| 摘要 |
1,258,967. Derivatives of antibiotic SL 1846. SANDOZ Ltd. 14 March, 1969 [16 April, 1968 (3)], No. 13527/69. Heading C2A. Novel derivatives of antibiotic SL 1846 having the formula in which (i) X and Y together represent a second bond between the carbon atoms to which they are attached, R is H and R 2 is OH; or (ii) X and Y together with the carbon atoms to which they are attached represent an epoxy group and R 1 and R 1 together represent =O; or (iii) X and Y together represent a second bond between the carbon atoms to which they are attached and R 1 and R 2 together represent =N-NH-CO-NH 2 , are prepared by (a) reducing antibiotic SL 1846 with a hydride, e.g. an alkali metal borohydride to give compound (i); or (b) reacting antibiotic SL 1846 with an organic peracid or hydrogen peroxide to give compound (ii); or (c) condensing antibiotic SL 1846 with semi-carbazide or a salt thereof to give (iii) preferably in the presence of an acid-binding agent, e.g. sodium acetate or potassium carbonate. The derivatives inhibit the production of antibodies and the formation of cellular immunity reactions and they may be formulated as pharmaceutical compositions, e.g. tablets, dragÚes, syrups, injectable solutions or suppositories containing conventional excipients. |
