发明名称 Carbamates of rapamycin
摘要 A compound of the structure <IMAGE> wherein R1 and R2 are each, independently, hydrogen or -CONH(CR3R4)n-X; R3 and R4 are each, independently, hydrogen, alkyl, aralkyl, cycloalkyl, halogen, or trifluoromethyl; X ix hydrogen, lower alkyl, cycloalkyl, trifluoromethyl, nitro, alkoxy, carboalkoxy, aralkyl, halo, dialkylamino, thioalkyl, or Y; Y is a phenyl group which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, dialkylamino, or alkylthio; n=0-5; with the proviso that R1 and R2 are not both hydrogen and when n=0, X is lower alkyl, cycloalkyl, aralkyl, or Y; or a pharmaceutically acceptable salt thereof when X is dialkylamino, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.
申请公布号 US5118678(A) 申请公布日期 1992.06.02
申请号 US19910686728 申请日期 1991.04.17
申请人 AMERICAN HOME PRODUCTS CORPORATION 发明人 KAO, WENLING;VOGEL, ROBERT L.;MUSSER, JOHN H.
分类号 C07D498/18 主分类号 C07D498/18
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