Phenylalanine enamide derivatives
    1.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07786177B2

    公开(公告)日:2010-08-31

    申请号:US12415546

    申请日:2009-03-31

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了式(1)的苯丙氨酸烯酰胺衍生物:其中R1是基团Ar1 L2Ar2Alk-,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是链-CH 2 -CH(R) - , - CH = C(R) - 或其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine Enamide Derivatives
    2.
    发明申请
    Phenylalanine Enamide Derivatives 失效
    苯丙氨酸酰胺衍生物

    公开(公告)号:US20090105291A1

    公开(公告)日:2009-04-23

    申请号:US12327311

    申请日:2008-12-03

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了式(1)的苯丙氨酸烯酰胺衍生物:其中R1是基团Ar1 L2Ar2Alk-,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接体原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是链-CH 2 -CH(R) - , - CH-C(R) - 或其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine enamide derivatives
    3.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07501437B2

    公开(公告)日:2009-03-10

    申请号:US11692612

    申请日:2007-03-28

    IPC分类号: C07D471/04 A61K31/4375

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk—in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述式(1)的苯丙氨酸烯酰胺衍生物:其中R1是Ar1L2Ar2Alk基团,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是其中R是羧酸(-CO 2 H)或其衍生物或生物试剂的链; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine enamide derivatives
    5.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07122556B2

    公开(公告)日:2006-10-17

    申请号:US10947032

    申请日:2004-09-22

    IPC分类号: C07D471/04 A61K31/4375

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk— in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述了式(1)的苯丙氨酸烯酰胺衍生物:其中R 1是基团Ar 1,L 2,Ar 2, > Alk-其中:Ar 1是任选取代的芳族或杂芳族基团; L 2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或杂亚芳基; 和Alk是其中R是羧酸(-CO 2 H 2 H)或其衍生物或生物固体的链; X是-O-或-S-原子或-N(R 2)基团,其中:R x,R y和 R“可以相同或不同,各自为氢原子或任选的取代基; 或R z是如前所定义的原子或基团,并且R x和R y连接在一起形成任选取代的螺环连接的脂环族或 杂环脂族基团 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine enamide derivatives
    6.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07645770B2

    公开(公告)日:2010-01-12

    申请号:US12327311

    申请日:2008-12-03

    IPC分类号: C07D471/04 A61K31/4375

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述式(1)的苯丙氨酸烯酰胺衍生物:其中R1是Ar1L2Ar2Alk-基团,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是链-CH 2 -CH(R) - , - CH-C(R) - 或其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Phenylalanine enamide derivatives
    7.
    发明授权
    Phenylalanine enamide derivatives 失效
    苯丙氨酸烯酰胺衍生物

    公开(公告)号:US07531549B2

    公开(公告)日:2009-05-12

    申请号:US11533117

    申请日:2006-09-19

    摘要: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immuno or inflammatory disorders or disorders involving the inappropriate growth or migration of cells.

    摘要翻译: 描述式(1)的苯丙氨酸烯酰胺衍生物:其中R1是Ar1L2Ar2Alk-基团,其中:Ar1是任选取代的芳族或杂芳族基团; L2是共价键或连接体原子或基团; Ar 2是任选取代的亚芳基或亚杂芳基; 并且Alk是一条链<?in-line-formula description =“In-line Formulas”end =“lead”?> - CH2-CH(R) - ,-CH-C(R) - 或<? -formulae description =“In-line Formulas”end =“tail”?>其中R是羧酸(-CO 2 H)或其衍生物或生物试剂; X是-O-或-S-原子或-N(R 2) - 基团,其中:可以相同或不同的R x,R y和R z各自为氢原子或任选的取代基; 或R z是如先前定义的原子或基团,并且R x和R y连接在一起以形成任选取代的螺环连接的脂环族或杂环脂族基团; 及其盐,溶剂合物,水合物和N-氧化物。 该化合物能够抑制整联蛋白与其配体的结合,并且可用于预防和治疗涉及细胞不适当生长或迁移的免疫或炎性疾病或病症。

    Method for installing a ground stud in composite structures
    10.
    发明授权
    Method for installing a ground stud in composite structures 有权
    在复合结构中安装接地螺柱的方法

    公开(公告)号:US08918993B2

    公开(公告)日:2014-12-30

    申请号:US13012635

    申请日:2011-01-24

    摘要: Apparatus for bleeding electrical charge and methods for installing a ground stud in a composite structure. The apparatus includes a ground stud and a composite structure including a hole. In one embodiment the ground stud engages the hole in the composite structure in a transition fit. In another embodiment the ground stud is countersunk within the composite structure. Embodiments of the present methods include drilling a hole in the composite structure; inserting the ground stud into the hole such that the ground stud is in electrical contact with conductive fibers within the composite structure; securing the ground stud to the composite structure; and attaching a connective device to the ground stud such that the connective device is in electrical contact with the ground stud. In some embodiments the ground stud and the composite structure engage one another in a transition fit. In some embodiments the ground stud includes a pin, and a portion of the pin that contacts the composite structure is non-threaded. In some embodiments the ground stud is countersunk within the composite structure.

    摘要翻译: 用于电荷放电的装置以及将复合结构中的接地柱安装的方法。 该装置包括接地柱和包括孔的复合结构。 在一个实施例中,接地螺柱以过渡配合接合复合结构中的孔。 在另一个实施例中,接地螺柱在复合结构内是埋头的。 本方法的实施例包括在复合结构中钻孔; 将接地螺栓插入孔中,使得接地螺柱与复合结构内的导电纤维电接触; 将地脚固定在复合结构上; 以及将连接装置连接到接地柱,使得连接装置与接地柱螺纹电接触。 在一些实施例中,接地螺柱和复合结构在过渡拟合中彼此接合。 在一些实施例中,接地螺柱包括销,并且接触复合结构的销的一部分是非螺纹的。 在一些实施例中,接地螺柱在复合结构内是埋头的。