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1. 发明授权

US5637590A Rapamycin amidino carbamates 失效
标题翻译：雷帕霉素脒基氨基甲酸酯
公开(公告)号：US5637590A
公开(公告)日：1997-06-10
申请号：US450772
申请日：1995-05-24
申请人： Jerauld S. Skotnicki , Yvette L. Palmer
发明人： Jerauld S. Skotnicki , Yvette L. Palmer
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/395 , C07D498/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted;with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构的化合物，其中R和R 1各自独立地为氢，或者R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN，-NO 2 ，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

2. 发明授权

US5559119A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5559119A
公开(公告)日：1996-09-24
申请号：US391399
申请日：1995-02-27
申请人： Jerauld S. Skotnicki , Yvette L. Palmer , Wenling Kao , Magid A. Abou-Gharbia
发明人： Jerauld S. Skotnicki , Yvette L. Palmer , Wenling Kao , Magid A. Abou-Gharbia
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN ，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; 每个独立地是5-7元饱和的，不饱和的或部分不饱和的杂环基团，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地含有O， S或NR8，并且可以任选被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

3. 发明授权

US5541192A Rapamycin amidino carbamates 失效
公开(公告)号：US5541192A
公开(公告)日：1996-07-30
申请号：US448902
申请日：1995-05-24
申请人： Jerauld S. Skotnicki , Yvette L. Palmer
发明人： Jerauld S. Skotnicki , Yvette L. Palmer
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/44 , A61K31/505 , A61K31/53
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5,--COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3R.sup.5, --OR.sup.5, --SR.sup.5, or Ar; R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6,--NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

4. 发明授权

US5532355A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5532355A
公开(公告)日：1996-07-02
申请号：US395012
申请日：1995-02-27
申请人： Jerauld S. Skotnicki , Yvette L. Palmer , Wenling Koa , Magid A. Abou-Gharbia
发明人： Jerauld S. Skotnicki , Yvette L. Palmer , Wenling Koa , Magid A. Abou-Gharbia
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6 or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN ，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R4是氢，烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; 各自独立地是5-7元饱和的，不饱和的或部分不饱和的杂环基，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地含有O，S或 NR8在杂环中，并且可以任选地被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

5. 发明授权

US06638972B2 Chroman and benzofuran derivatives as 5-hydroxytryptamine-6 ligands 失效
公开(公告)号：US06638972B2
公开(公告)日：2003-10-28
申请号：US10263913
申请日：2002-10-03
申请人： Michael Gerard Kelly , Lynne Padilla Greenblatt , Gan Zhang , Yvette L. Palmer , Steven Edward Lenicek
发明人： Michael Gerard Kelly , Lynne Padilla Greenblatt , Gan Zhang , Yvette L. Palmer , Steven Edward Lenicek
IPC分类号： A61K31352
CPC分类号： C07D311/58 , C07D307/81
摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

6. 发明授权

US06518272B2 Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents 失效
标题翻译：环烷基取代的芳基哌嗪，哌啶和四氢吡啶作为血清素能药
公开(公告)号：US06518272B2
公开(公告)日：2003-02-11
申请号：US10107866
申请日：2002-03-27
申请人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
发明人： Wayne E. Childers , Michael G. Kelly , Yvette L. Palmer , Edward J. Podlesny
IPC分类号： A61K3150
CPC分类号： C07D239/42 , C07D209/08 , C07D211/22 , C07D213/74 , C07D217/22 , C07D277/82 , C07D295/125 , C07D295/13 , C07D319/20
摘要： This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally be substituted at the 1-position with a C1-C3 alkyl group; or an optical isomer; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有作为5-HT 1A激动剂和拮抗剂的活性的化合物，其可用于治疗具有下列基团的焦虑，抑郁，认知缺陷和前列腺癌：X是选自以下的部分：n是从整数1到5中选择; R 1是任选取代的芳基或单或双环杂芳基，条件是杂芳基不是噻二唑; R2是H或烷基; R3是H，COR5，COOR5和CONR5R6; R 4是H，烷基，烯基，炔基，芳基，单或双环杂芳基，芳烷基和单或双环杂芳烷基，其中芳基或杂芳基任选被取代; R5和R6是H，烷基，烯基，炔基，环烷基，环烯基，金刚烷基和去月桂烷基或R5和R6一起可以形成5-7元的氮杂环，任选地含有选自O，S或NR4的另外的杂原子; 当R5或R6选自环烷基或环烯基时，环状基团可以任选在1-位被C1-C3烷基取代;或光学异构体; 或其药学上可接受的盐。

7. 发明授权

US06326381B1 Arylpiperidine and aryl-1,2,5,6-tetrahydropyidine amide derivates 失效
标题翻译：芳基哌啶和芳基-1,2,5,6-四氢吡啶酰胺衍生物
公开(公告)号：US06326381B1
公开(公告)日：2001-12-04
申请号：US09459801
申请日：1999-12-13
申请人： Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Wayne E. Childers
发明人： Michael G. Kelly , Gan Zhang , Yvette L. Palmer , Wayne E. Childers
IPC分类号： C07D40106
CPC分类号： C07D401/06 , C07D211/22
摘要： Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.
摘要翻译：化学式R 1，R 2，R 3，R 4，X和n的化合物在本说明书中定义，可用于治疗焦虑，抑郁和相关的中枢神经系统疾病以及其他相关病症，例如治疗酒精和药物戒断，性功能障碍和阿尔茨海默病。

8. 发明授权

US5463048A Rapamycin amidino carbamates 失效
标题翻译：雷帕霉素脒基氨基甲酸酯
公开(公告)号：US5463048A
公开(公告)日：1995-10-31
申请号：US259763
申请日：1994-06-14
申请人： Jerauld S. Skotnicki , Yvette L. Palmer
发明人： Jerauld S. Skotnicki , Yvette L. Palmer
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/395 , C07D498/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构的化合物，其中R和R 1各自独立地为氢，或者R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5，-COR 5，-CN，-NO 2 ，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R 4是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-NO 2，卤素，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐，其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

9. 发明授权

US5519031A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5519031A
公开(公告)日：1996-05-21
申请号：US391398
申请日：1995-02-27
申请人： Jerauld S. Skotnicki , Yvette L. Palmer , Wenling Kao , Magid A. Abou-Gharbia
发明人： Jerauld S. Skotnicki , Yvette L. Palmer , Wenling Kao , Magid A. Abou-Gharbia
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 member saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.7 is alkyl of 1-6 carbon atoms, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3,--NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof. which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：结构式II的化合物，其中R和R 1各自独立地为氢，R 2和R 3各自独立地为氢，烷基，烯基，炔基，-CO 2 R 5， COR 5，-CN，-NO 2，-SO 2 R 5，-SO 3 R 5，-OR 5，-SR 5或Ar; R 4是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-NO 2，卤素，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; R 5和R 6各自独立地为氢，烷基，烯基，炔基或Ar; ＆lt; IMAGE＆gt;和＆lt; IMAGE＆gt;各自独立地是5-7元饱和，不饱和或部分不饱和的杂环基团，其任选地与苯环或环烷烃或环烯烃稠合，其中杂环可以任选地在杂环中含有O，S或NR8，并且可以任选被R 7取代; R7是1-6个碳原子的烷基，烯基，炔基，-CF3，-NR5R6，-CO2R5，-COR5，CONR5R6，-NO2，卤素，-OR5，-SR5，-CN，-SO2R5，-SO3R5，-SO2NR5R6 ，或Ar; R 8是氢，烷基，烯基，炔基，-CF 3，-NR 5 R 6，-CO 2 R 5，-COR 5，CONR 5 R 6，-OR 5，-SR 5，-CN，-SO 2 R 5，-SO 3 R 5，-SO 2 NR 5 R 6或Ar; Ar是苯基，萘基或杂芳基，其中前述可以任选被取代; 条件是R和R 1都不是氢，或其药学上可接受的盐。其可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

10. 发明授权

US5508286A Rapamycin amidino carbamates 失效
公开(公告)号：US5508286A
公开(公告)日：1996-04-16
申请号：US450771
申请日：1995-05-24
申请人： Jerauld S. Skotnicki , Yvette L. Palmer
发明人： Jerauld S. Skotnicki , Yvette L. Palmer
IPC分类号： A61K31/435 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D498/18 , A61K31/395 , C07D498/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted; with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

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