New antibiotics having immunosuppressive activity,...

C - Chemistry – Metallurgy – 12 – P

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C12P 17/10 (2006.01) A61K 31/40 (2006.01) C07D 207/36 (2006.01) C07D 207/38 (2006.01) C07D 209/96 (2006.01)

Patent

CA 2138542

As new antibiotics are now obtained delaminomycins A, B and C which are represented by the general formula (I) or (I') shown below, or salts thereof, as well as delaminomycins A2, B2 and C2 which are represented by the general formula (II) or salts thereof. Further, there are obtained sulfuric acid esters of delaminomycins A2 to C2 which are represented by the general formula (III), or salts thereof. Delaminomycins according to this invention have an activity to inhibit preferentially T cells and there- fore are useful as an immunodepressant necessary for transplantation of organs and also as a medicinal agent utilizable in therapeutic treatment of immuno-defficiency diseases. Further, the delaminomycins have an activity to inhibit proliferation of cetain kinds of cancer cells and are useful as an antineoplastic agent. Moreover, the delaminomycins according to this invention are useful as an antibacterial agent in therapeutic treatment of infections by Gram-positive bacteria. General formula (I):- - 2 - Image (I) General formula (I'):- Image (I') wherein X denotes a hydroxyl group, methoxy group or hydrogen atom, but X is a hydroxyl group for delaminomycin - 3 - A, a methoxy group for delaminomycin B and a hydrogen atom for delaminomycin C. General formula (II):- (II) Image wherein Y denotes a hydroxyl group, methoxy group orhydrogen atom, but Y is a hydroxyl group for delaminomycin A2, a methoxy group for delaminomycin B2 and a hydrogen atom for delaminomycin C2. General formula (III):- (III) Image - 4 - wherein R stands for a sulfuric acid residue -S03H or a pharmaceutically acceptable salt of the sulfuric acid residue, and Y is a hydroxyl group for delaminomycin A2, a methoxy group for delaminomycin B2 and a hydrogen atom for delaminomycin C2.

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