| abstract |
Disclosed are 17-desmethylrapamycin analogues as represented by the general formula (I), wherein: x represents -CH2-; R1 represents =O or (H,H); R2 represents OH or OMe; R3 represents H, OH or OMe; R5 and R6 are each independently H or OH; R4 represents a 6- or 7-membered cycloalkyl moiety, or a 5- to 7-membered heterocycle as defined herein. Further disclosed is a process for their preparation, and the use of a compound as defined above in the preparation of a pharmaceutical medicament for the induction or maintenance of immunosuppression, the stimulation of neuronal regeneration or the treatment of cancer, B-cell malignancies, fungal infections, transplantation rejection, graft vs host disease, autoimmune disorders, diseases of inflammation and vascular disease is also disclosed. |