CPC分类号： C07D473/34

摘要： The present invention relates to compounds of the formula I,
in which B, D, E, G, X, Y, Z, R 1 , R 2 and s 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 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 the 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， 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，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，特别是作为药物中的活性成分，以及包含它们的药物组合物。

公开(公告)号：EP0797997B1

公开(公告)日：2005-06-15

申请号：EP97104345.0

申请日：1997-03-14

申请人： Aventis Pharma Deutschland GmbH

发明人： Breipohl, Gerhard, Dr. ,  Henke, Stephan, Dr. ,  Knolle, Jochen Dr. ,  Wirth Klausm Dr. ,  Hropot, Max, Dr. ,  Bickel, Martin, Dr.

IPC分类号： A61K38/08 ,  A61K38/04 ,  A61P1/16

CPC分类号： A61K38/043 ,  Y10S514/893

公开(公告)号：EP0933367A1

公开(公告)日：1999-08-04

申请号：EP97122520.6

申请日：1997-12-19

申请人： Hoechst Marion Roussel Deutschland GmbH ,  Genentech, Inc.

发明人： Peyman, Anuschirwan Dr. ,  Knolle, Jochen Dr. ,  Breipohl, Gerhard Dr. ,  Scheunemann, Karl-Heinz Dr. ,  Carniato, Denis Dr. ,  Gourvest, Jean-François Dr. ,  Gadek, Thomas R. Dr. ,  McDowell, Robert Dr. ,  Bodary, Sarah Catherine Dr. ,  Cuthbertson, Robert Andrew Dr. ,  Ferrara, Napoleane Dr.

IPC分类号： C07D239/16 ,  C07C279/20 ,  A61K31/505

CPC分类号： C07C279/20 ,  C07D239/16

摘要： The present invention relates to acylguanidine derivatives of the formula I
in which R 1 , R 2 , R 4 , R 5 , R 6 , A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of the formula I are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. 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 preparations comprising them.

摘要翻译： 本发明涉及式I 的酰基胍衍生物，其中R 1，R 2，R 4，R 5，R 6，A，m和n具有所指定的含义 在专利权利要求中，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成分。 它们是玻连蛋白受体拮抗剂和破骨细胞骨吸收抑制剂，例如适用于治疗或预防由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，特别是作为药物活性成分，以及包含它们的药物制剂。