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    • 9. 发明授权
    • Carbamates of rapaycin
    • 高分子化合物的氨基甲酸酯
    • US5559227A
    • 1996-09-24
    • US449593
    • 1995-05-24
    • Amedeo A. FailliOleg I. BleymanWenling KaoMagid A. Abou-Gharbia
    • Amedeo A. FailliOleg I. BleymanWenling KaoMagid A. Abou-Gharbia
    • A61K31/395A61K31/44A61K31/675C07D491/06C07D498/04C07D498/16
    • A61K31/70
    • A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12 and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.21 are each, independently, hydrogen, alkyl, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted; ##STR4## is a 5-7 membered saturated or partially unsaturated heterocyclic radical containing at least 2 ring nitrogens, wherein the heterocyclic ting may optionally contain NR.sup.22 in the heterocyclic ring, and the ring carbons may optionally be substituted by alkyl, arylalkyl, halogen, --CF.sub.3, --OR.sup.14, or --CO.sub.2 R.sup.10 ;R.sup.22 is hydrogen, alkyl, or arylalkyl;m=0-6;n=1-6;p=0-6; andr=1-6with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
    • 结构式II的化合物,其中R 1和R 2各自独立地为氢,-CONR 3(CR 4 R 5)m(CR 6 R 7)n(CR 8 R 9)pNR 10 R 11或者或者-CONR 3 R 13; R3是氢,烷基或芳基烷基; R 4,R 5,R 8和R 9各自独立地为氢,烷基,-OH,-CF 3或-F; R6是氢或-OR13; R7是氢或烷基; R 10是氢,烷基或芳基烷基; R 11,R 12和R 13各自独立地为 - (CR 15 R 16)r R 17; R 14为氢,1-6个碳原子的烷基,三(烷基)甲硅烷基,三(烷基)甲硅烷基乙基,三苯基甲基,苄基,烷氧基甲基,三(烷基)甲基乙氧基甲基或四氢吡喃基; R 15和R 16各自独立地为氢或烷基; R17是或-C 3BOND C-R21; R 18,R 19,R 20和R 21各自独立地为氢,烷基,卤素或苯基,其中苯基可以是任选的单,二或三取代; 含有至少2个环氮原子的5-7元饱和或部分不饱和杂环基,其中该杂环可以任意地含有杂环中的NR 22,并且该环碳可任选地被烷基,芳烷基,卤素, -CF 3,-OR 14或-CO 2 R 10; R 22是氢,烷基或芳基烷基; m = 0-6; n = 1-6; p = 0-6; 并且r = 1-6,条件是R 1和R 2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。