Trans cyclopentanyl purine analogs useful as immunosuppressants
    12.
    发明授权
    Trans cyclopentanyl purine analogs useful as immunosuppressants 失效
    用作免疫抑制剂的反戊环嘌呤类似物

    公开(公告)号:US5723466A

    公开(公告)日:1998-03-03

    申请号:US485263

    申请日:1995-06-07

    CPC分类号: C07D473/00 C07D487/04

    摘要: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y.sub.3, Y.sub.5 and Y.sub.9 are each nitrogen and Y.sub.7 and Y.sub.8 are a CH group, R is a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl, Q is NH.sub.2, halogen or hydrogen, Z is hydrogen, halogen, or NH.sub.2 ; or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

    摘要翻译: 本发明涉及式(1)的环戊烷基嘌呤类似物(1),其中环戊烷基环上3位的取代基相对于双环取代基为反式构型,Y 3,Y 5和Y 9分别为 氮和Y7和Y8是CH基,R是C1-C7烷基酰基或芳基酰基,Q是NH2,卤素或氢,Z是氢,卤素或NH2; 或其药学上可接受的盐,以及它们作为免疫抑制剂的用途。

    Method of effecting immunosuppression by administering carbocyclic
adenosine analogs
    13.
    发明授权
    Method of effecting immunosuppression by administering carbocyclic adenosine analogs 失效
    通过施用碳环腺苷类似物来实现免疫抑制的方法

    公开(公告)号:US5631258A

    公开(公告)日:1997-05-20

    申请号:US427937

    申请日:1995-04-26

    摘要: This invention relates to methods of effecting immunosuppression and inhibiting tumor necrosis factor .alpha. in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of a compound of the formula ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3 is N, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof. Also presented are pharmaceutical compositions comprising compounds of the same formula.

    摘要翻译: 本发明涉及在有需要的患者中进行免疫抑制和抑制肿瘤坏死因子α的方法,其包括向所述患者施用有效的免疫抑制量的式“IMAGE”化合物,其中环戊烷基环上的羟基取代基在CIS Y 3是N,Y 7,Y 8和Y 9各自独立地是氮或CH基,Q是NH 2,卤素或氢,Z是氢,卤素或NH 2; 或其药学上可接受的盐。 还提供了包含相同式的化合物的药物组合物。