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1. 发明授权

US5446048A Rapamycin oximes 失效
标题翻译：雷帕霉素肟
公开(公告)号：US5446048A
公开(公告)日：1995-08-29
申请号：US309816
申请日：1994-09-21
申请人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
发明人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
IPC分类号： C07D498/18 , A61K31/44
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, or Ar;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.6, aryloxy, or Ar;Ar is aryl which may be optionally mono-, di-, or tri-substituted;a=0-4;b=0-1;c=0-4;d=0-6;e=0-6; andf=0-6;or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R.sup.3 or R.sup.5 is --CO.sub.2 R.sup.8, R.sup.8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：其中R1是氢，烷基，烯基，炔基，三氟甲基，芳基烷基或Ar的结构化合物 R3是氢，烷基，烯基，炔基，三氟甲基，芳烷基或-CO2R8; R4是烷基，烯基，炔基，三氟甲基，芳基烷基，Ar，氨基烷基，硫代烷基，烷硫基烷基，羟基烷基或-CO 2 R 8; R5是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，Ar或-CO 2 R 8; R6是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R7是烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R8是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，芴基甲基或Ar; Y为O或S; X = N-O-（CH 2）f-Z或= N-O-Ar; Z是氢，烯基，炔基，烷氧基，氰基，氟，三氟甲基，-NR5R6，芳氧基或Ar; Ar是可任选被单，二或三取代的芳基; a = 0-4; b = 0-1; c = 0-4; d = 0-6; e = 0-6; 和f = 0-6; 或其药学上可接受的盐，条件是当f为0时，Z为氢，并且还提供当R3或R5为-CO2R8时，R8不为氢，可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤代理商

2. 发明授权

US5373014A Rapamycin oximes 失效
标题翻译：雷帕霉素肟
公开(公告)号：US5373014A
公开(公告)日：1994-12-13
申请号：US134237
申请日：1993-10-08
申请人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
发明人： Amedeo A. Failli , Robert J. Steffan , Craig E. Caufield , David C. Hu , Alexander A. Grinfeld
IPC分类号： C07D498/18 , A61K31/395 , C07D491/16
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, At, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, orAr;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.6, aryloxy, or Ar;Ar is aryl which may be optionally mono-, di-, or tri- substituted;a=0-4;b=0-1;c=0-4;d=0-6;e=0-6; andf=0-6;or a pharmaceutically acceptable salt thereof, with the proviso that when f is 0, Z is hydrogen and further provided that when R.sup.3 or R.sup.5 is --CO.sub.2 R.sup.8, R.sup.8 is not hydrogen which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
摘要翻译：其中R1是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar的结构化合物 R3是氢，烷基，烯基，炔基，三氟甲基，芳烷基或-CO2R8; R4是烷基，烯基，炔基，三氟甲基，芳基烷基，Ar，氨基烷基，硫代烷基，烷硫基烷基，羟基烷基或-CO 2 R 8; R5是氢，烷基，烯基，炔基，三氟甲基，芳烷基，At或-CO2R8; R6是氢，烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R7是烷基，烯基，炔基，三氟甲基，芳烷基或Ar; R8是氢，烷基，烯基，炔基，三氟甲基，芳基烷基，芴基甲基或Ar; Y为O或S; X = N-O-（CH 2）f-Z或= N-O-Ar; Z是氢，烯基，炔基，烷氧基，氰基，氟，三氟甲基，-NR5R6，芳氧基或Ar; Ar是可任选被单，二或三取代的芳基; a = 0-4; b = 0-1; c = 0-4; d = 0-6; e = 0-6; 和f = 0-6; 或其药学上可接受的盐，条件是当f为0时，Z为氢，并且还提供当R3或R5为-CO2R8时，R8不为氢，可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤代理商

3. 发明授权

US5525610A 42-Epi-rapamycin and pharmaceutical compositions thereof 失效
标题翻译： 42-Epi-雷帕霉素及其药物组合物
公开(公告)号：US5525610A
公开(公告)日：1996-06-11
申请号：US429374
申请日：1995-04-26
申请人： Craig E. Caufield , Alexander A. Grinfeld
发明人： Craig E. Caufield , Alexander A. Grinfeld
IPC分类号： C07D498/18 , A61K31/55 , C07D491/04 , C07D491/14 , C07D498/04 , C07D498/14
CPC分类号： C07D498/18
摘要： This invention comprises the compound of 42-Epimer Rapamycin of the following structural formula: ##STR1## as well as pharmaceutical compositions containing 42-Epi-Rapamycin and its use in methods for inducing immunosuppression and methods for treating transplantation rejection, graft vs. host disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphomas and hyperproliferative vascular disorders.
摘要翻译：本发明包括以下结构式的42-差向异构体雷帕霉素的化合物：以及含有42-Epi-Rapamycin的药物组合物及其在诱导免疫抑制的方法中的用途以及用于治疗移植排斥反应，移植物抗宿主病的方法，自身免疫疾病，炎症疾病，实体瘤，真菌感染，成人T细胞白血病/淋巴瘤和过度增殖性血管疾病。

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