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    &bgr;-phenylalanine derivatives as integrin antagonists
    7.
    发明授权
    &bgr;-phenylalanine derivatives as integrin antagonists 失效
    β-苯丙氨酸衍生物作为整联蛋白拮抗剂

    公开(公告)号：US06589972B2

    公开(公告)日：2003-07-08

    申请号：US09867835

    申请日：2001-05-30

    申请人： Andreas Schoop ,  Gerhard Mueller ,  Ulf Brueggemeier ,  Delf Schmidt ,  Beatrix Stelte-Ludwig ,  Joerg Keldenich

    发明人： Andreas Schoop ,  Gerhard Mueller ,  Ulf Brueggemeier ,  Delf Schmidt ,  Beatrix Stelte-Ludwig ,  Joerg Keldenich

    IPC分类号： A01N4350

    CPC分类号： C07C311/19 ,  C07C311/47

    摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4′, —COOR4″, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.

    摘要翻译： 本发明涉及通式（1）的化合物，其中R 4是-SO 2 R 4'，-COOR 4“，-COR 4'， - CONR 4'2或-CSNR 4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。 本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途 具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。

    &bgr;-phenylalanine derivatives as integrin antagonists
    8.
    发明授权
    &bgr;-phenylalanine derivatives as integrin antagonists 失效
    β-苯丙氨酸衍生物作为整联蛋白拮抗剂

    公开(公告)号：US06291503B1

    公开(公告)日：2001-09-18

    申请号：US09232738

    申请日：1999-01-15

    申请人： Andreas Schoop ,  Gerhard Mueller ,  Ulf Brueggemeier ,  Delf Schmidt ,  Beatrix Stelte-Ludwig ,  Joerg Keldenich

    发明人： Andreas Schoop ,  Gerhard Mueller ,  Ulf Brueggemeier ,  Delf Schmidt ,  Beatrix Stelte-Ludwig ,  Joerg Keldenich

    IPC分类号： A01N4356

    CPC分类号： C07C311/19 ,  C07C311/47

    摘要： The present invention relates to compounds of the general formula (1) wherein R4 is —SO2R4, —COOR4′, —COR4′, —CONR4′2 or —CSNR4′2; R4′ is hydrogen, a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; R4″ is a substituted or unsubstituted alkyl or cycloalkyl residue, a substituted or unsubstituted aryl residue or a saturated or unsaturated, optionally substituted heterocyclic residue; L is a sulphonamide, amide, ether, ester, keto, urea, thioether, sulphoxide or sulphone unit optionally extended by one or two methylene groups; and X is N, O or S; and their physiologically acceptable salts and stereoisomers. The present invention furthermore relates to a process for the preparation of the compounds of the formula (1), a pharmaceutical composition containing at least one of these compounds, and the use of compounds of the formula (1) for the production of a pharmaceutical composition having integrin-antagonistic action and in particular for the therapy and prophylaxis of cancer, osteolytic diseases such as osteoporosis, arteriosclerosis, restenosis and ophthalmic disorders.

    摘要翻译： 本发明涉及通式（1）的化合物，其中R4是-SO2R4，-COOR4'，-COR4'，-CONR4'2或-CSNR4'2; R 4'是氢，取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; R 4“是取代或未取代的烷基或环烷基残基，取代或未取代的芳基残基或饱和或不饱和的任选取代的杂环残基; L是任选被一个或两个亚甲基延伸的磺酰胺，酰胺，醚，酯，酮，脲，硫醚，亚砜或砜单元; X为N，O或S; 及其生理上可接受的盐和立体异构体。 本发明还涉及制备式（1）化合物的方法，含有这些化合物中的至少一种的药物组合物，以及式（1）化合物在制备药物组合物中的用途 具有整合素拮抗作用，特别是用于治疗和预防癌症，溶骨性疾病如骨质疏松症，动脉硬化，再狭窄和眼科疾病。