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1.发明授权
公开(公告)号：US5905085A
公开(公告)日：1999-05-18
申请号：US975552
申请日：1997-11-20
IPC分类号： C07D473/00 , C07D487/04 , C07D471/04 , A61K31/44 , A61K31/52 , C07D473/16
CPC分类号： C07D473/00 , C07D487/04
摘要： This invention relates to novel 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 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, 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）的新型跨环戊基嘌呤类似物，其中环戊烷基环上3位上的取代基相对于双环取代基为反式构型，Y 3和Y 8为CH，Y 5，Y 7和Y 9为 每个独立地是氮，R是氢，C 1 -C 7烷基酰基或芳基酰基，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，以及它们作为免疫抑制剂的用途。
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公开(公告)号：US5605903A
公开(公告)日：1997-02-25
申请号：US408365
申请日：1995-03-22
IPC分类号： A61K31/52 , C07D471/04 , A61K31/435
CPC分类号： A61K31/70 , A61K31/52 , C07D471/04 , Y10S514/825
摘要： This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is inthe CIS configuration relative to the bicyclic substituent,Y.sub.3, 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.
摘要翻译： 本发明涉及在有需要的患者中进行免疫抑制的方法，其包括施用有效量的式（1）的化合物，其中环戊烯基环上的羟基取代基相对于CIS构型相对于 双环取代基Y 3，Y 7，Y 8和Y 9各自独立地为氮或CH基，Q为NH 2，卤素或氢，Z为氢，卤素或NH 2; 或其药学上可接受的盐。
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公开(公告)号：US5624930A
公开(公告)日：1997-04-29
申请号：US408366
申请日：1995-03-22
IPC分类号： A61K31/52 , C07D471/04 , A61K31/435
CPC分类号： A61K31/70 , A61K31/52 , C07D471/04 , Y10S514/825
摘要： This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, 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.
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公开(公告)号：US5929079A
公开(公告)日：1999-07-27
申请号：US975088
申请日：1997-11-20
IPC分类号： C07D473/00 , C07D487/04 , C07D473/16 , A61K31/505 , C07D473/32 , C07D473/34
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, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, 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，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，Y 7，Y 8和Y 9分别为氮， R是氢，C 1 -C 7烷基酰基或芳基酰基，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，以及它们作为免疫抑制剂的用途。
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5.发明授权
公开(公告)号：US5916892A
公开(公告)日：1999-06-29
申请号：US975086
申请日：1997-11-20
IPC分类号： C07D473/00 , C07D487/04 , C07D473/16 , A61K31/505 , C07D473/32 , C07D473/34
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 hydrogen, 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，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，Y 7和Y 8为 CH基，R是氢，C 1 -C 7烷基酰基或芳基酰基，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，以及它们作为免疫抑制剂的用途。
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公开(公告)号：US5817672A
公开(公告)日：1998-10-06
申请号：US477344
申请日：1995-06-07
IPC分类号： C07D473/00 , C07D487/04 , C07D473/34 , A61K31/44 , C07D471/04 , C07D473/16
CPC分类号： C07D473/00 , C07D487/04
摘要： This invention relates to novel 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 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen, R is a hydrogen, 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）的新型环戊烷基嘌呤类似物（1），其中环戊烷基环上3位上的取代基相对于双环取代基为反式构型，Y 3和Y 8为CH， Y5，Y7和Y9各自独立地为氮，R为氢，C1-C7烷基酰基或芳基酰基，Q为NH2，卤素或氢，Z为氢，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。
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公开(公告)号：US5470857A
公开(公告)日：1995-11-28
申请号：US336706
申请日：1994-11-08
IPC分类号： A61K31/52 , C07D471/04 , A61K31/505 , C07D239/00 , C07D473/02
CPC分类号： A61K31/70 , A61K31/52 , C07D471/04 , Y10S514/825
摘要： This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, 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.
摘要翻译： 本发明涉及在有需要的患者中进行免疫抑制的方法，其包括施用有效量的式（1）的化合物，其中环戊烯基环上的羟基取代基相对于CIS构型相对于 双环取代基Y 3，Y 7，Y 8和Y 9各自独立地为氮或CH基，Q为NH 2，卤素或氢，Z为氢，卤素或NH 2; 或其药学上可接受的盐。
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公开(公告)号：US5244896A
公开(公告)日：1993-09-14
申请号：US824411
申请日：1992-01-23
IPC分类号： C07D471/04 , C07D473/00 , C07D487/04
CPC分类号： C07D473/00 , C07D471/04 , C07D487/04
摘要： This invention relates to novel carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, 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, and to their use as immunosuppressants.
摘要翻译： 本发明涉及式（1）的新型碳环腺苷化合物（1）其中环戊烷基环上的羟基取代基相对于双环取代基为CIS构型，Y 3，Y 7，Y 8和Y 9各自独立地为氮 或CH基团，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，以及它们作为免疫抑制剂的用途。
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公开(公告)号：US06436947B1
公开(公告)日：2002-08-20
申请号：US08975212
申请日：1997-11-20
IPC分类号： C07D47316
CPC分类号： C07D473/00 , C07D487/04
摘要： This invention relates to Trans cyclopentanyl purine analogs of the formula (1) wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y3, Y5 Y7, Y9 are each nitrogen and Y8 is a CH group, R is a hydrogen, a C1-C7 alkyl acyl or aryl acyl, Q is NH2, halogen or hydrogen, Z is hydrogen, halogen, or NH2; 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，其中环戊烷基环上3位上的取代基相对于双环取代基为反式构型，Y 3，Y 5 Y 7，Y 9各自为氮，Y 8为CH 基团，R是氢，C 1 -C 7烷基酰基或芳基酰基，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，以及它们作为免疫抑制剂的用途。
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公开(公告)号：US5817661A
公开(公告)日：1998-10-06
申请号：US485745
申请日：1995-06-07
IPC分类号： A61P37/06 , C07D473/00 , C07D487/04 , C07D473/34 , A61K31/52 , C07D471/04 , C07D473/16
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 Y.sub.7, Y.sub.9 are each nitrogen and Y.sub.8 is a CH group, R is a hydrogen, 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）的环戊烷嘌呤嘌呤类似物：其中环戊烷基环上3位上的取代基相对于双环取代基为反式构型，Y 3，Y 5 Y 7，Y 9为 每个氮和Y 8是CH基团，R是氢，C 1 -C 7烷基酰基或芳基酰基，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，以及它们作为免疫抑制剂的用途。
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