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    AZA-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
    77.
    发明授权
    AZA-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity 失效
    AZA-吲哚和具有鞘氨醇-1-磷酸（S1P）受体拮抗剂生物活性的相关化合物

    公开(公告)号：US08536339B2

    公开(公告)日：2013-09-17

    申请号：US13195121

    申请日：2011-08-01

    申请人： Haiqing Yuan ,  Richard L. Beard

    发明人： Haiqing Yuan ,  Richard L. Beard

    IPC分类号： C07D491/02 ,  C07D498/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(═O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X═O, NH, —C(═O)— or —N═CH—; and Each L is independently alkylene and carbonyl. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

    摘要翻译： 本发明提供了具有下式的本文公开的化合物：其中n为1或2; m为0或1; p为0,1或2; R1是芳基，杂芳基或烷基; R2是C1-6烃基，烷基酰基或羟基烷基; R3是芳基，杂芳基或烷基; R4是H，OH，-O-（C1-6烷基），-NH-（C1-6烷基）或氧化物; R5是H，卤素，C1-6烷基，O-（C1-6烷基），芳基，杂芳基，-C（= O）（C1-6烷基），取代或未取代的恶唑啉-2-基; X = O，NH，-C（= O） - 或-N = CH-; 并且每个L独立地是亚烷基和羰基。 还公开了与之相关的治疗方法，组合物和药物。

    AZA-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
    79.
    发明授权
    AZA-indoles and related compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity 失效
    AZA-吲哚和具有鞘氨醇-1-磷酸（S1P）受体拮抗剂生物活性的相关化合物

    公开(公告)号：US08263767B2

    公开(公告)日：2012-09-11

    申请号：US13195130

    申请日：2011-08-01

    申请人： Haiqing Yuan ,  Richard L. Beard

    发明人： Haiqing Yuan ,  Richard L. Beard

    IPC分类号： C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention provides compounds are disclosed herein having the formula: Wherein n is 1 or 2; m is 0 or 1; R1 is aryl, heteroaryl or alkyl; R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, —O—(C1-6 alkyl), —NH—(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O—(C1-6 alkyl), aryl, heteroaryl, —C(═O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X=O, NH, —C(═O)— or —N═CH—; and Each L is independently alkylene and carbonyl.

    摘要翻译： 本发明提供了具有下式的本文公开的化合物：其中n为1或2; m为0或1; R1是芳基，杂芳基或烷基; R2是C1-6烃基，烷基酰基或羟基烷基; R3是芳基，杂芳基或烷基; R4是H，OH，-O-（C1-6烷基），-NH-（C1-6烷基）或氧化物; R5是H，卤素，C1-6烷基，O-（C1-6烷基），芳基，杂芳基，-C（= O）（C1-6烷基），取代或未取代的恶唑啉-2-基; X = O，NH，-C（= O） - 或-N = CH-; 并且每个L独立地是亚烷基和羰基。