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    NOVEL GUANIDINO DERIVATIVES AS INHIBITORS OF CELL ADHESION
    1.
    发明授权
    NOVEL GUANIDINO DERIVATIVES AS INHIBITORS OF CELL ADHESION 有权
    NEW胍衍生物作为ZELLADHÄSIONHEMMER

    公开(公告)号：EP1313737B1

    公开(公告)日：2009-06-03

    申请号：EP01956555.5

    申请日：2001-07-23

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

    发明人： PEYMAN, Anushirwan ,  WILL, David ,  GADEK, Thomas, R. ,  McDOWELL, Robert ,  GOURVEST, Jean-François ,  RUXER, Jean-Marie ,  KNOLLE, Jochen

    IPC分类号： C07D473/34 ,  C07D487/04 ,  A61K31/52 ,  A61P19/10

    CPC分类号： C07D473/00 ,  C07D487/04

    摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R?1, 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.

    NOVEL GUANIDINO DERIVATIVES AS INHIBITORS OF CELL ADHESION
    2.
    发明公开
    NOVEL GUANIDINO DERIVATIVES AS INHIBITORS OF CELL ADHESION 有权
    NEW胍衍生物作为ZELLADHÄSIONHEMMER

    公开(公告)号：EP1313737A1

    公开(公告)日：2003-05-28

    申请号：EP01956555.5

    申请日：2001-07-23

    申请人： Aventis Pharma Deutschland GmbH ,  Genentech Inc.

    发明人： PEYMAN, Anushirwan ,  WILL, David ,  GADEK, Thomas, R. ,  McDOWELL, Robert ,  GOURVEST, Jean-François ,  RUXER, Jean-Marie ,  KNOLLE, Jochen

    IPC分类号： C07D473/34 ,  C07D487/04 ,  A61K31/52 ,  A61P19/10

    CPC分类号： C07D473/00 ,  C07D487/04

    摘要： The present invention relates to acylguanidino derivatives of formula (I), in which R?1, 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.

    PLATELET AGGREGATION INHIBITORS HAVING HIGH SPECIFICITY FOR GP IIbIIIa
    8.
    发明公开
    PLATELET AGGREGATION INHIBITORS HAVING HIGH SPECIFICITY FOR GP IIbIIIa 失效
    GP IIbIIIa具有高特异性的血小板聚集抑制剂

    公开(公告)号：EP0578728A1

    公开(公告)日：1994-01-19

    申请号：EP92909119.0

    申请日：1992-04-03

    申请人： GENENTECH, INC.

    发明人： BURNIER, John, P. ,  GADEK, Thomas ,  McDOWELL, Robert

    IPC分类号： A61K38 ,  A61P7 ,  C07K7 ,  C07K14

    CPC分类号： C07K14/78 ,  A61K38/00 ,  C07K7/02 ,  C07K14/75 ,  Y10S930/27

    摘要： On décrit un peptide contenant les séquences de reconnaisance tripeptidique RGD ou KGD dans un cycle et un groupe exocyclique portant une charge positive. Le composé se présente sous une forme thérapeutique afin d'être administré à un mammifère et fait preuve d'une spécificité et d'une efficacité élevées lorsqu'il est utilisé comme inhibiteur d'agrégation plaquettaire, sans produire d'effets secondaires indésirables.

    摘要翻译： 公开了在一个循环和带正电荷的环外基团中含有RGD或KGD三肽识别序列的肽。 该化合物为用于给予哺乳动物的治疗形式，并且当用作血小板聚集抑制剂时表现出高特异性和功效而不产生不希望的副作用。